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MB1: Principles > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

pharmacokinetics is

A

what the body does to a drug

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2
Q

pharmacodynamics is

A

what a drug does to the body

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3
Q

what is selectivity

A

ability of a drug to distinguish targets within the body

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4
Q

what is selective toxicity

A

drug targets are selective to pathogenic species only

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5
Q

what is an agonist

A

drug binding to receptor to produce a response

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6
Q

what is an antagonist

A

drug binding to a receptor to block or reduce actions of agonist

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7
Q

what is affinity

A

strength of association between ligand and receptor

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8
Q

what is efficacy

A

ability of an agonist to evoke cellular response

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9
Q

what is EC50

A

concentration of agonist eliciting half maximal effect

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10
Q

dose plotted against effectiveness produces a ___ curve on a log graph

A

sigmoidal

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11
Q

what is potency

A

ability of a drug to elicit EC50 at lesser dosages

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12
Q

what is reversible competitive antagonism

A

reversible agonist/antagonist at orthosteric site

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13
Q

what happens to the dose/response curve in reversible competitive antagonism

A

right shift - more drug required for effect

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14
Q

what is reversible non-competitive antagonism

A

antagonist binds to allosteric site

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15
Q

what happens to dose/response curve in reversible non-competitive antagonism

A

max response decreases but no right shift - efficacy lost but no increase in drug dose can help it

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16
Q

what is an autocrine signal

A

signal generated within cell to evoke its own response

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17
Q

what is a paracrine signal

A

short distance signalling to target local cells

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18
Q

what is an endocrine signal

A

slow acting and long range

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19
Q

types of ligand gated ion channels

A

chemical
voltage
mechanical/thermal

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20
Q

what does the alpha subunit of a g protein do

A

modulates enzyme effector

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21
Q

what does beta/gamma subunit of g protein do

A

modulates ion channels

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22
Q

nuclear receptors are bound to by hydrophilic/hydrophobic ligands

A

hydrophobic

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23
Q

ADME

A

Absorption
Distribution
metabolism
Excretion

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24
Q

4 ways a drug can pass across the cell membrane

A

endocytosis
passive diffusion
facilitated diffusion
active transport

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25
Q

principle sites for mediated drug transport

A 
blood brain barrier 
GI tract 
placenta 
renal tubule 
biliary tract
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26
Q

when pKa=pH a drug is

A

half ionised

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27
Q

weak bases accumulate in?

A

low pH

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28
Q

weak acids accumulate in?

A

high pH

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29
Q

small water soluble molecules accumulate in

A

total body water

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30
Q

large water soluble molecules accumulate in

A

ECF

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31
Q

highly plasma protein bound molecules, very large with charge accumulate in

A

blood plasma

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32
Q

what is the apparent volume of distribution

A

extent that a drug partitions between plasma and tissue

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33
Q

volume of distribution equation

A

Vd=dose/[drug]plasma

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34
Q

low Vd drugs remain in

A

vascular system

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35
Q

high Vd drugs remain in

A

adipose, muscle and non muscle

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36
Q

high Vd is anything around or greater than?

A

41L, average body volume

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37
Q

most important drug metabolising organ

A

liver

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38
Q

polar/non polar molecules are more readily metabolised

A

non polar

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39
Q

example of a drug that bypasses phase I metabolism

A

codeine

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40
Q

phase I metabolism

A

breakdown by oxidation, reduction or hydrolysis to produce a reactive metabolite

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41
Q

oxidation can produce harmful metabolites in phase I metabolism. name one

A

paracetemol broken down can cause liver failure

42
Q

high P450 activity means

A

lower drug plasma levels as metabolised faster

43
Q

low P450 activity levels means

A

higher drug plasma levels so potential adverse reaction

44
Q

Phase II metabolism

A

combination of drug with polar molecules to form water soluble metabolite

45
Q

true/false - phase II metabolism terminates all biological activity

A

true

46
Q

principle organ for drug elimination

A

kidneys

47
Q

how do toxic drug effects come about

A

metabolites bind to cell membrane in phase I and are not eliminated
increased drug dose so drug binds to off target receptor

48
Q

true/false - drug absorption IV is gradual

A

false - it is gradual in oral/IM and instantaneous IV

49
Q

what is clearance

A

volume of blood removed of drug per unit time

50
Q

clearance drug graph follows first/second order kinetics

A

first

51
Q

why is clearance important

A

estimates dose needed to maintain desired drug concentration in plasma

52
Q

clearance equation

A

CL= rate of drug elimination/[drug]plasma

53
Q

what does elimination half life determine

A

how much time required for a drug to be eliminated from body

54
Q

generally how many half lives before drug is eliminated from body

A

5

55
Q

calculation of t1/2

A

t1/2=0.693 x Vd/CL

56
Q

what is depolarisation

A

membrane becoming less negative

57
Q

what is hyperpolarisation

A

membrane becoming more negative

58
Q

what is repolarisation

A

membrane returning to resting value

59
Q

influx of sodium will cause cell to become more

A

positive

60
Q

efflux of potassium will cause cell to become more

A

negative

61
Q

what is the absolute refractory period

A

no stimulus can elicit 2nd AP

62
Q

what is the relative refractory period

A

some strong stimuli can elicit 2nd AP

63
Q

true/false - AP will always have same amplitude across an axon

A

true

64
Q

ways to increase AP transmission

A

increased axon diameter

increased myelin

65
Q

branches of ANS

A

sympathetic
parasympathetic
enteric

66
Q

what splits the preganglionic and postganglionic neurons

A

autonomic ganglion

67
Q

true/false - the sympathetic and parasympathetic systems oppose each other

A

false - they work complementary to each other

68
Q

the sympathetic nervous system orchestrates what response

A

stress and energy consumption

69
Q

the parasympathetic nervous system orchestrates what response

A

restorative, energy conservative

70
Q

neurotransmitter of preganglionic neuron

A

ACh

71
Q

neurotransmitters of postganglionic neuron

A

ACh

NA

72
Q

ACh from preganglionic neuron binds to what receptor?

A

nicotinic ACh receptors

73
Q

NA from postganglionic neuron binds to what receptor?

A

g protein coupled adrenoceptors

74
Q

ACh from postganglionic neuron binds to what receptor?

A

muscarinic ACh receptor

75
Q

alternative sympathetic neurotransmitters

A

ATP

Neuropeptide Y

76
Q

alternative parasympathetic neurotransmitters

A

VIP

NO

77
Q

___ and ___ provide rapid relaxation

A

ACh and NO

78
Q

___ provides slow relaxation

A

VIP

79
Q

___ provides very fast contraction

A

ATP

80
Q

____ provides moderately fat contraction

A

NA

81
Q

____ provides slow contraction

A

neuropeptide Y

82
Q

muscarinic ACh are ligand gated/g protein and have ___ subtypes

A

g protein

5

83
Q

features of cholinergic transmission

A 
uptake 
synthesis of ACh
storage 
AP
release 
degradation and reuptake
84
Q

how many types of nicotinic ACh receptors are there

A

4

85
Q

the all or nothing AP response is caused by what ion

A

sodium

86
Q

M1 muscarinic ACh receptors

A

Gq
phospholipase C
increased acid secretion in stomach

87
Q

M2 muscarinic ACh receptors

A

Gi
inhibits adenylyl cyclase
decreased HR

88
Q

M3 muscarinic ACh receptors

A

Gq
Phospholipase C
contraction of smooth muscle in bronchioles

89
Q

features of noradrenergic trnasmission

A 
uptake 
synthesis 
storage 
AP 
release 
reuptake by U1 and U2
metabolism in cell my MAO and COMT
90
Q

B1 adrenoceptors

A

Gs - adenylyl cyclase to increase cardiac rate and force

91
Q

B2 adrenoceptors

A

Gs - adenylyl cyclase

relax bronchial and vascular smooth muscle

92
Q

A1 adrenoceptors

A

phospholipase C

Vascular smooth muscle contraction

93
Q

A2 adrenoceptors

A

inhibits adenylyl cyclase

inhibits NA release

94
Q

what do presynaptic autoreceptors do

A

mediate negative feedback inhibition of transmitter release

95
Q

what antiplatelet blocks production of thromboxane 2 to prevent binding to receptor

A

aspirin

96
Q

how do prasugrel and clopidogrel act as antiplatelet

A

block ADP binding

97
Q

why are anticoagulants indicated in AF patients

A

risk of stroke

98
Q

how does warfarin act as an anticoagulant

A

inhibits vitamin K - used to synthesise VII, X, IX, II

99
Q

how does heparin act as an anticoagulant

A

binds to antithrombin III to increase affinity for it for IIa and Xa

100
Q

TPA acts as fibrinolysis as it

A

increases conversion of plasminogen to plasmin

MB1: Principles (10 decks)

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