A stepped-care approach to the treatment of hypertension has been developed to provide some practical guidelines for practicing physicians. Obviously, only drugs that are effective as monotherapy, and that are particularly well tolerated and safe, can be recommended for the use in the first step. In this discussion, evidence is provided in favor of using ACE inhibitors as first-step agents. They are effective in a large fraction of hypertensive patients when given as monotherapy and they are well tolerated even in the presence of associated diseases. They have a favorable hemodynamic profile, induce no tolerance, and can be combined with almost any other drug. They elicit few side effects, many of which are due to inadequate handling of the agents by the physician, and they appear to provide in general a particularly good quality of life to the patient.