Background: Rauwolfia vomitoria Afzel. (Apocynaceae) leaf is used to treat various diseases such as ascariasis, cancer, hypertension, other cardiovascular diseases, and various diseases in traditional medicine in Nigeria. This study evaluated the anthelminthic, antiproliferative and antihypertensive potentials of R. vomitoria leaf methanol extract in Wistar rats. In addition, the phytochemical, acute toxicity, total phenolic and flavonoid contents were also evaluated. Results: Qualitative phytochemical screening revealed the presence of various metabolites with flavonoids and alkaloids the most predominant, with different amount of total phenolic and flavonoid contents per gallic acid and rutin equivalent respectively. NMR and GC-MS studies on the R. vomitoria showed the presence of methyl stearate ester a fatty acid ester. In vitro antioxidant activity by inhibition of DPPH and H2O2 scavenging radicals showed an IC50 value of 1.614 mg/mL and 0.101 mg/mL Acute toxicity investigation showed that extract is well tolerated at doses up to 5,000 mg/kg body weight RVE after two weeks. Anthelminthic and antiproliferative effects of the RVE showed dose-dependent activities in time of paralysis/death of earthworms and growth of guinea corn radicles respectively. The blood pressure reduced significantly in normotensive and RVE-treated hypertensive rats in dosedependent fashion. There was significant dilation of the aortic blood vessel at high concentration of RVE with reduced heart rate and complete blockage of adrenaline and CaCl2 stimulatory effects. Conclusions: This study provided the justification that R. vomitoria leaf extract possessed anthelminthic, antiproliferative and antihypertensive potentials, hence, its use as an ethnomedicinal prescription for these conditions in traditional medicine. It further provides an avenue for new drug discovery.