zileuton (Zyflo, Zyflo CR)
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Introduction
Tradename: Zyflo, Zyflo CR
Indications
- prophylaxis for exercise or aspirin-induced bronchial asthma
Contraindications
- acute liver disease, serum ALT > 3X upper limit of normal
Dosage
Pharmacokinetics
- metabolized in the liver by cyt P450 1A2 & cyt P450 3A4
elimination via liver
Monitor
- serum ALT baseline, monthly for the 1st 3 months, every 2-3 months for the remainder of the 1st year, then periodically[5]
Adverse effects
- dyspepsia
- nausea
- myalgia
- abdominal discomfort
- increased serum alanine aminotransferase (serum ALT)
- agitation, aggression, anxiousness, dream abnormalities & hallucinations, depression, insomnia, irritability, restlessness, suicidal thinking & behavior (including suicide), & tremor[4]
Drug interactions
- may potentiate effects of drugs metabolized by cyt P450 1A2
- any drug which inhibits cyt P450 1A2 or cyt P450 3A4 can increase zileuton levels
- any drug which induces cyt P450 1A2 or cyt P450 3A4 can diminish zileuton levels
Mechanism of action
- inhibits leukotriene synthesis, lipoxygenase inhibitor?
- 5-lipoxygenase inhibitor
- inhibits cyt P450 1A2 thus its own metabolism
More general terms
Additional terms
- cytochrome p450 1A2 (cytochrome P3-450, phenacetin deethylase, cytochrome p450-4, CYP1A2)
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
References
- ↑ 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
- ↑ Prescriber's Letter 14(9): 2007 Extended-release zileuton (Zyflo CR) and its role in asthma Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230911&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 4.0 4.1 Food and Drug Administraton (FDA MedWatch) Updated Information on Leukotriene Inhibitors: Montelukast (marketed as Singulair), Zafirlukast (marketed as Accolate), and Zileuton (marketed as Zyflo and Zyflo CR) 6/12/2009 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