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Pulmonary - Leukotriene inhibitors
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montelukast Singulair ®
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Use Prophylaxis and chronic treatment of asthma in adults and children >/= 1 year of age; relief of symptoms of seasonal allergic rhinitis in adults and children >/= 2 years of age Mechanism of Action Selective leukotriene receptor antagonist that inhibits the cysteinyl leukotriene receptor. Cysteinyl leukotrienes and leukotriene receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. ---------------------------- Dosing: Oral: Children: 12-23 months: Asthma: 4 mg (oral granules) once daily, taken in the evening 2-5 years: Asthma or seasonal allergic rhinitis: 4 mg (chewable tablet or oral granules) once daily, taken in the evening 6-14 years: Asthma or seasonal allergic rhinitis: Chew one 5 mg chewable tablet/day, taken in the evening Children >/= 15 years and Adults: Asthma or seasonal allergic rhinitis: 10 mg/day, taken in the evening ---------------------------- Supplied: Granules: 4 mg/packet Tablet: 10 mg TTablet, chewable: 4 mg [contains phenylalanine 0.674 mg; cherry flavor]; 5 mg [contains phenylalanine 0.842 mg; cherry flavor] |
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zafirlukast (Accolate ®)
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Use Prophylaxis and chronic treatment of asthma in adults and children >/= 5 years of age Mechanism of Action Zafirlukast is a selectively and competitive leukotriene-receptor antagonist (LTRA) of leukotriene D4 and E4 (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle constriction and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. -------------------------- Dosing: Children 5-11 years: 10 mg twice daily Children >/= 12 years and Adults: 20 mg twice daily Elderly: The mean dose (mg/kg) normalized AUC and Cmax increase and plasma clearance decreases with increasing age. In patients >65 years of age, there is a two- to threefold greater Cmax and AUC compared to younger adults. -------------------------- Supplied: Tablet: 10 mg, 20 mg |
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zileuton (Zyflo ®)
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Use Prophylaxis and chronic treatment of asthma in children >/= 12 years of age and adults Mechanism of Action Specific inhibitor of 5-lipoxygenase and thus inhibits leukotriene (LTB4, LTC4, LTD4 and LTE4) formation. Leukotrienes are substances that induce numerous biological effects including augmentation of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability and smooth muscle contraction. -------------------------- Dosing: Children >/= 12 years of age and Adults: 600 mg 4 times/day with meals and at bedtime Elderly: Zileuton pharmacokinetics were similar in healthy elderly subjects (>65 years) compared with healthy younger adults (18-40 years) Dosing adjustment in hepatic impairment: Contraindicated in patients with active liver disease -------------------------- Supplied: Tablet: 600 mg |
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