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Pharmacology > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

Atropine SEs

A

Atropine flush: cutaneous vasodilation
Anti-PANS: dry mouth, blurred vision, dry eyes, tachycardia, constipation
CNS: restless, confusion, hallucination, delirium, depression

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2
Q

Parathion

A

Chem: organophosphate
Metabolism: phosphorylation enzyme, hydrolyzes v slowly
Risk: farmers
(More dangerous of the 2)

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3
Q

Carbachol

A

Chem: choline ester
Target: nicotenic and muscarinic
Metabolism: resistant to hydrolysis by AChE
Use: miosis during surgery, dec IOP s/p cataract surgery

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4
Q

Ipratropium and Tiotropium

A

Chem: wuarternary ammonium muscarinic antagonist
Use: tx COPD and asthma

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5
Q

Pyridostigmine

A

Chem: carbamate / quaternary ammonium (No CNS)
Metabolism: covalent bond formed w/ enzyme
Use: treats Myasthenia Gravis (most common)

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6
Q

Physostigmine

A

Chem: carbamate / tertiary amine (= CNS entry)
Metabolism: covalent bond formed w/ enzyme
Use: tx of OD w/ anticholinergic drugs (i.e. - Atropine)
SE: can aggravate depression of cardiac conduction in pt w/ suspected TCA (tricyclic antidepressant) overdose; convulsions, bradycardia

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7
Q

Tolterodine

A

Use: overactive bladder

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8
Q

Atropine

A

Chem: tertiary amine (effects CNS)
Mechanism: competitive binding to muscarinic receptors preventing ACh from binding

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9
Q

Methacholine

A 
Chem: choline ester 
Target: mainly muscarinic
Metabolism: resistant to hydrolysis (slowly hydrolyzed by AChE)
Uses: dx asthma
SE: exacerbation of asthma/COPD
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10
Q

Tubocurarine

A

Chem: nondepolarizing NM blocker
Mechanism: competitive antagonist
Use: adjuvant in anesthesia during surgery to relax skeletal muscle

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11
Q

Vesamicol

A

Mechanism: blocks vesicular ACh-H+ antiporter (VAChT) to prevent storage of ACh invesicles
Use: research

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12
Q

Rivastigmine

A

MOA: AChE inhibitor
Use: Alzheimer’s Dz and Parkinson’s dementia
SE: AV block

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13
Q

Tabun, Sarin, Soman

A

Chem: synthetic toxic nerve agents
Use: toxic poison

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14
Q

Homatropine, Cyclopentolate, Tropicamide

A

Use: produce mydriasis w/ cycloplegia for ophthalmologist exams
(Preferred to atropine bc of shorter duration of action)

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15
Q

Hemicholinium-3

A

MOA: blocks choline transporter (CHT1) pre-synaptically to prevent synthesis of ACh
Use: research

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16
Q

Hexamethonium, Mecamylamine, Trimethaphan

A

Chem: ganglion blockers (nicotenic antagonist)
Use: (not used now) were once used to tx HTN but had too many SEs

17
Q

Pilocarpine

A 
Chem: tertiary amine
MOA: partial muscarinic agonist
Metabolism: stable to hydrolysis by AChE
Use: 2° for open angle glaucoma, acute angle-closure glaucoma, dry mouth d/t radiation or Sjogren's 
SE: CNS disturbances
18
Q

Atropine Uses

A
  • Antisialogogue: before surgery to decrease resp secretions
  • HR: to increase HR or decrease AV-block
  • Antidote for OD of cholinergic drugs
  • Antidote for muscarine poisoning 🍄
  • Alleviate muscarinic SEs from AChE inhibitors
19
Q

Atropine Effects

A

Eye: mydriasis, cycloplegia (focus for distance)
GI: decreased gut tone and motility
GU: decreases bladder motility
CV (low dose): bradycardia d/t pre-synaptic M2 receptor blockade
CV (mod to high dose): tachycardia

20
Q

Nicotine

A

Chem: tertiary amine
Target: NMJ
Low doses: ganglionic stimulation by depolarization (PANS + SANS is what it resembles)
High doses: ganglionic blockade and NM blockade
Uses: smoking cessation therapy

21
Q

Botulinum Toxin

A

MOA: inhibits ACh release from pre-synaptic neuron
Use: locally in muscles for dz w/ muscle spasms, cosmetic tx of wrinkles

22
Q

Scopolamine

A

Use: prevents motion sickness; also used in anesthetic procedures to block short-term memory

23
Q

Glycopyrolate

A

Use (PO): inhibit GI motility

Use (IV): prevent bradycardia during surgery

24
Q

Atropine Metabolism

A

Rapidly absorbed, partially metabolized by liver, elimination via urine

t1/2 = 4h

25
Q

Succinylcholine

A

Chem: depolarizing NM blocker
MOA: binds nicotenic receptor and depolarizers the NMJ stimulating the receptor - eventually receptor desensitization
Use: flaccid paralysis for intubation, or ECT
SE: malignant hyperthermia d/t excessive Ca2+ release (tx w/ Dantrolene)

26
Q

Bethanechol

A

Chem: choline ester
Target: mainly muscarinic
Metabolism: resistant to hydrolysis by AChE
Uses: post-op/post-partum urine retention, atonic bladder
SE: sweating, flushing, salivation, diarrhea, nausea, abd pn, hypotension, bronchospasm

27
Q

Benztropine and Trihexyphenidyl

A

Use: tx Parkinson’s dz and extrapyramidal effects of antipsychotic drugs

28
Q

Neostigmine

A

Chem: carbamate / quaternary ammonium (NO CNS)
Metabolism: covalent bond formed w/ enzyme
Use: reversal of non-depolarizing NM blockers s/p surgery; prevention and tx of post-op distention and urinary retention, tx Myasthenia Gravis

29
Q

Echothiophate

A

Chem: organophosphate
Metabolism: phosphorylation enzyme, hydrolyzes v slowly
Use: chronic open-angle glaucoma, subacute or chronic angle-closure glaucoma

30
Q

Malathion

A

Chem: organophosphate
Metabolism: phosphorylation enzyme, hydrolyzes v slowly
Risk: farmers
(Rapidly metabolized so less dangerous)

31
Q

Edrophonium

A

Chem: quaternary ammonium (no CNS)
Metabolism: short-lived d/t reversible binding to active site of enzyme (no covalent bond)
Use: dx Myasthenia Gravis, reverse the effects of non-depolarizing muscular blockers

32
Q

Muscarine

A

Chem: alkaloid
Target: muscarinic

33
Q

Pralidoxime

A

MOA: reactivation of inhibited AChE
Use: tx of organophosphate insecticide poisoning

34
Q

Arecoline

A

Chem: natural alkaloid
Target: muscarinic and nicotenic

35
Q

Donepezil

A

MOA: AChE inhibitor
Use: Alzheimer’s Dz
SE: AV block

36
Q

Acetylcholine

A

Chem: choline ester
Metabolism: rapidly hydrolyzed by AChE
Uses: to obtain rapid miosis after cataract surgery

Pharmacology (27 decks)

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