Monograph
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 pharmacokinetics
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
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Characterization of ebastine, hydroxyebastine, and carebastine metabolism by human liver microsomes and expressed cytochrome P450 enzymes: major roles for CYP2J2 and CYP3A.
Liu KH, Kim MG, et al. Drug Metab Dispos. 2006 Nov;34(11):1793-7. |
16896065 |
| 2. | SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions.
Preissner S, Kroll K,et al. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. |
19934256 |
| 3. | Ebastine in the light of CONGA recommendations for the development of third-
Rico S, Antonijoan RM, et al. generation antihistamines J Asthma Allergy. 2009; 2: 73–92. |
21437146 |
| * | Government bodies | |
| 4. | Norwegian medicines agency (NOMA). Find medicine.
|
|
| * | Drug interaction databases | |
| 5. | Lexi-Interact, via UpToDate.
|
|
| 6. | The Danish Health and Medicines Authority. The drug interaction database.
|
|
| * | Summary of Product Characteristics | |
| 7. | Norwegian medicines agency (NOMA). Summary of Product Characteristics (SPC). (Kestine).
|
|
Similar drugs
Tradenames and packages
From some sources, we get a list of packages (United Kingdom, Ireland, Estonia).
Other sources contain more or less "clean" versions of the trade name (Denmark, Finland, Iceland, Lithuania, Norway).
What you see here is the raw data we get from each country, so there will appear to be duplicates. The bold names
are the searchable terms. The gray names that follow are all mapped to the bolded term.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors.
We strive to improve it continuously.
Netherlands
Belgium
Denmark
Norway
Poland
Luxembourg
Iceland
Finland
Latvia© NAPOS 2024