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PH 113 - Pharmacology 1 > PRELIM 03 - Pharmacodynamics > Flashcards

PRELIM 03 - Pharmacodynamics Flashcards

1
Q

Refers to the cellular macromolecule or macromolecular complex with which the drug interacts to elicit a cellular or systemic response

A

Receptor/Drug targets

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2
Q

Refers to the ability to bind to receptors

A

Affinity

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3
Q

Refers to the ability to activate receptors and generate a response

A

Efficacy/Intrinsic activity

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4
Q

Refers to the amount of drug needed to produce an effect; affected by both affinity and efficacy

A

Potency

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5
Q

Refers to the ability to distinguish between receptors

A

Specificity

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6
Q

Tissue response is proportional to number of receptors occupied; by Clark and Gadum (Theories of drug receptor interaction)

A

Occupancy theory

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7
Q

Retains the assumption that tissue response is proportional to number of receptors occupied; by Ariens and Stephenson (Theories of drug receptor interaction)

A

Modified occupancy theory

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8
Q

Drug receptor interaction effect is proportional to the rate of drug receptor combination; by Croxatto and Paton (Theories of drug receptor interaction)

A

Rate theory

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9
Q

According to the rate theory, __________ has a high rate of association and dissociation

A

Agonist

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10
Q

According to the rate theory, __________ has a high rate of association and low rate of dissociation

A

Antagonist

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11
Q

Combination of ligand and receptor produces a change in conformation of the receptor; by Koshland (Theories of drug receptor interaction)

A

Induced fit theory

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12
Q

Interaction of small molecules (drug) with macromolecule (receptor) results in SCP and NSCP; by Belleau (Theories of drug receptor interaction)

A

Macromolecular perturbation theory

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13
Q

According to the macromolecular perturbation theory, the _________ has an agonist effect

A

Specific conformational perturbation (SCP)

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14
Q

According to the macromolecular perturbation theory, the __________ has an antagonist effect

A

Nonspecific conformational perturbation (NSCP)

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15
Q

Proposes that when a ligand binds, this results in a change in receptor stage from inactive to active; by Black and Leff (Theories of drug receptor interaction)

A

Two-state receptor theory

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16
Q

Uses equilibrium dissociation constants for the interactions between the receptor and each ligand; by De lean et al. (Theories of drug receptor interaction)

A

Ternary complex model

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17
Q

According to the ternary complex model, the __________ factor denotes the mutual effect of the two ligands on each other’s affinity for the receptor

A

Cooperativity

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18
Q

__________ activity indicates the production of physiologic effect without the drug

A

Constitutive

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19
Q

2 receptor states (AI)

A

Active (Ra), Inactive (Ri)

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20
Q

Intrinsic activity is 1; Maximal shift to Ra (Characteristic of drug effect)

A

Agonist

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21
Q

Intrinsic activity is >0 and <1; Partial shift to Ra (Characteristic of drug effect)

A

Partial agonist

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22
Q

Intrinsic activity is 0; No effect on equilibrium (Characteristic of drug effect)

A

Antagonist

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23
Q

Intrinsic activity is <0; Shift to Ri (Characteristic of drug effect)

A

Inverse agonist

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24
Q

Prevents activation of receptor by agonist; may be competitive or noncompetitive (Types of antagonist)

A

Receptor antagonist

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25
Q

Opposes effects of agonist through a different receptor (Types of antagonist)

A

Physiologic antagonist

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26
Q

Renders a substance inactive by binding to it (Types of antagonist)

A

Chemical antagonist

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27
Q

Structurally similar to agonist, binds reversibly to the same site of agonist; can be overcome by increasing agonist concentration (Types of receptor antagonist)

A

Competitive antagonist

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28
Q

Cannot be overcome by increasing agonist concentration (Types of receptor antagonist)

A

Noncompetitive antagonist

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29
Q

Binds irreversibly (covalently) to the same site of agonist (Types of noncompetitive antagonist)

A

Irreversible antagonist

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30
Q

Binds to a different site (allosteric site) from the site of the agonist (Types of noncompetitive antagonist)

A

Allosteric inhibitor

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31
Q

Refers to the conversion of a signal carried by a chemical messenger into an intracellular response

A

Signal transduction

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32
Q

Channels that allow passive diffusion of ions down electrochemical gradients across the cell membrane

A

Ion channels

33
Q

Action potential across the cell membrane causes conformational change in the channel that opens or closes the gate (Types of ion channels)

A

Voltage-gated channels

34
Q

Binding of a chemical substance (a ligand) with the channel causes conformational in the channel that opens or closes the gate (Types of ion channels)

A

Ligand-gated channels

35
Q

3 components of G protein-coupled receptor (GEH)

A

G protein, Effector enzyme, Heptahelical receptor

36
Q

The largest and most diverse group of receptors

A

G protein-coupled receptor (GPCR)

37
Q

Meaning of G protein

A

Guanosine-nucleotide binding protein

38
Q

3 subunits of G protein (ABG)

A

Alpha (α), Beta (β), Gamma (γ)

39
Q

cAMP, DAG, IP3, and Ca2+ are all examples of __________

A

2° messengers

40
Q

Are enzymes that phosphorylates proteins

A

Receptor protein kinases

41
Q

Are enzymes that binds kinases which can phosphorylate proteins

A

Receptor bind protein kinases

42
Q

An example of receptor protein kinase that has intrinsic tyrosine kinase activity

A

Receptor tyrosine kinase

43
Q

Signal transducer protein of receptor tyrosine kinase

44
Q

__________ is a guanine nucleotide exchange factor (GEF) for Ras

A

Son of sevenless (SOS)

45
Q

SOS is a GEF for __________, a monomeric G protein located in the plasma membrane

46
Q

__________ is a serine protein kinase that is also called MAPKKK (Mitogen activated protein kinase kinase kinase)

47
Q

_________ is a factor that allows exchange of GDP for GTP; involved in activation

A

Guanine nucleotide exchange factor (GEF)

48
Q

________ are proteins that increase GTPase activity of G proteins or Ras; involved in inactivation

A

GTPase activating proteins (GAP)

49
Q

An example of receptor protein kinase that has intrinsic serine/threonine kinase activity

A

Receptor serine/threonine kinase

50
Q

Signal transducer protein of receptor serine/threonine kinase

51
Q

An example of receptor bind protein kinase that binds with JAK (Janus kinase), an example of tyrosine kinase

A

Cytokine receptor/JAK-STAT receptor

52
Q

Signal transducer protein of cytokine receptor/JAK-STAT receptor

A

Signal transducer and activator of transcription (STAT)

53
Q

A receptor enzyme that has intrinsic guanylyl cyclase activity

A

Receptor guanylyl cylase

54
Q

2 kinds of receptor guanylyl cyclase (MS)

A

Membrane-bound, Soluble

55
Q

2° messenger of receptor guanylyl cyclase

56
Q

Signal cascade of receptor guanylyl cyclase

57
Q

__________ receptors are used for hydrophobic drugs

A

Intracellular

58
Q

2 kinds of intracellular receptors (CN)

A

Cytosolic, Nuclear

59
Q

Signal cascade of intracellular receptors

A

Response element

60
Q

Refers to the ability of receptors to amplify signal duration and intensity

A

Signal amplification

61
Q

Response may be __________ or __________ (NG)

A

Non-genomic, Genomic

62
Q

E.g. ion influx/efflux, alteration of protein activity; is usually immediate and brief (Types of response)

A

Non-genomic

63
Q

E.g. gene expression; usually delayed and prolonged (Types of response)

64
Q

Refers to a decrease in response to a drug due to continued stimulation of receptors with agonists

A

Desensitization

65
Q

Refers to a rapid desensitization

A

Tachyphylaxis

66
Q

Happens due to endocytosis of receptors and sequestration inside cells

A

Downregulation

67
Q

A plot of the degree of a given response against the plasma concentration/dose of the drug

A

Graded-dose response curve

68
Q

A measure of the amount of drug necessary to produce an effect

69
Q

A measure of the ability of the drug to elicit a response when it interacts with a receptor; involves a drug’s maximum effect

70
Q

A plot of the proportion of the population that produces a response against the dose of the drug

A

Quantal-dose response curve

71
Q

__________ effect is also known as either-or effect

72
Q

The dose at which 50% of individuals exhibit the specified quantal therapeutic effect

A

Median effective dose (ED50)

73
Q

The dose at which 50% of individuals exhibit the specified quantal toxic effect

A

Median toxic dose (TD50)

74
Q

The dose at which 50% of individuals exhibit the specified quantal lethal effect

A

Median lethal dose (LD50)

75
Q

Refers to the range between the minimum therapeutic dose and the minimum toxic dose

A

Therapeutic window

76
Q

Refers to the ratio of the dose that produces toxic effect in half the population (TD50) to the dose that produces therapeutic effect (ED50) in half the population

A

Therapeutic index

77
Q

Refers to the ratio of the dose that produces toxic effect in 1% of the population (TD1) to the dose that produces therapeutic effect (ED99) in 99% of the population

A

Margin of safety

78
Q

__________ is an example of a drug that has a small therapeutic index

79
Q

__________ is an example of a drug that has a large therapeutic index

A

Penicillin

PH 113 - Pharmacology 1 (20 decks)

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