Methacholine
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215319102
2008-05-27T17:58:38Z
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{{drugbox
| IUPAC_name = 2-acetyloxypropyl-trimethyl-azanium
| image = Methacholine.svg
| CAS_number = 55-92-5
| CAS_supplemental = {{CAS|62-51-1}} (chloride)
| ATC_prefix =
| ATC_suffix =
| PubChem = 1993
| DrugBank =
| C = 8 | H = 18 | N = 1 | O = 2 | charge = +
| molecular_weight = 160.234 g/mol
| bioavailability =
| protein_bound =
| metabolism =
| elimination_half-life =
| excretion =
| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
| pregnancy_US = <!-- A / B / C / D / X -->
| pregnancy_category =
| legal_AU = <!-- Unscheduled / S2 / S3 / S4 / S8 -->
| legal_CA = <!-- / Schedule I, II, III, IV, V, VI, VII, VIII -->
| legal_UK = <!-- GSL / P / POM / CD / Class A, B, C -->
| legal_US = <!-- OTC / Rx-only / Schedule I, II, III, IV, V -->
| legal_status =
| routes_of_administration =
}}
'''Methacholine chloride''' is a synthetic [[choline]] [[ester]] that acts as a non-selective [[muscarinic receptor]] agonist in the [[parasympathetic nervous system]]. It is highly active at all of the muscarinic receptors, but has little effect on the [[nicotinic receptor]]s. 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 [[acetylcholinesterase]]s.
The primary clinical use of methacholine is to diagnose bronchial hyperreactivity, which occurs in [[asthma]]. This is accomplished through the [[methacholine challenge test]]. Other therapeutic uses are limited by its adverse cardiovascular effects, such as [[bradycardia]] and [[hypotension]], which arise from its function as a [[acetylcholine|cholinomimetic]].
Use of methacholine, as well as all other muscarinic receptor agonists, is contraindicated in patients with coronary insufficiency, gastroduodenal ulcers, and incontinence. The parasympathomimetic action of this drug will exacerbate the symptoms of these disorders.
== Brand Name ==
* Provocholine
== External links ==
* [http://www.provocholine.com Provocholine.com]
The primary clinical use of methacholine is to diagnose bronchial hyperresponsiveness (due to either hypersensitivity or hyperreactivity).
==References==
* {{cite book | author=Katzung, Bertram G. | title=Basic and Clinical Pharmacology | edition=9th | year=2004 | id=ISBN 0-07-141092-9}}
*{{cite journal | author = Lötvall J, Inman M, O'Byrne P | title = Measurement of airway hyperresponsiveness: new considerations | journal = Thorax | year = 1998 | month = May | volume = 53 | pages = 419–424 | url = http://thorax.bmjjournals.com/cgi/content/full/53/5/419 | pmid = 9708238}}
[[Category:Choline esters]]
[[Category:Quaternary ammonium compounds]]
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[[es:Metacolina]]