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Pharmacology 2100 > DRug receptors > Flashcards

DRug receptors Flashcards

1
Q

what is pharmacodynamic

A

what the drug does to the body

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2
Q

what is pharmacokinetics

A

what the body does to the drug

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3
Q

what is a ligand

A

substance that forms complex with receptors ex.drugs

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4
Q

what is a receptor

A

proteins that can bind to ligands

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5
Q

where can receptors be located

A

cell membrane
cytoplasm
nucleus

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6
Q

what does the receptor binding to the ligand do to post receptor signalling

A

activates or inactivates

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7
Q

what are the four receptor families

A

g protein coupled receptors
ion channels
enzyme linked receptors
intracellular receptors

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8
Q

what is the most common site of drug action

A

g protein coupled receptors

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9
Q

describe the structure of a receptor

A

single alpha helical peptide with seven transmembrane domains
extracellular domain contains the ligand binding area

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10
Q

describe the structure of a g protein

A

alpha subunit with diff forms

beta gamma subunit

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11
Q

what does the alpha subunit do

A

can bind to GDT and GTP

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12
Q

what does the BY subunit do

A

inhibits alpha subunit

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13
Q

how does the g protein function

A

occupied receptor changes shape and interacts with g protein which releases GDP and binds GTP. alpha subunit dissociates and activates adenylyl cyclase. hormone no longer present receptorconverts to resting state and GTP hydrolyzed to GDP

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14
Q

alpha subunits act on what? which on is inhibitory

A

adenylate cyclase

i is inhibitory

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15
Q

subunit q activates what

A

Phospholipase C

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16
Q

what are the second messengers activated by g proteins

A

camp
IP3
DAG
Ca

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17
Q

how do ligand channels work

A

ligand binding triggers confomational change in receptor and the channel opens

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18
Q

what is the ligand gated sodium channel

A

nicotinic acetylcholine

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19
Q

what is theligand gated calcium channel

A

NMDA

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20
Q

what is the ligand gated chloride channel

A

GABA

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21
Q

how are voltage gated channels different from ion gated

A

activated by changes in membrane ds potential not ligan

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22
Q

what is an ion pump

A

transmembrane protein that moves ions across pm against their concentration gradient

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23
Q

what is the cell membrane enzyme linked receptor

A

tyrosin kinase receptor

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24
Q

what is the structure of a tyrosin kinase receptor

A

spans the membrane in the form of dimers or multisubunit complexes

25
Q

how does the tyrosin kinase receptor function

A

ligand binds to receptor causing a conformational change forming dimers and converts kinases to active forms
induces receptor autophosphorylation

26
Q

what is an example of a intracellular enzyme lonked receptor

A

soluble guanylyl cyclase

27
Q

what is the structure of guanylyl cyclase

A

forms hterodimer with alpha and beta subunit
regulatory domain
coiled coil domain
cyclase domain

28
Q

how does guanylyl cyclase function

A

activated by nitroc oxide

activates second messenger cGMP

29
Q

what is the structure of a intracellular nuclear receptor

A

ligand binding part and DNA binding part

in nucleus

30
Q

how do nuclear receptors function

A

ligand diffuses into cell and interacts with the nuclear receptor then translocates to the nucleus
activated receptor binds to promoter region of gene resulting in gene expression

31
Q

what is bmax

A

maximal specific bindign of a ligand to receptor

32
Q

what is kd

A

concentration of drug where half maximal binding is observed

33
Q

describe affinity

A

how attracted the drug is to the receptor

34
Q

how does kd relate to affinity

A

as kd decreases the affinity increases

35
Q

describe selectivity

A

preference for one receptor over another

36
Q

what is e max

A

max effect induced by the drug

37
Q

ec50

A

concentration of the drug that produces an effect that is half the max

38
Q

describe potency

A

amount of drug needed to produce a given magnitude

39
Q

describe efficacy

A

ability of a drug to elicit a biological response by agonist, determined by emax

40
Q

what is an agonist

A

agent that can bind to a receptor and elicit a biologic response

41
Q

what is a full agonist

A

produces max response, mimics

42
Q

what is a partial agonist

A

activates receptor with a lower efficacy, will reduce effects of full agonist

43
Q

what is an inverse agonist

A

has a negative effect on the receptor

44
Q

what is an antagonist

A

drug combines wiht receptor but produces no response

45
Q

how do competitive antagonists work

A

compete with agonist by binding to the same site on the receptor, can be overcome by increasing concentration of agonist

46
Q

how do non competitve antagonists work

A

bond covalently or with such high affinity those receptors are unavailable to agonists

47
Q

how do allosteric antagonists work

A

bind to allosteric site which prevents receptor from activating even when agonist is attached

48
Q

define adverse effect

A

undesired harmful effect resukting from a medication

49
Q

what is TD50

A

drug dose that produces toxic effect in 50% of patients

50
Q

what is ED50

A

drug dose that produces therapeutic effect in 50% of patients

51
Q

how is ED50 and EC50 different

A

EC is to reach 50% of max biological response which ED is for 50% to reach therapeutic response

52
Q

how do you calculate the therapeutic index

A

TD50/ED50

53
Q

what does it mean if TI is high

A

there is a wide therapeutic window so it has high safetyy

54
Q

define idiosyncratic

A

individuals exhibit an unusual drug response

55
Q

define tachyphylaxis

A

acute rapid loss of response to a drug

56
Q

define tolerance

A

decreased response to a drug when the drug is taken repeatedly

57
Q

what is receptor desensitization

A

mechanism that reduces the receptor response to an agonist

58
Q

what are the four phases in drug development

A

1: small number, screen for safety
2: study efficacy
3: larger, safety and efficacy
4: large number post marketing studies

Pharmacology 2100 (13 decks)

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