Thienamycin: New Beta-Lactam Antibiotic with Potent Broad-Spectrum Activity

The in vitro activities of N-fonnimidoyl thienamycin (MK0787) and nine other antibiotics were tested against 129 Colonies of isolates to be tested were picked from nutrient agar slants, suspended in 1 ml of MuellerHinton broth, and incubated overnight at 370C. Fifty microliters of a 1:1,000 dilution of this culture in Mueller-Hinton broth was added to each well of the microtiter plate, resulting in final inocula (determined by representative colony counts) of from 4.5 x 104 to 1.0 x 1O colony-forming units per ml. The concentrations of antimicrobial agents in these wells ranged from 0.12 to 100 ug/ml. The MIC was defined as the lowest

Section: Resultsmentioning

confidence: 99%

In vitro activity of N-formimidoyl thienamycin (MK0787) against resistant strains of Pseudomonas aeruginosa, Staphylococcus epidermidis, Serratia marcescens, and Enterococcus spp

Livingston¹,

Elliott²,

Cobbs³

1981

“…Thienamycin exhibits potent activity against a wide variety of aerobic and anaerobic bacteria (5,6). However, thienamycin also possesses considerable chemical instability, remaining active only within a relatively narrow range of pH, temperature, and antibiotic concentration (2).…”

Section: Mk0787 (N-formimidoyl Thienamycin) Is Amentioning

confidence: 99%

In vitro activity of N-formimidoyl thienamycin (MK0787), a crystalline derivative of thienamycin

Horadam¹,

Smilack²,

Montgomery³

et al. 1980

232, 1979). This study presents in vitro susceptibility data on aerobic and facultatively anaerobic bacteria tested with N-formimnidoyl thienamycin and other antibiotics in current use in the treatment of infections with common pathogens. In contrast to investigations done in academic and university institutions, which may utilize relatively resistant organisms, isolates for the present study were collected sequentially from clinical infections encountered in a large community hospital. MATERIALS AND METHODS Microorganisms

“…In vitro studies of imipenem have demonstrated a broad spectrum of antibacterial activity (25,28) which includes both ,-lactamand aminoglycoside-resistant pathogens (10,14,22,26). In addition, the drug has been shown to be resistant to multiple 3-lactamases (3,21) and to possess marked in vitro activity against methicillin-resistant staphylococci (14,26,29).…”

mentioning

confidence: 99%

Pharmacokinetics of imipenem and cilastatin in patients with cystic fibrosis

Reed¹,

Stern²,

O'Brien³

et al. 1985

The pharmacokinetics of imipenem, a new carbapenem antibiotic, and cilastatin, a metabolic inhibitor, were evaluated in 17 patients with cystic fibrosis. Imipenem and cilastatin were combined in a ratio of 1:1 in the infusion solution, and patients intravenously received 30, 60, or 90 mg of imipenem per kg of body weight per day, divided into four equal doses. Pharmacokinetic evaluation after the first dose and again under steady-state conditions revealed biodisposition characteristics which were similar and independent of the daily dose administered. Cilastatin concentrations in serum paralleled those of imipenem. A linear relationship between dose and area under the serum concentration-time curve for both compounds was observed, suggesting a first-order pharmacokinetic process. A total of 50 and 78% of the doses of imipenem and cilastatin, respectively, were recovered unchanged in the urine. The renal clearances of imipenem and cilastatin averaged 54 and 88%, respectively, of the serum clearance. These data suggest that an extrarenal mechanism may be involved in the overall elimination of imipenem. No patient experienced any clinical or biochemical abnormalities during drug therapy.