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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

pharmacology

A

study of drugs that interact with living beings through chemical processes

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2
Q

pharmacodynamics

A

drugs acting on body

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3
Q

pharmacokinetics

A

body acting on drug (metabolism)

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4
Q

receptors

A

interacts with drug and initiates the biochemical events leading to effects

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5
Q

physiological receptor

A

receptor for something naturally made in body (muscarinic, adrenergic)

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6
Q

agonists

A

activate receptor

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7
Q

antagonists

A

block endogenous ligand

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8
Q

negative or positive allosteric modulator

A

endogenous ligand to be weaker / stronger (bind somewhere else besides active site)

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9
Q

generalized receptors

A

not normally a receptor, drug binds to it and alters function (voltage-gated Na+ channels)

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10
Q

how do drugs bind to receptors?

A

hydrogen bonds

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11
Q

what can be drugs

A

anything that produces a physiological effect (most small molecules)

large amount of drugs deviate (biologics)

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12
Q

ligand gated ion channels

A

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

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13
Q

G-protein coupled receptors

A

activates G protein with activate secondary messenger (cAMP) cascades

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14
Q

enzyme-linked (receptor tyrosine kinase)

A

activates signaling cascades through phosphorylation of substrates

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15
Q

nuclear receptor

A

steroid hormone are lipid soluble - allows to enter cell through lipid bilayer

activates or inhibits gene expression after binds to response elements

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16
Q

other receptors

A

no endogenous molecule acts on them, but affected by drugs

ex. proton pump, voltage gated ion channels, enzymes

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17
Q

physical properties of drug and structure determine (3 things)

A

binding
selectivity
affinity

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18
Q

selectivity

A

1 or many receptors

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19
Q

NOT ideal conditions of selectivity

A

bind to same receptor in multiple organs

bind to different receptors, especially when drug concentration in creases (more undesirable side effects)

20
Q

when are drugs more specific?

A

at low concentrations

21
Q

affinity

A

how readily and tightly does it bind

22
Q

high affinitiy

A

good drug receptor interaction, less drug needed to produce a response

23
Q

low affinity

A

poor drug receptor interaction, more drug needed to produce a response

24
Q

affinity is measured through

A

equilibrium dissociation constant (Kd)

25
Q

equilibrium dissociation constant

A

drug concentration for which 50% of that receptor is bound by the drug

26
Q

lower Kd

A

higher affinity

27
Q

higher Kd

A

lower affinity

28
Q

law of mass action

A

drug effects are reversible interactions - can tilt equilibrium

29
Q

when drug receptor complex is activated

A

conformational change

30
Q

potency

A

how much drug needed to produce certain effect

31
Q

efficacy

A

how big is the effect

32
Q

quantal dose response

A

yes or no situation

33
Q

therapeutic index

A

want high, so likelihood of toxicity is not reachable

34
Q

margin of safety

A

the higher the TI of MOS, the safer the drug

35
Q

antagonists

A

bind to receptor but don’t cause conformational change or biological response

36
Q

competitive antagonist

A

more drug necessary to achieve effect (surmountable)

-compete for active site but doesn’t activate it
-decrease in potency but no decrease in efficacy

37
Q

noncompetitive antagonist

A

antagonist that bind covalently (insurmountable)

-irreversibly bind to allosteroic site on receptor to prevent activation of receptor
-decrease in efficacy

38
Q

partial agonist

A

can’t achieve 100%
decrease effects of full agonist when given together

39
Q

inverse agonists

A

promotes inactive conformation - produce opposite effects of regular agonists

40
Q

allosteric modulators

A

bind to secondary, allosteric site to + or - regulate agonist binding / efficacy

41
Q

orthosteric drugs

A

bind to primary agonist site on receptor (no effect on signalling)

42
Q

tachyphylaxis

A

decrease response when same does is given repeatbly

43
Q

desensitization

A

receptor phosphorylated and binds B-arrestin

44
Q

inactivation

A

receptor removed from membrane (reversible)

membrane forms endosome so receptor is embedded in it can lead to degradation

45
Q

pharmacodynamic tolerance

A

chronic exposure to agonist can cause decrease in receptor number due to degradation of receptor or decrease in gene expression

46
Q

upregulation

A

greater receptor number

47
Q

REVIEW GRAPHS!!!

A

Pharmacology (6 decks)

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