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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
Galantamine (use)
One of Alzheimer drugs
26
Edrophonium (mechanism)
AChE inhibitor
27
Edrophonium (use)
Dx of myasthenia gravis historically (it's now dx by anti-AChR Ab test)
28
AChE inhibitors (side effects)
Exacerbation of COPD, asthma, peptic ulcers
29
Organophosphates (mechanism/toxicity)
Irreversible AChE inhibitor DUMBBELSS (diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skeletal m. and CNS, lacrimation, sweating, salivation)
30
Organophosphates/AChE inhibitors (antidote)
Atropine (competitive inhibitor) + pralidoxime (regenerates new AChE if given early)
31
Atropine (mechanism)
Nonselective muscarinic ANTAgonist
32
Atropine (3 uses)
Bradycardia, opthalmic (dilates pupil), fixes cholinergic crisis
33
Hematropine (mechanism)
Nonselective muscarinic ANTAgonist
34
Hematropine (use)
To produce mydriasis
35
Advantage of a-agonists over anti-muscarinic agents when concerning their use to produce mydriasis?
a-agonists don't produce cycloplegia at high doses like anti-muscarinic agents do
36
Tropicamide (mechanism)
Nonselective muscarinic ANTAgonist
37
Tropicamide (use)
To produce mydriasis
38
Benztropine (mechanism/CNS penetration/use)
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
Atropine (side effects)
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
Scopalamine (mechanism)
Nonselective muscarinic ANTAgonist
41
Scopalamine (2 uses/CNS penetration)
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
Ipratropium (mechanism and 2 uses)
``` 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
Tiotropium (2 uses)
COPD, asthma
44
Oxybutynin (mechanism and use)
Muscarinic ANTAgonist with predominant effects on M3 (SMC and glands) Reduces urgency/bladder spasm
45
"-fenacin" (mechanism/use)
Solifenacin, darifenacin Muscarinic ANTAgonist Reduces urgency/bladder spasm
46
"-terodine" (mechanism/use)
Tolterodine, fesoterodine Muscarinic ANTAgonist Reduces urgency/bladder spasm
47
Trospium (mechanism/use)
Muscarinic ANTAgonist | Reduces urgency/bladder spasm
48
Glycopyrrolate (mechanism)
Nonselective muscarinic ANTAgonist
49
Glycopyrrolate (2 uses)
REDUCES SECRETIONS - Pre-op to reduce airway secretions and salivation - Peptic ulcers
50
Antimuscarinic/anticholinergic (antidotes)
Physostigmine salicylate (AChE inhibitor that crosses BBB)
51
Pilocarpine (side effects)
Miosis and cyclospasm (don't have this w/ B-blocker glaucoma med)
52
Carbachol (side effects)
Miosis and cyclospasm (don't have this w/ B-blocker glaucoma med)
53
Trihexyphenidyl (mechanism and use)
``` Antimuscarinic For Parkinson (esp drug-induced or those w/ tremor as the prominent sx) ```
54
Digitalis (antidote)
Potassium (to correct hypokalemia if present)
55
Hemicholinium (mechanism)
Blocks choline uptake -> prevents ACh synthesis
56
Bromoacetylcholine (mechanism)
Blocks choline acetyltransferase -> can't make ACh
57
Vesamicol (mechanism)
Competitively blocks vesicular ACh transporter -> prevents ACh from entering secretory vesicles

Pharmacology (12 decks)

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