Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.
Active Ingredient / Synonyms
Bilastine | Bilastine |
Bilastine is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.
For symptomatic relief of nasal and non-nasal symptoms of seasonal rhinitis in patients 12 years of age and older and for symptomatic relief in chronic spontaneous urticaria in patients 18 years of age and older [FDA Label].
Mechanism of Action
Bilastine is a selective histamine H1 receptor antagonist (Ki = 64nM) [FDA Label]. During allergic response mast cells undergo degranulation which releases histamine and other subastances. By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells.
Bilastine is an antiallergenic and acts to reduce allergic symptoms such as nasal congestion and urticaria [FDA Label].
Bilastine has a Tmax of 1.13 h [FDA Label]. The absolute bioavailability is 61%. No accumulation observed with daily dosing of 20-100 mg after 14 days. Cmax decreased by 25 % and 33% when taken with a low fat and high fat meal compared to fasted state. Administration with grapefruit juice decreased Cmax by 30%.
Bilastine does not interact with the cytochrome P450 system and does not undergo significant metabolism in humans [FDA Label].
Bilastine is mainly excreted in the feces (66.5%) with some excreted in the urine (28.3%) [FDA Label]. Nearly all is excreted as the parent compound.
The mean half life of elimination is 14.5h [FDA Label].
Bilastine has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h [FDA Label].
The most common adverse effects experienced during clinical trials were abdominal pain, dizziness, headache, and somnolence [FDA Label]. Bilastine is associated with Q/T prolongation. The no observed adverse effect level of bilastine is 1200 mg/kg/day in rats and 125 mg/kg/day in dogs [A19750].
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