09 - Adrenergic Pharmacology Flashcards

(40 cards)

1
Q

Norepinephrine

A

primary transmitter at the sympathetic postganglionic neuron effector cell synapses in most tissues

exceptions:

  • eccrine sweat glands
  • vasodilator sympathetic fibers in skeletal muscle
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2
Q

Dopamine/Norepinephrine on renal blood vessels

A

dopamine vasodilates renal blood vessels

norepinephrine vasoconstricts

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3
Q

Tyrosine is hydroxylated by tyrosine hydroxylase to

A

DOPA

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4
Q

Tyrosine hydroxylase is inhibited by

A

metyrosine

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5
Q

DOPA is decarboxylated to

A

dopamine

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6
Q

dopamine is hydroxylated to

A

norepinephrine

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7
Q

NE and dopamine are transported into vesicles

inactivated by:

A

monoamine oxidase in the cytoplasm

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8
Q

increase stores of NE and dopamine

A

MAOIs

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9
Q

vesicular transport inhibted by

A

reserpine

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10
Q

entry of calcium triggers interaction among

A

SNARE proteins (VAMPs and SNAPs)

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11
Q

What are SNARE proteins

A

“SNAP (Soluble NSF Attachment Protein) REceptor”

The primary role of SNARE proteins is to mediate vesicle fusion, that is, the fusion of vesicles with their target membrane bound compartments (such as a lysosome). The best studied SNAREs are those that mediate docking of synaptic vesicles with the presynaptic membrane in neurons. These SNAREs are the targets of the bacterial neurotoxins responsible for botulism and tetanus.

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12
Q

entry of calcium inhibited by

promoted by

A

guanethidine

amphetamines and tyramine

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13
Q

diffusion and reupate via NET and DAT in synaptic cleft

inhibited by

A

cocaine and TCAs

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14
Q

metabolized by MAO and COMT into

inhibited by

A

metanephrines and VMA

MAOIs and COMT inhibitors (duh)

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15
Q

Site of autonomic drug action:

synthesis cholinergic and adrenergic inhibitors

A

hemicholinium

metyrosine

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16
Q

Site of autonomic drug action:

storage cholinergic and adrenergic inhibitors

A

vesamicol

reserpine

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17
Q

Site of autonomic drug action:

release cholinergic and adrenergic inhibitors

A

botulinium

guanethedine

18
Q

Site of autonomic drug action:

termination metabolism cholinergic and adrenergic inhibitors

A

neostigmine

MAOIs, COMTIs

19
Q

Site of autonomic drug action:

termination reuptake cholinergic and adrenergic inhibitors

A

none

cocaine, TCAs

20
Q

drug effects on adrenergic transmission

A

used in treatment of several diseases (pheochromocytoma, hypertension)
block sympathetic but NOT parasympathetic functions

other drugs promote catecholamine release - predictably cause sympathomimetics effects

21
Q

a1 adrenergic effects

- most vascular smooth muscle

A

contracts (increased vascular resistance)

22
Q

a1 adrenergic effects

- pupillary dilator muscle

A

contracts (mydriasis)

23
Q

a1 adrenergic effects

- pilomotor smooth muscle

A

contracts (erects hair)

24
Q

a1 adrenergic effects

- liver (in some species, eg, rat)

A

stimulates glycogenolysis

25
a2 adrenergic effects | - adrenergic and cholinergic nerve terminals
inhibits transmitter release
26
a2 adrenergic effects | - platelets
stimulates aggregation
27
a2 adrenergic effects | - some vascular smooth muscle
contracts
28
a2 adrenergic effects | - fat cells
inhibits lypolysis
29
a2 adrenergic effects | - pancreatic B cells
inhibits insulin release
30
B1 adrenergic effects | - heart
stimulates rate and force
31
B1 adrenergic effects | - juxtaglomerular cells of kidney
stimulates renin release
32
B2 adrenergic effects | - airways, uterine, and vascular smooth muscle
relaxes
33
B2 adrenergic effects | - liver (human)
stimulates glycogenolysis
34
B2 adrenergic effects | - pancreatic B cells
stimulates insulin release
35
B2 adrenergic effects | - somatic motor neuron terminals (voluntary muscle)
causes tremor
36
B2 adrenergic effects | - heart
stimulates rate and force
37
B3 adrenergic effects | - fat cells
stimulates lipolysis
38
dopamine1 (d1) adrenergic effects | - renal and other splanchnic blood vessels
dilates (decrease resistance)
39
d2 adrenergic effects | - nerve terminals
inhibits adenylyl cyclase
40
beta receptors mnemonic
1 heart, 2 lungs b1 heart b2 lungs