Ebastine

Ebastine
ATC Code R06AX22
Formula C32H39NO2
Molar Mass (g·mol−1) 469,6576
Physical State solid
CAS Number 90729-43-4
PUB Number 3191
Drugbank ID DB11742
Solubility insoluble in water

Basics

Ebastine is an antihistamine used to treat allergic symptoms such as rhinitis, conjunctivitis, and hives.The drug is sold commercially in tablet form and is usually well tolerated, as cardiotoxic side effects are mostly absent.

Pharmacology

Pharmacodynamics

Ebastine is an H1 receptor antagonist, which means that it displaces the neurotransmitter histamine from its receptor so that it cannot be activated. This triggers the anti-allergic effects, which prevent sneezing, swelling of the eyelids, itching, and other allergic reactions.
Da es sich bei Ebastin um ein H1-Antihistaminikum der 2. Generation handelt, treten keine sedierenden Wirkungen ein, da die Blut-Hirn-Schranke kaum passiert wird.

Pharmacokinetics

After oral ingestion, ebastine is rapidly absorbed and converted to the active metabolite carebastine by marked first-pass metabolism with the aid of the cytochrome P450 enzyme family. The drug then circulates bound to 95% plasma proteins and reaches maximum plasma concentration after approximately 2.6 to 4 hours. The half-life of carebastine is approximately 15 to 19 hours. Of the metabolite, 66% is excreted by the kidney.

Contraindications

Ebastine should not be used if hypersensitivity or hepatic insufficiency is present. The drug is also contraindicated during pregnancy or breastfeeding and in children under 12 years of age.

Drug interactions

Interactions may occur with concomitant use of ebastine with ketoconazole, itraconazole, erythromycin, or rifampicin.

Toxicity

Side effects

Adverse side effects include headache, morbid drowsiness, dry mouth, and gastrointestinal disturbances.

Toxicological Data

LD50 (dog, oral): >160 mg/kg
LD50 (Maus, oral): 4000 mg/kg
LD50 (Ratte, oral): 4000 mg/kg

Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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