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Block 10 > Intro to Autonomic Pharm > Flashcards

Intro to Autonomic Pharm Flashcards

1
Q

2 divisions of the PNS

A

Autonomic and Somatic

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2
Q

2 divisions of the autonomic nervous system

A

Sympathetic and Parasympathetic

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3
Q

4 neurotransmitters

A

Acetylcholine
Norepiniphrine
Dopamine
Epinephrine

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4
Q

Parasympathetic nervous system has a _____ presynaptic neuron and a _____ postsynaptic neuron.

A

long; short

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5
Q

Sympathetic nervous system has a _____ presynaptic neuron and a _____ postsynaptic neuron.

A

short; long

the ganglion is close to the spinal cord

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6
Q

5 neurotransmitter receptors

A 
Nicotinic receptors (2 varieties)
Muscarinic receptors (5 varieties)
Alpha receptors (2 varieties)
Beta receptors (3 varieties; only 2 are important)
Dopamine receptors (5 varieties; only 1 is important)
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7
Q

5 key features of neurotransmitter function that provide targets for drug therapy?

A 
synthesis
storage
release
termination of action
receptor effects
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8
Q

What is the fundamental difference between the methods of inactivation of acetylcholine vs. that of norepinephrine?

A

Acetylcholine is degraded rapidly by acetylcholinesterase.

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9
Q

2 cotransmitters within the vesicle released with acetylcholine

A

ATP

substance P

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10
Q

Functions of cotransmitters

A

modulation

feedback inhibition

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11
Q

function VAMPs and SNAPs

A

docking of vesicle with synaptic endplate in presynaptic neuron

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12
Q

clinical agent that inhibits VAMPs and SNAPs

A

botox

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13
Q

2 types of presynaptic receptors

A

Autoreceptors and Heteroreceptors

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14
Q

Autoreceptor

A

a receptor for the ligand that is being released from that synapse; turns off further release; ACTIVATES receptor when ligand is bound, but the activated receptor INHIBITS further release

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15
Q

Muscarinic receptor

A

?

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16
Q

Heteroreceptor

A

presynaptic receptor where cotransmitters may bind

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17
Q

On cholinergic presynaptic terminals ____ may bind to a heteroreceptor.

A

norepiniphrine

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18
Q

2 families of cholinergic receptors

A

Metabotropic and Ionotropic

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19
Q

Metabotropic receptors

A

function through a second messenger system; ex. muscarinic receptors; often G protein-coupled

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20
Q

Ionotropic receptors

A

ion channels; ex. nicotinic receptors; often calcium

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21
Q

Gq protein

A

works to increase levels of intracellular calcium; activation leads to neuronal activation; M1, M3, M5 muscarinic receptors

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22
Q

Gi protein

A

generated inhibitory response; M2, M4 muscarinic receptors

23
Q

Choline Ester drugs with minimal susceptibility to acetylcholinesterase (3)

A

Methacholine chloride
Carbachol chloride
Bethanechol chloride

24
Q

Reserpine

A

drug that prevents the packaging of dopamine into vesicles

25
Q

Metyrosine

A

drug that inhibits tyrosine hydroxylase which is part of the norepinephrine synthetic pathway

26
Q

Elimination mechanism for sympathetic system (adrenergic)

A

reuptake

27
Q

Norepinephrine reuptake pump

A

NET

28
Q

NET inhibitors

A

cocaine

tricyclic antidepressants

29
Q

effect of NET intibitors

A

exaggerated response of norepinephrine

30
Q

norepinephrine is an agonist of

A

alpha 1 = alpha 2

beta 1&raquo_space; beta 2

31
Q

epinephrine is an agonist of

A

alpha 1 = alpha 2

beta 1 = beta 2

32
Q

beta 1 receptors are found predominantly in the

A

heart

33
Q

beta 2 receptors are found predominantly in the

A

lungs

vasculature in skeletal muscle

34
Q

epinephrine causes ____ in skeletal muscle

A

vasodilation

35
Q

unlike with norepinephrine, you get a ____ of the pulse pressure with epinephrine

A

widening

36
Q

G protein coupled with alpha 1 adrenergic recepors

A

Gq

37
Q

Alpha 2 agonists cause ____ action

A

inhibitory

38
Q

Beta receptor agonists cause _____ action

A

stimulatory

39
Q

Epinephrine and Norepinephrine _____ calcium release from SR following the entry of calcium into the cardiac myocyte

A

stimulate

40
Q

Acetylecholine _____ the release of calcium from the SR

A

inhibits

41
Q

Malignant hyperthermia

A

a dysfunction of the ryanodine receptor caused by drugs; genetic predisposition

42
Q

Dantroline

A

a drug that repackages the calcium back into the SR

43
Q

2 enzymes involved in catecholamine synthesis (degradation?)

A

COMT (catechol-O-methyl transferase)

MAO (monoamine oxidase)

44
Q

Tumor that leads to excessive catecholamine secretion

A

Pheochromocytoma; pt tends to be massively hypertensive and massively affected by sympathetic stimulation

45
Q

How do you diagnose pheochromocytoma?

A

Look for metanephrine and vanillylmandelic acid (VMA) in urine.

46
Q

One way to treat parkinsonism is to elevate _____ levels in the brain.

A

Dopamine

47
Q

Treatment of someone with parkinsonism.

A

L-DOPA and inhibitors of L-DOPA metabolism in the periphery

48
Q

How do you maximize dopamine levels in the brain?

A

Monamine oxidase (MAO) inhibitors

49
Q

Why aren’t MAO inhibitors used much anymore?

A

MAO breaks down tyramine. If on MAO inhibitor, you can’t eat foods that are rich in tyramine (shit ton of foods). Scotch OK

50
Q

Important molecules in receptor desensitization?

A

beta-arrestins

51
Q

Rapid development of complete drug tolerance.

A

Tachyphylaxis

52
Q

beta receptor agonists ____ insulin receptor sensitivity

A

increase

53
Q

beta receptors lead to the release of _____ into circulation

A

free fatty acids

Block 10 (16 decks)

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