Bilastine is indicated for the symptomatic treatment of:
It is also used to relieve the symptoms of hay fever, including sneezing, itching, runny or blocked nose, and red, watery eyes.
Bilastine is a potent, effective, non-sedating, and long-acting antihistamine with a selective and high affinity for the H1 receptor—approximately three times higher than cetirizine and five times higher than fexofenadine.
Even at high concentrations, bilastine shows no significant affinity for around 30 other receptors, including muscarinic, serotonergic, dopaminergic, and noradrenergic receptors, nor for other histamine receptor subtypes (H2, H3, and H4).
It has an excellent safety profile and favorable pharmacokinetic properties. Bilastine does not require metabolic activation to exert its effect. It is primarily excreted unchanged, approximately 66.35% via feces (non-systemic route) and 28.31% via urine (systemic route).
Adults & adolescents (12 years of age and over): 20 mg tablet once daily for symptomatic relief of allergic rhinitis, urticaria and allergic rhinoconjunctivitis. The maximum recommended daily dose is 20 mg Bilastine (1 tablet) and should not be exceeded. If a dose is missed, the next scheduled dose should be taken. An extra dose should not be taken. 20 mg Bilastine tablet (1 tablet) once daily should be swallowed with water on an empty stomach to achieve optimal exposure to Bilastine.
Children between 6 to 11 years: 10 mg mouth dissolving tablet for the symptomatic relief of allergic rhinitis, allergic rhinoconjunctivitis and urticaria. The Mouth dissolving tablet is for oral use only. It should be placed in the mouth. It will disperse rapidly in saliva and can be easily swallowed. Alternatively, the mouth dissolving tablet can be dispersed
in a tea spoon of water before being swallowed by the children. The maximum recommended daily dose for children in between 6 to 11 years is 10 mg Bilastine mouth dissolving tablet (1 tablet) and should not be exceeded. If a dose is missed, the next scheduled dose should be taken. An extra dose should not be taken.
Children between 2 to 11 years: 4 ml once daily.
Concomitant administration of bilastine with ketoconazole, erythromycin, cyclosporine, or diltiazem increases bilastine plasma concentrations; however, these changes do not appear to affect the safety profile of any of the medications. The intake of 20 mg bilastine with alcohol results in psychomotor performance comparable to that observed with alcohol and placebo. Additionally, co-administration of bilastine 20 mg and lorazepam 3 mg for eight days did not enhance the central nervous system depressant effects of lorazepam.
Bilastine is contraindicated in patients with known hypersensitivity to the active substance or to any of the tablet’s excipients.
The most commonly reported adverse reactions in clinical trials were headache, dizziness, somnolence, and fatigue. These events occurred at a frequency comparable to that observed in patients receiving placebo.
There are no or limited data available regarding the use of bilastine in pregnant women. Animal studies do not indicate any direct or indirect harmful effects on reproductive toxicity, childbirth, or postnatal development. However, as a precautionary measure, it is advisable to avoid the use of bilastine during pregnancy.
The excretion of bilastine into human breast milk has not been studied. Therefore, a decision should be made by weighing the benefits of breastfeeding for the child against the benefits of bilastine therapy for the mother.
Treatment with bilastine 20 mg does not impair driving performance. However, patients should be advised that, in rare cases, drowsiness may occur, which could affect their ability to drive or operate machinery.
In clinical trials, elderly patients (≥65 years) showed no differences in efficacy or safety compared with younger patients. In individuals with severe renal impairment, the maximum plasma concentration following a 20 mg dose remains below the safety threshold for common adverse effects, including cardiac and central nervous system effects. Therefore, no dose adjustment is required in patients with renal impairment.
Bilastine is not metabolized in humans. As renal elimination is the primary route of excretion, biliary excretion plays only a minor role. Consequently, changes in liver function are not expected to have a clinically significant impact on bilastine elimination.
The efficacy and safety of bilastine in children under 2 years of age have not been established. Additionally, clinical experience in children aged 2 to 5 years is limited; therefore, bilastine should not be used in these age groups.
In clinical trials, administration of bilastine at doses 10 to 11 times higher than the therapeutic dose (220 mg as a single dose or 200 mg daily for 7 days) resulted in a twofold increase in treatment-emergent adverse events compared with placebo.
The most frequently reported adverse reactions were dizziness, headache, and nausea. No serious adverse events or significant prolongation of the QTc interval were observed.
Non-sedating antihistamines
Store below 30°C, protected from light and moisture. Keep out of reach of children.
What is Bilastine for?
What does Bilastine do?
What are the side effects of Bilastine?
What happens if you take too much Bilastine?
Can Bilastine be taken during pregnancy?
