Nitroglycerin has maintained its position in the treatment of angina pectoris for more than a century. Efficacy of oral nitrates has been established and compares well with that of other anti-anginal drugs. New delivery systems are being developed for sustained systemic nitrate action. Beneficial action of nitrates in congestive heart failure and their crucial role in unstable angina and acute myocardial infarction has further widened their therapeutic use. A plausible hypothesis of the mechanism of nitrate-induced vasodilation has been presented, involving production of nitrosothiols and activation of guanylate cyclase in the vascular smooth muscle. Recent developments suggest that the rate degradation of nitrates and formation of nitrosothiols in the vascular smooth muscle are linked, offering an explanation to the relatively rapidly developing, but partial vascular tolerance during high-dose nitrate therapy.