Montelukast Sodium

• G-G-Montelukast is indicated for:
• Prophylaxis and chronic treatment of asthma
• Acute prevention of Exercise-Induced Bronchoconstriction (EIB)

Relief of symptoms of Allergic Rhinitis (AR): Seasonal & Perennial Allergic Rhinitis

Montelukast is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene receptor (CysLT 1 ). 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. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma & allergic rhinitis, including airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.

Adults and adolescents with asthma or seasonal allergic rhinitis:

The dosage for adults and adolescents 15 years of age and older : Montelukast 10 mg tablet once daily.

Pediatric patients with asthma or seasonal allergic rhinitis:

The dosage for pediatric patients 6 to 14 years of age : Montelukast 5 mg tablet once daily.

The dosage for pediatric patients 2 years to 5 years of age : Montelukast 4 mg tablet once daily.

The dosage for pediatric patients 6 months to 5 years of age : Montelukast 4 mg oral granules once daily. This can be administered either directly in the mouth, or mixed with a spoonful of cold water or soft food at room temperature

Use in the pediatric patient : The safety and efficacy of Montelukast have been established in adequate and well-controlled studies in pediatric patients with asthma 6 months to 14 years of age. Safety and efficacy profiles in this age group are similar to those seen in adults. Hepatic Insufficiency : No dosage adjustment is required in patients with mild-to-moderate hepatic insufficiency. Renal Insufficiency : No dosage adjustment is recommended in patients with renal insufficiency. Elderly use : 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.

G-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 G-Montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (norethindrone 1mg/ethinyl estradiol 35mcg), terfenadine, digoxin, and warfarin. Although additional specific interaction studies were not performed, G-Montelukast was used concomitantly with a wide range of commonly prescribed drugs in clinical studies without evidence of clinical adverse interactions. These medications included thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines and decongestants. Phenobarbital, which induces hepatic metabolism, decreased the AUC of G-Montelukast approximately 40% following a single 10mg dose of G-Montelukast. No dosage adjustment for G-Montelukast is recommended. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P450 enzyme inducers, such as phenobarbital or rifampin, are co-administered with G-Montelukast.

Montelukast is contraindicated in patients who are hypersensitive to any component of this product.

Common : Diarrhoea, fever, gastrointestinal discomfort, headache, nausea, vomiting, skin reactions, upper respiratory tract infection. Uncommon : Akathisia, anxiety, arthralgia, asthenia, abnormal behavior, depression, dizziness, drowsiness, dry mouth, haemorrhage, irritability, malaise, muscle complaints, oedema, seizure, abnormal sensation, sleep disorders. Rare : Angioedema, concentration impaired, disorientation, eosinophilic granulomatosis with polyangiitis, erythema nodosum, hallucination, hepatic disorders, memory loss, palpitations, pulmonary eosinophilia, suicidal tendencies, tremor.

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. Because many drugs are excreted in human milk, caution should be exercised when Montelukast  is given to a nursing mother.

G-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 G-Montelukast can be continued during acute exacerbations of asthma. While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, G-Montelukast should not be abruptly substituted for inhaled or oral corticosteroids. G-Montelukast should not be used as monotherapy for the treatment and management of exercise induced bronchospasm. Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking G-Montelukast. Although G-Montelukast is effective in 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.

There were no adverse experiences in the majority of overdosage reports. The most frequently occurring adverse experiences were consistent with the safety profile of G-Montelukast and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity. 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.

Store in cool & dry place below 30°C, protect from light & moisture. Keep out of reach of children.