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Provocholine (METHACHOLINE)
Provocholine works by stimulating the M1 muscarinic acetylcholine receptor.
Provocholine (METHACHOLINE) is a cholinergic receptor agonist developed by Methapharm, targeting the muscarinic acetylcholine receptor M1. It is a small molecule, FDA-approved in 1986 for use as a diagnostic test for asthma. Provocholine is off-patent and has no generic manufacturers. As a cholinergic agonist, it works by stimulating the M1 receptor, which can lead to increased airway constriction in patients with asthma, making it useful for diagnostic purposes. Key safety considerations include the potential for increased airway constriction.
At a glance
| Generic name | METHACHOLINE |
|---|---|
| Sponsor | Methapharm |
| Drug class | Cholinergic Receptor Agonist |
| Target | Muscarinic acetylcholine receptor M1 |
| Modality | Small molecule |
| Therapeutic area | Respiratory |
| Phase | FDA-approved |
| First approval | 1986 |
Mechanism of action
Methacholine chloride is cholinergic agonist. Bronchial smooth muscle contains significant parasympathetic (cholinergic) innervation. Methacholine chloride agonizes the muscarinic receptors which eventually induce bronchoconstriction.
Approved indications
- Diagnostic Test for Asthma
Boxed warnings
- WARNING: SEVERE BRONCHOCONSTRICTION WARNING: SEVERE BRONCHOCONSTRICTION Severe bronchoconstriction can result from Provocholine administration (including the lowest dose). The use of Provocholine is contraindicated in pediatric and adult patients with baseline FEV1 < 60% predicted or adults with FEV1 < 1.5 L. Because of the potential for severe bronchoconstriction, the use of Provocholine in patients with clinically apparent asthma or wheezing is not recommended [ see Warnings and Precautions (5.1) ]. Emergency equipment and medication should be immediately available to treat acute respiratory distress. If severe bronchoconstriction occurs, reverse immediately with a rapid-acting inhaled bronchodilator agent (β-agonist) [ see Warnings and Precautions (5.1) ]. If baseline spirometry is not performed or is measured inaccurately, the initial FEV1 may be underestimated. In this situation, decreases in FEV1 may not be detected after administration of escalating Provocholine doses, which may result in administration of unnecessary higher doses and an increased risk for excessive bronchoconstriction [ see Warnings and Precautions (5.1) ]. WARNING: SEVERE BRONCHOCONSTRICTION See full prescribing information for complete boxed warning. Severe bronchoconstriction can result from Provocholine administration (including the lowest dose) (5.1) Use of Provocholine is contraindicated in pediatric and adult patients with baseline FEV1 < 60% predicted or adults with FEV1 < 1.5 L (5.1) Use of Provocholine is not recommended in patients with clinically apparent asthma or wheezing (5.1) If severe bronchoconstriction occurs, reverse immediately with a rapid-acting inhaled bronchodilator agent (β-Agonist) (5.1)
Common side effects
- Bronchospasm
- Headache
- Throat irritation
- Light-headedness
- Itching
Key clinical trials
- Effect of Ectoin® Inhalation Solution on Subjects With Mild Bronchial Asthma (NA)
- Body Composition Related Evaluation of Airway Tone and Hyper-rEactivity Using Oscillometry
- Examining Bronchial Hyperresponsiveness in Primary Ciliary Dyskinesia (NA)
- Diagnostic and Translational Values of Point-of-care Blood Eosinophils and Exhaled Nitric Oxide (FeNO) in People Referred by Primary Care for Suspected Asthma
- A Study to Compare the Relative Potency of Salbutamol Administered Via Metered Dose Inhalers (MDI) Containing Propellants HFA-152a to HFA-134a in Mild Asthmatics Aged 18 to 65 Inclusive (PHASE1)
- Exercise Induced Bronchoconstriction and Field Tests (NA)
- Pilot Study for the Application of Low Power External Bioelectronic Devices in the Diagnosis of Bronchial Asthma.
- BE Study of Albuterol Sulfate Inhalation Aerosol 90 mcg Per Actuation in Patients With Stable Mild Asthma (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Provocholine CI brief — competitive landscape report
- Provocholine updates RSS · CI watch RSS
- Methapharm portfolio CI