Pharmacy No. 84. Delivery of medicines to your home and office.

The pharmacy is closed on Sundays and holidays.

Medicines

my basket

Apteka84.kz is an online pharmacy that offers its customers medicines, medicinal and decorative cosmetics, dietary supplements, vitamins, baby food, intimate products for adults, medical equipment and thousands of other medical and cosmetic products at low prices. All data presented on the Apteka84.kz website is for informational purposes only and is not a substitute for professional medical care. Apteka84.kz strongly recommends that you carefully read the instructions for use contained in each package of medicines and other products. If you currently have any symptoms of the disease, you should seek help from a doctor. You should always tell your doctor or pharmacist about all the medicines you take. If you feel you need further help, please consult your local pharmacist or contact our GP online or by telephone.

Nixar Tablets, pack, 10 pcs, 20 mg, for oral administration, for ENT organs, for adults

Pharmacological properties

Pharmacodynamics
Bilastine is a long-acting non-sedating antihistamine that selectively blocks peripheral H1 receptors.

A significant therapeutic effect is observed 1 hour after taking the drug.

The antihistamine effect of bilastine lasts for 24 hours.

In clinical studies conducted in adults and adolescents with allergic rhinoconjunctivitis (seasonal and year-round), when using bilastine at a dose of 20 mg 1 time per day for 14-28 days, relief was noted in symptoms such as sneezing, rhinorrhea, itching and nasal congestion, itching sensation and burning in the eyes, lacrimation and redness of the eyes. The therapeutic effect of bilastine lasted 24 hours.

In clinical studies conducted in patients with chronic idiopathic urticaria, bilastine 20 mg once daily for 28 days resulted in relief of skin itching and a reduction in the number and size of blisters, decreased discomfort associated with urticaria, as well as improved sleep and quality of life.

Although little penetration of bilastine across the blood-brain barrier is possible, the central nervous system safety profile of bilastine studied in clinical studies was similar to that of placebo. Bilastine did not cause sedation (in clinical studies, the incidence of drowsiness and fatigue during treatment with bilastine was comparable to that in the placebo group) and had no effect on the central nervous system.

Bilastine does not have an anticholinergic effect. In clinical studies, the use of bilastine was not associated with prolongation of the QTc interval on the ECG or any other cardiovascular effects, either when used in supratherapeutic doses (200 mg once daily for 7 days) or when used simultaneously with P-gp inhibitors (ketoconazole, erythromycin).

Pharmacokinetics

Suction. After oral administration, bilastine is rapidly absorbed from the gastrointestinal tract. The time to reach maximum plasma concentration (TCmax) is 1.3 hours. The bioavailability of bilastine when taken orally is 61%. Concomitant food intake reduces the bioavailability of bilastine by 30%. No accumulation of the drug is observed.

Distribution. In vitro and in vivo studies have shown that bilastine is a substrate of P-glycoprotein and the organic anion transport protein OATP (see section “Interaction with other drugs”). Bilastine does not appear to be a substrate of the BCRP transporter or the renal transporters OTC2, OAT1 and OAT3. Bilastine has demonstrated weak inhibition of Z-glycoprotein, OATP2B1 and OCT1. Based on the results of in vitro studies, bilastine is not expected to inhibit the transporters P-glycoprotein, MRP2, BCRP, BSEP, OATP1B1, OATP1B3, OATP2B1, OAT1, OAT3, OCT1, OCT2, and NTCP in the systemic circulation. The concentration of half-maximal inhibition (IC50>300 μM) of bilastine of these transporters is estimated to be significantly higher than its calculated clinical maximum concentration (Cmax) in blood plasma, as a result of which the interaction of bilastine with them is not clinically significant. Based on these results, it cannot, however, be ruled out that bilastine inhibits carrier proteins in the intestinal mucosa (for example, D-glycoprotein). When used in therapeutic doses, the association of bilastine with blood plasma proteins is 84-90%.

Metabolism and excretion. Bilastine is slightly metabolized. After a single use, up to 95% of bilastine from the dose taken is excreted unchanged by the kidneys (28.3%) and bile (66.5%). In vitro studies have shown that bilastine is not an inducer or inhibitor of cytochrome P450 isoenzymes. The half-life (T1/2) of bilastine in healthy volunteers averages 14.5 hours.

In patients with mild renal failure (glomerular filtration rate (GFR) 50-80 ml/min/1.73 m2), the rate of bilastine elimination was not significantly different from that in patients without renal failure (glomerular filtration rate (GFR) >80 ml/min /1.73 m2). In patients with moderate renal failure (glomerular filtration rate (GFR) 30-50 ml/min/1.73 m2) and severe renal failure (GFR < 30 ml/min/1.73 m2), the rate of bilastine elimination is slowed, which may lead to to increase the concentration of bilastine in the blood plasma. It is not expected that changes in these pharmacokinetic parameters may affect the safety profile of bilastine, since the concentration of bilastine in the blood plasma in patients with renal failure remains within safe limits.

In case of liver failure, clinically significant changes in the pharmacokinetic parameters of bilastine do not occur, since bilastine is slightly metabolized in the liver. Pharmacokinetic data obtained in patients with hepatic impairment are not available.

There were no significant differences in the pharmacokinetic parameters of bilastine in patients over 65 years of age compared to those in patients aged 18 to 35 years. Pharmacokinetic data for bilastine in adolescents (12 to 17 years) are not available because pharmacokinetic data obtained in adults may be extrapolated from this population.

In the studied dose range (5-220 mg), the pharmacokinetics of bilastine is linear.

Overdose

Data regarding acute overdose were obtained only from clinical studies. When using bilastine in doses 10–11 times higher than therapeutic, side effects in healthy volunteers occurred 2 times more often than when using placebo. Side effects that were more commonly reported included dizziness, headache, and nausea. No serious adverse reactions or significant increase in the duration of the q-tc interval were noted. A crossover qt/qtc interval study examining the effect of repeated use of bilastine on ventricular repolarization did not show a statistically significant prolongation of the qtc interval.

Treatment. In case of overdose, symptomatic and supportive therapy is recommended. A specific antidote for bilastine is unknown.

Side effects

During clinical trials in patients with allergic rhinoconjunctivitis or chronic idiopathic urticaria, side effects with bilastine 20 mg occurred at approximately the same frequency as with placebo (12.7% and 12.8%). The results of the studies indicate that when using bilastine at a dose of 20 mg, the most frequently observed adverse reactions were headache, drowsiness, dizziness and fatigue. These adverse events were reported at approximately the same rate in patients receiving placebo.

The following are adverse reactions that are known or at least suspected to be related to bilastine and that were reported in more than 0.1% of patients receiving bilastine 20 mg in the clinical development program.

By frequency, side effects are divided into the following categories: very often (≥1/10); often (≥1/100 and 1/10); sometimes (≥1/1000 and 1/100); rare (≥1/10,000 and 1/1000); very rare (1/10,000), unknown (available data do not allow an estimate).

Infections and parasitic diseases: sometimes - oral herpes.

Eating and metabolic disorders: sometimes - increased appetite.

From the mental side: sometimes - anxiety, insomnia.

On the part of the organ of hearing and balance: sometimes - tinnitus, dizziness.

From the cardiovascular system: sometimes - right bundle branch block, sinus arrhythmia, prolongation of the QT interval on the ECG, other ECG abnormalities.

From the nervous system: often - drowsiness, headache; sometimes - dizziness.

From the respiratory system: sometimes - shortness of breath, discomfort in the nose, dry nose.

From the digestive system: sometimes - pain in the upper abdomen, abdominal pain, nausea, discomfort in the abdomen, diarrhea, dry mouth, dyspepsia, gastritis.

From the skin and subcutaneous fat tissue: sometimes - itching.

General and local disorders: sometimes - fatigue, thirst, worsening of existing diseases, fever, asthenia.

Additional research methods: increased activity of gamma-glutamyl transpeptidase, ALT, AST, increased creatinine levels in the blood, increased TG levels in the blood, increased body weight.

special instructions

In patients with moderate or severe renal impairment, the use of bilastine simultaneously with p-glycoprotein inhibitors (ketoconazole, erythromycin, cyclosporine, ritonavir, diltiazem, etc.) may lead to an increase in the concentration of bilastine in the blood plasma and, therefore, to an increased risk of its side effects . Therefore, in patients with moderate or severe renal impairment, bilastine should not be used concomitantly with p-glycoprotein inhibitors.

Use during pregnancy and lactation. Fertility. Clinical data are limited. Animal studies have not revealed any negative effects of the drug on fertility.

Pregnancy. There are no data on the use of bilastine in pregnant women.

Animal studies also showed no harmful effects of the drug (direct or indirect) on reproductive function, childbirth or postnatal development. Taking into account safety, Nixar should not be used during pregnancy.

Lactation. There are no data on whether bilastine passes into women's breast milk. The excretion of bilastine in milk has not been studied in animals. The decision to extend or discontinue breastfeeding, as well as to continue or discontinue therapy with Nixar, should be made taking into account the benefits of breastfeeding for the child, on the one hand, and the need for bilastine therapy for the mother, on the other.

Children. The safety and effectiveness of bilastine in children under 12 years of age have not been established.

The ability to influence reaction speed when driving vehicles or working with other mechanisms. According to a study of the effect of bilastine on the ability to drive vehicles, the use of bilastine at a dose of 20 mg does not affect the ability to drive vehicles. However, patients should be informed that in some cases the drug may cause drowsiness and thus affect the ability to drive vehicles and operate machines.

Application

Adults and children (ages 12 and up). The recommended dose is 20 mg (1 tablet) 1 time per day to relieve the symptoms of allergic rhinoconjunctivitis (seasonal and year-round) and urticaria.

The tablet should be taken orally 1 hour before or 2 hours after a meal or fruit juice.

Elderly patients. Elderly patients do not require dose adjustment. Experience with the drug in patients over 65 years of age is limited.

Renal dysfunction. Patients with impaired renal function do not require dose adjustment.

Liver dysfunction. There is no experience of clinical use of the drug in patients with impaired liver function. Since bilastine is not metabolized and is excreted primarily by the kidneys, impairment of liver function should not increase its systemic exposure to dangerous levels. Therefore, patients with impaired liver function do not require dose adjustment.

Duration of treatment. For patients with allergic rhinitis, the drug should be used only during contact with allergens. For people with seasonal allergic rhinitis, treatment can be stopped after the symptoms have subsided and resumed when they return. For patients with year-round allergic rhinitis, the drug can be used continuously during the period of contact with allergens. In patients with urticaria, the duration of therapy depends on the nature and duration of symptoms, as well as their dynamics.