Pharmacodynamics 2

Question 1

example: inhibition of agonist inactivation? (for NA)

Answer 1

drugs that inhibit NA uptake = cocaine and tricyclic antidepressents

Question 2

example: inhibition of agonist inactivation? (for 5HT)

Answer 2

SSRIs: elevate mood because now you have more synaptic 5HT = treats depression

Question 3

calcium channel blockers: effects? (3)

Answer 3

reduced Ca entry = anti anginal (reduced force of contraction and O2 consumption in heart). anti-dysrhythmic (reduces cardiac excitability). anti-hypertensive (vasodilation)

Question 4

Na channels responsible for what 2 things

Answer 4

initiation of membrane action potential, and propagation of AP

Question 5

Na channel blockers; what are the effects?

Answer 5

AP fails to generate, blocks nerve conduction.

Question 6

Na channel blockers: mechanism of action of? preferential blockage of?

Answer 6

mechanism of local anesthetics, preferential block of small pain fibers

Question 7

Na/K ATP ase inhibited by? effects? useful for what treatment

Answer 7

cardiac glycosides aka digoxin slows efflux of Na+ = increased intracellular Na = increased intracellular Ca = increases force of cardiac contraction - used to treat heart failure

Question 8

5 ways enzyme activity can be affected by drugs

Answer 8

drug an mimic enzyme product. drug may be enzyme substrate. drug can be changed to altered product. drug can inhibit enzyme activity. or promote enzyme activity.

Question 9

NO: produced by what and where? actions?

Answer 9

produced by NOS, in endothelial lining of blood vessels. diffuses to muscle to activated GC = elevates intracellular cGMP = relax smooth muscles, vasodilation

Question 10

drugs that act as NO donors: mimic? direct actions on ___?

Answer 10

mimic endogenous NO - direct actions on vasculature: relaxation reduces vascular resistance, used as vasodilators

Question 11

NO donor drugs: indirection actions on ___? 2 actions? results in? treats?

Answer 11

indirect actions on heart: dilates arteries = reduces afterload. dilates veins = reduces preload. results in reduced cardiac workload. treats angina

Question 12

drugs that serve as enzyme substrates: work by? example?

Answer 12

increasing levels of natural product of enzyme. ex: levodopa for parkinson’s disease

Question 13

drug may be changed to altered product of enzyme: example?

Answer 13

anti-metabolites: drug that inhibits use of metabolite; drug is often similar in structure to metabolite.

Question 14

antimetabolites: effects? uses?

Answer 14

toxic effects: slow cell growth and division. useful in chemotherapy.

Question 15

cholinesterase inhibitors: actions? treats?

Answer 15

prevents ACh breakdown = increase parasympathetic activity. treat alzheimer’s.

Question 16

cyclo-oxygenase: isoforms? purpose? inhibited by?

Answer 16

isoforms COX1 and II. prostaglandin biosynthesis. inhibited by NSAIDs like ASA, ibuprofen

Question 17

phosphodiesterase PDE inhibitors: effects?

Answer 17

prevent cAMP breakdown = positive inotropic actions, vasodilation, CNS actions, bronchodilation. cGMP = enhances NO vasodilation, anti-anginal, treats erectile dysfunction

Question 18

antiotensin converting enzyme inhibitors: action? effects?

Answer 18

inhibit ACE = reduce synthesis of angiotensin II and reduce bradykinin breakdown = vasodilation.

Question 19

ACE inhibitors used to treat? end with?

Answer 19

antihypertensive; treat heart failure. end with “april”