Singulair

Each 10-mg film-coated tablet contains 10.4 mg montelukast sodium, which is the molar equivalent to 10.0 mg of free acid. Each 5-mg chewable tablet contains 5.2 mg montelukast sodium, which is the molar equivalent to 5.0 mg of free acid. Each 4-mg chewable tablet and each packet of 4-mg oral granules contains 4.2 mg montelukast sodium, which is the molar equivalent to 4.0 mg of free acid.
MONTELUKAST (SINGULAIR) is a selective and orally active leukotriene receptor antagonist that specifically inhibits the cysteinyl leukotriene CysLT₁ receptor.
MONTELUKAST (SINGULAIR) is described chemically as [R-(E)]-1-[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropane acetic acid, monosodium salt.
The empirical formula is C₃₅H₃₅ClNNaO₃S, and its molecular weight is 608.18.
Montelukast sodium is a hygroscopic, optically active, white to off-white powder. Montelukast sodium is freely soluble in ethanol, methanol, and water and practically insoluble in acetonitrile.

Pharmacology: Pharmacodynamics: Montelukast causes potent inhibition of airway cysteinyl leukotriene receptors as demonstrated by the ability to inhibit bronchoconstriction due to inhaled LTD₄ in asthmatic patients. Doses as low as 5 mg cause substantial blockage of LTD₄-induced bronchoconstriction.
Montelukast causes bronchodilation within 2 hours of oral administration; these effects were additive to the bronchodilation caused by a β-agonist.
Clinical studies in adults 15 years of age and older demonstrated there is no additional clinical benefit to montelukast doses above 10 mg once daily. This was shown in two chronic asthma studies using doses up to 200 mg once daily and in one exercise challenge study using doses up to 50 mg, evaluated at the end of the once-daily dosing interval.
Pharmacokinetics: Absorption: Montelukast is rapidly and nearly completely absorbed following oral administration. For the 10-mg film-coated tablet, the mean peak plasma concentration (C_max) is achieved 3 hours (T_max) after administration in adults in the fasted state. The mean oral bioavailability is 64%. The oral bioavailability and C_max are not influenced by a standard meal.
For the 5-mg chewable tablet, the C_max is achieved 2 hours after administration in adults in the fasted state. The mean oral bioavailability is 73%. Food does not have a clinically important influence with chronic administration.
For the 4-mg chewable tablet, C_max is achieved 2 hours after administration in pediatric patients 2 to 5 years of age in the fasted state.
The 4-mg oral granule formulation is bioequivalent to the 4-mg chewable tablet when administered to adults in the fasted state. The coadministration of applesauce or a standard meal with the oral granule formulation did not have a clinically meaningful effect on the pharmacokinetics of montelukast as determined by AUC (1225.7 vs 1223.1 ng·hr/mL with and without applesauce, respectively, and 1191.8 vs 1148.5 ng·hr/mL with and without a standard meal, respectively).
Safety and efficacy were demonstrated in clinical studies where the 4-mg chewable tablet, 5-mg chewable tablet, and 10-mg film-coated tablet were administered without regard to the timing of food ingestion. The safety of MONTELUKAST (SINGULAIR) was also demonstrated in a clinical study in which the 4-mg oral granules were administered without regard to the timing of food ingestion.
Distribution: Montelukast is more than 99% bound to plasma proteins. The steady-state volume of distribution of montelukast averages 8 to 11 liters. Studies in rats with radiolabeled montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabeled material at 24 hours postdose were minimal in all other tissues.
Metabolism: Montelukast is extensively metabolized. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and pediatric patients.
In vitro studies using human liver microsomes indicate that cytochrome P450 3A4, 2C8 and 2C9 are involved in the metabolism of montelukast. Based on further in vitro results in human liver microsomes, therapeutic plasma concentrations of montelukast do not inhibit cytochromes P450 3A4, 2C9, 1A2, 2A6, 2C19, or 2D6.
Elimination: The plasma clearance of montelukast averages 45 mL/min in healthy adults. Following an oral dose of radiolabeled montelukast, 86% of the radioactivity was recovered in 5-day fecal collections and <0.2% was recovered in urine. Coupled with estimates of montelukast oral bioavailability, this indicates montelukast and its metabolites are excreted almost exclusively via the bile.
In several studies, the mean plasma half-life of montelukast ranged from 2.7 to 5.5 hours in healthy young adults. The pharmacokinetics of montelukast are nearly linear for oral doses up to 50 mg. No difference in pharmacokinetics was noted between dosing in the morning or in the evening. During once-daily dosing with 10-mg montelukast, there is little accumulation of the parent drug in plasma (∼14%).
Characteristics in Patients: Gender: The pharmacokinetics of montelukast are similar in males and females.
Elderly: The pharmacokinetic profile and the oral bioavailability of a single 10-mg oral dose of montelukast are similar in elderly and younger adults. The plasma half-life of montelukast is slightly longer in the elderly. No dosage adjustment in the elderly is required.
Race: Pharmacokinetic differences due to race have not been studied. In clinical studies, there do not appear to be any differences in clinically important effects.
Hepatic Insufficiency: Patients with mild-to-moderate hepatic insufficiency and clinical evidence of cirrhosis had evidence of decreased metabolism of montelukast resulting in approximately 41% higher mean montelukast area under the plasma concentration curve (AUC) following a single 10-mg dose. The elimination of montelukast is slightly prolonged compared with that in healthy subjects (mean half-life, 7.4 hours). No dosage adjustment is required in patients with mild-to-moderate hepatic insufficiency. There are no clinical data in patients with severe hepatic insufficiency (Child-Pugh score > 9).
Renal Insufficiency: Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast were not evaluated in patients with renal insufficiency. No dosage adjustment is recommended in these patients.
Adolescents and Pediatric Patients: The plasma concentration profile of montelukast following administration of the 10-mg film-coated tablet is similar in adolescents ≥ 15 years old and young adults. The 10-mg film-coated tablet is recommended for use in patients ≥ 15 years old.
Pharmacokinetic studies show that the plasma profiles of the 4-mg oral granule formulation in pediatric patients 6 months to 2 years of age, the 4-mg chewable tablet in pediatric patients 2 to 5 years of age, and the 5-mg chewable tablets in pediatric patients 6 to 14 years of age were similar to the plasma profile of the 10-mg film-coated tablet in adults. The 5-mg chewable tablet should be used in pediatric patients 6 to 14 years of age and the 4-mg chewable tablet in pediatric patients 2 to 5 years of age. The 4-mg oral granule formulation should be used for pediatric patients 6 months to 2 years of age. Since the 4-mg oral granule formulation is bioequivalent to the 4-mg chewable tablet, it can also be used as an alternative formulation to the 4-mg chewable tablet in pediatric patients 2 to 5 years of age.
Drug Interactions: Montelukast 10 mg once daily to pharmacokinetic steady state: did not cause clinically significant changes in the kinetics of an intravenous dose of theophylline; did not change the pharmacokinetic profile of warfarin or influence the effect of a single 30-mg oral dose of warfarin on prothrombin time or INR (International Normalized Ratio); did not change the pharmacokinetic profile or urinary excretion of immunoreactive digoxin; did not change the plasma concentration profile of terfenadine or its carboxylated metabolite and did not prolong the QTc interval following co-administration with terfenadine 60 mg twice daily.
Montelukast at doses of ≥ 100 mg daily to pharmacokinetic steady state: did not significantly alter the plasma concentrations of either component of an oral contraceptive containing norethindrone 1 mg/ethinyl estradiol 35 μg; did not cause any clinically significant change in plasma profiles of either prednisone and prednisolone following administration of either oral prednisone or intravenous prednisolone.
Phenobarbital, which induces hepatic metabolism, decreased the AUC of montelukast approximately 40% following a single 10-mg dose of montelukast; no dosage adjustment for MONTELUKAST (SINGULAIR) is recommended (see PRECAUTIONS).

MONTELUKAST (SINGULAIR) is indicated in adult and pediatric patients 6 months of age and older for the prophylaxis and chronic treatment of asthma, including the prevention of day- and nighttime symptoms, the treatment of aspirin-sensitive asthmatic patients, and the prevention of exercise-induced bronchoconstriction.
MONTELUKAST (SINGULAIR) is effective alone or in combination with other agents used in the maintenance treatment of chronic asthma. MONTELUKAST (SINGULAIR) and inhaled corticosteroids may be used concomitantly with additive effects to control asthma or to reduce the inhaled corticosteroid dose while maintaining clinical stability.
MONTELUKAST (SINGULAIR) is indicated for the relief of daytime and nighttime symptoms of allergic rhinitis (seasonal allergic rhinitis in adults and pediatric patients 2 years of age and older, and perennial allergic rhinitis in adults and pediatric patients 6 months of age and older), including nasal congestion, rhinorrhea, nasal itching, sneezing; nasal congestion upon awakening, difficulty going to sleep, and nighttime awakenings; tearing, itchy, red, and puffy eyes.

Recommended Dose: MONTELUKAST (SINGULAIR) should be taken once daily. For asthma, the dose should be taken in the evening. For allergic rhinitis, the time of administration may be individualized to suit patient needs.
Patients with both asthma and allergic rhinitis should take only one tablet daily in the evening.
Adults 15 Years of Age and Older with Asthma and/or Allergic Rhinitis: The dosage for adults 15 years of age and older is one 10-mg film-coated tablet daily.
Pediatric Patients 6 to 14 Years of Age with Asthma and/or Allergic Rhinitis: The dosage for pediatric patients 6 to 14 years of age is one 5-mg chewable tablet daily.
Pediatric Patients 2 to 5 Years of Age with Asthma and/or Allergic Rhinitis: The dosage for pediatric patients 2 to 5 years of age is one 4-mg chewable tablet daily or one packet of 4-mg oral granules daily.
Pediatric Patients 6 Months to 2 Years of Age with Asthma or Perennial Allergic Rhinitis: The dosage for pediatric patients 6 months to 2 years of age is one packet of 4-mg oral granules daily.
Administration of oral granules: MONTELUKAST (SINGULAIR) oral granules can be administered either directly in the mouth, mixed with a spoonful of cold or room temperature soft food (e.g., applesauce), or dissolved in 1 teaspoonful (5mL) of cold or room temperature baby formula or breast milk. The packet should not be opened until ready to use. After opening the packet, the full dose of MONTELUKAST (SINGULAIR) oral granules must be administered immediately (within 15 minutes). If mixed with food, or dissolved in baby formula or breast milk, MONTELUKAST (SINGULAIR) oral granules must not be stored for future use. MONTELUKAST (SINGULAIR) oral granules are not intended to be dissolved in any liquid other than baby formula or breast milk for administration. However, liquids may be taken subsequent to administration.
General Recommendations: The therapeutic effect of MONTELUKAST (SINGULAIR) on parameters of asthma control occurs within one day. MONTELUKAST (SINGULAIR) tablets, chewable tablets, and oral granules can be taken with or without food. Patients should be advised to continue taking MONTELUKAST (SINGULAIR) while their asthma is controlled, as well as during periods of worsening asthma.
No dosage adjustment is necessary for pediatric patients, for the elderly, for patients with renal insufficiency, or mild-to-moderate hepatic impairment, or for patients of either gender.
Therapy with MONTELUKAST (SINGULAIR) in Relation to Other Treatments for Asthma: MONTELUKAST (SINGULAIR) can be added to a patient's existing treatment regimen.
Reduction in Concomitant Therapy: Bronchodilator Treatments: MONTELUKAST (SINGULAIR) can be added to the treatment regimen of patients who are not adequately controlled on bronchodilator alone. When a clinical response is evident (usually after the first dose), the patient's bronchodilator therapy can be reduced as tolerated.
Inhaled Corticosteroids: Treatment with MONTELUKAST (SINGULAIR) provides additional clinical benefit to patients treated with inhaled corticosteroids. A reduction in the corticosteroid dose can be made as tolerated. The dose should be reduced gradually with medical supervision. In some patients, the dose of inhaled corticosteroids can be tapered off completely. MONTELUKAST (SINGULAIR) should not be abruptly substituted for inhaled corticosteroids.
Mode of Administration: MONTELUKAST (SINGULAIR) should be taken orally. For asthma, the dose should be taken in the evening. For allergic rhinitis, the time of administration may be individualized to suit patient needs.
Patients with both asthma and allergic rhinitis should take only one tablet daily in the evening.

No specific information is available on the treatment of overdosage with MONTELUKAST (SINGULAIR). In chronic asthma studies, MONTELUKAST (SINGULAIR) has been administered at doses up to 200 mg/day to adult patients for 22 weeks and in short-term studies, up to 900 mg/day to patients for approximately one week without clinically important adverse experiences.
There have been reports of acute overdosage in postmarketing experience and clinical studies with MONTELUKAST (SINGULAIR). These include reports in adults and children with a dose as high as 1000 mg. The clinical and laboratory findings observed were consistent with the safety profile in adults and pediatric patients. There were no adverse experiences in the majority of overdosage reports. The most frequently occurring adverse experiences were consistent with the safety profile of MONTELUKAST (SINGULAIR) and included abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.
It is not known whether montelukast is dialyzable by peritoneal- or hemodialysis.

Hypersensitivity to any component of this product.

The efficacy of oral MONTELUKAST (SINGULAIR) for the treatment of acute asthma attacks has not been established. Therefore, oral MONTELUKAST (SINGULAIR) should not be used to treat acute asthma attacks. Patients should be advised to have appropriate rescue medication available.
While the dose of concomitant inhaled corticosteroid may be reduced gradually under medical supervision, MONTELUKAST (SINGULAIR) should not be abruptly substituted for inhaled or oral corticosteroids.
Neuropsychiatric events have been reported in patients taking MONTELUKAST (SINGULAIR) (see ADVERSE REACTIONS). Since other factors may have contributed to these events, it is not known if they are related to MONTELUKAST (SINGULAIR). Physicians should discuss these adverse experiences with their patients and/or caregivers. Patients and/or caregivers should be instructed to notify their physician if these changes occur.
In rare cases patients receiving anti-asthma agents including leukotriene receptor antagonists, have experienced one or more of the following: eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy sometimes diagnosed as Churg-Strauss syndrome, a systemic eosinophilic vasculitis. These cases have been sometimes associated with the reduction or withdrawal of oral corticosteroid therapy. Although a causal relationship with leukotriene receptor antagonism has not been established, caution and appropriate clinical monitoring are recommended in patients receiving MONTELUKAST (SINGULAIR).
Use in Children: MONTELUKAST (SINGULAIR) has been studied in pediatric patients 6 months to 14 years of age (see DOSAGE & ADMINISTRATION). Safety and effectiveness in pediatric patients younger than 6 months of age have not been studied. Studies have shown that MONTELUKAST (SINGULAIR) does not affect the growth rate of pediatric patients.
Two controlled clinical studies have demonstrated that MONTELUKAST (SINGULAIR) did not affect the growth rate of prepubertal pediatric patients with asthma.
Use in the Elderly: In clinical studies, there were no age-related differences in the efficacy or safety profiles of MONTELUKAST (SINGULAIR).

MONTELUKAST (SINGULAIR) should be used during pregnancy only if clearly needed.
It is not known if MONTELUKAST (SINGULAIR) is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when MONTELUKAST (SINGULAIR) is given to a nursing mother.

MONTELUKAST (SINGULAIR) has been generally well tolerated. Side effects, which usually were mild, generally did not require discontinuation of therapy. The overall incidence of side effects reported with MONTELUKAST (SINGULAIR) was comparable to placebo.
Adults 15 Years of Age and Older with Asthma: MONTELUKAST (SINGULAIR) has been evaluated in approximately 2600 adult patients 15 years of age and older in clinical studies. In two similarly designed, 12-week placebo-controlled clinical studies, the only adverse experiences reported as drug related in ≥ 1% of patients treated with MONTELUKAST (SINGULAIR) and at a greater incidence than in patients treated with placebo were abdominal pain and headache. The incidences of these events were not significantly different in the two treatment groups.
Cumulatively, 544 patients were treated with MONTELUKAST (SINGULAIR) for at least 6 months, 253 for one year and 21 for 2 years in clinical studies. With prolonged treatment, the adverse experience profile did not change.
Pediatric Patients 6 to 14 Years of Age with Asthma: MONTELUKAST (SINGULAIR) has been evaluated in approximately 475 pediatric patients 6 to 14 years of age. The safety profile in pediatric patients is generally similar to the adult safety profile and to placebo.
In an 8-week, placebo-controlled clinical study, the only adverse experience reported as drug related in > 1% of patients treated with MONTELUKAST (SINGULAIR) and at a greater incidence than in patients treated with placebo was headache. The incidence of headache was not significantly different in the two treatment groups.
In studies evaluating growth rate, the safety profile in these pediatric patients was consistent with the safety profile previously described for MONTELUKAST (SINGULAIR).
Cumulatively, 263 pediatric patients 6 to 14 years of age were treated with MONTELUKAST (SINGULAIR) for at least 3 months and 164 for 6 months or longer. With prolonged treatment, the adverse experience profile did not change.
Pediatric Patients 2 to 5 Years of Age with Asthma: MONTELUKAST (SINGULAIR) has been evaluated in 573 pediatric patients 2 to 5 years of age. In a 12-week, placebo-controlled clinical study, the only adverse experience reported as drug related in > 1% of patients treated with MONTELUKAST (SINGULAIR) and at a greater incidence than in patients treated with placebo was thirst. The incidence of thirst was not significantly different in the two treatment groups.
Cumulatively, 426 pediatric patients 2 to 5 years of age were treated with MONTELUKAST (SINGULAIR) for at least 3 months, 230 for 6 months or longer, and 63 patients for 12 months or longer. With prolonged treatment, the adverse experience profile did not change.
Pediatric Patients 6 Months to 2 Years of Age with Asthma: MONTELUKAST (SINGULAIR) has been evaluated in 175 pediatric patients 6 months to 2 years of age. In a 6-week, placebo-controlled clinical study, the adverse experiences reported as drug related in > 1% of patients treated with MONTELUKAST (SINGULAIR) and at a greater incidence than in patients treated with placebo were diarrhea, hyperkinesia, asthma, eczematous dermatitis and rash. The incidences of these adverse experiences were not significantly different in the two treatment groups.
Adults 15 Years of Age and Older with Seasonal Allergic Rhinitis: MONTELUKAST (SINGULAIR) has been evaluated in 2199 adult patients 15 years of age and older for the treatment of seasonal allergic rhinitis in clinical studies. MONTELUKAST (SINGULAIR) administered once daily in the morning or in the evening was generally well tolerated with a safety profile similar to that of placebo. In placebo-controlled clinical studies, no adverse experiences reported as drug related in ≥ 1% of patients treated with MONTELUKAST (SINGULAIR) and at a greater incidence than in patients treated with placebo were observed. In a 4-week, placebo-controlled clinical study, the safety profile was consistent with that observed in 2-week studies. The incidence of somnolence was similar to that of placebo in all studies.
Pediatric Patients 2 to 14 Years of Age with Seasonal Allergic Rhinitis: MONTELUKAST (SINGULAIR) has been evaluated in 280 pediatric patients 2 to 14 years of age for the treatment of seasonal allergic rhinitis in a 2-week, placebo-controlled, clinical study. MONTELUKAST (SINGULAIR) administered once daily in the evening was generally well tolerated with a safety profile similar to that of placebo. In this study, no adverse experiences reported as drug related in ≥ 1% of patients treated with MONTELUKAST (SINGULAIR) and at a greater incidence than in patients treated with placebo were observed.
Adults 15 Years of Age and Older with Perennial Allergic Rhinitis: MONTELUKAST (SINGULAIR) has been evaluated in 3235 adult and adolescent patients 15 years of age and older with perennial allergic rhinitis in two, 6-week, placebo-controlled, clinical studies. MONTELUKAST (SINGULAIR) administered once daily was generally well tolerated, with a safety profile consistent with that observed in patients with seasonal allergic rhinitis and similar to that of placebo. In these two studies, no adverse experiences reported as drug related in ≥ 1% of patients treated with MONTELUKAST (SINGULAIR) and at a greater incidence than in patients treated with placebo were observed. The incidence of somnolence was similar to that of placebo.
Pooled Analyses of Clinical Trials Experience: A pooled analysis of 41 placebo-controlled clinical studies (35 studies in patients 15 years of age and older; 6 studies in pediatric patients 6 to 14 years of age) was performed using a validated assessment method of suicidality. Among the 9929 patients who received MONTELUKAST (SINGULAIR) and 7780 patients who received placebo in these studies, there was one patient with suicidal ideation in the group taking MONTELUKAST (SINGULAIR). There were no completed suicides, suicide attempts or preparatory acts toward suicidal behavior in either treatment group.
A separate pooled analysis of 46 placebo-controlled clinical studies (35 studies in patients 15 years of age and older; 11 studies in pediatric patients 3 months to 14 years of age) assessing behavior-related adverse experiences (BRAEs) was performed. Among the 11,673 patients who received MONTELUKAST (SINGULAIR) and 8827 patients who received placebo in these studies, the frequency of patients with at least one BRAE was 2.73% in patients who received MONTELUKAST (SINGULAIR) and 2.27% in patients who received placebo; the odds ratio was 1.12 (95% CI [0.93; 1.36]).
The clinical trials included in these pooled analyses were not designed specifically to examine suicidality or BRAEs.
Postmarketing Experience: The following side effects have been reported in postmarketing use: Infections and infestations: upper respiratory infection.
Blood and lymphatic system disorders: increased bleeding tendency, thrombocytopenia.
Immune system disorders: hypersensitivity reactions including anaphylaxis, very rarely hepatic eosinophilic infiltration.
Psychiatric disorders: agitation including aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, dysphemia (stuttering), hallucinations, insomnia, memory impairment, obsessive-compulsive symptoms, psychomotor hyperactivity (including irritability, restlessness, and tremor) somnambulism, suicidal thinking and behavior (suicidality), tic.
Nervous system disorders: dizziness, drowsiness, paraesthesia/hypoesthesia, very rarely seizure.
Cardiac disorders: palpitations.
Respiratory, thoracic and mediastinal disorders: epistaxis, pulmonary eosinophilia.
Gastrointestinal disorders: diarrhea, dyspepsia, nausea, vomiting.
Hepatobiliary disorders: increased ALT and AST, very rarely hepatitis (including cholestatic, hepatocellular, and mixed-pattern liver injury).
Skin and subcutaneous tissue disorders: angioedema, bruising, erythema multiforme, erythema nodosum, pruritus, rash, urticaria.
Musculoskeletal and connective tissue disorders: arthralgia, myalgia including muscle cramps.
Renal and urinary disorders: enuresis in children.
General disorders and administration site conditions: asthenia/fatigue, edema, pyrexia.

MONTELUKAST (SINGULAIR) may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma, and in the treatment of allergic rhinitis. In drug-interactions studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.
The area under the plasma concentration-time curve (AUC) for montelukast was decreased approximately 40% in subjects with co-administration of phenobarbital. No dosage adjustment for MONTELUKAST (SINGULAIR) is recommended.
In vitro studies have shown that montelukast is an inhibitor of CYP 2C8. However, data from a clinical drug-drug interaction study involving montelukast and rosiglitazone (a probe substrate representative of drugs primarily metabolized by CYP2C8) demonstrated that montelukast does not inhibit CYP2C8 in vivo. Therefore, montelukast is not anticipated to alter the metabolism of drugs metabolized by this enzyme (e.g. paclitaxel, rosiglitazone, and repaglinide.)
In vitro studies have shown that montelukast is a substrate of CYP 2C8, 2C9, and 3A4. Data from a clinical drug-drug interaction study involving montelukast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) demonstrated that gemfibrozil increased the systemic exposure of montelukast by 4.4-fold. Co-administration of itraconazole, a strong CYP 3A4 inhibitor, with gemfibrozil and montelukast did not further increase the systemic exposure of montelukast. The effect of gemfibrozil on systemic exposure of montelukast is not considered to be clinically meaningful based on clinical safety data with doses greater than the 10 mg approved dose in adults (e.g., 200 mg/day to adult patients for 22 weeks, and up to 900 mg/day to patients for approximately one week) where clinically important adverse experiences were not observed. Therefore, no dosage adjustment of montelukast is required upon co-administration with gemfibrozil. Based on in vitro data, clinically important drug interactions with other known inhibitors of CYP 2C8 (e.g., trimethoprim) are not anticipated. In addition, co-administration of montelukast with itraconazole alone resulted in no significant increase in the systemic exposure of montelukast.

MONTELUKAST (SINGULAIR) 4mg Chewable Tablet, 5 mg Chewable Tablet, 10mg Film-Coated Tablet and 4mg Oral Granules: Store at temperatures not exceeding 30°C.
Protect from moisture and light.

Antiasthmatic & COPD Preparations

R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.

Rx