Buy Rupafin pills 10 mg, 7 pcs
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Rupafin® [Rupatadine Fumarate]

H. Uriyah
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Clinical Pharmacology

Rupatadin belongs to the second generation of antihistamines and is a long-term and selectively acting peripheral blocker H1- histamine receptors. Some of its metabolites (desloratadine and 3-hydroxydelosloratadine) retain antihistamine activity and may contribute to the overall effectiveness of the drug Rupafin.
Rupatadin shows high affinity for H1- histamine receptors. In vitro rupatadine studies in high concentrations showed suppression of mast cell degranulation caused by immunological and non-immunological stimuli, suppression of chemotaxis of eosinophils and neutrophils, as well as release of cytokines (interleukin (IL) -5, IL-6, IL-8, GM-CSF (granulocyte-macrophage colloid, colloidal macrophage). factor)), in particular TNF-α (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 rupatadine selectivity for peripheral N1- histamine receptors, it does not significantly affect the activity of the central nervous system in doses of 10 or 20 mg / day.

Indications

Symptomatic treatment in adults and adolescents over 12 years old:

  • allergic rhinitis;
  • chronic idiopathic urticaria.

Composition

1 tablet contains rupatadina 10 mg.

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Rupafin® [Rupatadine Fumarate]

Dosage and Administration

Rupafin is taken orally, regardless of the meal. In adults and children over 12 years old, the recommended dose is 10 mg (1 tablet) 1 time / day.

Adverse reactions

Most often, patients receiving rupatadine reported adverse reactions to the drug, such as drowsiness, headache, and fatigue, occurring in 9.5%, 6.9%, and 3.2% of patients, respectively. In most cases, drug withdrawal was not required.

Classification of adverse reactions according to the frequency of development (number of registered cases / number of patients): very often - more than 1/10 of cases, often from 1/10 to 1/100 cases, infrequently - from 1/100 to 1/1000 cases.

From the nervous system: often - drowsiness, headache, dizziness, fatigue,asthenia; infrequently - decreased concentration, irritability.

On the part of the respiratory system: infrequently - nasal bleeding, dry nasal mucosa, pharyngitis, cough, dry throat, pain in the throat and larynx, rhinitis.

From the digestive system: often - dry mouth; infrequently - nausea, diarrhea, dyspepsia, vomiting, abdominal pain, constipation.

Metabolism and nutrition: Infrequently - increased appetite.

Skin and Subcutaneous Tissues: infrequently - rash.

From the musculoskeletal system: infrequently - back pain, arthralgia, myalgia.

On the part of the body as a whole: infrequently - thirst, malaise, fever, weight gain.

Changes in laboratory parameters: infrequently - increase in KFK, ALT, AST, change of indicators of functional hepatic tests.

Contraindications

WITHcaution should be prescribed to patients with an extended QT interval, uncorrected 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

Drug interactions

Interaction with ketoconazole and erythromycin

The combined use of rupatadine in a dose of 20 mg and ketoconazole or erythromycin enhances the systemic effects of rupatadine 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 with the separate use of these drugs.

However, rupatadine should be used with caution in conjunction with these drugs and other inhibitors of the CYP3A4 isoenzyme.

Interaction with grapefruit juice

The simultaneous intake of rupatadine and grapefruit juice 3.5 times enhances the overall effect of rupatadine. Do not eat grapefruit juice at the same time as taking the drug.

Interaction with ethanol

With simultaneous use with ethanol, rupatadine in a dose of 10 mg does not cause a more pronounced change in cognitive, psychomotor activity compared with ethanol alone. Rupatadin, taken in a dose of 20 mg, enhances the changes caused by the intake of ethanol.

Interaction with drugs that inhibit the central nervous system

We can not exclude the possibility of the interaction of rupatadine with other antihistamines and means of oppressive central nervous system.

Interaction with statins

Due to the fact that some of the statins, as well as rupatadin, are metabolized by the CYP3A4 isoenzyme of cytochrome P450, it is impossible to exclude the possibility of increasing the level of CPK in their combined use. For these reasons, rupatadine should be used with caution along with statins.

Overdosage

The literature does not describe cases of drug overdose. In a study on the clinical safety of rupatadine well tolerated at a daily dose of 100 mg for 6 days.
Symptoms: the most common adverse reaction is drowsiness.
Treatment: in case of accidental ingestion of the drug in very high doses, it is shown to cause vomiting in a patient followed by administration of Activated charcoal.If this manipulation is impossible or ineffective, it is necessary to wash the stomach with isotonic sodium chloride solution.

  • Brand name: Rupafin
  • Active ingredient: Rupatadine Fumarate
  • Dosage form: Pills.
  • Manufacturer: H. Uriyah
  • Country of Origin: Spain

Studies and clinical trials of Rupatadine Fumarate (Click to expand)

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