Pharmacokinetics of the new broad spectrum penicillin CP-33994-2.
1.0 g of the new broad spectrum penicillin CP-33994-2 ws given i.m. to volunteers with varying renal function levels. Peak values of 40-50 microgram/ml were commonly observed in serum. The serum half-life was 1.1-1.5 h in normal renal function and increased to 7.0-17.0 h in patients with inulin clearance values of 12-14 ml/min. There was an appreciable lag before apparent absorption. Absorption rates and protein binding were uninfluenced by renal function. The renal clearance of the penicillin was less than the glomerular filtration rate. This may be due to either chemical instability of the compound such that it is inactivated before assay, or a substantial portion is changed (instability, metabolism) before excretion. A minor adjustment in dosage schedule is necessary in reduced renal function. Even patients with an inulin clearance of 12-14 ml/min have urine concentrations which are of antibacterial interest, at least in acute urinary tract infections without anatomical or other particular problems.
D005260:Female; D006207:Half-Life; D006801:Humans; D007668:Kidney / Q000378:metabolism; D007674:Kidney Diseases / Q000378:metabolism; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D010406:Penicillins / Q000097:blood / Q000378:metabolism* / Q000652:urine; D011485:Protein Binding; D011725:Pyridines / Q000097:blood / Q000378:metabolism / Q000652:urine
D010406:Penicillins; D011725:Pyridines; C012497:pirbenicillin