Psychoactive Drugs Exam 1

cerbral cortex

Functions: Thought Voluntary movement Language Reasoning Perception FRONTAL LOBE: Higher order thinking Planning Inhibiting impulses Alcohol reduces frontal lobe response

Adderall

amphetamine/dextroamphetamine

lipophilic

Having an affinity for or an attraction to fat and oils (oil-loving).

Homeostasis

Homeostasis is the basis for withdrawal and tolerance Any self regulating process by which biological systems tend to maintain stability while adjusting to conditions that are optimal for survival In response to chronic alcohol use, liver creates more enzymes that metabolize alcohol. Leads to more tolerance.

Bioavailability

How much of the drug is avaible for use by the cells fter its been broken down Enzymes: protein that change one biochemical compound to another can increase or decrease bioavailability Small intestine: oral gastro drugs mostly absorbed in small intestine This required both lipid solubility and water solubility

Theophylline

Medication used to treat asthma. Opens up the airways.

The axons of a neuron may transmit electrical activity to ______. A) Muscles B) Organs C) Other neurons in the brain B) All of the above

All of the above

What effects the response of a drug dose between individuals? Metabolism Emotional state Previous drug use All of the above

All of the above

Blood Brain Barrier (BBB)

Not all drugs are psychoactive The BBB is the capillaries of the brain Most Capillaries: WEAK! Brain Capillaries: STRONG

Pharacodynamics

Drugs typically act on cells via receptors Receptors evolved to respond to natural substance in the body Drug causes some action in that cell

drug elimination

removal of a drug from the body

Acute(short term) effects of alcohol

- sedation - loss inhibition - impaired judgment - slurred speech and ataxia -increase dopamine -euphoria -short term eidheralp

Proof (alcohol)

Numerical value that is double the percentage of alcohol

How do we get drugs into the body?

Oral-digestion Membrane -oral -nasal -other membranes Pulmonary/respiratory Injection Transdermal(through the skin)

Water Solubility

Our tissues contain lots of water. Drugs that are water soluble diffuse into the blood stream quickly and easily

Artery

Oxygenated blood pumped from the heart through arteries Oxygenated blood passes through tissues in the capillaries Vein: De-oxygenated blood drains back to heart

parasympathetic/sympathetic nervous system

Parasympathetic: function is to conserve/restore your body's energy Sympathetic: flight or fight response

Alcohol flush reaction

People who flush when they drink are less able to break down acetaldehyde More common in women and east asians >4 drinks a week increases risk of high blood pressure, stroke and heart today

Do you think the speed at which you feel a psychoactive drug could affect how addictive it is?

Yes, it could make the drug more addictive or be a more impactful experience if it has a quick/instant on set.

How long does it take for drug to reach the brain when inhaled?

Almost instant

Which of the following is most closely associated with depression? Serotonin Dopamine GABA

Serotonin

Adenosine

a nucleoside; a combination of ribose and adenine; serves as a neuromodulator in the brain

Steps of Pharmacokinetics

absorption, distribution, metabolism, excretion

Major parts of the circulatory system

(from top down) -Vasculature of head/arms -Lungs (pulmonary)-Inhale to supply oxygen to body -Heart-pumps blood through the body -Veins-drain deoxygenated blood, towards the heart -Arteries-supply oxygenated blood, away from the heart -Liver-enzymes in the liver are the major way drugs are metabolized -Smal Intestine -Kidneys-important for drug elimination and metabolic byproducts -LUNGS-exhale to eliminate CO2 -Vasculature of legs/feet

Norepinephrine, acetylcholine, dopamine, serotonin, and amino acids are examples of _______.

Neurotransmitters

Anxiety and insomnia as a result of taking an anti-depressant are an example of what?

Side effects

Tolerance

you get used to the effects of a drug so you need more of it to get the same effect

Health risks of alcohol

§Sexual behavior §Alcohol use may enhance interest in sex but impair physiological arousal §Linked to risky sexual behavior (e.g. unprotected sex) §A factor in sexual assaults §Blackouts §Memory lapse, time period where person was conscious but can't remember a period of time. §A danger sign of excessive alcohol use §Crime and violence §Alcohol use is statistically related to: §Homicide §Assault, including family violence, sexual assault,suicide

Benzodiazepines

-most widely prescribed sedatives -prescribed as sleep aids and anti anxiety -enahnces response to GABA -opens up chloride channels making cells more resistant to excitation with positive ions. Neuron is less likely to fire. -legally prescribed but addictive -there is a potential for recreation use/abuse -don't demonize the drug, anxiety can be a serious and depilating condition -patients and docs should decide best treatment -clean=specific effect on GABA receptors -dirty=broad cascade of effects on GABA

barbituarates

-mostly absolute drug with more potential for overdose (higher therapeutic index) -largely been replaced by Benzodiazepines for sleep and anti anxiety -still used medically for anesthesia, epilepsy some intractable, migraines,

Gasotransmitters

Signaling molecules (gases) made in organisms body or originating outside the organism that are used to transmit chemical signals which induce physiological or biochemical changes in the organism, tissue or cell

Depressants (major effects and major subgroups)

-sedative=calming, reduction in anxiety -hypnotic-drowsiness, induction of sleep -tranquilizers, anti-anxiety, medication, sleeping pills, downers -depressants slow activity in central nervous system -slow reaction in CNS -slow reaction time and processing speed -think and act more slowly -interferes with REM sleep (memory) -removes inhibitions Includes -alcohol -barbiturates -benzodiazapines

Stimulants

-substances that can keep a person going mentally and physically -restricted stimulants: cocaine, and amphetamine -medically used

Oral Ingestion Digestion/gastrointestinal Digestive System

Absored into gastrointestinal tract Digestive System Mouth Throat Stomach Esophagus Small Intestine Large Intestine (elimination)

Describe the steps in an action potential

1. Neuron Fires: -the combines messages generate an electrical impulse 2. Axon -the impulse travels to the end of the axon 3. Neurotransmitters -the impulse causes neurotransmitters to be released from the axon 4. Synapse -neurotransmitters move across the gap (synaptic cleft) between neurons 5. Receptor -some neurotransmitters attach to special receptors on the receiving neuron 6. Message Received -messages are received on dendrites or on the cell body 7. Recycle -neurotransmitters are cleared from receptor sites and the synapse 8. New message -a new impulse can start in the receiving neuron

If a drug's elimination half life is 1 hour, how many hours until it is eliminated or changed completely in the body 7 minutes 7 hours 7 days 7 weeks

7 hours

Transdermal (through skin)

Skin absorption Thin skin vs thick skin (hairless) Skin patch -adhesive, rate controlling membrane, reservoir, backing

Acetylcholine

A neurotransmitter that enables learning and memory and also triggers muscle contraction

How does the speed of absorption impact the behavioral effects of a drugs?

A persons experience taking a drug that has immediate effect. For some people it might feel like too much too soon and freak them out, maybe more likely to get addicted if it's quick. More time to adjust with slower drugs,

Distillation

A process that separates the substances in a solution based on their boiling points

Pro/Con of transdermal administration

ALL OF THESE COULD BE PRO and CONS Slow release limited number of lipophilic drugs can pass through the barrier of the skin most of drug is not absorbed variability in human skin across people variability in human skin within people

Which of the following is/are true of alcohol elimination? A. Some alcohol is eliminated unchanged through the breath and skin B. Some alcohol is metabolized in the stomach C. 90% of alcohol is metabolized in the liver D. Some alcohol is excreted in urine E. All of the above

ALL of the above

How is alcohol consumed, absorbed and distributed throughout the body? aka pharmacokinetics of alcohol

Absorption -most absorbed in the villi/capillaries of the small intestine -some absorbed in the stomach -slower if there is food or water in the tummy Non-Gastrointestinal Absorption -can be absorbed through nasal cavities, enema or tampon or through thin mouth tissue -these methods bypass first-pass metabolism -more difficult to titrate dose -increased chance of brain toxicity -smoking alcohol(fast onset, recondenses in the lungs with potential adverse health consequences_ Distribution -blood alcohol concentration -easily passes through BBB -the measure of the concentration of alcohol in your blood expressed as a percentage in terms of grams per 100 ml -BAC increases when the absorption rate is greater than the elimination rate -everything from small intestine has to pass through liver to get to the brain

How do cells communicate?

Action potential: a brief electrical change in a synaptic neuron's charge that communicates with downstream postsynaptic neurons.

Active Transport

Active transport gets large molecules into the brain that the brain needs. Some drugs act like a Trojan horse and use these active transport mechanisms to sneak in.

Downers

Alcohol Barbituates Benzodiazepines

Mechanism of Action

Alcohol enhances the inhibitory effect of GABA Alcohol blocks the effects of the excitatory transmitter glutamate Effects on the dopamine system Increase dopamine in the mesolimbic system Reinforcing, rewarding effects Acute use Increase dopamine release (feel reward) Short term withdrawal effects, less reward than usual Chronic use Decrease dopamine release and down-regulate receptors Leads to less reward from normal pleasurable or rewarding things

Alcohol Behaviroal Effects

Alcohol is a solvent It dissolves organic compounds like lipids Mood changes can include -euphoria -reduced anxieties -reduced inhibitions Effects depend on the TIME COURSE -ex: greater effects are greater when ABC rises fast Effects are influenced by the individuals' alcohol experience -ex: higher BAC is needed to impair chronic heavy drinker Effects are influenced by expectations Ex: placebo effects explain many of the effects on social behavior

Membrane Absorption (oral, nasal, other membranes)

All highly vascularized (capillaries close to the surface) Drug can be dissolved and absorbed under the tongue (chewing tobacco, lsd, cbd, coca leaves Drugs can be snorted(skin is highly vascularized) aka cocaine, crushed pills Other: Rectal or vaginal, urethra, eyes (skin is highly vascularized)) suppository, liquid enema, ointment

Alcohol exerts its intoxicating effects through: A. GABA & Glutamate B. Dopamine C. Endorphins D. All of the above

All of the above

Psychoactive drugs are unique because they affect neurons in our ____ changing our thoughts, emotions, or perceptions. Peripheral Nervous System Central Nervous System Blood Liver

Central Nervous System

Alcohol by volume

Amount of alcohol in beer in terms of percentage volume of alcohol per volume of beer. CHANGE

How does transmitter removal occur

An enzyme present in the synaptic cleft breaks down any neurotransmitter lingering within the synapse OR the neurotransmitter is taken back into the presynaptic cell through the 12-helix reuptake transporter receptor present on the presynaptic membrane.

Which type of half life is impacted most by the rate of a drug's metabolism? A. Distribution Half Life B. Elimination Half Life

B. Elimination Half Life

Lipid Solubility

But our cells have fatty membranes called lipid bilayers. Oil and water don't mix. Fats are hydrophobic (afraid of water) For a drug to get into circulation through the intestinal wall it needs to be fat soluble

cocaine

Cocaine -leaf form -paste -white powder form -chewing or sucking leaves-slow absorption and onset of effects -insufflation (snorting) or cocaine -absorbed through nasal mucous -rapid absorption and onset of effects Intravenous injection -rapid and brief effects Smoked-freebase, crack cocaine -most rapid and most brief effects Coca Leaves -grown in the Andes -Inca culture -reduce fatigue and increase productivity -coca wine -coca leaf extract -slower onset and longer duration

Pros/Cons Oral Administiration

Con When drugs is needed immediately for lifesaving measures When the drug has low bioavailability Pros Easy to take When the drug is highly toxic

Hypothalamus

Functions: Body Temperature Basic Emotions Hunger Thirst Sleep/Wake Cycles Alcohol exerts effects on temperature thirst, sleep cycles

Cerrebellum

Functions: Movement Balance Posture Trouble with balance and walking due to alcohol's effect on cerrebellum

The main structural components of a typical neuron are

Dendrites, soma/cell-body, axon

Distribution Half Life

Distribution half life is the TIME it takes for drug to reach half of its max concentration Relates to the time it takes to distribute a drug though tissue (body water and fat) A Half Life is a way to describe a curve with a single number Imagine the body as a cup of water, various processes determine how long it takes the drug to be distributed through tissues after the initial dosage.

Additive Effects

Drug interactions in which the effect of a combination of two or more drugs with similar actions is equivalent to the sum of the individual effects of the same drugs given alone.

Dose Response Curve/Therapeutic Index

ED50= effective dose (dose required to produce a therapeutic effect in 50% of the population) TD50 -toxic dose -for 50% of the population A large therapeutic index means the drug is safer than one with a small therapeutic index

Hippocampus

Functions: learning and memory The hippocampus is one part of the limbic system that is important for memory and learning. Alcohol blackouts are due to its effects on the hippocampus

Drug Elinimation

Excreted unchanged through skin, breath, urine or bowel Pee, Poop, B.O, bad breath excretion via kidneys to urine drug can be unchanged drug metabolites can also be exerted long after effects of drug are over

True or False: Any substance that crosses the BBB is psychoactive.

FALSE-it must have a way to affect the brain

Intestinal Villi

Finger-like extensions of the intestinal mucosa that increase the surface area for absorption Drugs must be water and fat-soluble to get through cell walls and into the capillaries Drugs are absorbed into capillaries of small intensities

Methanol

For simple alcohol. Much more toxic than ethanol. alcohol in 'poorly made' moonshine. Very dangerous and can make you blind.

Long Term Effects (chronic) of alcohol

In n alcohol present-- decreased dopamine release and downregulate receptors leads to less reward from normal pleasurable or rewarding things Brain tissue loss and cognitive impairment Heart disease Alcohol-related pancreatitis cancer of the breast, mouth, throat and esophagus liver and colon liver disease The liver increases enzymes that metabolize alcohol à tolerance. • Brain also maintains homeostasis "Up-regulated"glutamate receptors (NMDA) "Down-regulated" GABA receptors The brain is adapting and attempting to get back to homeostasis No alcohol present àoveractivity àseizures, cell death

Pulmonary

Inhalation -smoking -inhaler for asthma -laughing gas Nasal/oral cavities larync and treachea lung bronchi alveoli capallaries pulmonary artery

Injection

Intravenous (direct to vein) Intradermal (think derm aka skin) -skin popping -heroin Intramuscular -into muscle -flu shot Subcutaneous -under skin -insulin Medical special case: spinal anethesia -epidural

What does it mean for a molecule of a drug to have higher potency than that of another drug?

It elicits a greater response from the cell

How do things pass the blood-brain barrier?

Large molecules do not pass BBB Molecules with low levels of lipid solubility do not penetrate the brain Lipid soluble molecules such a barbiturate drugs, rapidly cross through into the brain. Molecules that have a high electrical charge are slowed Active transport gets large molecules into the brain that the brain needs. Some drugs act like a Trojan horse and use these active transport mechanisms to sneak in.

Mechanisms of Action for Alcohol

Main neurotransmitter actions -enhances the inhibitory effect of GABA at the GABA receptor Blocks the effects of the excitatory transmitter glutamate Affects dopamine and opioid systems Alcohol causes changes practically every aspect of neuro conduction and neurotransmission Can change things like how soluble membrane is to different substances interact Affects membranes and receptors Most drugs alter functions only at the synapse, alcohol causes changes practically every aspect of neuroconduction & neurotransmission. Can change things like how soluble membrane is to different substances, interact with channel protein directly, change release of NTs Alcohol works on lots of different NTs (glutamate, GABA, dopamine, opioid receptors)

Brain Stem

Medulla Pons Midbrain Located between spinal cord and pons. Functions:cardiac, respiratory, vomiting, heart rate, breathing and blood pressure.Many key life or death functions High levels of alcohol can suppress these functions and be fatal

blood alcohol metabolism

Metabolism -liver metabolizes about 1/4 ounce of alcohol per hour Metabolism is based on a stable rate -"zero-order metabolism"-meaning a constant rate of elimination per unit time (a straight line) Liver adapts to chronic intake of alcohol by increasing enzyme activity -contributes to tolerance among heavy users For heavy alcohol users who have adapted to high alcohol intake -when alcohol is present, the metabolism of some other drugs is slower -when alcohol is not present, the metabolism of some other drugs is faster About 2% of alcohol is excreted/eliminated unchanged (breath, skin, urine) About 90% is metabolised in the liver Remainder is metabolized by enzymes in the rest of the body Alcohol---Alcohol dehydrogenase (enzyme #1)---Acetaldehyde---Aldehyde dehydrogenase (enzyme #2)---Acetic acid

Pharmaco Kinetics

Movement of drugs Determines a drugs actions Onset-when it starts Strength-how strongly it acts Duration-how long the effects last *Dose, the amount of drug taken, can affect other things like duration, strength and onset*

Neural Circuitry

Neuron Cell Body=grey matter Dendrite=gray matter Axon=white matter Myelin Sheath=white matter Synapse Neurotransmitter

How do networks of neurons become connected?

Neuroplasticity Neurons that fire together wire together Neurons out of sync, fail to link

How do enzymes regulate neurotransmitter availability?

They break down neurotransmitters

You enter into a clinical depression study and are directed to take a pill once a day for 6 weeks. You report daily that your mood seems to be improving and you feel less depressed. At the conclusion of the study, you learn that you were given a pharmacologically inert substance, despite feeling significant therapeutic responses. What were you taking? Serotonin reuptake inhibitor Monoamine oxidase inhibitor Benzodiazepine Placebo

Placebo

What are the 3 main parts of the brain stem?

Pons Medulla Midbrain

Possible causes of a hangover

Possible causes:§alcohol withdrawal, exposure to congeners (toxic byproducts of fermentation/distillation), dehydration, stomach upset, reduced blood sugar, and/or the accumulation of toxic byproducts of metabolism (e.g. acetaldehyde).

Pros/Cons of injection

Pro -precision -efficiency -quicker onset -bypasses first pass metabolism Con -infection from dirty needles (HIV/Aids) -pain and bruising -administration risk -long term use=damage to veins/clotting/collapsed veins

What does the BBB do?

Protects the brain from foreign substance in the blood that may injure the brain Protects the brain from hormones and neurotransmitters flowing through the rest of the body for other functions Maintains a constant environment for the brain

True or False? A drug cannot be psychoactive without getting past the blood brain barrier.

TRUE

True or False: Every drug that enters circulation will pass through the liver at some point.

TRUE But only gastrointestinal administration goes through First pass metabolism in the liver before entering circulation

Elimination Half Life

The amount of time for the drug concentration to decrease by 50% in the blood Represents primarily metabolic elimination Metabolic processes largely determine how long it takes the drug concentration to be reduced. Passive excretion only reduces the concretion a little bit Most drugs are changed or completely eliminated from the body in about seven of these elimination half lives

Drug Potency

The amount required to achieve an effect of a given intensity More potent drugs: a smaller amount for a larger effect.

Role of the heart

The heart pumps the blood supply through the entire body circulating this blood about once a minute

The hypothalamus is...?

The principle center in the brain responsible for the integration of our entire autonomic (involuntary or vegetative) nervous system. Hormones, body temp, etc.

Does the structure of synaptic buttons change how they affect the post synaptic neuron?

The shape and size of the axon terminal buttons and the dendrite spines affects the strength of their connection

Pharmacodynamics

The study of the interaction of a drug on receptors and how it effects behavior, physiology, or pharmacology

Agonist Drugs (not natural)

These drugs mimic natural agonist within the body, binding to receptors to create the same effect but often with a much more significant physiological response

If you reduce glutamate neurotransmitter release with some drug over a long period of time, the glutamate receptors will _______. A.Up-regulate B.Down-regulate

Up regulate

Withdrawal

When the drug is not available, you experience an effect opposite that of the drug

Drug Interactions

When two drugs are used together, their effects can be additive (the result is what you expect when you add together the effect of each drug taken independently), synergistic (combining the drugs leads to a larger effect than expected), or antagonistic (combining the drugs leads to a smaller effect than expected)

basal ganglia

a set of subcortical structures that directs intentional movements

Amphetamine

a type of stimulant often used to stay awake or to reduce appetite stimulated central nervous system

A drug that mimics the action of a neurotransmitter is termed a(n) ______________ for that transmitter, where a drug that blocks access of a neurotransmitter to its binding site, inhibiting action of the transmitter is termed a(n) ________________ for that transmitter.

agonist, antagonist

Why is alcohol addictive?

alcohol is a 'dirty drug' that affects GABA, Glutamate, Opioid, and Dopamine systems. Reinforcing, rewarding effects

barbiturate

any of a class of sedative and sleep-inducing drugs derived from barbituric acid.

Astrocyte

are characteristic star-shaped glial cells in the brain and spinal cord. The proportion of astrocytes in the brain is not well defined.

Drug in circulation access cells through the...?

capaliaries

Major Categories of Drugs

depressants stimulants opioids/narcotic analgesics hallucinogens inhalants cannabis other psychoactive agents Antipsychotics Antidepressants

first pass metabolism

drug metabolism that occurs in the intestines and liver during oral absorption of drugs into the systemic circulation must pass through liver before going to the brain

Drug Absorption

entrance of a drug into the bloodstream from its site of administration

Drug Abuse

intentionally using drugs in a way that is unhealthy or illegal

Define the following and be able to identify on an image of cell: Neuron Dendrite Axon Hillock Axon Terminal Buttons Synapse Pre-Synaptic Post-Synaptic Ion Channels Receptors

khkgk

A _______ therapeutic index means a drug is safer than one with a ________therapeutic index.

large, small

Metabolites

molecules made or broken down in the body

Limbic System

neural system located below the cerebral hemispheres; associated with emotions and drives

Drug Distribution

passage of a drug from the blood to the tissues and organs of the body

Alcohol passes through the BBB via??

passive diffusion through the capillary walls because it is small and is both lipid soluble and water soluble.

Sympathomimetic

pertaining to mimicking or copying the effect of the sympathetic nervous system

fetal alcohol syndrome

physical and cognitive abnormalities in children caused by a pregnant woman's heavy drinking alcohol easily crosses the placental barrier affecting the developing fetus-body and brain related to peak BAC, to duration of alcohol exposure and gestational timing 1.Growth retardation before and/or after birth 2.Pattern of abnormal features of the face and head 3.Evidence of CNS abnormality -structural and functional brain dysfunction

Drug addicition

physical or psychological dependence on a drug or medication. You need the drug to feel or function normally

Enzymes

protein that change one biochemical compound to another can increase or decrease bioavailability

Natural agonists

substances within the body that have evolved to produce a response when they bind to and switch on receptor

In what ways do neurons change with repeated stimuli?

size of dendrite contact point number of receptors on dendrite Number of vesicles in axon terminal size of electrical signal

What is one drink?

standard drink has about 1/2 ounce of pure ethanol {aka "alcohol} -12 oz of 4% ABV of beer -4 ounces of 12% ABV wine -1 ounce of 100 proof spirits (50% alcohol by volume)

Xanthines

the class of chemicals to which caffeine belongs

drug metabolism

the conversion of a drug from its active form to a nonactive form

drug misuse

the incorrect use of a prescription or OTC drug

Meninges

three protective membranes that surround the brain and spinal cord

Alveoli

tiny sacs of lung tissue specialized for the movement of gases between air and blood surface area of tennis court tight web of capillaries around each "grape" Lungs go straight to heart which circulates blood through the body and brain

down regulation/up regulation

up regulation: target cells form more receptors in response to the hormone down regulation: target cells lose receptors in response to the hormone

Hydrophilic

water loving

Addiction

when you crave the drug and seek out the drug even though it interferes with normal functioning relationships, and your health

(physical)dependence

when you need the drug to feel normal