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POM Exam II > Pharmacology II > Flashcards

Pharmacology II Flashcards

1
Q

most FDA approved drugs target which aspect of your body?

A

proteins

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2
Q

which proteins do drugs target?

A

receptors (agonist, antagonist, and inverse agonist), ion channels, enzymes, and carriers

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3
Q

agonist drugs mimic/block the effects of the endogenous agonists

A

mimic

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4
Q

antagonist drugs mimic/block the effects of the endogenous agonists

A

block

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5
Q

Kd

A

dissociation constant; concentration of drug for which 50% of receptors are occupied; direct reflection of affinity for the drug

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6
Q

x-axis

A

usually drug concentration

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7
Q

hill-langmuir equation

A

Y = [D]/ (Kd + [D]) Y (fraction bound to receptor) D = drug

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8
Q

the lower the Kd the more potent/efficacy the drug has

A

potent

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9
Q

potency

A

how much drug is needed for reaction

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10
Q

How would increased potency affect kd and affinity?

A

lower Kd = higher affinity

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11
Q

How would decreased potency affect kd and affinity?

A

higher kd = lower affinity

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12
Q

Does efficacy and potency correlate?

A

they do not necessarily correlate; there are drugs that can be more effective at lower potencies and vice versa

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13
Q

why does receptor occupancy not necessarily affect effectiveness?

A

signal amplification allows a smaller number of receptor occupancy for a larger reaction

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14
Q

receptor reserve

A

receptors that can bind agonist but do not have to to reach maximal effect

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15
Q

two types of antagonist drug molecules

A

competitive and noncompetitive

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16
Q

competitive antagonist

A

compete for the same spot as the endogenous molecule; binds reversibly

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17
Q

two types of non-competitive antagonist

A
  1. reversible 2. irreversible
18
Q

how does a competitive antagonist affect the potency and efficacy?

A

decrease in potency same efficacy

19
Q

how would a non-competitive antagonist affect potency and efficacy?

A

decrease in efficacy

20
Q

full agonist

A

elicits the maximal response from its receptor

21
Q

partial agonist

A

elicits sub-maximal response form its receptor

22
Q

neutral antagonist

A

decreases endogenous agonist but has no effect itself

23
Q

inverse agonist

A

inhibits the basal activity of a receptor in the absence of endogenous agoinist; can also be competitive antagonist and block the effects of endogenous agonists

24
Q

inverse agonist and competitive antagonist examples

A
  1. metoprolol: cardio- hypertension 2. losartan: cardio- hypertension 3. famotidine- GI- histamine blocker 4. naloxone- neuro- emergency treatment for heroin/opiod overdose 5. risperidone GI- histamine blocker
25
Q

dose-response curves are useful for describing effects that are continuous/quantal

A

continuous ex. pain, blood pressure, anxiety

26
Q

what does a does curve mean when the variable is quantal?

A

the curve shows the % of patients; uses a curve to describe a population

27
Q

therapeutic window

A

the dosage of drug from the minimum therapeutic effect to the minimum toxic does

28
Q

Therapeutic index (TI)

A

TD50 (toxic drug concentration where 50% is bound to receptor)/ ED50 (effective drug concentration where 50 % is bound to the receptors) or LD50 (lethal) / ED50

29
Q

higher or lower therapeutic index is better?

A

higher

30
Q

Why would the sape of a dose-response curve be different for therapeutic versus toxic effects?

A

different receptors may accound for therapeutic and toxic effects

31
Q

How is the therapeutic index affected if different receptors are used for therapeutic and toxic effects?

A

TI would grossly overestimate the safety of the drug

32
Q

certain saftey factors (CSF)

A

LD1 (lethal dose one)/ TD99 (therapeutic effect 99)

higher is better

33
Q

If you have drug A = 10 and drug B = 5 what is the overall synergy effect?

A

> 15

34
Q

If you have drug A = 10 and drug B = 5 what is the overall additive effect?

A

15

35
Q

If you have drug A = 10 and drug B = 5 what is the overall antagonist effect?

A

< 15

36
Q

potentiation

A

when drug A has a therapeutic effect and drug B does not have any therapeutic effect but helps increase the therapeutic affect of drug A

37
Q

example of potentiation

A

cephlasporin/penicillin and probenecid

38
Q

tolerance/desensitizaton

A

reduced effect with continued use of drug over a period of time

39
Q

tachyphylaxis

A

short-term tolerance/desensitization leaving durg less effective shortly after given due to desensitizatoin

40
Q

casues of desensitization

A
  1. receptor inactivation - uncoupling from signaling cascade
  2. receptor internalization via endosomes
  3. receptor down regulation via lysosome and break up
41
Q

how does tolerance/desensitization affect the dose response curve?

A

could decrease potency and eventually decrease eficacy

POM Exam II (11 decks)

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