pharm exam 1 Flashcards

1
Q

EC50

A

conc. of drug to get 50% of max response

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2
Q

Kd

A

conc. of free drug when 50% is bound to receptors

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3
Q

low Kd

A

high binding, slow dissociation

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4
Q

high Kd

A

low binding, fast dissociation

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5
Q

rightward shift on dose/response curve

A

lower affinity for same receptor, same maximal response

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6
Q

lower magnitude on dose/response curve

A

lower efficacy, lower maximal response

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7
Q

affinity

A

desire to bind

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8
Q

potency

A

amount to produce a response. lower EC50 lower potency.

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9
Q

efficacy

A

maximum possible response, also called intrinsic activity

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10
Q

intrinsic activity

A

also called efficacy, maximum response possible

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11
Q

quantal dose response

A

determines therapeutic ratio, all or none, ED50 and LD50

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12
Q

graded dose response curve

A

determines potency, maximal efficacy etc.

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13
Q

ED50

A

dose producing desired effect in 50% of population

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14
Q

LD50

A

dose produces lethal effect in 50% of population

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15
Q

TD50

A

dose that is toxic to 50% of population

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16
Q

calculate therapeutic index for humans

A

TD50/ED50

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17
Q

calculate margin of safety for humans

A

TD1/ED99

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18
Q

higher margin of safety correlates to:

A

safer drug

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19
Q

allosteric activator

A

binds to a different site than and increases response to agonist

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20
Q

competitive antagonist

A

binds to same site as agonist, decrease Kd or EC50

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21
Q

noncompetitive antagonist

A

bind to different site from agonist, decrease Emax

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22
Q

physiological antagonist

A

works through completely different mechanism

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23
Q

chemical antagonism

A

inactivates drug by chemically neutralizing, like antacids

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24
Q

partial agonist

A

less maximal response than agonist, lower efficacy

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25
Q

ligand regulated transmembrane enzyme examples (tyrosine kinases)

A

insulin, epidermal growth factor, nerve growth facter

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26
Q

cytokine receptor examples (utilize JAKs and STATs)

A

growth hormone, erythropoietin, interferons

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27
Q

ligand gated, voltage gated channel examples

A

nicotinic/Ach, GABA, benzodiazepines, barbiturates

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28
Q

Gs coupled receptors examples

A

beta 1 & 2 drugs, epinephrine, norepi (beta), dopamine, histamine

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29
Q

Gi coupled receptor examples

A

alpha 2 drugs, norepi (alpha), morphine

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30
Q

Gq/IP3/DAG coupled receptor examples

A

alpha 1 drugs

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31
Q

pharmacokinetic tolerance

A

drug induces enzymes for its own metabolism, warfarin with phenytoin

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32
Q

pharmacodynamic tolerance/cellular tolerance

A

change in receptor number or function

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33
Q

physiologic tolerance

A

two drugs with oppposing effects administered together (norepi, histamine)

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34
Q

competitive tolerance

A

agonist and antagonist administered together

35
Q

desensitization vs. down regulation

A

rapid, shuts down ion channels vs. decrease of receptor number

36
Q

idiosyncratic response

A

weird, unexpected response to drug e.g. fast and slow acetylation of isoniazid

37
Q

summation

A

two drugs add up regardless of mechanism 2+2=4

38
Q

additive

A

two drugs act on same mechanism 2+2=4

39
Q

synergism

A

2+2=7

40
Q

type I hypersensitivity

A

IgE mediated, anaphylaxis

41
Q

type II hypersensitivity

A

cytolytic, cytoxic. Igm then IgG. target red blood cells.

42
Q

type III hypersensitivity

A

arthus rxn, serum sickness antigen antibody complexes. target vessels, skin, joint, kidney

43
Q

type IV hypersensitivity

A

delayed hypersensitivity rxn, cell mediated, T cell response. poison ivy

44
Q

placebo

A

20 - 40% of people exhibit good or bad placebo response

45
Q

double blind study

A

researcher and patient unaware of drug content. eliminates bias

46
Q

single blind study

A

patient unaware of drug content

47
Q

the pharmacokinetic process

A

ADME, absorption, distribution, metabolism, elimination

48
Q

pharmacodynamic

A

what a drug does to the body

49
Q

pharmacokinetic

A

what the body does to a drug

50
Q

Vd

A

volume distribution based on 70kg person. drug in body (D)/concentration in plasma (Co)

51
Q

T1/2

A

half life

52
Q

CL

A

clearance

53
Q

first pass effect

A

oral drugs pass through liver and portal vein.metabolized some, decreases bioavailability

54
Q

gastric emptying

A

oral drugs reliant on time spent in stomach

55
Q

parenterl

A

non oral routes of drug admin

56
Q

speed of effect for different routes

A

IV > inhalation >oral

57
Q

definition of dose

A

enough drug to produce a desired effect in an average human with an average ability to absorb, distribute, metabolize, and eliminate the drug

58
Q

factors affecting appropriate dose

A

maturity fo organs, age of patient, organ pathology

59
Q

strong acids and bases

A

one way reaction

60
Q

weak acids and bases (most drugs)

A

reversible reactions

61
Q

initial state of most drugs

A

lipid soluble, non-ionized, capable of passing through lipid bilayer

62
Q

acid drug in an acid environment (or base in base)

A

less ionized, more lipid soluble, higher rate of absorption

63
Q

acid drug in basic environment (or base in acidic)

A

ionized, water soluble, low rate of absorption, ready for excretion

64
Q

ion trapping

A

putting a basic drug in acidic environment or visa versa, promotes excretion

65
Q

to speed up excretion of basic drug in urine

A

acidify the urine or visa versa

66
Q

henderson hasselbach and strong acids/bases

A

does not apply

67
Q

henderson hasselbach equation

A

ph - pka = A/HA or B/BH. if (-) yields a fraction. if (+) yields a whole number

68
Q

bioavailability for IV administered drugs

A

100%

69
Q

bioavailability for non-IV admin drugs

A

less than 100%. values will be given on test if necessary

70
Q

high Vd vs. low Vd

A

binding to peripheral tissue vs. mostly bound to plasma

71
Q

drugs bound to plasma protein

A

have low Vd and prolonged half lives

72
Q

first order elimination

A

plasma concentration is rate limiting. a percentage of drug is eliminated in a standard period of time

73
Q

zero order elimination

A

constant amount is eliminated in standard period of time. e.g. alcohol

74
Q

half life calculation

A

(0.7 x Vd)/CL

75
Q

5 half lives

A

to eliminate a drug or build up and be able to measure a steady state (Css)

76
Q

Css formula conceptual

A

CL and Vd are in denominator. decrease in either results in increased Css

77
Q

loading dose

A

one time large dose to create Css without repeated administration

78
Q

maintenance dose

A

doses given after loading dose to maintain Css

79
Q

loading dose equation

A

Vd x TC

80
Q

maintenance dose equation

A

(CL x TC / F) x dosing interval

81
Q

TC

A

desired target concentration

82
Q

F

A

bioavailability (1 if IV admin)

83
Q

dosing rate equation

A

CL x TC