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Montelair

 

Description
Square, beige film-coated tablet, shallow convex, bevel-edged and "HD" embossed on one face.


Composition
Each film-coated tablet contains:
Montelukast sodium equivalent to 10 mg montelukast.


Actions and Pharmacology
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.


Montelukast is a potent, orally active compound that significantly improves parameters of asthmatic inflammation. Based on biochemical and pharmacological bioassays, it binds with high affinity and selectivity to the CysLT1 receptor (in preference to other pharmacologically important airway receptors such as the prostanoid, cholinergic, or β-adrenergic receptor). Montelukast potently inhibits physiologic actions of LTC4, LTD4 and LTE4 at the CysLT1 receptor without any agonist activity.


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 litres. Studies in rats with radiolabelled Montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabelled material at 24 hours post-dose were minimal in all other tissues.

Metabolism
Montelukast is extensively metabolised. In studies with therapeutic doses, plasma concentrations of metabolites of Montelukast are undetectable at steady state in adults and children. 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.

Plasma Protein Binding
Plasma protein binding is more than 99% (Very high).


Elimination
The plasma clearance of Montelukast averages 45 ml/min in healthy adults. Following an oral dose of radiolabelled Montelukast, 86 of the radioactivity was recovered in 5-day faecal 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. It is not known whether Montelukast is removable by peritoneal dialysis or hemodialysis. The pharmacokinetics of Montelukast is nearly linear at doses of up to 50 mg.


Indications
For the prophylaxis and chronic treatment of asthma in adults and pediatric patients 12 months of age and older.
Montelukast is indicated in adults and pediatric patients 2 years of age and older for the relief of daytime and nighttime symptoms of seasonal allergic rhinitis.


Contraindications
Hypersensitivity to the active substance or to any of the excipients.


Precaution
The efficacy of oral Montelukast for the treatment of acute asthma attacks has not been established. Therefore, oral Montelukast should not be used to treat asthma attacks.


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 it they need more inhalations of short-acting β-agonists than usual. Montelukast should not be substituted 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 usually, but not always, have been associated with the reduction or withdrawal of oral corticosteroid therapy. The possibility that leukotriene receptor antagonists may be associated with emergence of Churg-Strauss syndrome can neither be excluded nor 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 nonsteroidal anti-inflammatory drugs.


Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

 

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