The volatile constituents, toxicity, antinociception, and anti-inflammatory activities of the essential oil obtained from the leaf of Mucuna pruriens utilis collected from Nigeria are reported. The essential oil was analyzed comprehensively utilizing gas chromatography (GC)-flame ionization detector and GC coupled with mass spectrometry (MS) using the HP-5 column. The antinociceptive and anti-inflammatory assays were analyzed by a hot plate, formalin, and carrageenan-induced edema assays, respectively. The essential oil was obtained in a yield of 0.2% (v/w) calculated on a dry weight basis. A total of 36 compounds representing 94.8% of the oil contents were identified. The oil contained a high content of ( E)-2-hexenal (19.0%), linalool (8.9%), 1-hexanol (6.6%), and trans-dehydroxylinalool oxide (5.2%). The analgesic property of the essential oil was slightly significant ( P < 0.5) only at the third hour for the 400 mg/kg while other doses are less active. The rate of inhibition was moderate (24.1%-54%) during the analgesic phase of the formalin assay. The rate of inhibition at the anti-inflammatory phases of both formalin and carrageenan were significantly high (100%) and P < 0.001 for all the doses during the reaction duration. The potential proinflammatory mechanism might be due to effects on several proinflammatory mediators, including, histamine, serotonin, and bradykinin, and the ability of the essential oils to act as centrally mediated opioid analgesic. Mucuna pruriens essential oils displayed a high anti-inflammation potential and can be used as a potential centrally mediated opioid antagonist against analgesia.