Products
Bilastin is commercially available in the form of tablets (Bilaxten). It was approved in many countries in 2011. In 2019, an oral solution and melting tablets for children were also registered.
Structure and properties
Bilastine (C28H37N3O3, Mr = 463.6 g/mol) is a benzimidazole and piperidine derivative. It was developed at FAES Farma in Spain. Bilastine is not a direct derivative of other antihistamines but shares structural elements with some representatives (e.g., mizolastine, fexofenadine).
Effects
Bilastine (ATC R06AX29) has antihistamine, antiallergic, and antiinflammatory properties and relieves symptoms of hay fever and urticaria. The effects are due to selective and potent antagonism at the histamine H1 receptor. Bilastine has a rapid onset of action (30-60 minutes) and a long duration of action (24 hours). The half-life is 14.5 hours. Bilastine is low sedative, non-anticholinergic and does not prolong the QT interval. This is in contrast to other antihistamines.
Indications
For symptomatic treatment of hay fever, allergic conjunctivitis, and urticaria.
Dosage
According to the SmPC. The medicine is taken once daily on an empty stomach, that is, at least one hour before or two hours after ingestion of food or fruit juice. Food and fruit juices may reduce bioavailability by up to 30%. For adults and adolescents 12 years of age and older.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Bilastine is a substrate of P-glycoprotein and a substrate and inhibitor of OATP. In contrast, it is poorly metabolized and, unlike other antihistamines, does not interact with CYP450.
- Food reduces the oral bioavailability of bilastine.
- Grapefruit juice or other fruit juices reduce the bioavailability of bilastine.
- Ketoconazole, erythromycin, diltiazem, ciclosporin, and ritonavir increase plasma concentrations of bilastine.
- A study with ethanol showed no enhancement of adverse effects.
Adverse effects
The most common potential adverse effects in clinical trials included headache, drowsiness, dizziness, and fatigue. However, these adverse effects were also observed with placebo.
