First Aid 245-249 Pharm Flashcards

(41 cards)

1
Q

Efficacy

A

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

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2
Q

Potency

A

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

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3
Q

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

A

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

Can be overcome with increasing substrate level

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4
Q

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

A

Shifts curve down - dec efficacy (as expected)

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5
Q

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

A

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

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6
Q

TD50

A

median toxic dose

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7
Q

ED50

A

median effective dose

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8
Q

Drugs with higher therapeutic index

A

digoxin, lithium, theophylline, warfarin

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9
Q

Parasympathetic Ach M-R are located where?

A

Cardiac, smooth muscle, gland cells, n. terminals

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10
Q

Sympathetic Ach M-R located where?

A

Sweat glands

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11
Q

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

A

Cardiac and smooth musc, gland cells, n. terminals

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12
Q

Sympathetic Dopamine-R located where?

A

renal a/v, smooth musc

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13
Q

What stimulates the adrenal medulla to release Epi, NE?

A

Ach

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14
Q

Which toxin prevents the release of Ach?

A

Botulinum toxin

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15
Q

Nicotinic Ach receptors are connected to which type of channels?

A

Ligand gated Na/K channels

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16
Q

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

A

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

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17
Q

Which receptors are Gq coupled ?

A

alpha 1, Muscarinic 1 & 3, H1, V1

18
Q

Which receptors are Gs coupled?

A

B1, B2, D1, H2, V2

19
Q

Which receptors are Gi coupled?

20
Q

Pathway of Gq

A

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

21
Q

Pathway of Gs/Gi

A

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
Q

Hemicholinium inhibits what?

A

the uptake of choline into a nerve terminal

23
Q

Vesamicol inhibits what?

A

The uptake of Ach into a vesicle

24
Q

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

A

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