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Pharmacology Exam 1 > Lecture 1: Pharmacodynamics > Flashcards

Lecture 1: Pharmacodynamics Flashcards

1
Q

actions of a drug on the body

A

pharmacodynamics

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2
Q

actions of the body on a drug

A

pharmacokinetics

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3
Q

normal function is to be a receptor for something naturally produced in the body

A

physiological receptor

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4
Q

a protein that isn’t normally a receptor, but a drug binds to it and alters its function

A

generalized receptor

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5
Q

what types of molecules can be drugs?

A

any chemical that interacts with a system to produce a physiological effect

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6
Q

what are “biologicals”

A

peptides/proteins/antibodies

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7
Q

the component of a cell or organism that interacts with a drug and initiates the biochemical events leading to its effects

A

receptor

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8
Q

most common way drugs bind receptor

A

hydrogen bonds

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9
Q

agonist

A

activate the receptor

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10
Q

antagonist

A

block the endogenous ligand

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11
Q

negative or posiitve allosteric modulator

A

cause the endogenous ligand to be weaker or stronger

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12
Q

channel opens (allow ions to pass) when a signaling molecule binds

A

ligand-gated ion channels

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13
Q

activates G proteins which activate second messenger cascades

A

G-protein coupled receptors

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14
Q

activates signaling cascades through phosphorylation of substrates

A

receptor tyrosine kinase

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15
Q

activates or inhibits gene expression

A

nuclear

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16
Q

GPCR, RTK, and LGIC are located where

A

cell membrane m

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17
Q

where are nuclear receptors located

A

cytosol

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18
Q

the physical properties of a drug and structure of a receptor determines:

A
  • binding
  • selectivity
  • affinity
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19
Q

drug-receptor binding equation (agonist)

A

D + R <-> DR <-> DR* ->-> response

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20
Q

ideal drug would function specifically on

A

desired organ system and receptor

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21
Q

most drugs either: (selectivity)

A
  • bind to the same receptors, but in multiple organs or
  • bind to different receptors, especially as drug concentration increases
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22
Q

the _ of a drug for a receptor described how readily and tightly that drug binds to the receptor

A

affinity

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23
Q

the lower the Kd, the _ the affinity for a receptor

A

higher

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24
Q

the higher the Kd, the _ the affinity of a drug for a receptor

A

lower

25
Q

high affinity =

A

good drug-receptor interaction; LESS drug needed to produce a response

26
Q

low affinity =

A

poor drug receptor interaction; MORE drug needed to produce a response

27
Q

Equilibrium dissociation constant

A

Kd

28
Q

X axis on ligand-receptor binding curves

A

concentration of drug (ligand)

29
Q

Y axis of ligand-receptor binding curves

A

fraction of receptors occupied by drug

30
Q

LR

A

ligand-receptor complexes

31
Q

R0:

A

total receptors

32
Q

Kd

A

concentration where half of receptors are occupied

33
Q

EC50 or ED50

A

concentration or dose needed to reach 50% of max effect

34
Q

Emax

A

maximal effect produced by the drug

35
Q

potency

A

how much of a drug is needed to produce a certain level of effect?
* EC50 commonly used

36
Q

efficacy

A

how big is the effect

37
Q

EC50 < Kd when

A

there are spare receptors

38
Q

how can maximal effect be achieved with less than 100% of the receptors occupied?

A

signal amplification by second messenger pathways

39
Q

ED50

A

median effective dose

40
Q

TD50

A

median toxic dose

41
Q

LD50

A

median lethal dose

42
Q

therapeutic index equation

A

(TD50 OR LD50) / ED50

43
Q

margin of safety

A

(LD1 or TD1) / ED99

44
Q

The higher the TI of MOS, the _ the drug

A

safer

45
Q

competitive antagonist

A

more drug necessary to achieve effect

46
Q

competitive antagonist are surmountable or insurmountable

A

surmountable

47
Q

noncompetitive antagonist

A

bind covalently

48
Q

noncompetitive antagonists are surmountable or insurmountable

A

insurmountable

49
Q

partial agonist

A

not able to achieve 100% effect

50
Q

buprenorphine

A

partial agonist, most potent but less efficacious

51
Q

inverse agonist

A

promote the inactive (R) conformation and therefore eliminate baseline/constitutuve signaling thereby producing effects opposite those regular agonists

52
Q

orthosteric drugs

A

binds to the primary agonist site on a receptor

53
Q

allosteric modulators

A

bind to a secondary, allosteric site to positively or negatively regulate agonist binding or efficacy

54
Q

tachyphylaxis

A

decreased response when same dose is given multiple times

55
Q

desensitization

A

receptor is phosphorylated and binds beta-arrestin

56
Q

inactivation

A

receptor removed from membrane

57
Q

upregulation

A

chronic antagonist exposure can cause this, greater receptor number

58
Q

up/down regulation depend on _ and _ (longest time frame compared to other mechanisms

A

internalization, transcription

59
Q

receptor drug binding equation (antagonist)

A

D + R<-> DR <-x-> DR* ->-> response

Pharmacology Exam 1 (15 decks)

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