[Degradation of ampicillin by urine of patients with complicated urinary tract infections and its protective effect of dicloxacillin (author's transl)].
In vitro enzymatic degradation rate of ampicillin (AB-PC) in urine of patients with complicated urinary tract infection and its protective effect of dicloxacillin (MDI-PC) was studied using a specific fluorometric assay for aminobenzylpenicilloic acid (AB-PA), which is converted from AB-PC by bacterial beta-lactamase. The results showed that average degradation rate of AB-PC in the urine of 10 patients were 12.2%, 21.5%, 34.3% and 48.2% at 15, 30, 60 and 120 minutes, respectively. While MDI-PC prevented the enzymatic transformation of AB-PC in such urinary samples and the average degradation rates at 15, 30, 60 and 120 minutes were considerably reduced to 7.7%, 12.2%, 21.6% and 32.8%, respectively. In vivo urinary excretion rate of AB-PA was compared between a total of 5 patients and 4 healthy volunteers after oral administration of 250 mg AB-PC. It was found that the patients excreted 9.1%, 10.7% and 12.7% of total dose at 0 approximately to 2 hours, 2 approximately to 4 hours, 4 approximately to 6 hours, respectively, while the average excretion rates in healthy volunteers were 1.54%, 2.88% and 7.94%, respectively. In 4 patients cross-over administration study, the combined dose of AB-PC and MDI-PC has been proved to clearly decrease the urinary excretion rate of AB-PA in 2 cases, but there was no significant difference in the average rate between the single and the combined dose.
D000667:Ampicillin / Q000008:administration & dosage / Q000378:metabolism / Q000652:urine*; D001711:Biotransformation; D004009:Dicloxacillin / Q000008:administration & dosage / Q000494:pharmacology*; D006801:Humans; D014552:Urinary Tract Infections / Q000378:metabolism / Q000652:urine*; D001618:beta-Lactamases / Q000652:urine
D000667:Ampicillin; D004009:Dicloxacillin; D001618:beta-Lactamases