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.
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.
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.