Pharmacodynamics: Ch 1

Question 1

definition of drug

Answer 1

exogenous chemical agent used to modify physiology

Question 2

definition of pharmacology

Answer 2

study of the use of chemical agents for therapeutic purposes

Question 3

definition of toxicology

Answer 3

Adverse effects of a drug

Question 4

site of action of drug

Answer 4

receptor

Question 5

drug that mimics a biological effect

Answer 5

agonist

Question 6

drug that inhibits a biological effect

Answer 6

antagonist

Question 7

Therapeutic effect and toxic effects are examples of?

Answer 7

pharmacodynamics

Question 8

what is pharmacodynamics?

Answer 8

what the drug does to the BODY; alter or modify existing physiologic or pathologic processes.

Question 9

absorption, distribution, metabolism, elimination are examples of what?

Answer 9

pharmacokinetics

Question 10

what is pharmacokinetics?

Answer 10

what the body does to the DRUG

Question 11

what is the basic principle of pharmacodynamics?

Answer 11

drugs have specific molecular targets (receptors) in the body
ex: lidocaine and penicillin

Question 12

Ion channel linked receptors

Answer 12

depolarize or hyperpolarize the membrane

Question 13

glutamate, 5-hydroxytryptamine, G-aminobutryic acid, and glycine receptors are all examples of what receptor class?

Answer 13

ion channel linked receptors

Question 14

G protein coupled receptors

Answer 14

• largest family of receptors
• target for half the drugs
• metabotropic receptors

Question 15

a (alpha) subunit: G protein

Answer 15

activates effectors when GTP bound and dissociated from BY (beta-gamma) subunits

Question 16

BY (beta-gamma) subunits: G protein

Answer 16

activated upon dissociation from alpha subunit; activates effectors when FREE

Question 17

examples of effectors

Answer 17

adenylate cyclase, PI3 kinase, protein kinase C

Question 18

receptor + agonist = ______

Answer 18

receptor turned on

Question 19

transmembrane receptors with intrinsic enzymatic activity

Answer 19

• tyrosine kinase
• tyrosine phosphatase
• serine/threonine kinase
• guanylyl cyclase

Question 20

receptors with associated enzyme activity

Answer 20

• enzyme activity is seperate from the ligand binding domain; enzyme dissociates from the receptor and **functions elsewhere in cell. **
• Examples: JAK, STAT

Question 21

intracellular receptors

Answer 21

receptor is inside the cell so the ligand must be able to pass through the membrane to bind; typically mediates DNA transcriptions
Example: steroid hormone receptors

Question 22

ion channel time

Answer 22

milliseconds

Question 23

G protein linked time

Answer 23

seconds

Question 24

transmembrane receptor times

Answer 24

minutes to hours

Question 25

intracellular receptor time

Answer 25

hours to days

Question 26

Drug binding affinity

Answer 26

covalent>ionic>hydrogen >hydrophobic

Question 27

Covalent bonds are _____ and ______

Answer 27

strongest, irreversible

Question 28

Ionic bonds are ____ , _____, and ____

Answer 28

most common, intermediate, reversible

Question 29

what is the structure activity relationship?

Answer 29

How the ligand fits into the receptor binding pockets. It reflects the summation of the drug binding forces, *******inducing a conformational change. ******* Examples: size, direct interaction, stereo-isomers

Question 30

what are some consequences of drug binding?

Answer 30

- changes in intracellular ions - small molecules through GPCRs - protein phosphorylation - DNA transcription

Question 31

maximal amount of ligand bound

Answer 31

Bmax

Question 32

concentration at which 50% of the receptors are bound with the ligand

Answer 32

KD

Question 33

what is the law of mass of action?

Answer 33

KD+ K2/K1 K1: rate of association K2: rate of dissociation

Question 34

Dose response curves use ___ and ____ compared to ligand curves which use ____ and ____

Answer 34

Emax, EC50, Bmax, KD

Question 35

efficacy measures

Answer 35

Emax

Question 36

Potency measures

Answer 36

EC50

Question 37

A full agonist elicits the ____ possible effect

Answer 37

maximal

Question 38

A partial agonist elicits a ____ than maximal effect

Answer 38

less

Question 39

Which agonist is less efficacious?

Answer 39

Partial

Question 40

measure of affinity

Answer 40

KD

Question 41

competes with a ligand for binding to a receptor

Answer 41

competitive antagonist

Question 42

binds to the receptor with high affinity, there is no apparent dissociation

Answer 42

irreversible (non-comp)

Question 43

a competitive antagonist shifts the ____

Answer 43

EC50

Question 44

a non-competitive antagonist reduce the ____

Answer 44

Emax

Question 45

block the tonic activity of a receptor, reducing basal activity

Answer 45

Inverse agonists

Question 46

Not every receptor needs to be occupied to achieve a maximal effect

Answer 46

Spare receptor

Question 47

attenuated response that occurs with sustained stimulation with a drug; physiological

Answer 47

tolerance

Question 48

refers to the modifications of the receptor to minimize signaling; cellular

Answer 48

densensitization

Question 49

the process by which the number of receptors is decreased; molecular

Answer 49

downregulation