teopranitol and Coronary-Disease

To evaluate the effects of the new compound teopranitol (KC 046) on blood volume distribution scintigraphic measurements were performed in 10 patients with coronary heart disease. The data were compared to the results in 10 untreated patients with coronary heart disease. The differences in blood volume distribution were calculated by the ratio of the impulse rates thorax/abdomen, thorax/thigh, thorax/shank and heart/total impulse rates assessed by scintigraphy, following in vivo labeling of red blood cells with 99m-Tc, before and after i.v. injection of 0.04 mg KC 046/kg body weight. A significant decrease of the ratios could be found, whereas the data in the untreated group did not change significantly. It is concluded from these results that the clinical improvement of the patients with coronary heart disease treated by KC 046 is caused by a significant shift of blood volume from the thoracic region into the abdomen and the legs, thus decreasing the preload of the left ventricle.

Topics: Aged; Chemical Phenomena; Chemistry; Coronary Circulation; Coronary Disease; Female; Humans; Male; Middle Aged; Radionuclide Imaging; Sugar Alcohols

The present study was designed to examine the effects of a new organic nitrate, teopranitol, in acute myocardial ischaemia. Adult cats were subjected to 5 h of myocardial ischaemia by permanent ligation of the left anterior descending coronary artery (LAD). Teopranitol (10 mg kg-1 X h) or physiological saline (vehicle) was infused i.v., beginning 30 min after LAD occlusion and continued until the end of the experiment. All animals subjected to myocardial ischaemia showed a significant elevation of the ST-segment within 20 min of LAD occlusion. In the LAD-vehicle group, the ST-segment elevation continued to increase; teopranitol attenuated this increase and significantly reduced the ST-segment elevation at 4 and 5 h (P less than 0.05). The loss of creatine phosphokinase-specific activity from the ischaemic myocardium was significantly reduced by teopranitol (P less than 0.05), indicating an improved preservation of myocardial tissue. There was a significant initial reduction in mean arterial blood pressure by teopranitol in sham-operated cats but no consistent change of this parameter, heart rate or the computed pressure-rate product in LAD-occluded cats. Teopranitol did completely reverse the ischaemia induced formation of platelet aggregates at 1 to 5 h (P less than 0.05). It is concluded that teopranitol exerts a significant protective effect in acute myocardial ischaemia in vivo that is independent of changes in systemic haemodynamics and might be associated with the generation of an antiplatelet activity in vivo.

Topics: Animals; Blood Pressure; Cats; Coronary Disease; Coronary Vessels; Creatine Kinase; Electrocardiography; Heart Rate; Ligation; Myocardium; Platelet Count; Sugar Alcohols