What is Bilastin?
Bilastine is a second-generation, non-sedating H1 antihistamine indicated for the treatment of allergic rhinoconjunctivitis (both seasonal and perennial) and chronic urticaria at a dose of 20 mg once daily in patients 12 years and older. 1, 2
Mechanism of Action and Pharmacology
- Bilastine works as a selective H1 receptor antagonist that blocks histamine-mediated allergic responses 1
- The drug is rapidly absorbed in the fasting state but absorption is significantly slowed when taken with food or fruit juice 2
- Bilastine must be taken at least one hour before or no sooner than two hours after meals to ensure proper absorption 2
- It is not distributed to the central nervous system, undergoes minimal metabolism, and is eliminated through kidneys and feces with a 14-hour half-life 1
- The drug has no effect on cytochrome P450, minimizing drug-drug interactions 1
Clinical Indications and Efficacy
Allergic Rhinoconjunctivitis
- Bilastine 20 mg once daily is effective for both nasal symptoms (including obstruction, rhinorrhea, itching, and sneezing) and ocular symptoms (tearing, redness, and itching) 1, 2
- Clinical trials demonstrate comparable efficacy to cetirizine 10 mg in reducing total symptom scores in seasonal allergic rhinitis 3
- In perennial allergic rhinitis, bilastine shows similar effectiveness to cetirizine when analyzed in European and Argentinean populations 4
- Long-term studies in Japanese patients show sustained efficacy for up to 52 weeks without loss of drug effectiveness 5
Chronic Urticaria
- Symptoms (itching and papule development) improve from the second day of treatment onwards, with efficacy similar to other antihistamines 1
Safety Profile and Tolerability
- Bilastine demonstrates a significantly better adverse event profile than cetirizine, with lower rates of somnolence (1.8% vs 7.5%, P<0.001) and fatigue (0.4% vs 4.8%, P=0.02) 3
- The therapeutic dose does not alter alertness or cause drowsiness, with effects similar to placebo 1
- Headache is the most frequently reported adverse effect 1
- No cardiotoxic effects have been observed at therapeutic doses 1
- Long-term treatment for up to 52 weeks shows excellent tolerability, with all adverse drug reactions being mild in severity 5
- No serious adverse events related to bilastine treatment have been reported in clinical trials 5
Dosing and Administration
- Standard dose: 20 mg once daily 1, 2
- Approved for adults and children over 12 years of age 1
- Must be taken on an empty stomach (at least 1 hour before or 2 hours after food) to avoid absorption interference 1, 2
Clinical Advantages
- Bilastine is effective for nasal obstruction, a symptom where antihistamines were previously thought to have limited benefit 2
- Quality of life improvements are consistently observed in both seasonal and perennial allergic rhinitis patients 5
- The non-sedating profile makes it suitable for patients who need to maintain alertness during daily activities 1, 3