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zafirlukast (Accolate)

Tradename: Accolate. Indications: 1) prophylaxis & chronic treatment of asthma in adults & children over 6 years of age 2) prophylaxis for exercise or aspirin-induced bronchial asthma Dosage: - 20 mg PO BID. Tabs: 20 mg. Storage: - store in orginal container - must be protected from light & moisture [6] Pharmacokinetics: -> metabolized in the liver by cyt P450 2C9 Monitor: - serum ALT & serum AST baseline & periodically [5] Adverse effects: 1) common: headache (13%) 2) uncommon (< 3%) - nausea, diarrhea, abdominal pain, increased LFTs, fever, respiratory infection in the elderly 3) rare - systemic eosinophilia - Churg-Strauss syndrome 4) other - agitation, aggression, anxiousness, abnormal dreams, hallucinations, depression, insomnia, irritability, restlessness, tremor [4] - behavior/mood changes, suicidality (suicidal thinking & behavior) & suicide [4] Drug interactions: 1) zafirlukast inhibits cyt P450 2C9 & 3A4 -> increases activity of warfarin 2) theophylline, terfenadine, erythromycin & aspirin decrease plasma levels of zafirlukast 3) any drug which inhibits cyt P450 2C9 (including zafirlukast itself) can increase zafirlukast levels 4) any drug which induces cyt P450 2C9 can diminish zafirlukast levels Mechanism of action: A leukotriene D4 receptor inhibitor.

Interactions

drug adverse effects of leukotriene receptor antagonists

Related

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)

General

heterocyclic compound, 2 rings leukotriene receptor antagonist miscellaneous pharmacologic agent

Properties

MISC-INFO: elimination route LIVER pregnancy-category B safety in lactation -

Database Correlations

PUBCHEM cid=5717

References

  1. Zeneca Pharmaceuticals
  2. Mayo Internal Medicine Board Review, 1998-99, Prakash UBS (ed) Lippincott-Raven, Philadelphia, 1998, pg 742
  3. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  4. 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. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com
  6. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com

Substructures

indole