[Pharmacological profile and clinical efficacy of transdermal patch containing emedastine difumarate (ALLESAGA® TAPE)]

Nihon Yakurigaku Zasshi. 2018;152(5):246-255. doi: 10.1254/fpj.152.246.
[Article in Japanese]

Abstract

ALLESAGA® TAPE is the first transdermal drug delivery system of emedastine difumarate, as a second-generation antihistamine, for allergic rhinitis. It has been suggested that the efficacy of emedastine difumarate in allergic rhinitis is mediated through a combination of chemical mediator release inhibitory effects and eosinophil chemotaxis inhibitory effects, in addition to a strong anti-histaminic effect. In the pharmacological evaluation on histamine-induced vascular hyperpermeability in rats, ALLESAGA® TAPE showed an anti-histaminic effect in a dose-dependent manner and exhibited a long-lasting anti-histaminic effect until 24 hours after administration. In the patients having allergic nasal symptoms, the plasma concentration of emedastine reached at steady-state within 7 days after multiple administration of ALLESAGA® TAPE. ALLESAGA® TAPE was effective for treating seasonal allergic rhinitis with sustained action throughout the day. Long-term application of ALLESAGA® TAPE raised no safety concerns in patients with perennial allergic rhinitis. Plasma drug concentrations showed little change over a long period and there was no decrease of efficacy. Based on the above results, ALLESAGA® TAPE is possible to provide a new option for the treatment of allergic rhinitis.

MeSH terms

  • Animals
  • Benzimidazoles / administration & dosage*
  • Histamine H1 Antagonists / administration & dosage*
  • Humans
  • Rats
  • Rhinitis, Allergic / drug therapy*
  • Transdermal Patch*
  • Treatment Outcome

Substances

  • Benzimidazoles
  • Histamine H1 Antagonists
  • emedastine