Pharmacokinetics of Single Oral Dosage of CS-866 (Olmesartan medoxomil), Angiotensin II Receptor Antagonist, Planned to be Clinically Used
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Accession number;03A0794394
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| Title;Pharmacokinetics of Single Oral Dosage of CS-866 (Olmesartan medoxomil), Angiotensin II Receptor Antagonist, Planned to be Clinically Used |
| Author;
TANAKA TAKANORI
(Aiseikai Osakikurinikku)
URAE RYUJI
(Aiseikai Osakikurinikku)
HISAOKA MASAFUMI
(Sankyo Co., Ltd., JPN)
SHIGA HIROSHI
(Sankyo Co., Ltd., JPN)
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Journal Title;Journal of Clinical Therapeutics & Medicines
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Journal Code:Y0906A
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ISSN:0910-8211
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VOL.19;NO.10;PAGE.1131-1142(2003)
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| Figure&Table&Reference;FIG.5, TBL.9, REF.13 |
| Pub. Country;Japan |
| Language;Japanese |
| Abstract;CS-866 (Olmesartan medoxomil) is an oral active angiotensin II receptor antagonist and an antihypertensive agent. It is converted to an active metabolite, RNH-6270, after oral administration. Since clinical dosage of CS-866 was estimated to be either of 5mg, 10mg, 20mg or 40mg based on the results of Phase II studies, the pharmacokinetics, pharmacodynamics, safety and tolerability after single administration of CS-866 at estimated clinical dosages were investigated in this trial. This was a randomized and open label study. 5mg, 10mg, 20mg or 40mg of CS-866 was orally administrated to 24 healthy male volunteers. AUC and Cmax of RNH-6270 showed linearity with dosage. Renal clearance and urinary excretion rate didn't change in this dosage range. Plasma rennin activity, plasma angiotensin I and II concentrations showed the trend of increase or decrease responding to the increase in dosage. The trend of decrease in blood pressure was observed and considered as a result of the pharmacological action of CS-866. This study suggested the pharmacokinetics of CS-866. This study suggested the pharmacokinetics of CS-866 in linear, and CS-866 is well tolerated and safe over the dose range investigated. (author abst.) |
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