SCREENING OF IQB-9302 

ACUTE TOXICITY IN MICE

Subcutaneous acute toxicity of IQB-9302 in mice was compared to that of Mepivacaine and Bupivacaine (INIBSA) by the method of Lorcke in groups of 15 male Swiss mice  (see here full report, PDF format in spanish, 128 KB) 

DL 50 was calculated on the basis of the mortality shown 48 hours after dosing  

RESULTS

  • Mepivacaine: 294 mg/kg (280 mg/kg)
  • Bupivacaine: 74 mg/kg (68 mg/kg)
  • IQB-9302: 89 mg/kg

    • These data are in close agreement with those obtained from literature (in parenthesis)  

CONCLUSION

Table 2 summarizes comparative activities and toxicities of some well-known local anesthetics in comparison with IQB-9302. Data of DL 50 of reference compounds have been obtained from literature (Aberg, G et al: Studies on the Duration of Local Anesthesia: Structure activity Relationships in a Series of Homologous local Anesthetics. Acta pharmacol et Toxicol. 1977, 41: 432-443) and are in good agreement with those obtained in our own experiments  

Toxic index has been calculated assuming DL50 of bupivacaine = 1.  

Anesthetic activity of reference compounds has been obtained from Covino B.: Pharmacology of local anesthetic agents, Br.J. Anaesth, 1986: 58: 701-716).  

IQB-9302's activity was calculated as the mean of the relative activity in comparison to mepivacaine in the three models.