Hemicholinium-3

Vesamicol

Botulinum toxin

Focal dystonias, torticollis, achalasia, strabismus, blepharospasm, pain syndromes, wrinkles, hyperhidrosis

Cardiac arrhythmia, syncope, hepatotoxicity, anaphylaxis, injection-site pain, dyspepsia, dysphagia, muscle weakness, neck pain, eyelid ptosis, fever

hypersensitivity and injection site infection

Produced by Clostridium botulium, degrades synaptobrevin and thus prevents synaptic vesicle fusion with axon terminal (presynaptic) membrane

Edrophonium

Neostigmine

Pyridostigmine

Ambenonium

Physostigmine

Diisopropyl fluorophosphate

Tacrine

Donepezil

Rivastigmine

Galantamine

Diagnosis of myasthenia gravis, Eaton-Lambert syndrome, and disorders resulting in muscle weakness (edrophonium)

Urinary or gastrintestinal motility agent, glaucoma, neuromuscular junction diseases such as myasthenia gravis (neostigmine, pryridostigmine, ambenonium)

Reversal of anticholinergic toxicity or induced paralysis in surgery (physostigmine)

Mechanical intestinal or urinary obstruction. Concomitant choline ester or depolarizing neuromuscular block use. Cardiovascular disease.

-Edrophonium is short-acting (2-10 mins);  rapid onseet of action makes it useful for diagnosis of muscle weakness.

-For chronic treatment of myasthenia gravis, longer-action cholinesterase inhibitors such as pyridostigmine, neostigmine, and ambenonium are preferred. 

-Neostigmine also has direct cholinergic agonist effect at Nm receptors.

-Topical application of cholinesterase inhibitor to the cornea of the eye decreases intraocular pressure by facilitating the outflow of aqueous humor

-Nonpolar structure makes physostigmine useful for treating CNS anticholinergic toxicity

Not applicable (sometimes encountered as a toxin)

Respiratory paralysis, bradycardia, bronchospasm, fasciculations, muscle cramps, weakness, CNS depression, agitation, confusion, delirium, coma, bronchorrhea, salivation, lacrimation, diaphoresis, vomiting, diarrhea, miosis

Not applicable

An organophosphate compound used as an insecticide, as a substrate for the production of organophosphate chemical weapons (nerve gases), and formerly as a topical miotic medication in ophthalmology

Mild to moderate Alzheimer's disease and dementia

Diarrhea, nausea, vomiting, cramps, anorexia, vivid dreams

Treatment-associated liver function test abnormalities (tacrine)

-Modest symptomatic benefits in Alzheimer's disease.

-Rivastigmine affects both acetylcholinesterase and butyrylcholinesterase by forming a carbamoylate complex with the enzymes.

-Galantamine also acts as a nonpotentiating ligand of nicotinic receptors

Methacholine

Carbachol

Bethanechol

Cevimeline

Pilocarpine

Asthma

Dyspnea, lightheadedness, headache, pruritus, throat irritation

Recent heart attack or stroke, aortic aneurysm, uncontrolled hypertension

Highly resistant to acetylcholinesterase; it is relatively selective for cardiovascular muscarinic cholinergic receptors.

Glaucoma (carbachol), urinary tract motility agent (bethanechol), Xerostomia in Sjogren's syndrome (cevimeline and pilocarpine)

Sweating, shivering, nausea, dizziness, increased frequency of urination, rhinitis (oral formulations)

Acute iritis or glaucoma after cataract extraction and narrow-angle (angle-closure) glaucoma

-Carbachol has enhanced nicotinic action relative to other choline esters; carbachol cannot be used systemically because of its unpredictable nicotinic action at autonomic ganglial topical application of carbachol to the cornea of the eye results in both pupillary constriction (miosis) and decreased intraocular pressure

-Bethanechol is almost completely selective for muscarinic receptors

-Pilocarpine and cevimeline (an M1 and M3 agonist) are used to treat xerostomia in Sjogren's syndrome

Succinylcholine

Stimulate opening of nicotinic ACh receptor channel and produce depolarization of the cell membrane; succinylcholine presists at the neuroeffector junction and activates the nicotinic receptor channels continuously, which results in inactivation of voltage-gated sodium channels so that they cannot open to support further action potentials (sometimes called "depolarizing blockade")

induction of neuromuscular blockade in surgery and intubation

Bradyarrhythmia, cardiac arrest, cardiac arrhythmia, malignant hyperthermia, rhabdomyolysis, respiratory depression, muscle rigidity, myalgia, raised intraocular pressure

Personal or family history of malignant hyperthermia, skeletal muscle myopathies, upper motor neuron injury, extensive denervation of skeletal muscle

-Short duration of action makes succinylcholine drug of choice for paralysis during intubation

-Causes transient fasciculations

Atropine

Scopolamine

Pirenzepine

Methscopolamine

Glycopyrrolate

Ipratropium

Tiotropium

Oxybutynin

Propantheline

Terodiline

Tolterodine

Fesoterodine

Trospium

Darifenacin

Solifenacin

Anticholinesterase overdoes, acute symptomatic bradycardia, premedication for anesthetic procedure, excessive salivation and mucus secretion during surgery, antidote to mushroom poisoning

Cardiac arrhythmia, coma, respiratory depression, raised intraocular pressure, tachycardia, constipation, xerostomia, blurred vision

narrow-angle glaucoma

-A naturally occurring alkaloid found in the plant Atropa belladonna

-Mainly muscarinic activity, marginal nicotinic effect

-More effective at reversal of exogenous rather than endogenous cholinergic activity

Motion sickness, nausea, and vomiting

Alteration in heart rate, drug-induced psychosis, somnolence, xerostomiaa, blurred vision

narrow-angle glaucoma

-significant CNS effects

-Delivered via transdermal patch

Peptic ulcer disease, surgically induced or vagally induced bradycardia (glycopyrrolate)

Cardiac arrhythmia, malignant hyperthermia, anaphylaxis, seizure, constipation, xerostomia, urinary retention, decreased sweating

gastrointestinal obstruction, narrow-angle glaucoma

-Alternative or additive agents to standard peptic ulcer disease therapies

-Methscopolamine and glycopyrrolate have delayed but measurable CNS and cognitive anticholinergic effects

Chronic obstructive pulmonary disease (COPD) and asthma

Paralytic ileus, anaphylaxis, oropharyngeal edema, abnormal taste in mouth, xerostomia (nasal spray)

Hypersensitivity

-Ipratropium is more effective than beta-adrenergic agonists in the treatment of COPD, but less effective in treating asthma

-Relative to ipratropium, tiotropium has been shown to have similar, and possibly superior, efficacy as a bronchodilator in the treatment of COPD

Hyperreflexic and overactive bladder and urge incontinence

constipation, diarrhea, nausea, dry mouth, application-site erythema, pruritus, urinary retention

narrow-angle glaucoma, gastric retention, urinary retention

-Oxybutynin, propantheline, tolterodine, fesoterodine, and trospium are nonspecific muscarinic receptor antagonists, whereas darifenacin and solifenacin and selective M3 receptor antagonists

-Tolterodine may cause less dry mouth than oxybutynin, and the newer M3-selective agents darifenacin and solifenacin may cause less dry mouth and constipation than nonselective agents

Pacuronium

Tubocurarine

Vecuronium

Rocuronium

Mivacurium

Induction of neuromuscular blockade in surgery and intubation

Hypertension, tachyarrhythmia, apnea, bronchospasm, respiratory failure, salivation, flushing (mivacurium)

Hypersensitivity

-Pancuroium and tubocurarine are long-acting agents; vecuronium and rocuronium are intermediate-acting agents; mivacurium is a short-acting agent

-Nondepolarizing blocking agents have variable adverse effects associated with ganglionic blockade, which can be reversed by administration of AChE inhibitors

Hypertension in patients with acute aortic dissection

Paralytic ileus, urinary retention, respiratory arrest, syncope, orthostatic hypotension, dyspepsia, diplopia, sedation

Trimethaphan - asphyxia, uncorrected respiratory insufficiency, neonates at risk for paralytic or meconium ileus, shock

Mecamylamine - coronary insufficiency, glaucoma, recent myocardial infarction, pyloric stenosis, renal insufficiency, patients treated with sulfonamides

-Mecamylamine and trimethaphan are administered when gaglionic blockade is desired; these drugs lower blood pressure while simultaneously blunting the sympathetic reflexes that would normally cause a deleterious rise in pressure at the site of the tear in case of aortic dissection