Overview
Bilastine is a second-generation antihistamine used for symptomatic relief of allergic conditions. It is a selective histamine H1-receptor antagonist with minimal sedative effects and no significant cardiac toxicity at therapeutic doses.
Mechanism of Action
Bilastine selectively antagonizes peripheral histamine H1 receptors, inhibiting histamine-mediated allergic responses. It has minimal penetration of the blood-brain barrier, resulting in low central nervous system effects.
Indications
- Symptomatic treatment of allergic rhinoconjunctivitis (seasonal and perennial)
- Symptomatic treatment of urticaria
Dosage
Adults and adolescents (12 years and older): 20 mg once daily. Should be taken on an empty stomach (at least 1 hour before or 2 hours after food).
Contraindications
- Hypersensitivity to bilastine or any excipients
- Severe renal impairment (creatinine clearance <30 mL/min)
- Concomitant use with grapefruit juice
Side Effects
- Headache
- Drowsiness
- Fatigue
- Dizziness
- Nausea
- Dry mouth
- Increased appetite
- Weight gain
Interactions
- Grapefruit juice: Increases bilastine plasma concentration
- Ketoconazole and erythromycin: May increase bilastine levels
- P-glycoprotein inhibitors: May increase bilastine absorption