First Aid 245-249 Pharm Flashcards Preview

FIRST aid 2015 - Sahaja > First Aid 245-249 Pharm > Flashcards

Flashcards in First Aid 245-249 Pharm Deck (41):
1

Efficacy

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

2

Potency

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

3

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

Shift curve to the R - more potency, no change in efficacy
Can be overcome with increasing substrate level

4

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

Shifts curve down - dec efficacy (as expected)

5

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

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

6

TD50

median toxic dose

7

ED50

median effective dose

8

Drugs with higher therapeutic index

digoxin, lithium, theophylline, warfarin

9

Parasympathetic Ach M-R are located where?

Cardiac, smooth muscle, gland cells, n. terminals

10

Sympathetic Ach M-R located where?

Sweat glands

11

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

Cardiac and smooth musc, gland cells, n. terminals

12

Sympathetic Dopamine-R located where?

renal a/v, smooth musc

13

What stimulates the adrenal medulla to release Epi, NE?

Ach

14

Which toxin prevents the release of Ach?

Botulinum toxin

15

Nicotinic Ach receptors are connected to which type of channels?

Ligand gated Na/K channels

16

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

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

17

Which receptors are Gq coupled ?

alpha 1, Muscarinic 1 & 3, H1, V1

18

Which receptors are Gs coupled?

B1, B2, D1, H2, V2

19

Which receptors are Gi coupled?

a2, M2, D2

20

Pathway of Gq

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

21

Pathway of Gs/Gi

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

22

Hemicholinium inhibits what?

the uptake of choline into a nerve terminal

23

Vesamicol inhibits what?

The uptake of Ach into a vesicle

24

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

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

25

Metyrosine inhibits which reaction?

Tyrosine --> DOPA

26

Reserpine does what?

Inhibits the uptake of Dopamine into a vesicle via VMAT

27

What stimulates and inhibits NE release into the synapse?

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

Inhibit - a2-R activation, Bretylium, Gaunethidine

28

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

Cocaine, TCAs, Amphetamine

29

Major functions of a1 -R?

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

30

Which G prot coupled receptor increases/dec insulin release?

B2, a2

31

Which receptor stimulates platelet aggregation?

a2-R

32

Which receptor increases vascular permeability?

H1-R

33

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

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

34

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

M2R

35

Reserpine is contraindicated with use of what other drug?

MAO inhibitors

36

Guanethidine mech / contraindicated with which drug?

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

37

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

It helps anchor them to plasma membrane

38

Which adr. rec'r dec uterine tone?

B2

39

Which rec'r activation causes broncioloconstriction?

H1

40

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

a1, V1

41

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

B1,a1