Pharmacotherapeutic group: Anti-infectives for systemic use. ATC code: J01DF01.
Pharmacodynamics: Aztreonam is a monocyclic beta-lactam antibiotic with potent bactericidal activity against a wide spectrum of Gram-negative aerobic pathogens. Unlike the majority of beta-lactam antibiotics, it is not an inducer in vitro of beta-lactamase activity. Aztreonam is usually active in vitro against those resistant aerobic organisms whose beta-lactamases hydrolyse other antibiotics.
Pharmacokinetics: Single 30-minute IV infusions of 0.5 g, 1.0 g and 2.0 g in healthy volunteers produced peak serum levels of 54, 90 and 204 mg/L, and single 3-minute IV injections of the same doses produced peak levels of 58, 125 and 242 mg/L. Peak levels of aztreonam are achieved at about one hour after IM administration. After identical single IM or IV doses, the serum concentrations are comparable at 1 hour (1.5 hours from the start of IV infusion), with similar slopes of serum concentrations thereafter.
The serum half-life of aztreonam averaged 1.7 hours in subjects with normal renal function, independent of the dose and route. In healthy subjects 60-70% of a single IM or IV dose was recovered in the urine by 8 hours, and urinary excretion was essentially complete by 12 hours.
Toxicology: Preclinical safety data: Aztreonam was well tolerated in a comprehensive series of preclinical toxicity and safety studies.
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