Epilepsy is a neurological disorder which is characterized with recurrent seizure. The antiepileptic drugs used in the treatment of epilepsy are associated with side effects. Several medicinal plants are used in the traditional treatment of epilepsy due to their therapeutic efficacy with low adverse effects. The leaf of Culcasia falcifolia is a medicinal plant which is traditionally used in Nandi County, Kenya in the treatment of epilepsy. The present study was designed to evaluate the safety, efficacy and antiepiletic activity of ethanol extract of C. falcilofia against PTZ induced seizure in laboratory mice. The study evaluated the anticonvulsant activity of ethanol extracts of Culcasia falcifolia on PTZ induced seizures in mice; the levels of endogenous antioxidant enzyme in brain tissue of the mice; the levels of neurotransmitters in brain tissue of the mice; skeletal muscle relaxation ability and locomotor activity of mice; the phytochemicals present in the extract; and identified and isolated the bioactive phytochemical in the leaf extract.