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Stereo-isomeric nitrates in the treatment of angina pectoris

  • Joseph E.F. Riseman
    Affiliations
    From the Medical Research Department of the Yamins Research Laboratory, Beth Israel Hospital, Boston, Mass., USA

    From the Departments of Medicine, Harvard Medical School and Tufts Medical School, Boston, Mass., USA
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  • Sidney Koretsky
    Affiliations
    From the Medical Research Department of the Yamins Research Laboratory, Beth Israel Hospital, Boston, Mass., USA

    From the Departments of Medicine, Harvard Medical School and Tufts Medical School, Boston, Mass., USA
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  • George E. Altman
    Affiliations
    From the Medical Research Department of the Yamins Research Laboratory, Beth Israel Hospital, Boston, Mass., USA

    From the Departments of Medicine, Harvard Medical School and Tufts Medical School, Boston, Mass., USA
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      Abstract

      • 1.
        1. The four stereo-isomers of pentitol pentanitrate (d-arabitol, l-arabitol, xylitol and adonitol pentanitrate) are highly effective in the prophylactic treatment of angina pectoris. They are especially effective when administered sublingually, but even when enclosed in gelatin capsules and swallowed, their use is followed by an increase in exercise tolerance in many patients. Clinically there is no clear-cut superiority of any one of these preparations over the other three; hence, the stereo-isomeric configuration of these compounds is not important in their utilization in angina pectoris.
      • 2.
        2. d-isosorbide dinitrate (Isordil), when administered sublingually, is also highly effective in the prophylactic treatment of angina pectoris. The rapidly soluble sublingual form of Isordil is much more effective than is the more slowly soluble preparation intended to be swallowed. Following the use of the sublingual form of isosorbide dinitrate, an increase in exercise tolerance becomes evident within a few minutes and persists for as long as one to four hours in some patients. When taken after the induction of pain, the sublingual form of isosorbide dinitrate decreased the duration of discomfort of the patient whose attacks otherwise were usually longer than one minute in duration. The use of the “sustained-action” tablets was not followed by a detectable increase in exercise tolerance, although many patients experienced headache.
      • 3.
        3. The activity of the nitrates in angina pectoris is not due to the number of —ONO2 groups in the nitrate molecule.
      • 4.
        4. The lag in onset and the prolonged duration of effect of the nitrates imply that their action is not immediately dependent on the concentration of the pure drug in the blood stream.
      • 5.
        5. Chlorothiazide and Recordil were of slight value in some patients with angina pectoris. The use of Amplivix and Persantin was not followed by any appreciable increase in exercise tolerance.
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