Species specificity of 2-aryl carbapenem-induced immune-mediated hemolytic anemia in primates

Toxicology. 1996 Apr 30;108(3):207-15. doi: 10.1016/0300-483x(96)03305-7.

Abstract

L-695,256 is a novel 2-fluorenonyl carbapenem antibiotic with significant antimicrobial activity against strains of methicillin-resistant Staphylococci. This prototype compound was administered intravenously to rhesus monkeys (Macaca mulatta) at does of 50 or 200 mg/kg/day for 2 weeks to assess toxicity and found to induce a hemolytic anemia characterized by extravascular hemolysis and splenomegaly. A subsequent study in this species in which 100 mg/kg/day was administered i.v. for 4 weeks showed that all animals were direct antiglobulin test (Coombs' test) positive for IgG with 20-25% reductions in the erythron. Following 3 weeks of recovery, the erythron had returned to normal, although it took an additional 2 months for the Coombs' test to become negative. Challenge of these same animals with 0.5 million U/kg (300 mg/kg/day) of penicillin intravenously indicated no apparent cross-reactivity. Since attempts to establish a model for this immune-mediated hemolytic anemia with this drug in rats or mice were unsuccessful, a 2-week i.v. study in squirrel monkeys (Saimiri sciureus) was conducted at a dose of 200 mg/kg/day. All animals in this study remained Coombs' test negative with no changes in the erythron, suggesting an increased sensitivity to beta-lactam-induced anemia in rhesus monkeys compared to other species. Further support for this hypothesis was obtained using the cephalosporin antibiotic, cefotetan. This compound induced a high incidence of Coombs' test positive hemolytic anemia at clinically relevant doses in rhesus monkeys, despite a very low incidence of this adverse effect in patients with many years of clinical use. These data suggest that although rhesus monkeys respond in a qualitatively similar manner to humans with regard to high doses of beta-lactam antibiotics, their sensitivity may overestimate the risk of immune-mediated hemolytic anemia for clinical use.

Publication types

  • Comparative Study

MeSH terms

  • Anemia, Hemolytic, Autoimmune / chemically induced*
  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / toxicity*
  • Carbapenems / administration & dosage
  • Carbapenems / toxicity
  • Cefotetan / toxicity
  • Coombs Test
  • Drug Administration Schedule
  • Drug Hypersensitivity / etiology*
  • Female
  • Hematocrit
  • Hemoglobins / analysis
  • Imidazoles / administration & dosage
  • Imidazoles / toxicity
  • Injections, Intravenous
  • Macaca mulatta
  • Male
  • Penicillin G / toxicity
  • Saimiri
  • Species Specificity

Substances

  • Anti-Bacterial Agents
  • Carbapenems
  • Hemoglobins
  • Imidazoles
  • L 695256
  • Cefotetan
  • Penicillin G