Lectures # 1 & 2 Flashcards

1
Q

Define: Drug

A

A medicine or other substance which has a physiologial effect when ingested or otherwise introduced into the body.

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2
Q

Define: Pharmacology

A

Study of the actions of drugs and their effects on living organisms.

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3
Q

Define: Neuropharmacology

A

study of drug-induced changes in nervous system cell functioning

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4
Q

Define: Psychopharmacology

A

emphasizes drug-induced changes in modd, thinking, and behavior.

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5
Q

Can drugs work on the nervous system but not affect brain or behavior?

A

Yes, drugs can work on the nervous system but not affect brain or behavior (example bronchodilators for asthma).

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6
Q

What is Neuropsychopharmacology?

A

When drugs work both on the nervous system and brain.

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7
Q

Define: Drug Action

A

molecular changes produced by a drug when it binds to a target site or receptor.

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8
Q

Define: Drug Effects

A

The changes in physiological or psychological functions that follow drug action.

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9
Q

Does the site of a drug’s action have to be the same as the site of effect?

A

No (morphine in eye).

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10
Q

Define: Therapeutic Effects

A

the drug-receptor interaction produces desired physical or behavioral changes.

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11
Q

Define: Side Effects

A

Everything that is not a Therapeutic effect

Therapeutic=what you want

side= what you don’t

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12
Q

Define: Specific Drug Effects

A

physical and biochemical interactions of a drug with a target site in living tissue.

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13
Q

Define: Nonspecific Drug Effects

A

based on unique characteristics of the individual (e.g., modd, expecations, perceptions, attitudes). Some texts say this is another term for placebo effects, but that is an oversimplification.

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14
Q

Are specific effects the same across individuals?

A

Yes, specific drug effects are the same across individuals.

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15
Q

Are nonspecific drug effects the same across individuals?

A

No, nonspecific drug effects are NOT the same across individuals.

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16
Q

What are some examples of nonspecific drug effects?

A

Placebo Effect

Alcohol happy/sad

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17
Q

Where do drugs have to go through to get to the brain?

A

For drug to get to the brain, it goes throu the blood.

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18
Q

Define: Bioavailability

A

amount of drug in the blood that is free to bind at target sites.

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19
Q

Define: Pharmacokinetic

A

component of drug action: the dynamic factors that contribute to bioavailability.

Pharmacokinetics deals with the movement (motion) of drugs in the body.

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20
Q

What are the Pharmacokinetic Factors?

A
  1. Routes of administration
  2. Absorption and distribution
  3. Binding
  4. Inactivation
  5. Excretion
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21
Q

why does route of administration matter?

A

Route of administration alters absorption rate, this effects blood levels of drug.

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22
Q

What is the most important factor in determining plasma drug levels?

A

The most important factor in determining plasma drug levels is the rate of passage of the drug through cell membranes.

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23
Q

What are cell membranes primarily?

A

Cell membranes are primarily phospholipids- in other words they are made of fat

24
Q

What are ions?

A

An Ion is an atom or molecule with a net electric charge due to the loss or gain of one or more electrons.

25
Q

What is the major property of membranes? what does this mean for ions?

A
  • The major property of membrans (and lipids in general): not permeable to charged ions
  • The molecular characteristics prevent most molecules from passing through unless they are fat-soluble
26
Q

Can lipid-soluble drugs pass through cell membranes? how?

A

Lipid-soluble drugs can pass through cell membranes by ** passive diffusion.**

27
Q

What is passive diffusion?

A

Passive transport is the diffusion of substances across a membrane. As we stated above, this is a spontaneous process and cellular energy is not expended. Molecules will move from where the substance is more concentrated to where it is less concentrated.

28
Q

What effect does ionazation have on drug absorption?

A

Aspirin passes more readily into the blood from the stomach than from the intestine.

29
Q

What do drug effects depend on?

A
  • How rapidly the drug reaches its target
  • Frequency and history of prior drug use
    • Physiological changes occur with use
  • Nosnpecific factors of characteristic of individuals and their environment
    • Conditioning plays a role in drug effect
30
Q

What do capillaries do? What are they?

A
  • Capillaries are the smallest blood vessels
  • Capillaries distribute blood to tissue, and drugs that are bioavailable are in the blood
  • Drugs can leave capillaries through pores, even if the drugs are not lipid-soluble
31
Q

Are capillaries in the brain different from capillaries in the rest of the body?

A
  • Yes!
  • Lipid-soluble drugs can easy enter brain tissue, but the blood-brain barrier limits movement of ionized molecules
  • Basically the brain is on lockdown
32
Q

What is the blood-brain barrier? Why is existance important?

A
  • The Blood-brain barrier is the separation between brain capilaries and the brain/CSF
  • It’s a form of high level security to protect the brain
  • Many substances in blood fluctuate significantly and would have disruptive effects on the brain if materials could move freely between the blood and the brain/cerebrospinal fluid (CSF)
33
Q

What is CSF?

A

CSF is Cerebrospinal fluid which fills the space around the brain and the spinal cord

34
Q

How are brain capillaries different from normal capillaries?

A
  • Capillaries in the rest of the body allow material to move from blood to surrounding cells
  • In brain, there are no clefts (instead tight junctions), movement of water-soluble molecules is minimal
35
Q

What is the purpose of the **tight junctions **found in brain capillaries?

A
  • Brain capillaries are surround by glial feet- extensions of glial cells called astrocytes
  • The feet help maintain tight junctions between capillary endothelial cells
  • Bottom line: the brain is very protected from potentially dangerous substances in the blood (but there are exceptions, like chemical trigger zone)
36
Q

What is a depot?

A

a place for the storage of large quantities of equipment, food, or some other commodity

37
Q

What happens at drug depots?

A
  • Depot binding is another impediment to a drug binding to target receptor
  • Drug depots: binding at inactive sites where no biological effect is initiated
    • Plasma proteins (e.g., albumin), muslce, fat, bone
  • If drug binds to these areas, can’t reach target or be metabolized by liver
  • HOWEVER: Depont binding is reversible
38
Q

What effects can depot binding have?

A
  • Many drugs can compete for depot binding sites
  • New drug can cause a drug that was depot bound to be displaced
  • In some cases this can result in accidental overdose (conscious awareness of depot bound drugs?)
  • Can also go in opposite direction
    • Lipid-soluble Thiopental enters brain and sedates, but depot binding redistributes it, brain level drops in 5 minutes
39
Q

What are first-order kinetics?

A
  • After inactivation via biotransformation (metabolism), metabolites are excreted
  • Generally a drug leaves the body at an exponential rate
40
Q

What is half-life?

A
  • Half-life is the time until 50% of the drug is out of the system (t1/2)
  • The half-life is needed to calculate interval between doses
  • Different drugs have different half-lives
41
Q

How are doses determined?

A
  • Goal with pharmaceuticals- have predictable amount of drug in system that remains constant
    • To calculate this, need to take into account previously administered dose leaves system (half-life), depot binding… everything we have talked about so far
42
Q

What is the goal of determining a dose?

A
  • Goal: **steady state plasma level **where absorption/distribution phase is equal to the metabolism/excretion phase
  • Generally occurs at 5 half-lives
43
Q

Where does most biotransformation occur?

A
  • Most biotransformation (drug metabolism) occurs in the liver
    • alcoholics “destorying their liver”
44
Q

How many types/phases of metabolism are there?

A
  • There are two types/phases of metabolism
45
Q

What are the two different types/phases of metabolism?

A
  • Type 1 or Phase 1: nonsynthetic modification by oxidation, reduction, or hydrolysis
  • Type 2 or phase 2: synthetic reaction requiring combination (conjugation) of the drug with a small molecule such as glucuronide, sulfate, or methyl groups
  • What you are left with is an ionized and biologically inactive substance
  • GENERAL SUMMARY: Type 1 involves changing molecular structure, Type 2 involves adding to structure
46
Q

What is drug tolerance?

A
  • Drug tolerance: diminished response to a drug after repeated exposure
    • Increasing dosages must be administered to obtain the same magnitude of biological effect
47
Q

What is cross tolerance?

A

Cross tolerance: tolerance to one drug can diminish effectiveness of a second drug

48
Q

What is metabolic tolerance?

A
  • **Metabolic tolerance (drug disposition tolerance): **repeated use of drug reduces amount of the drug avaiable at the target tissue.
  • Example: when drugs incrase their own rate of metabolism, by inducing liver microsomal enzymes
49
Q

What is pharmacodynamic tolerance?

A
  • **Pharmacodynamic tolerance **is when nerve cell funtion changes over time to compensate for continued action of drug upon it
  • Can lead to cell making fever receptors (down-regulatio) or making more receptors (up-regulation)
50
Q

What is behavioral tolerance?

A
  • **Behavioral tolerance **(context-specific tolerance): tolerance tha is only due to learned association with environment
    • Disappears in new environment
51
Q

What are unconditioned stimuli?

A

Many psychoactive drugs have reflexive effects (cortical arousal, elevated blood pressure, or euphoria) and act as unconditioned stimuli

52
Q

What are conditioned stimuli?

A
  • Conditioned stimuli is what is around the drugs themselves: the drug-taking procedure or the environment
    • Which may elicit a conditioned response even before the drug is taken (after learning)
53
Q

How does **behaviorla tolerance **work?

A
  • Conditioned response from environment associated with the drug administration elicits responses opposite to drug effect
  • The body is compensating for the drug it “expects” to get
  • This anticipatory conditioned response is compensatory and is behavioral tolerance
    • removal of this may lead to overdose (Sid Vicious as a famous example)
54
Q

What is operant conditioning?

A
  • Operant conditioning- modify behavior due to results/consequences (reinforcement or punishment)
    • Hos is this different from classical conditioning?
  • Operant conditioning can elicit behavioral tolerance
  • Example: Mice learn to run on moving ramp while intoxicated (other groups run on ramps and is separately intoxicated, cannot perform on ramp while intoxicated)
  • Alcoholics learn to appear “normal” while intoxicated
  • Only occurs with experience (requires learning)
55
Q

What is pavlovian or classical conditioning?

A
  • Classical conditioning
    • US-. UR, pair US with something else, it becomes CS, eventually that CS that did nothing on its own now causes CR