Pharmacokinetics of carumonam (AMA-1080) in patients with impaired renal function and in those undergoing hemodialysis.

The pharmacokinetics of carumonam (AMA-1080) were studied after a single intravenous 1.0-g dose was given to 26 subjects grouped according to their renal functions. Creatinine clearance (CLCR) was above 85, 50 to 84, 10 to 49, and below 10 ml/min/1.

Comparative pharmacokinetics of carumonam and aztreonam in mice, rats, rabbits, dogs, and cynomolgus monkeys.

The pharmacokinetic properties of carumonam (AMA-1080, Ro 17-2301) were studied in mice, rats, rabbits, dogs, and cynomolgus monkeys and compared with those of aztreonam. Carumonam administered subcutaneously in mice or intramuscularly in rats, rabbits, dogs, and cynomolgus monkeys at a dose of 20 mg/kg was readily absorbed and distributed at high concentrations in the plasma, kidneys, liver, and lungs, as was aztreonam. The peak level of carumonam in plasma, ranging from 41 micrograms/ml in mice to 68 micrograms/ml in monkeys; the area under the plasma concentration-time curve, ranging from 20 micrograms X h/ml in mice to 80 micrograms X h/ml in monkeys; the plasma half-life, ranging from 0.

[Cefotiam concentration in exudate from suction drain of patients with breast cancer following intravenous administration].

Cefotiam (CTM) in a dose of 2 g was given by intravenous bolus injection to 16 patients with breast cancer operated upon radical mastectomy with suction drainage. The materials of exudate from drain were taken at intervals by sterilized paper disc and determined by the paper disc method with Proteus mirabilis ATCC 21100 as the test organism to CTM concentrations. CTM concentrations in exudate from suction drain of patients increased quickly after intravenous injection, and reached to peak early time on 2 to 3 days after operation.

[Cefotiam concentration in exudates from the drainage of patients with acute peritonitis following intravenous administration].

Cefotiam dihydrochloride (CTM) in a dose of 2 g was given by intravenous bolus injection to 15 patients operated upon for acute or subacute abdominal organs. They were included to 5 cases of acute localized peritonitis due to perforative appendicitis, 3 of diffuse peritonitis due to perforative duodenal ulcer, 1 of diffuse peritonitis with intestinal obstruction, 1 of perforative sigmoid colon cancer, 2 of gastric cancer or polyp with cholelithiasis, and 3 of cholangitis with cholecyst-choledocholithiasis. The materials of exudate from drain were taken at intervals by sterilized paper disc and determined by paper disc bioassay method with Proteus rettgeri ATCC 9250 or Proteus mirabilis ATCC 21100 as the test organisms to CTM concentrations.

Relevance of in vitro antibacterial activities and pharmacokinetic properties of antipseudomonal beta-lactam antibiotics to their therapeutic effects on urinary tract infection caused by Pseudomonas aeruginosa P 9 in mice.

The therapeutic effects of seven antipseudomonal beta-lactam antibiotics on experimental urinary tract infection caused by Pseudomonas aeruginosa P 9 in mice were compared, and the results were analyzed in relation to their in vitro antibacterial activities and pharmacokinetic properties. The CD50 values were (mg/kg): cefsulodin, 6.19; cefoperazone, 162; sulbenicillin, 167; ticarcillin, 184; azlocillin, 121; mezlocillin, 390; and piperacillin, 227.