Summary:
Organic nitrates still constitute, like digitalis, an indispensable remedy. Amyl nitrite, discovered by Balard
was the first to be used for the therapy of angina pectoris by Sir T. Lauder Brunton in 1867. Nitroglycerin
(Glyceroltrinitrate) was synthetized by Ascanio Sobrero 1846 and was studied by Brunton, Tate, and
Murrel who published his paper on the treatment of angina pectoris in 1879. It has been soon recognised
that the main effect of nitrates is vasodilatation more pronounced in the veins, resulting in reduced venous
return, decrease of left and right ventricular end-diastolic pressure and volume and in a reduction in the
myocardioal oxygen demand. Sir William Osler was the first who suggested the use of nitroglycerin in
patients with congestive heart failure „when the pulse is hard and firm“, in his „Principles and Practice of
Medicine“ 1892. About fifty years later, L.Goldberg confirmed the antihypertensive effect of isosorbide
dinitrate in a double – leticin trial on hypertensive patients. The longacting nitrates isosorbide dinitrate
and isosorbide 5-mononitrate now share all the beneficial effects of nitroglycerin in patients with stable
and unstable angina and in selected patients with heart failure. The sustained-release tablets of isosorbide
5-mononitrate have been shown to be effective with long-term use without inducing tolerance. The author
also summaries basic data concerning the chemistry, pharmacology and clinical applications of organic
nitrates and nitrocompounds. The position of nitrates in the treatment of isolated systolic hypertension in
the elderly and of chronic heart failure is still to be established.
Key words:
nitrates, nitrites, nitroglycerin, isosorbide, dinitrate, isosorbide 5-mononitrate, amyl nitrite,
sodium nitroprusside, tolerance, glyceroltrinitrate.
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