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Pharmacology: Pharmacodynamics: Bilastine is a long-acting, non-sedating antihistamine with selective peripheral H1 receptor antagonist affinity. Bilastine has no affinity for muscarinic receptors.
Bilastine inhibited histamine-induced wheal and flare skin reaction for 24 hours following single dose.
Pharmacokinetics: Bilastine is rapidly absorbed after oral administration with a time to maximum plasma concentration of around 1.3 hours. Oral bioavailability is 61%. Bilastine is a substrate of Pgp and OATP. Bilastine does not appear to be a substrate of the transporter BCRP or renal transporters OCT2, OAT1 and OAT3. At therapeutic dose Bilastine is 84-90% bound to plasma proteins. Bilastine did not induce or inhibit activity of CYP450 isoenzymes in in vitro studies. The mean eliminate half-life was 14.5 hours.
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