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30 X 20 mg
Adults and adolescents (12 years of age and over): 20 mg bilastine (1 tablet) once daily for the relief of symptoms of allergic rhinoconjunctivitis (SAR and PAR) and urticaria.
The tablet should be taken one hour before or two hours after intake of food or fruit juice.
Elderly: No dosage adjustments are required in elderly patients.
Renal impairment: No dosage adjustment is required in patients with renal impairment.
Hepatic impairment: There is no clinical experience in patients with hepatic impairment. Since bilastine is not metabolized and renal clearance is its major elimination route, hepatic impairment is not expected to increase systemic exposure above the safety margin. Therefore, no dosage adjustment is
required in patients with hepatic impairment.
Paediatric population: There is no relevant use of bilastine in children aged 0 to 2 years for the indications of allergic rhino-conjunctivitis and urticaria. The safety and efficacy in children below 12 years have not yet been established.
Duration of treatment: For allergic rhinitis the treatment should be limited to the period of exposure to allergens. For seasonal allergic rhinitis treatment could be discontinued after the symptoms have resolved and reinitiated upon their reappearance. In perennial allergic rhinitis continued treatment may be
proposed to the patients during the allergen exposure periods. For urticaria the duration of treatment depends on the type, duration and course of the complaints.
Method of administration: Oral use. The tablet is to be swallowed with water. It is recommended to take the daily dose in one single intake.
Bilaxten is indicated for the symptomatic treatment of allergic rhino-conjunctivitis (seasonal and perennial) and urticaria in adults and adolescents (12 years of age and over).
Hypersensitivity to the active substance or to any of the excipients.
Paediatric population: Efficacy and safety of bilastine in children under 12 years of age have not been established.
In patients with moderate or severe renal impairment coadministration of bilastine with P-glycoprotein inhibitors, such as e.g, ketoconazole, erythromycin, cyclosporine, ritonavir or diltiazem, may increase plasmatic levels of bilastine and therefore increase the risk of adverse reactions of bilastine. Therefore, coadministration of bilastine and P-glycoprotein inhibitors
should be avoided in patients with moderate or severe renal impairment.
Effects on ability to drive and use machines: A study performed to assess the effects of bilastine on the ability to drive demonstrated that treatment with 20 mg did not affect the driving performance. However, patients should be informed that very rarely some people experience drowsiness, which may affect their ability to drive or use machines.
The incidence of adverse events in patients suffering from allergic rhinoconjunctivitis or chronic idiopathic urticaria treated with 20 mg bilastine in clinical trials was comparable with the incidence in patients receiving placebo (12.7% versus 12.8%).
The phase II and III clinical trials performed during the clinical development included 2525 patients treated with different doses of bilastine, of which 1697 received bilastine 20 mg. In these trials 1362 patients received placebo. The ADRs most commonly reported by patients receiving 20 mg bilastine for the indication of allergic rhinoconjunctivitis or chronic idiopathic urticaria
were headache, somnolence, dizziness, and fatigue. These adverse events occurred with a comparable frequency in patients receiving placebo.
See prescribing information for full details.
Interaction with food: Food significantly reduces the oral bioavailability of bilastine by 30%.
Interaction with grapefruit juice: concomitant intake of bilastine 20 mg and grapefruit juice decreased bilastine bioavailability by 30%. This effect may also apply to other fruit juices. The degree of bioavailability decrease may vary between producers and fruits. The mechanism for this interaction is an inhibition of OATP1A2, an uptake transporter for which bilastine is a substrate. Medicinal products that are substrates or inhibitors of OATP1A2, such as ritonavir or rifampicin, may likewise have the potential to decrease plasma concentrations of bilastine.
Interaction with ketoconazole or erythromycin: Concomitant intake of bilastine and ketoconazole or erythromycin increased bilastine AUC 2-fold and Cmax 2-3 fold. These changes can be explained by interaction with intestinal efflux transporters, since bilastine is substrate for P-gp and not metabolised. These changes do not appear to affect the safety profile of bilastine and ketoconazole or erythromycin, respectively. Other medicinal products that are substrates or inhibitors of P-gp, such as cyclosporine, may likewise have the potential to increase plasma concentrations of bilastine.
Interaction with diltiazem: Concomitant intake of bilastine 20 mg and diltiazem 60 mg increased Cmax of bilastine by 50%. This effect can be explained by interaction with intestinal efflux transporters, and does not appear to affect the safety profile of bilastine.
Interaction with alcohol: The psychomotor performance after concomitant intake of alcohol and 20 mg bilastine was similar to that observed after intake of alcohol and placebo.
Interaction with lorazepam: Concomitant intake of bilastine 20 mg and lorazepam 3 mg for 8 days did not potentiate the depressant CNS effects of lorazepam.
Paediatric population: Interaction studies have only been performed in adults. Extent of interaction with other medicinal products and other forms of interaction is expected to be similar in paediatric population from 12 to 17 years of age.
Pregnancy and Lactation
Pregnancy: There are no or limited amount of data from the use of bilastine in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity, parturition or postnatal development. As a precautionary measure, it is preferable to avoid the use of Bilaxten during pregnancy.
Breast-feeding: The excretion of bilastine in milk has not been studied in humans. Available pharmacokinetic data in animals have shown excretion of bilastine in milk. A decision on whether to discontinue/abstain from Bilaxten therapy must be made taking into account the benefit of breast-feeding for the child and the benefit of bilastine therapy for the mother.
Information regarding acute overdose of bilastine is retrieved from the experience of clinical trials conducted during the development and the post-marketing surveillance. In clinical trials, after administration of bilastine at doses 10 to 11 times the therapeutic dose (220 mg as single dose or 200 mg/day for 7 days) to healthy volunteers, frequency of treatment emergent adverse events was two times higher than with placebo. The adverse reactions most frequently reported were dizziness, headache and nausea. No serious adverse events and no significant prolongation in the QTc interval were reported. The information collected in the post-marketing surveillance is
consistent with that reported in clinical trials.
Critical evaluation of bilastine’s multiple dose (100 mg x4 days) effect on ventricular repolarization by a “thorough QT/QTc cross-over study” involving 30 healthy volunteers did not show significant QTc prolongation.
In the event of overdose symptomatic and supportive treatment is recommended.
There is no known specific antidote to bilastine.
Storage: Store below 30°C.