Montelukast (Singulair, Merck) Classification: Respiratory Agents; Miscellaneous Respiratory Agents Description: Singular ® may be confused with Sinequan ® Pharmacology: The cysteinyl leukotriene 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). Montelukast binds with high affinity and selectivity to the CysLT 1 receptor inhibiting the physiologic actions of LTD 4 without any agonist activity. ). 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. Pharmacokinetics: Absorption: Rapidly absorbed with a mean oral bioavailability of 64%.
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- Spring '14
- pH, Montelukast