Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

4 types of targets

A
  • receptors
  • ion channels
  • enzymes
  • carrier molecules/transporters
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Specificity

A

specific for that receptor (will key fit into lock)

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

Affinity

A

how well drug binds to receptor (will key turn)

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

intrinsic activity

A

magnitude of effect of drug once it is bound

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

competitive vs noncompetitive binding

A

reversible vs irreversible

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

Agonist

A

significant receptor affinity and full intrinsic activity- enhances physiological process

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

Full agonist

A

generates maximal response

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

Inverse agonist

A

generates response opposite of endogenous substance (stimulates receptor but gives opposite response)

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

Partial agonist

A

significant receptor affinity but only fractional intrinsic activity

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

agonist-antagonist

A

partial agonists that also have antagonist activity (when given with full agonist, it may decrease effect of full agonist)

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

Antagonist

A

significant receptor affinity but no intrinsic activity

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

potency and drug response curve

A

increased affinity of drug for receptor shifts curve to the left

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

slope of drug response curve

A

of receptors occupied for effect- steep slope= majority of receptors

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

efficacy and dose response curve

A

intrinsic ability to produce effect- higher plateau=greater efficacy

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

Drug response Equation

A

Drug + receptor = drug receptor complex = tissue response

DRC is usually constant but TR varies from person to person

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

C50

A

concentration associated with 50% of response

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

Timing and Potency

A

relative potency varies on time course of drug (peak effect fentanyl vs morphine)

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

ED50

A

effective dose in 50% of population (we use ED99)

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

TD50

A

toxic dose in 50% of population

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

LD50

A

lethal dose in 50% of population

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

Therapeutic Index

A

LD50/ED50

better TI for anesthesia is LD1/ED99

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

synergy

A

summing of simultaneous effects of 2+ drugs where combined effect is greater than effect of either drug when given alone (target different receptors)

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

additive

A

effect in which 2 substances/actions used in combination produce total effect same as sum of individual effects (target same receptors)

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

tachyphylaxis

A

rapid decrease in response to repeated doses over short period of time (ex- ephedrine)

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

desensitization

A

chronic loss of response over longer period of time or absolute loss of receptors (ex- beta adrenergic receptors)

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

tolerance

A

larger and larger doses required to produce same effect; altered sensitivity of receptors (ex- chronic opiate use)

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

Down regulation

A

continued stim. of cells; desensitize; receptors go down in number

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

up regulation

A

chronic administration of antagonist; make more receptors (beta blockers)

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

Sodium Ion Channels

A

activation of Na channels allows influx of Na into cell (positive/depolarization)

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

Local anesthetics

A

bind to Na channels in closed state (prevent Na influx)

Class 1 antiarrhythmics

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

CCBs

A

bind to receptors on voltage gated Ca ion channels- keeps them inactive/closed, prevents influx of Ca- slows down HR
Class IV antiarrhythmics

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

Class III antiarrhythmics

A

amiodarone, bretylium
block K ion channels- prolong depolarization
decrease portion of cardiac cycle where myocardial cells are excitable

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

Ligand Gated Ion channels

A

undergo conformational change after ligand binds to it extracellularly- opens pore in which ions travel down concentration gradient

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

GABA receptors in brain

A

ligand gated channel
inhibitory; anion (Cl) (GABAa)
when activated, neuron transmission is inhibited

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

Nicotinic receptors in brain

A

ligand gated channel

excitatory; cation (Na)

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

serotonin receptors in brain (5HT3)

A

ligand gated channel

excitatory, cation

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

glycine receptors in brain

A

ligand gated channel

inhibitory; anion

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

glutamate receptors in brain

A

ligand gated channel

excitatory

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

Anesthetic drugs that are agonist for GABA

A

benzos, barbituates, propofol, etomidate

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

How many subunits of 5 must ACh be bound to in nicotinic receptors to open?

A

2

41
Q

Opening of Nicotinic ACh receptor

A

allows Na and Ca to move in, K to move out

allows current flow to depolarize endplate

42
Q

Alpha 1 receptors

A

activation increases intracellular Ca, leading to muscle contraction
also inhibits insulin secretion and lipolysis

43
Q

Beta 1 receptors

A

located on postsynaptic membranes of heart
stimulation initiates kinase phosphorylation cascade through 2nd messenger system- increases intracellular Ca and increases troponin binding to Ca- +chorono, dromo, and inotropic effects

44
Q

Alpha 2 receptors

A

presynaptic nerve terminal
activation inhibits adenylate cyclase-decreasing entry of Ca
decreases release of NE, stimulation of postsynaptic receptors in CNS produces sedation and decreases SNS outflow

45
Q

Beta 2 receptors

A

postsynaptic on smooth muscle/glands
activates adenylate cyclase and 2nd messenger system- smooth muscle relaxation (bronchodilation, vasodilation, relaxation of uterus, bladder, gut; glycogenolysis, lipolysis, gluconeogenesis, insulin release)

46
Q

Muscarinic receptors

A

activates cholinergic receptors at postganglionic PNS junction of cardiac/smooth muscle
G protein coupled- 2nd messenger system

47
Q

nicotinic receptors

A

found at synaptic junctions of SNS and PNS ganglia

Ionotropic- affects Na flow

48
Q

M1 receptors

A

CNS, salivary glands, parietal cells

increases IP3/DAG -> CNS excitation, increased memory, locomotor activity, gastric acid secretion

49
Q

M2 receptors

A

heart

decreases cAMP -> decreased rate, force, AV conduction

50
Q

M3 receptors

A

smooth muscle, exocrine glands

increased IP3/DAG-> all smooth muscle contraction except: vasodilation, glandular secretion

51
Q

Non-depolarizers

A

antagonist to nicotinic receptors

channel remains closed, no ion flow

52
Q

Succinylcholine

A

agonist to nicotinic receptors
only 2 alpha subunit needed- opens channel
depolarizes but stays attached longer than ACh

53
Q

Zofran

A

5HT3 antagonist

54
Q

cyclic AMP

A 
intracellular 2nd messenger system
mobilizes stored energy
increased HR and force of contraction
relaxation of SMOOTH muscle
involved in nitric oxide pathway
55
Q

cyclic AMP effects

A

bronchodilation, prevents platelet aggregation, positive inotropic action in heart, antiglaucoma, reduces BP, reduces inflammation

56
Q

IP3

A

triggers release of Ca from storage vesicles

57
Q

Cardiac Signal Transduction- G protein

A

drugs stimulate Gs (increases cAMP) or Gi (inhibits cAMP) signals
affects influx of Ca and release from SR

58
Q

Cardiac Signal Transduction- IP3

A

increasing IP3 stimulates release of Ca from SR

59
Q

Vascular Signal Transduction- Gs proteins

A

increase in cAMP causes relaxation

60
Q

Vascular Signal Transduction- IP3

A

vascular smooth muscle contraction via protein phosphorylation

61
Q

Nitric Oxide

A

produced from amino acid L-arginine by enzymatic action of NOS
diffuses into vascular smooth muscle and binds to activate guanylyl cyclase (catalyzes dephosphorylation of GTP to cGMP)

62
Q

How does cGMP induce smooth muscle relaxation?

A
  • inhibits Ca entry into cell
  • activates K channels- hyperpolarization/relaxation
  • stimulates cGMP dependent protein kinase- activates myosin light chain phosphatase- leads to smooth muscle relaxation
63
Q

Vascular Effects of NO

A

vasodilation, antithrombotic effect, anti inflammatory effect, antiproliferative effect

64
Q

H1 receptors

A

stimulation causes hives, bronchoconstriction, motion sickness, separation of cell lining of vessels, and smooth muscle relaxation

65
Q

H2 receptors

A

found on parietal cells in stomach- mainly responsible for gastric acid levels

66
Q

Opioid Receptors (G protein)

A

inhibit adenyl cyclase, decrease conductance of Ca channels, open K channels, hyperpolarizes cells, decreases neuronal activity, suppress release of substance P

67
Q

Anticholinesterase Drugs

A

inhibit acetylcholinesterase- prevents breakdown of ACh (more ACH at NMJ)
edrophonium, neostigmine

68
Q

PDE inhibitors

A
  • milrinone, amrinone
  • competitive inhibitory action on PDE III isoenzyme
  • increased intracellular cAMP and cGMP, inward flow of Ca
  • positive inotropic and bronchial smooth muscle relaxation effect
69
Q

COX inhibitors

A

inhibit prostaglandin synthesis- NSAIDs, ASA, toradol

bad for renal insufficiency, asthma

70
Q

ACE inhibitors

A

prevents conversion of angiotensin I to II

captopril, enalapril

71
Q

lb to kg

A

1 kg = 2.2 lbs

72
Q

Calculating BMI

A

mass/height^2

73
Q

IBW

A

Female 105 lbs + 5 lbs(every in over 5’)

Male 106 lbs + 6 lbs (every in over 5’)

74
Q

Percentage of solution

A

move decimal place 1 to the right- how many mg/ml

75
Q

1:1000 and 1:200,000

A

1 mg/ml and 5 mcg/ml

76
Q

strongest to weakest bonds

A

covalent, ionic, hydrogen, van der waals

77
Q

isomers

A

same chemical formula but different structures

78
Q

stereoisomers

A

differ in spatial arrangements

enantiomeres- mirror images

79
Q

racemic mixtures

A

50/50 enantiomeres
each may have different effect, excretion, etc
thiopental, ketamine, bupivicaine, atracurium, etc

80
Q

hydrocarbons

A

all carbon atoms with H attached

81
Q

saturated hydrocarbons

A

all single bonded H

alkanes, hexanes

82
Q

unsaturated hydrocarbons

A

one or more double/triple bonds

alkenes (2), alkynes (3), benzene ring

83
Q

Amines

A

NH3
when 3 H ions, it is ammonia
metabolized by oxidation
rocuronium

84
Q

Alcohols

A

ROH

85
Q

Phenols

A

ROH where R is benzene ring

86
Q

Ethers

A

ROR
alkyl groups attached by oxygen
metabolized by hydroxylation
thioether, enflurane, isoflurane

87
Q

Carbonyl

A

C=O

88
Q

aldehydes

A

RCHO

89
Q

ketones

A

RCOR

90
Q

Carboxylic acids

A

RCOOH

91
Q

Esters

A

RCOOR
carbonyl attached to alkoxy
metabolized by hydrolysis
esmolol

92
Q

Amides

A

RCONH2
metabolism by hydrolysis and N oxidation
lidocaine

93
Q

Alkanes

A

usually contain only C/H
hydrophobic, lipophilic
metabolism usually by P450
halothane

94
Q

Alkenes

A

C/H atoms
contain at least 1 double bond (fixed)
metabolized by epoxide

95
Q

Alkyne

A

triple bond between 2 carbon atoms

metabolism not extensive (hard to break down)

96
Q

Aromatics

A

benzenes, phenyls, heterocyclics
metabolism similar to alkenes
double bond oxidized to epoxide
propofol

97
Q

Alcohols

A

contain hydroxyl group -OH
metabolized either by oxidation/conjugation
phenol- alcohol attached to benzene ring
albuterol

98
Q

Conjugate base

A

after acid donates proton

99
Q

conjugate acid

A

after base accepts proton

Pharm (5 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions