Dr.Martin Neurotransmitter

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8- There are __ (a) __ general structural classes of local anesthetics: ___ (b) ___ and ___ (c) ___.

2 , amino esters, amino amides

TRUE OR FALSE all muscles are equally sensitive to blockade by competitive blockers.

TRUE

TRUE OR FALSE : SPS--> FIGHT OR FLIGHT PSS--> REST OR DIGEST

TRUE

TRUE OR FALSE : GABA A GABA B AND GLCINE RECEPTORS ARE IPSP

TRUE

SYMPATHETIC STIMULATION ONTO THE Beta adrenoceptors RelaXed ciliary muscle iris cornea FLATTENED & WEAK LENS SYMPATHETIC STIMULATION **TAUT SUSPENSORY LIGAMENTS

To focus on a distant object

Alpha 1 receptors: Tetrahydrozoline HCl --> Visine

Treatment for irritated and red eyes

Central nervous system consists of _____________________________.

brain and spinal cord

What are nerves

bundles of sensory neurons and motor neurons

17- Which of the following events is responsible for the repolarization phase of the action potential? A. Opening of voltage gated Na+ channels B. Activation of the Na+/K+ pump C. Inactivation of voltage gated channels D. Opening of voltage gated K+ channels

PARASYMPATHETIC STIMULATION ONTO THE MUSCULARIC ach RECEPTOR CONTRACTED CILLARY MUSCLE ROUNDED STRONG LENS ** STACKENED SUSPENSORY LIGAMENTS

To focus on a close object

true or false The Voltage-gated Potassium Channel has only 2 phases. Open and inactivated. and potassium is moving from inner celluar to extracelluar

false open and closed

true or false Once the membrane potential reaches threshold, all voltage-gated Na+ channels open and this is called negative feedback

false positive feedback

iN MUSCLE CONTRACTION, WHAT HAPPENS IF THERE IS NO atp? WHAT IS IN CALLED ?

nO atp => NO DETACHMENT = RIGOR MORTIS

What ions are involved in the generation of an EPSP?

na moving in** due to Activation of ligand gated channels

5) Tetanus toxin: Block ____________.Inhibit NT release in the CNS=spastic paralysis

synaptobrevin.

Botulinum toxin: Block _______ or ____________. Inhibit ACh release at the NMJ=flaccid paralysis

syntaxin OR SNAP 25

WHat would happen if ..You block voltage-gated K+ channels? (TEA+)

too much potassium leadingto a continued refractory period

true or false Mydriasis (when an Alpha adrenoceptors mediate contraction of the radially oriented pupillary dilator muscle fibers in the iris ) is triggered by phenylephrine in a sympathetic stimulation

true

true or false Postganglionic neurons innervating the sweat glands release ach in theparasympathetic nervous system.

true

true or false Local potentials spread by passive current flow (electrotonic) and are bidirection yet cannot tgo long distance

true

true or false Simultaneously, as the voltage gated Na+ channel close ..voltage-gated K+ channels open, and K+ ions leave the cell

true

true or false Action potentials are generated in the initial segment and they propagate along the axon in order to reach the axon terminal

true remember all or none!!

true or false CENTRALLY ACTING SPASMOLYTIC DRUGS are gabapentin (neurotin) and pregabalin( lyrica)

true gaba!!!!

WHat would happen if ..You block the inactivation of voltage-gated Na+ channels? (δ-conotoxin)

will remain depolarized

Alpha 1 receptors: Pseudoephedrine --> Sudafed

Treatment for Nasal congestion

Generate slowly acting signals (hormones) nervous or endocrine systems ?

what are the 3 types of cns depressants ?

Analgesics (pain relievers) Barbiturates (sedative-hypnotic) Benzodiazepines (sedative-hypnotic)

Benzocaine (Americaine) Used topically to relieve pain or irritation caused by sunburn, toothache, insect bites, cold sore, etc. No basic aliphatic amine - not ________ soluble Formulated as gels, creams, and ointments Hydrolyzed by plasma _______________ _________ duration of action DDI - PABA blocks sulfonamide antibacterial activity.

Benzocaine (Americaine) Used topically to relieve pain or irritation caused by sunburn, toothache, insect bites, cold sore, etc. No basic aliphatic amine - not water soluble Formulated as gels, creams, and ointments Hydrolyzed by plasma cholinesterase Short duration of action DDI - PABA blocks sulfonamide antibacterial activity.

Steps Neuromuscular Function of muscles?

(1) arrival of electrical action potential at terminal of neuron causes Ca influx (2) Ach vesicles fuse with neuron membrane (3) Ach released from storage vesicles (4) Ach binds to muscle nicotinic receptor (5) Na flows into muscle (6) Na mobilizes intracellular Ca which activates muscle fibers (7) muscle fires (contracts) (8) Ach is hydrolyzed by AchE

Name two ways to block the motor end plate?

(1) block Ach at the muscle receptor (a) nondepolarizing neuromuscular blocking drugs (d-tubocurarine is prototype example) (2) excess Ach causes blockade (a) succinylcholine is prototype example (drugs and organophosphate pesticides that inhibit AchE and causes a rise in Ach, another example)

Phase II Blocking (desensitizing)

(1) membrane finally becomes repolarized (2) receptor can not be repolarized (made to fire) because it has become desensitized by the prolonged actions of succinylcholine which is sitting on the receptor

Tizanidine MOA

(a) congener of clonidine an alpha 2 agonist (b) alpha 2 agonist inhibits the release of NE (c) reduces spasticity with fewer cardiovascular effects compared compared to clonidine

name the non-depolarizing neuromuscular blocking drugs: isoquinolines

(a) d-tubocurarine (b) atracurium (c) doxacurium (d) cisatracurium (e) mivacurium "-CUR-"

Dantrolene 1) Derivative? 2) MOA?

(a) derivative of phenytoin (b) dantrolene blocks the release of Ca from the SR stores in skeletal muscle and inhibits muscle contraction

name the non-depolarizing neuromuscular blocking drugs: steroids

(a) pancuronium (b) vecuronium (c) pipecuronium (d) rocuronium "-NIUM"

nervous or endocrine systems ?

...

Enteric Neurons SYSTEM Release what 3 neurotransmitters?

-5ht -ach -cALCITONIN gENE rELATED pEPTIDE RECEPTOR (CGRP)

steps of crossbridge

...

Which would be more stable under physiological conditions? Esters or Amide

-Amide linkage has greater chemical stability vs. ester linkage (due to resonance)

GIVE 3 EXAMPLES OF THE 6 Toxic effects of local anesthetics

-CNS stimulation - restlessness, tremor; may lead to clonic convulsions (important toxic effects). -Followed by death due to respiratory and cardiovascular depression. -Direct systemic injection may lead directly to death. -Direct effects on myocardium - decreased electrical excitability, decreased conduction rate, negative inotropic effect. Sudden cardiac death. -Hypersensitivity - rare, but could entail dermatitis, asthma attack or fatal anaphylactic reaction. Allergy more frequent with esters. -Allergy to one ester rules out use of another ester, because the allergenic component is the metabolite para-aminobenzoic acid, produced by all esters. In contrast, allergy to one amide does not rule out the use of another amide.

A 60-year-old female patient started on a new antihypertensive medication recently. Her blood pressure seems to be under control, but she complains of fatigue, drowsiness, and fainting when she gets up from the bed (orthostatic hypotension). Which of the following drugs is she most likely taking? -Metoprolol. -Propranolol. -Prazosin. -Atenolol.

-Prazosin.

true or false Baclofen-- gaba b receptor activation cyclobenzaprine- unknown mechanism diazepam- gaba a tizanidine** similar to clonidine = alpha2 agonist dantrolene- blocks ryanodine (ryr1 ca2+)

...

true or false Prolonged receptor binding to the ligand leads to desensitization (receptors become unresponsive to specific or all ligands

...

. EPI also decreases the concentration of drug in the plasma,.. THEREFORE..

... decreasing the likelihood of adverse reactions.

How does a nerve impulse (action potential) pass along a neuron

-nerve impulse, or action potential, occurs within individual neurons and involves Na/K pump that actively pumps Na+ out of the cell and K+ into the cell, using ATP 1. Resting 2. Action then back to Resting Potential

Addition of epinephrine (1:200,000) generally doubles the duration of action of a local anesthetic by causing vasoconstriction which ....

...

MALIGNANT HYPERTHERMIA IS A rare interaction of succinylcholine with volatile anesthetics results in malignant hyperthermian in genetically susceptible people. IT IS TREATED BY RAPIDLY COOLING THE PT AND ADMINISTERING DANTROLENE

...

Na induce muscle contraction

...

Neuron structure axon carries the nerve impulse away from the cell body. Only one um in diameter but can be up to 4 m in length

...

during depolarization the electical and chemical gradient change is what causes ions to rush through a sodium channel during depolarization.

...

Functional Classification of Neurons

1 Sensory neurons (afferent)- OUTSIDE 2 Interneurons 3 Motor neurons (efferent)- IN CSN

1. Selectivity: Each ______ binds to a specific set of receptors 2) Receptors can (in the presynaptibe found on the postsynaptic or presynaptic membranes. Autoreceptors c membrane) provide a ________________ of neurotransmitter release 3) Receptors can be divided into ________ or metabotropic (G protein-coupled) 4) Receptors exist as cluster in the _____synaptic membrane 5) Prolonged receptor binding to the ligand leads to _____________ (receptors become unresponsive to specific or all ligands)

1 ligand 2 feedback control 3 ionotropic 4 post-synaptic 5 desensitization

WHAT ARE THE 3 Factors responsible for generating the resting membrane potential

1) Unequal distribution of charged particles or ions across the membrane( due to k) (electrochemical/CHEMICAL gradient) 2) Selective permeability(CHANNELS- TO ALLOW MOVEMENT OF IONS FROM ONE SIDE TO THE NEXT) to different ions (K+ and Na+ leak channels) 3) Active transport (Na+/K+ ATPase-minimal effect)

Cistracurium MOA

Competitive antagonists at skeletal muscle ACh-N receptors (Nondepolarizing muscle relaxant)

List 3 of the 5 Actions of BNZs (benzodiazepines)

1. Reduction of anxiety 2. Sedative and hypnotic actions 3. Anterograde amnesia 4. Anticonvulsant 5. Muscle relaxant

REVIEW OF the 6 steps of Cholinergic Neurotransmission

1. Acetylcholine synthesis • Formed by reaction of Acetyl CoA and choline (catalyzed by choline acetyltransferase) and transported into cytoplasm via sodium cotransporter 2. Storage • Packaged into vesicles via active transport. Matured vesicles also contain proteoglycan and ATP 3. Release • Action potential propagation triggers opening of calcium voltage-gated channels, which causes calcium influx. Increased intracellular calcium causes vesicles to fuse to cell membrane and release its contents (blocked by botulinum toxin/ black widow spider stimulates release of all contents) 4. Binding to a receptor • Binds to a specific postsynaptic receptor, which triggers a specific biological effect 5. Degradation • Acetylcholine broken down into acetate and choline via acetylcholinesterase 6. Recycling of choline • Transported back into cell where it is transformed into acetylcholine and stored

WHAT ARE THE 4 Modification of pain sensation

1. Acupuncture 2. Hypnosis 3. Stress 4. Drugs

List 2 of the 4 therapeutic affects of BNZs (benzodiazepines)

1. Anxiety disorders 2. Seizures 3. Sleep disorders 4. Muscular disorders

Inhibitory postsynaptic potential (or IPSP) _______ 1. Are produced by an increase in the membrane permeability to K+ or Cl- 2. Are generated by activation of nicotinic acetylcholine receptors at the motor end plate 3. Can result in a depolarization of the membrane potential 4. Are triggered by the inactivation of voltage-gated Na+ channels

1. Are produced by an increase in the membrane permeability to K+ or Cl-

DISRIBUTION OF BETA RECEPTORS 1 HEART 2 Airway Smooth Muscle 3 ADIPOSE/ LIPOLYSIS 4 Vascular Smooth Muscle

1. B1 2.B2 3. B1,B3 4. B2

TO TERMINATE MUSCLE CONTRACTION.. WHAT NEEDS TO HAPPEN

1. BREAKDOWN OF ACH BY ACETYLCHOLINESTERASE AND THE... 2. SEQUESTRATION OF CA INTO THE SR BY CA+ATPASE

A patient underwent a surgical procedure of 2 h. Anesthesia was provided by isoflurane, supplemented by intravenous midazolam and a nondepolarizing muscle relaxant. At the end of the procedure, a low dose of atropine was administered followed by pyridostigmine. The main reason for administering atropine was to 1. Block cardiac muscarinic receptors 2. Enhance the action of pyridostigmine 3. Prevent spasm of gastrointestinal smooth muscle 4. Provide postoperative analgesia 5. Reverse the effects of the muscle relaxant

1. Block cardiac muscarinic receptors

Structure of a Neuron

1. CELL BODY (soma) : contains the nucleus, cytoplasm, ribosomes, Golgi apparatus, mitochondria, Nissl bodies (or endoplasmic reticulum)protein synthesis 2.DENDRITES: thin cellular processes that receive input signals in a neuron ( that originate from cell body MAIN INPUT FOR NEURONS) 3.AXON: long cellular process designed for carrying electrical signals (action potentials/ ELECTRONIC SIGNALS) to other cells. Bundles of axons form nerves -COMMUNICATION!!!

WHAT ARE THE 3 CLASSES OF NEUROTRANSMITTERS??

1. CHOLINERGIC 2. MONAMINES 3.AMINO ACIDS

Increased excitability of a motoneurons→contraction of skeletal muscle→ rigidity (spasticity) WHAT 4 DRUGS TREAT THIS CONDITION

1. DIAZEPAM/ 2. baCLOFEN -- GABA RECEPTORS 3. TIZANIDINE -- ALPHA 2 AGONIST 4. DANTROLENE--BLOCKER OF EXCITATION

Main components of nervous tissue

1. Glial cells 2. Nerve cells or neurons

Consequences: Local anesthetics are more effective in rapidly firing nerves Local anesthetics increase the ____1._______ period Membrane depolarizations induced by increased extracellular K+ enhance the effect of local anesthetics-2. WHY? Increased extracellular Ca2+ reduces the effect of local anesthetics-3. WHY?

1. REFRACTORY 2.ION GRADIENT.. AND MAKES ACTION POTENTIAL LAST LONGER 3. INCREASED CALCIUM WILL REDUCE THE AFFECT OF THE LOCAL ANN BECUSE THERE IS MORE COMPETITION..MORE CALCIUM ..MORE ACH.. MORE COPETTION TO OVERSOME EFFECT OF THE COMPETITIVE DRUG

What are two types of Cholinergic receptors?

1. Muscarinic 2. Nicotinic

Classification of adrenergic receptors based on their agonist potencies BETWEEN THE NEURO TRANSMITTERS 1. ALPHA 2. BETA

1. NE>EPI,>ISO 2. iSO>EPI> NE

The 3 main components of a chemical synapse are:

1. Presynaptic membrane: 2. Synaptic cleft 3. Postsynaptic membrane

Skeletal Muscle Relaxants HAVE WHAT 3 FUNCTIONS

1. Provide muscle relaxation 2. Treat spasticity (spasmolytics) 3. Treat wrinkles

THE 4 Clinical pharmacology of neuromuscular blockers (NMBs) ARE

1. Surgery relaxation * - One of the most important applications 2. Endotracheal intubation 3. Control of ventilation 4. Treatment of Convulsions:

Regulation of Neurotransmitter Activity 1. Synthesis 2. Storage 3. ? 4. Receptor binding 5.? 6. Presynaptic receptors

1. Synthesis 2. Storage 3. Release 4. Receptor binding 5. Degradation/Reuptake 6. Presynaptic receptors

What are the 6 sequential steps in neurotransmission of cholinergic neurons?

1. Synthesis 2. Store 3. Release 4. Bind of ACh 5. degradation of neurotransmitter in synaptic cleft 6. recycle choline and acetate *Synaptic cleft is the space between the nerve endings and adjacent receptors located on nerves or effector organs*

Neurotranmitters Small molecule transmitter Monoamines (___________, serotonin, histamine) Catecholamines (dopamine, norepinephrine, _____________) Amino acids (glutamate, ________,, glycine)

1. ach 2.epi 3.GABA

Example(s) of ester-type local anesthetics:

1. procaine (Novocain) 2. tetracaine (pontocaine) 3. Cocaine 4. ALL OF THE ABOVE

Nervous System TARGETS: WHAT 3 THINGS :

1. skeletal muscles, 2. heart 3. glands

Endocrine System TARGETS: WHAT 4 THINGS

1. visceral organs 2. heart 3. smooth muscles 4. glands

A new drug was given by subcutaneous injection to 25 normal subjects in a phase 1 clinical trial. The cardiovascular effects are summarized in the table below. Which of the following drugs does the new experimentalagent most resemble? 1. Atropine 2. Epinephrine 3. Isoproterenol 4. Phenylephrine 5. Physostigmine

HOW MANY CRANIAL NERVES ARE THERE? & WHAT 4 ARE Parasympathetic fibers originate in brain stem and sacral portion of spinal cord ??

12 CRANIAL NERVES & III, VII, IX, X

15- Based on your knowledge of local anesthetic SAR, which of the following drug(s) will block the sodium channel by binding to the hydrophobic site: A. Drug B only B. Drug C and D only C. Drug A only D. All of the above.

15. A (Rational: Drug B, Benzocaine, is the only local anesthetic that lacks a hydrophilic portion/ does not need to be in cationic form to bind to the sodium channel)

2) Spasmolytics: centrally-acting drugs used to treat ____________.

2) Spasmolytics: centrally-acting drugs used to treat spasticity

Which one of the following is a common feature of both the sympathetic and parasympathetic branches of the ANS? 1. Postganglionic neurons release norepinephrine onto the effector organs 2. Acetylcholine release from preganglionic neurons activates nicotinic acetylcholine receptors located in postganglionic neurons 3. The cell bodies of preganglionic neurons originate in the brain stem 4. Postganglionic neurons stimulate the relaxation of renal vascular smooth muscles by releasing dopamine

2. Acetylcholine release from preganglionic neurons activates nicotinic acetylcholine receptors located in postganglionic neurons

Which of the following is correct regarding the neuromuscular blocking agnets (NMBAs)? 1. Nondepolarizing NMBAs are administered orally. 2. Cholinesterase inhibitors reduce the effects of nondepolarizing NMBAs. 3. Nondepolarizing NMBAs affect diaphragm muscles first. 4. Effects of depolarizing neuromuscular blockers can be reversed using cholinesterase inhibitors.

2. Cholinesterase inhibitors reduce the effects of nondepolarizing NMBAs.

Adrenaline added to local anaesthetic solution for infiltration anesthesia affords the following Except: 1. Prolongs the duration of local anaesthesia 2. Makes the injection less painful 3. Provides a more bloodless field for surgery 4. Reduces systemic toxicity of the local anaesthetic

2. Makes the injection less painful

A muscarinic receptor antagonist would probably not be needed for reversal of the skeletal muscle relaxant actions of a nondepolarizing drug if the agent used was 1. Cisatracurium 2. Pancuronium 3. Tubocurarine 4. Vecuronium

2. Pancuronium

In order to terminate Neurotransmitter Activity...what 2 processes must take place? 1. Breakdown 2. ?

2. Reuptake

Which one of the following accurately refers to a and b adrenoceptors? 1. These receptors use Glycine as a co-activator 2. These receptors are G-protein coupled 3. These receptors can be found in sympathetic preganglionic neurons 4. These are ionotropic receptors

2. These receptors are G-protein coupled

Compound X100 has the following effect on neurons: 1) X-100 prolongs the duration of the action potential ten-fold (from 2 msec to 20 msec); 2) X-100 does not change the resting membrane potential; 3) X-100 causes a ten-fold increase in the duration of the absolute refractory period. Based on your current knowledge of neuronal physiology, determine what is the most likely effect of this drug on the nervous system. 1. X-100 blocks the activity of the Na+/K+ pump 2. X-100 prevents the inactivation of voltage-gated Na+ channels 3. X-100 increases the number of leak K+ channels open at rest 4. X-100 blocks the opening of voltage-gated Na+ channels

2. X-100 prevents the inactivation of voltage-gated Na+ channels

Spasmolytic acts by interfering with muscle fiber excitation-coupling mechanism. 1. baclofen (Lioresal) 2. dantrolene (Dantrium) 3. tizanidine (Zanaflex)

2. dantrolene (Dantrium)

Effectiveness of local anesthetics when injected into infected tissue: 1. greater effect (greater anesthesia) 2. reduced effect (reduced anesthesia) 3. no difference

2. reduced effect (reduced anesthesia)

Release of NE from presynaptic neurons is blocked by which one of the following drugs? 1. Imipramine 2. Cocaine 3. Guanethidine 3. Reserpine

Order the following events in the order they take place at the neuromuscular junction 1-Depolarization of the nerve terminal induces calcium entry 2-Acetylcholine diffuses into synaptic cleft 3-Action potential arrives at the axon nerve terminal 4-Vesicles containing acetylcholine fuse with the presynaptic membrane 5-Acetylcholine binds to nicotinic ACh receptors in the postsynaptic membrane The correct order is:

3 1 4 2 5

TRUE OR FALSE All NMBA are injected intravenously. All are highly polar and inactive orally.

TRUE

Depression is often associated with what neurotransmitter disorder? 1. A deficiency of dopamine 2. An imbalance between glutamatergic and GABA neurotransmission 3. A deficiency of 5-HT 4. An excess of GABA

3. A deficiency of 5-HT

Why will you use dantrolene as a spasmolityc drug? 1. Because dantrolene blocks nicotinic acetylcholine receptors at the neuromuscular junction 2. Because dantrolene inhibits the generation of action potentials in skeletal muscle fibers 3. Because dantrolene prevents the release of calcium from the sarcoplasmic reticulum in skeletal muscles 4. Because dantrolene activates GABAA receptors on a motor neurons

3. Because dantrolene prevents the release of calcium from the sarcoplasmic reticulum in skeletal muscles

Results of local vasoconstriction on local anesthetics 1. increased local anesthetic neuronal uptake 2. reduced local anesthetic blood levels 3. Both 4. Neither

3. Both

Which of the following drugs has spasmolytic activity and could also be used in the management of seizures caused by overdose of a local anesthetic? 1. Baclofen 2. Cyclobenzaprine 3. Diazepam 4. Tizanidine

3. Diazepam

Local anesthetics block nerve conduction by: 1. Blocking all cation channels in the neuronal membrane 2. Depolarization the neuronal membrane 3. Interfering with depolarization of the neuronal membrane 4. Both 'B' and 'C' are correct

3. Interfering with depolarization of the neuronal membrane

blocked by botulinum toxins ex. toxin in black widow spider venom causes all the ACh stored in synaptic vesicle to empty all contents into the synaptic gap

3. Release of Acetylcholine

A 3-year-old child has been admitted to the emergency department having swallowed the contents of 2 bottles of a nasal decongestant. The active ingredient of the medication is a potent, selective α-adrenoceptor agonist drug. Which of the following is a sign of α-receptor activation that may occur in this patient? 1. Bronchodilation 2. Cardiac acceleration (tachycardia) 3. Pupillary dilation (mydriasis) 4. Renin release from the kidneys 5. Vasodilation of the blood vessels of the skin

3.. number 2 .. tachycardia is b receptor

All of the following are correct regarding adrenergic receptors, EXCEPT: 1. α1 Receptors are primarily located on the postsynaptic membrane in the effector organs. 2. α2 Receptors are primarily located on the presynaptic sympathetic nerve terminals. 3. β1 Receptors are found mainly in the heart. 4. β2 Receptors are found mainly in adipose tissue.

Clinical condition associated with spasticity 1. Hypertension 2. Stroke 3. multiple sclerosis 4. 1 & 3 5.1, 2, & 3

4. 1 & 3

From the following list, choose the events that are absolutely required for neurotransmitter release at the NMJ? 1. Arrival of an action potential to the nerve end terminal 2. Opening of voltage-gated Ca2+ channels in the nerve end terminal 3. Fusion of neurotransmitter-filled synaptic vesicles with the presynaptic membrane 4. All of the above

4. ALL OF THE ABOVE

Which one of the following is NOT true regarding local anesthetics? 1. Local anesthetics block voltage-gated Na + channels when they are in the inactivated state 2. Local anesthetics block voltage-gated Na+ channels in a time- and voltage-dependent manner 3. Local anesthetics block the action potential in axons that fire at very high rates 4. Local anesthetics bind to the outer pore of voltage-gated Na+ channels and block Na+ influx

4. Local anesthetics bind to the outer pore of voltage-gated Na+ channels and block Na+ influx

Which drug is most likely to cause hyperkalemia leading to cardiac arrest in patients with extensive burns? 1. Baclofen 2. Dantrolene 3. Rocuronium 4. Succinylcholine

4. Succinylcholine

The effect of parasympathetic stimulation on the eye is to __________ the ciliary muscle and to __________ the pupil. 1. contract, dilate 2. relax, constrict 3. relax, dilate 4. contract, constrict

4. contract, constrict

Characteristics of phase I depolarizing neuromuscular blockade due to succinylcholine include: 1. Easy reversibility with nicotinic receptor antagonists 2. Marked muscarinic blockade 3. Muscle fasciculations only in the later stages of block 4. Reversibility by acetylcholinesterase (AChE) inhibitors 5. Sustained tension during a period of tetanic stimulation

5. Sustained tension during a period of tetanic stimulation

The pKa of most local anesthetics is in the range of .... WHAT IS THE EXCEPTION... UNIONIZED FORM?

7.5-9.0 Exception: benzocaine, pKa ~ 3.5.) un-ionized form at pH 7.4

Spasticity can be treated with drugs that decrease activation of ______motoneurons, including: Diazepam, a GABA__ receptor agonist Baclofen, a GABA__ receptor agonist Tizanidine, an a__ agonist Centrally-acting __________ gabapentin

A B 2 SPASMOLYTICS

WHEN GOING FROM THE PERIPHERY TO THE BRAIN.. WHAT ARE THE 2 FIBERS THAT UES THE PAIN PATHWAY?

A DELTA fibers & C fibers

a specific type of epidural block in which a needle is inserted into the caudal canal via the sacral hiatus.

A caudal block

TRUE OR FALSE All Sub-Types α1, α2, β1, β2, β3 are G-protein linked with 7 transmembrane helices.

TRUE

Threshold is the minimum current required for the cell membrane to generate an action potential. This is the correct answer. A) True B) False

A) True

The absolute refractory period is the period of time during which This is the correct answer. A) a second action potential cannot be generated. B) a second action potential is generated. C) the action potential ceases. D) the action potential decreases in magnitude. E) the action potential changes direction.

A) a second action potential cannot be generated.

An action potential generates local currents that tend to ________ the membrane immediately adjacent to the action potential. This is the correct answer. A) depolarize B) repolarize C) hyperpolarize D) stabilize E) neutralize

A) depolarize

Specific local anesthetic agents A. Cocaine Restricted to use as topical anesthetic. WHY?? B. Lidocaine Intermediate duration (_________ min). Widely used. Amide of choice in patients allergic to esters. C. Benzocaine Low solubility. Not absorbed. SO HOW DO YOU USE IT? D. Procaine - NovocainR Short duration (_________ min) E. Other synthetic local anesthetics. These drugs vary mainly in: potency, rate of onset of action, duration of action, and toxicity. GIVE AN EXAMPLE AND HOW LONG THE DURATION

A. Controlled substance subject to abuse. B. Lidocaine 60 - 120 min C. Benzocaine Applied directly to wounds. D. Procaine - NovocainR (20 - 45 min) E. Other synthetic local anesthetics. Bupivicaine - long duration (400 - 450 min)

β2 postsynaptic effector cells: smooth muscle (in lungs), cardiac muscle Bronchodilation; vasodilation; relaxation of visceral smooth muscle; hepatic glycogenolysis and gluconeogenesis ( B2 AGONIST TO TREAT ASTHMA)

BETA 2

SELECTIVE, DIRECT ACTING , ADRENERGIC AGONISTS

A1 - PHENYLEPHRINE A2 CLONIDINE B1 DOBUTAMINE B2 TERBUTALINE

NONSELECTIVE, DIRECT ACTING , ADRENERGIC AGONISTS

A1, A2 OXYMETAZOLINE B1,B2 ISOPROTERENOL A1,A2 EPINE. A1,A2,B1 NOREPI

ADRENERGIC AGONISTS MIXED ACTING

A1,A2,B1,B2 EPHEDRINE

2ND GENERATION SELECTIVE BETA RECEPTOR ANTAGONIST

ACEBUTOLOL ATENOLOL BISOPROLOL ESMOLOL METOPROLOL

4 DRUGS USED FOR TREATMENT OF BPH (BENIGN PROSTATIC HYPERPLASIA )

ALFUZOSIN ( UROXATRAL) DOXAZOSIN( CARDURA ) TAMSULOSIN ( FLOMAX ) TERAZOSIN ( HYTRIN) DATT

postsynaptic effector cells, esp. smooth muscle Vasoconstriction; contraction of genitourinary muscles (sphinctures), relaxation of GI smooth muscle, hepatic glycogenolysis. HYPERTENSIVE DRUGS

ALPHA 1

presynaptic adrenergic nerve terminals (autoreceptor), platelets, lipocytes, smooth muscle - ANTIHYPERTENSIVE DRUGS Inhibition of transmitter NE release; counteraction of α1 .

ALPHA 2

ALPHA1 antagonists have been used as an alternative to surgery in patients with symptomatic benign prostatic hypertrophy. Blockade of the ALPHA receptors decreases tone in the smooth muscle of the bladder neck and ___________and improves urine flow. ________ and ____________ are more potent inhibitor of the ALPHA1A receptors found on the smooth muscle of the prostate. This selectivity accounts minimal effect on blood pressure.

ALPHA1 antagonists have been used as an alternative to surgery in patients with symptomatic benign prostatic hypertrophy. Blockade of the ALPHA receptors decreases tone in the smooth muscle of the bladder neck and prostate and improves urine flow. Tamsulosin and Silodosin are more potent inhibitor of the ALPHA1A receptors found on the smooth muscle of the prostate. This selectivity accounts minimal effect on blood pressure.

RELEASING AGENTS INDIRECT ACTING

AMPHETAMINE

Actions: Not all muscles are equally sensitive to blockade by competitive blockers. Small, rapidly contracting muscles of the ________& ___________ are most susceptible and are paralyzed first, followed by the fingers. Thereafter, the _______, _______, AND ____________ muscles are paralyzed, then the i____________ muscles are affected, and lastly, the diaphragm muscles are paralyzed. The muscles recover in the _________ manner.

Actions: Not all muscles are equally sensitive to blockade by competitive blockers. Small, rapidly contracting muscles of the face and eye are most susceptible and are paralyzed first, followed by the fingers. Thereafter, the limbs, neck, and trunk muscles are paralyzed, then the intercostal muscles are affected, and lastly, the diaphragm muscles are paralyzed. The muscles recover in the reverse manner.

What is the effect of administering isoproterenol?

Acts on b1, b2, b3 Heart: (b1) HR, CO, contractility, lusitropy increase Eye: no effect Bronchial smooth muscle: relaxation (b2) blood vessels to skin: no effect blood vessels to skeletal muscle: vasodilation (b2) GI bladder/tone: no clinical effect (b2) sphincter: no effect blood glucose: some increase

Cyclobenzaprine (Flexeril), carisoprodol (Soma), metaxalone (Skelaxin) Mechanisms of action unclear Main effect may be CNS depressant effect Efficacy difficult to evaluate due to lack of controlled studies Benzodiazepines or analgesics may be more effective. These are not effective in chronic neurological disease. what am i used for ??

Acute muscle spasm

Synthesis: from AA tyrosine Storage: small synaptic vesicles with dense core Elimination: reuptake, inactivation by monoamine oxidase (MAO) OR catechol-o-methyltransferase (COMT) Receptors: a and b adrenoceptors, all are G-protein coupled Receptor location: target of sympathetic postganglionic neurons, heart and blood vessels, brain Site of action: CNS (spinal cord, lymbic system), gastrointestinal tract (secretion and peristalsis) WHICH NeurotransmiTTER??

Adrenergic Neurotransmission

3RD GEN - SELECTIVE BETA RECEPTOR ANTAGONIST

BETAXOLOL CELIPROLOL NEBIVOLOL* SENSITIVE OF ALL B BLOCKERS

Succinylcholine MOA

Agonist at ACh-N receptors causing initial twitch then persistent depolarization Stimulates ANS Ganglia and M Receptors.

Atracurium is degraded spontaneously in the __________ and by ester hydrolysis. Atracurium is metabolized to laudanosine, which can provoke seizures.

Atracurium is degraded spontaneously in the plasma and by ester hydrolysis. Atracurium is metabolized to laudanosine, which can provoke seizures.

A. Progressive degeneration of motoneurons leading to muscle weakness B. Riluzole - inhibits glutamate neurotransmission C. Questionable effectiveness D. No serious adverse effects E. No other treatments available this is for

Amyotrophic lateral sclerosis

wrinkles associated with aging and decrease muscle tone WITH WHAT DRUG

BOTOX

Mivacurium MOA? ADR? Kinetics?

Competitive antagonists at skeletal muscle ACh-N receptors (Nondepolarizing) ADR: Histamine release Kinetics: Degraded in plasma by ChE, thus is shortest acting.

What are the uses of Carbachol?

Direct acting cholinergic agent- In the eye, as a miotic agent to treat glaucoma by causing pupillary contraction and a decrease in intraocular pressure. Onset of miosis 10-20 min. Reduction on intraocular pressure for 4-8 hrs.

d-Tubocurarine MOA? ADR?

Competitive antagonists at skeletal muscle ACh-N receptors (Nondepolarizing) [ANS ganglion block (tubocurarine)] ADR: Releases histamine. AchE inhibitors (neostigmine, edrophonium, pyridostigmine) increase Ach levels which competes off the blocker drug and recovery follows.

Atracurium MOA? ADR?

Competitive antagonists at skeletal muscle ACh-N receptors (Nondepolarizing). ADR: Laundanosine Formations (a metabolite that induces seizures)

Action Potential IS THE self-propagating wave of Na+ OUT and K+ IN

FALSE : ACTION POTENTIAL self-propagating wave of Na+ in and K+ out.

TRUE OR FALSE : Sensory neurons carry sensory information from receptors to PNS

FALSE : Sensory neurons carry sensory information from receptors to CNS

Therapeutic uses: Atropine (other)

Antispasmodic (active isomer, I-hyoscyamine) - because it blocks receptors of acetylcholine, therefore no contractions Antidote for cholinergic agonists (AChE, mushroom poisoning) Antisecretory (upper and lower respiratory tract prior to surgery)

this drug has Thiophene ring instead of a benzene ring.

Articaine

What connects axon to cell Body??

Axon Hillock

The pKa of most local anesthetics is between 7.5 and 9.0, Except: A.Lidocaine B.Benzocaine C. Cocaine D. Procaine

13- Which two local anesthetic drugs will undergo hydrolysis via plasma cholinesterase? A. Drug A and D B. Drug B and C C. Drug C and D D. Drug A and B Drug A = Dibucaine , Drug B = Articaine , Drug C = Tetracaine , Drug D = Ropivacaine.

B (Rational: Drug B because it contains the Methoxy ester, and Drug C because it is a amide Ester)

An action potential A) prevents the neuron cell membrane from altering its charge. This is the correct answer. B) causes the inside of the neuron cell membrane to become positive and the outside negative. C) causes the inside of the neuron cell membrane to become positive and the outside neutral. D) causes the outside of the neuron cell membrane to become positive and the inside negative. E) causes the outside of the neuron cell membrane to become positive and the inside neutral.

B) causes the inside of the neuron cell membrane to become positive and the outside negative.

ction potential propagation occurs in both directions along the axon. A) True This is the correct answer. B) False

B) false

WHICH STATEMENT IS FALSE ABOUT THE CHOLINERGIC NEUROTRANSMISSION: A.-Synthesis: reaction of choline and acetyl-CoA (choline acetyltransferase) * made to drive reaction! Storage: small CLEAR synaptic vesicles B.-Elimination: breakdown by enzyme POLYMERASE (PE) C.-Receptors -Bind 2 mole of : nicotinic ionotropic? (ligand-gated pentamer) and muscarinic (metabotropic) G protein-coupled) AChR D. -Receptor location: Neuromuscular junction, autonomic ganglia, target of postganglionic parasympathetic neurons and brain

B. CORRECT IS Elimination: breakdown by enzyme acetylcholinesterase (ASE)

1. GABA derivative. Appears to act in spinal cord. 2. GABAB agonist. 3. Side effects - sedation, insomnia, dizziness, weakness, ataxia (incoordination). Seizure threshold may be lowered. 4. Sudden withdrawal may cause hallucinations, anxiety and tachycardia. 5. Uses - Treatment of spasticity caused by multiple sclerosis or spinal trauma. WHAT DRUG AM I ?

BACLOFEN

postsynaptic effector cells: HEART, lipocytes, brain. Increased cardiac rate & force; relaxation of GI smooth muscle (diminished GI motility) ARYTHEMIA ..**SO BBLOCKERS.. BLOCK____

BETA 1

Which of the following agents causes persistent depolarization follows by desensitization of nicotinic receptor A. Rocuronium B. Succinylcholine C. Acetylcholine D. Dantrolene

B. Succinylcholine

Adverse effects, contraindications, and precautions of β receptor antagonists such as propranolol?

BRONCHOCONSTRICTION ARRHYTHMIAS PERIPHERAL VASOCONSTRICTION SEXUAL IMPAIRMENT dISURBANCE IN METABOLISM DRUG INTERACTION

Involve activation of baroreceptors in carotid sinus and aortic arch and is made up of ... Components: baroreceptors, sensory afferent neuron, cardiovascular control center (vasomotor center), autonomic efferent neurons Any changes in MAP triggers __________

Baroreceptor Reflex

Beta 1 & 2: Isoproterenol --> Isuprel; prototype for beta 1 & beta 2 receptors

Therapeutic uses of _______________ - -Bladder muscle dysfunction (overactive bladder) - refractory to or intolerant of anticholinergic medication -Blepharospasm (Benign essential blepharospasm is a disorder characterized by involuntary spasm of the eyelids ) -Cervical dystonia (botulinum toxin B) -Migraine (Chronic) -Severe hyperhidrosis of axilla - inadequately managed by topical agents -Strabismus (imbalance of the muscles of the eyeball.-- crosseyed) -Upper limb spasticity

Botulinum toxins (A)

Potent neurotoxin produced by Clostridium botulinum Mechanism of action : A - SNAP (synaptosome-associated proteins) B - VAMP (vesicle-associated membrane proteins) Prevents release of acetylcholine by interfering with vesicle fusion-->. paralysis what am I?

Botulinum toxins

Most potent local anesthetic

Bupivacaine

The following is NOT true about local anaesthetics: A. The local anaesthetic is required in the unionized form for penetrating the neuronal membrane B. The local anaesthetic approaches its receptor only from the intraneuronal face of the Na+ channel C. Cocaine was the first synthetic local anaesthetic D. The local anaesthetic combines with its receptor in the ionized cationic form

C. Cocaine was the first synthetic local anaesthetic

3RD GEN - NON SELECTIVE BETA RECEPTOR ANTAGONIST

CARVEDIOLOL*A1 ANTAG. CATEOLOL BUCINDOLOL LABETALOL *A1 ANTAG.

baCLOFEN, CARISOPRODOL, DIAZEPAM, METHOCARBAMOL, ORPHENADRINE, AND TIZANIDINE ARE ALL __________ ACTING RELAXANTS

CENTRALLY ACTING

WHAT ARE THE 3 POSSIBLE PHASES THE VOLTAGE GATED SODIUM CHANNEL COULD BE IN??

CLOSED... OPEN ... AND INACTIVATED

CNQX IS THE BLOCKER FOR WHICH OF THE 3 RECEPTORS?? AND MG2+, MK801 ARE BLOCKERS FOR WHICH RECEPTORS

CNQX IS THE BLOCKER FOR AMPA MG2+, MK801 ARE BLOCKERS FOR NMDA

It produces short-term euphoria, energy, and talkativeness in addition to potentially dangerous physical effects like raising heart rate and blood pressure. WHAT IS THIS?>

COCAINE

UPTAKE INHIBITOR INDIRECT ACTING

COCAINE

The amino amide-type local anesthetics are metabolized primarily in the liver by ________ and ________.

CYP1A2 and CYP3A4.

Chronic back pain and painful fibromyalgic conditions ARE ....

Centrally acting & Direct acting (Dantrolene)

Synthesis: reaction of choline and acetyl-CoA (choline acetyltransferase) * made to drive reaction! Storage: small clear synaptic vesicles Elimination: breakdown by enzyme acetylcholinesterase (ASE) Receptors -Bind 2 mole of : nicotinic ionotropic? (ligand-gated pentamer) and muscarinic (metabotropic) G protein-coupled) AChR Receptor location: Neuromuscular junction, autonomic ganglia, target of postganglionic parasympathetic neurons and brain WHICH NeurotransmiTTER??

Cholinergic Neurotransmission

What is edrophonium used?

Cholinomimetic agent - Limited use, in diagnosis of myasthenia gravis. Excess drug may cause a cholinergic crisis (use atropine as antidote)

Therapeutic uses of irreversible cholinomimetic agents: Echothiophate

Chronic treatment of open-angle glaucoma. Not a first-line agent in treatment of glaucoma. Limited use for many side effects and risk for causing cataracts.

may change the heart rate and rhythm by affecting the electrical conduction system of the heart and the nerves that influence it, such as by changing the rhythm produced by the sinoatrial node.

Chronotropic

Cisatracurium, which has the same pharmacokinetic properties as ______________, is less likely to have these effects.

Cisatracurium, which has the same pharmacokinetic properties as atracurium, is less likely to have these effects.

72- Atoms or functional groups that contain identical number of valence electrons and exhibits broadly similar physicochemical properties are called ____ (a) ____.

Classical Bioisosteres

A child requires multiple minor surgical procedures in the nasopharynx. Which drug has high surface local anesthetic activity and intrinsic vasoconstrictor actions that reduce bleeding in mucous membranes?

Cocaine

_________________ is an important exception because it has intrinsic sympathomimetic action due to its inhibition of norepinephrine reuptake into nerve terminals.

Cocaine

Surface activity (ability to reach superficial nerves when applied to the surface of mucous membranes) is a property of certain local anesthetics, especially ____________ and ____________(both only available as topical forms).

Cocaine and benzocaine

Rocuronium MOA

Competitive antagonists at skeletal muscle ACh-N receptors (Nondepolarizing muscle relaxant) - Steroid, metabolized in liver.

Vecuronium MOA

Competitive antagonists at skeletal muscle ACh-N receptors (Nondepolarizing muscle relaxant) - steroid metabolized in liver.

3- All of the following are correct regarding adrenergic receptors, except: A. Alpha1 receptors are primarily located on the postsynaptic membrane in the effector organs B. Alpha2 receptors are primarily located on the presynaptic sympathetic nerve terminals C. Beta1 receptors are found mainly in the heart. D. Beta2 receptors are found mainly in adipose tissue.

THE DIRECT ACTING RELAXANT IS

DANTROLENE

WHERE ARE THE 3 OriginS of Sympathetic Preganglionic Fibers in Spinal Cord

DORSAL HORNS LATERAL HORNS VENTRAL HORNS

3 DRUGS USED FOR TREATMENT OF HTZ

DOXAZOSIN( CARDURA ) PRAZOSIN (MINIPRES) TERAZOSIN ( HYTRIN)

1. Acts directly on skeletal muscle. 2. Decreases Ca release from SR. 3. Side effects and toxicity - Potential for hepatotoxicity with fatal hepatitis in 1:1000 patients treated for 60 days or more. Hepatic function altered in 1% of patients. Most common side effect is weakness. 4. Uses - Reduces spasticity in hemiplegic patients. Half of cerebral palsy patients are improved. Treatment of malignant hyperthermia What am I??

Dantrolene

Depolarizing Relaxant Drugs The extremely short duration of action of ______________(5-10 min) is due to its rapid hydrolysis by ___________________ and ______________ in the liver and plasma, respectively.

Depolarizing Relaxant Drugs The extremely short duration of action of succinylcholine (5-10 min) is due to its rapid hydrolysis by butyrylcholinesterase and pseudocholinesterase in the liver and plasma, respectively.

WHAT ARE THE 2 Neuromuscular blocking agents:

Depolarizing agents & Nondepolarizing agents

Diabetes: Non-selective β blockers: Decrease GLYCO_______ and decrease glucagon secretion. ____-Blockers also attenuate the normal physiologic response to hypoglycemia. They should be used with great caution, because pronounced hypoglycemia. a β1-selective antagonist is preferred, since these drugs are less likely to ________ recovery from hypoglycemia

Diabetes: Non-selective β blockers: Decrease glycogenolysis and decrease glucagon secretion. -Blockers also attenuate the normal physiologic response to hypoglycemia. They should be used with great caution, because pronounced hypoglycemia. a β1-selective antagonist is preferred, since these drugs are less likely to delay recovery from hypoglycemia

Side effects of Cholinergic agonists?

Diarrhea Diaphoresis Miosis (pupil constriction) Nausea Urinary urgency Intestinal cramps Salivation Indirect-Acting Cholinergic Agonists acetylcholinesterase inhibitors can be reversible or irreversible pharmacological properties Examples of reversible indirect-acting cholinergic agonists "stigmines": physostigmine, pyridostigmine, neostigmine. Also, edrophonium

Adverse effects observed with cholinergic drug

Diarrhea Diaphoresis (sweating) Miosis (contraction of pupils) Nausea Urinary urgency

May increase effectiveness of presynaptic inhibition in the spinal cord. Useful in spinal lesions and some cases of cerebral palsy. WHAT DRUG AM I?

Diazepam - benzodiazpines

What are the uses of Bethanechol?

Direct acting cholinergic agent - In urology, to stimulate atonic bladder in postpartum or postoperative, nonobstructive urinary retention. May also be used to treat neurogenic atony as well as megacolon.

What are the uses of Pilocarpine?

Direct acting cholinergic agent - Used to treat glaucoma and drug of choice in the emergency lowering of intraocular pressure of narrow-angle and wide-angle glaucoma. Onset of action: few min. Effect lasts 4-8 hrs and can be repeated. -Can enter the systemic circulation and CNS.

Cocaine (______________ reuptake inhibitor) discovered in 1860 by Niemann (Noted its anesthetic effect on tongue), structure was solved in 1924 Used _______________ for the first time as a local anesthetic in 1884 for eye surgery. • Gave birth to local anesthetic agents

Dopamine surgically

Synthesis: from the AA tyrosine Storage: small synaptic vesicles with dense core Elimination: reuptake OR inactivation by monoamine oxidase (MAO) and catechol-o-methyltransferase (COMT) Receptors: Dopaminergic receptors (D1-D5), all are G-protein coupled Receptor location: postganglionic sympathetic neurons innervating renal vascular smooth muscles, nigrostriatal system, mesocortical system WHICH NeurotransmiTTER??

Dopaminergic Neurotransmission

History OF Nondepolarizing (competitive) blockers During the 16th century, European explorers found that natives in the Amazon Basin of South America were using ________, an arrow poison that produced _______________ paralysis, to kill animals. The active compound, ___________, and its modern synthetic analogs have had a major influence on the practice of _________ and surgery. The neuromuscular blocking agents have significantly increased the safety of anesthesia, because_______anesthetic is required to produce muscle relaxation.

During the 16th century, European explorers found that natives in the Amazon Basin of South America were using curare, an arrow poison that produced skeletal muscle paralysis, to kill animals. The active compound, d-tubocurarine, and its modern synthetic analogs have had a major influence on the practice of anesthesia and surgery. The neuromuscular blocking agents have significantly increased the safety of anesthesia, because less anesthetic is required to produce muscle relaxation.

Sensory receptors and neurons in GI tract and enteric plexuses ---> cns--->Enteric motor neurons in enteric plexuses (involuntary) --->Smooth muscles, glands and endocrine cells in GI which nervous system ??

ENS

Generation of an action potential is determined by the strength of__________

EPSP

Interplay of ______ and _______ can limit the ability of a neuron to generate an action potential

EPSP and IPSP

Benzocainea Cocainea Procaine Tetracainea WHAT STRUCTURES?

ESTERS

What is Selectivity?

Each ligand binds to a specific set of receptors

Effects NOT due to blockade of ß-adrenergic receptors α1 antagonism - labetolol and carvedilol Contributes to their __________________ effect Partial ß-agonist activity (ISA - intrinsic sympathomimetic activity) - acebutolol, labetolol, penbutolol, pindolol May produce______bradycardia or bronchoconstriction, but clinical value of this additional activity is unclear Local anesthetic action (membrane stabilizing effect) - acebutolol, labetolol, metoprolol, pindolol, propranolol.

Effects NOT due to blockade of ß-adrenergic receptors α1 antagonism - labetolol and carvedilol Contributes to their antihypertensive effect Partial ß-agonist activity (ISA - intrinsic sympathomimetic activity) - acebutolol, labetolol, penbutolol, pindolol May produce less bradycardia or bronchoconstriction, but clinical value of this additional activity is unclear Local anesthetic action (membrane stabilizing effect) - acebutolol, labetolol, metoprolol, pindolol, propranolol.

Effects due to blockade of ß-adrenergic receptors Cardiovascular effects: ______________ BP in hypertension Negative ______________ effect (reducing heart rate). Negative___________ effect (decrease cardiac contractility)

Effects due to blockade of ß-adrenergic receptors Cardiovascular effects: Decrease BP in hypertension Negative chronotropic effect (reducing heart rate). Negative inotropic effect (decrease cardiac contractility)

IF A sensory transmission from a local area of the body to the CNS is blocked. ... WHAT IS THIS CALLED ?

Local anesthesia

Adrenergic Receptor Agonists Sympathomimetics Endogenous mediators of sympathetic stimulation __Norepinephrine/ EPI??__ - postganglionic sympathetic neurotransmitter __Norepinephrine/ EPI??__ - hormone released from adrenal medulla

Endogenous mediators of sympathetic stimulation Norepinephrine - postganglionic sympathetic neurotransmitter Epinephrine - hormone released from adrenal medulla

Assembly of neurons innervating the walls of the gastrointestinal system are organized into the myenteric and submucous plexuses

Enteric Nervous System

true or false :Resting Potential is the state of being ready to send an action potential. The axon membrane is polarized. - Positive outside axon and negative inside maintained by active transport by Na/K pump 3 Na IN and 2 K OUT. Membrane potential is -55 mv

FALSE : Resting Potential is the state of being ready to send an action potential. The axon membrane is polarized. - Positive outside axon and negative inside maintained by active transport by Na/K pump Na OUT and K IN. Membrane potential is -70 mv

TRUE OR FALSE Dantrolene Potential for hepatotoxicity with fatal hepatitis Most common side effect is weakness.

TRUE

TRUE OR FALSE Greater vasodilation -- longer duration of action; reduced systemic absorption

FALSE Greater vasodilation -- increased systemic absorption; reduced duration of action

TRUE OR FALSE THE PERIPHERAL NERVOUS SYSTEM IS WHERE One oligodendrocyte forms the myelin sheath for several axons

FALSE THE CNS

TRUE OR FALSE **Non- Catecholamines : Epinephrine Norepinephrine Isoproterenol Dopamine Properties of catecholamine compounds : 1. High potency 2. Rapid inactivation (COMT and by MAO) 3. Poor penetration into CNS **Catecholamines Phenylephrine, ephedrine, and amphetamine. Compounds lacking the catechol hydroxyl groups Longer half-lives, because they are not inactivated by COMT. Poor substrates for MAO and, thus, show a prolonged duration of action. Increased lipid solubility permits greater access to the CNS.

FALSE Catecholamines Epinephrine Norepinephrine Isoproterenol Dopamine Properties of catecholamine compounds : 1. High potency 2. Rapid inactivation (COMT and by MAO) 3. Poor penetration into CNS Non-catecholamines Phenylephrine, ephedrine, and amphetamine. Compounds lacking the catechol hydroxyl groups Longer half-lives, because they are not inactivated by COMT. Poor substrates for MAO and, thus, show a prolonged duration of action. Increased lipid solubility permits greater access to the CNS.

TRUE OR FALSE In infected tissue, extracellular pH is HIGHER; more drug in UNionized state; less likely to diffuse into the cell; INCREASING local anesthetic effect

FALSE In infected tissue, extracellular pH is lower; more drug in ionized state; less likely to diffuse into the cell; reduced local anesthetic effect

TRUE OR FALSE GLYCINE IS COACTIVATOR FOR ALL 3 RECEPTORS AND GLUTAMATE IS COACIVATOR FOR NMDA

FALSE ACTIVATOR FOR ALL 3 RECEPTORS : GLUTAMATE. AND COACTIVATOR FOR NMDA IS GLYCINE

TRUE OR FALSE Cocaine is a powerfully addictive stimulant drug made from the leaves of the coca plant native to South AFRICA

FALSE Cocaine is a powerfully addictive stimulant drug made from the leaves of the coca plant native to South America.

TRUE OR FALSE Local anesthetics are weak ACIDS at physiological pH they are charged or in their cationic form, which can cross the membrane

FALSE Local anesthetics are weak bases: at physiological pH they are charged or in their cationic form, which cannot cross the membrane

Succinylcholine affects heart via autonomic ganglia HIGH doses - negative inotropic and chronotropic responses due to stimulation of parasympathetic ganglia. Can be attenuated by administration of an anticholinergic drug (e.g. glycopyrrolate, atropine). LOWdoses - positive inotropic and chronotropic effects may be observed due to stimulation of sympathetic ganglia. TRUE OR FALSE

FALSE Low doses - negative inotropic and chronotropic responses due to stimulation of parasympathetic ganglia. Can be attenuated by administration of an anticholinergic drug (e.g. glycopyrrolate, atropine). High doses - positive inotropic and chronotropic effects may be observed due to stimulation of sympathetic ganglia.

TRUE OR FALSE Neuron structure dendrites provide a CONSTRICTED surface area for connecting with other neurons. They pick up a nerve impulse and carry it towards the DENDRITES

FALSE Neuron structure dendrites provide a LARGE surface area for connecting with other neurons. They pick up a nerve impulse and carry it towards the CELL BODY

TRUE OR FALSE One Schwann cell forms the myelin sheath for MULTIPLE AXON

FALSE One Schwann cell forms the myelin sheath for ONE AXON

TRUE OR FALSE : Peripheral Nervous System CONSIST OF Oligodendrocytes

FALSE Schwann cells!!!!!!!

TRUE OR FALSE The benzodiazepines have both an antipsychotic activity and analgesic action, because they affect the autonomic nervous system.

FALSE The benzodiazepines have neither antipsychotic activity nor analgesic action, and they do not affect the autonomic nervous system.

Diazepam MOA

Facilitates GABA-ergic transmission in CNS GABAA receptor activation—postsynaptic

Baclofen MOA

Facilitates spinal inhibition of motor neurons (Gaba-b) GABAB receptor activation: pre- and postsynaptic

Where are the muscarinic receptors located?

Found on ganglia of the peripheral nervous system on the autonomic effector organs (heart, smooth muscle, brain, and excrine glands) Blocked by Atropine

Modulators: Benzodiazepines Barbiturates FOR WHICH GABA??

GABA A

Synthesis: from the AA glutamate (glutamate decarboxylase or GAD) Storage: small clear synaptic vesicles Elimination: reuptake and breakdown by GABA transaminase (GABA-T) Receptors: GABAA (ligand-gated pentamer), GABAB (G-protein coupled) and GABAC (ligand-gated pentamer only found in retina) Receptor location: throughout the CNS (major inhibitory NT) FOR WHICH NEUROTRANSMITTER ??

GABA Neurotransmission

Accumulation of aqueous humor in anterior chamber leads to the development of ___________.

GLAUCOMa

______________ is the most common excitatory neurotransmitter in central synapses (CNS) Synapses may contain both ionotropic and metabotropic receptors Due to _____ blockade, NMDA receptors coexist with ______ Ionotropic receptors use glycine as co-activator

GLUTAMATE Mg2+, AMPA

Nicotinic Receptor Antagonists

Ganglionic blocking agents Neuromuscular blocking agents

Endocrine System (wireless & diffused)

Generate slowly acting signals (HORMONES)

TRUE OR FALSE Duration of blockade is strongly correlated with the elimination half-life.

TRUE

How do nondepolarizing neuromuscular blocking agents interact with aminoglycoside antibiotics?

Gentamicin and tobramycin inhibit ACh release from cholinergic nerves by competing with calcium ions. They synergize with pancuronium and other nondepolarizing blockers, enhancing the blockade.

1. Cholinomimetics (pilocarpine): stimulate ciliary muscle, opening the canal of Schlemm (for outflow of aqueous humor) 2. Cholinesterase inhibitors (physostigmine) 3. b receptor blockers: prevent formation of aqueous humor 4. Prostaglandin derivates: stimulate outflow of aqueous humor 5. Carbonic anhydrase inhibitors: inhibit formation of aqueous humor all treat what condition ??

Glaucoma

Synthesis: from Krebs cycle intermediate a-ketoglutarate Elimination: reuptake by astrocytes (glutamate-glutamine conversion) Receptors: Ionotropic (NMDA, kainate and AMPA), metabotropic (or G-protein-coupled) Receptor location: throughout the CNS (major excitatory NT) WHICH NeurotransmiTTER??

Glutamate Neurotransmission

Act as a co-ligand for NMDA receptors (excitation) or bind to inhibitory glycine receptors Elimination: reuptake by GLYT Receptors: ionotropic receptor, allows Cl- flow. Strychnine-sensitive Receptor location: throughout the CNS (major inhibitory NT in spinal cord) FOR WHICH NEUROTRANSMITTER ??

Glycine Neurotransmission

How do nondepolarizing neuromuscular blocking agents interact with halogenated hydrocarbon anesthetics?

Halothane enhances neuromuscular blockade by exerting a stabilizing action at the NMJ. Sensitizes the NMJ to the effects of neuromuscular blockers.

58- Numerous structurally related compounds can be represented by a relatively simple structure. It is called ___ (a) ___ structure.

MArkush Structure

Synthesis: from the AA histidine Elimination: reuptake OR inactivation by diamine oxidase (histaminase) Receptors: H1-H3 receptors, all are G-protein coupled Source: neurons in tuberomammillary nucleus of the hypothalamus, cells in gastric mucose and mast-cells WHICH NeurotransmiTTER??

Histaminergic Neurotransmission

Other adverse effects of succinylcholine Hyperkalemia

Hyperkalemia. Increased INTRAOCCULARPRESSURE* Increased intragastric pressure Muscle pain

GIVE 3 OF THE 7 CLINICAL USES OF B ANTAGONISTS

Hypertension Ischemic heart disease - angina Cardiac arrhythmias Heart failure Glaucoma Hyperthyroidism - block symptoms Neurologic diseases - migraine, certain tremors, anxiety, PTSD

IS THE INACTIVATION GATE FOUND IN THE INTRACELLULAR FLUID OR EXTRACELLULAR FLUID?

INNERCELLULAR

mAChR and aAR regulate the _________.

IRIS

M2 Cholinergic receptors are found..

In cardiac tissue; they decrease cAMP or increase K+ efflux

Where is neostigmine contraindicated?

In intestinal or urinary bladder obstruction. Should not be used in patients with peritonitis or inflammatory bowel disease. Because the contraction of smooth muscle caused by the medication would worsen the preexisting condition.

M1 Cholinergic receptors are found....

In neurons; they can increase IPG and increase DAG

Therapeutic use of Ipratropium and Tiotropium

Inhaled - As bronchodilators for maintenance treatment of bronchospasm associated with COPD, chronic bronchitis and emphysema Pending approval for asthma (patients unable to use adrenergic agonists) Positively charged - only local effects Tiotropium - once a day, ipratropium - up to 4 times daily

Cyclobenzaprine MOA Clinical used? ADR:?

Inhibition of spinal stretch reflex - used for acute injury/ inflammation. Hallucinations, Confusion.

TRUE OR FALSE Influx of calcium into the neurons triggers the release of norepinephrine

TRUE

e.g. labetalol, metoprolol, pindolol and propranolol are metabolized by the liver. WHAT CLASS OF BETA BLOCKERS

LIPID SOLUBLE BETA BLOCKER

Kidney: Blockade of ß1-receptors inhibit the release of renin from juxta-glomerular cells. Peripheral vasoconstriction: Nonselective blockade of β receptors prevents β2-mediated vasodilation in skeletal muscles, increasing peripheral vascular resistance

Feed back inhibition caused by concentration of ________: Excess of ________ causes dephosphorylation of tyrosine hydroxylase (dephosphorylated form: inactive)

L DOPA L DOPA

is useful in acute heart ischemic, ventricular arrhythmias, for example, after myocardial infarction WHAT DRUG AM I?

LIDOCAINE

What ion channels are invovled with what processes? Leak channels=> _______________potential Voltage-gated ion channels => _____________ potential Ligand-gated ion channels => _____________ potential

Leak channels=> resting membrane potential Voltage-gated ion channels => action potential Ligand-gated ion channels => graded / synaptic potential

Lidocaine (Xylocaine) - Prototype Most commonly used amino___________-type local anesthetic Topical - relieve burning, itching, and pain Injection - dental or minor surgery Very _________ soluble _________onset _____________ DOA than esters CNS toxicities Restlessness Slurred speech Seizures

Lidocaine (Xylocaine) - Prototype Most commonly used amino amide-type local anesthetic Topical - relieve burning, itching, and pain Injection - dental or minor surgery Very lipid soluble Rapid onset Longer DOA than esters CNS toxicities Restlessness Slurred speech Seizures

Articaine Benzocaine (topical) Bupivacaine Chloroprocaine Cocaine (topical) Dibucaine (topical) Etidocaine Levobupivacaine Lidocaine (Xylocaine) Lidocaine and bupivacaine mixture (Duocaine) Lidocaine and prilocaine eutectic mixture (topical) (EMLA cream) Mepivacaine Prilocaine Procaine Proparacaine (ophthalmic) Ropivacaine Tetracaine What kind of drugs ?

Local Anesthetics

Class of drugs that block nerve conduction when applied locally to nerves Used to treat pain

Local anesthesia

Local anesthesia is the condition that results when sensory transmission from a local area of the body to the CNS is _____________. The local anesthetics constitute a group of chemically _______ agents (esters and amides) that block the sodium channels of excitable membranes. Class of drugs that block NERVE ____________________ when applied locally to nerves Used to treat ________.

Local anesthesia is the condition that results when sensory transmission from a local area of the body to the CNS is blocked. The local anesthetics constitute a group of chemically similar agents (esters and amides) that block the sodium channels of excitable membranes. Class of drugs that block nerve conduction when applied locally to nerves Used to treat pain

Local anesthetics block voltage-gated ______ channels in a voltage- and time-dependent manner Affinity for local anesthetics _______ when voltage-gated Na+ channels are in the _______________or inactivated states

Local anesthetics block voltage-gated Na+ channels in a voltage- and time-dependent manner Affinity for local anesthetics increases when voltage-gated Na+ channels are in the activated or inactivated states

Local anesthetics have a _________ effect on small diameter fibers: they fire _______ and have ___________ duration action potentials

Local anesthetics have a greater effect on small diameter fibers: they fire faster and have longer duration action potentials

These are macrophage cells, they act as the first and main form of active immune defense in the central nervous system

MIcroglia

MYLINATION =_______________!- FASCILITATE, SPEED UP THE VELOCITY OF ___________________. MYLINATION IS NOT CONTINUOUS IT ONLY CONTAINS CERTAIN SEGMENTS OF ________

MYLINATION = ** INSULATED** !!- FASCILITATE, SPEED UP THE VELOCITY OF **ACTION POTENTIAL** MYLINATION IS NOT CONTINUOUS IT ONLY CONTAINS CERTAIN SEGMENTS OF **AXON**

This is a generic term for cells in the CNS which are neither neurons nor microglia (or tissue-based macrophages). These cells include astrocytes, oligodendrogliocytes and glioblasts, Schwann cells; they provide nutrition, physical support and synthesise myelin.

Macroglia

THESE ARE ALL GENERAL ANESTETICS THAT HAVE A DRUG INTERACTION WITH NMBAS Succinylcholine and halothane - WHAT IS THE DRUG INTERACTION

Malignant hyperthermia

Many shorter-acting local anesthetics: have _________________ properties and are readily absorbed into the blood from the injection site after administration. The duration of local action is therefore limited unless blood flow to the area is _________________. This can be accomplished by administration of a __________________ (usually an α-agonist sympathomimetic) with the local anesthetic agent.

Many shorter-acting local anesthetics: have vasodilation properties and are readily absorbed into the blood from the injection site after administration. The duration of local action is therefore limited unless blood flow to the area is reduced. This can be accomplished by administration of a vasoconstrictor (usually an α-agonist sympathomimetic) with the local anesthetic agent.

Mechanism of action Competitive antagonist at α1 receptors Prazosin (Minipress) Use Management of _____________ Tamsulosin (Flomax) Unique structure among α1A antagonists Use Benign prostatic hypertrophy Adverse effects Orthostatic hypotension and tachycardia First dose syncope (FAINTING) Nasal congestion Abnormal ejaculation - internal urethral sphincter does not close

Mechanism of action Competitive antagonist at α1 receptors Prazosin (Minipress) Use Management of hypertension Tamsulosin (Flomax) Unique structure among α1A antagonists Use Benign prostatic hypertrophy Adverse effects Orthostatic hypotension and tachycardia First dose syncope (FAINTING) Nasal congestion Abnormal ejaculation - internal urethral sphincter does not close

Used to provide regional analgesia, anesthesia by local infiltration, and epidural. Similar activity profile as Lidocaine Expect longer DOA (2-2.5h)

Mepivacaine

I. Clinical issues associated with cocaine -Drug dependency -Mood swing -Insomnia -High blood pressure, -Tachycardia -Cognitive impairment, -Drug withdrawal -Allergic reactions II. Stability issues with coccaine Degradation during sterilization When the structure of Ecgonine is known, development of cocaine analogues accelerated so we hydralyzed and came out with what 3 structures ?

Methanol, Ecgnine, and benzoic acid

2 families of cholinoreceptors. What are they?

Muscarinic & Nicotinic

Tizanidine MOA

Muscle relaxant: Pre- and postsynaptic inhibition - α2 Agonist in spinal cord α2 - inhibitory through inhibition of ACh release.

Uses of Nondepolarizing Neuromuscular Blocking Agents?

Muscle relaxation during surgery (intubation and for orthopedic surgery)

Schwann cells secrete fatter layers upon the Axon called what ??

Myelin... and creates myelin sheath.

NON SELECTIVE B(1ST GEN)-BETA RECEPTOR ANTAGONIST

NADOLOL PENBUTOLOL PINDOLOL PROPRANOLOL- (PROTOTYPE) TIMOLOL*EYE- ORAL SOTALOL LEVOBUNOLOL* EYE METIPRANOLOL*EYE

cell body ..soma..and/or cyton consist of the nucleus .. which has the mitochondria and endoplasmic reticulum. The E.r contains what??

NIssl Bodies!! ( characteristic feature of neurons)

tHE 3 Ionotropic glutamate receptors ARE

NMDA KAINATE AMPA

COMEPTIETIVE IS : nON coMPETITIVE IS :

NONDEPOLARIZATING DEPOLARIZING

CURARE CISATRACURIUM MIVACURIUM PANCURONIUM VECURONIUM ARE ALL WHAT KIND OF REACTANTS ...

NONDEPOLARIZING NEUROMUSCULAR REACTANTS

ARE ALL NEURONS MYELINATED ?? IF NOT ... GIVE EXAMPLE

NOT ALL NEURONS ARE MYELINATED ! NODES OF RAVIER HAS NOT MYLINATION

What are the 2 systems are the main regulatory systems of the body

Nervous and Endocrine

Polypeptide molecules, synthesized in cell body and transported to axon terminal

Neuromodulators

_________________: induce muscle paralysis by blocking skeletal muscle activity THIS Can be further divided into: Nondepolarizing relaxing drugs (tubocurarine, pancuronium): bind to ________ and prevent ACh binding Depolarizing relaxing drugs (___________)

Neuromuscular blockers: induce muscle paralysis by blocking skeletal muscle activity Can be further divided into: Nondepolarizing relaxing drugs (tubocurarine, pancuronium): bind to nAChR and prevent ACh binding Depolarizing relaxing drugs (succinylcholine)

WHaT DOES NMBA STAND FOR ?

Neuromuscular blocking agents

Typical example of cholinergic synaptic transmission ...

Neurotransmission at the Neuromuscular Junction

TRUE OR FALSE Pancuronium is excreted unchanged in urine.

TRUE

THIS IS Located in CNS, adrenal medulla, autonomic ganglia, and neuromuscular junction (NMJ)

Nicotinic receptors

Therapeutic uses of tropicaminde and cyclopentolate

Ophtalmic solutions: mydriasis and cycloplegia Tropicamide - mydriasis for 6 h, cyclopentolate - mydriasis for 24 h.

Therapeutic uses: Atropine (the eye)

Ophthalmic solutions - causes mydriasis, unresponsiveness to light and cycloplegia Permits the measurement of refractive errors without interference by the accommodative capacity of the eye Use other drugs for pupillary dilation if cycloplegia is not needed (Phenylephrine or similar alpha-adrenergic drugs) Has been replaced by short-acting antimuscarinic May induce acute attack of pain in the eye in patients with narrow-angle glaucoma

Receptors: G protein-coupled Receptor location: Nerve endings in GI tract, substantia gelatinosa in spinal cord Function: decrease GI motility, analgesic WHICH TRANSMITTER??

Opioid Peptides

Examples of irreversible indirect-acting cholinergic agonists

Organophosphates: echothiophate (tx glaucoma) insecticides (ex malthion), nerve gas

NON SELECTIVE ALPHA BLOCKERS Irreversible (covalent) binding to α receptors Irreversible (covalent) binding to α receptors Oral, short half-life but long duration of action (24-48 h) TOXICITY • gastrointestinal irritation PHENTOLAMINE OR PHENOXYBENZAMINE

PHENOXYBENZAMINE

USED AS ANTIDOTE FOR PHENCHROMOCYTOMA

PHENOXYBENZAMINE

NON SELECTIVE ALPHA BLOCKER Competitive pharmacologic antagonism at α receptors Pheochromocytoma, antidote to overdose of α agonists Oral, IV • short half-life Duration: 2-4 h PHENTOLAMINE OR PHENOXYBENZAMINE

PHENTOLAMINE

One Schwann cell forms the myelin sheath for ONE AXON

PNS (Peripheral Nervous System)

nervous system is made up of what 2 parts ?

PNS and CNS

FIRST SYNTHETIC ANESTHETIC

PROCAINE IN 1905

wHAT ARE THE 4 TYPES OF PAINFUL SENSATIONS

Painful sensations 1. Pricking 2. Burning 3. Itching 4. Stabbing

-Decrease heart rate -decrease rate of depolarization in sinoatrial node -Increase AV nodal delay (negative dromotropic effect) -Decrease contraction of atria ONLY (negative inotropic effect) -No effect on epinephrine secretion from adrenal medulla

Parasympathetic

Therapeutic uses of benztropine and trihexyphenidyl

Parkinson's disease (largely replaced by levodopa/carbidopa) adjunct therapy, specially in geriatric patients who cannot tolerate stimulants

Depolarizing agents

Phase I: fasciculations ( initial depolarization ) Phase II: (flaccid paralysis)

_______________ used and prolongs action MORE than EPI

Phenylephrine

from cocaine we got.... Ecgonine... then Benzoyl tropine .. then __________ ( fortunately it lacked severe toxicity but had low potency. & DOA)

Procaine

Prototype of Amino Ester is _________________ Prototype of Amino Amide is ________________

Procaine Ldocaine

Describe depolarizing neuromuscular blocking agents

Prototype: succinylcholine succinylcholine binds to nicotinic receptors, opening the channel in the receptor, depolarization, then receptor becomes desensitized and blockade occurs Uses: its short duration of action makes it ideal for certain procedures - endoscopy, endotracheal intubations (sometimes given in continuous IV) - KNOW THIS

Two genetic polymorphisms that manifest with Succinylcholine?

Prolonged apnea (Enzyme used to break down Succinylcholine, is morphed doesn't work, patient stays asleep) Malignant Hyperthermia (Ca++ Doors in SR stay open)

TRUE OR FALSE ANAXONIC NEURONS HAVE NO AXONS AND CANNOT CONDUCT AXON POTENTIAL TEY CAN PRODUCE LOCAL POTENTIALS OR GRADIENT POTENTIALS

TRUE

MYASTHENIA GRAVIS IS THE PRODUCT OF REDUCTION OF ACH RECEPTORS AND. ______________________

REDUCTION OF NMJ FOLDINGS

In the presence of vasoconstrictors (e.g. epinephrine): Reduced __________ absorption Prolongation of conduction blockade _________________ neuronal uptake (higher local concentration) ________________ blood levels.

Reduced systemic absorption Prolongation of conduction blockade Increased neuronal uptake (higher local concentration) Reduced blood levels.

IN THE ENS THE SUBMUCOUS PLEXUSES REGULATE

Regulate blood flow/ epithelial cell function

IN THE ENS THE myenteric REGULATES ..

Regulate digestive tract movements

Renal function: Reduced blood pressure causes a ___________ in renal perfusion, resulting in an increase in Na+ retention and plasma volume. Eye Decreased IOP

Renal function: Reduced blood pressure causes a decrease in renal perfusion, resulting in an increase in Na+ retention and plasma volume. Eye Decreased IOP

1. Striated 2. Multiple nuclei 3. Large number of mitochondria 4. Cell membrane (sarcolemma) and transverse tubules (T-tubules) 5. Cytoplasm (sarcoplasm) 6. Sarcoplasmic reticulum (Ca2+ storage reservoir) 7. Myofibrils: bundle of overlapping actin and myosin filaments all factors of what kind of fibers?

Skeletal Muscle Fibers

Used for minor surgery Optically active amino amide-type local anesthetic. Potent and long DOA (3-15h)

S-Ropivacaine (Noropin)

Stimulation of the ___ node by the autonomic ___ regulates heart rate

SA Nervous System

bOTH SOMATIC AND AUTONOMIC EFFERENT FIBERS ORIGINATE FROM THE BRAIN STEM OR SPINAL CORD BUT WHICH ONE HAS one efferent neuron innervating the effector organ AND WHICH ONE HAS 2 EFFERENT NEURON?

SOMATIC ONE EFFERENT NEURON AUTONOMIC HAS 2 EFFERENT NEURONS

DEPOLARIZING NEUROMUSCULAR REACTANT IS

SUCCINYLCHOLINE-Two ACh molecules.

Microglia

SUPPORT( eliminate disease from nervous system/ tissue)

Cholinergic side effects/toxicity

Salivation Urinary urgency Intestinal cramps Diarrhea Miosis Neuromuscular blockade - inactivation of receptors in the presence of agonists because of desensitization, therefore the receptors just get inactivated and the effects of acetylcholine or other agonists is not seen

Aqueous humor is produced by the ciliary epithelium and it exits through the canal of _____________.

Schlemm

Synthesis: from the AA tryptophan Elimination: reuptake OR inactivation by monoamine oxidase (MAO) Receptors: G protein-coupled receptors 5-HT1-5-HT7, ligand-gated receptor 5-HT3 Source: Blood platelets, gastro-intestinal tract, raphe nuclei Receptor location: CNN (spinal cord, lymbic system), gastrointestinal tract (secretion and peristalsis) WHICH NeurotransmiTTER??

Serotonergic Neurotransmission

Muscarinic Receptor Antagonists: Scopolamine

Similar peripheral effects to those of atropine Greater action on CNS (observed at therapeutic doses) Longer duration of action

THIS Can result from lesions at various levels of CNS: -multiple sclerosis, spinal trauma, cerebral palsy, stroke -Dysfunction in the descending pathways that control the activity of the motor neurons. IS ASSOCIATED WITH ..

Spasticity and muscle spasms

DIFFERENCE BETWEEN SPASTICITY AND SPASMOLYTIC

Spasticity: stiff muscles due to increase tonic stretch reflexes (associated with spinal cord injury, cerebral palsy, multiple sclerosis, and stroke) Spasmolytic: used to treat spasticity

ACh packaged and stored into presynpatic vesicles by (via) active transport process coupled to efflux protons contain ACh & adenosine triphosphate (ATP) & proteoglycan THIS IS CALLED ?

Storage of acetylcholine in vesicles

a modified sympathetic ganglion found in the adrenal gland

The Adrenal Medulla

Adverse effects of ________________ Hyperthermia: concomitant use with halothane (general anesthetic) has occasionally caused malignant hyperthermia (with muscular rigidity, metabolic acidosis, and hyperpyrexia) in genetically susceptible people. Tx: rapid cooling and dantrolene (blacks calcium release from SR of muscle cells), thus reducing heat production and relaxing muscle tone. Apnea: In patients with reduced ChE function due to paralysis of diaphragm. Careful or no use in patients with electrolyte imbalances who also use digoxin or diuretics Hyperkalemia: dangerous in burn patients or those with massive tissue damage

Succinylcholine

Depolarizing muscle relaxant?

Succinylcholine Stimulates ANS ganglia and M receptors

GIVE 4 OF THE 7 Clinical uses of local anesthetics

Surface anesthesia( skin,cornea, and mucous membranes ) Infiltration anesthesia. (injected directly into the tissue) Field block anesthesia. (A. Subcutaneous injection interrupts neural conduction. B. Results in anesthesia distal to the site of injection. C.Useful on extremities and scalp.) Nerve block anesthesia. (A. Injection into individual nerves or nerve plexus. Produces large area of anesthesia with small amount of drug. B. Brachial plexus - upper extremities; intercostal nerve - anterior abdominal wall; cervical plexus - neck.) Intravenous regional anesthesia. (Injection of local anesthetic into a vein of exsanguinated* extremity. Arterial blood flow must be kept occluded to prevent anesthetic from getting into system.) LIKE BP CUFF** Spinal anesthesia. (Produced by injection into lumbar subarachnoid space below the termination of the cord. .. CAN CAUSE HYPOTENSION.. SO PLACE PT IN HEAD DOWN POSITION TO INCREASE VENOUS RETURN TO THE HEART**Lidocaine and tetracaine used most widely. ) Epidural anesthesia. (Injection into epidural space. These drugs may cross the placenta, so when used during labor and delivery systemic toxicity to the neonate may be evident. )

-increase hr, -depolarization in SA, - decrease AV nodal delay, -Increase Contradiction of atria and ventricles, - increase secretion of epinephrine

Sympathetic

Sympathetic NS= ___________ division Parasympathetic NS= _________ division

Sympathetic NS= thoracolumbar division Parasympathetic NS= craniosacral division

The amplitude of local synaptic potentials is proportional to the strength of the stimulation is referred to as ...

Synaptic Potential

Choline transported from extracellular fluid into cytoplasm of cholinergic neuron by energy dependent carrier system that cotransport sodium inhibited by drug hemicholinium choline is permanently positive charge (do to quaternary nitrogen) thus cannot diffuse through membrane. only negative charges can. THIS IS CALLED WHAT?

Synthesis of Acetylcholine

uptake = rate limiting step in ACh synthesis. Formed by reaction of Acetyl CoA and choline (catalyzed by choline acetyltransferase) transported into cytoplasm via sodium cotransporter WHAT IS THIS CALLED

Synthesis of Acetylcholine

THESE ARE ALL GENERAL ANESTHETICS THAT HAVE A DRUG INTERACTION WITH NMBAS ...Isoflurane (most); desflurane, enflurane, sevoflurane (some); nitrous oxide (little) WHAT IS THE DRUG INTERACTION

THAT HELP THE BLOCK.. ENHANCE THE STIMULUS- POTENTIATE THE BLOCK

WHat regulates the activity of the ENS ?

THe ANS

WHat is the advantage conduction of an action potential?

THe action potential can propagate faster along the axon since there is less current loss across the membrane.

TRUE OR FALSE Effects due to blockade of ß-adrenergic receptors Lungs Bronchoconstriction: Blocking β2 receptors in the lungs of susceptible patients causes contraction of the bronchiolar smooth muscle. Therefore, β-blockers, particularly, nonselective -Blockers, are contraindicated in patients with COPD or asthma. Less with ß1-selective agents Cardioselective may be tolerated in COPD

TRUE

TRUE OR FALSE ALPHA 2 COUNTERACT ALPHA 1

TRUE

TRUE OR FALSE AT REST, neurons have an EXCESS of negative chaRges close to the intracellular side of the membrane

TRUE

TRUE OR FALSE Cocaine was the first ANESTHETIC

TRUE

TRUE OR FALSE Drug effects on adrenergic transmission Metyrosine is a tyrosine hydroxylase inhibitor. It decreases catecholamines caused by a type of adrenal gland tumor (pheochromocytoma). Reserpine blocks catecholamine storage &used for hypertension treatment. Guanethidine blocks release of catecholamine and used for hypertension treatment. Amphetamine promotes catecholamine release. Amphetamine is used to treat attention deficit disorder with hyperactivity (ADHD). Imipramine inhibits reuptake of norepinephrine (TCA antidepressant). MAO inhibitors may increase the stores of these transmitters and other amines in the nerve endings. E.g., Selegiline (deprenyl) for Parkinson's disease treatment. And Phenelzine and tranylcypromine for depression treatment. COMT inhibitors: Entacapone and Tolcapone are selective and reversible inhibitor of catechol-O-methyltransferase (COMT). They are used for the management of signs and symptoms of Parkinson's disease.

TRUE

TRUE OR FALSE GABA A AND GLYCINE RECEPTORS ARE IONOTROPIC

TRUE

TRUE OR FALSE Generally small nerve fibers are more sensitive than larger diameter ones

TRUE

TRUE OR FALSE Mechanism of action OF NEUROMUSCULAR BLOCKERS .. Phase 1 block: depolarization (nAChR flickering, membrane depolarization) Phase 2 block: desentization (unclear)

TRUE

TRUE OR FALSE Most are well absorbed orally. Some undergo extensive first pass metabolism and have low bioavailability. Most effects due to blockade of ß-adrenergic receptors. But, these drugs have other effects, which may play a role in their therapeutic actions, including: α1 receptor blockade, partial ß agonist activity, and a local anesthetic action (Na channel block).

TRUE

TRUE OR FALSE Sympathetic autonomic ganglia run along the spinal cord Parasympathetic ganglia are located near the effector organ

TRUE

TRUE OR FALSE The half-life of most beta-blockers is relatively short; those eliminated by the kidney tend to have longer half-life.

TRUE

TRUE OR FALSE Macroglia MAIN CHARACTERISTIC IS FOR function AND CONSIST OF Oligodendrocytes, Schwann cells, Astrocytes (Protoplasmic or Fibrous) peripherial and nervous systems - AND THE development of blood brain barrier

TRUE

TRUE OR fALSE Twitch summation results from a sustained elevation in cytosolic calcium

TRUE

true or false bipolar neurons contain one axon and one dendrite. They have 2 process and are found usually in the ear( like the olfactory epithelium) and eye nerves ( like the retina)

TRUE

true or false the multipolar neuron is the most common type of neuron in the body. They contain mulit processes with ONE AXON and SEVERAL DENDRITES

TRUE

Target tissues FOR ADRENERGIC SYSTEM ARE liver, smooth muscles, lungs, heart and vascular system.

Target tissues FOR ADRENERGIC SYSTEM

_____________________ and ______________ lead to the allergic reaction of PABA

Tetracaine and Benzocaine lead to the allergic reaction of PABA

7. Regarding the spasmolytic drugs, which of the following statements is not accurate? (A) Baclofen acts on GABA receptors in the spinal cord to increase chloride ion conductance (B) Cyclobenzaprine decreases both oropharyngeal secretions and gut motility (C) Dantrolene has no significant effect on the release of calcium from cardiac muscle (D) Diazepam causes sedation at doses commonly used to reduce muscle spasms (E) Intrathecal use of baclofen is effective in some refractory cases of muscle spasticity

The answer is A. Baclofen activates GABA-b receptors in the spinal cord. However, these receptors are coupled to K+ channels. GABA-a receptors in the CNS modulate chloride ion channels, an action facilitated by diazepam and other benzodiazepines.

5. The clinical use of succinylcholine, especially in patients with diabetes, is associated with: (A) Antagonism by pyridostigmine during the early phase of blockade (B) Aspiration of gastric contents (C) Decreased intragastric pressure (D) Histamine release in a genetically determined population (E) Metabolism at the neuromuscular junction by acetylcho-linesterase

The answer is B. Fasciculations associated with succinylcholine may increase intragastric pressure with possible complications of regurgitation and aspiration of gastric contents. The complication is more likely in patients with delayed gastric emptying such as those with esophageal dysfunction or diabetes. Histamine release resulting from succinylcholine is not genetically determined.

4. Which of the following drugs is the most effective in the emergency management of malignant hyperthermia? (A) Baclofen (B) Dantrolene (C) Gabapentin (D) Secobarbital (E) Vecuronium

The answer is B. Prompt treatment is essential in malignant hyperthermia to control body temperature, correct acidosis, and prevent cal- cium release. Dantrolene interacts with the RyR1 channel to block the release of activator calcium from the sarcoplasmic reticulum, which prevents the tension-generating interaction of actin with myosin.

10. Myalgias are a common postoperative complaint of patients who receive large doses of succinylcholine, possibly the result of muscle fasciculations caused by depolarization. Which drug administered in the operating room can be used to pre- vent postoperative pain caused by succinylcholine? (A) Baclofen (B) Cisatracurium (C) Dantrolene (D) Lidocaine (E) Morphine

The answer is B. The depolarizing action of succinylcholine at the skeletal muscle end plate can be antagonized by small doses of depolarizing blockers. To prevent skeletal muscle fasciculations and the resulting postoperative pain caused by succinylcholine, a small nonparalyzing dose of a nondepolarizing drug is often given immediately before succinylcholine.

Questions 2 and 3. A patient underwent a surgical procedure of 2 h. Anesthesia was provided by isoflurane, supplemented by intravenous midazolam and a nondepolarizing muscle relaxant. At the end of the procedure, a low dose of glycopyrrolate was administered followed by pyridostigmine. 2. The main reason for administering the muscarinic receptor antagonist was to (A) Enhance the action of pyridostigmine (B) Prevent spasm of gastrointestinal smooth muscle (C) Prevent activation of cardiac muscarinic receptors (D) Provide postoperative analgesia (E) Reverse the effects of the muscle relaxant

The answer is C. Acetylcholinesterase inhibitors used for reversing the effects of nondepolarizing muscle relaxants cause increases in ACh at all sites where it acts as a neurotransmitter. To offset the resulting side effects, including bradycardia, a muscarinic blocking agent is used concomitantly. Although atropine is effective, glycopyrollate is usually preferred because it lacks CNS effects.

9. Which drug has spasmolytic activity and could also be used in the management of seizures caused by overdose of a local anesthetic? (A) Baclofen (B) Cyclobenzaprine (C) Diazepam (D) Gabapentin (E) Tizanidine

The answer is C. Diazepam is both an effective antiseizure drug and a spasmolytic. The spasmolytic action of diazepam is thought to be exerted partly in the spinal cord because it reduces spasm of skeletal muscle in patients with cord transection. Cyclobenzaprine is used for acute local spasm and has no antiseizure activity.

Epinephrine --> Adrenalin; prototype for alpha and beta receptors

Treatment for Anaphylactic shock

Questions 2 and 3. A patient underwent a surgical procedure of 2 h. Anesthesia was provided by isoflurane, supplemented by intravenous midazolam and a nondepolarizing muscle relaxant. At the end of the procedure, a low dose of glycopyrrolate was administered followed by pyridostigmine. 3. A muscarinic receptor antagonist would probably not be needed for reversal of the skeletal muscle relaxant actions of a nondepolarizing drug if the agent used was (A) Cisatracurium (B) Mivacurium (C) Pancuronium (D) Tubocurarine (E) Vecuronium

The answer is C. One of the distinctive characteristics of pancuronium is that it can block muscarinic receptors, especially those in the heart. It has sometimes caused tachycardia and hypertension and may cause dysrhythmias in predisposed individuals.

6. Which drug is most often associated with hypotension caused by histamine release? (A) Baclofen (B) Pancuronium (C) Tizanidine (D) Tubocurarine (E) Vecuronium

The answer is D. Hypotension may occur with tubocurarine and with the spasmolytic drug tizanidine. In the case of tubocurarine, the decrease in blood pressure may be due partly to hista- mine release and to ganglionic blockade. Tizanidine causes hypotension via α2-adrenoceptor activation like its congener clonidine.

1. Characteristics of phase I depolarizing neuromuscular blockade due to succinylcholine include: (A) Easy reversibility with nicotinic receptor antagonists (B) Marked muscarinic blockade (C) Muscle fasciculations only in the later stages of block (D) Reversibility by acetylcholinesterase (AChE) inhibitors (E) Sustained tension during a period of tetanic stimulation

The answer is E. Phase I depolarizing blockade caused by succinylcholine is not associated with antagonism at muscarinic receptors, nor is it reversible with cholinesterase inhibitors. Muscle fasciculations occur at the start of the action of succinylcholine.

8. Which drug is most likely to cause hyperkalemia leading to cardiac arrest in patients with extensive burns? (A) Baclofen (B) Cyclobenzaprine (C) Dantrolene (D) Rocuronium (E) Succinylcholine

The answer is E. Skeletal muscle depolarization by succinylcholine releases potassium from the cells, and the ensuing hyperkalemia can be life-threatening in terms of cardiac arrest. Patients most susceptible include those with extensive burns, spinal cord injuries, neurologic dysfunction, or intra-abdominal infection.

The direct conversion of an action potential into a chem signal will take place where?

The axon terminal

Beta 2 receptors: Albuterol --> Proventil

Treatment for Asthma

Beta 2 receptors: Salmeterol --> Serevent

Treatment for Asthma & COPD

Beta 1 receptors: Dobutamine --> Dobutrex

Treatment for Bradycardia

Therapeutic uses OF Succinylcholine : Because of its __________ and ________________, succinylcholine is useful when rapid ______________ intubation is required during the induction of anesthesia. Pharmacokinetics: Succinylcholine is injected ______. Its brief duration of action (several minutes: extremely short) results from ___________and rapid _______________by plasma cholinesterase. Genetic variants in which plasma _______________________ levels are low or absent leads to _________________ neuromuscular paralysis.

Therapeutic uses: Because of its rapid onset and short duration of action, succinylcholine is useful when rapid endotracheal intubation is required during the induction of anesthesia. Pharmacokinetics: Succinylcholine is injected intravenously. Its brief duration of action (several minutes: extremely short) results from redistribution and rapid hydrolysis by plasma cholinesterase. Genetic variants in which plasma pseudocholinesterase levels are low or absent leads to prolonged neuromuscular paralysis.

1. Short-acting, centrally-active, α2-adrenergic agonist similar to clonidine 2. Increases presynaptic inhibition of motor neurons 3. Useful in multiple sclerosis or spinal cord injury 4. May have additive effect with baclofen WHAT DRUG AM I?

Tizanidine (Zanaflex)

Two Major Attributes of Local Anesthetics A. Formulations I._________ Free base (neutral) - often for gel or ointment Carmex cold sore treatment. II. _____________ Ionizable basic aliphatic amino group. HCl salts for water soluble dosage forms. B. Structural classes I. Esters II. Amides

Topical Injectable solutions

Beta 2 receptors: Terbutaline --> Brethine

Treatment to prevent premature labor

69- True/False : Isomeric purity is always desired for a drug

True-(Hint: Desired, but not required as long as the non-desirable isomer dot not cause harmful effect.)

WHAT ARE THE 3 various types of neurons in the nervous system

UNI, BI,MULTIPOLAR NEURON

thin filament is the actin... what are the components

actin mole... actinhelix + tropomycin and tropin( calcium binding protein)

Therapeutic uses of reversible cholinomimetic agents: Physostigmine

Used in atony of bladder or intestine, Can be used to treat glaucoma but pilocarpine is more effective. Also used in treatment of overdoses of drugs with anticholinergic actions, such as atropine, phenothiazines, and tricyclic antidepressants - Enters the CNS; actions for 2-4 hours

Therapeutic Uses of reversible cholinomimetic agents: Neostigmine

Used in atony of bladder or intestine. Symptomatic treatment of myasthenia gravis (immune response against nicotinic receptors in nerve junction). Also used as antidote for tubocurarine and other competitive neuromuscular blocking agents. Polar, does not enter CNS Actions for 1/2-2 hours

Pancuronium may increase heart rate -- HOW?

VAGOLYTIC EFFECT - VAGUS NERVE AND CAUSES

Voltage-gated Na+ channels consist of ____ repeats with ___ trans-membrane domains each (S1-S6) ___ constitute the voltage sensor. The hairpin between __and ___ is the pore forming domain Upon a membrane depolarization, voltage-gated Na+ channels go from closed to open (activated state). An open channel undergoes fast ____________.

Voltage-gated Na+ channels consist of 4 repeats with 6 trans-membrane domains each (S1-S6) S4 constitute the voltage sensor. The hairpin between S5 and S6 is the pore forming domain Upon a membrane depolarization, voltage-gated Na+ channels go from closed to open (activated state). An open channel undergoes fast inactivation

which ion channel consist of 1 subunit with 4 domains (I-IV), each domain have 6 transmembrane segments with a voltage sensor and a pore hair loop and is the same structure of ca* channels...

Voltage-gated Na+ channels:

e.g. atenolol are cleared by the kidney. WHAT CLASS OF BETA BLOCKERS

WATER SOLUBLE BETA BLOCKER

Dantrolene MOA

Weakens muscle contraction by reducing myosin-actin interaction Blocks RyR1 - Ca2+ channels in skeletal muscle

21- Which one of the following events is most likely to trigger an action potential A. Summation of graded (or synaptic) depolarizing potentials capable of bringing the membrane potential to threshold B. Opening of leak K+ channels leading to membrane hyperpolarization C. Temporal summation of excitatory and inhibitory postsynaptic potentials equal amplitude D. A decrease in the permeability of the membrane at rest.

22- Graded potentials : A. Are local changes in the membrane potential that occur in varying amplitudes B. Can generate depolarizing spikes that spread actively along the membrane surface C. Are involved in the repolarization of membrane potential during the generation of an action potential D. Occur in an "all-or-none" fashion.

THE ONLY Competitive antagonism at α2 receptors

Yohimbine

23- Inhibitory postsynaptic potential ( or IPSP) ________ A. Are produced by increase in the membrane permeability to K+ and Cl- B. Are generated by activation of nicotinic acetylcholine receptors at the motor end plate C. Can result in a depolarization of membrane potential D. Are triggered by the inactivation of voltage-gated Na+ channels.

45- A patient underwent a surgical procedure of 2 h. Anesthesia was provided by isofluane, supplemented by intravenous midazolam and a nondepolrizing muscle relaxant. At the end of procedure, a low dose of atropine was administered followed by pyridostigmine. The main reason for administering atropine was to: A. Block the cardiac muscuranic receptors B. Enhance the action of pyridostigmine C. Prevent spasm of gastrointestinal smooth muscle D. Provide postopertative analgesia E. Reverse the effect of the muscle relaxant

77- Which of the following is correct regarding Beta-blockers? A. Treatment with Beta-blockers should not be stopped abruptly B. Propranolol is a cardioselective Beta-blocker C. Beta-blockers may cause orthostatic hypotension D. Cardioselective Beta-blockers worsen asthma E. Beta-blockers decrease peripheral resistance by causing vasorelaxation

Norepinephrine acts on two types of adrenoceptors:

a adrenoceptors: & b adrenoceptors

71- Lead compound are identified first and then targeted later in the ___(a)___ drug discovery approach whereas it is opposite in the ___(b)___ approach

a)= past, (b) = genomic/proteomic (Present and future approach). Note: Not sure about this answer.

Graded potentials: a. Are local changes in the membrane potential that occur in varying amplitudes b. Can generate depolarizing spikes that spread actively along the membrane surface c. Are involved in the repolarization of the membrane potential during the generation of an action potential d. Occur in an "all-or-none" fashion

a. Are local changes in the membrane potential that occur in varying amplitudes

a. At low doses: OF NONPOLARIZING AGENTS These drugs bind with _____________ and prevent the binding of acetylcholine. These drugs prevent depolarization of the muscle cell membrane and inhibit muscular ___________ Because these agents compete with acetylcholine at the receptor, they are called _______________ blockers. Their action can be overcome by increasing the concentration of acetylcholine in synaptic gap, for example, by administration of cholinesterase inhibitors, such as ______________, __________________, or edrophonium. b. At high doses: Nondepolarizing blockers can block ion channels of the end plate. This leads to further ___________ of NEUROMUSCULAR transmission.

a. At low doses: These drugs bind with nicotinic receptor and prevent the binding of acetylcholine. These drugs prevent depolarization of the muscle cell membrane and inhibit muscular contraction. Because these agents compete with acetylcholine at the receptor, they are called competitive blockers. Their action can be overcome by increasing the concentration of acetylcholine in synaptic gap, for example, by administration of cholinesterase inhibitors, such as neostigmine, pyridostigmine, or edrophonium. b. At high doses: Nondepolarizing blockers can block ion channels of the end plate. This leads to further weakening of neuromuscular transmission.

The pKa of most local anesthetics is between 7.5 and 9.0, Except:

benzocaine,

Which one of the following events is most likely to trigger an action potential? a. Summation of graded (or synaptic) depolarizing potentials capable of bringing the membrane potential to threshold b. Opening of leak K+ channels leading to membrane hyperpolarization c. Temporal summation of excitatory and inhibitory postsynaptic potentials of equal amplitude d. A decrease in the Na+ permeability of the membrane at rest

a. Summation of graded (or synaptic) depolarizing potentials capable of bringing the membrane potential to threshold

16- Myelination increases the conduction velocity of an action potential along the axon A. True B. False

a. true

stimulation of the SNS will lead to a.contraction of the radial layer of muscle in the iris (dilator) b. stimulate ach release from secretory cells in the adrenal medulla c.decrease in hr and decrease ventricular contractions d. generation of motor end plate potentials

a.contraction of the radial layer of muscle in the iris (dilator)

Which of the following DOES NOT apply to Schwann cells a.produce the myelin sheath for the axon of neurons in the CNS b. form the myelin sheath of onle one axon c. are glial cells found in the PNS d. surround each axon with several concentric rings of myelin

a.produce the myelin sheath for the axon of neurons in the CNS

adrenoceptors secondary messengers a1 : a2: b1 : b2: b3: d1 (dopamine):

a1 : + ca, +dag a2: -camp b1 : +camp b2: +camp b3: +camp d1 (dopamine): +camp

Articaine Bupivacaine Lidocainea Mepivacaine Ropivacaine WHAT STRUCTURES?

aMIDES

Alzheimer disease have significant loss in cholinergic neurons in temporal lobe and entorhinal cortex. What drugs are available to treat the disease?

acetylcholinesterase (AchE) Inhinitors

THe steps for mucle contraction

ach travel through cleft... create synapse and travels through to the postsynapse .. where the ach binds to acetylgated cation channel.. then while traveling unidirectionally .. the sarcoplasmic reticulum releases calcium once action potential travels through the t tubule...the calcium binds to the troponin and allows for myosin binding site to become available ( as the s.r reuptakes the ca) so a contraction can take place .. and once calcium is unavailable .. then back to resting state

Amino Amides*** Increased stability Requires liver amidases Increased activity Lipophilic Less _____________

alergic reaction

Discovery of natural alkaloid Isogramine led to the synthesis of Lidocaine having an ___ amide or ester??? ____ functionality • More stable than procaine

amide

What are the 4 different types of neurotransmotters?

amino acids monoamides peptides other

9- ___ (a) ____ class of local anesthetics are more unstable compared to ___ (b) ____due to their rapid ___ (c) ____ in the plasma.

amino ester, amindes , hyrolyses ( plasma cholinesterase)

11- Benzocaine is ___ (a) ___ class of local anesthetic whereas lidocaine belongs to ___ (b) ___ class of local anesthetics.

amino esters , amino amides

whAT DOES acetylcholinesterase DO?

an ENZYME THAT Breakdown of ACh

Autonomic sensory receptors and neurons----> cns---->Autonomic motor neurons (sympathetic & parasympathetic-involuntary)---> Smooth and cardiac muscles, glands and adipose tissue which nervous system ??

ans

Drugs may reduce propranolol effects by stimulating its metabolism, such as barbiturates, phenytoin and__________.

arbiturates, phenytoin and rifampin.

12- Which of the following is likely to occur when a local anesthetic is co-administered with a vasoconstrictor? A. Duration of action is decreased. B. Duration of action is prolonged. C. Duration of action is unchanged.

14- The mechanism of action of a local anesthetic can best be described by which of the following statements? A. A local anesthetic blocks nerve conductance via nonspecific interactions with lipids bilayer and, therefore reduces sodium ion passage through the sodium channels B. A local anesthetic blocks nerve conductance by binding to specific sites on sodium channels and therefore reduces sodium ion passage through these channels C. A local anesthetic blocks nerve conductance by binding to specific sites on potassium channels and therefore reduces potassium ion passage through these channels D. A local anesthetic blocks nerve conductance via nonspecific interactions with the lipid bilayer and, therefore, reduces potassium ion passage through the potassium channels.

20- Compound X100 has the following effect on neurons: 1-) X100 prolongs the duration of the action potential ten-folds ( from 2 msec to 20 msec); 2-) X100 does not change the resting membrane potential; 3-) X100 causes a ten-fold increase in the duration of the absolute refractory period. Based on your current knowledge of neural physiology, determine what is the most likely effect A. X100 blocks the activity of Na+/K+ pump B. X100 prevents the inactivation of voltage gated Na+ channels C. X100 increases the number of leaks K+ channels open at rest D. X100 blocks the opening of the voltage-gated Na+ channels.

25- Which one of the following accurately refers to alpha and Beta adrenoceptors A- These receptors use Glycine as a co activator B- These receptors are G-protein coupled C- These receptors can be found in sympathetic preganglionic neurons D- These are ionotropic receptors

26- Which one of the following is a common feature of both sympathetic and parasympathetic branches of the ANS? A. Postganglionic neurons release Norepinepherine onto effector organs B. Acetylcholine release from preganglionic neurons activates nicotinic acetylcholine receptors located in postganglionic neurons C. The cell bodies of preganglionic neurons originate in the brain stem D. Postganglionic neurons stimulate the relaxation of renal vascular smooth muscles by releasing dopamine.

32- The pKa of most anesthetics is between 7.5 and 9.0, Except A. Lidocaine B. Benzocaine C. Cocaine D. Procaine

35- Effect of local anesthetic- mediated vasodilation on pharmacokinetic characteristics: A. Greater vasodilation—longer duration of action, reduced systemic absorption B. Greater vasodilation---Increased systemic absorption, reduced duration of action

36- Effectiveness of local anesthetics when injected into infected tissues: A. Greater effect ( greather anesthesia) B. Reduced effect ( reduced anesthesia ) C. No difference

38- Adrenaline added to local anesthetic solution for infiltration anesthesia affords the following EXCEPT: A. Prolongs the duration of local anesthesia B. Makes the injection less painful C. Provides a more bloodless field of surgery D. Reduces systemic toxicity of local anesthetic

39- A child requires multiple minor surgical procedures in the nasopharynx. Which drug has high surface local anesthetic activity and intrinsic vasoconstrictor actions that reduces bleeding in mucous membranes? A. Bupivacaine B. Cocaine C. Lidocaine D. Procaine E. Tetracaine

41- Which of the following agents causes persistent depolarization followed by desensitization of nicotinic receptor: A. Rocuronium B. Succinylcholine C. Acetylcholine D. Dantrolene

43- Which of the following is correct regarding neuromuscular blocking agents (NMBAs) A. Nondepolarizing NMBAs are administered orally. B. Cholinesterase inhibitors reduce the effect of nondepolirizing NMBAs C. Nondepolarizing NMBAs affect diaphragm muscles first D. Effect of depolarizing neuromuscular blockers can be reversed by cholinesterase inhibitors.

46- A muscarinic receptor antagonist would probably not be needed for reversal of skeletal relaxant actions of a nondepolarizing drug if the agent used was A. Cisatracurium B. Pancuronium C. Tubocurarine D. Vecuronium

47- Which of the following drugs is the most effective in the emergency management of malignant hyperthermia? A. Baclofen B. Dantrolene C. Gabapentin D. Secobarbital E. Vecuronium

5- A 3-year-old child has been admitted to the emergency department having swallowed the contents of 2 bottles of a nasal decongestant. The active ingredient if the medication is a potent, selective alpha adrenoceptor agonist drug. Which of the following is a sign of alpha-receptor that may occur to this patient? A. Bronchodilation B. Pupillary dilation (mydriasis) C. Cardiac acceleration (tachycardia) D. Renin release from the kidney E. Vasodilation of the blood vessels of the skin

52- Which Spasmolytic acts by interfering with muscle fiber excitation coupling mechanism? A. Baclofen (Lioresal) B. Dantolene (dantrium) C. Tizanidine (Zanaflex)

53- Compounds that reveal some activities in the very first screening are known as: A. Leads B. Hits C. Pharmacophores D. All of the above

54- Structure activity relationship study must follow the identification of a pharmacophore: A. True B. False

55- Drug discovery and development is a highly efficient process because the screening of a few hundred hits usually results in a viable drug candidate: A. True B. False

6- A new drug was given by subcutaneous injection to 25 normal subjects in phase 1 clinical trial. The cardiovascular effects are summarized in the table below. Which of the following drugs does the new experimental agent most resemble? table : cont peak sys. bp -- 116 -- 156 dia bp -- 76--96 card.out -- 5.0--7.7 hr -- 71.2-- 94.3 A. Atropine B. Epinephrine C. Isoproterenol D. Phenylephrine E. physostigmine

61- During drug discovery and development process, which of the following stages a molecule is typically subjected for identification of its pharmacophore? A- A hit B- A lead C- A FDA approved drug D- All of the above

63- If the two molecules listed below exist as they are drawn, they are called: A. Enantiomers B. Conformational isomers C. Distereoisomers D. Geometric isomers

66- The Molecules A and B are in __ (i) ___ and ___ (ii) ___ conformation, respectively: A. (i) = trans and (ii) = cis B. (i) = cis and (ii) = trans C. (i) = cis and (ii) = cis D. (i) = trans and (ii) = trans

76- A beta-blocker was prescribed for hypertension in a female asthma patient. After about a week of treatment, the asthma attack got worse, and the patient was asked to stop taking the beta-blocker. Which one of the following beta-blockers would you suggest as an alternative for this patient that is less likely to worsen her asthma? A. Propranolol B. Metoprolol C. Labetatol D. Carvedilol

postsynaptic effector cells: lipocytes Lipolysis ..MORE ENERGY .. NEEDED FOR FIGHT OR FLIGHT SCENARIO

bETA 3

___________facilitate secretion of aqueous humor from the ciliary epithelium

bETA ADRENALRECEPTORS

EPI should not be injected in tissues supplied by end arteries(fingers, toes, ears, nose, penis) ...WHY??

because gangrene could result.

steps of crossbridge

bind-- myosin crossbridge to actin powerstroke--crossbridge bends.. pulling myofilament, inward detach--crossbridge detach at end of powerstroke and is back to original position (ATP NEEDED TO DETTACH) bind--crossbridge binds to more distal actin actin mole. and repeat

Changes in____________ trigger the baroreceptor reflex

blood pressure

Side effects of cholinergic antagonists

blurred vision mydriasis urinary retention confusion constipation tachy dry mouth sandy eyes

HOW DO Local anesthetics used to block pain transmission (or sympathetic vasoconstrictor impulses)...

by blocking voltage-gated Na+

1-Release of NE from presynaptic neurons is blocked by which one of the following drugs? A. Imipramine B. Cocaine C. Guanethidine D. Reserpine

18- At midpoint of the depolarization phase of an action potential, which of the following events is most likely to occur A. The activation gate of Na+ channels is closed B. The activation gate of K+ channels is open C. The activation gate of Na+ channels is open D. The inactivation gate of Na+ channels is closed

19- Which of the following events is consistent with the effect of a drug the blocks the opening of voltage-gated K+ channels? A- The resting membrane potential will become more hyperpolarized B- The duration of the action potential will decrease significantly C- After an action potential the membrane potential will remain depolarized for a long time D- Action potentials will propagate faster along the axon

2- Which of the following is correct regarding adrenergic neurotransmission? A. Epinephrine is the major neurotransmitter released from sympathetic nerve terminals. B. Norepinephrine is mainly released from the adrenal glands. C. Tricyclic antidepressants and cocaine prevent reuptake of norepinephrine into nerve terminals D. Monoamine oxidase (MAO) converts dopamine to norepinephrine in the nerve terminal.

24- Depression is often associated with what neurotransmitter deficiency? A. A deficiency of dopamine B. An imbalance between glutamatergic and GABA neurotransmission C. A deficiency of 5-HT D. An excess of GABA

28- Order the following events in the order they take place at neuromuscular junction: 1- Depolarization of the nerve terminal induces calcium entry 2- Acetylcholine diffuses in to synaptic cleft 3- Action potential arrives at the axon nerve terminal 4- Vesicles containing acetylcholine fuse with the presynaptic membrane 5- Acetylcholine binds to nicotinic Ach receptor in the postsynaptic membrane A. 1,4,2,3,5 B. 2,4,5,1,3 C. 3,1,4,2,5 D. 1,3,4,2,5

30- Why will you use Dantrolene as a spasmolytic drug? A. Because dantrolene blocks nicotinic acetylcholine receptors at the neuromuscular junction B. Because dantrolene inhibits the generation of action potentials in skeletal muscles fibers C. Because dantrolene prevents the release of calcium from the sarcoplasmic reticulum in skeletal muscles D. Because dantrolene activates GABA-a receptors on alpha motor neurons

33- The following is NOT true about local anesthetics A. The local anesthetic is required in the unionized form for penetration in the neuronal membrane B. The local anesthetic approaches it's receptor only from the intraneuronal face of the Na+ channel C. Cocaine was the first synthetic local anesthetic D. The local anesthetic combines with its receptor in the ionized cationic form.

34- Result of local vasoconstriction on local anesthetic: A. Increased local anesthetic neuronal uptake B. Reduced local anesthetic blood levels C. Both D. Neither

37- Local anesthetics block nerve conduction by: A- Blocking all cation channels in the neuronal membrane B- Depolarization of the neuronal membrane C- Interfering with depolarization of the neuronal membrane D- Both B and C are correct.

4- Which of the following drugs with its therapeutic dose stimulates Beta-1 receptor only? A. Epinephrine B. Dopamine C. Dobutamine D. Norepinephrine

51- Which of the following drugs has spasmolytic activity and could also be used in the management of seizures caused by overdose of local anesthetic? A- Baclofen B- Cyclobenzaprine C- Diazepam D- Tizanidine

62- How do these two compound relate to each other? A. Enantiomers B. Conformational isomers C. Diastereoisomers

64- The molecules below (A and B) are: A. Distereoisomers B. Conformational isomers C. Enantiomers D. None of the above.

7- A 65-year-old woman with impaired renal function and a necrotic ulcer in the sole of her right foot is admitted to the ward from the emergency department. She has long-standing type 2 diabetes mellitus and you wish to examine her retinas for possible vascular changes. Which of the following drug is a good choice when pupillary dilation---but not cyclopegia is desired A. Isoproterenol B. Norepinephrine C. Phenylepherine D. Pilocarpine E. Tropicamide

73- A 60 -year old female patient started on new antihypertensive medication recently. Her blood pressure seems under control, but she complains of fatigue, drowsiness, and fainting when she gets up from bed (orthostatic hypotension). Which of the following drugs is she most likely taking? A. Metoprolol B. Propranolol C. Prazosin D. Atenolol

The amides are metabolized in the liver, in part by ___________________ isozymes. Liver dysfunction may increase the _________________ half-life of amide local anesthetics (and _____________ the risk of toxicity).

cytochrome P450 ELIMINATION INCREASE

Which of the following drugs with its therapeutic dose stimulates beta-1 receptor only? 1. Epinephrine 2. Dopamine 3. Dobutamine 4. Norepinephrine

Which one of the following events is consistent with the effect of a drug that blocks the opening of voltage-gated K+ channels? a. The resting membrane potential will become more hyperpolarized b. The duration of the action potential will decrease significantly c. After an action potential, the membrane potential will remain depolarized for a long time d. Action potentials will propagate faster along the axon

c. After an action potential, the membrane potential will remain depolarized for a long time

How do nondepolarizing neuromuscular blocking agents interact with cholinesterase inhibitors?

can overcome the action of nondepolarizing neuromuscular blockers, but, with increased dosage, ChE inhibitors can cause a depolarizing block as a result of elevated ACh concentrations at the endplate membrane, enhancing the blockade.

. If the proliferation of extrajunctional receptors is great enough, sufficient potassium may be released to result in ________________.

cardiac arrest.

What are neurons?

cells that carry information to and from the CNS

Therapeutic uses of reversible cholinomimetic agents: Pyridostigmine and ambenonium

chronic management of myasthenia gravis. DOA= 3-6 hrs and 4-8 hrs. Side effects similar to neostigmine.

m1 m4 m5

cns

____________________ is key relationship between nervous and endocrine system

communication

Sufficient duration of action: Minimize local blood flow (duration of action can be extended by addition of a vasoconstrictor) Eg. Epinephrine _____________ smooth muscles of local capillaries→________________ the local blood flow →__________ the time of the local anesthetic at targeted site. Rapid onset and potency : Increase the __________ of the drug Drug can cross neuronal membrane easily (desirable) Protein Binding Enhances duration of action of lipophilic agents Enhances _______________ (CNS and Neuromuslar)

constricts reduces prolongs lipophilicity toxicity

Neuron structure: cell body

contains nucleus and other organelles

Side effects of physostigmine

contraction of visceral smooth muscle hypotension Miosis Bradycardia

Examples of Nondepolarizing Neuromuscular Blocking Agents?

curariform drugs (atracurium, pancuronium) prototype: tubocurarine (curare) - not in US

Marked contraction of the ciliary muscle, which often occurs with cholinesterase inhibitorintoxication is called ______________.

cyclospasm

27- The effect of parasympathetic stimulation on the eye is to ______ the ciliary muscle and to _____ the pupil. A. Contract, dilate B. Relax, constrict C. Relax, dilate D. Contract, constrict

29- From the following list, choose the events that are absolutely required for neurotransmitters release at the NMJ: A. Arrival of an Action potential to the nerve terminal B. Opening of voltage-gated Ca2+ channels in the nerve end terminal C. Fusion of neurotransmitter-filled synaptic vesicle with the presynaptic membrane D. All of the above

31- Which of the following is NOT true regarding local anesthetics A. Local anesthetics block voltage-gated Na+ channels when they are in the inactivated state B. Local Anesthetics block voltage-gated Na+ channels in a time and voltage dependent manner C. Local anesthetics block the action potential in axons that fire at very high rate D. Local anesthetics bind to outer pore of voltage-gated Na+ channels an block Na+ influx.

44- Which drug is most likely to cause hyperkalemia leading to cardiac arrest in patient with extensive burns? A. Baclofen B. Dantrolene C. Rocuronium D. Succinylcholine

48- Which drug is most associated with hypotension caused by histamine release? A- Baclofen B- Pancuronium C- Tizanidine D- Tubocurarine E- Vecuronium

49- A 40-year-old woman, admitted to the emergency department after a car collision, had multiple surgeries to repair her injuries and was placed on mechanical ventilation to assist respiration. On day 13 she was scheduled for a Transesophageal echocardiogram and was given muscle relaxant intravenously to facilitate the procedure. Soon afterward, the patient suffered cardiac arrest, and cardiopulmonary resuscitation was performed successfully. The serum level recorded just before the arrest peaked at 7.3 mEq/L (normal range for serum potassium 3.5 to 5.5 mEq/L), which of the following muscle relaxant most likely caused arrest? A. Cisatracurium B. Vecuronium C. Tubocurarine D. Succinylcholine E. Dantrolene

50- Clinical conditions associated with spasticity: A- Hypertension B- Stroke C- Multiple Sclerosis D- B and C E- A, B and C

60- A process that involes removal of structural elements/ functional groups of lead at a time to find out the minimum structure necessary for a desired activity is called A- SAR B- Identification of a hit C- Identification of lead D- Identification of a pharmacophore

65- Molecules A and B below are: A. Enantiomers B. Distereoisomers C. Conformational isomers D. Geometric isomers

75- A 56-year old man has hypertension and an enlarged prostate, which biopsy shows to be benign prostatic hyperplasia. He complains of urinary retention. Which of the following drugs would be the appropriate initial therapy? A. Albuterol B. Atenolol C. Metoprolol D. Prazosin E. Timolol

the prototype neuromuscular blocker.

d-tubocurarine is no longer in widespread clinical use,

1) Non-depolarizing neuromuscular blockers: competitive antagonist of nAChR:_____________&______________

d-tubocurarine, pancuronium

3) Direct-acting muscle relaxant: Inhibit ryanodine receptor channels, preventing the release of calcium from the sarcoplasmic reticulum: _____________

dantrolene

Target organs: visceral organs, heart, smooth muscles, glands nervous or endocrine systems ?

MOA of Nondepolarizing Neuromuscular blocking agents?

displaces acetylcholine from binding site in nicotinic receptors and therefore no depolarization of the skeletal muscles occurs

40- Which of the following are examples of Ester-type local anesthetics? A. Procaine (Novocain) B. Tetracaine (pontocaine) C. Cocaine D. A and C E. A,B, and C

42- Characteristics of phase I depolarizing neuromuscular blockade due to succinylcholine include: A. Easy reversibility with nicotinic receptor B. Marked muscarinic blockade C. Muscle fasciculation only in the later stage of block D. Reversiblility by acetylcholinesterase (AchE) inhibitors E. Sustained tension during a period of tetanic stimulation

74- A new antihypertensive drug was tested in an animal model of hypertension. The drug when given alone reduces blood pressure in the animal. Norepinepherine when given in the presence of this drug did not cause any significant change in blood pressure or heart rate in the animal. The new drug is similar to which of the following drugs in terms of its pharmacological mechanism of action? A. Prazosin B. Clonidine C. Propranolol D. Metoprolol E. Carvedilol

TRUE OR FALSE : Motor neurons carry response information from CNS to Affectors

effectors

Opposite of SLUDGE-BBB dry mouth dry eyes difficulty urinating and defecating decreased GI motility bronchodilation pupil dilation sweating variable metabolic effects - insulin, glycogenolysis, lipolysis CNS stimulation

effects of adrenergic activation

aminoglycosides effect on muscle relaxants?

enhances neuromuscular blockade neostigmine, pyridostigmine AchE Inhibitors To Reverse Drug Actions. inhibit AchE and increase Ach at the motor end plate

Neurotranmitters Large molecule transmitters (neuromodulators: substance P, vasopressin, ____________)

enkephalin

"wireless & diffused" nervous or endocrine systems ?

Control body activities over long periods nervous or endocrine systems ?

MOA: Local anesthetics block or decrease the__________of nerve cells(sensory neurons). Agents block nerve conductance by inhibition of Na+ ion influx through voltage-gated sodium channels. Inhibition of an action potential or depolarization of the excitable neuron.

excitability

56- Which of the following can be the source lead compounds? A. Bacterial products B. Plant products C. Fungal products D. Library of synthetic compounds E. Library of semisynthetic compounds F. All of the above

70- True/False: Isomeric purity is an absolute requirement for a drug to be marketed

false

true or false Vesicle-associated membrane proteins (VAMPs)= Syntaxin, SNAP 25 Synaptosomal nerve associated proteins (SNAPs) = Synaptobrevin

false Vesicle-associated membrane proteins (VAMPs)= Synaptobrevin Synaptosomal nerve associated proteins (SNAPs) = Syntaxin, SNAP 25

TRUE OR FALSE Action potentials are brief changes in membrane potential that occur when the inside of the cell becomes more negative . Action potentials never have constant amplitude and duration Action potentials are always repolarizing=the inside of the cell becomes more positive

false - positive - always - depolarizing

true or False Contraction occurs as the result of actin filaments sliding on top of myosin filaments. Thin filaments slide toward the RIGHT of the sarcomere Actin and myosin filaments change length during the contraction process. nOT the length of the sarcomere changes during a contraction (SLiding filament theory )

false Contraction occurs as the result of actin filaments sliding on top of myosin filaments. Thin filaments slide toward the CENTER of the sarcomere Actin and myosin filaments DO NOT change length during the contraction process. Only the length of the sarcomere changes during a contraction

true or false glycine&GABA are Excitatory neurotransmitters acetylcholine& noradrenaline are Inhibitory neurotransmitters

false Excitatory neurotransmitters: acetylcholine, noradrenaline Inhibitory neurotransmitters: glycine, GABA

true or false it is not necessary to conduct depolarization in order to activate the active voltage gate channel.

false IT IS NECESSARY

true or false The presence of a resting membrane potential ( WHICH IS generated by the separation of SIMILAR charges across the membrane ) allows neurons to generate electrical signals (action potentials) that can travel short distances

false OPPOSITE CHARGES ACROSS THE MEMBRANE AND TRAVEL LONG DISTANCES

true or false unipolar (one process) neurons are only find in invertabrates and pseudo unipolar neurons are found in humans and are specific to sensory neurons. they contain dendrites. mainly found in spinal region)

false they do not contain dendrites

10- _____ (a) ____ (Ionized vs free bases) forms of local anesthetics are suitable for topical application as creams

free bases

Nerve cells or neurons

generate & conduct electrical signals)

Linear relationship between amplitude of stimulation and amplitude of local potential and Occurs in any area of the membrane (except in axons) action or graded potential

graded

Muscarinic Receptor Antagonists: Atropine

has both central and peripheral actions general effects last 4 hours unless applied topically in the eye (days) Pharmacokinetics: readily absorbed, partially metabolized by liver, eliminated primarily in urine t1/2 = about 4 hours

67- Molecules identified through the very first screening of thousands of molecules are called ___(a)___

hits

59- While studying SAR, a Scientist synthesized a series of analogues of E-triopidine (See the scheme below). This approach of optimization is called: ______(a)_______

homologation

M3 cholinergic receptors are found...

in smooth muscle glands, they increase IP3 and increase DAG

WHAT IS THE ROLE OF MYELINATION??

increase the conduction velocity of an action potential along the axon

THESE ARE ALL GENERAL ANTIBIOTICS THAT HAVE A DRUG INTERACTION WITH NMBAS ., gentamicin or tobramycin WHAT IS THE DRUG INTERACTION

inhibit acetylcholine release from cholinergic nerves, this leads to enhancement of neuromuscular blockade. DRUG AFFECT STRONGER

modifying the force or speed of contraction of muscles

inotropic

68- Potential drug candidate molecules identified through the evaluation of hits are called ___(a)___

leads

WHat is Ryanodine Receptor CHannels

located in the sarcoplasmic/endoplasmic reticulum membrane and are responsible for the release of Ca2+ from intracellular stores during excitation-contraction coupling in both cardiac and skeletal muscle.

How do nondepolarizing neuromuscular blocking agents interact with calcium-channel blockers?

may increase the neuro-muscular blockade of nondepolarizing blockers as well as depolarizing blockers

Ganglionic Blocking Agent Examples

mecamylamine, trimethaphan, nicotine* (not a true antagonist, agonist and causes desensitization)

Termination of local drug action by: _______________ Systemic distribution (minimizes the concentration of a drug at the local site)

metabolism

mAChR regulate the shape of the lens for _______vision

near

4) Cholinesterase inhibitors: inhibit the breakdown of ACh. Increases the concentration of ACh at the NMJ:___________&____________

neostigmine, physostigmine

WHat would happen if .. You block voltage-gated Na+ channels? (tetrodotoxin, local anesthetics)

no action potential

WhAT ARE THE 4 IDEAL PROPERTIES OF A LOCAL ANESTETIC

non-irritating to tissue no permanent damage low systemic toxicity rapid onset

Preganglionic neurons and parasympathetic postganglionic fibers release acetylcholine (ACh) YET Sympathetic postganglionic fibers release ______________,_____________ or ______________.

norepinephrine, acetylcholine or dopamine

"wired & specific" nervous or endocrine systems ?

Coordinate rapid, precise responses nervous or endocrine systems ?

Generate signals that propagate rapidly (action potentials) nervous or endocrine systems ?

Target organs: skeletal muscles, heart, glands nervous or endocrine systems ?

57- The minimal structure that is needed to elicit pharmacological response is called __ (a)__

pharmacophore

Therapeutic uses of DARIFENACIN, FESOTERODINE, OXYBUTYNIN, SOLIFENACIN, TOLTERODINE, AND TROSPIUM CHLORIDE

overactive urinary bladder disease

THESE ARE ALL CHOLINESTERASE INHIBITORS THAT HAVE A DRUG INTERACTION WITH NMBAS Cholinesterase inhibitors: Drugs such as neostigmine, physostigmine, pyridostigmine, and edrophonium WHAT IS THE DRUG INTERACTION

overcome the action of nondepolarizing neuromuscular blockers... THEREFORE DECREASING THE AFFECT

negative chronotropic effect negative dromotropic effect negative inotropic effect parasympathetic or sympathetic

parasympathetic

Metabolism of ester local anesthetics is carried out by _____________________________ (pseudocholinesterases).

plasma cholinesterases

which ion structure consists of two subunits, each with two pore hair loops and 4 transmembrane domains (M1-4)

potassium leak channels

What does atropine do for the eye?

prevented or reversed by muscarinic blocking drugs

Therapeutic use of scopolamine

prevention of motion sickness blockade of short-term memory (anesthetic procedures)

Once the action potential reaches the axon terminal, it sends a chemical signal to other neurons or effector organs... This is called __________ transmission

synaptic

are drugs that when given topically or by regional injection to a localized area, produces a state of local anesthesia by __________ blocking the nerve conductance that transmit the feeling of pain from the targeted site to the ________.

reveribly brain

Unique Attributes of Local Anesthetics Regional injection (application) at site of action: Produces a _______________ blockade. Selective for sensory neurons with ____________ effect on the motor neurons. E.g. Lidocaine is used as a dental anesthetic or as a local anesthetic for minor surgery

reversible minimal

Vecuronium and __________are deacetylated in the liver, and their clearance may be prolonged in patients with hepatic disease. These drugs are also excreted unchanged in the bile.

rocuronium

The __________ is the functional unit of skeletal muscles

sarcomere

Anesthesia - the loss of ___________ with or without loss of consciousness.

sensation

Relay neurons connec

sensory neurons with motor neurons

Addition of epinephrine (1:200,000) generally doubles the duration of action of a local anesthetic by causing vasoconstriction which ....

slows down the rate at which the anesthetic is washed out of the tissue.

The local anesthetics constitute a group of chemically similar agents (esters and amides) that block the ______________ of excitable membranes.

sodium channels

2 other names for cell body is ...

soma and/or cyton

Somatic and special sensory receptors and neurons ---> cns--->Somatic motor neurons -----> Skeletal Muscles which nervous system ??

somatic

Peripheral nervous system consists of__________________________.

spinal nerves and cranial nerves

2) Depolarizing neuromuscular blockers: Agonist of nAChR:_____________

succinylcholine

Phase I Blocking? What enhances this phase?

succinylcholine only drug in this class. (1) succinylcholine binds to nicotinic receptor and opens the (2) channel and motor end plate depolarizes (3) muscle contracts (4) succinylcholine not rapidly removed and channel remains open (depolarized) and can not respond to new impulses (5) flaccid paralysis results (6) AchE inhibitor drugs enhance this Phase I Blocking (good trivia question)

Describe polymorphisms in the population regarding metabolizing succinylcholine ?

succinylcholine removed by plasma cholinesterase. plasma cholinesterase genetic polymorphisms have been identified which take longer than 10-15 min to hydrolyzed succinylcholine. molecular variant results in longer patient recovery time, prolonged apnea

Glial cells 3 FUNCTIONS

support nourish protect the neurons

positive chronotropic effect positive dromotropic effect positive inotropic effect parasympathetic or sympathetic

sympathetic

WHAT IS THE orderly evolution of block components

sympathetic transmission THEN temperature, pain, light touch, and finally motor block.

The space between axon terminal of one neuron and the axon body is called what ?

synapse

Ciliary muscle contraction also puts tension on _______________________which drains aqueous humor into the canal of Schlemm.

the trabecular meshwork

Botulinum Toxin used for?

treatment for spastic condition lasts from weeks to several months. Cholinergic nerve terminals and decreasing the release of ACh, causing a neuromuscular blocking effect.

Therapeutic uses of reversible cholinomimetic agents: Tacrine, donepezil, rivastigmine, and galantamine

treatment of Alzheimer's disease, where patients have a deficiency of cholinergic neurons in the CNS. decrease in amount of acetylcholine in synaptic cleft - so inhibiting enzyme will increase acetylcholine. They delay but not stop progression of this disease. Side effects: hepatotoxicity (tacrine), GI distress.

True or False ? Neurofibrils help maintain the SHAPE of the cell.

true

terminal boutons ( nerve ending ) send signals to other neurons.. true or false

true

true or false blockade of excitable nerve conduction leads to a loss of pain sensation and impairment to some motor function.

true

true or false Clinical uses of Adrenoceptor Agonists & Sympathomimetic Drugs Epinephrine - α and ß agonist Norepinephrine - more α-selective, also ß1 Dopamine - shock

true

true or false Cocaine is a local anesthetic with a peripheral sympathomimetic action that results from inhibition of transmitter reuptake at noradrenergic synapses. It readily enters the CNS and produces an amphetamine-like psychological effect. A rapid onset of action can be obtained when smoked, snorted into the nose, or injected, has made cocaine a heavily abused drug.

true

true or false Action potential unable to travel backward along the axon because Absolute and relative refractory period( CANNOT GENERATE ACTION POTENTIAL)

true

true or false INCREASE DIAMETER OF AXON TO INCREASE SPEED // MYLENATION INCREASE THE PROPaGATION AND PROCESSING OF INFORMATION

true

true or false Increased outflow reduces intraocular pressure, and is a very useful result in patients with glaucoma.

true

at rest parasympathetic activity prevails:

vagal tone

which ion channel consist of 4 separate subunits (tetramer), each subunit has 6 transmembrane domains with a voltage sensor and a pore hair loop

voltage gated potassium channel

α1 antagonists decrease peripheral vascular resistance and __________ arterial blood pressure by causing the relaxation of both arterial and venous smooth muscle. However, the first dose of these drugs produces an exaggerated hypotensive response that can result in syncope (fainting). This action, termed a "first-dose" effect, may be minimized by adjusting the first dose to one-third or one-fourth of the normal dose, and by giving the drug at bedtime.

α1 antagonists decrease peripheral vascular resistance and lower arterial blood pressure by causing the relaxation of both arterial and venous smooth muscle. However, the first dose of these drugs produces an exaggerated hypotensive response that can result in syncope (fainting). This action, termed a "first-dose" effect, may be minimized by adjusting the first dose to one-third or one-fourth of the normal dose, and by giving the drug at bedtime.

Baclofen Botulinum toxin type A Botulinum toxin type B Carisoprodol Chlorzoxazone Cyclobenzaprine Dantrolene Diazepam Gabapentin Orphenadrine Riluzole Tizanidine What kind of drugs ?

• MUSCLE RELAXANTS (SPASMOLYTICS)

Atracurium Cisatracurium Pancuronium Rocuronium Succinylcholine Tubocurarine Vecuronium WHat kind of drugs

Dr.Martin Neurotransmitter

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