Clinical Evaluation of Endralazine (BQ22708), A New Vasodilator, in Essential Hypertension

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Abstract
In the treatment of severe hypertension, the choice of vasodilators is limited by their side effects, of which lupus erythematosus syndrome induced by hydralazine is potentially the most serious, particularly in patients with the slow acetylator phenotype. A new vasodilator, endralazine, which is related to hydralazine but which is not metabolized to any great extent by acetylation is described. In 6 essential hypertensives not adequately controlled by combined .beta.-blocker and diuretic therapy, the additional administration of the 1st dose of 10 mg endralazine resulted in a significant reduction in blood pressure, without orthostatic symptoms but associated with significant increases in heart rate and plasma noradrenaline [norepinephrine] concentration. These 6 patients and another 9 similar hypertensive patients were then prescribed twice daily endralazine for 4 wk with significant improvement in blood pressure control. During this short period of maintenance treatment with endralazine, the single dose observations were repeated and no significant changes in heart rate or plasma noradrenaline concentration were observed.