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Pharmacology > Pharmacodynamics > Flashcards

Pharmacodynamics Flashcards

1
Q

What is delineated under pharmacodynamics?

A

Drug receptors Dose-response curves MOA

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2
Q

What is the difference between a hyperbolic and sigmoidal dose-response curve?

A

Hyperbolic when drug dose vs response Sigmoidal when log of drug dose vs response

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3
Q

What is ED50

A

dose of drug that produces 50% maximal effect

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4
Q

What is Emax

A

maximal drug effect

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5
Q

What is a graded response?

A

Magnitude of response of population mean or single person –> “how much”

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6
Q

What is a quantal response?

A

frequency of individuals responding to a pre-defined variable

–> does a response occur, in how many yes or no, binary responses

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7
Q

Describe cumulative vs noncumulative quantal dose-response graphs

A

Cumulative: resposne of individuals to the dose and all doses lower than it

Noncumulative: response of individuals to only one dose

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8
Q

What are ED50, TD50 and LD50 in a cumulative quantal dose-response graph?

A

ED50: median effective dose

TD50: median toxic dose

LD50: median lethal dose

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9
Q

What is the equation for a therapuetic index?

A

TD50/ ED50

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10
Q

The higher the TI, the …

A

safer the drug

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11
Q

What is the therapeutic window?

A

range of doses that provides safe and effective therapy

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12
Q

Is it better for a drug to have a narrow or high therapeutic window?

A

High–> more space between therapeutic effect and adverse reaction

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13
Q

What is potency?

A

amount of drug required to produce specific pharm effect

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14
Q

What represents potency?

A

ED50

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15
Q

The lower the ED50, the…

A

more potent the drug

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16
Q

What is efficacy?

A

maximal pharm effect that a drug can produce

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17
Q

What represents efficacy?

A

Emax

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18
Q

The greater the Emax, …..

A

the more efficacious the drug

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19
Q

What relates the total number of receptors available to bind a drug?

A

efficacy

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20
Q

What kind of bonds do most drugs bind?

A

non-covalent

Reversible (ionic, hydrogen, hydrophobic)

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21
Q

Why aren’t covalent bonds used with most drugs?

A

since irreversible bonds, must resynthesize receptor or remove drug via enzyme

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22
Q

Describe relationship of Kd to affinity

A

inverse

low Kd, high affinity

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23
Q

Describe affinity in terms of drug dose

A

inverse

high affinity, low drug dose required

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24
Q

What affinity requires more drug due to poor receptor-drug interaction?

A

low affinity

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25
Q

What is the relationship of Bmax to Emax?

A

Bmax is maximal binding on a drug-receptor curve

Emax is maximal effect of drug on dose-response curve

BOTH look the same on graph–> Kd=EC50 on x axis

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26
Q

What is the difference between Kd and EC50?

A

same thing–> Kd used on drug-receptor graph, EC50 used on dose-response graph

27
Q

What is the relationship of Kd to selectivity?

A

higher Kd, lower affinity, more selective, affects fewer targets, fewer adverse effects

28
Q

Do agonists or antagonists have intrinsic activity?

A

Agonists ONLY

29
Q

What is intrinsic activity?

A

ability of drug to change receptor function and produce physiological response on binding

30
Q

Do antagonists change receptor function?

A

NO, no intrinsic activity to prevent agonist from binding instead

31
Q

What types of agonists exist?

A

Full

Partial

Inverse

32
Q

Describe full agonists

A

fully activate receptors

produce maximal effect when all receptors occupied

maximal intrinsic activity

33
Q

What is a main difference between full and partial agonists?

A

intrinsic activity

34
Q

Describe partial agonists

A

partially activate receptor on binding

produce sub-maximal effect when all receptors occupied

intrinsic efficacy varied (always sub-maximal)

35
Q

Describe inverse agonists

A

decrease receptor signaling

decrease response at receptors

intrinsic activity present and related to inhibition of receptor function

opposite of full and partial agonist

36
Q

What types of antagonists exist?

A

pharmacologic

chemical

physiologic

37
Q

Describe pharmacologic (receptor) antagonism

A

act as same receptor as endogenous ligand or agonists

38
Q

Describe chemical antagonism

A

makes another drug unavailable

DOESN’T interact with receptor

39
Q

Describe physiologic antagonism

A

1 pathway antagonizes another pathway with different receptors

40
Q

What types of pharmacologic antagonists exist?

A

Competitive and Non-competitive

41
Q

Can competitive antgonist be displaced?

A

yes if enough drug is there

42
Q

What are the types of non-competitive antagonists

A

Irreversible

Allosteric

43
Q

Why are irreversible antagonists irreversible

A

they form covalent bonds over binding site

44
Q

Action of allosteric antagonist

A

bind to site other than agonist binding site–> prevent or reduce binding OR prevent activation of receptor

45
Q

EC50 increases

Emax does not change

A

competitive antagonist

46
Q

Emax decreases

EC50 does not change

A

noncompetitive antagonist

47
Q

Which antagonist is this

A

competitive antagonist

48
Q

Which antagonist is this

A

Noncompetitive

49
Q

What is the function of a full agonist

A

mimiks action of endogenous chemicals at receptors

50
Q

What drugs can block actions of endogenous ligands at receptors?

A

antagonists

partial agonist

inverse agonist

51
Q

What are drugs designed to target

A

important regulatory proteins in signaling pathways

52
Q

What part of the G-protein receptor has GTPase activity

A

alpha subunit

53
Q

What does Gs activate

A

adenylyl cyclase–> AC activation

54
Q

What does Gi activate

A

adenylyl cyclases–> AC INHIBITION

55
Q

What does Gq activate

A

phospholipase C–> PLC activation

56
Q

What does G 12/13 activate

A

Rho GTPases–> cytoskeletal rearrangements

57
Q

What downregulates G-protein receptors

A

beta-arrestin

G-protein coupled receptor kinase

protein phosphatase

58
Q

What trigger JAK receptors

A

growth hormone

erythropoietin

leptin

INF-2, 10, 15

59
Q

Why are receptor tyrosine kinases target for cancer drugs?

A

oncogenes in growth factor pathways

point mutation sites in cancer

anticancer drugs inhibit upregulated GF signaling

60
Q

Point mutations in Ras cause what cancer

A

pancreatic adenocarcinoma

61
Q

Point mutations in Raf cause what cancer

A

melanoma

62
Q

Where are nuclear receptors

A

cytoplasm

63
Q

What activate nuclear receptors

A

lipophilic so can cross into cytoplasm and activate receptor

steroid and thyroid hormones

vitamins D and A

lipid mediators

64
Q

Why is L-type calcium channel a drug target?

A

everywhere, can cause arrhythmias, angina, HTN, constipation

Pharmacology (6 decks)

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