Rupatadine: a new selective histamine H1 receptor and platelet-activating factor (PAF) antagonist. A review of pharmacological profile and clinical management of allergic rhinitis

Drugs Today (Barc). 2003 Jun;39(6):451-68. doi: 10.1358/dot.2003.39.6.799450.


Rupatadine is a new agent for the management of diseases with allergic inflammatory conditions, such as seasonal and perennial rhinitis. The pharmacological profile of rupatadine offers particular benefits in terms of a strong antagonist activity towards both histamine H1 receptors and platelet-activating factor (PAF) receptors. Rupatadine has a rapid onset of action, and its long-lasting effect (>24 h) permits once-daily dosing. Rupatadine should not be used in combination with the cytochrome P450 inhibitors, such as erythromycin or ketoconazole, due to an increase in AUC and Cmax for rupatadine, although no clinically relevant adverse events have been reported. In addition, rupatadine, at the recommended dose of 10 mg, has been shown to be free of sedative effects and not to cause significant changes in the corrected QT interval in special populations, including the elderly, nor when coadministered with erythromycin or ketoconazole. Preclinical data have also shown that rupatadine and its main active metabolites did not interfere with cloned human HERG channel and did not affect in vitro isolated dog Purkinje fibers at concentrations at least 2000 times greater than those obtained with therapeutic doses in humans. Rupatadine is clinically effective in relieving symptoms in patients with seasonal and perennial allergic rhinitis. Newly published data on its efficacy and safety suggest that this compound may improve the nasal and non-nasal symptoms in comparison to other currently available second generation H1 receptor antihistamines.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Cyproheptadine / adverse effects
  • Cyproheptadine / analogs & derivatives*
  • Cyproheptadine / pharmacokinetics
  • Cyproheptadine / therapeutic use*
  • Dose-Response Relationship, Drug
  • Histamine H1 Antagonists / adverse effects
  • Histamine H1 Antagonists / pharmacokinetics
  • Histamine H1 Antagonists / therapeutic use*
  • Humans
  • Platelet Activating Factor / antagonists & inhibitors*
  • Rhinitis, Allergic, Perennial / drug therapy*
  • Rhinitis, Allergic, Seasonal / drug therapy*


  • Histamine H1 Antagonists
  • Platelet Activating Factor
  • rupatadine
  • Cyproheptadine