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 | |
| 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. |
B1 (Au), B (U.S.) |
| Legal status | |
| Routes | Oral |
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Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), which is usually taken just once daily.
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.
External links
- Accolate, Accoleit, Vanticon (manufacturer's website)
- Zafirlukast (patient information)
Drugs for obstructive airway diseases: asthma/COPD (R03) | |
|---|---|
| Adrenergics, inhalants | Short acting β2-agonists: Salbutamol/Levosalbutamol • Fenoterol • Terbutaline Long acting β2-agonists (LABA): Bambuterol • Clenbuterol • Formoterol • Salmeterol other: Epinephrine • Isoproterenol • Orciprenaline |
| Glucocorticoids | Beclometasone • Budesonide • Ciclesonide • Fluticasone • Mometasone |
| Anticholinergics | Ipratropium • Tiotropium |
| Mast cell stabilizers | Cromoglicate • Nedocromil |
| Xanthines | Aminophylline • Theobromine • Theophylline |
| Leukotriene antagonists | Montelukast • Pranlukast • Zafirlukast |
| Combination products | Budesonide/formoterol • Fluticasone/salmeterol • Ipratropium/salbutamol |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
