Disease relevance of tigemonam

• The expanded spectrum of activity against gram-negative bacteria observed with tigemonam thus extends oral beta-lactam coverage to include members of the Enterobacteriaceae that are intrinsically or enzymatically resistant to broad-spectrum penicillins and cephalosporins [1].
• The proposed MIC quality-control range of tigemonam for E. coli ATCC 25922 is 0.13 to 0.5 micrograms/ml [2].
• Tigemonam inhibited beta-lactamases of E. cloacae and Pseudomonas aeruginosa but did not induce beta-lactamases [3].
• In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective [4].
• In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin [4].

High impact information on tigemonam

• Oral and parenteral administration of aztreonam and oral administration of tigemonam to conventional mice caused a decrease in the number of aerobic gram-negative rods in the feces [5].
• Tigemonam was not hydrolyzed by the common plasmid beta-lactamases such as TEM-1 and SHV-1 or by the chromosomal beta-lactamases of Enterobacter, Morganella, Pseudomonas, and Bacteroides spp [3].
• Some Enterobacter cloacae and Citrobacter freundii strains resistant to aminothiazole iminomethoxy cephalosporins and aztreonam were resistant to tigemonam [3].
• Tigemonam was highly resistant to hydrolysis by the eight beta-lactamase enzymes tested [2].
• The excellent activity of tigemonam against beta-lactamase-producing bacteria reflected its marked stability to hydrolysis by isolated enzymes [1].

Chemical compound and disease context of tigemonam

• Aztreonam was more active against Pseudomonas spp., and tigemonam was more active against some streptococci [2].
• In addition, tigemonam was superior to cefuroxime, which is under development as an oral pro-drug, and more active than cefixime against several genera of the Enterobacteriaceae [1].
• The activity of tigemonam against the enteric bacteria, Haemophilus species, and Neisseria species was, in general, comparable to that of the quinolone norfloxacin [1].
• It is concluded that tigemonam should play an important role in the treatment of nosocomial infections that do not require parenteral therapy and in the treatment of multiresistant community-acquired infections [6].
• Five strains of Escherichia coli, Serratia marcescens, and Proteus vulgaris were exposed to a new monobactam, tigemonam, in comparison with aztreonam [7].

Biological context of tigemonam

• Tigemonam may have a valuable role in the management of infection caused by enterobacteria, particularly if bioavailability following oral administration is confirmed in human subjects [8].
• Protein binding in human serum was found to be 62.5%; the presence of serum had only a modest effect on the activity of tigemonam [9].

Anatomical context of tigemonam

• In vitro activity of tigemonam against urinary tract pathogens [10].
• Minimum bactericidal concentrations and time-kill determinations indicated that tigemonam showed remarkable bactericidal activity, with a 9% reduction in colony-forming units after 2 h at a dose corresponding to fourfold its minimum inhibitory concentration [11].

Associations of tigemonam with other chemical compounds

• Furthermore, in vitro aztreonam was about twice as potent as tigemonam, but in vivo the reverse was the case [12].
• Comparative in-vitro activity of tigemonam, a new monobactam [13].

Analytical, diagnostic and therapeutic context of tigemonam

• It is concluded that tigemonam is a candidate for clinical trials in patients with infections caused by Gram-negative aerobes other than pseudomonas and acinetobacter [13].
• Tigemonam at a concentration of 4 micrograms/mL or less inhibited 72.7% of the strains with minimum inhibitory concentrations ranging from 0.03 or less to more than 512 micrograms/mL [6].
• The study, evaluated by kinetic turbidimetry, has shown that tigemonam exerts a prelytic increase in optical density (OD) similar to that of other beta-lactam antibiotics [7].

References