Inhibition of Theophylline Metabolism by Suplatast and Its Metabolites in Rats(Biopharmacy)
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概要
- 論文の詳細を見る
The inhibitory effect of suplatast (ST), an anti-allergic drug, on theophylline (TP) metabolism was investigated in rats in vivo and in vitro. Intravenous injection of aminophylline (AP) at 10mg/kg of TP equivalent was performed with or without pretreatment by oral administration of 100mg/kg of ST 2.5h prior to AP. In the ST-pretreated group, plasma concentration (Cp), the area under Cp-time profile (AUC) and urinary excretion of TP increased significantly, and urinary excretion of TP metabolites, 1,3-dimethyluric acid (DMU) and 1-methyluric acid (1MU) decreased significantly. Metabolic clearance of DMU (CL_<DMU>) and that of 1MU (CL_<1MU>) were remarkably suppressed by ST pretreatment, however, renal clearance (CLr) of TP did not change. To compare the inhibitory effect of ST on TP metabolism with that of its main metabolite (M1) in vivo, a concomitant intravenous injection of AP (10mg/kg of TP equivalent) with ST or M1 (40mg/kg of ST equivalent) was carried out. In the M1 group, Cp and AUC of TP increased significantly, and the total body clearance of TP decreased significantly. In contrast, ST did not induce these changes. Then, the inhibitory effect of ST and M1 on TP metabolism in vitro was evaluated using rat-liver microsomes. ST and M1 suppressed DMU formation in a competitively inhibitory manner, and their equilibrium dissociation constants (K_i) were 822 and 731μM, respectively. In conclusion, inhibition of TP metabolism by ST was demonstrated in vivo and in vitro, and the involvement of M1 and/or other metabolites in this drug interaction was suggested.
- 公益社団法人日本薬学会の論文
- 2005-06-01
著者
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KAWAKAMI Junichi
Department of Pharmacy, The University of Tokyo Hospital, Faculty of Medicine, University of Tokyo
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ADACHI Isao
Department of Hospital Pharmacy, Toyama Medical and Pharmaceutical University
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MIYAMOTO Etsuko
Department of Anesthesiology, Kansai Medical University
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Miyamoto E
Faculty Of Pharmaceutical Science Hokuriku University
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Miyamoto Etsuko
Department Of Anesthesiology Kansai Medical University
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Adachi Isao
Department Of Hospital Pharmacy Toyama Medical And Pharmaceutical University
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Miyamoto Etsuko
Faculty Of Pharmaceutical Science Hokuriku University
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KIZAWA Makiko
Department of Hospital Pharmacy, Toyama Medical and Pharmaceutical University
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AONO Shuka
Department of Hospital Pharmacy, Toyama Medical and Pharmaceutical University
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Aono Shuka
Department Of Hospital Pharmacy Toyama Medical And Pharmaceutical University
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Kizawa Makiko
Department Of Hospital Pharmacy Toyama Medical And Pharmaceutical University
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Kawakami Junichi
Department Of Hospital Pharmacy Hamamatsu University School Of Medicine
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Kawakami Junichi
Dep. Of Hospital Pharmacy Hamamatsu Univ. School Of Medicine
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ADACHI Isao
Department of Applied Mathematics Osaka University
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