REVIEW : New Drug and Recent Technique : Pharmacological, Pharmacokinetic and Clinical Properties of Olopatadine Hydrochloride, a New Antiallergic Drug
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概要
- 論文の詳細を見る
Olopatadine hydrochloride (olopatadine, 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid monohydrochloride) is a novel antiallergic/histamine H1-receptor antagonistic drug that was synthesized and evaluated in our laboratories. Oral administration of olopatadine at doses of 0.03 mg/kg or higher inhibited the symptoms of experimental allergic skin responses, rhinoconjunctivitis and bronchial asthma in sensitized guinea pigs and rats. 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. Olopatadine exerted no significant effects on action potential duration in isolated guinea pig ventricular myocytes, myocardium and human ether-a-go-go-related gene channel. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. 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, pruritis cutaneous, psoriasis vulgaris and erythema exsudativum multiforme in December, 2000. Ophthalmic solution of olopatadine was also approved in the United States for the treatment of seasonal allergic conjunctivitis in December, 1996 (Appendix: also in the European Union, it was approved in February 2002).
- 社団法人 日本薬理学会の論文
- 2002-04-01
著者
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小林 智
協和発酵工業株式会社 医薬開発本部非臨床開発部
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Ohmori K
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Ohmori Kenji
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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HAYASHI Ken-ichi
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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KAISE Toshihiko
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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OHSHIMA Etsuo
Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd.
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KOBAYASHI Satoshi
Pharmaceuticals Research and Development Division, Kyowa Hakko Kogyo Co., Ltd.
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YAMAZAKI Takashi
Pharmaceuticals Research and Development Division, Kyowa Hakko Kogyo Co., Ltd.
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MUKOUYAMA Akimichi
Pharmaceuticals Research and Development Division, Kyowa Hakko Kogyo Co., Ltd.
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Horikoshi Kaori
協和醗酵工業
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Horikoshi K
Drug Development Research Laboratories Pharmaceutical Research Institute Kyowa Kogyo Co. Ltd.
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Kaise Toshihiko
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Ohmori K
Drug Development Research Laboratories Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd
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Ohshima Etsuo
Pharmaceutical Research Center Kyowa Hakko Kogyo Co. Ltd.
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Ohshima Etsuo
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Hayashi Ken-ichi
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Katagiri S
Faculty Of Engineering Niigata University
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Ohmori K
Sumitomo Metal Mining Co. Ltd. Chiba Jpn
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Kobayashi Satoshi
Analytical And Pharmacokinetic Department Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co.
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Kobayashi Satoshi
Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Mukouyama Akimichi
Pharmaceuticals Research And Development Division Kyowa Hakko Kogyo Co. Ltd.
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Kobayashi Satoshi
Analytical & Pharmacokinetic Laboratories Pharmaceutical Research Institute Kyowa Hakko Hagyo Co
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Kobayashi Satoshi
Drug Development Research Laboratories Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.
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Yamazaki Takashi
Pharmaceuticals Research And Development Division Kyowa Hakko Kogyo Co. Ltd.
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