This review is restricted to blood pressure lowering and related pharmacological effects of selected antihypersensive drugs in man. Data from animal studies, which may have important clinical significance, are included. Detailed mechanisms of action, clinical pharmacology, and pharmacokinetics of antihypertensive drugs are not included (see 1-15). The number of clinically effective antihypersensive agents available is ever increasing. However, these may be classified into five main categories acoording to their major mechanism of action: drugs with CNS mode of action, adrenoceptor blocking drugs, vasodilators, diuretics, and angiotensin analogues and angiotensin converting enzyme inhibitors. It is quite difficult to show the existence of simple relationships between the plasma concentration of most antihypertensive drugs and their circulatory effects, especially the antihypertensive effect.