Epimers of moxalactam: in vitro comparison of activity and stability

Antimicrob Agents Chemother. 1981 Jul;20(1):30-2. doi: 10.1128/AAC.20.1.30.

Abstract

Moxalactam exists in two epimeric forms, R and S. The in vitro activity of these two epimers was compared with that of material available for clinical and laboratory use (R + S moxalactam). Generally, R moxalactam was twice as active as the S form. The stability of R + S moxalactam was studied at 37, 20, 4 and -20 degrees C in buffer and serum. Only in serum at 37 degrees C was there any appreciable loss of activity (half-life, 8 h). The stability of R and S epimers was studied separately, and the composition of the resulting equilibrium was investigated. At 37 degrees C in serum, one-half of the excess of either R or S over the equilibrium mixture was converted into the equilibrium mixture in 1.5 h. The proportions of R to S in an equilibrium mixture in buffer were 50:50, but in serum they were 45:55. It is doubtful whether these differences in stability and activity will have any significant clinical importance.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • Cephalosporins / pharmacology*
  • Cephamycins / blood
  • Cephamycins / pharmacology*
  • Drug Stability
  • Half-Life
  • Humans
  • Moxalactam
  • Species Specificity
  • Stereoisomerism

Substances

  • Anti-Bacterial Agents
  • Cephalosporins
  • Cephamycins
  • Moxalactam