Ritipenem acoxilの胆汁中移行と外科感染症における臨床効果

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  • Biliary excretion of ritipenem acoxil and its clinical efficacy in surgical infections

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The kinetic profile and clinical efficacy of ritipenem acoxil (RIPM-AC), a new oral penem, were investigated.<BR>RIPM-AC was administered orally to 2 patients at dose of 200 mg t. i. d. for 3 days. At 2-5 hours after the last administration before cholecystectomy, the gallbladder tissue concentration of ritipenem (RIPM), the active form of RIPM-AC, was not detectable. The concentrations in gallbladder bile were 0.12 and 0.64μg/ml, respectively.<BR>RIPM-AC was administered orally to 7 patients undergoing biliary drainage at a single dose of 400 mg. The maximum plasma concentration was 0.16-8.66 μg/ml at 1-2 hours after administration, and the maximum bile concentration was 0.10-17.3μg/ml at 1-4 hours.<BR>RIPM-AC was administered to 31 patients with surgical infections at doses of 150-400 mg t. i. d. for 3-9 days. The clinical efficacy was excellent in 9, good in 18 and fair in 4, with the efficacy rate being 87.1%.<BR>The bacteriological efficacy rates were 93.8% (15/16) in Gram-positive bacteria, 80.0% (20/25) in Gram-negative bacteria and 100% (18/18) in anaerobic bacteria.<BR>As side effects, diarrhea was noted in 1 case, and liver function test values were elevated in 2 cases.

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