Patients often take antimalarial drugs indiscriminately without a doctor’s prescription as treatment for uncomplicated malaria in the tropics, especially in Africa, where malaria is endemic. If these patients eventually visit clinicians during complications, the clinicians request liver functions tests, which include Serum bilirubin and albumin, from the medical laboratories before making clinical decisions. The study was done to evaluate the effects of artesunate (antimalarial) on serum bilirubin and albumin of Wistar rats. The study was conducted on a total of 30 rats (5 groups of 6 rats each). Rats in the control group were given distilled water only while those in test groups were administered with 2.0mg/kg, 4.0mg/kg, 8.0mg/kg, and 16.0mg/kg of artesunate, respectively. Bilirubin was estimated using Jendrassik and Grof method while Albumin was estimated using Bromocresol green binding method (BCG). The results and statistical analysis indicated remarkable differences (P<0.05) in total bilirubin (TB), unconjugated bilirubin (UB), and albumin between the test and control groups but not in conjugated bilirubin (CB) (P> 0.05) between the test and control groups. The marked increase in total bilirubin was dose-dependent and attributed to unconjugated hyperbilirubinaemia resulting from increased lysis of red blood cells initiated by the drug. People in malaria-endemic areas and who take antimalarials often should evaluate their liver functions at least once a year.