zafirlukast (Accolate)
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Introduction
Tradename: Accolate.
Indications
- prophylaxis & chronic treatment of asthma in adults & children over 6 years of age
- prophylaxis for exercise or aspirin-induced bronchial asthma
Dosage
Tabs: 20 mg.
Storage
- store in orginal container
- must be protected from light & moisture[6]
Pharmacokinetics
- metabolized in the liver by cyt P450 2C9
elimination via liver
Monitor
Adverse effects
- common: headache (13%)
- uncommon (< 3%)
- nausea, diarrhea, abdominal pain, increased LFTs, fever, respiratory infection in the elderly
- rare
- other
- agitation, aggression, anxiousness, abnormal dreams, hallucinations, depression, insomnia, irritability, restlessness, tremor[4]
- behavior/mood changes, suicidality (suicidal thinking & behavior) & suicide[4]
Drug interactions
- zafirlukast inhibits cyt P450 2C9 & 3A4
- increases activity of warfarin
- theophylline, terfenadine, erythromycin & aspirin decrease plasma levels of zafirlukast
- any drug which inhibits cyt P450 2C9 (including zafirlukast itself) can increase zafirlukast levels
- any drug which induces cyt P450 2C9 can diminish zafirlukast levels
Mechanism of action
A leukotriene D4 receptor inhibitor
More general terms
Additional terms
- allergic angiitis & granulomatosis of Churg-Strauss; eosinophilic granulomatosis with polyangiitis (EGPA)
- cysteinyl leukotriene receptor (LTC4 receptor, LTD4 receptor)
- cytochrome P450 2C9; cytochrome P450 BP-1; cytochrome P450 MP-4; S-mephenytoin-4-hydroxylase; limonene 6-monooxygenase; limonene 7-monooxygenase (CYP2C9, CYP2C10)
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
References
- ↑ Zeneca Pharmaceuticals
- ↑ Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 742
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 4.0 4.1 4.2 FDA Safety Alert 6/12/2009 Updated Information on Leukotriene Inhibitors: Montelukast (marketed as Singulair), Zafirlukast (marketed as Accolate), and Zileuton (marketed as Zyflo and Zyflo CR) http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/DrugSafetyInformationforHeathcareProfessionals/ucm165489.htm
- ↑ 5.0 5.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 6.0 6.1 Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300622&pb=PRL (subscription needed) http://www.prescribersletter.com