Montelukast: Drug Information
1. Drug Name
Generic Name
Montelukast
Brand Name(s)
- Pakistan: BrandX
- India: BrandY
- US: BrandZ
- UK: BrandW
2. Pharmacological Class
Class
Leukotriene receptor antagonist
Subclass
Cysteinyl leukotriene receptor antagonist
3. Mechanism of Action
Montelukast selectively antagonizes the cysteinyl leukotriene receptor (CysLT1) and inhibits the actions of leukotriene D4 (LTD4) and other cysteinyl leukotrienes (LTC4 and LTE4) on the CysLT1 receptor. This action prevents bronchoconstriction, airway edema, and inflammation caused by these substances.
4. Indications
Primary Indications
- Asthma, including prevention of daytime and nighttime symptoms
- Allergic rhinitis
Off-label Uses
- Exercise-induced bronchoconstriction
- Chronic idiopathic urticaria
5. Dosage and Administration
Standard Dosage
The dosage of montelukast varies depending on the condition being treated and the age of the patient. Consult with a healthcare provider for specific dosing.
Route of Administration
Montelukast is administered orally as tablets or granules.
Special Populations
- Pediatric: Dosing is age-dependent.
- Geriatric: No dosage adjustment necessary based on age alone.
6. Pharmacokinetics
Absorption
Montelukast is well absorbed after oral administration.
Distribution
It is extensively bound to plasma proteins.
Metabolism
Metabolized extensively in the liver via CYP2C8 and CYP3A4.
Excretion
Excreted mainly via bile.
Half-life
The elimination half-life is approximately 2.7 to 5.5 hours.
7. Contraindications
Montelukast is contraindicated in patients with hypersensitivity to any component of the product.
8. Warnings and Precautions
- Neuropsychiatric events have been reported; monitor for changes in behavior.
- Eosinophilia and vasculitic rash have been reported; discontinue if these symptoms occur.
- Churg-Strauss syndrome has been reported with montelukast use.
9. Side Effects
Common Side Effects
- Headache
- Abdominal pain
- Thirst
Serious Side Effects
- Hepatitis
- Pancreatitis
- Cholestatic hepatitis
10. Drug Interactions
Major Interactions
- Phenobarbital
- Rifampin
Moderate Interactions
- Warfarin
- Phenytoin
Minor Interactions
- Aspirin
- Fluconazole
11. Pregnancy and Lactation
Pregnancy Category
Category B - Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women.
Breastfeeding Considerations
It is not known whether montelukast is excreted in human milk, caution should be exercised when montelukast is administered to a nursing mother.
12. Patient Counseling Information
- Take montelukast exactly as prescribed, even if you feel well.
- Do not decrease your dose or stop taking montelukast without first talking to your healthcare provider.
- Report any unusual symptoms to your healthcare provider immediately.