First Aid 245-249 Pharm

Question 1

Efficacy

Answer 1

maximum effect a drug can produce - inc efficacy = inc y value

Question 2

Potency

Answer 2

amount of drug needed for given effect - Inc potency = to the left

Question 3

Competitive antagonist shifts a curve in what direction? Does it affect potency? Efficacy?

Answer 3

Shift curve to the R - more potency, no change in efficacy

Can be overcome with increasing substrate level

Question 4

Noncompetitive antagonist shifts curve in what direction? Does it affect potency? Efficacy?

Answer 4

Shifts curve down - dec efficacy (as expected)

Question 5

Partial agonist - location of action. Does it affect potency? Efficacy?

Answer 5

Acts on the active site - same location as full agonist. Lower maximal effect, and therefore decreased efficacy. Potency is not related.

Question 6

TD50

Answer 6

median toxic dose

Question 7

ED50

Answer 7

median effective dose

Question 8

Drugs with higher therapeutic index

Answer 8

digoxin, lithium, theophylline, warfarin

Question 9

Parasympathetic Ach M-R are located where?

Answer 9

Cardiac, smooth muscle, gland cells, n. terminals

Question 10

Sympathetic Ach M-R located where?

Answer 10

Sweat glands

Question 11

Sympathetic (NE) stimulate alpha/beta -R where?

Answer 11

Cardiac and smooth musc, gland cells, n. terminals

Question 12

Sympathetic Dopamine-R located where?

Answer 12

renal a/v, smooth musc

Question 13

What stimulates the adrenal medulla to release Epi, NE?

Answer 13

Ach

Question 14

Which toxin prevents the release of Ach?

Answer 14

Botulinum toxin

Question 15

Nicotinic Ach receptors are connected to which type of channels?

Answer 15

Ligand gated Na/K channels

Question 16

Muscarinic Ach receptors have what type of mechanisms, and what are the subtypes?

Answer 16

G protein coupled receptors acting through second messangers - 5 subtypes: M1-5

Question 17

Which receptors are Gq coupled ?

Answer 17

alpha 1, Muscarinic 1 & 3, H1, V1

Question 18

Which receptors are Gs coupled?

Answer 18

B1, B2, D1, H2, V2

Question 19

Which receptors are Gi coupled?

Answer 19

a2, M2, D2

Question 20

Pathway of Gq

Answer 20

PLC –> PIP2 splits into DAG + IP3. DAG –>PKC, IP3 –> inc Ca –> smooth musc contraction

Question 21

Pathway of Gs/Gi

Answer 21

Gs and Gi stimulate and inhibit AC, respectively. AC –> inc cAMP –> stimulate PKA –> stimulate Ca in heart and myosin light chain kinase in smooth musc

Question 22

Hemicholinium inhibits what?

Answer 22

the uptake of choline into a nerve terminal

Question 23

Vesamicol inhibits what?

Answer 23

The uptake of Ach into a vesicle

Question 24

What stimulates/inhibits the release of Ach into a synapse?

Answer 24

Ach release into a synapse is stimulated by Ca2+ and inhibited by Botulinum toxin

Question 25

Metyrosine inhibits which reaction?

Answer 25

Tyrosine –> DOPA

Question 26

Reserpine does what?

Answer 26

Inhibits the uptake of Dopamine into a vesicle via VMAT

Question 27

What stimulates and inhibits NE release into the synapse?

Answer 27

Stimulate: ATII- R activation, Ca 2+, Amphetamine, Ephedrine

Inhibit - a2-R activation, Bretylium, Gaunethidine

Question 28

Which drugs inhibit the reuptake of NE into the nerve terminal?

Answer 28

Cocaine, TCAs, Amphetamine

Question 29

Major functions of a1 -R?

Answer 29

Inc vascular smooth m contraction, mydriasis, inc GI/Bladder sphinter musc contraction

Question 30

Which G prot coupled receptor increases/dec insulin release?

Answer 30

B2, a2

Question 31

Which receptor stimulates platelet aggregation?

Answer 31

a2-R

Question 32

Which receptor increases vascular permeability?

Answer 32

H1-R

Question 33

Which receptor increases H20 permeability and resorption in the kidney, and which part of the tubules?

Answer 33

V2R - (V 2in the 2-bules! ) in the collecting duct

Question 34

Which G prot coupled receptor decreases heart rate and atrial contractility?

Answer 34

M2R

Question 35

Reserpine is contraindicated with use of what other drug?

Answer 35

MAO inhibitors

Question 36

Guanethidine mech / contraindicated with which drug?

Answer 36

Guanethidine binds NE filled vesicles to stop NE realease, CI w/ TCAs (will inhibit uptake of Guanethidine)

Question 37

Fun fact: Most G prot coupled rec’r have carboxylated tails with palmitoyl @ cysteine residues

Answer 37

It helps anchor them to plasma membrane

Question 38

Which adr. rec’r dec uterine tone?

Answer 38

B2

Question 39

Which rec’r activation causes broncioloconstriction?

Answer 39

H1

Question 40

Which two rec’rs, when (+)’d, will cause vascular smooth muscle contraction?

Answer 40

a1, V1

Question 41

Dopamine at high levels can affect which receptors? (Other than D-R)

Answer 41

B1,a1