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Cholinergic Agonists Flashcards

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1
Q

Action of direct cholinergic agonists

A

activate cholinoceptors

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2
Q

Action(s) of indirect cholinergic agonists

A
  • stimulate release of acetylcholine
  • inhibit acetylcholinesterase
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3
Q

What tissues are Nm receptors found in, what is the response, what is the mechanism?

A

skeletal muscle; depolarization and contraction; ligand-gated opening of Na/K channel

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4
Q

What tissues are Nn receptors found in, what is the response, and what is the mechanism?

A

Found in the ganglions (post-ganglionic); depolarization; ligand-gated opening of Na/K channel
Found in adrenal medulla; catecholamine secretion; ligand-gated opening of Na/K channel

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5
Q

What type of receptor does acetylcholine have the highest affinity for?

A

Muscarinic» Nicotinic

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6
Q

What tissues are M1 receptors found in , what is the response, and what is the mechanism?

A

Post-ganglionic receptors, depolarization, Gq

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7
Q

What tissues are M2 receptors found in, what is the response, and what is the mechanism?

A

Heart, inhibition, Gi (activates K+ channels)

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8
Q

What tissues are M3 receptors found in, what is the response, and what is the mechanism?

A

smooth muscle, exocrine glands, epithelium; contraction, secretion, and relaxation; Gq

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9
Q

What is the endogenous neurotransmitter for Muscarinic receptors?

A

acetylcholine

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10
Q

Main structural components of acetylcholine?

A

Acetyl group (ester) + choline group (charged quaternary amine)

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11
Q

exogenous cholinergic neurotransmitters

A

muscarine & nicotine

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12
Q

muscarine poisoning symptoms

A

bradycardia, nausea, cramps, vomiting, diarrhea, bronchoconstriction, salivation, visual disturbances, sweating, hypotension

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13
Q

can muscarine cross the BBB?

A

no

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14
Q

Direct acting cholinergic agonist classes

A

Choline esters, alkaloids

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15
Q

Indirect acting cholinergic agonist classes

A

reversible & irreversible; organophosphates & stigmines

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16
Q

Muscarinic agonist effect in the heart

A

M2 activation = decreased HR, conduction, and force

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17
Q

Muscarinic agonist effect in exocrine glands

A

M3 activation = increase in secretion

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18
Q

Muscarinic agonist effect in smooth muscles

A

M3 activation = increase in contraction

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19
Q

Muscarinic agonist effect in sphincters

A

M3 activation = relaxation

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20
Q

Muscarinic agonist effect in CNS

A

only by M1 activation = tremor, hypothermia, locomotor activity, improved cognition

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21
Q

Carbachol class

A

direct acting cholinergic receptor agonist; esters

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22
Q

methacholine class

A

direct acting cholinergic receptor agonist; esters

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23
Q

bethanechol class

A

direct acting cholinergic receptor agonist; esters

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24
Q

What receptors are ACh and carbachol active on?

A

both n and m

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25
What is the effect of B substitutions on acetylcholine?
reduce AChE activity; more selective for Muscarinic
26
What is the effect of a substitutions on acetylcholine?
selective for Nicotinic
27
What is the effect of carbamate group on ACh?
resistant to AChE
28
Alkaloids
muscarine, nicotine, pilocarpine
29
pilocarpine indication & effects
glaucoma; promotes sweating, urination, urination, and salivation
30
Pilocarpine receptor & clinical use
M3 agonist; promotes outflow of aqueous humor (glaucoma), xerostomia
31
Bethanechol clinical use
GI stimulation; treatment of urinary retention
32
methacholine clinical use
test for hyperreactive airways
33
carbachol clinical use
ocular (surgery, glaucoma)
34
Side effects of muscarinic receptor direct agonists
DUMBBELS- diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation, salivation, sweating
35
muscarinic receptor direct agonist contraindications
asthma, coronary insufficiency, peptic ulcer
36
nicotinic receptor locations
skeletal muscle endplate (Nm), Autonomic ganglia (Nn), Brain (CNS) (Nn)
37
varenicline indication (chantix)
smoking cessation
38
Varenicline MOA
Nicotinic receptor partial agonist (CNS)
39
Bupropion (wellbutrin) Indication
smoking cessation (nicotinic receptor partial agonist)
40
What does AChE do?
hydrolyzes (inactivates) ACh using catalytic triad; has an anionic site and esteratic site to bind to ACh
41
reversible anticholinesterase agents (categories)
alcohol, carbamates, other (donepezil)
42
irreversible anticholinesterase agents
organophosphates
43
Edrophonium
Quaternary ammonium alcohol
44
pralidoxime action
hydrolyzes organophosphate & regenerates AChE
45
pralidoxime clinical use
used for organophosphate poisoning (pesticide + nerve gas)
46
Atropine class/ action
muscarinic receptor antagonist (especially in CNS)
47
Atropine clinical use
used in conjunction with pralidoxime for organophosphate poisoning; helps with overstim. of cholinergic receptors.
48
Donepezil class/action
AChE inhibitor
49
Donepezil clinical use
Treats symptoms of alzheimers; crosses the BBB
50
Rivastigmine/Epastigmine class/action
reversible AChE inhibitor crosses the BBB
51
Rivastigmine/ Epastigmine clinical use
Alzheimer's Disease
52
Galantamine class/action
Reversible competitive AChE inhibitor, may be a nicotinic receptor agonist
53
Galantamine clinical use
Treatment of Alzheimers
54
Memantine class/action
NMDA receptor antagonist (not cholinergic)
55
Memantine clinical use
Slows progression of Alzheimers; often used with donepezil
56
edrophonium clinical use/ action
Reversible AChE inhibitor; diagnostic for myasthenia gravis
57
neostigmine clinical use/action
Reversible AChE inhibitor; Myasthenia gravis, bladder distension, used in surgery
58
physostigmine clinical use/action
reversible AChE inhibitor; glaucoma, alzheimers, antidote to anticholinergic overdose
59
Donepezil clinical use/action
reversible AChE inhibitor; Alzheimer's disease
60
Echothiophate clinical use/action
irreversible AChE inhibitor; glaucoma
61
Cholinergic Agent side effects
SLUD- salivation, lacrimation, urination, defecation
62
Treatment for Cholinergic Agent side effects
cholinergic receptor antagonist (Atropine) for irreversible AChE inhibitor, (Pralidoxime)
63
Contraindications to parasympathomimetic drugs
Asthma and COPD, coronary deficiency, peptic ulcer, obstruction of urinary or GI tract, epilepsy
64
atropine action
competitive muscarinic receptor antagonist
65
atropine selectivity
Muscarinic >> Nicotinic active at M1, M2, and M3
66
Classes of Muscarinic Antagonists
Tertiary Amines, Quaternary Amines
67
What are tertiary amine muscarinic antagonists used for clinically?
Ocular and CNS applications
68
What are quaternary amine muscarinic antagonists used for clinically?
GI tract and peripheral (no BBB access)
69
Atropine/Scopolamine -ine's
Muscarinic antagonists; used for motion sickness
70
Ipratropium/ tiotropium
derivative of belladonna alkaloids -- muscarinic antagonist
71
benztropine
tertiary amine; used for parkinson's disease (side effect: sedative activity)
72
Ipatropium
COPD and asthma (M3 antagonist; opens the airway)
73
glycopyrrolate use
Pre-op to reduce secretions (anti-muscarinic)
74
Tolterodine
used for overactive bladder; M3 antagonist (M3 selective)
75
M3 selective muscarinic antagonists for OAB
Solifenacin, Oxybutynin, and Darifenacin
76
Neuromuscular blocking drugs
anti-nicotinic; look like ACh

Therapeutics (7 decks)

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