Bliztin

Bilastine.

Each tablet contains Bilastine 20 mg.

Pharmacology: Pharmacodynamics: Bilastine is a long-acting, non-sedating antihistamine with selective peripheral H₁ receptor antagonist affinity. Bilastine has no affinity for muscarinic receptors.
Bilastine inhibited histamine-induced wheal and flare skin reaction for 24 hours following single dose.
Pharmacokinetics: Bilastine is rapidly absorbed after oral administration with a time to maximum plasma concentration of around 1.3 hours. Oral bioavailability is 61%. Bilastine is a substrate of Pgp and OATP. Bilastine does not appear to be a substrate of the transporter BCRP or renal transporters OCT2, OAT1 and OAT3. At therapeutic dose Bilastine is 84-90% bound to plasma proteins. Bilastine did not induce or inhibit activity of CYP450 isoenzymes in in vitro studies. The mean eliminate half-life was 14.5 hours.

Symptomatic treatment of allergic rhino-conjunctivitis (seasonal and perennial) and urticaria.
Bilastine is indicated in adults and adolescents (12 years of age and over).

Adults and adolescents (12 years of age and over): 20 mg Bilastine (1 tablet) once daily for the relief of symptoms of allergic rhino-conjunctivitis (seasonal allergic rhinitis (SAR) and perennial allergic rhinitis (PAR)) and urticaria.
The tablet should be taken one hour before or two hours after intake of food or fruit juice.
Older people: No dosage adjustments are required in older patients. There is little experience in patients above the age of 65.
Patients with renal impairment: No dosage adjustment is required in patients with renal impairment.
Patients with 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 in the indications allergic rhino-conjunctivitis and urticaria (seasonal and perennial). 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.

Overdose and treatment: In the case of an acute Bilastine overdose, 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.
There is no known specific antidote to Bilastine. Symptomatic and supportive treatment is recommended.

Hypersensitivity to the active substance or to any of the excipients.

Based on the Ministry of Public Health's Announcement: 1. This medicine may cause drowsiness therefore should not drive or operate machinery or perform activities which may be at risk of falling from the height.
2. While using this medicine, should not drink alcohol or anything that is mixed with alcohol.
3. Use with caution in children below 1 year of age, the first trimester pregnancy and breast-feeding.

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: Treatment with Bilastine 20 mg may 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.
Use in Children: Efficacy and safety of Bilastine in children under 12 years of age have not been established.

Pregnancy: There are no or limited amount to data from the use of Bilastine in pregnant women. Bilastine should be avoided during pregnancy.
Breast-feeding: It is unknown whether Bilastine is excreted in human breast milk. The excretion of Bilastine in milk has not been studied in animal. A decision on whether to discontinue/abstain from Bilastine therapy must be made considering the benefit of breast-feeding for the child and the benefit of Bilastine therapy for the mother.

Infections: Uncommon: Oral herpes.
Metabolism and nutrition disorders: Uncommon: Increased appetite.
Psychiatric disorders: Uncommon: Anxiety, insomnia.
Nervous system disorders: Common: Somnolence, headache.
Uncommon: Dizziness.
Ear and labyrinth disorders: Uncommon: Tinnitus, vertigo.
Cardiac disorders: Uncommon: Right bundle branch block, sinus arrhythmia, electrocardiogram QT prolonged, other ECG abnormalities.
Frequency not known: Palpitation, tachycardia.
Respiratory, thoracic and mediastinal disorders: Uncommon: Dyspnoea, nasal discomfort, nasal dryness.
Gastrointestinal disorders: Uncommon: Upper abdominal pain, abdominal pain, nausea, stomach discomfort, diarrhea, dry mouth, dyspepsia, gastritis.
Skin and subcutaneous tissue disorders: Uncommon: Pruritus.
General disorders and administration site conditions: Uncommon: Fatigue, thirst, improved pre-existing condition, pyrexia, asthenia.
Investigations: Uncommon: Increased gamma-glutamyltransferase, alanine aminotransferase increased, aspartate aminotransferase increased, blood creatinine increased, blood triglycerides increased, increased weight.

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 and C_max. These changes can be explained by interaction with intestinal efflux transporter, since Bilastine is substrate for P-gp and not metabolized. 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 C_max of Bilastine. This effect can be explained by interaction by 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.

Store below 30°C.

Antihistamines & Antiallergics

R06AX29 - bilastine ; Belongs to the class of other antihistamines for systemic use.

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