Rupatadine: global safety evaluation in allergic rhinitis and urticaria

Expert Opin Drug Saf. 2016 Oct;15(10):1439-48. doi: 10.1080/14740338.2016.1221399. Epub 2016 Aug 19.


Introduction: Rupatadine is a second-generation H1-antihistamine with dual affinity for histamine H1 and PAF receptors. Rupatadine is indicated for the treatment of allergic rhinitis and urticaria.

Areas covered: A Medline search was conducted to identify preclinical and clinical studies of rupatadine. This was supplemented with additional articles obtained from online sources. The focus of this review is on the safety profile of rupatadine.

Expert opinion: The review of these data indicates that rupatadine is highly selective for histamine H1-receptors, exhibits additional PAF antagonism in in vitro and in vivo studies, does not cross the blood-brain barrier, and has similar adverse events comparable with other second-generation antihistamines. Rupatadine is a safe and well tolerated drug in patients over 2 years old, with no central nervous system or cardiovascular effects and it can be taken with or without foods.

Keywords: H1-antihistamine; H1-receptor antagonist; PAF antagonist; Rupatadine; allergic rhinitis; chronic spontaneous urticaria; intermittent; perennial; persistent; pharmacodynamics; pharmacokinetics; safety; seasonal; second-generation antihistamine; therapeutic use; urticaria.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Animals
  • Anti-Allergic Agents / adverse effects
  • Anti-Allergic Agents / pharmacokinetics
  • Anti-Allergic Agents / therapeutic use
  • Blood-Brain Barrier / metabolism
  • Cyproheptadine / adverse effects
  • Cyproheptadine / analogs & derivatives*
  • Cyproheptadine / pharmacokinetics
  • Cyproheptadine / therapeutic use
  • Histamine H1 Antagonists / adverse effects
  • Histamine H1 Antagonists / pharmacokinetics
  • Histamine H1 Antagonists / therapeutic use
  • Humans
  • Platelet Activating Factor / antagonists & inhibitors
  • Rhinitis, Allergic / drug therapy*
  • Urticaria / drug therapy*


  • Anti-Allergic Agents
  • Histamine H1 Antagonists
  • Platelet Activating Factor
  • rupatadine
  • Cyproheptadine