Haemodynamics and Pharmacokineticsof Flosequinan (BTS 49 465) after Single and Multiple Oral Administration in Healthy Volunteers.

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概要

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• The effect on haemodynamics, pharmacokinetics, and safety of BTS 49 465 (flosequinan; 7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone) were investigated in six healthy volunteers after single oral administration and in six other healthy volunteers after repeated oral administration.The antihypertensive action of BTS 49 465 was observed beginning from 30min after single oral administration and continuing for 6hr. Pulse rate increased in accordance with the decrease in blood pressure. A steady state of plasma BTS 53 554, a major metabolite of flosequinan, was achieved on day 6 of multiple oral administration.The t1/2 (biological half life) after the final dose of the repeated administration was the same as that after single administration.This study demonstrated that BTS 49 465 is rapidly absorbed by the gastrointestinal tract given that the tmax (peak time) of BTS 49 465 is 30min. The t1/2 of BTS 49 465 is 2.1hr, while the t1/2z of BTS 53 554 is 29hr, which supports a once-daily regimen. Two percent of BTS 49 465 and 51% of BTS 53 554 were excreted in the urine within 96hr after flosequinan administration. After multiple oral administration BTS 53 554 plasma concentration reached a steady state on day 6 and on day 10. After final dosing, the t1/2 was comparable to that after single oral administration.BTS 49 465 and BTS 53 554 did not accumulate in the body after multiple oral administration. Absorption and excretion after multiple oral administration were comparable to those after single oral administration.Adverse reaction was limited to mild headache in all volunteers after single oral administration and in 5 of 6 volunteers after multiple oral administration. This symptom was, however, transient and improved without any treatment. There were no abnormal findings in the physiological or laboratory examinations.

著者

• 西内 健

  健康保険鳴門病院循環器科

• 斎藤 史郎

  徳島大学第1内科

• 瀬部 俊彦

  徳島大学第一内科

• 小富 正昭

  大塚製薬 (株) 徳島研究所代謝分析研究部

• 清水 剛文

  大塚製薬 (株) 徳島研究所代謝分析研究部

• 加地 公代

  大塚製薬 (株) 徳島研究所代謝分析研究部

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