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UNMC PA Pharmacology > Presynaptic Drugs > Flashcards

Presynaptic Drugs Flashcards

1
Q

Rate limiting step of ACh synthesis

A

Transport of choline into pre-synaptic nerve endings by a Na+ choline co-transporter

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2
Q

ACh is stored in ____.

A

Nerve terminal vesicles

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3
Q

ACh is released when ____

A

Stimulated by an action potential/Ca2+ influx; causes exocytosis of ACh vesicle

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4
Q

OnabotulinumtoxinA (Botox) function

A

Inhibit ACh release

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5
Q

OnabotulinumtoxinA MOA

A

Neurotoxic proteases endocytosed into cholinergic nerve terminals and inactive SNAP-25 needed to dock vesicle membrane

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6
Q

OnabotulinumtoxinA causes _____ paralysis and inactivates _____ glands

A

Flaccid; sweat

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7
Q

OnabotulinumtoxinA duration of action

A

3-4 months

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8
Q

Clinical uses of OnabotulinumtoxinA

A

Muscle spasms
Cosmetic
Hyperhidrosis
Migraines
Overactive bladder

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9
Q

Sides effect of OnabotulinumtoxinA

A

Dysphasia
Difficulty breathing
Muscle weakness
Urinary retention

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10
Q

OnabotulinumtoxinA black box warning

A

Distant spread beyond injection site

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11
Q

What tissues are M3 receptors found in?

A

Smooth muscle, glands, endothelium

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12
Q

M3 receptors are a ____ G-protein coupled receptor

A

Gq (activate PLC to initiate cascade to increase Ca2+)

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13
Q

M2 receptors are found in the _____

A

Heart

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14
Q

M2 receptors are ___ G-protein coupled receptors

A

Gi ( decrease cAMP, increase K+ efflux to cause hyperpolarization)

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15
Q

Prototype muscarinic ACh agonist

A

Muscarine

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16
Q

Muscarine activates ____

A

All muscarinic receptor types

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17
Q

Prototype muscarinic ACh antagonist

A

Atropine

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18
Q

Atropine blocks ____

A

All muscarinic receptor subtypes

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19
Q

Nicotinic receptors are ____ ion channels

A

Ligand-gated

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20
Q

When stimulated nicotinic receptors increase ___ permeability, causing ______

A

Na+; depolarization

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21
Q

Nn receptors are located in _____

A

Ganglia and adrenal medulla

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22
Q

Nn receptor high affinity agonist

A

Nicotine

23
Q

Nn receptor prototype antagonist

A

Mecamylamine

24
Q

Nm receptors are located in the ______ junction

A

Neuromuscular

25
Q

Nm receptor low affinity agonist

A

Nicotine

26
Q

Nm receptor prototype antagonist

A

D-tubocurarine

27
Q

After stimulating N receptors, nicotine ____ the receptor

A

Desensitizes (acts like an antagonist)

28
Q

What enzyme rapidly hydrolyzes ACh to terminate cholinergic neurotransmission?

A

Acetylcholinesterase (AchE)

29
Q

Inhibition of AChE causes ACh to ____

A

Accumulate in the synapse, resulting in increased stimulation and then desensitization

30
Q

Butyrylcholinesterase function

A

Drug metabolizing enzyme that controls plasma levels of choline ester drugs

31
Q

Synthesis of Catecholamine Pathway

A

Tyrosine —> dopa —> dopamine —> norepinephrine—> epinephrine

32
Q

Tyrosine is converted to dopa in the ____

A

Cytosol

33
Q

Dopamine is converted to norepinephrine in ____

A

Vesicles

34
Q

Norepinephrine is converted to epinephrine in the ___ of the ____.

A

Cytosol; adrenal medulla

35
Q

Catecholamines are degraded by ____ if they are not stored

A

Mitochondrial monoamine oxidase

36
Q

Catecholamines are actively transported into vesicles by ___

A

Vesicular monoamine transporter-2 (VMAT-2)

37
Q

Tyramine can cause a ___ crisis

A

Hypertensive

38
Q

Tyramine mechanism

A

Displaces NE from storage vesicles; increased cytosolic NE triggers it’s release by reverse transport through NET

39
Q

Patients on MAOIs need to have ____ restrictions to reduce intake of ____

A

Dietary; tyramine (wine and cheese effect)

40
Q

Methyldopa is a prodrug that is converted to ____

A

Methyl-NE

41
Q

Methyldopa MOA

A

Lowers BP by decreasing sympathetic outflow from the CNS to the heart, vasculature, and kidneys

42
Q

Methyldopa clinical use

A

Gestational hypertension

43
Q

Methyldopa side effects

A

Sedation
Dry mouth
Edema
Autoimmune hemolytic anemia (long term use)

44
Q

Pre-synaptic adrenergic receptor subtype

A

Alpha 2

45
Q

Post synaptic adrenergic receptor subtypes

A

Alpha 1, Beta 1,2, and 3

46
Q

All adrenergic receptors are coupled to ____

A

G Proteins

47
Q

Alpha 1 receptors are G_

A

Gq

48
Q

Alpha 2 receptors are G_

A

Gi

49
Q

All Beta receptors are G_

A

Gs

50
Q

Beta 1 receptors cause ___
Beta 2 receptors cause ___

A

Contraction
Relaxation

51
Q

Monoamine oxidase inhibitors (MAOIs) are used for:

A

Depression
Parkinson’s

52
Q

Cocaine blocks ____ from being reabsorbed

A

Norepinephrine

53
Q

____ clears circulating Catecholamines

A

Catecholo-methyltransferase (COMT)

54
Q

Major Catecholamine metabolite excreted in urine

A

VMA

UNMC PA Pharmacology (23 decks)

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