Lecture 7 Flashcards

1
Q

Dose response curve depicts what?

A

The efficacy and potency of a drug

Depicts the drug dose vs. the magnitude of drug effect

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2
Q

Where is the maximal effect shown on a dose response curve?

A

The asymptote, this is where side effects may be increased but no additional therapeutic effect is increased.

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3
Q

What is affinity?

A

The ability of the drug to bind to a receptor

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4
Q

What is efficacy?

A

The relationship between receptor occupancy and the ability to initiate or alter a biological response.

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5
Q

What is potency?

A

The amount of drug required to produce and effect of given intensity.

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6
Q

What is ED50?

A

Median effective dose.

This is the dose at which 50% of people show a therapeutic effect.

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7
Q

What is TD50

A

Median toxic dose

This is the dose at which 50% of people show a toxic effect

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8
Q

Margin of safety

A

Also called the therapeutic window.

Ranges of doses between ED50 and serious effects of TD50

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9
Q

Describe Pharmacokinetics

A

Pharmacokinetics is the fate of a drug in the body (what the body does to the drug)

ADME

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10
Q

Describe pharmacodynamics

A

Pharmacodynamics is the biochemical and physiological effects of a drug on the body (what the drug does to the body)

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11
Q

What does ADME stand for?

A

Absorption, Distribution, Metabolism, and excretion

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12
Q

Absorption

A

The process of a substance entering the bloodstream

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13
Q

Distribution

A

The dispersion of substances throughout the fluids of the body

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14
Q

Metabolism

A

The breakdown of drug into metabolites

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15
Q

Excretion

A

The elimination of substances from the body.

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16
Q

What are some examples of pharmacodynamics

A

activity of a drug at intended target

the side effects

duration in the body

17
Q

What factors can affect drug absorption?

A

chemical properties of the drug itself(i.e lipophilicity)

Drug formulation (extended release)

Presence of food, excess mucus or other drugs

18
Q

What is first pass metabolism?

A

Orally administered drugs are often metabolized by the liver before reaching much of the circulatory system. This is first pass metabolism.

19
Q

What is bioavailability?

A

Ratio of amount of drug entering systemic circulatory system to amount of drug ingested

20
Q

What is the one-compatrment model? How is it different from the two or multicompartment model.

A

One compartment model is when a drug rapidly equilibrates with all body tissues. The two or multi compartment model differentially stays in specific tissues.

21
Q

What can influence a drug to be either one-compartment of two- or multicompartment model?

A

The chemical properties of a drug

22
Q

What is the BBB and how does it work?

A

The blood brain barrier.

The brain is protected from many drugs by tightened capillary walls.

23
Q

What makes the tightened capillary walls of the BBB?

A

The endfeet of astrocytes which makes it much harder for many molecules to enter the brain.

24
Q

What kind of drugs can pass easily through these barriers?

A

Lipid soluble drugs?

25
Q

What binds drugs and can distribute them throughout the body?

A

Plasma proteins that are in the blood.

26
Q

Will drugs that bind to a plasma membrane pass the BBB?

A

No, unless they detach from the plasma proteins. Thus drugs with high protein affinity may not be ideal for psychiatric disorders.

27
Q

What is the most common plasma protein?

A

Albumin

28
Q

What is T(1/2)

A

Elimination half life, the time it takes for the body to eliminate half of the peak blood levels.

29
Q

What is steady state? And when does it usually occur?

A

Steady state refers to when the overall intake of a drug is in equilibrium with its clearance rate.

This usually occurs reached after 4-5 elimination half-lives.

30
Q

What is CYP and what does it do?

A

Cytochrome p450s.

CYP is a liver enzyme that breaks down drugs.

31
Q

What is UGT and what does it do?

A

UDP-glucuronyl transferases.

UGT is a liver enzyme that breaks down drugs.

32
Q

What can create variability in rates of drug metabolism?

A

An example would be genetic variants of CYP and UGT

33
Q

Metabolism often involves what?

A

Derivatization and conjugation

34
Q

Are all drug metabolites inactive?

A

No, an example would be the metabolite norfluoxetine that is made from fluoxetine. Norfluoxetine is also an SSRI.

35
Q

Name 5 modes of excretion

A

Urine, Feces, milk, sweat, expired air