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antiallergic agent - H1-histamine receptor blockerBilustin 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 lasts 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.
Suction. After oral administration, 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%. A simultaneous meal 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) of 30-50 ml / min / 1.73 m2) and severe severity (GFR <30 ml="" min="" 1="" 73="" m2="" the="" elimination="" rate="" of="" bilastin="" slows="" down="" which="" can="" lead="" to="" an="" increase="" in="" plasma="" concentration="" changing="" pharmacokinetic="" parameters="" does="" not="" affect="" safety="" profile="" since="" blood="" patients="" with="" renal="" insufficiency="" remains="" within="" acceptable="" limits="" br="">In hepatic insufficiency, clinically significant changes in pharmacokinetic parameters of bilastin do not occur, since bilastin is slightly metabolized in the liver.
Pharmacokinetic parameters of bilastin in elderly patients are similar to those in young patients.
- 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.
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.
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Dosage and Administration
For oral use.
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 tablet 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 older than 65 years is insignificant.
Possible side effects are listed below in descending frequency of occurrence: very often (≥ 1/10), often (≥ 1/100, 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 tissue
Nervous system disorders
Often: drowsiness, headache;
Infrequently: anxiety, insomnia.
Infrequently: increase in appetite, increase in body weight.
Disturbances from an organ of hearing and labyrinth disturbances
Infrequently: tinnitus, vertigo.
Disorders of the respiratory system, organs of the 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 His bundle, 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.
Infrequently: thirst, fatigue, asthenia, fever, an increase in plasma triglyceride concentration, an increase in plasma creatinine, increased activity of liver enzymes (aspartate aminotransferase, alanine aminotransferase, gamma-glutamyl transferase).
- 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.
With 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 simultaneous use of bilastin at a dose of 20 mg and diltiazem at a dose of 60 mg C max of bilastin increased by 50%. Such effects can be explained by the interaction at the level of carrier proteins (including the P-glycoprotein), which are responsible for the removal of 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 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 bilastin and lorazepam enhance, the overwhelming effect of lorazepam on the central nervous system was not detected.
Pregnancy and Lactation
The use of the drug Nixar during pregnancy is contraindicated due to the lack of clinical data on the safety of use in pregnant women.
In connection with the lack of data on the penetration of bilastin into breast milk, if necessary, the use of the drug Nixar during breastfeeding, at the time of admission, breastfeeding should be stopped.
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="" simultaneous="" use="" of="" p-glycoprotein="" with="" inhibitors="" may="" lead="" to="" an="" increase="" in="" bilastin="" concentration="" blood="" plasma="" which="" increases="" the="" risk="" side="" effects="" this="" regard="" patients="" moderate="" severe="" renal="" insufficiency="" caution="" should="" be="" exercised="" ketoconazole="" erythromycin="" cyclosporine="" ritonavir="" diltiazem="" etc="" p="">
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 high concentration of attention. When the described adverse events should refrain from performing these types of activities.
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 a significant lengthening of the QT interval, were noted.
Treatment: symptomatic and supportive therapy. There is no specific antidote.
- Brand name: Nixar
- Active ingredient: Bilastine
- Manufacturer: Faes Pharma S.A.
- Country of Origin: Spain
Studies and clinical trials of Bilastine (Click to expand)
- ChemInform Abstract: Alternative Synthesis of Bilastine.
- The effects of bilastine compared with cetirizine, fexofenadine, and placebo on allergen-induced nasal and ocular symptoms in patients exposed to aeroallergen in the Vienna Challenge Chamber
- Comparative inhibition by bilastine and cetirizine of histamine-induced wheal and flare responses in humans
- Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo for the symptomatic treatment of seasonal allergic rhinitis: a randomized, double-blind, parallel-group study
- Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients
- Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study
- Bilastine in allergic rhinoconjunctivitis and urticaria
- Bilastine: Environmental risk assessment
- Bilastine: Impurities safety profile
- Bilastine. Preclinical toxicology review
- Oncogenicity risk assessment of bilastine: A novel antihistamine compound
- Toxicokinetics of bilastine in animals: The effects of the dose and route of administration
- Pharmacokinetic-Pharmacodynamic Modelling of the Antihistaminic (H1) Effect of Bilastine
- Effects of Bilastine on T-wave Morphology and the QTc Interval
- Bilastine for the treatment of urticaria
- Integration of preclinical and clinical knowledge to predict intravenous PK in human: Bilastine case study
- Evaluation of the Single-dose Pharmacokinetics of Bilastine in Subjects with Various Degrees of Renal Insufficiency
- Bilastine: a guide to its use in the treatment of symptomatic allergic rhinoconjunctivitis and urticaria
- Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo in the treatment of perennial allergic rhinitis
- Alternative Synthesis of Bilastine
- An overview of the novel H1-antihistamine bilastine in allergic rhinitis and urticaria