Hemodializability of Pimobendan and Its Active Metabolite, UD-CG212, in Patients with Congestive Heart Failure Undergoing Hemodialysis.

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The hemodializability of a non-glycosidic, positive inotropic agent, pimobendan and its active metabolite, UD-CG 212, was studied in 5 patients (4 males and 1 female) with congestive heart failure and end-stage renal failure undergoing hemodialysis (HD). Pimobendan (1.25 or 2.5 mg) was orally administered 2 hours before the HD session began and plasma samples (5 mL each) were obtained from the inlet and outlet portions of the dialyzer at 0, 1, 2, 3 hours during the HD session and at the end of the procedure. HD was performed with a mean duration of 220 minutes and a blood flow rate (Q) of 200 mL/min. The plasma concentrations of pimobendan and UDCG 212 were determined using the HPLC-fluorescence detection method, and the half-life, extraction ratio (E) of dialyzer, HD clearance (CLHD), and the estimated amounts of the drugs eliminated by HD (Ae, HD) were calculated for both compounds. The results showed that pimobendan and UC-CG 212 possessed the half-lives (t 1/2) of 1.9±1.6 and 3.1±1.9 hours (mean±SD), the E of 0.08±0.02 and 0.1±0.02 and CLHD of 10.2±7.0 and 13.4±2.3 mL/min, respectively. The Ae, HD during a single, 4-hr session of HD were calculated to be 6.2±4.1 and 11.4±1.6 μg for pimobendan and UD-CG 212, respectively, thus indicating the sum of these amounts to account for less than 2% of the dose of pimobendan administered. The mean CLHD obtained from the patients was considered to be equivalent to 1% or less than the reported systemic clearance of patients with end-stage renal failure. In conclusion, HD was thus considered to have no clinically significant influence, if any, at all on the elimination of both pimobendan and its active metabolite, thereby no supplemental dosages seem to be necessary after undergoing HD.

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  • 病院薬学

    病院薬学 26 (4), 438-442, 2000

    一般社団法人 日本医療薬学会

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