Rupatadine: pharmacological profile and its use in the treatment of allergic rhinitis

Abstract

Keywords:Rupatadine is a once-daily, non-sedating, selective and long-acting new drug with a strong antagonist activity towards both histamine H1 receptors and plateletactivating factor receptors. The use of rupatadine is indicated in adult and adolescent patients (> 12 years of age) suffering from intermittent and persistent allergic rhinitis. In the treatment of these conditions, rupatadine is at least as effective as ebastine, cetirizine, loratadine and desloratadine. Avery good safety profile of rupatadine has been evidenced in various studies, including a long-term (1-year) safety study. Rupatadine does not present drug-drug interactions with azithromycin, fluoxetine and lorazepam, but should not be administered concomitantly with known CYP3A4 inhibitors.antihistamine, platelet-activating factor, rhinitis, rupatadine.

Cardiac Safety of Rupatadine in a Single‐Ascending‐Dose and Multiple‐Ascending‐Dose Study in Healthy Japanese Subjects, Using Intensive Electrocardiogram Assessments—Comparison With the Previous White Caucasian Thorough QT Study

“…18 The concomitant administration of rupatadine with potent CYP3A4 inhibitors (like ketoconazole and erythromycin) should be avoided, and comedication with moderate CYP3A4 inhibitors should be used with caution. 19 On the other side, no clinically relevant modifications in mean pharmacokinetic parameters of rupatadine and active metabolites were observed when azithromycin at therapeutic doses was coadministered. 20 Finally, rupatadine 10 mg did not appear to increase the depressant effect of alcohol (0.8 g/kg) after a single dose, both on subjective and objective measurements of psychomotor performance, including quantitative electroencephalography.…”

“…In vitro metabolism studies in human liver microsomes indicate that rupatadine is mainly metabolized by cytochrome P450 (CYP) 3A4, and a genetic polymorphism in its biotransformation is unlikely . The concomitant administration of rupatadine with potent CYP3A4 inhibitors (like ketoconazole and erythromycin) should be avoided, and comedication with moderate CYP3A4 inhibitors should be used with caution . On the other side, no clinically relevant modifications in mean pharmacokinetic parameters of rupatadine and active metabolites were observed when azithromycin at therapeutic doses was coadministered .…”

Development of a highly sensitive LC–MS/MS method for simultaneous determination of rupatadine and its two active metabolites in human plasma: Application to a clinical pharmacokinetic study

“…A c c e p t e d M a n u s c r i p t 8 The developed LC-MS/MS method was used for a pharmacokinetic study in volunteers who received single and multiple oral doses of RTFT. The mean plasma 120 concentrations of RT, DT and 3-OH-DT were illustrated in Fig.…”

“…It is extensively metabolized by P450 3A4 [2,8], and the major metabolites of RT are desloratadine (DT) and 28 3-hydroxydesloratadine (3-OH-DT), which are active and contribute to the overall efficacy of the drug [4,9,10]. It is essential to evaluate the potential effect of the 29 main metabolites and their back-conversion to the parent drug during analysis.…”

Therapeutic Targeting of Eosinophil Adhesion and Accumulation in Allergic Conjunctivitis

“…Rupatadine is a selective and long-acting new drug with a strong antagonistic activity toward both histamine H1 receptors and platelet-activating factor receptors. It showed potent anti-allergic activity in vitro , including inhibition of mast cell degranulation and eosinophil chemotaxis, and in vivo (Sudhakara et al, 2009); moreover, rupatadine can inhibit CD18 and CD11b (Barron et al, 2004). …”