Placebo-controlled comparison of the efficacy and tolerability of once-daily moxonidine and enalapril in mild-to-moderate essential hypertension

Küppers, H; Jäger, Bodo; Luszick, Joachim; Gräve, Michael; Hughes, Peter R.; Kaan, E. C.

doi:10.1097/00004872-199715010-00010

Cited by 44 publications

(31 citation statements)

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“…5 Moxonidine effectively reduces blood pressure; however, side effects such as dizziness and dry mouth are much less than with the older centrally acting antihypertensives, ie, clonidine. 10 Indeed, these side effects seem to be due to activation of central ␣ 2 -receptors. Moxonidine, however, stimulates the imidazoline-1 receptors in the ventrolateral area of the medulla oblongata, which, at least in animals, leads to a decreased sympathetic tone in resistance vessels, the heart, and the kidney.…”

mentioning

confidence: 99%

I ₁ -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

Wenzel

Spieker

et al. 1998

Hypertension

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Abstract-Moxonidine is an I 1 -imidazoline receptor agonist that reduces blood pressure in hypertensives. Experimental data suggest that moxonidine inhibits central sympathetic activity. However, whether such a mechanism is involved in vivo in humans is still unclear. We investigated the effects of 0.4 mg moxonidine orally on muscle sympathetic nerve activity and heart rate in an open study in 8 healthy volunteers. Furthermore, we studied the effects of 0.4 mg moxonidine on muscle sympathetic nerve activity, heart rate, blood pressure, 24-hour blood pressure profile, and hormone plasma levels in 25 untreated hypertensives in a double-blind, placebo-controlled study. Moxonidine decreased muscle sympathetic nerve activity in both healthy volunteers (PϽ0.05 versus baseline) and hypertensives (PϽ0.02 versus placebo). Plasma norepinephrine also decreased (PϽ0.01), whereas plasma epinephrine and renin levels did not change (PϭNS). Furthermore, moxonidine decreased systolic (PϽ0.0001) and diastolic (PϽ0.001) blood pressure. Heart rate decreased after moxonidine in healthy subjects (PϽ0.05); in hypertensives, heart rate decreased during the night hours (PϽ0.05) but not during daytime (PϭNS). Plasma levels of LDL, HDL, and total cholesterol were not influenced by the drug (PϭNS). Moxonidine decreases systolic and diastolic blood pressure by inhibiting central nervous sympathetic activity. This makes this new drug suitable for the treatment of human hypertension and possibly for other cardiovascular diseases with increased sympathetic nerve activity, ie, ischemic heart disease and heart failure.

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confidence: 99%

I ₁ -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

Wenzel

Spieker

et al. 1998

Hypertension

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“…• Достижение целевого АД (моксонидин и перин-доприл в многочисленных исследованиях доказали свою гипотензивную эффективность, а периндоприл во многих прямых сравнительных исследованиях был эффективнее других ингибиторов ангиотензинпре-вращающего фермента (иАПФ) и сартанов) [5][6][7][8][9][10].…”

Section: для чего нужная новая комбинация блокаторов раас с агонистамunclassified

Combination of Ace Inhibitor With Agonist of I1 -Imidazoline Receptors: New Opportunities for Antihypertensive Therapy

Недогода¹

2016

Russ J Cardiol

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“…7,13,[23][24][25][26][27] The fall in resting arterial pressure was progressive and significant at each therapeutic dose. In addition, moxonidine was also shown to reduce the peak levels of blood pressure attained during IHG and CPT.…”

Section: Greenwood Et Al I 1 -Imidazoline Agonism: Sympathetic Mechanmentioning

confidence: 99%

“…28 Finally, moxonidine produced no significant effect on heart rate, which is also consistent with the results of earlier trials. 27,29,30 This may be related to a lack of effect on the vagal control of heart rate, which is greater than the sympathetic control at rest, as confirmed by an absence of change in cardiac BRS. Also, any moxonidinemediated decrease in heart rate due to its sympatholytic effect may be opposed by a reflex increase in heart rate through vagal inhibition resulting from the decrease in arterial pressure.…”

Section: Greenwood Et Al I 1 -Imidazoline Agonism: Sympathetic Mechanmentioning

confidence: 99%

Chronic I ₁ -Imidazoline Agonism

et al. 2000

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Abstract-Evidence exists for a state of sympathetic hyperactivity in essential hypertension, and moxonidine, a new central sympathetic inhibitor, has been introduced for its treatment. Acute administration of moxonidine lowers peripheral sympathetic neural output. This study examined the effect of chronic moxonidine therapy, at increasing therapeutic doses, on resting peripheral sympathetic activity and vascular resistance and their responses to physiological reflex maneuvers. Twelve newly diagnosed patients with essential hypertension were studied sequentially at least 1 month apart, initially on no therapy, then on 200 g, and finally on 400 g of oral moxonidine daily. Changes in heart rate, arterial blood pressure, calf vascular resistance, and peripheral sympathetic drive were assessed at rest and during reflex maneuvers. Peroneal microneurography was used to quantify peripheral sympathetic vasoconstrictor activity by single-unit and multiunit techniques. Moxonidine therapy progressively reduced resting mean arterial pressure (PϽ0.0001) without affecting heart rate. At 200 g daily, there was a significant reduction in sympathetic nerve activity (PϽ0.001) and calf vascular resistance (PϽ0.01). At 400 g daily, further reductions were smaller and insignificant.Responses to cold stimulus and isometric handgrip exercise showed a similar pattern, with the greatest magnitude of change at 200 g daily. In patients with essential hypertension, chronic moxonidine therapy inhibited resting sympathetic vasoconstrictor drive and also its reflex responses. The magnitude of inhibition became less as the therapeutic dose was increased, suggesting that moxonidine may be more effective under conditions of high sympathetic activity.

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Placebo-controlled comparison of the efficacy and tolerability of once-daily moxonidine and enalapril in mild-to-moderate essential hypertension

Abstract: Moxonidine is an effective and well-tolerated antihypertensive, at least as good as other established forms of antihypertensive medication. The trough:peak ratio of 0.7 indicates that the drug will be effective administered once a day.

Cited by 44 publications

References 9 publications

I ₁ -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

I ₁ -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

Combination of Ace Inhibitor With Agonist of I1 -Imidazoline Receptors: New Opportunities for Antihypertensive Therapy

Chronic I ₁ -Imidazoline Agonism

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Placebo-controlled comparison of the efficacy and tolerability of once-daily moxonidine and enalapril in mild-to-moderate essential hypertension

Abstract: Moxonidine is an effective and well-tolerated antihypertensive, at least as good as other established forms of antihypertensive medication. The trough:peak ratio of 0.7 indicates that the drug will be effective administered once a day.

Cited by 44 publications

References 9 publications

I 1 -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

I 1 -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

Combination of Ace Inhibitor With Agonist of I1 -Imidazoline Receptors: New Opportunities for Antihypertensive Therapy

Chronic I 1 -Imidazoline Agonism

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I ₁ -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

I ₁ -Imidazoline Agonist Moxonidine Decreases Sympathetic Nerve Activity and Blood Pressure in Hypertensives

Chronic I ₁ -Imidazoline Agonism