Methacholine chloride 100mg powder for nebuliser solution vials
Requires a prescription from a doctor or prescriber
Official documents, adverse reaction reporting, and safety monitoring
Report a side effect
Submit a Yellow Card report to the MHRA
Official medicine documents
Yellow Card
Report side effects (MHRA)
Drug safety updates
MHRA alerts for Methacholine
Safety monitoring data
Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
View Drug Analysis Profile
Browse all Drug Analysis Profiles A–Z
Browse all iDAP reports
Interactive Drug Analysis Profiles for all medicines
Report a side effect
Submit a Yellow Card report to the MHRA
Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
View EudraVigilance report
Suspected adverse reactions reported for Methacholine
About EudraVigilance
Learn about EU pharmacovigilance and safety monitoring
EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
MHRA licensed products
View all licensed products for Methacholine on the MHRA register
Provocholine 100mg powder for nebuliser solution vials
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Guidelines from the National Institute for Health and Care Excellence
NICE clinical guidance(1)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
Pharmacy stock checkers
Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.
Supply & safety information
Official UK regulator monitoring and safety alerts
Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. Shortage and safety information sourced from MHRA drug safety updates (gov.uk, Crown Copyright under OGL v3.0).
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 1 · Randomised trials: 1 · 1965–2025
Showing the 50 most relevant studies, sorted by most relevant.
F. Hargreave, G. Ryan, N. Thomson, et al.
The Journal of allergy and clinical immunology, 1981
A. Coates, J. Wanger, D. Cockcroft, et al.
European Respiratory Journal, 2017
Dixon AE, Garrow OJ, Duchene B, et al.
2025
- Lung
- Asthma
- Obesity
BACKGROUND: People with obesity and asthma often experience poor asthma control and frequent exacerbations, and exhibit airway hyperresponsiveness (AHR) that may be mitigated by elevating lung volume. Our objective was to determine if nocturnal continuous positive airway pressure (CPAP) mitigates AHR in people with obesity, both with and without asthma. METHODS: We performed a double-blinded randomized controlled trial at two centers. Participants with BMI ≥ 30 kg/m2 with (n = 20) and without (n = 20) asthma were randomized to 7 nights of CPAP of 10 cmH2O or sham CPAP (4 cmH2O). Baseline airway physiology and response to methacholine were measured by oscillometry before and after CPAP intervention. Airway responsiveness was quantified by PC100AX - the concentration of methacholine producing a 100% increase in the area under the reactance curve, and also by the concentration response change in R5 and AX at the peak concentration of methacholine. RESULTS: The change in resistance at 19 Hz improved numerically in controls assigned to CPAP 10 cmH2O versus sham (-0.29 ± 0.08 versus − 0.07 ± 0.31 H2O.s.L−1, p = 0.07). AHR to methacholine was reduced numerically in controls assigned to CPAP 10 cmH2O versus sham, with the mean PC100AX (SD) being 0.43 (0.64) versus − 0.87 (0.64) mg/ml, p = 0.17. There was a modest difference in the change in the R5 concentration response in controls with CPAP 10 versus sham (median (IQ range): -0.55 (-1.14, 0.05) versus 0.31 (-0.20, 0.51), p = 0.04). CPAP 10 cmH2O versus sham did not change lung function or airway responsiveness in participants with asthma, but there was a trend toward an ameliorating effect in individuals with obesity alone. CONCLUSIONS: AHR in obese asthma is not simply related to the mechanical effects of obesity causing a reduction in lung volume. Subclinical abnormalities in airway responsiveness in people with obesity but without asthma might improve with nocturnal CPAP. TRIAL REGISTRATION: This study was registered on clinicaltrials.gov (NCT02953431, last update June 21, 2024).
Abstract licence: CC BY-NC-ND
R. Crapo, R. Casaburi, A. Coates, et al.
American journal of respiratory and critical care medicine, 2000
A. Jatakanon, Sam Lim, S. Kharitonov, et al.
Thorax, 1998
J. Spergel, E. Mizoguchi, J. Brewer, et al.
The Journal of clinical investigation, 1998
E. F. Juniper, P. Frith, C. Dunnett, et al.
Thorax, 1978
G. O'Connor, D. Sparrow, Don Taylor, et al.
The American review of respiratory disease, 1987
J. Seltzer, B. G. Bigby, M. Stulbarg, et al.
Journal of applied physiology, 1986
E. F. Juniper, E. F. Juniper, P. Frith, et al.
Thorax, 1981
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
Not available
Mechanism
Asthma is a complicated condition associated with airway remodelling, including…
Food interactions
1 warning
Human targets
5 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Methacholine was granted FDA approval on October 31, 1986, and is marketed under the trademark PROVOCHOLINE® by Methapharm Inc.[L31763]
[L31763]
Known interactions with other medicines. Always consult a healthcare professional.
Showing 50 of 364 interactions
Methacholine is a non-specific mAChR agonist, capable of acting on all mAChR subtypes.[A229623][A229628][A229633] However, in the context of AHR, methacholine's ability to induce bronchoconstriction through M3 receptors is clinically relevant.[A229603][A229618][A229643] In addition, M3 agonism may increase the release of pro-inflammatory cytokines, further contributing to AHR.[A17070] The inhibitory effect of M2 agonism by methacholine is likely also important, as shown by animal studies using mice with impaired M2 function, and by observations that eosinophilic inflammation, such as occurs in asthma, negatively impacts M2 function.[A229613] Hence, asthmatic patients are more sensitive to inhaled cholinergic agonists such as methacholine; this forms the basis for the methacholine challenge test, which diagnoses AHR through an increased methacholine-induced response.[A229648][L31763]
Proteins and enzymes this drug interacts with in the body
Proteins that transport this drug across cell membranes
PMID:10454528 PMID:10525100 PMID:10966938 PMID:17509700 PMID:20722056 PMID:33124720
Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium.
Relative uptake activity ratio of carnitine to TEA is 11.3 .
PMID:10454528 PMID:10525100 PMID:10966938
In intestinal epithelia, transports the quorum-sensing pentapeptide CSF (competence and sporulation factor) from B.subtilis which induces cytoprotective heat shock proteins contributing to intestinal homeostasis .
PMID:18005709
May also contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
ATC V04CX03
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Methacholine
Additional database identifiers
Drugs Product Database (DPD)
9543
ChemSpider
1916
BindingDB
48918
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1952
GenAtlas
CHRM3
GeneCards
CHRM3
GenBank Gene Database
X15266
GenBank Protein Database
32324
Guide to Pharmacology
15
UniProt Accession
ACM3_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1951
GenAtlas
CHRM2
GeneCards
CHRM2
GenBank Gene Database
M16404
GenBank Protein Database
177990
Guide to Pharmacology
14
UniProt Accession
ACM2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1950
GenAtlas
CHRM1
GeneCards
CHRM1
GenBank Gene Database
X52068
GenBank Protein Database
34451
Guide to Pharmacology
13
UniProt Accession
ACM1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1953
GenAtlas
CHRM4
GeneCards
CHRM4
GenBank Gene Database
M16405
GenBank Protein Database
61970253
Guide to Pharmacology
16
UniProt Accession
ACM4_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1954
GenAtlas
CHRM5
GeneCards
CHRM5
GenBank Gene Database
M80333
GenBank Protein Database
177988
Guide to Pharmacology
17
UniProt Accession
ACM5_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:10969
GenAtlas
SLC22A5
GeneCards
SLC22A5
GenBank Gene Database
AF057164
GenBank Protein Database
3273741
UniProt Accession
S22A5_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite:
- DrugBank 6.02024Recommended citationKnox C., Wilson M., Klinger C.M., et alDrugBank 6.0: the DrugBank Knowledgebase for 2024Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
- DrugBank 5.02018Wishart D.S., Feunang Y.D., Guo A.C., et alDrugBank 5.0: a major update to the DrugBank database for 2018Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
- DrugBank 4.02014Law V., Knox C., Djoumbou Y., et alDrugBank 4.0: shedding new light on drug metabolismNucleic Acids Res. 2014 Jan 142(1):D1091-7
- DrugBank 3.02011Knox C., Law V., Jewison T., et alDrugBank 3.0: a comprehensive resource for 'omics' research on drugsNucleic Acids Res. 2011 Jan39(Database issue):D1035-41
- DrugBank 2.02008Wishart D.S., Knox C., Guo A.C., et alDrugBank: a knowledgebase for drugs, drug actions and drug targets.Nucleic Acids Research2008 Jan36(Database issue):D901-6
- DrugBank 1.02006Wishart D.S., Knox C., Guo A.C., et alDrugBank: a comprehensive resource for in silico drug discovery and exploration.Nucleic Acids Research2006 Jan 134(Database issue):D668-72