Monlastik

Each film-coated tablet contains: Montelukast (as Sodium) 10 mg.

Leukotriene Receptor Antagonist.
Pharmacology: Mechanism of Action: Montelukast is an orally active compound that binds with high affinity and selectively to the cysteinyl leukotrienes type-1 (CysLT1) receptor (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or beta-adrenergic 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 airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process. 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. Montelukast inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.
Pharmacokinetics: Peak plasma concentrations of Montelukast are achieved in 3 to 4 hours after oral doses. The mean oral bioavailability is 64%. Montelukast is more than 99% bound to plasma proteins. It is extensively metabolized in the liver by cytochrome P450 isoenzymes CYP3A4, CYP2A6, and CYP2C9, and is excreted principally in the feces via the bile.

Montelukast is indicated for chronic treatment of asthma in adults and pediatric patients 12 months of age and older.
Montelukast is indicated for the relief of 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).

Montelukast 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.
Pediatric Patients 6 to 14 years of age with asthma and/or allergic rhinitis: One 5 mg chewable tablet daily. No dosage adjustment.
Pediatric Patients 2 to 5 years of age with asthma and/or allergic rhinitis: One 4 mg chewable tablet daily.
Exercise-induced Bronchoconstriction (EIB) in patients 15 years of age and older: For prevention of EIB, a single dose of Montelukast tablets should be taken at least 2 hours before exercise. An additional dose of Montelukast should not be taken within 24 hours of a previous dose. Patients already taking one tablet daily for another indication (including chronic asthma) should not take an additional dose to prevent EIB. A short-acting (beta)-agonist should be available for rescue of patients.
Or as prescribed by the physician.

Hypersensitivity to any component of this product.

Montelukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus.
Patients should be advised to have appropriate rescue medication available. Therapy with Montelukast can be continued during acute exacerbations of asthma. While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, Montelukast should not be abruptly substituted for inhaled or oral corticosteroids.
Montelukast should not be used as monotherapy for the therapy and management of exercise-induced bronchospasm. Patients who have exacerbations of asthma after exercise should continue to use their usual regimen of inhaled (beta)-agonist as prophylaxis and have available for rescue a short-acting inhaled (beta)-agonist. Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking Montelukast. Although Montelukast is effective improving airway function in asthmatics with documented aspirin sensitivity, it has not been shown to truncate bronchoconstrictor response to aspirin and other non-steroidal anti-inflammatory drugs in aspirin-sensitive asthmatic patients.
Eosinophilic Conditions: In rare cases, patients with asthma on therapy with Montelukast may present with systemic. Physicians should be alerted to eosinophilia, vasolitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients.

Common side effects include dyspepsia, abdominal pain, rash, dizziness, headache, fatigue, fever, trauma, cough, nasal congestion.
Blood and lymphatic system disorders: Increased bleeding tendency.
Immune system disorders: Hypersensitivity reactions including anaphylaxis hepatic eosinophilic infiltration.
Psychiatric disorders: Dream abnormalities including nightmares, hallucinations, insomnia, irritability, anxiety, restlessness, agitations including aggressive behavior, tremor, depression, suicidal thinking and behavior (suicidality) in very rare cases.
Nervous system disorders: Dizziness, drowsiness, paresthesia/hypoesthesia, seizure.
Cardiac disorders: Palpitations.
Gastrointestinal disorders: Diarrhea, dry mouth, dyspepsia, nausea, vomiting.
Hepatobiliary disorders: Elevated levels of serum transaminases (ALT, AST), cholestatic hepatitis.
Skin and subcutaneous tissue disorders: Angioedema, bruising, urticaria, pruritus, rash, erythema nodosum.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia including muscle cramps.
General disorders and administration site conditions: Asthenia/fatigue, malaise, oedema.
Very rare cases of Churg-Strauss Syndrome (CSS) have been reported during Montelukast treatment in asthmatic patients. In rare cases, patients with asthma on therapy with Montelukast may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome. A casual association between Montelukast and these underlying conditions has not been established.

Licensed product information recommends caution when potent inducers of the cytochrome P450 isoenzyme CYP3A4 such as phenytoin, phenobarbital, or rifampicin are given with Montelukast.
On Corticosteroids, with reports of peripheral oedema in patients given Montelukast and prednisone.
With Phenobarbital, peak serum concentrations after a single dose of Montelukast 10 mg were reduced by 20% in 14 healthy subjects who took phenobarbital 100 mg daily for 14 days, and area under the serum concentration-time curve was reduced by 38%. However, it was not thought that montelukast doses would need adjustment if given with phenobarbital.

Store at temperatures not exceeding 30°C. Protect from light and moisture.

Antiasthmatic & COPD Preparations

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

Rx