Montelukast

The cysteinyl leukotrienes (LTC 4 , LTD 4 , LTE 4 ) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors.

• Montelukast sodium chewable tablets are a leukotriene receptor antagonist indicated for: • Prophylaxis and chronic treatment of asthma in patients 2 years of age and older ( 1.1 ). • Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 6 years of age and older ( 1.2 ).ICD-10: J45.909

• • Hypersensitivity to any component of this product. • Hypersensitivity to any component of this product ( 4 ).contraindicated

Administration (by indications): • Asthma ( 2.1 ): Once daily in the evening for patients 2 years and older. • Acute prevention of EIB ( 2.2 ): One tablet at least 2 hours before exercise for patients 6 years of age and older. • Seasonal allergic rhinitis ( 2.3 ): Once daily for patients 2 years and older. • Perennial allergic rhinitis ( 2.3 ): Once daily for patients 2 years and older. Dosage (by age) ( 2 ): • 15 years and older: one 10-mg tablet. • 6 to 14 years: one 5-mg chewable tablet. • 2 to 5 years: one 4-mg chewable tablet. Patients with both asthma and allergic rhinitis should take only one dose daily in the evening ( 2.4 ). 2.1 Asthma Montelukast sodium should be taken once daily in the evening. The following doses are recommended: For adults and adolescents 15 years of age and older: one 10-mg tablet. For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet. For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet. Safety and effectiveness in pediatric patients less than 12 months of age with asthma have not been established. who miss a dose should take the next dose at their regular time and should not take 2 doses at the same time. There have been no clinical trials in patients with asthma to evaluate the relative efficacy of morning versus evening dosing. The pharmacokinetics of montelukast are similar whether dosed in the morning or evening. Efficacy has been demonstrated for asthma when montelukast was administered in the evening without regard to time of food ingestion. Montelukast sodium should be taken once daily in the evening.

• Do not prescribe montelukast sodium to treat an acute asthma attack ( 5.2 ). • Advise patients to have appropriate rescue medication available ( 5.2 ). • Inhaled corticosteroid may be reduced gradually. Do not abruptly substitute montelukast sodium for inhaled or oral corticosteroids ( 5.3 ). • Patients with known aspirin sensitivity should continue to avoid aspirin or non-steroidal anti-inflammatory agents while taking montelukast sodium ( 5.4 ). • Systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, has been reported. These events have been sometimes associated with the reduction of oral corticosteroid therapy ( 5.5 and 6.2 ). • Inform patients with phenylketonuria that the 4-mg and 5-mg chewable tablets contain phenylalanine ( 5.6 ). 5.1 Neuropsychiatric Events Serious neuropsychiatric (NP) events have been reported with of montelukast sodium. These postmarketing reports have been highly variable and included, but were not limited to, agitation, aggressive behavior or hostility, , depression, disorientation, disturbance in attention, dream abnormalities, dysphemia (stuttering), hallucinations, insomnia, irritability, memory impairment, -compulsive symptoms, restlessness, somnambulism, suicidal thoughts and behavior (including suicide), tic, and tremor. NP events have been reported in adult, , and pediatric patients with and without a previous history of psychiatric disorder.

Most common adverse reactions (incidence ≥5% and greater than placebo listed in descending order of frequency): upper respiratory infection, fever, headache, pharyngitis, cough, abdominal pain, diarrhea, otitis media, influenza, rhinorrhea, sinusitis, otitis ( 6.1 ). To report SUSPECTED ADVERSE REACTIONS, contact Hetero Labs Limited at 1-866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . See 17 for PATIENT COUNSELING INFORMATION and Medication Guide. Revised: 05/2020 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. In the following description of clinical trials experience, adverse reactions are listed regardless of causality assessment. The most common adverse reactions (incidence ≥5% and greater than placebo; listed in descending order of frequency) in controlled clinical trials were: upper respiratory infection, fever, headache, pharyngitis, cough, abdominal pain, diarrhea, otitis media, influenza, rhinorrhea, sinusitis, otitis. Adults and Adolescents 15 Years of Age and Older with Asthma Montelukast sodium has been evaluated for safety in approximately 2950 adult and adolescent patients 15 years of age and older in clinical trials.

8.1 Pregnancy Risk Summary Available data from published prospective and retrospective cohort studies over decades with montelukast use in pregnant women have not established a drug-associated risk of major birth defects [see Data] . In animal reproduction studies, no adverse developmental effects were observed with oral administration of montelukast to pregnant rats and rabbits during organogenesis at doses approximately 100 and 110 times, respectively, the maximum recommended human daily oral dose (MRHDOD) based on AUCs [see Data] . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Poorly or moderately controlled asthma in pregnancy increases the maternal risk of perinatal adverse outcomes such as preeclampsia and infant prematurity, low birth weight, and small for gestational age. Data Human Data Published data from prospective and retrospective cohort studies have not identified an association with montelukast sodium use during pregnancy and major birth defects.

Metabolism

Absorption Montelukast is rapidly absorbed following oral administration. After administration of the 10-mg film-coated tablet to fasted adults, the mean peak montelukast plasma concentration (C max ) is achieved in 3 to 4 hours (T max ).

No specific information is available on the treatment of overdosage with montelukast sodium. In the event of overdose, it is reasonable to employ the usual supportive measures; e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive therapy, if required. It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis.

• Feb 20, 1998NDANDA020829Organon
• Feb 20, 1998NDANDA020830Organon
• Jul 26, 2002NDANDA021409Organon
• Aug 3, 2012ANDAANDA202096Aurobindo Pharma Ltd
• Aug 3, 2012ANDAANDA201515Torrent Pharms Ltd
• Aug 3, 2012ANDAANDA202468Aurobindo Pharma Ltd
• Aug 3, 2012ANDAANDA200889Sandoz Inc
• Aug 3, 2012ANDAANDA090984Torrent Pharms Ltd

1. 1Dyspnoea19,00011%
2. 2Asthma18,47911%
3. 3Drug Ineffective12,8817.5%
4. 4Fatigue11,9006.9%
5. 5Cough11,3226.6%
6. 6Headache10,7006.2%
7. 7Nausea9,3495.5%
8. 8Pneumonia9,0535.3%
9. 9Wheezing8,9765.2%
10. 10Pain8,3884.9%
11. 11Off Label Use7,2594.2%
12. 12Anxiety7,0604.1%
13. 13Diarrhoea6,9584.1%
14. 14Malaise6,8854.0%
15. 15Dizziness6,5943.8%

The 10 most recently updated of 366 ClinicalTrials.gov registrations naming Montelukast as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Treating Exacerbations of Asthma With Oral Montelukast in Children
  Completed · Phase 2 · Interventional · 90 enrolled · Vanderbilt University Medical Center
  NCT05819541updated 2026-06-12
• BElumosudil for Bronchiolitis Obliterans Prevention/Therapy (BEBOP)
  Recruiting · Phase 2 · Interventional · 45 enrolled · Dana-Farber Cancer Institute
  NCT05922761updated 2026-06-10
• MOntelukast as a Potential CHondroprotective Treatment Following Anterior Cruciate Ligament Reconstruction (MOCHA Trial)
  Recruiting · Early phase 1 · Interventional · 30 enrolled · Austin V Stone
  NCT04572256updated 2026-06-10
• Premedication to Reduce Amivantamab Associated Infusion Related Reactions
  Active not recruiting · Phase 2 · Interventional · 68 enrolled · Janssen Research & Development, LLC
  NCT05663866updated 2026-06-08
• PK, Safety and Preliminary Efficacy Study of Montelukast in Critically Ill Infants With Developing Bronchopulmonary Dysplasia
  Recruiting · Phase 1 · Phase 2 · Interventional · 28 enrolled · Duke University
  NCT07101640updated 2026-06-02
• SMART 2D: Study of Montelukast's Effects on Renal and Cardiovascular Health in Adolescents and Young Adults With Type 2 Diabetes
  Not yet recruiting · Early phase 1 · Interventional · 50 enrolled · University of Colorado, Denver
  NCT07409714updated 2026-05-14
• Effect of Montelukast on Inflammatory Markers and Cardiac Injury in Patients With Acute Myocardial Infarction
  Recruiting · Phase 2 · Interventional · 80 enrolled · October 6 University
  NCT07537868updated 2026-05-08
• Does Montelukast Decrease Post Adenotonsillectomy Pain in Children
  Completed · Phase 3 · Interventional · 116 enrolled · Children's Hospital Medical Center, Cincinnati
  NCT02793375updated 2026-04-21
• A Pilot Study of Mirabegron and Montelukast in Cirrhotic Patients
  Completed · Phase 4 · Interventional · 78 enrolled · Kafrelsheikh University
  NCT07533565updated 2026-04-16
• Comparison of Antihistamine and Antileukotriene Add-On Therapy to Intranasal Corticosteroid in Allergic Rhinitis
  Not yet recruiting · Phase 4 · Interventional · 32 enrolled · Liaquat National Hospital & Medical College
  NCT07532993updated 2026-04-16

Frequently asked questions

How does Montelukast work?

The cysteinyl leukotrienes (LTC 4 , LTD 4 , LTE 4 ) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors.

What is Montelukast used for?

According to FDA labeling, Montelukast carries indications including: Montelukast sodium chewable tablets are a leukotriene receptor antagonist indicated for: • Prophylaxis and chronic treatment of asthma in patients 2 years of age and older ( 1.1 ). • Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 6 years of age and older ( 1.2 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Montelukast?

Montelukast is classified as Leukotriene receptor antagonists, Leukotriene Receptor Antagonist, Leukotriene Receptor Antagonists, Bronchodilation, Decreased Tracheo-Bronchial Mucosal Edema.

What are the brand names for Montelukast?

Montelukast is marketed under brand names including Singulair.

What are the contraindications for Montelukast?

Montelukast labeling lists contraindications including: • Hypersensitivity to any component of this product. • Hypersensitivity to any component of this product ( 4 ).. Always consult the full prescribing information and a clinician.