Amodiaquine (AQ) is a 4-aminoquinoline antimalarial with schizonticidal action against different strains of Plasmodia. This study assessed the effect of the drug on some macromolecules of the brain of albino Wistar rats. Twenty-four adult Wistar rats weighing between 150-180 g were divided into four groups of six animals each. Group 1 served as the control and received distilled water, while groups 2, 3 and 4, the experimental groups, were treated with 17.50 mg/kg, 8.75 mg/kg and 8.75 mg/kg of AQ, respectively. The treatment lasted three days for groups 2 and 3, and six days for group 4. The brains of the animals were removed, weighed and preserved in sucrose tris-KCl-MgCl (STKM) buffer for some macromolecule analysis. The total proteins (TP) and triacylglycerol (TAG) showed no significant (p> 0.05) differences between the experimental groups compared to the control, and there was no significant (p> 0.05) difference within the experimental groups. In the cholesterol (CH) estimation, the control had significantly (p< 0.01, p< 0.001) higher concentration than groups 3 and 4 respectively, but not group 2. CH concentration in group 2 was, however, significantly (p< 0.05, p< 0.01) higher than that in groups 3 and 4 respectively. These results reveal that AQ caused insignificant change to brain TP and TAG, but significantly altered the CH in the brain of Wistar rats.