Bilastine: Indications, Dosing, and Safety
Primary Indications
Bilastine is a second-generation oral antihistamine indicated for the symptomatic treatment of allergic rhinoconjunctivitis (seasonal and perennial) and chronic urticaria in adults and children. 1, 2
Recommended Dosing
Adults and Adolescents (≥12 years)
Children (6 to <12 years)
- 10 mg once daily administered orally 3, 2
- Pharmacokinetic studies demonstrate that the 10 mg pediatric dose achieves similar exposure to the 20 mg adult dose, with median pediatric/adult ratios for AUC₀₋₂₄ and Cmax of 0.93 and 0.91, respectively 3
Children (2 to 5 years)
- 10 mg once daily using orodispersible tablets 4
- Recent phase 3 data support this dosing in children as young as 2 years, showing linear pharmacokinetics with peak plasma concentrations at 1 hour (634.91 ng/mL) 4
- Body weight and age do not significantly affect pharmacokinetic parameters in this age group, so no dose adjustments are necessary 4
Special Populations
- No dosage adjustments required in patients with renal impairment, hepatic impairment, or elderly patients 2
Administration Considerations
Bilastine should NOT be administered at meal times to avoid interference with the absorption process 1. This is a critical administration requirement that distinguishes bilastine from many other antihistamines.
Mechanism and Pharmacology
- Bilastine is a highly selective H1-receptor antagonist with minimal central nervous system penetration 1, 2
- Elimination half-life: 14 hours, supporting once-daily dosing 1
- Rapid onset of action: 15 minutes for parenteral formulations, 30 minutes for oral formulations 5
- Elimination occurs through kidneys and feces with minimal metabolism 1
- No interaction with cytochrome P450 system, limiting potential for drug-drug interactions 1, 2
Safety Profile
Common Adverse Effects
- Headache is the most frequently reported adverse effect 1
- Treatment-emergent adverse events in children aged 2-5 years occurred in 21.6% of patients, with none being severe 4
- In children aged 6-11 years, the incidence of treatment-emergent adverse events was similar between bilastine and placebo 3
Key Safety Advantages
- No sedative effects: Bilastine shows no effect on drowsiness or alertness at therapeutic doses, even with parenteral formulations 1, 5, 2
- No cardiotoxic effects: No changes in heart rate or QT interval at therapeutic doses 1
- No anticholinergic effects: Unlike first-generation antihistamines 2
- Somnolence rates are comparable to placebo (0.4-3%) 1
Efficacy Data
- Maximum wheal reduction: 70-74% across all formulations 5
- Maximum flare reduction: 77-81% across all formulations 5
- Significantly superior to first-generation antihistamines (e.g., dexchlorpheniramine showed only 25.85% wheal reduction and 28.65% flare reduction) 5
- Symptoms of chronic urticaria improve from the second day of treatment onwards 1
Clinical Positioning
Bilastine represents a suitable first-line option for allergic rhinoconjunctivitis and urticaria across age groups from children as young as 2 years to elderly patients 2. Its lack of sedation, absence of drug interactions, and no need for dose adjustments in special populations make it particularly advantageous for patients requiring long-term antihistamine therapy or those taking multiple medications 2.
The requirement to take bilastine away from meals is the primary practical consideration that may affect patient adherence 1.