Cholinergic Drugs Flashcards Preview

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Flashcards in Cholinergic Drugs Deck (36):
1

Atropine SEs

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

2

Parathion

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

3

Carbachol

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

4

Ipratropium and Tiotropium

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

5

Pyridostigmine

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

6

Physostigmine

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

7

Tolterodine

Use: overactive bladder

8

Atropine

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

9

Methacholine

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

10

Tubocurarine

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

11

Vesamicol

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

12

Rivastigmine

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

13

Tabun, Sarin, Soman

Chem: synthetic toxic nerve agents
Use: toxic poison

14

Homatropine, Cyclopentolate, Tropicamide

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

15

Hemicholinium-3

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

16

Hexamethonium, Mecamylamine, Trimethaphan

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

17

Pilocarpine

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

Atropine Uses

- 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

Atropine Effects

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

Nicotine

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

Botulinum Toxin

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

22

Scopolamine

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

23

Glycopyrolate

Use (PO): inhibit GI motility
Use (IV): prevent bradycardia during surgery

24

Atropine Metabolism

Rapidly absorbed, partially metabolized by liver, elimination via urine

t1/2 = 4h

25

Succinylcholine

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

Bethanechol

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

Benztropine and Trihexyphenidyl

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

28

Neostigmine

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

Echothiophate

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

30

Malathion

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

31

Edrophonium

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

Muscarine

Chem: alkaloid
Target: muscarinic

33

Pralidoxime

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

34

Arecoline

Chem: natural alkaloid
Target: muscarinic and nicotenic

35

Donepezil

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

36

Acetylcholine

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