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Methacholine

Cholinesterase Inhibitor · Diagnostic Agent for Bronchial Airway Hyperreactivity

Also known as PROVOCHOLINE

Cholinesterase InhibitorDiagnostic Agent for Bronchial Airway Hyperreactivity
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Contraindicated in pregnancy
FDA category + note
Top interactionssee all 12
  • BucindololSevereTextbookG&G 14e · p212
  • CeliprololSevereTextbookG&G 14e · p212
  • Esmolol HydrochlorideSevereTextbookG&G 14e · p212
  • NebivololSevereTextbookG&G 14e · p212

Mechanism

Methacholine is a muscarinic agonist. It stimulates muscarinic receptors in the tracheobronchial tree, leading to bronchoconstriction and increased tracheobronchial secretions. Asthmatic patients exhibit an intense bronchoconstriction and reduction in vital capacity upon administration, which is used for diagnostic purposes.

Indications

Diagnosis of bronchial airway hyperreactivity in patients who do not have clinically apparent asthma

Dosing

Adult
Dose adjustments Manufacturer advises dose reduction of 33% in mild to moderate impairment. l RENAL IMPAIRMENT Dose adjustments Manufacturers advise reduce daily dose by half in moderate to severe renal impairment. l EFFECT ON LABORATORY TESTS May interfere with methacholine test—manufacturer advises stop treatment 96 hours prior to test.…

Contraindications

  • Severe airflow limitation
  • Recent myocardial infarction or stroke
  • Uncontrolled hypertension
  • Pregnancy
  • Patients taking β adrenergic receptor antagonists (may cause exaggerated or prolonged response)
  • GI obstruction
  • Urinary retention
  • Asthma
  • Chronic obstructive pulmonary disease

Side effects

Common
BronchoconstrictionIncreased tracheobronchial secretionsGI crampsDiarrheaNauseaVomitingLacrimationSalivationSweatingUrinary urgencyVision problems
Serious
  • Intense bronchoconstriction
  • Reduction in vital capacity
  • Severe bronchospasm (requiring emergency treatment)

Pregnancy & lactation

Pregnancy

Contraindicated in pregnancy

Drug interactions

Bucindolol
Severe
Textbook

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: G&G 14e · p212

Celiprolol
Severe
Textbook

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: G&G 14e · p212

Esmolol Hydrochloride
Severe
Textbook

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: G&G 14e · p212

Nebivolol
Severe
Textbook

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: G&G 14e · p212

Penbutolol
Severe
Textbook

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: G&G 14e · p212

Acebutolol
Severe
Database

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: DDInter

Atenolol
Severe
Database

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: DDInter

Betaxolol
Severe
Database

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: DDInter

Bisoprolol
Severe
Database

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: DDInter

Carteolol
Severe
Database

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: DDInter

Carvedilol
Severe
Database

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: DDInter

Esmolol
Severe
Database

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: DDInter

Related guidelines

Other Cholinesterase Inhibitor drugs

Ask House about Methacholine

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team