Nixar tablets 20 mg blister No. 30

Instructions for Nixar tablets 20 mg blister No. 30

Composition

active ingredient: bilastine;

1 tablet contains bilastine 20 mg;

Excipients: microcrystalline cellulose, sodium starch glycolate (type A), colloidal anhydrous silicon dioxide, magnesium stearate.

Dosage form

Pills.

Main physicochemical properties: oval, biconvex white tablets with a score line (length 10 mm, width 5 mm) without lines or cracks on the surface. The score line is intended solely to break the tablet for easier swallowing, and not to divide into equal doses.

Pharmacotherapeutic group

Antihistamines for systemic use. Other antihistamines for systemic use. Bilastine. ATX code R06A X29.

Pharmacological properties

Pharmacodynamics.

Mechanism of action: Bilastine is a long-acting, non-sedating histamine antagonist, a highly selective blocker of peripheral H1 receptors that does not bind to muscarinic receptors.

After a single application, bilastine inhibits the development of histamine-induced skin reactions, manifested by blisters and redness, for 24 hours.

Clinical efficacy and safety: In clinical studies conducted in adults and adolescents with allergic rhinoconjunctivitis (seasonal and perennial), bilastine 20 mg once daily for 14-28 days was effective in relieving symptoms such as sneezing, nasal discharge, nasal itching, nasal congestion, itchy eyes, tearing and redness. Symptoms were effectively controlled by bilastine for 24 hours.

In two clinical studies in patients with chronic idiopathic urticaria, bilastine 20 mg once daily for 28 days was effective in reducing the intensity of itching and the number and size of wheals, as well as the discomfort caused by urticaria. Patients also experienced improvements in sleep and quality of life.

In clinical studies with bilastine, no clinically significant prolongation of the QTc interval or any other cardiovascular effects were observed, even when administered at a dose of 200 mg per day (10 times the clinical dose) for 7 days in 9 subjects or when co-administered with P-glycoprotein (P-gp) inhibitors such as ketoconazole (24 subjects) and erythromycin (24 subjects). In addition, a thorough QT study was conducted in 30 volunteers.

In controlled clinical trials, the CNS safety profile of bilastine and placebo at the recommended dose of 20 mg once daily was similar, and the incidence of somnolence with bilastine was not statistically different from that with placebo. Bilastine at doses up to 40 mg daily did not affect psychomotor performance in clinical trials or the ability to drive in a standard driving test.

In elderly patients (≥ 65 years) who participated in phase II and III studies, the efficacy and safety of the drug did not differ from those in younger patients.

In a post-marketing study conducted in 146 elderly patients, no differences in the safety profile were found compared to other adult participants.

Children.

Adolescents (aged 12–17 years) were enrolled in the clinical development program. Of these, 128 adolescents received bilastine in clinical trials (81 in double-blind studies of allergic rhinoconjunctivitis), and the remaining 116 adolescents were randomized to active comparator or placebo. No differences in efficacy and safety were observed between adults and adolescents.

In a 12-week controlled clinical study in children aged 2 to 11 years (a total of 509 children, of whom 260 received 10 mg bilastine: 58 subjects were aged 2 to < 6 years, 105 subjects were aged 6 to < 9 years and 97 subjects were aged 9 to < 12 years, and 249 subjects were treated with placebo: 58 subjects were aged 2 to < 6 years, 95 subjects were aged 6 to < 9 years and 96 subjects were aged 9 to < 12 years) at the recommended paediatric dose of 10 mg once daily, the safety profile of bilastine (n = 260) was similar to that of placebo (n = 249), with adverse reactions occurring in 5.8% and 8.0% of patients receiving 10 mg bilastine and placebo, respectively. Both 10 mg bilastine and placebo resulted in a small reduction in sleepiness and sedation as assessed by the Pediatric Sleep Quality Questionnaire, with no statistically significant difference between treatment groups. In children aged 2 to 11 years, no significant difference in QTc was observed after 10 mg bilastine per day compared to those receiving placebo. A special questionnaire on the quality of life of children with allergic rhinoconjunctivitis or chronic urticaria showed an overall improvement in scores over 12 weeks, with no statistically significant difference between the bilastine and placebo groups. A total of 509 children participated in the study, including 479 participants with allergic rhinoconjunctivitis and 30 participants with diagnosed chronic urticaria. 260 children received bilastine, 252 (96.9%) for the treatment of allergic rhinoconjunctivitis and 8 (3.1%) for the treatment of chronic urticaria. Similarly, 249 children received placebo: 227 (91.2%) for the treatment of allergic rhinoconjunctivitis and 22 (8.8%) for the treatment of chronic urticaria.

The European Medicines Agency has waived the obligation to submit the results of studies with bilastine in all paediatric subjects below 2 years of age (see section 4.2).

Pharmacokinetics.

Absorption: After oral administration, bilastine is rapidly absorbed, with peak plasma concentrations occurring approximately 1.3 hours after administration. No accumulation was observed. The mean oral bioavailability of bilastine is 61%.

Distribution: In vitro and in vivo studies have shown that bilastine is a substrate of P-gp (see Interactions with ketoconazole, erythromycin and diltiazem) and OATP (see Interactions with grapefruit juice). Bilastine does not appear to be a substrate of BCRP or the renal transporters OST2, OAT1 and OAT3. In vitro data do not suggest that bilastine inhibits the activity of transport proteins such as P-gp, MRP2, BCRP, BSEP, OATP1B1, OATP1B3, OATP2B1, OAT1, OAT3, OCT1, OCT2 and NTCP in the systemic circulation, as its ability to inhibit P-gp, OATP2B1 and OCT1 is negligible and is characterized by an IC50 ≥ 300 μM, which significantly exceeds the estimated maximum plasma concentration (Cmax) in the case of clinical use of bilastine. Therefore, such interactions are unlikely to be of clinical significance. However, these results indicate that inhibition of transport proteins located in the intestinal mucosa (e.g. P-gp) by bilastine cannot be excluded. At therapeutic doses, bilastine is 84-90% bound to plasma proteins.

Biotransformation: In in vitro studies, bilastine did not show the ability to induce or inhibit the activity of CYP450 isoenzymes.

Conclusion: In a mass balance study conducted in healthy adult volunteers, after a single dose of 20 mg 14C-bilastine, almost 95% of the administered dose was recovered in urine and feces (28.3% and 66.5%, respectively) as unchanged bilastine, suggesting that bilastine is only slightly metabolized in humans. The mean elimination half-life of bilastine in healthy volunteers is 14.5 hours.

Linearity: In the dose range studied (5 to 220 mg), bilastine exhibits linear pharmacokinetics with low interindividual variability.

Kidney dysfunction. A study in patients with different renal function showed that in case of normal renal function (GFR: > 80 ml/min/1.73 m2) the mean AUC0-¥ (± sd.) is 737.4 (± 260.8) ng•h/ml, in case of mild renal impairment (GFR: 50–80 ml/min/1.73 m2) this indicator is 967.4 (± 140.2) ng•h/ml, in case of moderate impairment (GFR: 30–<50 ml/min/1.73 m2) – 1384.2 (± 263.23) ng•h/ml, and in case of severe impairment (GFR: <30 ml/min/1.73 m2) – 1708.5 (± 699.0) ng•hr/ml.

Hepatic impairment. Pharmacokinetic data in patients with hepatic impairment are not available. Bilastine is not metabolised in humans. The results of a study in patients with renal impairment showed that bilastine is mainly excreted by the kidneys and is likely to be excreted only to a minor extent in the bile. Changes in hepatic function have no clinically significant effect on the pharmacokinetics of bilastine.

Elderly patients. Data on the pharmacokinetics of the drug in patients over 65 years of age are limited. The pharmacokinetic parameters of bilastine in patients over 65 years of age and in patients 18–35 years of age are not statistically significantly different.

Children: Pharmacokinetic data in adolescents (12–17 years) are not available, as extrapolation of data from adults is considered appropriate for this medicinal product.

Pharmacokinetic data in children were obtained in a phase II pharmacokinetic study involving 31 children aged 4 to 11 years with allergic rhinoconjunctivitis or chronic urticaria who received 1 bilastine orodispersible tablet 10 mg once daily. Analysis of the pharmacokinetic data on plasma bilastine concentrations showed that after administration of bilastine at a dose of 10 mg once daily, recommended for the treatment of pediatric patients, its systemic exposure is consistent with that observed in adults and adolescents after administration of the drug at a dose of 20 mg, and the mean AUC value in children aged 6 to 11 years is 1014 ng•h/ml. These results were generally below the maximum safe level established on the basis of data on the use of the drug in adults at a dose of 80 mg once daily according to the safety profile of the drug. These results confirmed that a bilastine dose of 10 mg orally once daily is a reasonable therapeutic dose for pediatric patients aged 6 to 11 years with a body weight of at least 20 kg.

Indication

Symptomatic treatment of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria.

Contraindication

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

Interaction with other medicinal products and other types of interactions

Interaction studies have been conducted only in adults and are listed below.

Interaction with food. Food reduces the bioavailability of bilastine taken orally by 30%.

Interaction with grapefruit juice. When bilastine 20 mg was co-administered with grapefruit juice, the bioavailability of bilastine was reduced by 30%. A similar effect may also be observed with other fruit juices. The extent of the reduction in bioavailability may vary depending on the manufacturer of the juice and the fruit. The mechanism of this interaction is inhibition of the transporter protein OATP1A2, for which bilastine is a substrate (see section 5.2). Medicinal products that are substrates or inhibitors of OATP1A2 (e.g. ritonavir or rifampicin) may also reduce the plasma concentration of bilastine.

Interaction with ketoconazole or erythromycin. When 20 mg bilastine once daily was co-administered with 400 mg ketoconazole once daily or 500 mg erythromycin three times daily, the AUC of bilastine was doubled and the Cmax was increased 2-3-fold. Such changes can be explained by interactions at the level of transport proteins responsible for the excretion of drugs from intestinal cells, since bilastine is a substrate for P-glycoprotein and is not metabolized (see section "Pharmacokinetics"). The safety profile of bilastine, on the one hand, and ketoconazole or erythromycin, on the other, is probably not affected by these changes. Other drugs that are substrates or inhibitors of P-gp (e.g. cyclosporine) may also increase the plasma concentration of bilastine.

Interaction with diltiazem. When 20 mg bilastine once daily was co-administered with 60 mg diltiazem once daily, the Cmax of bilastine was increased by 50%. This effect can be explained by an interaction at the level of transport proteins (see section 5.2) responsible for the excretion of drugs from intestinal cells; this effect is unlikely to affect the safety profile of bilastine.

Interaction with ethyl alcohol. After simultaneous use of alcohol and bilastine at a dose of 20 mg once a day, psychomotor functions were at the same level as after simultaneous use of alcohol and placebo.

Interaction with lorazepam. When bilastine 20 mg once daily was administered concomitantly with lorazepam 3 mg once daily for 8 days, no enhancement of the CNS depressant effect of lorazepam was observed.

Children. Drug interaction studies have only been performed in adults. As there is no clinical experience with the interaction of bilastine with other drugs, food or fruit juices in children, the results of interaction studies in adults should be taken into account when prescribing bilastine to pediatric patients. There are no clinical data on the basis of which it could be concluded whether changes in AUC or Cmax due to interactions affect the safety profile of bilastine in children.

Application features

Children: The efficacy and safety of bilastine in children under 2 years of age have not been established, and clinical experience in children aged 2 to 5 years is limited, therefore bilastine should not be prescribed to these age groups.

In patients with moderate or severe renal impairment, concomitant use of bilastine with P-glycoprotein inhibitors (ketoconazole, erythromycin, cyclosporine, ritonavir or diltiazem, etc.) may lead to increased plasma levels of bilastine and, consequently, an increased risk of its side effects. Therefore, concomitant use of bilastine and P-glycoprotein inhibitors should be avoided in patients with moderate or severe renal impairment.

This medicine contains less than 1 mmol (23 mg) sodium per tablet, i.e. essentially 'sodium-free'.

Use during pregnancy or breastfeeding

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 function, parturition or postnatal development. For safety reasons, it is preferable to avoid the use of Nixar® during pregnancy.

Breastfeeding. Studies on the excretion of bilastine into human milk have not been conducted. Available pharmacokinetic data have shown that bilastine is excreted in breast milk in animals. A decision on whether to continue/discontinue breast-feeding or to discontinue/abstain from Nixar® therapy should be made taking into account the benefit of breast-feeding for the child and the benefit of bilastine therapy for the mother.

Fertility: Limited or no clinical data are available. A study in rats did not reveal any adverse effects on fertility.

Ability to influence reaction speed when driving vehicles or other mechanisms

A study of the effect of bilastine on the ability to drive showed that treatment with bilastine at a dose of 20 mg in adults did not affect the ability to drive. However, since individual response to the drug may vary, patients should be advised to refrain from driving or operating other machinery until their own response to bilastine is known.

Method of administration and doses

Dosage.

Adults and children (12 years of age and older): 20 mg bilastine (1 tablet) once daily for the relief of symptoms of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria.

The tablet should be taken 1 hour before or 2 hours after food or fruit juice (see section “Interaction with other medicinal products and other types of interactions”).

Duration of treatment. Patients with allergic rhinoconjunctivitis should use the drug only during the period of contact with allergens. Patients with seasonal allergic rhinitis should stop treatment after symptoms subside and resume after their return. Patients with perennial allergic rhinitis should use the drug continuously during the period of contact with allergens. In the case of urticaria, the duration of treatment depends on the nature and duration of symptoms, as well as their dynamics.

Special patient groups.

Elderly patients: No dose adjustment is required for elderly patients (see sections 5.2 and 5.1).

Renal impairment: Studies conducted in adults at high risk (patients with renal impairment) have shown that there is no need to adjust the dose of bilastine for adults (see section 5.2).

Hepatic impairment. There is no clinical experience in adult patients with hepatic impairment. However, since bilastine is not metabolized and is excreted unchanged in the urine and feces, hepatic impairment is not expected to increase its systemic exposure to a dangerous level in adult patients. Therefore, no dose adjustment is required in adult patients with hepatic impairment (see section 5.2).

Children.

- Children aged 6 to 11 years with a body weight of at least 20 kg.

This group of patients can be prescribed bilastine, orodispersible tablets, 10 mg, as well as bilastine, oral solution, 2.5 mg/ml.

- Children under 6 years of age with a body weight of up to 20 kg.

Currently available data are described in sections 4.4, 4.8, 4.8, 4.9, 5.1, 5.2, 5.3, 5.4, 5.5, 5.6, 5.7, 5.8, 5.9, 5.1, 5.2, 5.3, 5.4, 5.6, 5.8, 5.9, 5.1, 5.2, 5.3, 5.4, 5.5, 5.6, 5.6, 5.7, 5.8, 5.9, 5.1, 5.2, 5.3, 5.4, 5.5, 5.6, 5.6, 5.7, 5.8, 5.9, 5.1, 5.1, 5.2, 5.3, 5.4, 5.5, 5.6, 5.6, 5.7, 5.8, 5.9, 5.1, 5.1, 5.2, 5.3, 5.4, 5.5, 5.6, 5.7, 5.8, 5.9, 5.1, 5.1, 5.2, 5.3

The safety and efficacy of bilastine in children with renal or hepatic impairment have not been established.

Method of application.

For oral use.

The tablets should be taken with water. The daily dose is recommended to be taken in one go.

Children

The drug with the active ingredient bilastine 20 mg is intended for use in children aged 12 years and older.

Overdose

Information on acute overdose with bilastine was obtained during clinical trials conducted during development and post-marketing surveillance. In clinical trials, after administration of bilastine to 26 healthy adult volunteers at doses exceeding the therapeutic dose by 10-11 times (220 mg as a single dose or 200 mg daily for 7 days), the incidence of adverse reactions was twice as high as with placebo. The most commonly reported adverse reactions were dizziness, headache and nausea. There were no reports of serious adverse reactions and no significant prolongation of the QTc interval. The information collected during post-marketing surveillance is consistent with the data obtained during clinical trials.

In a thorough crossover study of QT/QTC intervals in 30 healthy adult volunteers, a critical assessment of the effects of multiple doses of bilastine (100 mg × 4 days) on ventricular repolarization revealed no significant prolongation of the QTC interval.

There are no data on overdose in children. In case of overdose, symptomatic and supportive treatment is recommended.

The specific antidote to bilastine is unknown.

Adverse reactions

General safety profile in adult and adolescent patients. In clinical trials in adult and adolescent patients with allergic rhinoconjunctivitis or chronic idiopathic urticaria, adverse reactions with bilastine 20 mg occurred at approximately the same frequency as with placebo (12.7% vs. 12.8%). Phase II and III clinical trials conducted during clinical development included 2525 adult and adolescent patients treated with various doses of bilastine, of whom 1697 received bilastine 20 mg. In these trials, 1362 patients received placebo. Patients receiving bilastine 20 mg for the indication allergic rhinoconjunctivitis or chronic idiopathic urticaria most frequently reported the following adverse reactions: headache, somnolence, dizziness and fatigue. These adverse reactions occurred at a frequency comparable to the frequency of adverse reactions in patients receiving placebo.

Table of adverse reactions in adult and adolescent patients. The table below lists adverse reactions that were possibly related to bilastine and occurred in more than 0.1% of patients treated with bilastine 20 mg during clinical development (N = 1697).

The frequency of adverse reactions is defined as follows: very common (≥ 1/10); common (≥ 1/100 - < 1/10); uncommon (≥ 1/1000 - < 1/100); rare (≥ 1/10000 - < 1/1000); very rare (< 1/10000); unknown (cannot be estimated from the available data).

Reactions that occur rarely and very rarely, as well as those whose frequency is unknown, have not been included in the table.

Frequency not known (cannot be estimated from the available data): palpitations, tachycardia, hypersensitivity reactions (such as anaphylaxis, angioedema, dyspnoea, rash, localised/localised oedema, and erythema) and vomiting have been reported in the post-marketing period.

Description of selected adverse reactions in adult and adolescent patients. Somnolence, headache, dizziness and fatigue were observed in both patients receiving bilastine 20 mg and patients receiving placebo. The reporting rates were 3.06% vs. 2.86% for somnolence; 4.01% vs. 3.38% for headache; 0.83% vs. 0.59% for dizziness; 0.83% vs. 1.32% for fatigue.

Information collected during post-marketing surveillance confirmed the safety profile observed during clinical development.

General safety profile in children: During clinical development, the frequency, type and severity of adverse reactions in adolescents (12-17 years) were similar to those in adults. The information collected in this group (adolescents) during post-marketing surveillance was confirmed by the results of clinical trials.

The percentage of children (2–11 years) who experienced adverse reactions after treatment of allergic rhinoconjunctivitis or chronic idiopathic urticaria with bilastine 10 mg during a 12-week controlled clinical trial was comparable to the percentage of patients receiving placebo (68.5% vs. 67.5%).

The most frequently reported adverse reactions in 291 children (2–11 years) treated with bilastine (orodispersible tablets) in clinical trials (#260 children in the safety study, 31 children in the pharmacokinetic study) included headache, allergic conjunctivitis, rhinitis, and abdominal pain. These adverse reactions were reported with comparable frequency in 249 patients treated with placebo.

Table of adverse reactions in children. The table below lists adverse reactions that were possibly related to bilastine and occurred in more than 0.1% of children (2–11 years) who received bilastine during clinical development.

The frequency of adverse reactions is distributed as follows: very common (≥ 1/10); common (≥ 1/100 - < 1/10); uncommon (≥ 1/1000 - < 1/100); rare (≥ 1/10000 - < 1/1000); very rare (< 1/10000); unknown (cannot be estimated from the available data).

Reactions that occur rarely and very rarely, as well as those whose frequency is unknown, have not been included in the table.

#260 children received the drug during clinical safety studies, 31 children received the drug during pharmacokinetic studies

Description of selected adverse reactions in children. Headache, abdominal pain, allergic conjunctivitis and rhinitis were observed in both children treated with bilastine 10 mg and children treated with placebo. The reported frequencies were: 2.1% vs. 1.2% for headache; 1.0% vs. 1.2% for abdominal pain; 1.4% vs. 2.0% for allergic conjunctivitis and 1.0% vs. 1.2% for rhinitis.

Reporting of suspected adverse reactions. Reporting of adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua or via the company website https://www.berlin-chemie.ua.

Expiration date

5 years.

Do not use the drug after the expiration date indicated on the package.

Storage conditions

No special storage conditions are required. Keep out of the reach of children.

Packaging

10 tablets in a blister; 1 or 2, or 3, or 5 blisters in a cardboard box.

Vacation category

According to the recipe.

Producer

Menarini-Von Heyden GmbH.

Location of the manufacturer and address of its place of business

Leipziger Strasse 7-13, 01097 Dresden, Germany.

Producer

A. Menarini Manufacturing Logistics and Services S.r.L.

Location of the manufacturer and address of its place of business

Via Campo di Pile, 67100 L'Aquila (AC), Italy.

Applicant

Menarini International Operations Luxembourg S.A.

Applicant's location

1, Avenue de la Gare, L-1611 Luxembourg, Luxembourg.

Reviews

There are no reviews for this product.

+ Add review

Write a review

Nixar tablets 20 mg blister No. 30

My mark:

Continue

There are no reviews for this product, be the first to leave your review.

new

Hit

Itopride Farmak tablets 50 mg blister No. 40

In stock

0

445.76 грн.

Add to Cart

new

Hit

Rabezol enteric-coated tablets 20 mg No. 28

In stock

0

568.21 грн.

Add to Cart

new

Hit

Ototon ear drops bottle 16 g

In stock

0

334.10 грн.

Add to Cart

new

Hit

Cipralex film-coated tablets 10 mg No. 28

In stock

0

1 262.09 грн.

Add to Cart

new

Hit

Sold out

SinuSalt nasal rinse 250 ml bottle with nasal adapter cap and silicone tube + saline mixture in bags No. 26

Распродано

0

852.70 грн.

new

Hit

Sold out

Balm Star 10 g

Распродано

0

61.00 грн.

new

Hit

Farisil sore throat spray for oral cavity 1.5 mg/ml with lemon flavor 30 ml

In stock

0

415.64 грн.

Add to Cart

new

Hit

Filorga Optim-Eyes Eye Contour with hyaluronic acid 15 ml

In stock

0

1 579.54 грн.

Add to Cart

new

Hit

Omeprazole capsules 40 mg No. 30

In stock

0

391.22 грн.

Add to Cart

new

Hit

Sold out

CBD OIL WITH CANNABIDIOL 10% SPRAY 10ML MINT

Распродано

0

982.20 грн.