Parenteral toxicological profile of the monocyclic  -lactam antibiotic SQ 26,776 in mice, rats and dogs

Keim, G. R.; Sibley, Peter L.; Hines, Fred A.; Miller, MarkA .; Peterson, A. E.; Yoon, Yong‐Ho

doi:10.1093/jac/8.suppl_e.141

Cited by 16 publications

(3 citation statements)

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“…Due to its spectrum of activity, its low systemic and local toxicity, the convenient pharmacokinetics, and the very low immunological cross-reactivity with other 3-lactam antibiotics, AZT may be especially useful as an alternative to the more toxic aminoglycosides in many clinical settings (13,18,29,33).…”

Section: Resultsmentioning

confidence: 99%

Evaluation of aztreonam in the treatment of severe bacterial infections

Romero-Vivas¹,

Rodríguez‐Créixems²,

Bouza³

et al. 1985

Antimicrob Agents Chemother

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Aztreonam (AZT) is a member of a new class of monocyclic synthetic P-lactam agents with in vitro activity against the vast majority of gram-negative bacteria, including members of the family Enterobacteriaceae and most isolates of Pseudomonas aeruginosa. The compound is inactive against aerobic, gram-positive and anaerobic bacteria. It is likely that this selective spectrum of action causes minimal disturbance of normal human fecal flora, thus decreasing the risk of overgrowth of enterococci and other resistant strains (12,15,21,23,34,35).High levels of AZT in serum can be obtained with a 1-g parenteral dose, protein binding is about 56%, and the terminal half life in serum is 1.7 h. AZT is not metabolized in the body, renal excretion occurs by glomerular filtration, and about 65% of the antibiotic is recovered unchanged from the urine (18,29,(31)(32)(33).With these considerations in mind, we evaluated the clinical efficiency, tolerance, and toxicity of AZT in the treatment of 46 patients with 50 episodes of severe bacterial infections. MATERIALS AND METHODSPatients. Forty-six hospitalized patients were selected for the study. All had clear symptoms and signs of infection and microorganisms supposedly responsible for the infection had been identified within the previous 48 h.We considered as urinary tract infection (UTI) the isolation of significant bacteriuria (>105 CFU/ml) in the presence of related clinical symptoms. Our single case with respiratory tract infection was a patient with pneumonia defined by the presence of fever and pulmonary infiltrates and the isolation of a single pathogen from an endotracheal aspiration. Our diagnoses of osteomyelitis were supported by the presence of concomitant bacteremia in one case, with the isolation of the responsible microorganisms during surgical procedures in six patients and direct isolation from an open * Corresponding author.

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Section: Resultsmentioning

confidence: 99%

Evaluation of aztreonam in the treatment of severe bacterial infections

Romero-Vivas¹,

Rodríguez‐Créixems²,

Bouza³

et al. 1985

Antimicrob Agents Chemother

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“…In addition, the striking similarity between the antibacterial spectrum and potency of azthreonam and aminoglycosides suggests a new alternative therapy for the initial treatment of bacterial infections before laboratory identification of a pathogen. This would be particularly feasible if azthreonam, a beta-lactam antibiotic, proves to have a more favorable safety profile than aminoglycosides, as suggested by early studies in animals (5).…”

Section: Discussionmentioning

confidence: 99%

Single-dose pharmacokinetics of the monobactam azthreonam (SQ 26,776) in healthy subjects

Swabb¹,

Sugerman²,

McKinstry³

1982

Antimicrob Agents Chemother

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Azthreonam (SQ 26,776) is a new, completely synthetic, monocyclic betalactam 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, twocompartment 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 p,g/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-', 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 ,ug/ ml, respectively. Other kinetic parameters were similar to thbse 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.Azthreonam (SQ 26,776) (Fig.

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“…(Brown και συν. 1967, Albers-Shonberg 1978, Keim 1981). Εξάλλου, η εισαγωγή των συνδυασμών αναστολέων των β-λακταμασών με σκευάσματα β-λακτάμης ευαίσθητα στις β-λακταμάσες γιά την in vivo αντιμετώπιση της μικροβιακής αντοχής αποτελεί άκρως ενδιαφέρουσα προσθήκη στα αντιμικροβιακά θεραπευτικά σχήμα τα και έχει σαν στόχο της να μειώσει την ευρεία χρησιμοποίηση των αμινογλυκοσιδών στην καθημερινή ιατρική.…”

Section: χρώση της πηκτήςunclassified

Κλινικοεργαστηριακή Αξιολόγηση Των Συνδυασμών Του Αναστολέα Των Β-Λακταμασών Σουλμπακτάμης (CP - 45899) Με Αμπικιλλίνη Και Με Άλλα Χημειοθεραπευτικά Β - Λακτάμης

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Parenteral toxicological profile of the monocyclic -lactam antibiotic SQ 26,776 in mice, rats and dogs

Cited by 16 publications

References 0 publications

Evaluation of aztreonam in the treatment of severe bacterial infections

Evaluation of aztreonam in the treatment of severe bacterial infections

Single-dose pharmacokinetics of the monobactam azthreonam (SQ 26,776) in healthy subjects

Κλινικοεργαστηριακή Αξιολόγηση Των Συνδυασμών Του Αναστολέα Των Β-Λακταμασών Σουλμπακτάμης (CP - 45899) Με Αμπικιλλίνη Και Με Άλλα Χημειοθεραπευτικά Β - Λακτάμης

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