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IC > 1.3 Cholinergic Pharmacology > Flashcards

1.3 Cholinergic Pharmacology Flashcards

1
Q

_______ cholinomimetic agents directly bind and activate muscarinic or nicotinic receptors

A

direct acting

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2
Q

________ agents inhibit acetylcholinesterase, reduce hydrolysis of acetylcholine, increase endogenous Ach concentration in synpatic clefts, stimulates cholinoceptors to evoke increased responses

A

indirect acting

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3
Q

cholinoceptors are either ________ linked (muscarinic) or ________ (nicotinic)

A

G protein linked

ion channels

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4
Q

G protein linked cholinoceptors, located in CNS/tissues targeted by PNS, and vascular endothelium

A

muscarinic receptors

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5
Q

ion channels with receptors located on all ANS postganglionic cells, and muscles, result in electrical changes, prolonged agonist abolishes effector b/c we can diminish the electrochemical gradient (depolarizing blockade)

A

nicotinic receptors

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6
Q
  • esters of choline or alkaloids

- choline esters: quaternary, insoluble in lipids, poorly distributed to CNS

A

direct acting cholinoceptor agonists

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7
Q

choline ester with exclusively muscarinic action?

A

methacholine chloride

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8
Q

choline esters with duration of action much longer than Ach, negligible susceptibility to cholinesterase?

A

carbachol chloride and bethanechol chloride

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9
Q

pilocarpine, nicotine, and lobeline are _______ cholinomimetic alkaloids with CNS activity, more lipophilic than choline esterss

A

tertiary

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10
Q
  • all _______ receptors are G protein coupled
  • agonist binding activates IP3, DAG cascade, increases potassium flux
  • in some tissues inhibits adenylyl cyclase activity and opens K+ channels
A

muscarinic

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11
Q
  • _______ receptor activation results in electrical and ionic hcanges
  • depolarization of nerve cell or neuromuscular end plate membrane
  • prolonged agonist occupany abolishes effector response, depolarizing blockage, and can produce muscle paralysis
A

nicotinic

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12
Q

-______ agonists in the eye produce contraction of iris (miosis), contraction of ciliary muscle (accommodation), and facilitiates aqueous humor outflow

A

muscarinic

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13
Q

muscarinic agonists in CV system ______ peripheral vasculature resistance, and direct effect is to ____ heart rate

A

reduce

slow

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14
Q

IV infusions of acetylcholine caused vasodilation and reduce ______, by releasing _______ that relaxes smooth muscle

A

blood pressure

nitric oxide

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15
Q

muscarinic ________ evokes SNS reflex, increase in heart rate
-larger Ach doses mask this reflex

A

vasodilation

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16
Q

cholinergic effects on respiratory system:

  • ____ smooth muscle of bronchial tree
  • glands of mucosa stimulated to secrete
  • _______ symptoms of asthma
A

contracts

exacerbates

17
Q

cholinergic effects on GI tract:

  • increases secretions and _____ activity
  • contracts _______ muscle and relaxes sphincters
A

peristaltic

longitudinal

18
Q

cholinergic effects on GU tract:

  • ______ detrusor muscle
  • ______ trigone and sphincter muscles
  • promotes voiding
A

contracts

relaxes

19
Q

cholinergic effects on secretory glands:

-_______ of secretion by thermoregulatory sweat glands

A

stimulation

20
Q

major site of action of nicotinic agonists with simulatenous SNS and PNS discharge?

A

autonomic ganglia

21
Q
  • only activates vascular muscarinic receptors (endothelium)
  • NO, vasodilation, reflex tachycardia
  • effects blocked by atropine (muscarinic antagonist)
A

low dose acetylcholine

22
Q
  • activates M receptors on vascular endothelial cells (NO, vasodilation)
  • activates cardiac M receptors (profound bradycardia, slows AV conduction, reduces force of myocardial contractions)
A

high dose acetylcholine

23
Q

a simple alcohol bearing a quaternary ammonium group,indirect cholinmimetic (inhibits acetylcholinesterase)

A

edrophonium

24
Q
  • carbamic acid esters of alcohols, carbamates

- indirect cholinomimetic, 30 min-6hrs inhibition

A

neostigmine, physostigmine, carbaryl (rapid CNS effects)

25
Q

echothiphate, soman, sarin, malathion, parathion are _______, which are organic derivatives of phosphoric acid, indirect cholinomimetics

A

insecticides

26
Q

organophosphates bind and are hydrolyzed, resulting in a phosphorylated AchE active site, bond extremely stable
-before aging, _______ can restore function

A

2-pralidoxime (2-PAM)

27
Q

cholinesterase inhibitors for closed angle glaucoma reduce intraocular pressure by _________ of the ciliary body, facilitating outflow of aqueous humor

A

contraction

28
Q

cholinesterase ________ used for postop ileus, congenital megacolon, urinary retention, reflux esophagitis, insufficient salivary secretion

A

inhibitors

29
Q

drug used for reversal of competitive blockade by cholinomimetics, a muscarinic antagonist

A

atropine

30
Q
  • fatal dose 40mg, emetic
  • CNS stimulation - convulsions, coma, respiratory arrest
  • respiratory paralysis
  • HTN, cardiac arrhythmias
  • treatment: M and adrenergic antagonists
A

nicotinic toxicity

31
Q
  • acetylcholine
  • bethanechol
  • carbachol
  • cevimeline
A

direct muscarinic agonists, choline esters

32
Q

muscarine

pilocarpine

A

direct muscarinic agonist, alkaloids

33
Q

nicotine

varenicline

A

direct nicotinic agonist

34
Q 
neostigmine
physostigmine
pyridostigmine
reivastigmine
ambenonium
demecarium
carbaryl
A

carbamates, cholinesterase inhibitors

35
Q 
echothiphate
soman
sarin
parathion
malathion
isoflurophate
DFP
A

organophosphates, cholinesterase inhibitors

IC (29 decks)

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