Monte

Rx  MONTE

COMPOSITION:

MONTE* 4 Tablet: Each dispersible tablet contains:

Montelukast sodium equivalent to Montelukast   4mg

MONTE* 5 Tablet: Each chewable tablet contains:

Montelukast sodium equivalent to Montelukast   5mg

MONTE* 10 Tablet: Each film-coated tablet contains:

Montelukast sodium equivalent to Montelukast   10mg

DESCRIPTION:

Montelukast sodium, the active ingredient in montelukast sodium tablets, is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene CysLT1 receptor. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma ( such as, airway edema, smooth muscle contraction and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma). The empirical formula is C35H35CINNaO3S, and its molecular weight is 608.18. The structural formula is:

PHARMACODYNAMICS:

The cysteinyl leukotrienes (LTC 4, LTD 4, LTE 4) are potent inflammatory eicosanoids released from various cells including mast cells and eosinophils. These important proasthmatic mediators bind to cysteinyl leukotriene receptors (CysLT) found in the human airway and cause a number of airway actions, including bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitment. Montelukast potently inhibits physiologic actions of LTC 4, LTD 4, and LTE 4 at the CysLT 1 receptor without any agonist activity.

PHARMACOKINETICS:

Absorption:

Montelukast is rapidly absorbed following oral administration. After administration of the 10-mg film-coated tablet to fasted adults, the mean peak montelukast plasma concentration (Cmax) is achieved in 3 to 4 hours (Tmax). The mean oral bioavailability is 64%. The oral bioavailabilty and Cmax are not influenced by a standard meal in the morning.

Montelukast 4 mg dispersible tablet the mean C_max is achieved 2 hours after administration in pediatric patients 2 to 5 years of age in the fasted state.

For the 5-mg chewable tablet, the mean Cmax is achieved in 2 to 2.5 hours after administration to adults in the fasted state. The mean oral bioavailabilty is 73% in the fasted state versus 63% when administered with a standard meal in the morning.

Distribution:

Montelukast is more than 99% bound to plasma proteins. The steady state volume of distribution of montelukast averages 8 to 11 liters. 

Metabolism:

Montekulast is extensively metabolized in liver and its metabolites are excreted almost exclusively via the bile

Excretion:

The plasma clearance of montelukast averages 45 mL/min in healthy adults. 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 is nearly linear for oral doses up to 50 mg. No difference in pharmacokinetics was noted between dosing in the morning or in the evening.

INDICATIONS:

      MONTE (Montelukast) is indicated for prophylaxis and chronic treatment of asthma,

      MONTE (Montelukast) is indicated to relieve runny nose caused by allergies,

      MONTE (Montelukast) is indicated to relieve runny nose caused by allergies

      MONTE (Montelukast) is indicated for treatment of ASA- sensitive asthma (Aspirin induced asthma),

      MONTE (Montelukast) is indicated for prevention of exercise-induced bronchoconstriction,

      MONTE (Montelukast) is indicated for atopic dermatitis,

      MONTE (Montelukast) is indicated for chronic idiopathic urticaria.

CONTRAINDICATIONS:

Montelukast is contraindicated to patients with hypersensitivity to any component of this product.

WARNING AND PRECAUTIONS:

·         Acute Asthma

Montelukast sodium 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 sodium 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.

·         Concomitant Corticosteroid Use

While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, montelukast sodium should not be abruptly substituted for inhaled or oral corticosteroids.

·         Aspirin Sensitivity

Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking montelukast sodium. Although montelukast sodium 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.

·         Neuropsychiatric Events

Neuropsychiatric events have been reported in adult, adolescent, and pediatric patients taking montelukast sodium. Post-marketing reports with montelukast sodium use include agitation, aggressive behavior or hostility, anxiousness, depression, disorientation,disturbance in attention, dream abnormalities, hallucinations, insomnia, irritability, memory impairment, restlessness, somnambulism, suicidal thinking and behavior (including suicide), and tremor. The clinical details of some post-marketing reports involving montelukast sodium appear consistent with a drug-induced effect.

Patients and prescribers should be alert for neuropsychiatric events. Patients should be instructed to notify their prescriber if these changes occur. Prescribers should carefully evaluate the risks and benefits of continuing treatment with montelukast sodium if such events occur.

·         Eosinophilic Conditions

Patients with asthma on therapy with montelukast sodium 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 events usually, but not always, have been associated with the reduction of oral corticosteroid therapy. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients.

USE IN PREGNANCY AND LACTATION:

Pregnancy: There are no adequate and well-controlled studies of Montelukast in pregnant women. Because animal reproductive studies are not always predictive of human response, so Montelukast should be used during pregnancy only if clearly needed.

Lactation: It is not known if Montelukast is excreted in human milk. Because many drugs are excreted in human milk, so caution should be exercised when Montelukast is given to a nursing mother.

DRUG INTERACTIONS:

Ø  Montelukast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma. In drug-interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following medicinal products: theophylline, prednisolone, prednisone, oral contraceptives (ethinyl estradiol/ norethindrone 35/1), terfenadine, digoxin and warfarin.

Ø  Cytochrome P-450 inducers: Although Phenobarbital induces hepatic metabolism, no dosage adjustment for Montelukast is recommended. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P-450 enzyme inducers, such as Phenobarbital or Rifampin, are co-administered with Montelukast.

ADVERSE EFFECTS:

Hypersensitivity reactions, including anaphylaxis, angioedema, pruritis, urticaria and, very rarely, hepatic eosinophilic infiltration, dream abnormalities, drowsiness, irritability, and restlessness.

DOSAGE AND ADMINISTRATION:

·         Adults (15 years of age or over): 10 mg daily to be taken in the evening. 

·         Children (6-14 years of age): 5 mg daily to be taken in the evening. 

·         Children (6 months-5 years of age): 4 mg daily to be taken in the evening.

Safety and effectiveness of Montelukast in pediatric patients younger than two years of age have not been established. The safety and efficacy of Montelukast was demonstrated in clinical trials where it was administered in the evening without regard to the time of food ingestion.

OVERDOSAGE:

There were no adverse experiences reported in the majority of overdosage reports. The most frequent adverse experiences observed were thirst, mydriasis, hyperkinesia, and abdominal pain. 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.

STORAGE:
Store in a cool and dry place

COMMERCIAL PACKAGING:

Monte 4/5/10 is available in a strip of 10 tabs.

Each box contains 10×10's.