Nixar, tablets 20 mg 30 pcs

anti-allergic agent – H1-histamine receptor blocker

Pharmacodynamics:
Bilastin is an antihistamine agent of long-term action, selectively blocks peripheral H1-receptors.
Significant therapeutic effect is observed one hour after taking the drug, the antihistamine action lasts for 24 hours.
Bilastin may slightly penetrate through the blood-brain barrier, but it has no significant effect on the central nervous system and has no sedative effect.

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

Pharmacokinetics:

Intake. After oral administration, bilastin is rapidly absorbed from the gastrointestinal tract. Time of reaching maximum concentration in blood plasma (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 blood plasma proteins is 84-90%.

Metabolism and excretion. Bilastin is slightly 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 an increase in plasma concentration of bilastine. Changes in pharmacokinetic parameters have no effect on the safety profile of bilastin, since the plasma concentration of bilastin in patients with renal insufficiency remains within the limits of acceptable values.

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

– Allergic (seasonal and year-round) rhinoconjunctivitis: elimination or relief of symptoms (sneezing, nasal congestion, nasal mucosa itching, rhinorrhea, burning and itching sensation in the eyes, red eyes, lacrimation);

– Urticaria: elimination or reduction of skin itching, rash.

Active ingredient

Composition

Active ingredient:

Bilastin – 20.00 mg;

Associates:

Microcrystalline cellulose – 103.00 mg,

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

colloidal silicon dioxide – 0.50 mg,

magnesium stearate – 0.50 mg.

Description:

Oval, biconvex white tablets, with a one-sided ridge for division.

How to take, the dosage

Ingestion.

Unless otherwise prescribed by the physician, the following doses of the drug Nixar are recommended for relieving 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 a day.

The maximal daily dose of bilastine is 20 mg, because increasing of 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.

When bilastine at a dose of 20 mg and diltiazem at a dose of 60 mg, Cmaxc of bilastine was increased by 50%. These effects can 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 the concentration of bilastin in blood plasma.

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.

When bilastin and lorazepam are used concomitantly, no enhancement, suppressive effect of lorazepam on the central nervous system has been 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 concentration of bilastin in blood plasma, which increases the risk of side effects. In this regard, in patients with renal insufficiency of moderate and severe severity 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. However, patients should be warned that in very rare cases dizziness and somnolence may occur, which in turn may affect the ability to drive vehicles or perform other activities requiring increased concentration. In case of occurrence of the above mentioned adverse effects one should refrain from performing the mentioned activities.

Contraindications

– Hypersensitivity to bilastin or excipients of the drug;
– Age under 12 years (effectiveness and safety has not been established);
– Pregnancy and breast-feeding.

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-glutamyltransferase).

Overdose

Symptoms:when using bilastin at a dose 10-11 times higher than the recommended dose, side effects occurred twice as often as when using placebo. The most frequent symptoms were dizziness, headache, and nausea. There were no serious side effects, including significant prolongation of the QT interval.

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