Duramont

Montelukast sodium.

Duramont tablet also contains the following excipients: Red oxide of iron, yellow oxide of iron and titanium dioxide as colorants.

Pharmacology: Montelukast sodium is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene CysLT receptor.
Mechanism of Action: The cysteinyl leukotrienes (LTC4, LTD4, LTE4) 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. 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 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 is an orally active compound that binds with high affinity and selectivity to the CysLT1 receptor (in preference to other pharmacologically important airway receptors eg, prostanoid, cholinergic or β-adrenergic receptor). Montelukast inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.
Pharmacokinetics:  Montelukast is rapidly absorbed following oral administration. After administration of the 10-mg tablet, the mean peak montelukast plasma concentration (C_max) is achieved in 3-4 hrs (T_max). The mean oral bioavailability is 64%. Montelukast is >99% bound to plasma proteins. The steady-state volume of distribution of montelukast averages 8-11 L. Studies in rats with radiolabeled montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabeled material at 24 hrs post-dose were minimal in all other tissues. Montelukast is extensively metabolized. In vitro studies using human liver microsomes indicate that cytochromes P-450 3A4 and 2C9 are involved in the metabolism of montelukast.
The plasma clearance of montelukast averaged 45 mL/min in healthy adults. Montelukast and its metabolite are excreted almost exclusively via the bile. In several studies, the mean plasma half-life (t_½) of montelukast ranged from 2.7-5.5 hrs in healthy young adults.
The pharmacokinetics of montelukast are similar in males and females. 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 t_½ of montelukast is slightly longer in the elderly. No dosage adjustment in the elderly is required.
Hepatic Insufficiency: No dosage adjustment is required in patients with mild to moderate hepatic insufficiency. The pharmacokinetics of montelukast in patients with more severe hepatic impairment or with hepatitis have not been evaluated.
Renal Insufficiency: Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast have not been evaluated in patients with renal insufficiency. No dosage adjustment is recommended in these patients.

For the prophylaxis and chronic treatment of asthma, prevention of exercise-induced bronchoconstriction and the relief of symptoms of seasonal allergic rhinitis.

Adults and Adolescents ≥15 years: Usual dose: 10 mg once daily.
Children ( 6-14 years): 5 mg once daily.
Seasonal Allergic Rhinitis: Adults and Children ≥15 years: 10 mg once daily in the evening.
Exercise-Induced Bronchoconstriction (EIB): For prevention of EIB, a single dose of montelukast should be taken at least 2 hrs before exercise. An additional dose of montelukast should not be taken within 24 hrs of a previous dose. Patients already taking 1 tab daily for another indication (including chronic asthma) should not take an additional dose to prevent EIB. All patients should have available for rescue, a short-acting β-agonist.

Hypersensitivity to montelukast or to any component of Duramont.

General: 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. Patients who have exacerbations of asthma after exercise should have available for rescue, a short-acting inhaled β-agonist.
While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, montelukast should not be abruptly substituted for inhaled or oral corticosteroids.
Patients with known aspirin sensitivity should continue avoidance of aspirin or nonsteroidal anti-inflammatory agents while taking montelukast.
Use in pregnancy: Pregnancy Category B: No teratogenicity was observed in animal studies. Montelukast crosses the placenta following oral dosing in rats and rabbits. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, montelukast should be used during pregnancy only if clearly needed.
Use in lactation: Studies in rats have shown that montelukast is excreted in milk. It is not known if montelukast is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when montelukast is given to a nursing mother.

Use in pregnancy: Pregnancy Category B: No teratogenicity was observed in animal studies. Montelukast crosses the placenta following oral dosing in rats and rabbits. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, montelukast should be used during pregnancy only if clearly needed.
Use in lactation: Studies in rats have shown that montelukast is excreted in milk. It is not known if montelukast is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when montelukast is given to a nursing mother.

Montelukast is generally well tolerated with a safety profile similar to that of placebo.
Asthenia/fatigue, fever, abdominal pain, trauma, dyspepsia, gastroenteritis, dental pain, dizziness, headache, congestion, nasal cough, influenza, rash may occur in some patients.
The additional adverse reactions reported in post-marketing use include hypersensitivity reactions, hallucinations, drowsiness, irritability, restlessness, tremor, depression, insomnia, paraesthesia/hypoesthesia and very rarely seizures; muscle cramps; increased bleeding tendency, bruising; palpitations; edema; nausea, vomiting, dyspepsia, diarrhea, thirst, hyperkinesis (in young children), sleep disturbances, abnormal dreams, agitation, aggression, seizures, arthralgia, pruritus and Churg Strauss syndrome have also been reported.

Montelukast has been administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma with no apparent increase in adverse reactions. In drug interaction 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 (norethindrone 1 mg/ethinyl estradiol 35 mcg), terfenadine, digoxin and warfarin. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P-450 enzyme inducers eg, phenobarbital or rifampin, are co-administered with montelukast.

Store at temperature not exceeding 30°C.
Shelf-life: 24 months.

Antiasthmatic & COPD Preparations / Antihistamines & Antiallergics

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

POM

FC tab 10 mg x 10's.