Nitrate delivery systems in perspective. A decade of progress

Abstract

In recent years the use of nitroglycerin and long-acting nitrate compounds in clinical practice has been increasing. Only 10 to 15 years ago these drugs, at least in oral formulation, were felt to have no clinical utility because of concern that potent hepatic enzyme activity would degrade sufficient amounts of the nitrate compounds from reaching the systemic circulation. However, it is now recognized that oral nitrate administration when given in sufficient amounts achieves therapeutic plasma concentrations and desired clinical effects. Nitrates are routinely used for the treatment of stable and unstable angina and also play a role in therapy for complications of myocardial infarction. Nitrates are very effective agents for preload reduction in vasodilator therapy of congestive heart failure. A wide variety of nitrate delivery systems, including the standard oral and sublingual formulations, and as well as the new transdermal nitroglycerin discs and buccal nitroglycerin, are now available. Sublingual nitroglycerin, isosorbide dinitrate, and buccal nitroglycerin are used for acute treatment of attacks of ischemic chest pain. For ambulatory patients, long-acting therapy can be administered by oral, topical ointment, transdermal disc, and buccal nitroglycerin formulations. Each compound has a slightly different onset and duration of action, which is in part dose-dependent. The relative merits and problems with each of the formulations are reviewed. Intravenous nitroglycerin is now commercially available and plays an increasing role in the intensive care units. It is an ideal drug for acute chest pain syndromes, including acute myocardial infarction. Specialized tubing does not need to be employed. The wide variety of nitrate delivery systems available to physicians makes use of this tried and true therapy practical and easy to carry out for clinicians.