Nixar, tablets 20 mg 10 pcs

Anti-allergic agent – H1-histamine receptor blocker.

Pharmacodynamics:

Bilastin is a long-acting antihistamine agent that selectively blocks peripheral H1-receptors.

The significant therapeutic effect is observed one hour after taking the drug, the antihistamine effect lasts for 24 hours.

Possible minor penetration of bilastin through the blood-brain barrier, but bilastin has no significant effect on the central nervous system and does not cause sedation.

It has no anticholinergic effect. No prolongation of the QT interval on the ECG is observed.

Pharmacokinetics:

Intake. After oral administration, bilastin is rapidly absorbed from the gastrointestinal tract. Time of reaching maximum blood plasma concentration (TSmax) is 1.3 h. Bioavailability of bilastin when taken orally is 61%. Concomitant intake of food reduces the bioavailability of bilastin by 30%. No drug accumulation is observed. Binding to plasma proteins is 84-90%.

Metabolism and excretion. Bilastin is mildly metabolized, after a single use up to 95% of the administered dose is excreted unchanged by the kidneys (28.3%) and with the bile (66.5%). The elimination half-life (T1/2) is on average 14.5 hours.

In 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 elimination rate of bilastine is slowed, which may lead to increased plasma bilastine concentration.

Changing pharmacokinetic parameters has no effect on the safety profile of bilastin, since the plasma concentration of bilastin in patients with renal impairment remains within tolerance.

In hepatic insufficiency there are no clinically significant changes in pharmacokinetic parameters of bilastin since bilastin is slightly metabolized in the liver.

The pharmacokinetic parameters of bilastin in elderly patients are similar to those in younger patients.

Indications

Active ingredient

Composition

Active ingredient:

microcrystalline cellulose – 103.00 mg,

sodium carboxy-methyl starch (type A) – 1.00 mg,

How to take, the dosage

Ingestion.

Unless otherwise prescribed by the physician, the following doses of the drug Nixar are recommended for stopping symptoms of allergic rhinoconjunctivitis and urticaria:

Adults and children over 12 years: 1 tablet of the drug Nixar, which corresponds to 20 mg of bilastine, once daily.

The maximum daily dose of bilastine is 20 mg, as increasing the dose does not increase the therapeutic effect.
The tablet is taken one hour before a meal or 2 hours after a meal (or fruit juice).

In allergic rhinoconjunctivitis the drug is used for the entire period of contact with allergens.

In case of urticaria, treatment is continued until the symptoms disappear or are relieved.

In patients with impaired hepatic and renal function, no dose adjustment is required.

Dose adjustment is not required in elderly patients. There is little experience with Nixar® in patients over 65 years of age.

Interaction

In concomitant use of bilastine with ketoconazole or erythromycin the area under the curve “concentration-time” (AUC) of bilastine increased by 2 times, and the maximum concentration (Cmax) – by 2-3 times.

Concomitant administration of bilastine at a dose of 20 mg and diltiazem at a dose of 60 mg increased Cmaxc of bilastine by 50%. These effects may be explained by the interaction at the level of carrier proteins (including P-glycoprotein) responsible for excretion of drugs from intestinal cells, the substrate of which is bilastin.

Concomitant use of bilastin and other drugs that are substrates or inhibitors of P-glycoprotein (e.g., cyclosporine) may increase plasma concentration of bilastin.

Grapefruit and other fruit juices decrease the bioavailability of bilastin by 30%. This interaction is due to the ability of fruit to inhibit the activity of the organic anion transporter protein OATP1A2, for which bilastin is a substrate. Drugs that are substrates or inhibitors of OATP1A2 (e.g., ritonavir or rifampicin) may decrease the plasma concentration of bilastin.

Bilastin does not increase the effects of ethanol on the central nervous system.

In concomitant use of bilastin and lorazepam no enhancement, suppressive effect of lorazepam on the central nervous system was found.

Special Instructions

In patients with moderate renal insufficiency (GFR 30-50 ml/min/1.73 m2) and severe renal insufficiency (GFR < 30 ml/min/1.73 m2) concomitant use with P-glycoprotein inhibitors may lead to increased plasma concentration of bilastin, which increases the risk of side effects.

In this regard, in patients with moderate to severe renal insufficiency, caution should be exercised when concomitant use of bilastine with P-glycoprotein inhibitors (ketoconazole, erythromycin, cyclosporine, ritonavir, diltiazem, etc.).

The effect on the ability to drive:

In a study conducted to evaluate the effect of bilastine at a dose of 20 mg on driving ability, no adverse effect of the drug was found.

Patients should be cautioned, however, that in very rare cases dizziness, somnolence may occur, which in turn may affect the ability to drive vehicles or perform other activities requiring increased concentration.

In case of the occurrence of the described adverse events, you should refrain from performing the specified activities.

Contraindications

Hypersensitivity to bilastin or excipients of the drug;

Under 12 years of age (efficacy and safety not established);

pregnancy and breastfeeding.

Side effects

Possible side effects are listed below in descending frequency of occurrence: very frequently (≥1/10), frequently (≥1/100, < 1/10), infrequently (≥1/1000, < 1/100), rarely (≥1/10000, < 1/1000), very rarely (< 1/10000), including individual reports.

Gastrointestinal disorders
Infrequent: dry oral mucosa, diarrhea, dyspepsia, gastritis, abdominal pain, upper abdominal pain, stomach discomfort, nausea.

Skin and subcutaneous tissue disorders
Infrequent: skin itching.

Nervous system disorders
Often: drowsiness, headache;
Infrequently: dizziness.

Psychiatric disorders
Infrequent: anxiety, insomnia.

Metabolic disorders
Infrequent: increase in appetite, weight gain.

Hearing and labyrinth disorders
Infrequent: tinnitus, vertigo.

Respiratory system, thorax and mediastinum disorders
Infrequent: shortness of breath, dry nasal mucosa, nasal discomfort.

Cardiovascular system disorders
Infrequent: right bundle branch block, sinus arrhythmia, prolongation of QT interval in electrocardiogram, other electrocardiogram changes.

Infectious and parasitic diseases
Infrequent: herpetic lesions of the oral cavity.

Other:
Infrequent: thirst, increased fatigue, asthenia, fever, increased concentration of triglycerides in plasma, increased concentration of creatinine in plasma, increased activity of “liver” enzymes (aspartate aminotransferase, alanine aminotransferase, gamma-glotamyltransferase).

Overdose

Symptoms: in clinical trials in healthy volunteers when bilastine was administered at a dose 10-11 times therapeutic (220 mg once or 200 mg daily for 7 days), side effects occurred 2 times more often than when using placebo. The most frequently reported symptoms were dizziness, headache, and nausea. No serious side effects, including significant prolongation of the QTc interval, were observed. The information obtained in post-registration studies confirms the safety profile of bilastine described in the pre-registration clinical trials.

The evaluation of the effects of multiple supratherapeutic doses of bilastine (100 mg daily for 4 days) on ventricular repolarization (QT/QTc interval crossover study) in 30 healthy volunteers showed no significant prolongation of the QTc segment on the cardiogram.

Treatment: symptomatic and supportive therapy. There is no specific antidote.