Oral Administration of Nitrates

Abstract

Until 1980 oral administration of nitrates was the only practical way to achieve therapeutic plasma levels of nitrates for long periods in ambulatory patients. For two decades oral ISDN has been the almost exclusive drug for this indication. It allowed long-term prophylaxis of angina pectoris and treatment of congestive heart failure. Although in 1972 it was questioned whether a sufficient amount of ISDN can avoid first-pass hepatic elimination and reach the systemic circulation, it was shown shortly thereafter that this is the case, and ISDN regained its position as first-choice nitrate for chronic oral administration. Recently other nitrates have been used successfully for long-term oral administration. It has been noted that IS-5-MN has some pharmacokinetic advantages for oral administration. Oral sustained-release nitroglycerin formulations have also been used.