Histamont -B

1. Generic Name
Bilastine Montelukast
2. Qualitative and Quantitative composition
Bilastine……………………….. 20 mg
Montelukast……………….. 10 mg
3. Dosage form and strength
Film coated tablets containing 20mg of Bilastine and 10mg of Montelukast.
4. Mechanism of action
Bilastine
Bilastine is a selective histamine H1 receptor antagonist (Ki = 64nM). During allergic response mast cells undergo degranulation which releases histamine and other subastances.
By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells.
Montelukast
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-(CysLT1) receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other proinflammatory 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 a number of airway actions, including 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 MONTELUKAST Product Monograph Page 14 of 33 with symptoms of allergic rhinitis. Intranasal challenge with CysLTs has been shown to increase nasal airway resistance and symptoms of nasal obstruction. Montelukast has not been assessed in intranasal challenge studies. The clinical relevance of intranasal challenge studies is unknown. Montelukast is an orally active compound that 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.
5 .Packaging Information
Histamont -B TABLETS is available in pack of 10 tablets.
6. Storage and handling instructions
Store in cool and dry place. Keep medicine away from children.