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[MT 6314] - 1st Shifting > QUIZLET Unit 2 - Drug Receptors and Pharmacodynamics (1) > Flashcards

QUIZLET Unit 2 - Drug Receptors and Pharmacodynamics (1) Flashcards

1
Q

Actions/effects of the drug on the body

A

Pharmacodynamics

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2
Q

Specific molecules in a biologic system with which drugs interact to produce changes in the function of the system.

A

Receptors

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3
Q

It is the fundamental event that initiates the action of the drug

A

Interaction between the drug and the receptor

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3
Q

It mediates the actions of both pharmacologic agonists and antagonists

A

Receptors

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4
Q

Specific binding region of the macromolecule.

A

Receptor site or Recognition site

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5
Q

Best characterized drug receptors

A

Regulatory proteins

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5
Q

Receptor that Mediates the action of endogenous chemical signals like neurotransmitters, autacoids, and hormones.

A

Regulatory proteins

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6
Q

Receptor thatInhibited (or less commonly, activated) by binding a drug

A

Enzymes

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7
Q

dihydrofolate reductase, the receptor for methotrexate are examples of this receptor

A

Enzymes

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8
Q

Na+ /K+ ATPase, the membrane receptor for digitalis are examples of this receptor

A

Transport Proteins

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9
Q

tubulin, the receptor for colchicine, an anti-inflammatory drug are the examples of this receptor

A

Structural Proteins

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10
Q

Molecules that translate the drug-receptor interaction into a change in cellular activity

A

Effectors

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11
Q

TRUE or FALSE: Some receptors are also effectors.

A

True

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12
Q

Transmembrane signaling mechanism in which the drug crosses the plasma membrane and acts on intracellular receptor

A

Lipid-soluble

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13
Q

Transmembrane signaling mechanism in which it regulates the opening of the ion channel (e.g. GABA, excitatory acetylcholine

A

Ligand-gated transmembrane ion channel

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14
Q

Transmembrane signaling mechanism in which it modulates production of an intracellular second messenger [e.g., catecholamine (epinephrine)].

A

Transmembrane receptor is coupled with an effector enzyme by G protein

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15
Q

G protein Receptor for β-Adrenergic amines, histamine, serotonin, glucagon, and many other hormones

A

Gs

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16
Q

G protein receptor for α2-Adrenergic amines, acetylcholine (muscarinic), opioids, serotonin, and many others

A

Gi1, Gi2, Gi3

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17
Q

G protein receptor for Odorants (olfactory epithelium)

A

Golf

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18
Q

G protein receptor for Neurotransmitters in brain (not yet specifically identified)

A

Go

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19
Q

G protein receptor for Acetylcholine (muscarinic), bombesin, serotonin (5-HT2), and many others

A

Gq

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20
Q

G protein receptor for Photons (rhodopsin and color opsins in retinal rod and cone cells)

A

Gt1, Gt2

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21
Q

Conservation of water by the kidneys mediated by

A

vasopressin

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21
Q

Mobilization of stored energy (breakdown of carbohydrates in the liver stimulated by

A

Catecholamines

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21
Q

Mediates hormonal responses

A

Cyclic Adenosine Monophosphate (cAMP)

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21
Q

Calcium homeostasis by

A

parathyroid hormone

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21
Q

Measure of drug efficacy

A

Emax

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21
Q

Few signaling roles in a few cell types like the intestinal mucosa and vascular smooth muscle cells

A

Cyclic Guanosine Monophosphate (cGMP)

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21
Q

Heart rate and contraction by

A

beta-adrenomimetic catecholamine

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21
Q

Bind to receptors linked to G proteins while others bind to receptor tyrosine kinases.

A

Calcium and Phosphoinositides

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21
Q

Causes relaxation of vascular smooth muscles by a kinase-mediated mechanism

A

cGMP

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21
Q

Maximal response that can be produced by a drug

A

Emax

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22
Q

Response of a particular receptor-effector system is measured against increasing concentration of a drug.

A

Graded Dose-Response Curve

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22
Q

TRUE or FALSE: The smaller the EC50, the greater the potency of the drug

A

True

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22
Q

Measure of drug potency

A

EC50

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22
Q

Half-maximal effective concentration

A

EC50

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23
Q

Concentration of drug that produces 50% of maximal effect

24
Q

TRUE or FALSE: Smaller concentration at EC50 = more potent

25
Q

total density or concentration of receptors

26
Q

refers to the Total number of receptor sites.

27
Q

Equilibrium dissociation constant

28
Q

Concentration of drug required to bind 50% of the receptors

29
Q

Measure of the affinity of a drug for its binding site on the receptor

30
Q

TRUE or FALSE: Smaller KD means greater affinity of drug to receptor

31
Q

what happens to the graph as more antagonist are added to the body?

A

It shifts to the right

32
Q

Transduction process between the occupancy of receptors and production of specific effect. Highly efficient coupling can be elicited by a full agonist and spare receptors

33
Q

Maximal drug response is obtained at less than maximal occupation of the receptors.

A

Spare receptors

34
Q

EC50=KD50

A

no spare receptors

35
Q

EC50<KD50

A

there are still more spare receptors

36
Q

EC50>KD50

A

All receptors are occupied before the EC50 is reached

37
Q

Non-regulatory molecules of the body

A

Inert Binding Sites

38
Q

It buffers the concentration of the drug

A

Inert Binding sites

39
Q

Binding with these molecules will result to no detectable change in the function of the biologic system.

A

Inert Binding sites

40
Q

Binds to the receptor and directly or indirectly bring about an effect.

41
Q

Agonists that Produces less than the full effect, even when it has saturated the receptors

A

Partial agonist

42
Q

Acts as an inhibitor in the presence of a full agonist.

A

Partial agonist

43
Q

a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.

A

Inverse agonist

44
Q

Binds but do not activate the receptors.

A

Antagonist

45
Q

Competes with agonist receptor.

A

Competitive Antagonist

46
Q

Binds to the receptor reversibly without activating the effector system.

A

Competitive antagonist

47
Q

Therapeutic implications produced by the competitive antagonist depends on the concentration of antagonist (e.g., propranolol)

A

Degree of inhibition

48
Q

Therapeutic implications where a competitive antagonist depends on the concentration of agonist that is competing for binding to the receptor.

A

Clinical Response

49
Q

Binds with the receptor via covalent bonds.

A

Irreversible Antagonist

50
Q

More dependent on the rate of turnover of receptors.

A

Irreversible antagonist

51
Q

Receptor is not available to bind the agonist.

A

Irreversible antagonist

52
Q

What happens to the concentration effect curve in an irreversible antagonist

A

moves downward

53
Q

Antagonist that Does not depend on interaction with the agonist’s receptor

A

Chemical Antagonist

54
Q

Drug that interacts directly with the drug being antagonized to remove it or to prevent it from reaching its target.

A

Chemical Antagonist

55
Q

Antagonist that Makes use of the regulatory pathway

A

Physiologic antagonist

56
Q

Antagonist where Effects that are less specific and less easy to control.

A

Physiologic Antagonist

57
Q

Response gradually diminishes even if the drug is still there (after reaching an initial high level of response).

A

Receptor desensitazation

58
Q

Graph of the fraction of a population that shows a specified response to increasing doses of a drug.

A

Quantal Dose-Response Curve

59
Q

ED50

A

Median effective dose

60
Q

TD50

A

Median toxic dose

61
Q

LD50

A

Median Lethal dose

62
Q

Ratio of the TD50 (or LD50) to the ED50 determined from the quantal dose-response curves

A

Therapeutic Index

63
Q

TRUE or FALSE: A therapeutic margin of 2-100 is preferrable than an index of 2-10

64
Q

Dosage range between the minimum effective therapeutic concentration or dose (MEC) and the minimum toxic concentration or dose (MTC).

A

Therapeutic Window

65
Q

Maximal effect an agonist can produce if the dose is taken to very high levels.

A

Maximal efficacy

66
Q

Amount of drug needed to produce a given effect

67
Q

Caused by differences in metabolism (genetic) or immunologic mechanisms

A

Idiosyncratic response

68
Q

Intensity of the drug is decreased; Large dose of the drug is needed to have an effect.

A

Hyporeactive Response

69
Q

Decreased sensitivity acquired as a result of exposure to the drug

70
Q

Intensity of the drug is increased or exaggerated

A

Hyperreactive response

71
Q

Tolerance develops after a few doses.

A

Tachyphylaxis

72
Q

decrease in number of receptors.

A

down-regulation

73
Q

increase in number of receptors.

A

up-regulation

74
Q

Drug has been taken for a long time, then abruptly discontinued.

A

Overshoot Phenomenon/Rebound Hypertension

75
Q

What to do to avoid/circumvent toxic effects?

A

o Give low doses

o Carefully monitor the patient

o Employ ancillary procedures

o Use a safer drug

[MT 6314] - 1st Shifting (23 decks)

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