pharmacology Flashcards

(80 cards)

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
what are cytochrome p450 CYP proteins
monooxygenases, haem proteins in hepatocytes
26
what do cytochrome p450 CYP proteins do
mediate oxidation reactions of lipid soluble drugs
27
what happens in phase 2 reactions
conjugation
28
what happens in conjugation
adds an endogenous compound, increasing polarity, occurs in the liver
29
example of a endogenous compound
glucuronyl, sulphate, methyl, acetyl group
30
what is glucuronidation
transfer of glucuronic acid ti electron rich atoms on substrate by UDP-glucuronyl transferase
31
drug excretion
by kidney, glomerular filtration, tubular secretion, drug leaves in urine
32
what state does the drug leave in
unchanged(charged) or more polar
33
glomeruar filtrtion
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
active tubular secteruon
capillaries -> proximal tubule - can secrete protein bound drugs
35
examples of active tubular secretion transporters
OAT- acidic eg penicillin and OCT basic eg morphine
36
factors influencing reabsorption
at distal tubule, lipid solubility, porality, urinary flow rate, urine pH (alkaline increased acid seretion acidic increases basic secretion
37
efferent
away from cns
38
afferent
towards cns
39
ganglion
group of nerve cell bodies that house a synapse
40
parasympathetic
long pre ganglionic, short post ganglionic
41
parasympathetic pre ganglionic
cranium to sacrum - CN3,7,9,10 - ACh neurotransmitter, nicotinic receptor
42
parasympathetic post ganglionic
Ach neurotransmitter, muscularinic recpetor
43
functions of parasympathetic
decreased HR, increased GI motility, relaxes sphincters, erection, constricts bronchi, stimulates mucus production
44
sympathetuc
short preganglionic, long post ganglionic
45
preganglionic sympathetic
from thoracolumbar - ACh neurotransmitter, nicotinic receptor
46
long post ganglionic
NA nuerotransmitter, activates G protein coupled adrenic
47
functions of sympathetic nervous system
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
what causes release of transmitter
ca ++ induced via exocytosis
49
ligand gated channels
seperate glycoprotein subunits
50
what do ligand gated channels do
allows for rapid permuability in certain ions
51
what are G protein coupled receptors
muscularinic Ach receptors and adrenic receptors
52
extra and intracellular components of a g protein coupled receptor
extracellular NH2, intracellular COOH
53
what is a G protein
peripheral protein with a,b,y subunit and GTP/GDP binding site
54
mechanism of G protein protein coupled receptors
agonist actvates the receptor, GDP dissocaited from a subnit and GTP binds and monitors activity of effector
55
turning off g protein signalling
a subunit is GTPase and hydrolysis GTP to GDP and pi and by sub units recombine
56
what happens at cholinergic transmission
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
pre ganglionic nicotinic cholinergic
central cation conducting ligand gated channel
58
post ganglionic muscarinic cholinergic
activated by G protein receptors
59
M1 g proetin
Gq
60
M2 g protein
Gi
61
M3 g protein
Gq
62
use of M1
increased gastric acid secretion
63
use of m2
decreased HR
64
use of m3
increased salivary secretion and bronchial smooth musvlr contraction
65
sympathetic nicotinic cholinergic
5 glycoprotein subunits form a central cation conducting channel, activated by ligand gated channels
66
noradrenic transmission
adrenceptor activation, NA reuptake by transporters U1 and U2
67
NA metabolism
monoamine oxidase MAO and cotechol-0-methyltransferase COMT
68
beta 1 G protein
Gsgsg
69
beta 2 g protein
gsf
70
alpha 1 g protein
gq
71
alpha 2 g protein
gi
72
beta 1
increased HR and force
73
beta 2
bronchial and vascular smooth muscle relaxation
74
alpha 1
vascular smooth muscle contraction
75
alpha 2
inhibits NA release
76
cocaine effect on ANS
adrenoceptor stimualtiobm peripheral vasoconstriction (a1) and cardiac arrhtmias (b1)
77
amphetamine effect on ANS
same as cocaine
78
prazosin effect on ANS
selective competitive antagonist of a1 adrenoceptors, vasodilates (anti hypertensive)
79
atenolol effect on ANS
seceletive competitive antagonits of b1 adrenoceptors
80
atropine effect on ANS
competitive muscularinic ACh receptor antagonist