Sympathomimetics Flashcards

1
Q

monoamine

A

amino group connected to aromatic ring by two carbons

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2
Q

catecholamine

A

monoamine with catechol (benzene with two hydroxy)

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3
Q

biosynthesis catecholamines

A

L-Tyrosine
L-DOPA
Dopamine
Norepinephrine
Epinephrine

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4
Q

norepinephrine neurotransmission

A

tyrosine into ending, then to dopa
dopamine into vesicle by VMAT
dopamine to NE
calcium opens channel and vesicles fuse
NE binds adrenergic receptors

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5
Q

stereochemical requirements for adrenoceptor binding

A

catechol
amine
hydroxy
R stereochemistry

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6
Q

epinephrine receptor selectivity

A

more selective beta but alpha 1 and 2 beta 1 and 2

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7
Q

norepinephrine receptor selectivity

A

alpha 1 and 2 and beta 1 NO BETA 2

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8
Q

alpha 1 receptor Gq

A

vasocontriction
pupil dilation
ejaculation
urine inhibition
GI inhibition

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9
Q

alpha 2 receptor Gi

A

vasoconstriction
prejunctional NE inhibition
in cns decrease CV SNS input

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10
Q

beta 1 receptor Gs

A

cardiac stimulation
renin secretion

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11
Q

beta 2 receptor Gs

A

cardiac stimulation
bronchodilation
uterine relaxation
GI inhibition
vasodilation

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12
Q

what do alpha 1 agonists due

A

nasal decongestion
vascular failure in shock and tachycardia

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13
Q

why is phenylephrine not very effective? first pass metabolism

A

cant reach site, broken down in the liver

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14
Q

where is alpha 1 found?

A

smooth muscle, heart, liver

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15
Q

alpha 1 drug structure

A

imidazoline connected to carbon

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16
Q

where is alpha 2 found?

A

pre synaptically

17
Q

what do alpha 2 agonists do

A

hypertension
pain
glaucoma
inhibit SNS activity

18
Q

methyldopa is a

A

prodrug, not very soluble tho so methyldopate used for iv

19
Q

where is beta 1 found

A

heart, kidney

20
Q

what do beta 1 agonists do

A

shock, congestive heart failure

21
Q

what do beta 1 antagonists do

A

hypertension, angina, arrhythmias, congestive heart failure

22
Q

where is beta 2 found

A

smooth muscle

23
Q

what do beta 2 agonists do

A

asthma, premature labor

24
Q

what do beta 2 antagonists do

A

glaucoma

25
Q

where is beta 3 found

A

urinary bladder

26
Q

what does beta 3 agonist do

A

overactive bladder

27
Q

2 meta hydroxys on benzene ring receptor type

A

beta 2

28
Q

indirect acting sympathomimetics structure

A

no MAO or COMT

29
Q

lack of hydroxyl on indirect effect

A

increased CNS activity

30
Q

how to get from amphetamine to methamphetamine

A

lose beta carbon

31
Q

how do maois work

A

NE can not degrade, increased sympathetic action

32
Q

tyramine

A

high levels in beer/cheese/wine, increase NE which could lead to hypertensive crisis

33
Q

NET inhibitors action

A

inhibit reuptake of NE so it stays in the synaptic cleft

34
Q

non stim ADHD meds

A

atomoxetine, guanfacine, clonidine

35
Q

stim ADHD meds

A

methylphenidate, amphetamine