Nixar pills 20mg №10

Composition

Active substance:

bilustin - 20.00 mg;
Excipients: microcrystalline cellulose - 103.00 mg, sodium carboxymethyl starch (type A) - 1.00 mg, colloidal silicon dioxide - 0.50 mg, Magnesium stearate - 0.50 mg.

Description: Oval, biconvex pills of white color, with a unilateral risk for division.

Mechanism of action

antiallergic agent - H1-histamine receptor blocker

Pharmacodynamics:
Bilustin is a long-acting antihistamine that selectively blocks peripheral H1 receptors.
A significant therapeutic effect is observed an hour after taking the drug, the antihistamine effect persists for 24 hours.
A slight penetration of bilastin through the blood-brain barrier is possible, but bilastin does not have a significant effect on the central nervous system and does not cause a sedative effect.
It has no anticholinergic action. Elongation of the QT interval on the ECG is not observed.

Pharmacokinetics:

Suction. After ingestion, bilastin is rapidly absorbed from the gastrointestinal tract. The time to reach the maximum plasma concentration (TCmax) is 1.3 hours. The bioavailability of orally ingested bilastin is 61%. Simultaneous food intake reduces the bioavailability of bilastin by 30%.Cumulation of the drug is not observed. Communication with plasma proteins - 84-90%.
Metabolism and excretion. Bilustin is metabolized slightly, after a single use up to 95% of bilastin from the accepted dose is excreted unchanged by the kidneys (28.3%) and with bile (66.5%). The half-life (T1 / 2) averages 14.5 hours.
In case of moderate renal failure (glomerular filtration rate (GFR) 30-50 ml / min / 1.73 m2) and severe severity (GFR <30 ml / min / 1.73 m2), the elastin elimination rate slows down, which can lead to to an increase in plasma concentration of bilastin. Changing the pharmacokinetic parameters does not affect the safety profile of bilastin, since the concentration of bilastin in the blood plasma in patients with renal insufficiency remains within acceptable limits.
In hepatic insufficiency, clinically significant changes in pharmacokinetic parameters of bilastin do not occur, since bilastin is slightly metabolized in the liver.
The pharmacokinetic parameters of bilastin in elderly patients are similar to those in young patients.

Indications

- Allergic (seasonal and year-round) rhinoconjunctivitis: elimination or relief of symptoms (sneezing, nasal congestion, itching of the nasal mucosa, rhinorrhea, burning sensation and itching in the eyes, redness of the eyes, tearing);
- urticaria: elimination or reduction of pruritus, rash.

Contraindications

- Hypersensitivity to bilastine or auxiliary components of the drug;
- age up to 12 years (efficacy and safety have not been established);
- pregnancy and breastfeeding period.

Side effects

Possible side effects are listed below in descending frequency of occurrence: very often (≥ 1/10), often (≥ 1/100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000, <1/1000), very rarely (<1/10000), including individual messages.
Disorders of the gastrointestinal tract
Infrequently: dryness of the oral mucosa, diarrhea, dyspepsia, gastritis, abdominal pain, pain in the upper abdomen, discomfort in the stomach, nausea.
Violations of the skin and subcutaneous tissues
Infrequently: pruritus.
Nervous system disorders
Often: drowsiness, headache;
Infrequently: dizziness.
Mental disorders
Infrequently: anxiety, insomnia.
Metabolic disorders
Infrequently: increase in appetite, increase in body weight.
Disturbances from an organ of hearing and labyrinth disturbances
Infrequently: tinnitus, vertigo.
Violations of the respiratory system, chest and mediastinum
Infrequently: shortness of breath, dry nasal mucosa, discomfort in the nose.
Violations of the cardiovascular system
Infrequently: blockade of the right leg of the bundle of His, sinus arrhythmia, lengthening of the QT interval on the electrocardiogram, other changes on the electrocardiogram.
Infectious and parasitic diseases
Infrequently: herpetic lesion of the oral cavity.
Other:
Infrequently: thirst, fatigue, asthenia, fever, an increase in plasma triglyceride concentration, an increase in plasma creatinine, an increase in liver enzyme activity (aspartate aminotransferase, alanine aminotransferase, gamma-glutamyl transferase).

Interaction

With the simultaneous use of bilastin with Ketoconazole or Erythromycin, the area under the concentration-time curve (AUC) of bilastin increased by 2 times, and the maximum concentration (Cmax) - by 2-3 times.
With the simultaneous use of bilastin at a dose of 20 mg and diltiazem at a dose of 60 mg Cmax of bilastine increased by 50%. Such effects can be explained by the interaction at the level of carrier proteins (including P-glycoprotein), which are responsible for removing drugs from intestinal cells, the substrate of which is bilastin. With the simultaneous use of bilastin and other drugs that are substrates or inhibitors of P-glycoprotein (for example, cyclosporine), the concentration of bilastin in the blood plasma may increase.
Grapefruit and other fruit juices reduce the bioavailability of bilastin by 30%. This interaction is due to the ability of fruits to suppress the activity of the carrier protein of organic anions OATP1A2, for which bilustin is a substrate. Drugs that are substrates or inhibitors of OATP1A2 (for example, ritonavir or rifampicin) can reduce the concentration of bilastin in the blood plasma.
Bilustin does not enhance the effect of ethanol on the central nervous system.
With the simultaneous use of bilastine and lorazepam enhance, the overwhelming effect of lorazepam on the central nervous system was not detected.

How to take, the course of administration and dosage

Inside
Unless otherwise prescribed by a doctor, the following doses of Nixar are recommended to relieve symptoms of allergic rhinoconjunctivitis and urticaria:
Adults and children over 12 years old: 1 pill of the drug Nixar, which corresponds to 20 mg of bilastin, once a day.
The maximum daily dose of bilastin is 20 mg, since increasing the dose does not lead to an increase in the therapeutic effect.
A pill is taken one hour before meals or 2 hours after a meal (or fruit juice).
In allergic rhinoconjunctivitis, the drug is used during the entire period of contact with allergens.
For urticaria, treatment is continued until the symptoms disappear or relieve.
In patients with impaired liver and kidney function, dose adjustment is not required.
Elderly patients dose adjustment is not required. Experience with the use of the drug Nixar® in persons over 65 years is insignificant.

Overdosage

Symptoms: when applying bilastina in a dose that exceeds the recommended 10-11 times, side effects occurred 2 times more often than when using placebo. The most common symptoms were dizziness, headache, nausea. No serious side effects, including significant lengthening of the QT interval, were noted.
Treatment: symptomatic and supportive therapy.There is no specific antidote.

Special notes

In patients with moderately severe renal failure (GFR 30-50 ml / min / 1.73 m2) and severe severity (GFR <30 ml / min / 1.73 m2), concurrent use with P-glycoprotein inhibitors may lead to an increase in bilastin concentration in blood plasma, which increases the risk of side effects. In this regard, in patients with moderate to severe renal failure, caution should be exercised with simultaneous use of bilastin with P-glycoprotein inhibitors (ketoconazole, erythromycin, cyclosporine, ritonavir, diltiazem, etc.).

Impact on the ability to drive trans. Wed and fur .:

In a study conducted to assess the effect of bilastin at a dose of 20 mg on the ability to drive vehicles, the negative effect of the drug was not identified. However, patients should be warned that in very rare cases, dizziness or drowsiness may occur, which in turn may affect the ability to drive vehicles or to perform other activities that require increased concentration of attention. When the described adverse events should refrain from performing these activities.