Coronary heart disease (CHD) is the leading cause of morbidity and mortality across the entire world, in which
reversion of angina or improvement of ECG remains an unrealistic therapeutic option for most patients, suggesting that
microvascular dysfunction or impaired oxygen delivery might be critical factors in CHD. This research article, thus presents
the rationale basis, clinical and experimental, for the first therapeutic innovation addressing the role of red blood cell
(RBC) H/K and O2/CO2 exchanges in CHD. It is followed by a randomized single-blind trial of Amiloride and Optimal
Medical Therapy (OMT, n=35 cases) vs OMT alone (n=35 cases) in patients having angina, ST-T alteration and a defective
RBC-K transport. All patients had serial clinical evaluation, Ion Transport Studies, ECGs and non-invasive aortic
waveform and cardiovascular hemodynamic recordings. Statistical analysis was performed by SAS.
Results: Amiloride rapidly improved RBC-K (93.5 ±4 vs 84.5 ±4 mmol/lc, p= < 0.001), angina (80% of cases, 1.5 ±0.3
weeks, CI:1.72 to 1.45), CCS Class (1.3 ±0.5 vs 3.1 ±0.8, p < 0.001) vs patients with OMT alone CCS Class (3.2 ± 0.4 vs
3.3 ± 0.5, p =0.21). Reversion of angina was sustained through the next 6-months (87% vs 26 % in OMT, RR 2.1, odds ratio
6.31, Pearson 2 34.6,p < 0.0001 at 95% CI) and 1-year (85% vs 37% OMT). At 6-months of amiloride, ECG became
normal (29% vs 0%, RR uncalculated-time, odds ratio , Pearson 2 42.4 at 95% CI, p < 0.0001), improved (55% vs
29%; RR2.1, odds ratio 3.16, 95% CI, p < 0.0001) or unchanged (15% vs 67% OMT). At 1-year, seven patients on amiloride
(18%) exhibited evidence of electrical regeneration of the heart, not observed with placebo.
In Conclusion: This therapeutical innovation of amiloride improves RBC H/K and O2/CO2 function, and reverses angina,
ST-T alterations while inducing electrical regeneration of the heart, in patients receiving optimal medical treatment for
angina. The article has short discussion on the relevant patents to the topic.