The combination of cobinamide and sulfanegen is highly effective in mouse models of cyanide poisoning

Clin Toxicol (Phila). 2011 Jun;49(5):366-73. doi: 10.3109/15563650.2011.584879.

Abstract

Context: Cyanide is a component of smoke in residential and industrial fires, and accidental exposure to cyanide occurs in a variety of industries. Moreover, cyanide has the potential to be used by terrorists, particularly in a closed space such as an airport or train station. Current therapies for cyanide poisoning must be given by intravenous administration, limiting their use in treating mass casualties.

Objective: We are developing two new cyanide antidotes--cobinamide, a vitamin B(12) analog, and sulfanegen, a 3-mercaptopyruvate prodrug. Both drugs can be given by intramuscular administration, and therefore could be used to treat a large number of people quickly. We now asked if the two drugs would have an augmented effect when combined.

Materials and methods: We used a non-lethal and two different lethal models of cyanide poisoning in mice. The non-lethal model assesses neurologic recovery by quantitatively evaluating the innate righting reflex time of a mouse. The two lethal models are a cyanide injection and a cyanide inhalation model.

Results: We found that the two drugs are at least additive when used together in both the non-lethal and lethal models: at doses where all animals died with either drug alone, the combination yielded 80 and 40% survival in the injection and inhalation models, respectively. Similarly, drug doses that yielded 40% survival with either drug alone, yielded 80 and 100% survival in the injection and inhalation models, respectively. As part of the inhalation model, we developed a new paradigm in which animals are exposed to cyanide gas, injected intramuscularly with an antidote, and then re-exposed to cyanide gas. This simulates cyanide exposure of a large number of people in a closed space, because people would remain exposed to cyanide, even after receiving an antidote.

Conclusion: The combination of cobinamide and sulfanegen shows great promise as a new approach to treating cyanide poisoning.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Antidotes / administration & dosage*
  • Cobamides / administration & dosage*
  • Cyanides / poisoning*
  • Cysteine / administration & dosage
  • Cysteine / analogs & derivatives*
  • Disease Models, Animal
  • Drug Therapy, Combination
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Prodrugs / administration & dosage*

Substances

  • Antidotes
  • Cobamides
  • Cyanides
  • Prodrugs
  • cobinamide
  • 3-mercaptopyruvic acid
  • Cysteine