Ebastine

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.

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.

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