QUIZLET Unit 2 - Drug Receptors and Pharmacodynamics (1)

Question 1

Actions/effects of the drug on the body

Answer 1

Pharmacodynamics

Question 2

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

Answer 2

Receptors

Question 3

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

Answer 3

Interaction between the drug and the receptor

Question 3

It mediates the actions of both pharmacologic agonists and antagonists

Answer 3

Receptors

Question 4

Specific binding region of the macromolecule.

Answer 4

Receptor site or Recognition site

Question 5

Best characterized drug receptors

Answer 5

Regulatory proteins

Question 5

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

Answer 5

Regulatory proteins

Question 6

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

Answer 6

Enzymes

Question 7

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

Answer 7

Enzymes

Question 8

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

Answer 8

Transport Proteins

Question 9

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

Answer 9

Structural Proteins

Question 10

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

Answer 10

Effectors

Question 11

TRUE or FALSE: Some receptors are also effectors.

Answer 11

True

Question 12

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

Answer 12

Lipid-soluble

Question 13

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

Answer 13

Ligand-gated transmembrane ion channel

Question 14

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

Answer 14

Transmembrane receptor is coupled with an effector enzyme by G protein

Question 15

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

Answer 15

Gs

Question 16

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

Answer 16

Gi1, Gi2, Gi3

Question 17

G protein receptor for Odorants (olfactory epithelium)

Answer 17

Golf

Question 18

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

Answer 18

Go

Question 19

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

Answer 19

Gq

Question 20

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

Answer 20

Gt1, Gt2

Question 21

Conservation of water by the kidneys mediated by

Answer 21

vasopressin

Question 21

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

Answer 21

Catecholamines

Question 21

Mediates hormonal responses

Answer 21

Cyclic Adenosine Monophosphate (cAMP)

Question 21

Calcium homeostasis by

Answer 21

parathyroid hormone

Question 21

Measure of drug efficacy

Answer 21

Emax

Question 21

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

Answer 21

Cyclic Guanosine Monophosphate (cGMP)

Question 21

Heart rate and contraction by

Answer 21

beta-adrenomimetic catecholamine

Question 21

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

Answer 21

Calcium and Phosphoinositides

Question 21

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

Answer 21

cGMP

Question 21

Maximal response that can be produced by a drug

Answer 21

Emax

Question 22

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

Answer 22

Graded Dose-Response Curve

Question 22

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

Answer 22

True

Question 22

Measure of drug potency

Answer 22

EC50

Question 22

Half-maximal effective concentration

Answer 22

EC50

Question 23

Concentration of drug that produces 50% of maximal effect

Answer 23

EC50

Question 24

TRUE or FALSE: Smaller concentration at EC50 = more potent

Answer 24

True

Question 25

total density or concentration of receptors

Answer 25

Bmax

Question 26

refers to the Total number of receptor sites.

Answer 26

Bmax

Question 27

Equilibrium dissociation constant

Answer 27

KD

Question 28

Concentration of drug required to bind 50% of the receptors

Answer 28

KD

Question 29

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

Answer 29

KD

Question 30

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

Answer 30

True

Question 31

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

Answer 31

It shifts to the right

Question 32

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

Answer 32

Coupling

Question 33

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

Answer 33

Spare receptors

Question 34

EC50=KD50

Answer 34

no spare receptors

Question 35

EC50

Answer 35

there are still more spare receptors

Question 36

EC50>KD50

Answer 36

All receptors are occupied before the EC50 is reached

Question 37

Non-regulatory molecules of the body

Answer 37

Inert Binding Sites

Question 38

It buffers the concentration of the drug

Answer 38

Inert Binding sites

Question 39

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

Answer 39

Inert Binding sites

Question 40

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

Answer 40

Agonist

Question 41

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

Answer 41

Partial agonist

Question 42

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

Answer 42

Partial agonist

Question 43

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

Answer 43

Inverse agonist

Question 44

Binds but do not activate the receptors.

Answer 44

Antagonist

Question 45

Competes with agonist receptor.

Answer 45

Competitive Antagonist

Question 46

Binds to the receptor reversibly without activating the effector system.

Answer 46

Competitive antagonist

Question 47

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

Answer 47

Degree of inhibition

Question 48

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

Answer 48

Clinical Response

Question 49

Binds with the receptor via covalent bonds.

Answer 49

Irreversible Antagonist

Question 50

More dependent on the rate of turnover of receptors.

Answer 50

Irreversible antagonist

Question 51

Receptor is not available to bind the agonist.

Answer 51

Irreversible antagonist

Question 52

What happens to the concentration effect curve in an irreversible antagonist

Answer 52

moves downward

Question 53

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

Answer 53

Chemical Antagonist

Question 54

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

Answer 54

Chemical Antagonist

Question 55

Antagonist that Makes use of the regulatory pathway

Answer 55

Physiologic antagonist

Question 56

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

Answer 56

Physiologic Antagonist

Question 57

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

Answer 57

Receptor desensitazation

Question 58

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

Answer 58

Quantal Dose-Response Curve

Question 59

ED50

Answer 59

Median effective dose

Question 60

TD50

Answer 60

Median toxic dose

Question 61

LD50

Answer 61

Median Lethal dose

Question 62

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

Answer 62

Therapeutic Index

Question 63

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

Answer 63

True

Question 64

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

Answer 64

Therapeutic Window

Question 65

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

Answer 65

Maximal efficacy

Question 66

Amount of drug needed to produce a given effect

Answer 66

potency

Question 67

Caused by differences in metabolism (genetic) or immunologic mechanisms

Answer 67

Idiosyncratic response

Question 68

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

Answer 68

Hyporeactive Response

Question 69

Decreased sensitivity acquired as a result of exposure to the drug

Answer 69

Tolerance

Question 70

Intensity of the drug is increased or exaggerated

Answer 70

Hyperreactive response

Question 71

Tolerance develops after a few doses.

Answer 71

Tachyphylaxis

Question 72

decrease in number of receptors.

Answer 72

down-regulation

Question 73

increase in number of receptors.

Answer 73

up-regulation

Question 74

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

Answer 74

Overshoot Phenomenon/Rebound Hypertension

Question 75

What to do to avoid/circumvent toxic effects?

Answer 75

o Give low doses o Carefully monitor the patient o Employ ancillary procedures o Use a safer drug