Calotropis procera Aiton (Calotropis) is a wild-growing plant used for a variety of disease conditions such as leprosy, ulcers, tumor and healing of wounds. The present study was conceived to evaluate the toxicological effect of the latex following systemic use in SpragueDawley rats with a view to understanding its potential safety in treating wounds and preventing keloid formation in human. Haematological evaluation revealed a significant and progressive reduction of the packed cell volume (PCV) and red blood cell count at high doses of the latex. There was no significant effect on the differential count except for lymphocytes which showed significant reduction following increasing concentrations of the latex. Similarly, the latex exhibited no significant effect on the renal indices of the rats: uric acid, urea and creatinine levels. A significant (P<0.05) decrease in blood glucose was decrease at the same dose, but there was no significant change in the levels of the albumin, alanine transaminases and alkaline phosphatases in all the treated groups. Histopathological studies showed no remarkable effect on the tested organs except for the testes where there was destruction of the seminiferous tubules. In conclusion, these results suggest that Calotropis latex is relatively safe when used acutely especially through the oral route and in lower doses when administered through the intra-peritoneal route in rats. However, there is need for caution when higher doses are administered because of the toxic effects on the genitourinary systems particularly in males.