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PubMed · 11527020

Tedisamil (Solvay).

N A Flores
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Abstract

Tedisamil, a potassium channel blocker (class III anti-arrhythmic agent)from Solvay, is in phase II trials for the potential treatment of atrial fibrillation [342434]. The drug had completed phase III trials for angina pectoris [342434], [177648], and although an NDA dossier for angina pectoris in refractory patients was ready for filing with the US FDA, Solvay has decided to pursue the broader indication of atrial fibrillation instead [342434]. Tedisamil is bradycardic without producing a negative inotropic effect. In a canine model of exercise-induced angina, myocardial function was maintained. In rat, rabbit, canine and simian hearts, there was a marked prolongation of action potential, due to tedisamil's modulating effects on potassium channels. Diastolic arterial pressure was not influenced [276934]. Tedisamil also rapidly terminated sustained atrial fibrillation and prevented its reinitiation in a canine model of the condition [315378]. The class III antiarrhythmic effect of tedisamil is related predominantly to the strong blocking effect of the drug on the rapid component of the delayed rectifier potassium current [334806].

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Angina PectorisAnimalsAnti-Arrhythmia AgentsBridged Bicyclo Compounds, HeterocyclicClinical Trials as TopicCyclopropanesHumansPotassium Channel BlockersJournal Article

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N A Flores. 2001. Tedisamil (Solvay).. https://pubmed.ncbi.nlm.nih.gov/11527020/

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OBJECTIVE: Ischemic preconditioning is an increased tolerance to myocardial ischemia during the second of two consecutive exercise tests. ATP-sensitive K(+) channel blockers, such as glinides and sulfonylurea drugs, can induce loss of ischemic preconditioning. This study aimed to investigate the effects of repaglinide, a hypoglycemic agent with an affinity for myocardial ATP-sensitive K (+)channels, on the results of consecutive exercise tests in patients with diabetes and multivessel coronary artery disease. METHODS: Forty-two patients with type 2 diabetes and chronic stable angina pectoris, and two-vessel or three-vessel disease participated in this study. The patients underwent two consecutive treadmill exercise tests (phase 1). On the day after these exercise tests, 2 mg of oral repaglinide was given to the patients. One week later, two exercise tests were repeated consecutively (phase 2). RESULTS: All patients achieved 1.0-mm ST-segment depression during the four exercise tests (T1, T2, T3, and T4). In phase 2, seven patients improved in time to onset of 1.0-mm ST-segment depression. The worsening of the time to onset of 1.0-mm ST-segment depression in phase 2 demonstrated ischemic preconditioning block in 83.3% of patients (P=0.0001). Even the postexercise electrocardiographic parameters (ST-segment depression morphology and magnitude and arrhythmias) were significantly different between the groups with and without pharmacologic ischemic preconditioning block (P=0.031). CONCLUSIONS: Repaglinide, an oral hypoglycemic agent with ATP-sensitive K(+) channel-blocker activity, eliminated the myocardial ischemic preconditioning in patients with coronary disease and diabetes.

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