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[Randomized, double-blind comparison of isosorbide-5-mononitrate and delayed-action nifedipine in patients with stable exertional angina. Multicenter Study Group].

The therapeutic effects of IS-5-MN and s.r. nifedipine were investigated in this double-blind, randomized, group-comparative, multicenter study over 2 weeks, in 251 patients with stable reproducible exercise-induced angina. After 2 weeks' treatment with IS-5-MN 20 mg b.i.d. or t.i.d., 61% of the patients were responders who showed an increase in total exercise time (to moderately severe angina) of greater than or equal to 20% in comparison with placebo in the run-in phase. The corresponding responder rate after s.r. nifedipine 20 mg b.i.d. or 40 mg b.i.d. was 53%. Both IS-5-MN and s.r. nifedipine significantly increased the total exercise time, the time to angina onset and to greater than or equal to 1 mm ST-depression, and significantly reduced the rate pressure product and the ST-segment depression at peak exercise in comparison with placebo in the run-in phase. The improvement in quality of life as indicated by the reduction in anginal episodes and intake of short-acting nitrates was comparable with both drugs. The pattern and incidence of all AEs were as expected in the two active treatment groups. The daily treatment costs for a 20 mg b.i.d. dosing regimen for both drugs in the Federal Republic of Germany was 64% higher for s.r. nifedipine than with IS-5-MN.

Angina Pectoris↗

[Effectiveness of the delayed-action form of isosorbide 5-mononitrate in ischemic heart disease].

Isosorbit 5-mononitrate is useful in ischaemic heart disease and in cardiac failure because of its favourable pharmacokinetic properties, in particular the absence of the so-called first pass effect, the great biological availability and long elimination time. The authors demonstrated on the preparation Elentan long, Schwarz Monheim GFR, which contains 50 mg isosorbit 5-mononitrate the improved efficiency of the left ventricle after three months administration to 15 patients with confirmed ischaemic heart disease, by exerting a favourable effect on the diastolic, systolic and global left ventricular function. Nitrates are drugs of first choice in some forms of ischaemic heart disease and are also effective in cardiac failure because they exert a marked effect on some cardiac functions on which the efficiency of the left ventricle depends. Elentan long proved, while using simple dosage, a preparation with favourable characteristics as regards biological availability and nitrate tolerance.

Coronary Disease↗

[Clinical evaluation of isosorbide dinitrate (ISDN) spray: a study on the plasma concentrations of ISDN and on its hemodynamic effects using three administration routes].

The effects of ISDN spray has been evaluated using oral, nasal or tracheal routes in patients under enflurane anesthesia. These 30 patients were in ASA I or II physical status without cardiovascular, kidney or liver diseases. Under enflurane anesthesia, hemodynamic parameters (blood pressure and heart rate), blood gas and plasma concentration of ISDN were measured at several points before and after drug administration. The plasma concentration reached a maximum point (C max) 4 min after drug administration in the oral group (O-group) and nasal group (N-group), and the values obtained were 48.4 +/- 5.4 ng.ml-1 and 87.4 +/- 13.8 ng.ml-1 respectively. The C max of the N-group was significantly higher than that of O-group (P less than 0.05). In the O- and N-groups, systolic blood pressure decreased 10% and 17%, after 4 min (P less than 0.05) and recovered 20 after min. Diastolic blood pressure decreased in both groups after 4 min (P less than 0.05). Heart rate significantly increased in the N-group (P less than 0.05), and continued to change up to 60 min after drug administration. In both groups, PaO2/FIO2 decreased 14% and 9% after 10 min (P less than 0.01). In the tracheal group, plasma concentration did not increase and these hemodynamic changes were not observed. These results suggest that nasal route of ISDN spray is the best route of administration.

Administration, Intranasal↗