Comparative study of endralazine and hydralazine for the treatment of hypertension uncontrolled by a beta-blocker and diuretic. Endralazine and hydralazine were compared in a randomized double-blind, parallel group study lasting 1 year in 30 patients with essential hypertension inadequately controlled by a beta-blocker and a diuretic. Dosage ranged from 10 mg to 30 mg endralazine per day and from 75 mg to 200 mg hydralazine per day according to patient response. The results showed that endralazine was at least as effective as hydralazine in reducing blood pressure. Patients' tolerance, assessed by drop-out rate, was significantly better (p less than 0.05) in the endralazine group. No cases were found of drug-induced lupus-like syndrome on endralazine as opposed to 2 cases with hydralazine
Effect of food intake on plasma levels and antihypertensive response during maintenance therapy with endralazine. A sensitive HPLC assay has been used to determine the effect of food on plasma endralazine levels in 8 patients with essential hypertension. Subjects were investigated whilst on maintenance therapy with endralazine combined with a fixed antihypertensive baseline treatment for at least 4 weeks, samples being collected after the usual oral morning dose of endralazine (5 mg and 10 mg), on two occasions at least 7 days apart. Endralazine was administered with the concomitant therapy in randomised order once 90 min before and once immediately after a standard breakfast. Acetylator status did not affect its pharmacokinetics in the postprandial study after a 5 mg dose, the peak
Endralazine, a new peripheral vasodilator--a randomized cross-over trial against dihydralazine. In a randomized cross-over trial in 23 patients with essential hypertension, a new peripheral vasodilator, endralazine, in a dose of 10-20 mg t.i.d. was compared with dihydralazine in a dose of 25-50 mg t.i.d. All patients also received pindolol (a beta-blocker) in a dose of 5-15 mg t.i.d. The lowest dose of both drugs was given to all patients for 2 weeks and was increased only if indicated. Endralazine was more effective than dihydralazine, but the side effects were about the same in frequency and severity, apart from flushing, which was more common with endralazine. Patients receiving endralazine in the second phase of the cross-over design continued to be treated with endralazine for a period
Comparison of once daily endralazine with placebo in the treatment of hypertension uncontrolled by a beta-blocker and diuretic. We report the first placebo controlled parallel group study of once daily endralazine (5-20 mg) in hypertension uncontrolled by a beta-blocker plus a diuretic. Following a 4-week run-in period 22 patients with a sitting mean arterial pressure (MAP) greater than 110 mm Hg were entered into the study and received either endralazine 5 mg or placebo. Blood pressure was measured 2 h and 24 h after dosing and the drug dose doubled at 2 and 4 weeks if the 24-h MAP remained greater than 110 mg Hg. The final blood pressure assessment was made after 6 weeks treatment in the 19 patients who completed the study. Three patients withdrew from the study because of side effects
[Methodologic approach to individual evaluation of the pharmacodynamic effects of single doses of hydralazine, endralazine, prazosine and propranolol in hypertension patients]. The possibility to apply impedance cardiography technique and individual statistical analysis based on Dixon's criterion to pharmacodynamic studies of single hydralazine ( apressine ), prazosine ( pratsiol ), endralazine
Clinical evaluation of endralazine (BO22708), a new vasodilator, in essential hypertension. In the treatment of severe hypertension the choice of vasodilator is limited by side-effects, of which the lupus erythematosus syndrome induced by hydralazine is potentially the most serious, particularly in patients with the slow acetylator phenotype. This study describes the clinical evaluation of a new vasodilator, endralazine, which is related to hydralazine but which is not metabolised to any great extent by acetylation. In 6 essential hypertensives not adequately controlled by combined beta-blocker and diuretic therapy the additional administration of the first dose of 10 mg endralazine resulted in a significant reduction in blood pressure, without orthostatic symptoms, but associated with significant
A dose-finding study of the combination of pindolol, clopamide and endralazine in the treatment of moderate-to-severe hypertension. This study compared the efficacy of a beta-blocker, pindolol, and a diuretic, clopamide, plus a vasodilator, endralazine, in the treatment of 30 patients suffering from moderate-to-severe hypertension. Different doses of endralazine were tested. This study showed that hypertension was controlled in 76,7% of patients receiving a combination of pindolol 10 mg and clopamide 5 mg (Viskaldix; Sandoz) plus endralazine 5 mg, and in 90% it was controlled by a combination of pindolol 10 mg, clopamide 5 mg and endralazine 10 mg daily. In 3 patients it was necessary to give pindolol 10 mg, clopamide 5 mg and endralazine 10 mg twice daily. Side-effects occurred in 5 patients
marked in hypertensive than in normotensive subjects. Prizidilol increases renal plasma flow like hydralazine and depresses glomerular filtration rate and fractional sodium excretion like endralazine. In addition to the fall in arterial pressure, efferent vasodilation and/or a specific effect on the glomerular ultrafiltration coefficient Kf may account for the striking decrease in filtration fraction.
Effects of intravenous endralazine in essential hypertension. The effects of endralazine, administered intravenously, on blood pressure, heart rate, forearm blood flow, plasma renin activity, aldosterone, adrenaline and noradrenaline were studied in five patients with essential hypertension. Endralazine reduced peripheral vascular resistance, resulting in decrease in mean arterial pressure from 141 to 116 mm Hg and increase in heart rate from 67 to 92 beats/min. Plasma renin activity, adrenaline and noradrenaline increased significantly after endralazine infusion. All effects observed are consistent with endralazine acting as a peripheral vasodilating drug.
The pharmacokinetics of endralazine in essential hypertensives and in normotensive subjects. The direct-acting vasodilator, endralazine, in combination with a beta-adrenoceptor blocker significantly reduced the blood pressures of normotensive volunteers and of patients with essential hypertension. The mean terminal elimination half-life for endralazine of 136 min in hypertensive patients did not differ significantly from the 155 min in normotensive subjects. In normal subjects the mean oral bioavailability for endralazine was 75% and the mean clearance was 780 ml/min. There were no significant pharmacokinetic differences between fast and slow acetylators. The administration of endralazine to steady state in the hypertensive patients was associated with an increase in terminal elimination half