cholinomimetics Flashcards

1
Q

name two direct agonists that are receptor nonspecific

A
  • ACh

- carbachol

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2
Q

name three direct agonists that are muscarinics

A
  • methacholine
  • bethanechol
  • pilocarpine
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3
Q

name three direct agonists that are nicotinic

A
  • nicotine

- varenicline

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4
Q

name a short acting cholinesterase inhibitor (cholinomimetic)

A

edrophonium

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5
Q

name two intermediate acting cholinesterase inhibitors (carbamates)

A
  • neostigmine

- physostigmine

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6
Q

name five long acting cholinesterase inhibitors (organophosphates)

A
  • echothiophate
  • parathion
  • malathion
  • sarin
  • soman
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7
Q

name a presynaptic indirect cholinomimetic

A

metoclopramide

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8
Q

what is the one exception to the rule that sympathetics are stimulated by NE?

A

sympathetic sweat glands are stimulated by ACh

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9
Q

what clears ACh from blood quickly?

A

plasma pseudocholinesterase

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10
Q

where are muscarinic (M) receptors found?

A

1) effector tissues innervated by PS fibers
2) select post ganglionic sympathetic targets (sweat glands)
3) endothelium

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11
Q

what are the expected physiological signs of muscarinic receptor agonism?

A

1) hypotension

2) paradoxical bradycardia (when there should be tachycardia)

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12
Q

what does DUMBBELSS stand for?

A
clinical signs of muscarinic activation
Diarrhea
Urination
Miosis (contraction of iris)
Bronchorrhea
Bradycardia
Emesis (increased stomach and GI tone)
Lacrimation (tearing)
Salivation
Sweating
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13
Q

what are the two nicotinic receptors and where are they found?

A

1) Nn found in all autonomic ganglia and in CNS

2) Nm found at NMJ on skeletal muscle

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14
Q

nicotinic receptors are what kind of channel?

A

ligand gated Na/K channels, depolarization triggers action potential

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15
Q

what is the main result of nicotine toxicity?

A

1) PSANS and SANS stimulation
2) paradoxical flaccid paralysis due to ACh inhabiting receptors for prolonged period, cannot be practically reversed, must wait for agonist to clear on its own

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16
Q

how is methacholine used clinically?

A

1) asthma airway challenge

17
Q

how is bethanechol used? what replaced it?

A
  • was used to relieve GI dysmotility

- replaced by metoclopramide

18
Q

how is pilocarpine used clinically?

A

topically in the eye to relieve glaucoma

19
Q

what is the only direct acting nicotinic agonist aside from nicotine and what is it used for?

A

varenicline, smoking cessation

20
Q

how does varenicline work?

A
  • prevents dopamine surges (no chemical reward) and also prevents low dopamine and cravings
  • it stimulates nicotinic receptors less than nicotine does
21
Q

side effects of varenicline

A
  • suicidal thoughts

- neuropsychiatric symptoms

22
Q

how is varenicline secreted?

A

urine

23
Q

what do all ChE inhibitors block?

A

1) plasma ChE
2) AChE
3) RBC AChE

plasma ChE is inhibited first which protects AChE at first

24
Q

What are AChE inhibitor side effects?

A

DUMBBELSS, same as muscarinic agonists

25
Q

what is the major hazard of AChE inhibitor overdose?

A

respiratory inundation

1) paralysis of intercostals and diaphragm
2) increase in bronchial secretions
3) central resp arrest

26
Q

what is the chemical significance of short acting AChE inhibitors?

A

they are competitive inhibitors and do not form ester bonds to AChE

27
Q

edrophonium cross BBB?

A

no

28
Q

edrophonium how given?

A

IV or IM

29
Q

edrophonium half life

A

extremely short (minutes)

30
Q

how is edrophonium used clinically?

A

to Dx myasthenia gravis, patients notice rapid increase in muscle strength

31
Q

physostigmine cross BBB?

A

yes

32
Q

clinical use of physostigmine

A

occasionally used to treat CNS signs of muscarinic blockers

33
Q

neostigmine cross BBB?

A

no, because designed with quaternary ammonium group

34
Q

clinical use of neostigmine?

A
  • myasthenia gravis

- treatment is an exercise in brinksmanship

35
Q

echothiophate clinical use

A

was used to treat narrow angle glaucoma but largely replaced

36
Q

malathion and parathion

A

insecticides

37
Q

sarin and soman

A

nerve gas, weapons of mass destruction

38
Q

how would we treat organophosphate poisoning?

A
  • muscarinic blockers such as atropine to manage DUMBBELSS/SLUDGE
  • pralidozime (2-PAM) is the antidote
39
Q

how is carbachol classified?

A

receptor non-specific direct acting cholinomimetic