Both hypertension and dyslipidemia raise the risk of cardiovascular disease because they have proinflammatory effects and increase oxidative stress. The aim of this study was to evaluate the effects of rosuvastatin and metformin on inflammation and oxidative stress in patients with hypertension and dyslipidemia. This open parallel-group clinical study involved 48 patients with hypertension and dyslipidemia. Of these, 16 were treated with rosuvastatin, 10 mg/day, while 16 received metformin, 1700 mg/day, and the 14 in the control group received starch placebo, 10 mg/day. The following variables were recorded during the study: age, weight, body mass index, blood pressure, glucose, total cholesterol, low-density lipoprotein (LDL) cholesterol, high-density lipoprotein (HDL) cholesterol, triglycerides, interleukin-6 (IL-6), tumor necrosis factor-alpha (TNFalpha) glutathione reductase (GSH), glutathione peroxidase (GPx), and superoxide dismutase (SOD). Administration of 10 mg/day of rosuvastatin decreased total cholesterol by 41.7%, LDL cholesterol by 63.0%, and triglycerides by 10.7%, and increased HDL cholesterol by 6.3%. Pharmacological treatment with either rosuvastatin or metformin lead to reductions in IL-6, TNFalpha, GSH and GPx levels and an increase in the SOD level, and there were significant interactions between the two treatment groups for these variables. Rosuvastatin improved the lipid profile. Moreover, both rosuvastatin and metformin reduced inflammation and oxidative stress. These results demonstrate the presence of an additional cardioprotective effect, which may result from a direct mechanism of action or be a pleiotropic effect. Further long-term studies are required to determine whether rosuvastatin or metformin can be used to decrease the cardiovascular risk resulting from oxidative stress and inflammation.