Single-dose pharmacokinetics of the monobactam azthreonam (SQ 26,776) in healthy subjects
Open Access
- 1 June 1982
- journal article
- research article
- Published by American Society for Microbiology in Antimicrobial Agents and Chemotherapy
- Vol. 21 (6), 944-949
- https://doi.org/10.1128/aac.21.6.944
Abstract
Azthreonam (SQ 26,776) is a new, completely synthetic, monocyclic beta-lactam antimicrobial agent that is highly active in vitro against most gram-negative bacteria. The pharmacokinetics of single intravenous doses of 125 to 4,000 mg, studied in 36 healthy male subjects, were best described by an open, linear, two-compartment kinetic model. The mean peak serum levels at 5 min after completion of 3-min infusions of 500-, 1,000- and 2,000-mg doses were 58, 125, and 242 micrograms/ml, respectively. The mean terminal serum half-life for all doses was 1.66 h, and the apparent volume of distribution was 0.18 liter/kg. The mean serum clearance was 1.27 ml min-1 kg-1, and urinary excretion averaged 68% of the doses administered. The pharmacokinetics of single intramuscular doses of 250 to 1,000 mg, studied in 18 subjects, were best described by a linear, one-compartment model, with first-order absorption and elimination. The mean peak serum levels occurring at 1 h after doses of 250, 500, and 1,000 mg were 12, 22, and 46 micrograms/ml, respectively. Other kinetic parameters were similar to those for intravenous administration. Tolerance of azthreonam was good, with only a mild rash in one subject and with mild to moderate transient elevations in serum transaminases and lactate dehydrogenase in two subjects.This publication has 6 references indexed in Scilit:
- Monocyclic β-lactam antibiotics produced by bacteriaNature, 1981
- Parenteral toxicological profile of the monocyclic -lactam antibiotic SQ 26,776 in mice, rats and dogsJournal of Antimicrobial Chemotherapy, 1981
- Pharmacokinetics of the monobactam SQ 26,776 after single intravenous doses in healthy subjectsJournal of Antimicrobial Chemotherapy, 1981
- In-vivo properties of SQ 26,776Journal of Antimicrobial Chemotherapy, 1981
- Antibacterial activity of a monocyclic -lactam SQ 26,776Journal of Antimicrobial Chemotherapy, 1981
- GR 20263, a new broad-spectrum cephalosporin with anti-pseudomonal activityAntimicrobial Agents and Chemotherapy, 1980