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

A

dopamine

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

A

Gi

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
Q

what does stimulation of beta3 receptors lead to

A

an increase in lipolysis

26
Q

what effects does epinephrine primarily have at low concentrations

A

beta1 and beta2 effects

27
Q

what effect does norepinephrine have on alpha1 and beta1 receptors

A

agonist

28
Q

what do D1 dopaminergic receptors activate

A

adenylyl cyclase in vascular smooth muscle cells, leading to increased cAMP levels and vasodilation

29
Q

what drug irreversibly inhibits VMAT, resulting in vesicles that lose their ability to concentrate and store norepinephrine and dopamine

A

reserpine

30
Q

what drug acts as a false neurotransmiter

A

guanadrel

31
Q

what do alpha1 selective adrenergic agonists increase

A

peripheral vascular resistance

32
Q

what drug is an alpha2-receptor agonist that lowers blood pressure by acting in brainstem vasomotor centers to suppress sympathetic outflow to the periphery

A

clonidine

33
Q

what are Beta2 selective agonists useful in the treatment of

A

asthma

34
Q

what is metaproterenol used for the treatment of

A

obstructive airway disease and acute bronchospasm

35
Q

what non-selective beta-adrenergic antagonist is lipophilic and has high CNS penetration

A

timolol

36
Q

what is the major difference between pindolol and acebutolol

A

pindolol is beta-nonselective; acebutolol is beta1-selective

37
Q

what are levobunolol and carteolol used for the treatment of

A

glaucoma