Major advances in the diagnostic, evaluation, and particularly surgical treatment of aortic regurgitation (AR) have redefined the role of medical treatment. In acute AR, aortic valve replacement (AVR) is the only life-saving treatment. Medical treatment may improve the hemodynamic state temporarily before surgery. Rationale of medical treatment in chronic AR is based on the natural history and pathophysiology of the disease. The primary goal is to optimize the time of the AVR. If there is any symptom and/or left ventricular (LV) dysfunction, early AVR is required. Vasodilators should only be considered as a short-term treatment before surgery if there is evidence of severe heart failure or as a long-term treatment if AVR is contraindicated because of cardiac or noncardiac factors. In asymptomatic patients with severe chronic AR and normal LV function (even if the left ventricle is moderately dilated), vasodilators may prolong the compensated phase of chronic AR, although proof of their efficacy in delaying AVR is limited. Nifedipine is the best evidence-based treatment in this indication. ACE inhibitors are particularly useful for hypertensive patients with AR. beta-Adrenoceptor antagonists (beta-blockers) may be indicated to slow the rate of aortic dilatation and delay the need for surgery in patients with AR associated with aortic root disease. Furthermore, they may improve cardiac performance by reducing cardiac volume and LV mass in patients with impaired LV function after AVR for AR.