- Available:In stock304
- Availability date:2020-07-30
- Dosage form:bottle
- In stock:304 Items
active ingredient: rupatadine fumarate;
1 ml contains rupatadine fumarate 1.28 mg in terms of rupatadine 1 mg;
excipients: sodium hydrophosphate anhydrous, citric acid anhydrous, methyl parahydroxybenzoate (E 218), propylene glycol, sucrose, sodium saccharin, banana flavor, purified water.
Dosage form. Oral solution.
Basic physical and chemical properties: clear, colorless or yellowish liquid with a banana smell.
Pharmacotherapeutic group. Other antihistamines for systemic use. ATX code R06A X28.
Rupatadine belongs to the second generation of antihistamines and is a long-acting histamine antagonist with selective peripheral antagonistic activity to H1 receptors. Some of its metabolites (Desloratadine and its hydroxylated metabolites) retain antihistamine activity and may partially contribute to the overall effectiveness of the drug.
Studies of rupatadine in vitro in high concentrations showed inhibition of mast cell degranulation caused by immunological and non-immunological stimuli, as well as the release of cytokines, in particular TNF, from human mast cells and monocytes. The clinical significance of the observed experimental data has yet to be confirmed.
Pharmacodynamic effect (reduction of the area with blisters, antihistamine effect) was also observed 4 weeks after treatment.
Since rupatadine has the ability to block the release of histamine and other inflammatory mediators, it is expected to be effective in treating the symptoms of other types of urticaria, in addition to Chronic Spontaneous Urticaria.
Rupatadine is rapidly absorbed after an average dose of 5 mg with an average Tmax of 0.5 hours after administration. The average Cmax was 2.5 ng/mL after a single oral dose. In terms of exposure, the average total area under the curve (AUC) was 8.86 ng•H/ML. All these values are similar to those obtained in adults and adolescents.
The average Half-Life of rupatadine in children was 3.12 hours, which is less than for tablets taken by adults and adolescents.
Effect of food intake
Studies of the interaction of food with an oral solution of rupatadine have not been conducted. Studies of the effects of food intake were conducted in adults and adolescents using rupatadine in 10 mg tablets. Food intake increases the systemic effects of rupatadine on the body (AUC) by approximately 23 %. The maximum concentration in blood plasma (Cmax) as a result of food intake does not change. These differences are not clinically relevant.
Metabolism and elimination
In the adult excretion study, 34.6% of rupatadine administered is excreted in the urine, and 60.9% in feces collected in 7 days. Rupatadine undergoes significant presystemic metabolism when administered orally. Unchanged active substance is found in the urine and feces only in small amounts. This means that rupatadine is almost completely metabolized. Overall, the active metabolites of Desloratadine and other hydroxylated derivatives accounted for 27% and 48% of the total systemic exposure to active substances, respectively. In vitro studies of metabolism in human liver microsomes have shown that rupatadine is metabolized mainly with the participation of cytochrome P450 (CYP 3A4).
Symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) and urticaria in children aged 2 to 11 years.
Hypersensitivity to rupatadine or to any other component of the drug.
Interactions with other drugs and other types of interactions.
Studies of the interaction of rupatadine in the form of an oral solution in children have not been conducted.
Interaction studies were conducted only in adults and adolescents (over 12 years of age) using rupatadine in the form of 10 mg tablets.
Effect of other medications on rupatadine
Co-administration with potent CYP3A4 inhibitors (including itraconazole, ketoconazole, voriconazole, posaconazole, HIV protease inhibitors, clarithromycin, nefazodone) should be avoided. Caution should be exercised when co-administered with moderate CYP3A4 inhibitors (erythromycin, flucanozol, diltiazem).
Co – administration of rupatadine at a dose of 20 mg and ketoconazole or erythromycin increases the systemic effect of rupatadine by 10 times and the latter-by 2-3 times. These combinations are not accompanied by changes in the QT interval or an increase in the frequency of adverse reactions compared to the individual use of these drugs.
Interaction with grapefruit
Simultaneous administration of rupatadine in tablets of 10 mg and grapefruit juice increases the overall effect of rupatadine by 3.5 times. This is because grapefruit juice contains one or more components that inhibit CYP3A4 and can increase the plasma concentration of drugs that are metabolized by CYP3A4, such as rupatadine. In addition, it has been suggested that grapefruit may affect the intestinal transport systems of drugs such as glycoprotein-P. Do not use grapefruit juice at the same time as taking the drug.
Effect of rupatadine on other medications
Caution should be exercised when prescribing rupatadine concomitantly with other drugs that are metabolized and have a narrow therapeutic index, since data on the effect of rupatadine on other drugs are limited.
Interaction with alcohol
After taking alcohol, a dose of rupatadine 10 mg slightly affects the results of some tests for psychomotor performance, which does not significantly differ from the effect of taking only one alcohol. A dose of 20 mg increased the changes caused by alcohol intake.
Interaction with CNS depressants
As with other antihistamines, interactions with CNS depressants cannot be excluded.
Interaction with statins
Asymptomatic increases in creatine phosphokinase have sometimes been reported during clinical trials of rupatadine. The risk of interaction with statins (some of which are also metabolized by the cytochrome P450 CYP3A4 isoenzyme) is unknown. Therefore, rupatadine should be used with caution when co-administered with statins.
The combination of rupatadine with potent CYP3A4 inhibitors should be avoided, and caution should be exercised when prescribing with moderate CYP3A4 inhibitors.
It may be necessary to adjust the dose of sensitive CYP3A4 substrates (for example, simvastatin, lovastatin) and CYP3A4 substrates with a narrow therapeutic index (for example, cyclosporine, tacrolimus, sirolimus, everolimus, cisapride), since rupatadine may increase the concentration of these drugs in blood plasma.
The effect of rupatadine in 10 mg tablets on cardiac function was evaluated in the adult Thorough QT/QTc study, in which rupatadine at a dose exceeding the therapeutic dose by 10 times did not affect the ECG and thus did not cause caution regarding cardiac safety. However, rupatadine should be used with caution in patients with prolonged QT interval, patients with unadjusted hypokalemia, patients with persistent proarrhythmic conditions, such as clinically significant bradycardia, acute myocardial ischemia.
Increased creatine phosphokinase, alanine aminotransferase, and aspartate aminotransferase levels have been reported, as well as changes in liver function tests as infrequent side effects of rupatadine in 10 mg tablets in adults.
Concomitant administration of rupatadine with grapefruit juice is not recommended.
Patients with renal or hepatic insufficiency: due to the lack of clinical experience, the use of the drug in patients with impaired renal or hepatic function is not recommended.
Children: the safety and efficacy of rupatadine in children under 2 years of age have not been established.
This medicine contains sodium saccharin, so it can be harmful to the teeth. Patients with rare hereditary forms of fructose intolerance, glucose-galactose malabsorption syndrome, or sucrose-isomaltase deficiency should not take this medication.
The drug contains methyl parahydroxybenzoate, which can cause allergic reactions (possibly delayed).
Use during pregnancy or lactation.
The drug is used for children.
Data on a limited number (2) of pregnancies during which rupatadine was taken indicate that there are no side effects of rupatadine on pregnancy or fetal/newborn health. Currently, there are no other relevant epidemiological data. Animal studies have not found any direct or indirect harmful effects on pregnancy, embryo/fetus development, delivery, or postnatal development. As a precautionary measure, it is recommended to avoid using the drug during pregnancy.
Rupatadine penetrates into animal milk. It is not known whether rupatadine passes into a woman's breast milk. The decision to discontinue breast-feeding or discontinue/abstain from rupatadine therapy should be made taking into account the benefits of breast-feeding for the child and the benefits of treatment for the mother.
There are no clinical data on the effect of the drug on fertility. Animal studies have shown a significant reduction in fertility at exposure levels higher than in humans at the maximum therapeutic dose.
Ability to influence the reaction rate when driving vehicles or other mechanisms.
The drug is used for children.
Rupatadine at a dose of 10 mg had no effect on the ability to drive a car and work with other mechanisms in the conducted clinical studies. However, the patient should first assess their own response to treatment with the drug before driving a car or working with other mechanisms.
Dosage and administration.
To ensure accurate dosing, the package contains a syringe dispenser.
Insert a syringe dispenser into the neck of the bottle and measure the required amount of solution, taking into account the age and body weight of the child.
Please note that if the bottle contains an adapter placed in the neck, then insert the dispenser syringe tightly into the adapter neck and turn the bottle upside down, gently pull the plunger, drawing the liquid into the dispenser syringe to the desired mark. After collecting the required amount of solution, turn the bottle to its original position and carefully remove the syringe dispenser from the bottle.
After use, wash the parts of the dispenser syringe with warm water.
Children from 2 to 11 years old
With a body weight of 10 kg or more, but less than 25 kg: 2.5 ml (2.5 mg rupatadine) of Oral Solution 1 time a day, regardless of food intake.
With a body weight of 25 kg or more: 5 ml (5 mg of rupatadine) of Oral Solution 1 time a day, regardless of food intake.
The drug should be used in children aged 2 to 11 years.
Since there is insufficient data on the use of the drug in children under 2 years of age, it is not recommended to use it in this age category.
No cases of drug overdose have been reported in adults and children. In a clinical safety study, rupatadine was well tolerated at a daily dose of 100 mg for 6 days. The most common adverse reaction was drowsiness. In case of accidental ingestion of very high doses, symptomatic treatment should be carried out and the necessary maintenance measures should be taken.
The frequency of adverse reactions is determined as follows: often (≥ 1/100 1/1000 .
From the blood and lymphatic system: infrequently – eosinophilia, neutropenia.
From the nervous system: often – headache, drowsiness; infrequently – dizziness.
From the gastrointestinal tract: infrequently-nausea.
From the skin and connective tissue: infrequently – eczema, night sweats.
Infections and infestations: infrequently – flu, nasopharyngitis, upper respiratory tract infections.
Common disorders: infrequently-fatigue.
Expiration date. 2 years.
Shelf life after the first opening of the bottle is 12 months.
Do not use after the expiration date indicated on the package.