Effect of Gnetum africana on the pharmacokinetic parameters of chloroquine was investigated. Chloroquine phosphate (200 mg/Kg) was concurrently administered to overnight fasted albino rats. Blood samples were collected 15, 30, 60, 120, 240 and 480 minutes after administration through cardiac puncture. Serum concentration of chloroquine was evaluated spectrophotometrically. The results indicated that the extract significantly decreased C max (9.17%), Ka (3.06%), Ke (45.38%), Cl (48.46%) and AUC (0-8) (16.90%). The extract also increased the values of t1/2 (83.11%), t max (100.00%). The LD50 of the extract was 5.25 g/Kg. Phytochemical screening revealed the presence of steroids, tannins, flavonoids and traces of phlobatanins and alkaloids. Proximate and elemental analyses showed that the plant contained Sodium (26.37 + 0.01ppm), Potassium (32.84 + 0.02 ppm), Copper (0.01 + 0.00 ppm), Calcium (6.53 + 0.01ppm), Magnesium (7.58+ 0.02 ppm), Iron (2.01 + 0.02 ppm), Zinc (0.93 + 0.03 ppm), Lead (0.02 + 0.01 ppm), Moisture (10.90 + 0.91 mg/100 g), Crude protein (15.31 + 1.12 mg/100g), Crude fibre (4.20 + 0.21 mg/100 g), Crude fat (10.60 + 0.65 mg/100 g), Ash (5.40 + 0.30 mg/100g), Carbohydrate (74.49 + 0.23 mg/100 g) and Energy (407.80 Kcal). The results of this work showed that concurrent administration of the extract of Gnetum africana affected some of the pharmacokinetic parameters of chloroquine. Malaria patients on chloroquine therapy should therefore be advised to beware of consuming Gnetum africana .