Full Prescribing Info
Montelukast sodium.
Each film coated tablet contains: Montelukast sodium USP equivalent to Montelukast 10 mg.
Excipients/Inactive Ingredients: Microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulphate, magnesium stearate, purified water and opadry 20A520035 yellow.
Pharmacotherapeutic group: Leukotriene receptor antagonist. ATC code: R03DC03.
Pharmacology: Pharmacodynamics: The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids released from various cells including mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT1) receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other pro-inflammatory cells (including eosinophils and certain myeloid stem cells). CysLTs have been correlated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitment. In allergic rhinitis, CysLTs are released from the nasal mucosa after allergen exposure during both early- and late-phase reactions and are associated with symptoms of allergic rhinitis. Intranasal challenge with CysLTs has been shown to increase nasal airway resistance and symptoms of nasal obstruction.
Pharmacodynamic effects: Montular contains Montelukast which is an orally active compound and binds with high affinity and selectivity to the CysLT1 receptor. In clinical studies, montelukast inhibits bronchoconstriction due to inhaled LTD4 at doses as low as 5 mg. Bronchodilation was observed within 2 hours of oral administration. The bronchodilation effect caused by a beta-agonist was additive to that caused by montelukast. Treatment with montelukast inhibited both early- and late-phase bronchoconstriction due to antigen challenge. Montelukast, compared with placebo, decreased peripheral blood eosinophils in adult and paediatric patients. In a separate study, treatment with montelukast significantly decreased eosinophils in the airways (as measured in sputum) and in peripheral blood while improving clinical asthma control.
Pharmacokinetics: Absorption: Montelukast is rapidly absorbed following oral administration. For the 10-mg film-coated tablet, the mean peak plasma concentration (Cmax) is achieved 3 hours (Tmax) after administration in adults in the fasted state. The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal. Safety and efficacy were demonstrated in clinical trials where the 10mg film-coated tablet was 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 8-11 liters. Studies in rats with radiolabelled montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabelled 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 children.
Cytochrome P450 2C8 is the major enzyme in the metabolism of montelukast. Additionally CYP 3A4 and 2C9 may have a minor contribution, although itraconazole, an inhibitor of CYP 3A4, was shown not to change pharmacokinetic variables of montelukast in healthy subjects that received 10 mg montelukast daily.
In vitro studies using human liver microsomes indicate that cytochrome P450, 3A4, 2A6 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. The contribution of metabolites to the therapeutic effect of montelukast is minimal.
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 that montelukast and its metabolites are excreted almost exclusively via the bile.
Characteristics in Patients: No dosage adjustment is necessary for the elderly or mild to moderate hepatic insufficiency. Studies in patients with renal impairment have not been undertaken. Because montelukast and its metabolites are eliminated by the biliary route, no dose adjustment is anticipated to be necessary in patients with renal impairment. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (Child-Pugh score >9).
With high doses of montelukast (20 and 60 fold the recommended adult dose), decrease in plasma theophylline concentration was observed. This effect was not seen at the recommended dose of 10 mg once daily.
Montular is indicated in the treatment of asthma as add-on therapy in those patients with mild to moderate persistent asthma who are inadequately controlled on inhaled corticosteroids and in whom "as-needed" short acting beta-agonists provide inadequate clinical control of asthma. In those asthmatic patients in whom Montular is indicated in asthma, Montular can also provide symptomatic relief of seasonal allergic rhinitis.
Montular is also indicated in the prophylaxis of asthma in which the predominant component is exercise-induced bronchoconstriction.
Dosage/Direction for Use
Dosage: The dosage for adults and adolescents 15 years of age and older with asthma, or with asthma and concomitant seasonal allergic rhinitis is one 10-mg tablet daily to be taken in the evening.
General recommendations: The therapeutic effect of Montular on parameters of asthma control occurs within one day. Montular may be taken with or without food. Patients should be advised to continue taking Montular even if their asthma is under control, as well as during periods of worsening asthma. Montular should not be used concomitantly with other products containing the same active ingredient, montelukast.
No dosage adjustment is necessary for the elderly, or for patients with renal insufficiency, or mild to moderate hepatic impairment. There are no data on patients with severe hepatic impairment. The dosage is the same for both male and female patients.
Therapy with Montular in relation to other treatments for asthma: Montular can be added to a patient's existing treatment regimen.
Inhaled corticosteroids: Treatment with Montular can be used as add-on therapy in patients when inhaled corticosteroids plus "as needed" short acting beta-agonists provide inadequate clinical control. Montular should not be substituted for inhaled corticosteroids.
Montelukast should not be used in children below 15 years of age due to the high content of active substance.
Other dosage forms with appropriate strengths are available for younger children.
Mode of administration: Oral.
In chronic asthma studies, montelukast 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 overdose in post-marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1,000 mg (approximately 61 mg/kg in a 42 month old child). The clinical and laboratory findings observed were consistent with the safety profile in adults and paediatric patients. There were no adverse experiences in the majority of overdose reports.
Symptoms of overdose: The most frequently occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.
Management of overdose: No specific information is available on the treatment of overdose with montelukast. It is not known whether montelukast is dialysable by peritoneal- or haemodialysis.
Hypersensitivity to the active substance or to any of the excipients listed previously.
Special Precautions
Patients should be advised never to use oral montelukast to treat acute asthma attacks and to keep their usual appropriate rescue medication for this purpose readily available. If an acute attack occurs, a short-acting inhaled β-agonist should be used. Patients should seek their doctors' advice as soon as possible if they need more inhalations of short-acting β-agonists than usual.
Montelukast should not be substituted abruptly for inhaled or oral corticosteroids.
There are no data demonstrating that oral corticosteroids can be reduced when montelukast is given concomitantly.
In rare cases, patients on therapy with anti-asthma agents including montelukast may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. 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, physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. Patients who develop these symptoms should be reassessed and their treatment regimens evaluated.
Treatment with montelukast does not alter the need for patients with aspirin-sensitive asthma to avoid taking aspirin and other non-steroidal anti-inflammatory drugs.
Effects on Ability to Drive and Use Machines: Montular is not expected to affect a patient's ability to drive a car or operate machinery. However, in very rare cases, individuals have reported drowsiness or dizziness.
Use In Pregnancy & Lactation
Pregnancy: Animal studies do not indicate harmful effects with respect to effects on pregnancy or embryonal/fetal development.
Limited data from available pregnancy databases do not suggest a causal relationship between montelukast and malformations (i.e. limb defects) that have been rarely reported in worldwide post marketing experience.
Montular may be used during pregnancy only if it is considered to be clearly essential.
Lactation: Studies in rats have shown that montelukast is excreted in milk. It is not known if montelukast is excreted in human milk.
Montular may be used in nursing mothers only if it is considered to be clearly essential.
Adverse Reactions
The following drug-related adverse reactions in clinical studies were reported commonly (≥1/100 to <1/10) in asthmatic patients treated with montelukast and at a greater incidence than in patients treated with placebo: See table.

Click on icon to see table/diagram/image

With prolonged treatment in clinical trials with a limited number of patients for up to 2 years for adults, and up to 12 months for paediatric patients 6 to 14 years of age, the safety profile did not change.
Post-marketing Experience: Adverse reactions reported in post-marketing use are listed by System Organ Class and specific adverse experience term as follows. Frequency categories were estimated based on relevant clinical trials.
Each Adverse Experience Term by the incidence reported in the clinical trials data base: Very Common (≥1/10), Common (≥1/100 to <1/10), Uncommon (≥1/1000 to <1/100), Rare (≥1/10,000 to <1/1000), Very Rare (<1/10,000).
Infections and infestations: Very common: Upper respiratory infection@.
Blood and lymphatic system disorders: Rare: Increased bleeding tendency.
Immune system disorders: Uncommon: Hypersensitivity reactions including anaphylaxis.
Very rare: Hepatic eosinophilic infiltration.
Psychiatric disorders: Uncommon: Dream abnormalities including nightmares, insomnia, somnambulism, anxiety, agitation including aggressive behaviour or hostility, depression, psychomotor hyperactivity (including irritability, restlessness, tremor).
Rare: Disturbance in attention, memory impairment.
Very rare: Hallucinations, disorientation, suicidal thinking and behaviour (suicidality).
Nervous system disorders: Uncommon: Dizziness, drowsiness, paraesthesia/hypoesthesia, seizure.
Cardiac disorders: Rare: Palpitations.
Respiratory, thoracic and mediastinal disorders: Uncommon: Epistaxis.
Very rare: Churg-Strauss Syndrome (CSS) (see Precautions).
Very rare: Pulmonary eosinophilia.
Gastrointestinal disorders: Common: Diarrhoea**, nausea**, vomiting**.
Uncommon: Dry mouth, dyspepsia.
Hepato-biliary disorders: Common: Elevated levels of serum transaminases (ALT, AST).
Very Rare: Hepatitis (including cholestatic, hepatocellular, and mixed-pattern liver injury).
Skin and subcutaneous tissue disorders: Common: Rash**.
Uncommon: Bruising, urticaria, pruritus.
Rare: Angiooedema.
Very Rare: Erythema nodosum, erythema multiforme.
Musculoskeletal and connective tissue disorders: Uncommon: Arthralgia, myalgia including muscle cramps.
General disorders and administration site conditions: Common: Pyrexia**.
Uncommon: Asthenia/fatigue, malaise, oedema.
@This adverse experience, reported as very common in the patients who received montelukast, was also reported as very common in the patients who received placebo in clinical trials.
**This adverse experience, reported as common in the patients who received montelukast, was also reported as common in the patients who received placebo in clinical trials.
§ Frequency Category: Rare.
Adverse Drug Reactions: Inform doctors about unexpected reactions after using drugs.
Drug Interactions
Montelukast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma. In drug-interactions studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following medicinal products: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/l), terfenadine, digoxin and warfarin.
The area under the plasma concentration curve (AUC) for montelukast was decreased approximately 40% in subjects with co-administration of phenobarbital. Since montelukast is metabolised by CYP 3A4, 2C8, and 2C9, caution should be exercised, particularly in children, when montelukast is co-administered with inducers of CYP 3A4, 2C8, and 2C9, such as phenytoin, phenobarbital and rifampicin.
In vitro studies have shown that montelukast is a potent inhibitor of CYP 2C8. However, data from a clinical drug-drug interaction study involving montelukast and rosiglitazone (a probe substrate representative of medicinal products primarily metabolized by CYP 2C8) demonstrated that montelukast does not inhibit CYP 2C8 in vivo. Therefore, montelukast is not anticipated to markedly alter the metabolism of medicinal products metabolised by this enzyme (e.g., paclitaxel, rosiglitazone, and repaglinide).
In vitro studies have shown that montelukast is a substrate of CYP 2C8, and to a less significant extent, of 2C9, and 3A4. In a clinical drug-drug interaction study involving montelukast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) gemfibrozil increased the systemic exposure of montelukast by 4.4-fold. No routine dosage adjustment of montelukast is required upon co-administration with gemfibrozil or other potent inhibitors of CYP 2C8, but the physician should be aware of the potential for an increase in adverse reactions.
Based on in vitro data, clinically important drug interactions with less potent inhibitors of CYP 2C8 (e.g., trimethoprim) are not anticipated. Co-administration of montelukast with itraconazole, a strong inhibitor of CYP 3A4, resulted in no significant increase in the systemic exposure of montelukast.
Store below 30°C.
Shelf Life: 24 months.
MIMS Class
Antiasthmatic & COPD Preparations / Antihistamines & Antiallergics
ATC Classification
R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.
FC tab 10 mg (beige colored, round shape, biconvex, plain on both sides) x 10 x 10's.
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