521 Exam 1 Drugs

List the Choline esters (Direct muscarinic agonists)

Bethanechol

Carbachol

Bethanechol

Activates muscarinic receptors

Uses: Atony

Carbachol

Muscarinic and Nicotinic activator

Uses: Topically for glaucoma

List the Non-Choline esters (Direct muscarinic agonists)

Pilocarpine, muscarine, cevimeline

Pilocarpine

Activates muscarinic receptor

Uses: Sjorgen syndrome, Acute glaucoma

may cause vascosintriction

muscarine

Activates muscarinic receptor

Uses: Mushrooms

cevimeline

M3 selective muscarinic receptor

Uses: Sjogren syndrome

List the Nicotinic Agonists

Nicotine

Varenicline

Nicotine

Activates N receptors, opens NA+ K+ channels

Uses: Smoking cessation

Side effects: hypertension, nausea, vomiting, diarrhea, tachycardia

Varenicline

Partial N agonist

Uses: Smoking cessation

Side effects: hypertension, sweat, diarrhea, polyuria, sensory disturbance

List the Alcohol Anticholinesterase drugs

Edrophonium

Edrophonium

Inhibits AchE and amplifies Ach

Uses: Reverse Nm blockade post surgery

Diagnose myasthenia gravis

Side effects: increases para effects, nausea, vomiting, diarrhea

List the carbamates Anticholinesterase drugs

Neostigmine

Pyridostigmine

Physostigmine

Neostigmine

Inhibits AchE and amplifies Ach, nicotinic agonist

Uses: Reverses Nm blockade, treat myasthenia gravis

Side effects: long duration increases para effects, nausea, vomiting, diarrhea

Pyridostigmine

Inhibits AchE and amplifies Ach

Uses: Treat myasthenia

Side effects: long duration increases para effects, nausea, vomiting, diarrhea

Physostigmine

Inhibits AchE and amplifies Ach

Uses: reverse atropine poison, acute glaucoma topical

Side effects: long duration increases para effects, nausea, vomiting, diarrhea + seizures

List the Anticholinesterase drugs for alzheimer’s

Donepezil, Rivastigmine, Galantamine, Tacrine

Donepezil, Rivastigmine, Galantamine, Tacrine

Cholinesterase inhibitors

Uses: Alzheimer’s

Side effects: Nausea, vomiting

*Tacrine is not used anymore due to hepatotoxicity

List the organophosphate Anticholinesterase drugs

Parathion

Malathion

Sarin, tabun

Echothiopate

Parathion

Inhibits AchE and amplifies Ach

Uses: insecticide that lasts says to weeks

Lethal

Malathion

Inhibits AchE and amplifies Ach

Uses: insecticide that lasts days

Not as lethal as parathion

Sarin, Tabun

Inhibits AchE and amplifies Ach

Uses: Terrorist gas

Lethal

Echothipate

Inhibits AchE and amplifies Ach

Uses: FORMERLY for glaucoma

Motion Sickness Muscarinic Antagonists

Scopolamine

GI Disorder Muscarinic Antagonists

Dicyclomine

Glycopyrrolate

Long acting Ophthalmology Muscarinic Antagonists

Atropine

Scopolamine

Short acting Ophthalmology Muscarinic Antagonists

Tropicamide

Cyclopentolate

Homatropine

Respiratory Muscarinic Antagonists

Ipratropium, Tiotropium, Aclidinium, Umeclidinium

Urinary Muscarinic Antagonists

Oxybutynin , Darifenacin, Solifenacin, Tolteridone, Fesoterodine, Trospium(Less CNS affect)

Cholinergic Poisoning Muscarinic Antagonists

Atropine

2PAM (Pralidoxime)

Scopolamine

Uses: Motion Sickness

Toxicity: tachycardia, blurred vision, delirium, drowsiness, amnesia, dry mouth

Dicyclomine, Glycopyrrolate

MOA: competitive antagonist at M3 receptors

Uses: IBS, minor diarrhea

Toxicity: Tachycardia, confusion, urinary retention, increased intraocular pressure, constipation

Atropine, Homatropine, Cyclopentolate, Tropicamide

MOA: Competitive antagonist @ all M receptors

Uses: Eye exam

Toxicity: acute closed angle glaucoma

Ipratropium, Tiotropium, Aclidinium, Umeclidinium

MOA: competitive nonselective antagonist @ all M receptors

Uses: COPD, Asthma (acute)

Toxicity: dry mouth, cough

shortest dur: Ipratropium

Oxybutynin , Darifenacin, Solifenacin, Tolteridone, Fesoterodine,Trospium(Less CNS affect)

MOA: slight M3 selective muscarinic antagonist

Uses: Urge incontinence

Toxicity: tachycardia, constipation, increased intraocular pressure, dry mouth, aggravate BPH

*Trospium—>Less CNS affect

Atropine

MOA: non selective competitive antagonist @ all M receptors in CNS and periphery

Use: antidote for cholinesterase poisoning & mushroom poisoning

Pralidoxime (2PAM)

MOA: AchE regenerator

Use: antidote for ach poisoning, must use early

Toxicity: Muscle weakness

List the Short Acting Nondepolarizing NMJ Blockers

Mivacurium

List the Intermediate acting Non depolarizing NMJ Blockers

Atracurium, Cisatracurium, Rocuronium, Vecuronium

List the Long acting Non depolarizing NMJ Blockers

Pancuronium, pipecuronium, D-Tubocurarine

List the Depolarizing short acting NMJs

Succinylcholine

Sugammadex

Can reverse rocuronium & vecuronium

Uses for NMJ Blockers

Surgical Relaxation

Endotracheal intubation

Control of ventilation

Treat convulsions