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
Metyrosine
drug that inhibits tyrosine hydroxylase which is part of the norepinephrine synthetic pathway
26
Elimination mechanism for sympathetic system (adrenergic)
reuptake
27
Norepinephrine reuptake pump
NET
28
NET inhibitors
cocaine | tricyclic antidepressants
29
effect of NET intibitors
exaggerated response of norepinephrine
30
norepinephrine is an agonist of
alpha 1 = alpha 2 | beta 1 >> beta 2
31
epinephrine is an agonist of
alpha 1 = alpha 2 | beta 1 = beta 2
32
beta 1 receptors are found predominantly in the
heart
33
beta 2 receptors are found predominantly in the
lungs | vasculature in skeletal muscle
34
epinephrine causes ____ in skeletal muscle
vasodilation
35
unlike with norepinephrine, you get a ____ of the pulse pressure with epinephrine
widening
36
G protein coupled with alpha 1 adrenergic recepors
Gq
37
Alpha 2 agonists cause ____ action
inhibitory
38
Beta receptor agonists cause _____ action
stimulatory
39
Epinephrine and Norepinephrine _____ calcium release from SR following the entry of calcium into the cardiac myocyte
stimulate
40
Acetylecholine _____ the release of calcium from the SR
inhibits
41
Malignant hyperthermia
a dysfunction of the ryanodine receptor caused by drugs; genetic predisposition
42
Dantroline
a drug that repackages the calcium back into the SR
43
2 enzymes involved in catecholamine synthesis (degradation?)
COMT (catechol-O-methyl transferase) | MAO (monoamine oxidase)
44
Tumor that leads to excessive catecholamine secretion
Pheochromocytoma; pt tends to be massively hypertensive and massively affected by sympathetic stimulation
45
How do you diagnose pheochromocytoma?
Look for metanephrine and vanillylmandelic acid (VMA) in urine.
46
One way to treat parkinsonism is to elevate _____ levels in the brain.
Dopamine
47
Treatment of someone with parkinsonism.
L-DOPA and inhibitors of L-DOPA metabolism in the periphery
48
How do you maximize dopamine levels in the brain?
Monamine oxidase (MAO) inhibitors
49
Why aren't MAO inhibitors used much anymore?
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
Important molecules in receptor desensitization?
beta-arrestins
51
Rapid development of complete drug tolerance.
Tachyphylaxis
52
beta receptor agonists ____ insulin receptor sensitivity
increase
53
beta receptors lead to the release of _____ into circulation
free fatty acids