Applied pharmacology 7th priority - theoritical

What are the uses of morphine since it has analgesic effect one of the main effects

1-Acute trauma. Chronic visceral pain Postoperative pain Cancer pain Myocardial infarction. Pre-anesthesia CV surgery

How are the effects of morphine divided?

1-main effects 2- inhibitory effects 3- stimulatory effects

How are opioids classified?

1-opioid analgesics 2- opioid antitussives 3- opioid-antidiarrheal

What are the uses of partial agnosits

1. Analgesic in severe pain. 2. Alternative to methadone for treatment of opioid addicts (long-acting, slowly dissociates from receptors); given sublingually.

What are the advanatages of pure agonists over pure agonist

1. Less addiction (less euphorialess craving).

Pethidine differs from morphine in:

1. Less constipating (shorter acting). 2. Less respiratory depressant in neonates1 & does not delay labor preferred during labor 3. Atropine-like action:, 4. Risk of convulsions (. NOT used for more than 48 hours.

What are the different sources for opioids ?

1. Plant: 2. Synthetic: 3. Endogenous:

What are the uses of morphine since it hs sedation action one of the main actions of morphine

2. In anesthesia Pre-anesthesia CV surgery

what may be the uses of morphine due to its inhibitory effect ?

3. Acute pulmonary edema in LVF following myocardial infarction: 4. Antitussive

Pethidine is not used for more than ?

48 hours

what are the uses of morphine due to its stimulatory effects ?

5. Antidiarrheal

How morphine provide analgesia effect ?

Decrease Pain perception & emotional response to pain

Why is naltrexone given in alcohol abuse

Decrease craving in chronic alcoholics prevents release

Why pethididne is preferred in labor

Decrease risk of asyphyxia neonaturum

benzodiazepine (e.g. midazolam) - opioid analgesic (e.g. fentanyl). what is the advantge in concious sedation

Easily reversed by flumazenil & naloxone (advantage).

what is concious sedation

(Amnesia, sedation & analgesia without complete loss of consciousness)

what is ctz stimulation due to morphine do ?

Extra : The chemoreceptor trigger zone (CTZ) for emesis, also commonly known as the area postrema (AP), is located within the dorsal surface of the medulla oblongata, on the floor of the fourth ventricle of the brain. The CTZ contains receptors that detect emetic agents in the blood and relays that information to the vomiting center, which is responsible for inducing the vomiting reflex.

How is morphine supplied

Given IV - IM - SC - epidural - orally (extensive 1st pass metabolism).

What are the disadvantages of tramadol?

High risk of convulsions

what are the adverse effects and contraindications of morphine due to its inhibitory effects ?

Hypotension Respiratory depression & asphyxia neonatorum Intracranial tension CI: head injury Delayed labor

why morphine is contraindicated in Asthmsa

Hypotension - itching - bronchospasm (

What are the different types of NSAIDS ? Mention all names

I. Prototype NSAID: acetylsalicylic acid (aspirin). II. Nonselective NSAIDs (ibuprofen, naproxen, diclofenac, piroxicam, indomethacin). III. Selective COX-2 Inhibitors: Celecoxib.

How is naloxone administered?

IV

How are opioid antidiarrheal different from morphine ?

Less addictive than morphine)

What are opiods antitussive and how are they different from morphine ?

Less addictive than morphine)

Is naltrexone long or short acting

Long acting

Is naltrexone short or long acting

Long acting

is morphine now used as an antidiarrheal ?

Loperamide Diphenoxylate (less addictive, more widely used)

When is naltrexone used

Maintenance therapy in addicts

When is naloxone used

Management of acute toxicity

What are the adverse effects and contraindications of morphine since it has the 3 main actions ?

Masks pain CI: acute undiagnosed abdomen Sedation - Narcosis Drug dependence

what are the contraindications and adverse effects of morphine due to its stimulatory effects ?

Miosis Nausea - vomiting (CI: enlarged prostate Biliary colic (CI) Constipation (CI: asthma)

What is tramadol?

Mixed opiod and nonopiod

When is fentanyl preferred and why?

More potent than morphine with rapid onset & shorter action (preferred in anesthesia).

What are the different types of pure agonists ?

Morphine , perhidine , fentanyl

What are the examples of opiod analgesics

Morphine. Syntheticopioids.

Types of pure opioid antagonist

Naloxone - Naltrexone

What is another name for opiod analgesics

Narcotic analgesics

Is the main effect of morphine alwYs euphoria

No can be dysphoria

How are analgesics classified ?

Non opiods and opiods

What are nsaids and their effects ?

Nonsteroidal anti-inflammatory drugs (NSAIDs) are a heterogeneous group having anti-inflammatory, analgesic & antipyretic effect

What are some examples of non-opiods analgesics ?

Nonsteroidalanti-inflammatorydrugs. Paracetamol.

When is Naltrexone used?

Opioid abuse. - alcohol abuse

What is the mechanism of action of opioids?

Opioid receptors Mu (mediate most effects of opioids), kappa & delta, are receptors present in the CNS and periphery (e.g. GIT).

Define opiod

Opioids are drugs with morphine-like effects.

What are other names for dynorphins

Opiopeptides

How is naltrexone administered ?

Oral

What are the forms of supply of pethidine

Oral IM

What are the uses of tramadol?

Oral IM IV

How are other NSAIDs different from acetylsalicylic acid in action ?

Other NSAIDs cause competitive reversible inhibition of COX enzymes.

How paracetamol is diffrrent than NSAIDS

Paracetamol is an analgesic-antipyretic with weak anti-inflammatory action.

How are partial agonists administered ?

Parentral - sublingual

What is buprenorphine

Partial mu receptor agonist

How may times and whyvia naloxone given in cases of acute opioid toxicity ?

Repeated as necessary to avoid relapse into coma since duration of action is shorter than opioids.

is morphine now used as an antitussive ?

Replaced by Codeine Dextromethorphan (less addictive)

Why naloxone is given in asyphyxia neonatorum?

Respiratory stimulant in opioid- induced respiratory depression in newborns.

Is naloxone long or short acting

Short acting

what is the treatment of acute morphine toxicity

Support respiration

to what does tolerance develop in cases of morphine intake

Tolerance develops to all effects except constipation & miosis.

why morphine is contraindicated for people with enlarged prostate

Urine retention (also increase ADH)

When is pethidine used?

Used in ACUTE moderate & severe pain e.g. trauma, postoperative pain, biliary colic or labor pain.

When are nonopiod analgesics used ?

Used in mild to moderate pain (see NSAIDs)

When are opiod analgesics used ?

Used in moderate to severe pain

what are other contraindications of morphine

age extremes - hypothyroidism - liver dysfunction

What is the function of COX 1

constitutive (present normally in tissues regulating its physiologic functions), responsible for forming protective PGs in GIT & kidney.

what will happen due to the inhibitory effect of morphine on the uterine tone

delayed labor

why is morphine contraindicated in cases of liver dysfunction

due to decreased metabolsim

What are examples of endogenous opioids?

endorphins - encephalin - dynorphins

What are the examples of synthetic opioids?

fentanyl - methadone - heroin - pethidine...

WHAT ARE THE SIDE EFFECTS OF FENTANYL

high anesthetic doses leads to chest wall rigidity and decrease thoracic compliance and decrease ventilation

what are the stimulatory effect of urinary and GI tracts by morphine ?

increase tone of wall & sphincters (spasmogenic) but prevent peristalsis therefore stools stagnate & harden due to fluid absorption.

What is the function of COX 2?

inducible (in inflammation), constitutive in endothelium & kidney.

Mechanism of action of Acetylsalicylic acid,

irreversibly inhibits (acetylates) cyclooxygenase enzymes (COX-1, COX-2)inhibits conversion of arachidonic acid to endoperoxidesinhibits PG & TXA2 production.

what are the uses of concios sedation ? BY WHAT

minor procedures or for diagnostic purposes like endoscopy -IV benzodiazepine (e.g. midazolam) - opioid analgesic (e.g. fentanyl).

what is the stimulatory effect of morphine to the oculomotor nucleus

miosis

What are examples of plant sources of opioids ?

morphine - codeine

What is the atropine like action that pethidine has

n: dry mouth, blurred vision,

how morphine helps in cases of Acute pulmonary edema in LVF following myocardial infarction ?

preload & after load Respiratory distress Anxiety all decrease

What are endogenous opioids?

released in the body, acting on opioid receptors, producing morphine-like effects.

what are some other effects of morphine

seizures & rigidity in high doses

What are morphine and codeine termed ? What are they? What are they products of?

termed opiates; natural alkaloids; products of opium poppy).

what will morphine cause due to inhibition of the vaso motor center ?

venular & arterial VD

When is there a high risk of Convulsion of pethidine and why?

with high dose or in renal failure due to accumulation of toxic pethidine metabolite, is norpethidine NOT used for more than 48 hours.

When is tramadol prescribed as an analgesic

• Analgesic in postoperative & chronic moderate pain & in neuropathic pain.

How is tramadol different from morphine ?

• Weak Mu agonist (only partially antagonized by naloxone). • Less constipation, respiratory depression & addiction than morphine.

What are the examples of opioids antidiarheal?

-Loperamide Diphenoxylate (See GIT)

what are the different uses of fentanyl ?

1- Iv epidural spinal transdermal patch patient controlled infusion 1. Analgesic in severe pain e.g. perioperative & cancer pain. 2. In anesthesia (for its analgesic & sedative effects):

when is fentanyl specificaaly used for Anesthesia purposes

1- Pre-anesthetic medication 2- IV anesthetic in cardiovascular surgery ( safer ) 3- concious sedation , neuroleptanalgesia - seizure

What is the indications of administration of Naltrexone

1- opioid abuse 2- alcohol abuse

What are the main effects of morphine ?

A. Analgesia B. Sedation C. Euphoria

what are the stimulatory effects of morphine ?

A. Oculomotor nucleus B. CTZ C. Urinary & GI Tracts D. Histamine release

what are the inhibitory effects of morphine ? what centers do they inhibit?

A. inhibit VMC B. Respiratory center depression C. Cough center D. Uterine tone

When is naloxone used?

Acute opioid toxicity - asphyxia neonatorum

How is tramadol analgesic

Analgesic acting by inhibiting uptake of 5- HT and NA.

Define analgesics

Analgesics are drugs that relieve pain due to multiple causes.

Why is naltrexone given in opoid abuse ?

Blocks euphoria of opioids → loss of desire to take drug (prevents relapse).

what will happen due to inhibition of the respiratory center due to morphine ?

CO2 → Cerebral VD & increased intracranial tension which then may lead to death el brain ytz7l2 in foramen magnum

What are the two cyclooxygenase enzymes ?

CoX1 and COX2

What are the examples of opioids antitussive ?

Codeine Dextromethorphan (See Respiration)

what are the signs and symptoms and what is the diagnostic key for acute morphine toxicity ?

Coma Respiratory Depression Pin pointed pupil ( diagnostic)