Acute Porphyria Drugs

Acute Porphyria Drug Database

R06AX22 - Ebastine
Propably not porphyrinogenic
PNP
Rationale
Ebastine is not found to be an inducer or mechanism-based inhibitor of any major CYP enzymes, and no pharmacokinetic porphyrinogenic effects are suspected.
Chemical description
Histamine H1-receptor antagonist.
Therapeutic characteristics
Ebastine is an antiallergic agent used in the treatment of allergic rhinitis, conjunctivitis and urticaria. It is administered orally.
Metabolism and pharmakokinetics
Ebastine is subject to rapid and extensive first pass metabolism in the liver by CYP enzymes (SPC). CYP 3A4 and CYP 2J2 are the main enzymes that metabolizes ebastine to desalkylebastine and hydroxyebastine. Hydroxyebastine is further metabolized to carebastine, which is pharmacologically active (Liu 2006). Clinical drug-drug interaction studies have been carried out, mostly studying the potential effects other drugs (mainly CYP-inhibitors) have on ebastine as a substrate of CYP 3A4 (Rico 2009). No drug-drug interaction with ebastine as a perpetrator is described or suspected in interaction databases Preissner 2010, NOMA, Lexi-Interact, The Danish Health and Medicines Authority).

References

  1. Scientific articles
  2. Liu KH, Kim MG, et al. Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: major roles for CYP2J2 and CYP3A. Drug Metab Dispos. 2006 Nov;34(11):1793-7. PMID 16896065. #4719
  3. Preissner S, Kroll K,et al. SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. PMID 19934256. #4721
  4. Rico S, Antonijoan RM, et al. Ebastine in the light of CONGA recommendations for the development of third- generation antihistamines J Asthma Allergy. 2009; 2: 73–92. PMID 21437146. #4720
  5. Government bodies
  6. Norwegian medicines agency (NOMA). Find medicine. #1412
  7. Drug interaction databases
  8. Lexi-Interact, via UpToDate. #1152
  9. The Danish Health and Medicines Authority. The drug interaction database. #1298
  10. Summary of Product Characteristics
  11. Norwegian medicines agency (NOMA). Summary of Product Characteristics (SPC). (Kestine). #2919
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