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[Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug].

Abstract
Olopatadine is a selective histamine H1-receptor antagonist possessing inhibitory effects on the release of inflammatory lipid mediators such as leukotriene and thromboxane from human polymorphonuclear leukocytes and eosinophils. Olopatadine also inhibited the tachykininergic contraction in the guinea pig bronchi by prejunctional inhibition of peripheral sensory nerves. Oral administration of olopatadine inhibited passive cutaneous anaphylaxis in rats, experimental allergic rhinitis and bronchial asthmatic responses in actively sensitized guinea pigs. Olopatadine exerted no significant effects on action potential duration in isolated guinea pig myocardium and ventricular myocytes. Olopatadine was highly and rapidly absorbed in healthy volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was low in the elimination of olopatadine. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials. Olopatadine was approved in Japan for the treatment of allergic rhinitis, chronic urticaria, eczema dermatitis, prurigo, pruritus cutaneous, psoriasis vulgaris and erythema exsudativum multiforme in December, 2000.
AuthorsK Ohmori, T Ikemura, H Kobayashi, A Mukouyama
JournalNihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 118 Issue 1 Pg. 51-8 (Jul 2001) ISSN: 0015-5691 [Print] Japan
PMID11496828 (Publication Type: English Abstract, Journal Article, Review)
Chemical References
  • Anti-Allergic Agents
  • Dibenzoxepins
  • Histamine H1 Antagonists
  • Inflammation Mediators
  • Olopatadine Hydrochloride
Topics
  • Animals
  • Anti-Allergic Agents (pharmacokinetics, pharmacology)
  • Clinical Trials as Topic
  • Depression, Chemical
  • Dibenzoxepins (pharmacokinetics, pharmacology)
  • Histamine H1 Antagonists (pharmacokinetics, pharmacology)
  • Humans
  • Inflammation Mediators (metabolism)
  • Olopatadine Hydrochloride
  • Passive Cutaneous Anaphylaxis (drug effects)
  • Pruritus (drug therapy)
  • Rhinitis, Allergic, Perennial (drug therapy)
  • Urticaria (drug therapy)

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