Bilastin

Bilastine is a 2nd generation antihistamine used for symptomatic treatment of allergic rhinoconjuctivitis (allergic disease of the nasal mucosa and eyes) and urticaria (hives). Unlike other antihistamines, it has a hardly sedating, fast and long-lasting effect.

Pharmacodynamics

During an allergic reaction, histamine and other substances are released from the cells of the body's defense system. Bilastine binds to the H1 receptor instead of histamine and thus inhibits their activation. This reduces allergic symptoms. Since it has no effect on the central nervous system, it does not have a sedative effect.
Die Effekte des Wirkstoffes halten bis zu 24 Stunden an.

Pharmacokinetics

Bilastine is 61% absorbed and is 84-90% protein-bound in plasma. It is a substrate of the P-glycoprotein and an inhibitor of the organo-anion transporter and, unlike other antihistamines, does not interact with the CYP450 enzyme. In keeping with its long duration of action, it has a half-life of 14.5 hours. The active ingredient is excreted largely unchanged in the feces and urine.

Wechselwirkungen

Food, especially grapefruit juice, reduces oral bioavailability, so the drug should be taken fasting. A high-fat meal also significantly inhibits absorption.
Die gleichzeitige Anwendung des Antihistaminikums mit Ketokonazol, Ritonavir, Erythromycin, Diltiazem und Ciclosporin sollte vermieden werden.

Side effects

Possible adverse reactions include headache, dizziness, and drowsiness or fatigue.

Toxicological Data

NOAEL (rat): 1200 mg/kg/day.
NOAEL (Hund): 125 mg/kg/Tag