Pharm 4 Flashcards

1
Q

Pharmacodynamics

A

action of the drug inside the body. deals with physiological/biochemical effects of drugs, their mechanism of action at macromolecular/subcellular/organsystem levels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

how do drugs work

A

modifying underlying biochemical/physicological process_..NOT de novo

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

physical properties of drugs

A

mass, adsorptive property, osmotic activty, radioactivty

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

how do laxatives work

A

draw water into lumen

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

mass examples

A

bulk laxatives –> bran,

methylcellulose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

adsorbtion

A

binding to a drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

adsorptive property examples

A

charcoal, kaolin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

osmotic activity examples

A

magnesium sulfate, mannitol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

example of a diuretic

A

mannitol draws water into the kidney to remove water

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

radioactivity example

A

iodine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

chemical properties

A

antacids like Al(OH)3,

Mg(OH)2 neutralize gastric HCL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

example of a drug acting on an enzyme

A

enalapril inhibits ACE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

example of drug acting on receptor

A

most durgs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

actions of drug receoptr interaction

A

molecular/conformational changes,
alteration of enzyme activity,
changes in permeability/transport processes,
cascade of changes leading to a response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

types of drug action

A

stimulation,
depression,
replacement,
cytotoxic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

stimulation

A

selective enhancement of the level of activity of specialized cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

epinephrine stimulates

A

heart

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

pilocarpine stimulates

A

salivary gland - PNS stimulant

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

depression

A

selective diminution of activity of specialized cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

barbiturates depress

A

cns reticular activating system and produce sleep

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

quinidine depresses

A

heart - antiarrithemic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

drugh that stimulates one cell and depresses another cell type

A

acetylcholine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

replacement examples

A

insuline in diabetes mellitus,

levodopa in parkinsonism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

cytotoxic effects examples

A

anticancer drugs produe cytotoxic actions against neoplastic cells,
antibiotics produce cytotoxic action against microbes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

most drugs act by

A

binding to receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

functions of receptors

A

propagation of signals from outside to inside,
amplify the signal,
adapt to short term and long term changes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

receptor families

A

channel linked/ligand gated,
g protein linked/coupled,
kinase linked,
intracellular receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

channel linked (ligand gated)

A

ionotropic,
selective ion channel Na, K, Ca, Cl,
drug binding results in opening or closing of chnnel,
fastest (milliseconds)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

g protein linked/coupled

A

metabotropic - cell membrane receptors linked through g proteins to effector mechanisms which include –adenylyl cyclase, phospholipase C,
channel regulation,
takes seconds to produce

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

kinase linked

A

(minutes) enzyme linked receptor,
phosphorylation of tyrosines .
Mst imp is to transport glucose receptors to surface

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

intracellular receptor

A

(hours) in cytosol or nucleus,
take longer time bc proteins need to be made,
eg steroids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

channel linked examples

A

nicotinic cholinergic receptors,

GABA a and NMDA receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

g protein examples

A

alpha and beta adrenergic receptors,

histamine receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

kinase linked examples

A

insuline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

intracellular receptor examples

A

steroids, tyroxine, vit-D

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

ligand gated ion channel example

A

cholinergic nicotinic receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

affinity

A

the bility of the drug to bind to the receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

intrinsic activity (IA)

A

ability of a drug to activate the receptor and produce the response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

agonist

A

drug which binds to the receptor, activates it and produces the response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

what has both affinity and intrinsic activity

A

agonist

41
Q

examples of agonists

A

morphine, epinephrine, acetylcholine

42
Q

antagonist

A

binds to the receptor but will not activate the receptor

43
Q

what has affinity but no intrinsic activity

A

antagonist

44
Q

examples of antagonists

A

prazosin (alpha rec), atenolol (beta rec), atropine (muscarinic rec)

45
Q

partial agonist

A

it will activate the receptor but produce submaximal response (however, antagonizes the action of a full agonist)

46
Q

example of a partial agonist

A

pentazocine –partial agonist at opioid receptor

47
Q

what agonist will produce unsurmountable antagonism

A

noncompetitive binding at an alosteric site

48
Q

inverse agonist

A

activates the receptors to produce an effect in the opposite direction to that of agonist

49
Q

example of inverse agonist

A

beta carbolines produce the effects opposite to diazepam

50
Q

affinity + IA (1)

A

agonist

51
Q

affinity + IA (0)

A

antagonist

52
Q

affinity + IA (0 to 1)

A

partial agonist

53
Q

affinity + IA (0 to -1)

A

inverse agonist

54
Q

drug potency

A

the amount of drug needed to produce the response (lower the doe required, higher will be the potency and vice versa)

55
Q

drug efficacy

A

the maximum response of the drug (more important)

56
Q

the position of the dose response curve on the dose axis is an index of

A

drug potency

57
Q

the upper limit of the drug response curve is an index of

A

efficacy of the drug

58
Q

steep slope in the DRC indicates

A

small increase in does markedly increases the response

59
Q

the steepest part of the DRC is witing

A

25-75% of drug dose (30-70% is said to be linear)

60
Q

types of dose response relationships

A

graded dose response, quantal(all or none) dose response

61
Q

graded dose response

A

gradual increase in concentration and thereby response in one individual, animal, or tissue but only to a limit

62
Q

ceiling effect

A

seen when further increase in dose does not exhibit the increase in response which occurs at a ceiling dose. Denotes all receptors are occupied.

63
Q

shape of graded dose response relationship

A

hyperbolic curve plotting dose, sigmoid if plotting log dose

64
Q

graded dose response relationship is significan in

A

studying the effect of drug on single tissue or animal,
determining the potency and efficacy of drugs,
studying the comparison between agonists and antagonists

65
Q

quantal (all or none) dose response

A

studies the influence of the magnitude of the dose on the proportion of a population that response;
shows if the determined response is seen with a given dose or not at all

66
Q

is quantal dose response a continuous relationship

A

no

67
Q

quantal dose response is significant in determining

A

median effective dos (ED50) median lethal does (LD50) and therapeutic index (TI)

68
Q

therapeutic index formula

A

TI = LD50/ED50

69
Q

the gap btw the therapeutic and adverse DRC indicates

A

safety margin of the drug or therapeutic index

70
Q

the higher the therapuetic index

A

the better bc a small increase won’t lead to toxicity

71
Q

combined effects of drugs

A

synergism and antactonism

72
Q

interaction of drugs can occure on a

A

parmacokinetic level or pharmacodynamic level

73
Q

synergism

A

when the action of one drug is faciitated or inreased by the other

74
Q

types of synergism

A

additive and supraadditive (potentiation)

75
Q

does a synergistic drug have to produce an effect if given alone

A

no

76
Q

additive synergism

A

effect of (A + B) = effect of A + effect of B

77
Q

additive synergism: asprine + acetaminophen

A

an analgesic/antipyretic

78
Q

additive synergism: nitrous oxide + ether

A

general anesthetic

79
Q

additive synergism:ephedrien + theophylline

A

bonchodialator

80
Q

supraadditive (potentiation) synergism

A
when 2 or more drugs are given together the effecto of combination is greater than the individual effects of the comonents : 
effect of (A + B) > effect of A + effect of B
81
Q

supraadditive (potentiation) synergism: acetylcholine + physostigmeine

A

physostigmine prevents the breakdown of acetylcholine

82
Q

supraadditive (potentiation) synergism: levodopa + carbidopa

A

carbidopa is a dopacecarboxylase inhibitor–>less levodopa metabolism/ dopamine prodicued in the periphery, more for CNS

83
Q

supraadditive (potentiation) synergism: sulfamethoxazole + trimethoprim

A

sulfamethoxazole blcks folate synthase and trimethoprim blocks folate reductase. Individually they are bacteriostatic but together they are bacteriocidal (cotrimoxazoles). Sequential blockade/folate inhibition

84
Q

antagonism

A
when one drug decreases or inhibits the action of another:
effect of (A + B) < effect of A + effect of B
85
Q

types of antagonism

A

physico-chemical, physiological/functional, receptor/pharmacological

86
Q

physicochemical antagonsim

A

two drugs that react chemicallly and form an inactive product

87
Q

Physico-chemical example

A

EDTA (anticoagulant and metal chelator) complex with heavy metals

88
Q

physiological/functional antagonism

A

tow drugs actig through different receptors or mechanisms produce opposite effects

89
Q

physiological/functional antagonsim example

A

histamine and epinephrine on bronchial tissue (epi will reduce bronchoconstriction but they act on their own receptors), insuline and glucagon on blood glucose levels

90
Q

receptor/pharmacological antagonism

A

two drugs action through the same receptors or mechanisms produce opposite effects or one prevents another from producing pharmacological effects

91
Q

receptor/pharmacological antagonism example

A

beta blockers occupy beta receptors and preent epinephrine from binding and producing effects–stimulation of the heart is decreased

92
Q

types of receptor/pharmacological antagonsim

A

competitive/equilibrium/reversible type, noncompetitive/nonequilibrium/permanent type

93
Q

receptor - comp vs noncomp

A

same rec vs different allosteric site

94
Q

compared to agonist - comp vs noncomp

A

resembles agonist vs does not resemble agonist

95
Q

DRC - comp vs non comp

A

parallel rightward shift vs flattening

96
Q

effect - comp vs noncomp

A

reduces affinity/potency by inactivating agonist molecules vs reduce intrinsic activity by inactivating receptors

97
Q

intensity of response - comp vs noncomp

A

depends on concentration of both agonist and antagonist vs depends only on the concentration of the antagonist

98
Q

competitive antagonist examples

A

Ach - atropine,
morphine - naloxone,
prazosin - epinephrine

99
Q

noncompetitive antagonist

A

diazepam–bicuculline,

phenoxybenzamine (irreversible alpha 1 blocker) and epinephrine