title: Human pharmacokinetics of BL-P1654 compared with ampicillin.
abstract: BL-P1654 is a new ureido-penicillin which has significant activity against both pseudomonas and klebsiella. Its pharmacokinetics were evaluated in five studies in four healthy adult male volunteers after 1-g doses given as: 5- and 30-min intravenous infusions, a 30-min infusion 1 h after the oral administration of 1 g of probenecid, and an intramuscular injection. For comparison, volunteers also received a 30-min infusion of 1 g of ampicillin. Serum levels of the antibiotic were found to fit a two-compartment open model using a Burroughs-5500 computer. After a 30-min infusion, peak serum levels of BL-P1654 (72.8 mug/ml [standard deviation] +/- 5.9) were 50% greater than those of ampicillin (53.6 +/- 8.9). Six hours later, the relative difference was even greater (4.58 +/- 0.25 versus 0.35 +/- 0.09). At 75 min after the 1-g intramuscular injection of BL-P1654, peak serum levels averaged 28.4 +/- 10.3 mug/ml. The half-life of BL-P1654 (2.04 h) was significantly longer than for ampicillin (1.15 h), and the renal clearances of BL-P1654 and ampicillin were 79 versus 244 ml/min per 1.73 m(2), respectively. Probenecid produced no significant change in blood levels, volume of distribution, half-life, or renal clearance, indicating that there is no net tubular secretion of this antibiotic.
mesh_terms: D000667:Ampicillin / Q000378:metabolism*; D006146:Guanidines / Q000008:administration & dosage / Q000378:metabolism; D006801:Humans; D007273:Injections, Intramuscular; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D008954:Models, Biological; D010397:Penicillanic Acid / Q000031:analogs & derivatives; D010406:Penicillins / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism; D011339:Probenecid / Q000494:pharmacology; D014508:Urea / Q000008:administration & dosage / Q000378:metabolism
chemical_list: D006146:Guanidines; D010406:Penicillins; C009705:BLP 1654; D000667:Ampicillin; D010397:Penicillanic Acid; D014508:Urea; D011339:Probenecid