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CPR II > Cholinergic Agonists and Antagonists- Kruse > Flashcards

Cholinergic Agonists and Antagonists- Kruse Flashcards

(59 cards)

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1
Q

what is the parasympathetic neurotransmitter

A

Ach

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2
Q

what are the parasympathetic receptors

A

nAchR, mAChR

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3
Q

what are the sympathetic neurotransmitters

A

NE>Epi (DA) and Ach

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4
Q

what are the sympathetic receptors

A

alpha, beta, (D), nAchR, and mAChR

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5
Q

what are the 4 steps that occur at the cholinergic nerve terminal

A

1) ACh synthesis
2) ACh storage
3) ACh release
4) ACh destruction

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6
Q

what are the 4 steps that occur at the adrenergic nerve terminal

A

1) Synthesis
2) Storage
3) Release
4) Reuptake

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7
Q

two molecules that come together to synthesize Ach

A

AcCoA and Choline

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8
Q

Enzyme that synthesizes Ach

A

ChAT

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9
Q

Ach is stored in…

A

a vesicle

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10
Q

what stimulates the Ach vesicle to fuse and release the Ach

A

Ca2+

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11
Q

Ach is destroyed by

A

Acetylcholinesterase

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12
Q

enzyme that synthesizes dopa from tyrosine

is this outside/inside the vesicle

A

tyrosine hydroxylase

outside the vesicle

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13
Q

enzyme that synthesizes dopamine from dopa

is this outside/inside the vesicle

A

aromatic amino acid decarboxylase

outside the vesicle

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14
Q

dopamine is then stored in…

A

a vesicle

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15
Q

dopamine is converted to NE by…

A

dopamine Beta hydroxylase

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16
Q

what stimulates fusion of dopamine/NE vesicle

A

Ca2+

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17
Q

Once the catecholamines bind to receptor they are..

A

taken up again into the pre-synaptic cleft

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18
Q

M1, M3, and M5 are what type of GPCRs

A

Gq/11 that use the IP3, DAG cascade

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19
Q

M2 and M4 are what type of GPCRs

A

Gi/o that inhibit cAMP production

M2 also activates K+ channels

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20
Q

M1 main location?

A

nerves

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21
Q

M2 main locations?

A

heart, nerves, smooth muscle

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22
Q

M3 main locations?

A

glands, smooth muscle, endothelium

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23
Q

M4 and M5 main locations?

A

CNS

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24
Q

In most organs, except heart, which Muscarinic receptor is predominant

25
which M receptor is dominant in the heart
M2
26
two types of cholinergic agonists are?
direct-acting drugs and indirect-acting drugs (by inhibiting the action of acetylcholinesterase)
27
what are the 4 direct-acting cholinergic agonists that are uncharged and highly absorbed
Muscarine and Pilocarpine (action mainly at muscarinic) AND Nicotine and Lobeline (action mainly nicotinic)
28
what are the 4 direct-acting cholinergic agonists that are charged and poorly absorbed
Acetylcholine, Methacholine, Carbachol, and Bethanechol
29
What are the 3 groups of AChE inhibitors
Alcohols (reversible) Carbamic acid esters (reversible, but longer lasting than alcohols) Organophosphates (irreversible)
30
what are the 4 charged and poorly absorbed AChE inhibitors
Neostigmine, Carbaryl, Physostigmine, Edrophonium
31
what are the 6 uncharged and highly absorbed AChE inhibitors
Echothiophate, Soman, Parathion, Paraoxon, Malathion, Malaoxon
32
what is the treatment if there is toxicity due to the action of direct-acting cholinergic agonists
atropine and parenteral anticonvulsants
33
Use of Acetylcholine as a direct-acting agent
approved for intraocular use during surgery and causes miosis (reduction in pupil size)
34
Use of Bethanechol as a direct-acting agent
primarily affects urinary and GU tracts
35
Use of Carbachol as a direct-acting agent
treatment for glaucoma or produce miosis during surgery
36
Use of Cevimeline as a direct-acting agent
treats dry mouth (xerostomia) in patients with Sjogren
37
Use of Pilocarpine as a direct-acting agent
approved for xerostomia in pts with Sjogren, miosis during surgery, and glaucoma
38
What is the FDA approved drug for smoking cessation
Varenicline (Chantix)
39
Varenicline (Chantix) is...
a partial agonist that binds with high affinity and selectivity to nAChRs
40
MOA of Varenicline
sustained release of dopamine to help with withdrawl symptoms of smoking cessation
41
Adverse effects of Varenicline
nausea, neuropsychiatric symptoms
42
clinical uses of indirect-acting cholinergic agonists
Glaucoma, Dementia, Antidote to anticholinergic poisoning, Reversal of neuromuscular paralysis, Myasthenia gravis, AChE inhibitor toxicity(SLUDGE symptoms, effects on NMJ)
43
prototype antimuscarinic agent is...
atropine
44
drug used for motion sickness
scopolamine
45
drugs used for GI disorders
atropine, dicyclomine, glycopyrrolate, hyoscyamine
46
drugs used in opthalmology
atropine, cyclopentolate, homatropine, scopolamine, tropicamide
47
drugs for respiratory disorders
ipratropium, tiotropium
48
drugs for urinary disorders
Darifenacin, Oxybutynin, Solifenacin, Toterodine, Trspium
49
Drugs used for cholinergic poisoning
atropine and pralidoxime
50
drugs for movement disorders
benztropine, biperiden, orphenadrine, procyclidine, trihexyphenidyl
51
Anticholinergics for Parkinson
mAChR antagonists can reduce tremors not as effective as standard dopaminergic therapy tertiary amines benztropine, trihexyphenidyl, and procyclidine
52
Anticholinergics for motion sickness
Scopolamine
53
Anticholinergics for Anesthesia
Atropine given to block vagal reflexes induced by manipulation of visceral organs Atropine or glycopyrrolate paired with cholinesterase inhibitor to block parasympatheitc effects
54
anticholinergics for opthalmologic disorders
mAChR used for cycloplegia or prolonged mydriasis is required alpha adrenergic receptor agonists are shorter acting and have less adverse effects Homatropine and atropine used to prevent synechia formation in uveitis and iritis (long-acting agents)
55
Anticholinergics for respiratory disorders
asthma and COPD will use Ipratrpium and tiotropium; these are inhalation mAChR antagonists
56
Anticholinergics for GI disorders
mAChR antagonists treats Traveler's diarrhea often combined with opioid antidiarrheal drug to discourage abuse of opioid agent (ex. Lomotil - combo of atropine and diphenoxylate)
57
Anticholinergics for GU disorders
mAChR antagonists provide relief in urinary urgency agents are usually selective of the M3 subtype Oxybutynin is prototype selective M3 antagonist- has side effects of dry mouth, dizziness, constipation Darifenacin, Solifenacin, and Tolterodine are also selective for M3- have longer half-lives and reduced incidence of xerostomia and onstipation
58
anticholinergics for cholinergic poisoning
atropine given, no effective treatment at nAChR (pralidoxime) atropine useless in delayed onset mushroom poisoning
59
anticholinergics adverse effects and contraindications
glaucoma prostatic hyperplasia acid-peptic disease

CPR II (3 decks)

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