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Cholinergic Agents Flashcards

1
Q

Nicotine (mechanism)

A

Nicotinic ACh receptor agonist

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2
Q

Succinylcholine (mechanism)

A

Nicotinic ACh receptor agonist (Nm at neuromuscular jx)

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3
Q

Bethanechol (mechanism)

A

Muscarinic receptor agonist (predominantly M3)

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4
Q

Bethanechol (use)

A

Activate bowels and bladder

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5
Q

Succinylcholine (use)

A

Depolarizing blockade for brief paralysis during surgical procedure

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6
Q

Succinylcholine (metabolism)

A

By pseudocholinesterase, so effects can’t be reversed by AChE inhibitor

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7
Q

Succinylcholine (side effects)

A

Malignant hyperthermia
Exaggerated hyperkalemia leading to arrhythmias (life-threatening!) in pts w/ crush/burn injuries, denervating injuries (quadriplegia, Guillain-Barre), myopathies -> so use non-depolarizing one for these ppl instead

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8
Q

Carbachol (mechanism)

A

Nonselective cholinergic agonist (activates both nicotinic and muscarinic)

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9
Q

Carbachol (use)

A

Topically for eye stuff (glaucoma, pupillary constriction, relief of IOP)

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10
Q

Pilocarpine (mechanism)

A

Nonselective muscarinic agonist, but M3 effects predominate so it contracts ciliary m. and pupillary sphincter and is a potent stimulator of sweat, tears, saliva (you cry, drool, sweat on your PILOw)

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11
Q

Pilocarpine (use)

A

Topically for glaucoma (open-angle and closed-angle) - esp in emergency (very effective at opening meshwork into canal of Schlemm)

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12
Q

Methacholine (mechanism)

A

Nonselective muscarinic agonist

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13
Q

Methacholine (use)

A

Challenge for asthma dx

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14
Q

Neostigmine (mechanism)

A

AChE inhibitor

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15
Q

Neostigmine (3 uses/CNS penetration)

A
  1. myasthenia gravis
  2. reverse of nondepolarizing neuromuscular jx blockade OR phase II of depolarizing NMJ blockade
  3. postop ileus&urinary retention
    does NOT penetrate CNS
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16
Q

Pyridostigmine (mechanism)

A

AChE inhibitor

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17
Q

Pyridostigmine (use/CNS penetration)

A 
Myasthenia gravis (long acting)
does NOT penetrate CNS
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18
Q

Physostigmine (mechanism)

A

AChE inhibitor

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19
Q

Physostigmine (use/CNS penetration)

A

Fixes atropine overdose (fixes anticholinergic toxicity)

DOES cross CNS

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20
Q

Donepezil (mechanism)

A

AChE inhibitor

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21
Q

Donepezil (use)

A

One of Alzheimer drugs

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22
Q

Rivastigmine (mechanism)

A

AChE inhibitor

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23
Q

Rivastigmine (use)

A

One of Alzheimer drugs

24
Q

Galantamine (mechanism)

A

AChE inhibitor

25
Q

Galantamine (use)

A

One of Alzheimer drugs

26
Q

Edrophonium (mechanism)

A

AChE inhibitor

27
Q

Edrophonium (use)

A

Dx of myasthenia gravis historically (it’s now dx by anti-AChR Ab test)

28
Q

AChE inhibitors (side effects)

A

Exacerbation of COPD, asthma, peptic ulcers

29
Q

Organophosphates (mechanism/toxicity)

A

Irreversible AChE inhibitor
DUMBBELSS (diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal m. and CNS, lacrimation, sweating, salivation)

30
Q

Organophosphates/AChE inhibitors (antidote)

A

Atropine (competitive inhibitor) + pralidoxime (regenerates new AChE if given early)

31
Q

Atropine (mechanism)

A

Nonselective muscarinic ANTAgonist

32
Q

Atropine (3 uses)

A

Bradycardia, opthalmic (dilates pupil), fixes cholinergic crisis

33
Q

Hematropine (mechanism)

A

Nonselective muscarinic ANTAgonist

34
Q

Hematropine (use)

A

To produce mydriasis

35
Q

Advantage of a-agonists over anti-muscarinic agents when concerning their use to produce mydriasis?

A

a-agonists don’t produce cycloplegia at high doses like anti-muscarinic agents do

36
Q

Tropicamide (mechanism)

A

Nonselective muscarinic ANTAgonist

37
Q

Tropicamide (use)

A

To produce mydriasis

38
Q

Benztropine (mechanism/CNS penetration/use)

A

Can cross BBB to block muscarinic neurons in corpus striatum
Parkinson’s disease (improves tremor and rigidity, but little effect on bradykinesia -> good for drug-induced parkinson or those w/ tremor as the predominant sx)

39
Q

Atropine (side effects)

A

Hot as a hare, dry as a bone, red as a beet, blind as a bat (cycloplegia & mydriasis - can cause acute angle-closure glaucoma in eldery), mad as a hatter (disorientation), constipation

40
Q

Scopalamine (mechanism)

A

Nonselective muscarinic ANTAgonist

41
Q

Scopalamine (2 uses/CNS penetration)

A

Motion sickness, crosses BBB
Fixes problems created by myasthenia gravis drugs (help tone down anti-muscarinic effects so they can affect only the receptor that’s a problem - nicotinic receptor)

42
Q

Ipratropium (mechanism and 2 uses)

A 
Muscarinic ANTAgonist with predominant effects on M3 (SMC and glands)
For COPD (first line), asthma (second line) -> poorly absorbed systematically so less systemic effects
43
Q

Tiotropium (2 uses)

A

COPD, asthma

44
Q

Oxybutynin (mechanism and use)

A

Muscarinic ANTAgonist with predominant effects on M3 (SMC and glands)
Reduces urgency/bladder spasm

45
Q

“-fenacin” (mechanism/use)

A

Solifenacin, darifenacin
Muscarinic ANTAgonist
Reduces urgency/bladder spasm

46
Q

“-terodine” (mechanism/use)

A

Tolterodine, fesoterodine
Muscarinic ANTAgonist
Reduces urgency/bladder spasm

47
Q

Trospium (mechanism/use)

A

Muscarinic ANTAgonist

Reduces urgency/bladder spasm

48
Q

Glycopyrrolate (mechanism)

A

Nonselective muscarinic ANTAgonist

49
Q

Glycopyrrolate (2 uses)

A

REDUCES SECRETIONS

  • Pre-op to reduce airway secretions and salivation
  • Peptic ulcers
50
Q

Antimuscarinic/anticholinergic (antidotes)

A

Physostigmine salicylate (AChE inhibitor that crosses BBB)

51
Q

Pilocarpine (side effects)

A

Miosis and cyclospasm (don’t have this w/ B-blocker glaucoma med)

52
Q

Carbachol (side effects)

A

Miosis and cyclospasm (don’t have this w/ B-blocker glaucoma med)

53
Q

Trihexyphenidyl (mechanism and use)

A 
Antimuscarinic
For Parkinson (esp drug-induced or those w/ tremor as the prominent sx)
54
Q

Digitalis (antidote)

A

Potassium (to correct hypokalemia if present)

55
Q

Hemicholinium (mechanism)

A

Blocks choline uptake -> prevents ACh synthesis

56
Q

Bromoacetylcholine (mechanism)

A

Blocks choline acetyltransferase -> can’t make ACh

57
Q

Vesamicol (mechanism)

A

Competitively blocks vesicular ACh transporter -> prevents ACh from entering secretory vesicles

Pharmacology (12 decks)

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