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Pharm Exam 1 > 7- Cholinomimetric Drugs > Flashcards

7- Cholinomimetric Drugs Flashcards

1
Q

bind directly to and activate muscarinic or nicotinic cholinoceptos

A

direct-acting cholinomimetics

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2
Q

produce their effects by inhibiting the action of acetylcholinesterase, thus preventing the destruction of endogenous Ach

A

indirect-acting cholinomimetics

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3
Q

direct acting muscarinic agonists (6)

A 
Acetylcholine
Methacholine
Carbachol
Bethanechol
Muscarine
Pilocarpine
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4
Q

direct acting muscarinic agoinst that are choline esters (4)

A

acetylcholine
methacholine
carbachol
bethanechol

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5
Q

direct acting muscarinic agonist that are alkaloids (2)

A

muscarine

pilocarpine

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6
Q

direct acting alkaloid cholinoceptors (4)

A

muscarine
pilocarpine
nicotine
succinylcholine

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7
Q

indirect acting reversible cholinesterase inhbitors (5)

A 
edrophonium
neostigmine
physostigmine
denepezil
tacrine
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8
Q

indirect acting irreversible organophosphate cholinesterase inhibitors (4)

A

echothiphate
malathion
parathion
sarin

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9
Q

why do choline esters have poor GI absorption and poor CNS distribution?

A

cationic quaternary ammonium compounds that make them insoluble in lipid

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10
Q

which of the choline esters have methyl groups giving them a longer half life?

A

methacholine and bethanechol

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11
Q

which of the choline esters are insusceptible to cholinesterase?

A

carbachol and bethanechol

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12
Q

effects of choline esters on the cardiovascular system

A
  • hypotension from direct vasodilation
  • bradycardia at high doses
  • slowed conduction and prolonged refractory period of AV node
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13
Q

effects of choline esters on GI system

A
  • increased tone and increased contractile activity of gut
  • increased acid secretion
  • nausea, vomiting, cramps, and diarrhea
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14
Q

effects of choline esters on genitourinary tract

A

involuntary urination from increased bladder motility and relaxation of sphincter

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15
Q

effects of choline esters on eye

A

miosis: contraction of sphincter muscle, resulting in reduced intraocular pressure

contraction of ciliary muscle; accomodated for near vision

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16
Q

effects of choline esters on respiratory system

A

bronchoconstriction

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17
Q

effects of choline esters on glands

A

increased secretory activity, resulting in increased salivation, lacrimation and sweating

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18
Q

Ach: _______ destruction by AchE

A

rapid

–> limited clinical use

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19
Q

muscarinic effects of Ach

A

cardio - low doses = vasodilation –> tachycardia
high doses = bradycardia; decreased AV conduction and negative inotropy

bronchial constricition and increased secretion

salivary excretion, tears, sweat

urinary bladder contraction

short lasting miosis in eye

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20
Q

nicotinic effects of Ach

A

not commonly seen since Ach does not penetrate the fat surrounding skeletal muscle and autonomic ganglia

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21
Q

clinical use of Ach

A

eye surgery (short-lasting miosis)

provocation test in coronary angiography (dx coronary vasospasm)

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22
Q

how does methacholine compare to Ach

A

similar in action

longer half life

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23
Q

diagnosis of bronchiolar hypersensitivity:

A

methacholine challenge

excessive bronchoconstriction via M3 receptors in bronchial muscle in asthmatic pts.

24
Q

therapeutic doses of carbachol

A

both nicotinic and muscarinc effects

25
Q

high doses of carbachol

A

may induce cardiac arrest

26
Q

topical application for glaucoma

A

carbachol

contracts ciliary muscle which enlarges canal of schlemm and increases drainage of aqueous humor and decreases intraocular pressure

27
Q

what are the indications for bethanechol?

A

-gastric atony (after vagotomy to reduce reflux; increases lower esophageal tone)

  • gastric emptying abnormalitie
  • urinary retention (in absence of obstruction)
28
Q

where does bethanechol predominately act?

A

M3

29
Q

effects on bethanechol on genitourinary and gastrointestinal tract?

A

increase detrusor tone, decrease outlet resistance of internal sphincter

increase motility and secretion

30
Q

does muscarine have nicotinic acitivity?

A

no

31
Q

signs of muscarine poisoning

A

salivation, sweat, tear flow

abdominal pain, nausea, diarrhea, blurred vision, dyspnea

symptoms subside w/i 2 hrs

severe may lead to death

32
Q

which is more potent muscarine or Ach?

A

muscarine (100x)

also longer duration of action than Ach because not broken down by AchE

33
Q

Pilocarpine predominate effects

A

opthalmic via M3

contracts iris sphincter muscles –> miosis

frees entrance to canal of Schlemm (therapy ofr narrow-angle glaucoma)

enhances tone of trabecular network (therapy for wide-angle glacuoma)

contract ciliary muscle for accommmodation and loss of far vision

34
Q

drug of choice for glaucoma

A

pilocarpine

35
Q

what does a pilocarpine hypersensitivity indicate?

A

PANS dysfunction

test on autonomic state

36
Q

why is pilocarpine given for xerostomia?

A

given orally to stimualte saliva secretion

37
Q

contraindications for direct acting cholinoceptor agonists

A

peptic ulcers

GI tract disorders

asthma

38
Q

drug interactions with anti-muscarinc properties (do not use with direct acting cholinoceptor agonists)

A

quinidine (antiarrhythmics)

procainamide (antiarrhythmics)

tricyclic antidepressants

39
Q

prototypical agonist for nAch receptors

A

nicotine

40
Q

action of nicotine on Nm receptors

A
  • skeletal muscle contraction
  • fasiculations, spasm
  • depolarizing blockade
41
Q

action of nicotine on Nn receptors

A

increased HR
both symp and para effects depending on system

peripheral vasoconstriciton

increased gut motility and secretion

increased RR

nausea and vomiting via emetic chemoreceptors

42
Q

clinical indication for nicotine

A

aid smoking cessation

43
Q

used to differentiate myasthenia from cholinergic crisis

A

edrophonium

  • will show imporvement
  • short acting
44
Q

do neostigmine and pyridostigmine go into the CNS?

A

no (quartenary amines)

45
Q

what are the clinical uses for neostigmine and pyridostigmine

A

ileus, urinary retention, myasthenia, reversal of non-depolarizing NM blockers

46
Q

does physostigmine enter the CNS?

A

yes (tertiary amine)

47
Q

clinical use for physostigmine

A

glaucoma

48
Q

antidote in atropine overdose

A

physostigmine

49
Q

do donepezil and tacrine enter CNS?

A

yes - lipid soluble

50
Q

clincal use donepezil and tacrine

A

alzheimer disease

51
Q

nerve gas

A

sarin

52
Q

malathion and parathion are…

A

insecticides

53
Q

which of the organophosphates has clinical use?

A

echothiophosphate for glaucoma

this group has limited clinical use because they are irreversible inhibtors of AchE

54
Q

DUMBBELSS

A

symptoms of intoxication of cholinesterase inhibitors

diarrhea
urination
miosis
bronchiolar constriction
bradycardia
excitement
lacrimation
sweating 
salivation
55
Q

antidote for cholinesterase inhbitor intoxication

A

atropine (muscarinc receptor agonist)

56
Q

what drug could be used to regenerate AchE?

A

pralidoxim aka 2PAM

Pharm Exam 1 (16 decks)

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