Review of Pharmacodynamics

Question 1

a competitive antagonist can be overcome by increasing ______ concentration

Answer 1

agonist

Question 2

pharmacologic agent that can not be overcome by increasing agonist concentration

Answer 2

irreversible antagonist

Question 3

drug that binds its receptor but produces a smaller effect at full dosage than a full agonist

Answer 3

partial agonist

Question 4

a graph of the fraction of a population that shows a specified response at progressively increasing doses

Answer 4

quantal dose response curve

Question 5

increase on the y axis gives a drug increased _______, while the farthest left on the x axis gives a drug increased ________

Answer 5

efficacy

potency

Question 6

presence of a competitive antagonist will shift dose response curve where?

Answer 6

to the right

Question 7

• effect not completely overcome by increasing agonist concentration
• number of functional receptors is decreased
• Emax decreases, b/c fewer functional receptors are available
• cause a nonparallel, downward shift of LDR curve for the agonist to the right

Answer 7

irreversible/allosteric antagonists

Question 8

• effects occur at lower concentrations of ligand than binding parameters predict
• not all receptors have to be occupied for max effect
• receptor activation is not the limiting step
• dose response curve shifted to left (increased potency), relative to results in cells or tissues without

Answer 8

spare receptors

Question 9

TSH works in the adenylyl cyclase system through _______ path as a stimulatory agonist

Answer 9

Gs

Question 10

M2 agonist (such as pilocarpine) work as inhibitory agonists in the _____ path

Answer 10

Gi

Question 11

alpha-1, vasopressin, TXA2, endothelin, angiotensin receptors, muscarinic receptors, histamine, and bradykinin work through what signaling system?

Answer 11

Gq –> PLC –> IP3 –> Calcium and DAG –> PKC

Question 12

stimulates adenylyl cyclase to increase cAMP, coupled receptors (dopamine, epi, glucagon, histamine, vasopressin)

Answer 12

Gs

Question 13

inhibits adenylyl cyclase (dopamine D2, epi a2, M2)

Answer 13

Gi

Question 14

stimulates phospholipase C, coupled receptors are ang 2, epi (alpha-1), oxytocin, vasopressin, histamine H1

Answer 14

Gs

Question 15

acetylcholine, histamine, bradykinin, VEGf cause ________ via a nitric oxide dependent endothelial path

Answer 15

vasodilation

Question 16

signal via ______:

• glucocorticoids
• mineralocorticoids
• vitamin D
• thyroid hormone
• retinoic acid

Answer 16

gene expression

Question 17

therapeutic index formula?

Answer 17

LD50/ED50

Question 18

margin of safety formula?

Answer 18

LD1/ED99