Name: | zafirlukast |
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PubChem Compound ID: | 5717 |
Molecular formula: | C31H33N3O6S |
Molecular weight: | 575.676 g/mol |
Synonyms: |
Carbamic acid, (3-((2-methoxy-4-((((2-methylphenyl)sulfonyl)amino)carbonyl)phenyl)methyl)-1-methyl-1H-indol-5-yl)-, cyclopentyl ester; Accoleit; cyclopentyl 3-[2-methoxy-4-(2-methylphenylsulfonylcarbamoyl)benzyl]-1-methyl-1H-indol-5-ylcarbamate; Zafirlukast; Accolate; Accolate (TN); Olmoran; Cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate; Zafirst; Respix.
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Name: | zafirlukast |
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Name (isomeric): | DB00549 |
Drug Type: | small molecule |
Brand: | Accolate |
Category: | Anti-Asthmatic Agents, Leukotriene Antagonists |
CAS number: | 107753-78-6 |
Indication: | For the prophylaxis and chronic treatment of asthma. |
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Pharmacology: |
Zafirlukast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA) indicated for the prophylaxis and chronic treatment of asthma. Patients with asthma were found in one study to be 25-100 times more sensitive to the bronchoconstricting activity of inhaled LTD4 than nonasthmatic subjects. In vitro studies demonstr...
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Mechanism of Action: |
Zafirlukast is a selective and competitive receptor antagonist 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 alt...
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Absorption: | Rapidly absorbed following oral administration, reduced following a high-fat or high-protein meal. |
Protein binding: | 99% |
Biotransformation: | Hepatic |
Route of elimination: | The most common metabolic products are hydroxylated metabolites which are excreted in the feces. |
Half Life: | 10 hours |
Clearance: | apparent oral cl=20 L/h 11.4 L/h [7-11 yrs] 9.2 L/h [5-6 yrs] |
Toxicity: | Side effects include rash and upset stomach. |
Affected organisms: | Humans and other mammals |
Food interaction: |
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