Zafirlukast
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Zafirlukast
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| Systematic (IUPAC) name | |
| cyclopentyl N-[3-{[2-methoxy-4-[(2-methylphenyl) sulfonylcarbamoyl]phenyl]methyl}-1-methyl-indol-5-yl] carbamate |
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| Identifiers | |
| CAS number | |
| ATC code | R03 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C31H33N3O6S |
| Mol. mass | 575.676 g/mol |
| Pharmacokinetic data | |
| Bioavailability | Unknown |
| Protein binding | 99% |
| Metabolism | Hepatic (CYP2C9-mediated) |
| Half life | 10 hours |
| Excretion | Biliary |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral |
Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma. It is available as a tablet.
Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.
Zafirlukast is marketed by AstraZeneca with the brand names Accolate, Accoleit, and Vanticon. It was the first LTRA to be marketed in the USA and is now approved in over 60 countries, including the UK, Japan, Italy, Spain, Canada, Brazil, China and Turkey.
[edit] External links
- Accolate, Accoleit, Vanticon (manufacturer's website)
- Zafirlukast (patient information)
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| Anticholinergics | Ipratropium, Tiotropium |
| Short acting β2-agonists | Salbutamol, Terbutaline |
| Long acting β2-agonists (LABA) | Bambuterol, Clenbuterol, Fenoterol, Formoterol, Salmeterol |
| Corticosteroids | Beclometasone, Budesonide, Ciclesonide, Fluticasone |
| Leukotriene antagonists | Montelukast, Pranlukast, Zafirlukast |
| Xanthines | Aminophylline, Theobromine, Theophylline |
| Mast cell stabilizers | Cromoglicate, Nedocromil |
| Combination products | Budesonide/formoterol, Fluticasone/salmeterol, Ipratropium/salbutamol |
