pharmacology Flashcards

1
Q

pharmacodynamics

A

biological effects of a drug and mechanism of action

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2
Q

pharmacokinetics

A

absorption, distribution, metabolism and excretion of a drug and its metabolites

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3
Q

affinity

A

the strength of association between ligand and receptor

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4
Q

efficacy

A

the ability of a drug to evoke a cellular response

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5
Q

efficacy of partial agonists compared to agonists

A

lower

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6
Q

competitive antagonist

A

binding of agonist and antagonist occurs at the same site, causes a right parallel shift on the curve

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7
Q

non competitive antagonist

A

agonist binds at the orthosteric site, antagonist binds to allosteric site, no activation when the antagonist is bough, depresses slope on curve

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8
Q

what is potency

A

drug concentration needed for given effect

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9
Q

factors affecting absorption

A

solubility, chemical stability, lipid to water partition coefficient (lipid solubility), degree of ionization (depends on pKa and pH at absorption site, physicochemical interactions, tablet form, GI motility

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10
Q

what is pKa

A

pH when 50% of the drug is ionised and 50% is unionised

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11
Q

what is EC50

A

agonist concentration that elicits a half maximal response

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12
Q

what does equipotent mean

A

working over the same concentration range

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13
Q

first order kinetics

A

elimination rate directly proportional to the drug conc, plasma conc falls exponentially

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14
Q

elimination rate in 1st order kinetics equation

A

elimination rate = plasma conc x Cl

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15
Q

what is steady state

A

rate of drug elimination = rate of drug administration

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16
Q

when is steady state reached

A

after approx 5 half lifes

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17
Q

relationsip required for iV to reach steady state

A

hyperbolic

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18
Q

oral bioavailabili

A

F, fraction of drug administered that enters systemic circulation

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19
Q

zero order saturation kinetics

A

initially eliminated at constamt rate - not proportional to concentration, when plasma concentration > Km of an enzyme that metabolites it it becomes first order

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20
Q

what is drug metabolism

A

m converting drugs into more polar/less active metabolites that arent reabsorbed by the renal tubure for excretio by the liver

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21
Q

what drugs gain activity from metabolism

A

codiene - morphine

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22
Q

what drug is unchanged by drug metabolism

A

diazepam - nordiazepam

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23
Q

phase 1 metabolism

A

makes a drug more polar and reactive

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24
Q

example of phase 1 reactions

A

oxidation, reduction, hydrolysis

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25
Q

what are cytochrome p450 CYP proteins

A

monooxygenases, haem proteins in hepatocytes

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26
Q

what do cytochrome p450 CYP proteins do

A

mediate oxidation reactions of lipid soluble drugs

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27
Q

what happens in phase 2 reactions

A

conjugation

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28
Q

what happens in conjugation

A

adds an endogenous compound, increasing polarity, occurs in the liver

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29
Q

example of a endogenous compound

A

glucuronyl, sulphate, methyl, acetyl group

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30
Q

what is glucuronidation

A

transfer of glucuronic acid ti electron rich atoms on substrate by UDP-glucuronyl transferase

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31
Q

drug excretion

A

by kidney, glomerular filtration, tubular secretion, drug leaves in urine

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32
Q

what state does the drug leave in

A

unchanged(charged) or more polar

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33
Q

glomeruar filtrtion

A

drugs bound to large plasma proteins in equilibrium in blood between unbound and protein bound form, only unbound can enter filtrate via glomerular filtration

34
Q

active tubular secteruon

A

capillaries -> proximal tubule - can secrete protein bound drugs

35
Q

examples of active tubular secretion transporters

A

OAT- acidic eg penicillin and OCT basic eg morphine

36
Q

factors influencing reabsorption

A

at distal tubule, lipid solubility, porality, urinary flow rate, urine pH (alkaline increased acid seretion acidic increases basic secretion

37
Q

efferent

A

away from cns

38
Q

afferent

A

towards cns

39
Q

ganglion

A

group of nerve cell bodies that house a synapse

40
Q

parasympathetic

A

long pre ganglionic, short post ganglionic

41
Q

parasympathetic pre ganglionic

A

cranium to sacrum - CN3,7,9,10 - ACh neurotransmitter, nicotinic receptor

42
Q

parasympathetic post ganglionic

A

Ach neurotransmitter, muscularinic recpetor

43
Q

functions of parasympathetic

A

decreased HR, increased GI motility, relaxes sphincters, erection, constricts bronchi, stimulates mucus production

44
Q

sympathetuc

A

short preganglionic, long post ganglionic

45
Q

preganglionic sympathetic

A

from thoracolumbar - ACh neurotransmitter, nicotinic receptor

46
Q

long post ganglionic

A

NA nuerotransmitter, activates G protein coupled adrenic

47
Q

functions of sympathetic nervous system

A

increases HR and force of contraction, reduces GU motility, constricts sphincters, vasoconstriction, relaxation of skeletal muscle, adrenaline release from adrenal gland, ejaculation relaxes ronchim decreases mucus production

48
Q

what causes release of transmitter

A

ca ++ induced via exocytosis

49
Q

ligand gated channels

A

seperate glycoprotein subunits

50
Q

what do ligand gated channels do

A

allows for rapid permuability in certain ions

51
Q

what are G protein coupled receptors

A

muscularinic Ach receptors and adrenic receptors

52
Q

extra and intracellular components of a g protein coupled receptor

A

extracellular NH2, intracellular COOH

53
Q

what is a G protein

A

peripheral protein with a,b,y subunit and GTP/GDP binding site

54
Q

mechanism of G protein protein coupled receptors

A

agonist actvates the receptor, GDP dissocaited from a subnit and GTP binds and monitors activity of effector

55
Q

turning off g protein signalling

A

a subunit is GTPase and hydrolysis GTP to GDP and pi and by sub units recombine

56
Q

what happens at cholinergic transmission

A

at a post synaptcu cell, choline uptake, ACh synthesis and storage, AP, Ca influx, ACh release, activator activation, ACH degradation to choline and acetate terminates transmission, choline reused

57
Q

pre ganglionic nicotinic cholinergic

A

central cation conducting ligand gated channel

58
Q

post ganglionic muscarinic cholinergic

A

activated by G protein receptors

59
Q

M1 g proetin

A

Gq

60
Q

M2 g protein

A

Gi

61
Q

M3 g protein

A

Gq

62
Q

use of M1

A

increased gastric acid secretion

63
Q

use of m2

A

decreased HR

64
Q

use of m3

A

increased salivary secretion and bronchial smooth musvlr contraction

65
Q

sympathetic nicotinic cholinergic

A

5 glycoprotein subunits form a central cation conducting channel, activated by ligand gated channels

66
Q

noradrenic transmission

A

adrenceptor activation, NA reuptake by transporters U1 and U2

67
Q

NA metabolism

A

monoamine oxidase MAO and cotechol-0-methyltransferase COMT

68
Q

beta 1 G protein

A

Gsgsg

69
Q

beta 2 g protein

A

gsf

70
Q

alpha 1 g protein

A

gq

71
Q

alpha 2 g protein

A

gi

72
Q

beta 1

A

increased HR and force

73
Q

beta 2

A

bronchial and vascular smooth muscle relaxation

74
Q

alpha 1

A

vascular smooth muscle contraction

75
Q

alpha 2

A

inhibits NA release

76
Q

cocaine effect on ANS

A

adrenoceptor stimualtiobm peripheral vasoconstriction (a1) and cardiac arrhtmias (b1)

77
Q

amphetamine effect on ANS

A

same as cocaine

78
Q

prazosin effect on ANS

A

selective competitive antagonist of a1 adrenoceptors, vasodilates (anti hypertensive)

79
Q

atenolol effect on ANS

A

seceletive competitive antagonits of b1 adrenoceptors

80
Q

atropine effect on ANS

A

competitive muscularinic ACh receptor antagonist