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Methacholine (Provocholine)

University of Saskatchewan · FDA-approved active Small molecule

Methacholine is a cholinergic agonist that binds to muscarinic acetylcholine receptors on airway smooth muscle, causing bronchoconstriction.

Methacholine is a cholinergic agonist that binds to muscarinic acetylcholine receptors on airway smooth muscle, causing bronchoconstriction. Used for Diagnostic agent for methacholine challenge test to assess airway hyperresponsiveness in suspected asthma.

At a glance

Generic nameMethacholine (Provocholine)
SponsorUniversity of Saskatchewan
Drug classCholinergic agonist
TargetMuscarinic acetylcholine receptors (M3)
ModalitySmall molecule
Therapeutic areaRespiratory/Pulmonology
PhaseFDA-approved

Mechanism of action

Methacholine mimics the action of acetylcholine by directly stimulating muscarinic receptors on bronchial smooth muscle, leading to airway constriction. This property makes it useful as a diagnostic agent to provoke airway hyperresponsiveness in patients suspected of having asthma or other obstructive airway diseases. The degree of bronchoconstriction in response to methacholine challenge correlates with airway hyperreactivity.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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