Rupafin - instructions for use, reviews, analogs and formulations (10 mg tablets) of an antihistamine drug for the treatment of urticaria, rhinitis and other manifestations of allergies in adults, children and pregnancy. Composition and alcohol
In this article, you can read the instructions for using an antihistamine drug Rupafin. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Rupafin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Rupafin in the presence of existing structural analogues.Use for the treatment of urticaria, rhinitis and other manifestations of allergy in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.
Rupafin - refers to the second generation of antihistamines and is a long-term and selectively acting blocker of peripheral H1-histamine receptors. Some of its metabolites (desloratadine and 3-hydroxydesloratedadine) retain antihistamine activity and can contribute to the overall effectiveness of the drug.
Rupatadine (the active substance of the drug Rupafin) shows a high affinity for H1-histamine receptors. Studies of rupatadine in high concentrations showed inhibition of degranulation of mast cells caused by immunological and non-immunological stimuli, inhibition of the chemotaxis of eosinophils and neutrophils, and the release of cytokines (interleukin (IL) -5, IL-6, IL-8, GM-CSF (granulocyte- macrophage colony-stimulating factor), in particular TNF-alpha (tumor necrosis factor-alpha) from mast cells and human monocytes. In addition, rupatadine caused a dose-dependent suppression of the expression of neutrophil adhesion molecules.
Due to the selectivity of rupatadine against peripheral H1-histamine receptors, it has no significant effect on the activity of the central nervous system at doses of 10 or 20 mg per day.
Since the release of histamine is a key link in the pathogenesis of all urticaria, it is expected that when Rupafin is prescribed in accordance with clinical recommendations, it can effectively reduce the severity of the symptoms of not only chronic idiopathic, but also other hives.
Composition
Rupatadine fumarate + excipients.
Pharmacokinetics
Rupafin is rapidly absorbed after oral administration. The pharmacokinetics of rupatadine is linear for doses of 10 to 40 mg. The binding ratio of rupatadine to plasma proteins is 98.5-99%. Since rupatadine has never been used intravenously in humans, there is no data on its absolute bioavailability. Eating a meal increases the overall effect of rupatadine on the body. The effect on one of its active metabolites and on the basic inactive metabolite is practically the same (a decrease of about 5% and 3%, respectively). Rupatadine undergoes significant pre-systemic metabolism when ingested.Unchanged active substance is found in urine and in feces only in small amounts. This means that rupatadine is almost completely metabolized. In the study of human excretion (40 mg of 14C-rupatadine), 34.6% of the drug was excreted by the kidneys, and 60.9% by the intestine within 7 days.
Indications
Symptomatic treatment in adults and adolescents over 12 years of age:
- allergic rhinitis;
- Pollinosis;
- hives.
Forms of release
Tablets 10 mg.
Other dosage forms, be it drops, capsules or ointment, do not exist.
Instructions for use and dosing regimen
Inside, regardless of food intake.
In adults and children over 12 years, the recommended dose is 10 mg (1 tablet) 1 time per day.
Side effect
- drowsiness;
- headache;
- dizziness;
- fatigue;
- asthenia;
- decreased concentration of attention;
- irritability;
- nose bleed;
- dryness of the nasal mucosa;
- pharyngitis;
- cough;
- dryness in the throat;
- pain in the pharynx and in the larynx;
- rhinitis;
- dry mouth;
- nausea, vomiting;
- constipation, diarrhea;
- dyspepsia;
- stomach ache;
- increased appetite;
- rash;
- backache;
- arthralgia;
- myalgia;
- thirst;
- malaise;
- fever;
- increase in body weight.
Contraindications
- kidney failure;
- liver failure;
- pregnancy;
- lactation period;
- children under 12 years of age (efficacy and safety not established);
- rare hereditary intolerance to galactose, lactase deficiency or glucose-galactose insufficiency insufficiency syndrome;
- hypersensitivity to the components of the drug.
Application in pregnancy and lactation
The drug Rupafin is contraindicated in pregnancy and lactation.
Use in children
Contraindicated in children under 12 years of age (efficacy and safety not established).
Application in elderly patients
Caution should be given to elderly patients (65 years and older).
Since the results for rupatadine and its metabolites were not clinically significant, it was concluded that when the drug is administered to elderly patients, a dose adjustment of 10 mg is not required.
special instructions
Caution should be given to patients with prolonged QT interval, unadjusted hypokalemia, persistent proarrhythmic conditions such as clinically significant bradycardia,acute myocardial ischemia; elderly patients (65 years and older); simultaneously with statins, simultaneously with grapefruit juice.
Impact on the ability to drive vehicles and manage mechanisms
When applying the drug at a dose of 10 mg, there was no effect on the ability to drive and other mechanisms. At the same time, there are reports of drowsiness, noted during treatment with Rupafin. In this regard, it is recommended to be cautious when driving a car or engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions until an individual patient's reaction to rupatadine is established.
Drug Interactions
Interaction with Ketoconazole and erythromycin
Joint application of Rupafin in a dose of 20 mg and ketoconazole or Erythromycin increases systemic exposure to rupatadine 10 times and the last - 2-3 times. These combinations are not accompanied by changes in the QT interval or an increase in the incidence of adverse reactions compared with the separate use of these drugs.
However, rupatadine should be used with caution in conjunction with these drugs and with other inhibitors of the CYP3A4 isoenzyme.
Interaction with grapefruit juice
Simultaneous reception of rupatadine and grapefruit juice 3.5 times strengthens the general action of rupatadine. Do not take grapefruit juice while taking the drug.
Interaction with ethanol
With simultaneous use with ethanol (alcohol), Rupafin 10 mg does not cause a more pronounced change in cognitive, psychomotor activity compared with the intake of ethanol alone. Rupatadine, taken in a dose of 20 mg, enhances the changes caused by the intake of ethanol.
Interaction with drugs that depress the central nervous system
It is impossible to exclude the possibility of Rufafin's interaction with other antihistamines and CNS depressants.
Interaction with statins
Due to the fact that some of the statins, as well as rupatadine, are metabolized by the cytochrome P450 isoenzyme CYP3A4, it is impossible to exclude the possibility of increasing the level of CKD when they are used together. For these reasons, rupatadine should be used with caution at the same time as statins.
Analogues of medicinal product Rupafin
Rupafin does not have structural analogs for the active substance.
Analogues for the pharmacological group (antihistamines):
- Allergodyl;
- Astemizole;
- Vibrocil;
- Histaglobin;
- Histalong;
- Histafen;
- Gifast;
- Desloratadine;
- Diazoline;
- Diphenhydramine;
- Donormil;
- Zirtek;
- Zodak;
- Kestin;
- Claritin;
- Clemastine;
- Cold storage;
- Levocetirizine;
- Lomilan;
- Loratadine;
- Mebhydrogen;
- Parliamentary;
- Pipolphen;
- Suprastin;
- Suprastinex;
- Tavegil;
- Telfast;
- Fexofenadine;
- Femizol;
- Pheniramine maleate;
- Fenistil;
- Fenkarol;
- Chloropyramine;
- Cetirizine;
- Cetrin;
- Ezlor;
- Erespal;
- Erius;
- Erolin.
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