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Therapeutics > Cholinergic Agonists > Flashcards

Cholinergic Agonists Flashcards

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
Q

What is the effect of B substitutions on acetylcholine?

A

reduce AChE activity; more selective for Muscarinic

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26
Q

What is the effect of a substitutions on acetylcholine?

A

selective for Nicotinic

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27
Q

What is the effect of carbamate group on ACh?

A

resistant to AChE

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28
Q

Alkaloids

A

muscarine, nicotine, pilocarpine

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29
Q

pilocarpine indication & effects

A

glaucoma; promotes sweating, urination, urination, and salivation

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30
Q

Pilocarpine receptor & clinical use

A

M3 agonist; promotes outflow of aqueous humor (glaucoma), xerostomia

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31
Q

Bethanechol clinical use

A

GI stimulation; treatment of urinary retention

32
Q

methacholine clinical use

A

test for hyperreactive airways

33
Q

carbachol clinical use

A

ocular (surgery, glaucoma)

34
Q

Side effects of muscarinic receptor direct agonists

A

DUMBBELS- diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation, salivation, sweating

35
Q

muscarinic receptor direct agonist contraindications

A

asthma, coronary insufficiency, peptic ulcer

36
Q

nicotinic receptor locations

A

skeletal muscle endplate (Nm), Autonomic ganglia (Nn), Brain (CNS) (Nn)

37
Q

varenicline indication (chantix)

A

smoking cessation

38
Q

Varenicline MOA

A

Nicotinic receptor partial agonist (CNS)

39
Q

Bupropion (wellbutrin) Indication

A

smoking cessation (nicotinic receptor partial agonist)

40
Q

What does AChE do?

A

hydrolyzes (inactivates) ACh using catalytic triad; has an anionic site and esteratic site to bind to ACh

41
Q

reversible anticholinesterase agents (categories)

A

alcohol, carbamates, other (donepezil)

42
Q

irreversible anticholinesterase agents

A

organophosphates

43
Q

Edrophonium

A

Quaternary ammonium alcohol

44
Q

pralidoxime action

A

hydrolyzes organophosphate & regenerates AChE

45
Q

pralidoxime clinical use

A

used for organophosphate poisoning (pesticide + nerve gas)

46
Q

Atropine class/ action

A

muscarinic receptor antagonist (especially in CNS)

47
Q

Atropine clinical use

A

used in conjunction with pralidoxime for organophosphate poisoning; helps with overstim. of cholinergic receptors.

48
Q

Donepezil class/action

A

AChE inhibitor

49
Q

Donepezil clinical use

A

Treats symptoms of alzheimers; crosses the BBB

50
Q

Rivastigmine/Epastigmine class/action

A

reversible AChE inhibitor
crosses the BBB

51
Q

Rivastigmine/ Epastigmine clinical use

A

Alzheimer’s Disease

52
Q

Galantamine class/action

A

Reversible competitive AChE inhibitor, may be a nicotinic receptor agonist

53
Q

Galantamine clinical use

A

Treatment of Alzheimers

54
Q

Memantine class/action

A

NMDA receptor antagonist (not cholinergic)

55
Q

Memantine clinical use

A

Slows progression of Alzheimers; often used with donepezil

56
Q

edrophonium clinical use/ action

A

Reversible AChE inhibitor; diagnostic for myasthenia gravis

57
Q

neostigmine clinical use/action

A

Reversible AChE inhibitor; Myasthenia gravis, bladder distension, used in surgery

58
Q

physostigmine clinical use/action

A

reversible AChE inhibitor; glaucoma, alzheimers, antidote to anticholinergic overdose

59
Q

Donepezil clinical use/action

A

reversible AChE inhibitor; Alzheimer’s disease

60
Q

Echothiophate clinical use/action

A

irreversible AChE inhibitor; glaucoma

61
Q

Cholinergic Agent side effects

A

SLUD- salivation, lacrimation, urination, defecation

62
Q

Treatment for Cholinergic Agent side effects

A

cholinergic receptor antagonist (Atropine)
for irreversible AChE inhibitor, (Pralidoxime)

63
Q

Contraindications to parasympathomimetic drugs

A

Asthma and COPD, coronary deficiency, peptic ulcer, obstruction of urinary or GI tract, epilepsy

64
Q

atropine action

A

competitive muscarinic receptor antagonist

65
Q

atropine selectivity

A

Muscarinic&raquo_space; Nicotinic
active at M1, M2, and M3

66
Q

Classes of Muscarinic Antagonists

A

Tertiary Amines, Quaternary Amines

67
Q

What are tertiary amine muscarinic antagonists used for clinically?

A

Ocular and CNS applications

68
Q

What are quaternary amine muscarinic antagonists used for clinically?

A

GI tract and peripheral (no BBB access)

69
Q

Atropine/Scopolamine -ine’s

A

Muscarinic antagonists; used for motion sickness

70
Q

Ipratropium/ tiotropium

A

derivative of belladonna alkaloids – muscarinic antagonist

71
Q

benztropine

A

tertiary amine; used for parkinson’s disease (side effect: sedative activity)

72
Q

Ipatropium

A

COPD and asthma (M3 antagonist; opens the airway)

73
Q

glycopyrrolate use

A

Pre-op to reduce secretions (anti-muscarinic)

74
Q

Tolterodine

A

used for overactive bladder; M3 antagonist (M3 selective)

75
Q

M3 selective muscarinic antagonists for OAB

A

Solifenacin, Oxybutynin, and Darifenacin

76
Q

Neuromuscular blocking drugs

A

anti-nicotinic; look like ACh

Therapeutics (7 decks)

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