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Methacholine: Wikis


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Systematic (IUPAC) name
CAS number 55-92-5
62-51-1 (chloride)
ATC code none
PubChem 1993
Chemical data
Formula C 8H18NO2 +
Mol. mass 160.234 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Methacholine (Provocholine) is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.



The primary clinical use of methacholine is to diagnose bronchial hyperreactivity,[1] which is the hallmark of asthma and also occurs in chronic obstructive pulmonary disease. This is accomplished through the bronchial challenge test. Other therapeutic uses are limited by its adverse cardiovascular effects, such as bradycardia and hypotension, which arise from its function as a cholinomimetic.


It is highly active at all of the muscarinic receptors, but has little effect on the nicotinic receptors. Methacholine has a charged quaternary amine structure, rendering it insoluble to lipid cell membranes. Clinically, this means that it will not cross the blood-brain barrier and has poor absorption from the gastrointestinal tract. It is broken down at a relatively slow rate within the body, due to its resistance to acetylcholinesterases.


Use of methacholine, is contraindicated in patients with recent heart attack or stroke, uncontrolled hypertension, known severe airway disease, or an aortic aneurysm. It may be used with caution by nursing or pregnant mothers and patients taking certain medications for myasthenia gravis[2].


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