Pharmacodynamics. Bilastine is a long-acting antihistamine, does not cause sedation, selectively binds to peripheral h1-receptors and does not bind to m-cholinergic receptors.
After a single application of bilastine for 24 hours, it suppresses the development of skin reactions caused by histamine, with blisters and erythema.
In clinical trials involving patients with allergic rhinoconjunctivitis (seasonal and year-round), while using bilastine at a dose of 20 mg 1 time per day for 14-28 days, relief of symptoms such as sneezing, nasal discharge, itching was noted. in the nose, nasal congestion, itchy eyes, watery eyes and redness of the eyes. The therapeutic effect of bilastine persisted for 24 hours.
In clinical studies involving patients with chronic idiopathic urticaria, while using bilastine at a dose of 20 mg 1 time per day for 28 days, a decrease in the severity of itching and a decrease in the number and size of blisters were noted; in addition, the patients experienced less discomfort due to urticaria. The patients experienced improved sleep and well-being.
No clinically significant lengthening of the QT interval on the ECG, nor other disorders of the cardiovascular system were observed in the course of the clinical studies of bilastine.
Pharmacokinetics. Suction. After oral administration, bilastine is rapidly absorbed, and its Cmax in blood plasma is reached 1.3 hours after administration. No accumulation of the preparation in the body was detected. The average bioavailability for oral administration is 61%.
Distribution. According to in vitro and in vivo studies, bilastine is a substrate for P-glycoprotein and OATP carrier protein. Bilastine is obviously not a substrate for the BCRP transporter or the OST, OAT1 and OAT3 transporter. Data from in vitro studies do not suggest that bilastine inhibits the activity of carrier proteins such as P-gp, MRP2, BCRP, BSEP, OATP1B1, OATP1B3, OATP2B1, OAT1, OAT3, OCT1, OCT2, and NTCP in the systemic circulation, since it the ability to inhibit P-gp, OATP2B1 and OCT1 is insignificant and is characterized by an IC50 value of ≥300 μm, which significantly exceeds the calculated Cmax value in blood plasma in the case of its clinical use. Thus, these interactions are clinically insignificant. However, the results of similar studies indicate that inhibition by bilastine of carrier proteins found in the intestinal mucosa (for example, P-gp) cannot be ruled out. After application in therapeutic doses, bilastine binds to blood plasma proteins by 84–90%.
Biotransformation. During in vitro studies, bilastine did not show the ability to induce or suppress the activity of cytochrome P450 isoenzymes.
Excretion. According to a study conducted with the participation of volunteers, after a single use of 14C-bilastine at a dose of 20 mg, almost 95% of the administered dose ended up in the urine and feces (28.3 and 66.5%, respectively) in the form of unchanged bilastine, from which it can be concluded that in the human body, bilastine is metabolized slightly. On average, T½ of bilastine in healthy volunteers is 14.5 hours.
Linearity. In the dose range from 5 to 220 mg, the pharmacokinetic parameters of bilastine vary in direct proportion to the dose; however, they differ insignificantly in different healthy volunteers.
Symptomatic treatment for allergic rhinoconjunctivitis (seasonal and perennial) and urticaria.
Adults and children (over 12 years old). the recommended dose is 20 mg (1 tablet) once a day to relieve symptoms of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria.
The tablet should be taken orally 1 hour before or 2 hours after a meal or fruit juice.
Elderly patients. Elderly patients do not need dose adjustment. The experience of using the preparation in patients over the age of 65 is limited.
Impaired renal function. No dose adjustment is required in patients with impaired renal function.
Liver dysfunction. There is no experience of clinical use of the preparation in patients with impaired liver function. Since bilastine is not metabolized and is excreted mainly by the kidneys, impaired liver function should not lead to an increase in its systemic action to a dangerous level. Therefore, dose adjustment is not required for patients with impaired liver function.
Duration of treatment. For patients with allergic rhinitis, the preparation should be used only during contact with allergens. For people with seasonal allergic rhinitis, treatment can be stopped when symptoms have subsided and resumed when symptoms return. For patients with perennial allergic rhinitis, the preparation can be used continuously during the period of contact with allergens. In patients with urticaria, the duration of therapy depends on the nature and duration of the symptoms, as well as on their dynamics.
Hypersensitivity to the active substance (bilastine) or to any of the excipients.
In clinical studies in patients with allergic rhinoconjunctivitis or chronic idiopathic urticaria, side effects with the use of bilastine at a dose of 20 mg occurred with approximately the same frequency as with the use of placebo (12.7 and 12.8%). The results of the conducted studies indicate that when using bilastine at a dose of 20 mg, such adverse reactions as headache, drowsiness, dizziness and fatigue were most often noted. with approximately a similar frequency, these adverse events were detected in patients taking placebo.
The following are adverse reactions that have been recognized, or at least likely to be associated with bilastine, and have been reported in more than 0.1% of patients treated with bilastine 20 mg in the clinical development program.
By frequency, side effects are divided into the following categories: very often (≥1 / 10); often (≥1 / 100 and 1/10); sometimes (≥1 / 1000 and 1/100); rarely (≥1 / 10,000 and 1/1000); very rare (1/10 000), unknown (available data do not allow for an estimate).
Infections and parasitic diseases: sometimes - oral herpes.
Disorders of nutrition and metabolism: sometimes - increased appetite.
From the side of the psyche: sometimes - anxiety, insomnia.
On the part of the organ of hearing and balance: sometimes - tinnitus, dizziness.
From the side of the cardiovascular system: sometimes - blockade of the right bundle branch, sinus arrhythmia, prolongation of the Q – T interval on the ECG, other abnormalities on the ECG.
From the nervous system: often - drowsiness, headache; sometimes dizziness.
From the respiratory system: sometimes - shortness of breath, discomfort in the nose, dry nose.
From the digestive system: sometimes - pain in the upper abdomen, abdominal pain, nausea, abdominal discomfort, diarrhea, dry mouth, dyspepsia, gastritis.
On the part of the skin and subcutaneous tissue: sometimes itching.
General and local disorders: sometimes - fatigue, thirst, intensification of existing diseases, fever, asthenia.
Additional research methods: an increase in the activity of gamma-glutamyl transpeptidase, ALT, ASAT, an increase in the level of creatinine in the blood, an increase in the level of TG in the blood, an increase in body weight.
In patients with moderate or severe renal impairment, the use of bilastine simultaneously with p-glycoprotein inhibitors (ketoconazole, erythromycin, cyclosporin, ritonavir, diltiazem, etc.) can lead to an increase in the concentration of bilastine in the blood plasma and, therefore, to an increased risk of its side effects ... therefore, patients with moderate or severe impairment of renal function should not use bilastine concurrently with p-glycoprotein inhibitors.
Use during pregnancy and lactation. Fertility Clinical data are limited. Animal studies have not revealed a negative effect of the preparation on fertility.
Pregnancy. There are no data on the use of bilastine in pregnant women.
In the course of animal studies, no harmful effects of the preparation (direct or indirect) on reproductive function, childbirth or postnatal development were also noted. Taking into account the safety, the preparation Nixar should not be used during pregnancy.
Lactation. There is no data on whether bilastine passes into the breast milk of women. The release of bilastine with milk in animals has not been studied. The decision to extend or terminate breastfeeding, as well as to continue or discontinue Nixar therapy should be made taking into account the benefits of breastfeeding for the child, on the one hand, and the need for bilastine therapy for the mother, on the other.
Children. The safety and effectiveness of bilastine for children under 12 years of age has not been confirmed.
The ability to influence the reaction rate when driving or working with other mechanisms. According to a study of the effect of bilastine on the ability to drive vehicles, the use of bilastine at a dose of 20 mg does not affect the ability to drive vehicles. However, patients should be informed that in some cases the preparation may cause drowsiness and, thus, affect the ability to drive vehicles and operate machinery.
Interaction with food. food reduces the bioavailability of oral bilastine by 30%.
Interaction with grapefruit juice. In the case of the use of bilastine at a dose of 20 mg simultaneously with grapefruit juice, the bioavailability of bilastine decreased by 30%. A similar effect can be observed with other fruit juices. The degree of bioavailability reduction may differ depending on the manufacturer of the juice and the fruit from which it is derived. This interaction is due to the ability of fruit components to suppress the activity of the organic anion carrier protein OATP1A2, for which bilastine is a substrate. Preparations that are substrates or inhibitors of OATP1A2 (for example, ritonavir or rifampicin) can also reduce the concentration of bilastine in the blood plasma.
Interaction with ketoconazole or erythromycin. In the case of taking bilastine simultaneously with ketoconazole or erythromycin, the AUC of bilastine increased by 2 times, and Cmax - by 2–3 times. Such effects can be explained by the interaction at the level of carrier proteins responsible for the elimination of preparations from intestinal cells, since bilastine is a substrate of P-glycoprotein and is not metabolized. The safety profile of bilastine, on the one hand, and ketoconazole or erythromycin, on the other, are probably not affected by these effects. Other preparations that are substrates or inhibitors of P-glycoprotein (for example, cyclosporine) can also increase the concentration of bilastine in the blood plasma.
Interaction with diltiazem. In the case of taking bilastine at a dose of 20 mg simultaneously with diltiazem at a dose of 60 mg, the Cmax of bilastine increased by 50%. This effect can be explained by the interaction at the level of carrier proteins responsible for the elimination of preparations from intestinal cells; this effect probably does not affect the safety profile of bilastine.
Interaction with ethyl alcohol. After the simultaneous intake of alcohol and bilastine at a dose of 20 mg, psychomotor functions were at the same level as after the simultaneous intake of alcohol and placebo. Bilastine does not affect psychomotor functions when taken with ethyl alcohol.
Interaction with lorazepam. In the case of the use of bilastine at a dose of 20 mg simultaneously with lorazepam at a dose of 3 mg for 8 days, no increase in the inhibitory effect of lorazepam on the central nervous system was detected.
Data on acute overdose have been obtained only in clinical trials. against the background of the use of bilastine in doses 10–11 times higher than the therapeutic doses, side effects in healthy volunteers occurred 2 times more often than against the background of placebo. side effects that were more common included dizziness, headache, and nausea. serious adverse reactions and a significant increase in the duration of the q – tc interval were not observed. in a cross-sectional study measuring the q – t / q – tc intervals, in which the effect of repeated use of bilastine on ventricular repolarization was studied, no statistically significant lengthening of the q – tc interval was found.
Treatment. In case of overdose, symptomatic and supportive therapy is recommended. The specific antidote for bilastine is unknown.
Does not require special storage conditions.
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