Efficacy and safety of rilmenidine for arterial hypertension

Beau, Bertrand; Mahieux, Florence; Paraire, Marie; Laurin, Sylvie; Brisgand, Brigitte; Vitou, Philippe

doi:10.1016/0002-9149(88)90474-2

Cited by 30 publications

(4 citation statements)

References 21 publications

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“…Rilmenidine (2‐(dicyclopropylmethyl)‐amino‐2‐oxazoline) is a centrally acting antihypertensive drug with binding selectivity to newly described I 1 imidazoline receptors (identified in the lateral reticular nucleus in the brainstem and proximal tubular cells in the kidney) over α 2 ‐adrenoceptors [1–5]. It has dose‐dependent blood pressure lowering effects above 0.5 mg in both healthy and hypertensive subjects.…”

Section: Introductionmentioning

confidence: 99%

Concentration‐effect relationships of two infusion rates of the imidazoline antihypertensive agent rilmenidine for blood pressure and development of side‐effects in healthy subjects

Visser

Gerven

Schoemaker

et al. 2001

Brit J Clinical Pharma

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Aims The aim of this study was to compare the effect pro®les of i.v. administered rilmenidine aimed at the same target plasma concentration, but attained with different rates. Methods The study was placebo-controlled, randomized, double-blind, doubledummy, three-way, cross-over in nine healthy volunteers. All subjects randomly received either a fast infusion, a slow infusion or a placebo infusion. The target concentration was set at 8 ng ml x1 with a ®vefold difference in the time to reach the maximum concentration. Saccadic eye movements, electroencephalography (EEG), blood pressure and heart rate were measured every half hour. Drug plasma concentrations, adverse events, salivary¯ow and visual analogue scales were obtained every hour.Results Changes in systolic/diastolic blood pressure at the end of the infusion were (mean t s.d.) 13.3t16.4/7.9t7.5 mmHg with the fast infusion and 16.3t12.7/10.2t7.9 mmHg during the slow infusion, compared with 0.0t13.2/ 1.3t8.3 mmHg for the placebo occasion. Decrease of saccadic peak velocity (SPV) at the end of the infusion was 18.0t5.2% during the fast infusion, 23.0t7.0% with the slow infusion, and 6.1t5.2% with placebo. PK/PD analysis showed similar concentration-dependent linear reduction in SPV and blood pressure up to the maximum observed rilmenidine plasma level for both the fast and the slow infusion. Conclusions The rate of infusion of rilmenidine in healthy volunteers does not in¯uence the PK/PD relationship of saccadic eye movements and blood pressure up to the maximum observed rilmenidine plasma concentrations. Rilmenidine causes clear concentration-dependent blood pressure reductions in healthy volunteers.

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Section: Introductionmentioning

confidence: 99%

Concentration‐effect relationships of two infusion rates of the imidazoline antihypertensive agent rilmenidine for blood pressure and development of side‐effects in healthy subjects

Visser

Gerven

Schoemaker

et al. 2001

Brit J Clinical Pharma

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“…3,17) Rilmenidine has been shown to reduce both systolic and diastolic blood pressure in patients with essential hypertension effectively in both long term (one year) and short term (four week) therapy regimens. 6,18) An important characteristic for any antihypertensive medication is its ability to regress left ventricular hypertrophy. Rilmenidine has been proven to be effective in this task when used for a 1-year time interval.…”

Section: Discussionmentioning

confidence: 99%

<b>Short Term Effects of Rilmenidine on Left Ventricular Hypertrophy and Systolic and Diastolic Function in Patients with Essential Hypertension</b>

2003

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SUMMARYThe short term (three months) effects of rilmenidine on systemic hypertension induced left ventricular hypertrophy (LVH) and left ventricular systolic and diastolic functions in comparison with those of perindopril and nifedipine-slow release (SR) formulation were studied. The short term effects of rilmenidine on biochemical parameters and lipid profiles were evaluated.Sixty patients (39 men, 21 women) with a mean age of 59 ± 14 years and with mild to moderate systemic arterial hypertension were enrolled in three groups. The first group received 1 mg/day of rilmenidine, the second group 4 mg/day of perindopril, and the third group 20 mg/day of nifedipine SR. All drugs induced a similar decrease in systolic and diastolic blood pressure (BP) values. Left ventricular mass (LVM) and LVM index decreased equally in all groups associated with a significant increase in the E/A ratio. The ratio between the reduction in LVM and decrease in mean arterial pressure (LVM/mmHg) was higher in groups 1 and 2. Negative correlations between LVM and LVMI, E/A, and the dv/dt ratio were obtained. Rilmenidine did not change the blood chemistry and lipid profile values.Despite its neutral effect on lipid profile and biochemical parameters, rilmenidine is as effective as perindopril and nifedipine in controlling hypertension and decreasing left ventricular hypertrophy. (

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“…(2-[dicyclopropylmethyl]-amino-2oxazoline) is a centrally acting antihypertensive agent with binding selectivity to the I 1 -imidazoline receptors over ␣ 2 -adrenergic receptors. [1][2][3][4] It has dose (concentration)-dependent blood pressure-lowering effects at greater than 0.5 mg in both healthy and hypertensive subjects. Rilmenidine is registered in several European countries at a recommended dose of one 1-mg tablet once or twice daily.…”

Section: Rilmenidinementioning

confidence: 99%

Concentration‐effect relationships of two rilmenidine single‐dose infusion rates in hypertensive patients

Visser

Post

Nanhekhan

et al. 2002

Clin Pharma and Therapeutics

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Efficacy and safety of rilmenidine for arterial hypertension

Cited by 30 publications

References 21 publications

Concentration‐effect relationships of two infusion rates of the imidazoline antihypertensive agent rilmenidine for blood pressure and development of side‐effects in healthy subjects

Concentration‐effect relationships of two infusion rates of the imidazoline antihypertensive agent rilmenidine for blood pressure and development of side‐effects in healthy subjects

<b>Short Term Effects of Rilmenidine on Left Ventricular Hypertrophy and Systolic and Diastolic Function in Patients with Essential Hypertension</b>

Concentration‐effect relationships of two rilmenidine single‐dose infusion rates in hypertensive patients

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