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Physiology > Pharmacology I > Flashcards

Pharmacology I Flashcards

1
Q

define pharmacology

A

the branch of medicine concerned with the uses, effects and modes of action of drugs

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2
Q

define pharmakinetics

A

the actions of the body on the drugs

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3
Q

define pharmadynamics

A

the actions the drugs have on the body

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4
Q

what does ADME mean?

A

A absorption
D distribution
M metabolism
E elimination

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5
Q

Drug-receptor interactions:

Agonist

A

drug or natural ligand
activates the receptor
sometimes selective and sometimes not

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6
Q

Drug-receptor interactions:

anatgonist

A

*bind to receptor but do not activate
interfere with agonist
typically shift dose-response to the right

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7
Q

Drug-receptor interactions:

allosteric activator

A

postitive allosteric modulator
*binds to receptor site separate from agonist site
potentiates effects

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8
Q

Drug-receptor interactions:

allosteric inhibitor

A

negative allosteric modulator
bind receptor site separate from agonist site
*noncompetitive
*actions often reversible

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9
Q

in the absence of drugs, the two isoforms are in equilibrium and what is favored

A

receptor inactive

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10
Q

what is a full agonists

A

has a much high affinity for the active receptor conformation and mass action thus favors the formation of the active receptor bound to the drug complex with a much larger observed effect**

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11
Q

Partial agonists

A

produce lower response at receptor occupancy than full agonist

  • intermediate affinity for both inactive and active receptor(less affinity than full agonist)
  • does not stabilize active receptor-drug complex as well as a full.
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12
Q

Inverse agonist

A

have a greater affinity for inactive receptor, reduce constitutive activity, and may produce a contrasting physiologic result

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13
Q

conventional antagonist

A

equal affinity for the active and inactive receptor and thus no change in constitutive activity.
**flat line on graph

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14
Q

what is the effective concentration 50?

A

drug concentration where effect is half the maximum

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15
Q

what is the Kd?

A

drug concentration where receptor occupancy is half the maximum

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16
Q

what causes a shift to the right in the EC50?

A

agonist and a competitive antagonist

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17
Q

what causes a drop in the agonist effect?

A

agonist and a noncompetitive antagonist

**no shift in EC50

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18
Q

what is the plateau?

A

the max effect of the agonist effect

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19
Q

what is the threshold?

A

the lowest dose that causes a measurable effect

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20
Q

receptors are spare for a given pharmacologic response if it is possible to do what?

A

elicit a maximal biologic response at a concentration of agonist that does not result in occupancy of the full complement of available receptors.
-so after one dose you can give another dose and get a maximal effect again due to spare receptors

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21
Q

additive drug-receptor interactions

A

sum of the two drugs is equal to the two drugs

22
Q

synergistic drug-receptor interactions

A

the sum of the two drugs is greater than the sum of the two drugs

23
Q

antagonistic drug-receptor interactions

A

additive effect is less than the sum of the two drugs

eg. antidote

24
Q

chemical antagonist

A

does not involve receptor
eg. protein that is positively charged at physiologic pH counteracting the effects of a drug that is negatively charged by ionic binding that makes the other drug unavailable to interact

25
Q

physiological antagonist

A

involves endogenous regulatory pathways mediated by different receptors

26
Q

what does efficacy mean?

A

refers to the number of receptors that must be activated to yield a maximum response.

27
Q

A drug with high efficacy needs to stimulate only a small or large percentage of receptors?

A

small percentage
**lower dosing needed
vertical response

28
Q

a drug with a lesser efficacy (but still not considered to be a full agonist) has to activate a small or larger proportion of receptors?

A

larger percentage of receptors
**higher dosing needed
verticle response

29
Q

what does potency mean?

A

the relative concentrations of two or more drugs that produced the same drug effect. This effect is usually chosen is 50% of the maximal effect and the dose causing this effect is called the EC50

30
Q

is potency a vertical or horizontal relationship?

A

horizontal

31
Q

what is the therapeutic index?

A

toxic dose/effective dose

you want a wide range and a big number

32
Q

what is the therapeutic range?

A

the dose between toxicity and therapy

33
Q

what is margin of safety?

A

the amount of drug that is lethal to 1% divided by the amount of drug that causes beneficial effect in 99%

34
Q

a wide margin of safety means what?

A

a large difference between toxic dose and therapeutic dose

35
Q

what does parenteral mean?

A

not by way of intestine or GI tract

36
Q

intravenous

A

very rapid, easier to titrate avoids sub. cutaneous irritation, overdoses may have effects too immediate to reverse

37
Q

intramuscular

A 
prompt absorption (5 minutes owing to blood flow) 
large volumes possible, sometimes painful
38
Q

subcutaneous

A

adsorption may be less rapid (i.e. 15 minutes)

smaller volumes than intramuscular, sometimes painful

39
Q

enteral

A

by way of the intestine or GI
Buccal or sublingual
oral
rectal

40
Q

buccal or sublingual enteral

A

under tongue or incheek

41
Q

oral enteral

A

most common and convenient, onset of effects in 30 min.
most unpredictable
absorption via duodenum
first pass metabolism

42
Q

rectal enteral

A

solution(enema) or suppository

less first pass than oral

43
Q

the initial distribution of drug into tissues is determined by what?

A

rate of blood flow

44
Q

the concentration of drug at a particular site is related to what?

A

affinity

45
Q

plasma binding proteins and gastric emptying time can play roles T/F

A

true

46
Q

what is the fastest way to deliver a drug?

A

inhalation

47
Q

topical delivery

A

applied to a surface

48
Q

transdermal delivery

A

onset of effect in 15 min
slow and sustained
nicotine patch

49
Q

what is a loading dose?

A

a boosted initial dose to get the concentration higher than the therapy level to start immediate effects

50
Q

what is a maintenance dose?

A

doses that keep the concentration in the therapy range or window

Physiology (14 decks)

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