Rupatadine

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[edit] BRAND NAMES

[edit] STRUCTURE

Rupatadine.jpg

[edit] MECHANISM OF ACTION

Rupatadine is long-acting tricyclic second generation (non-sedating) antihistamine. It acts as an antagonist at peripheral histamine (H1) receptors. Some of its metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug. Histamine is a substance that causes allergic symptoms. When histamine (H1) receptors are blocked, histamine cannot have its effect, and this leads to a decrease in the symptoms of allergy.

Rupatadine also, antagonizes the platelet-activating factor (PAF). PAF is considered an important mediator in allergic and inflammatory reactions.

As with other second-generation antihistamines, does not easily cross the blood-brain barrier and is believed to be non-sedating at therapeutic doses.

[edit] INDICATIONS

  • Chronic Idiopathic Urticaria
  • Seasonal and perennial allergic rhinitis to relief symptoms such as sneezing, rhinorrhea and nasal pruritus, occular pruritus and tearing.

[edit] DOSAGE

  • Adults and adolescents 12 Years of Age and Over: 10 mg once daily with or without food.

[edit] CONTRAINDICATIONS

Hypersensitivity to Rupatadine.

[edit] WARNINGS AND PRECAUTIONS

[edit] INTERACTIONS

  • Grapefruit juice (A CYP3A4 inhibitor) : The administration of rupatadine with grapefruit juice is not recommended. (The concomitant administration of grapefruit juice increased 3.5 times the systemic exposure of rupatadine)
  • CYP3A4 inhibitors like ketoconazole, itraconazole, nefazodone and macrolide antibiotics (e.g. erythromycin, clarithromycin), increase the systemic exposure to rupatadine. (Use with caution)

[edit] PREGNANCY AND LACTATION

  • Pregnancy: Data on a limited number (2) exposed pregnancies indicate no adverse effects of rupatadine on pregnancy or on the health of the foetus/newborn child. To date, no other relevant epidemiological data are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Caution should be exercised when prescribing rupatadine to pregnant women.
  • Lactation: Rupatadine is excreted in animal milk. It is unknown whether rupatadine is excreted into breast milk. Due to the lack of human data, caution should be exercised when prescribing rupatadine to lactating women.

[edit] SIDE EFFECTS

Most common adverse reactions are somnolence (9.5%), headache (6.9%), fatigue (3.2%) and dry mouth.

Uncommon (1/1000 to < 1/100): Abnormal liver function test, disturbance in attention, epistaxis, nasal dryness, pharyngitis, cough, dry throat, nausea, abdominal pain upper, diarrhea, rash, back pain, myalgia, increased appetite.

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[edit] REFERENCES