pharm chapter 10 Flashcards

1
Q

what amino acid are catecholamines synthesized from

A

tyrosine

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2
Q

where is epinephrine predominantly synthesized

A

in chromatin cells of the adrenal medulla

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3
Q

what is the first step in catecholamine synthesis

A

oxidation of tyrosine to DOPA

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4
Q

what is the rate limiting step in catecholamine synthesis

A

tyrosine hydroxylase

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5
Q

where does the conversion of tyrosine to dopamine occur

A

within the cytoplasm

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6
Q

what transports dopamine into synaptic vesicles

A

VMAT

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7
Q

what converts dopamine to norepinephrine once inside the vesicles

A

dopamine beta hydroxylase

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8
Q

where is VMAT1 primarily expressed

A

peripherally (adrenal, sympathetic ganglia)

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9
Q

where is VMAT2 primarily expressed

A

in the CNS

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10
Q

where is VAChT expressed

A

in cholinergic neurons

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11
Q

what converts norepinephrine to epinephrine once it returns to the cytosol

A

PNMT

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12
Q

what does alpha-methyltyrosine inhibit

A

tyrosine hydroxyls

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13
Q

what transporter does cocaine inhibit

A

the norepinephrine transporter

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14
Q

what does reserpine inhibit

A

the vesicular monoamine transporter

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15
Q

what transporter mediates the reuptake of catecholamine into the neuronal cytoplasm

A

NET

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16
Q

what does MAO-A preferentially degrade

A

serotonin, norepinephrine, and dopamine

17
Q

what does MAO-B most readily degrade

18
Q

what do MAO inhibitors have efficacy in the treatment of

A

depression

19
Q

what do the pathways of alpha 1 receptors activate

A

phospholipase C

20
Q

what antagonists are found to be effective in treatment of BPH

A

alpha1 receptor antagonists

21
Q

what do alpha2-adrenoreceptors activate

22
Q

where are beta1 adrenoceptors localized primarily

A

in the heart and kidney

23
Q

where are beta2 adrenoceptors mostly expressed

A

smooth muscle, liver, and skeletal muscle

24
Q

where are beta3 adrenoceptors expressed specifically

A

adipose tissue

25
what does stimulation of beta3 receptors lead to
an increase in lipolysis
26
what effects does epinephrine primarily have at low concentrations
beta1 and beta2 effects
27
what effect does norepinephrine have on alpha1 and beta1 receptors
agonist
28
what do D1 dopaminergic receptors activate
adenylyl cyclase in vascular smooth muscle cells, leading to increased cAMP levels and vasodilation
29
what drug irreversibly inhibits VMAT, resulting in vesicles that lose their ability to concentrate and store norepinephrine and dopamine
reserpine
30
what drug acts as a false neurotransmiter
guanadrel
31
what do alpha1 selective adrenergic agonists increase
peripheral vascular resistance
32
what drug is an alpha2-receptor agonist that lowers blood pressure by acting in brainstem vasomotor centers to suppress sympathetic outflow to the periphery
clonidine
33
what are Beta2 selective agonists useful in the treatment of
asthma
34
what is metaproterenol used for the treatment of
obstructive airway disease and acute bronchospasm
35
what non-selective beta-adrenergic antagonist is lipophilic and has high CNS penetration
timolol
36
what is the major difference between pindolol and acebutolol
pindolol is beta-nonselective; acebutolol is beta1-selective
37
what are levobunolol and carteolol used for the treatment of
glaucoma