Pharmacokinetics of the monobactam SQ 26,776 after single intravenous doses in healthy subjects.

Autor: Swabb, E. A., Leitz, M. A., Pilkiewicz, F. G., Sugerman, A. A.
Zdroj: Journal of Antimicrobial Chemotherapy (JAC); 1981, Vol. 8 Issue suppl_E, p131-140, 10p
Abstrakt: SQ 26,776 (SQ) is a new, completely synthetic, monocyclic beta-lactam antimicrobial agent active in-vitro against Gram-negative bacteria. The pharmacokinetics of this monobactam were studied in healthy male subjects. Single intravenous doses of 125–4000 mg or normal saline placebo were infused over 3 min by random assignment to 48 subjects. The pharmacokinetics were best described by an open, linear, two-compartment kinetic model. The mean peak serum levels at 5 min after completion of the infusion of 500, 1000, and 2000-mg doses were 58, 125 and 242 mg/l. The mean terminal serum half-life for all doses was 1.66 h, and the apparent volume of distribution was 0.18 l/kg. Mean serum clearance was 1.27 ml/min/kg and urinary excretion averaged 68% of the doses administered. Tolerance of SQ was good, with only a mild rash in 1/36 subjects and mild transient elevation in serum transaminases and LDH in 1/36 subjects. The in-vitro antibacterial activity and the overall acceptable pharmacokinetics and tolerance of SQ in man suggest that it may prove to be an effective chemotherapeutic agent for infections due to Gram-negative bacteria. [ABSTRACT FROM PUBLISHER]
Databáze: Complementary Index