Some specific features of the 24-hour blood pressure (BP) pattern are linked to the progressive injury of target tissues and the triggering of cardiac and cerebrovascular events. Thus, there is growing interest in how to best tailor the treatment of hypertensive patients according to the circadian BP pattern of each individual. Significant administration-time differences in the kinetics (i.e., chronokinetics) plus beneficial and adverse effects (i.e., chronodynamics) of antihypertensive medications are well known. Thus, bedtime dosing with nifedipine GITS is more effective than morning dosing, while also significantly reducing adverse effects. The dose-response curve, therapeutic coverage, and efficacy of doxazosin GITS are all markedly dependent on the circadian time of drug administration. Moreover, valsartan administration at bedtime, as opposed to upon wakening, results in an improved diurnal/nocturnal BP ratio, increased percentage of controlled patients, and significant reduction in urinary albumin excretion in hypertensive patients. Chronotherapy provides a means of individualizing the treatment of hypertension according to the circadian BP profile of each patient, and constitutes a new option to optimize BP control and to reduce the risk of cardiovascular disease (myocardial infarction and stroke) and of end-organ injury of the blood vessels and tissue of the heart, brain, kidney, eye, and other organs.