Ketanserin and Red Blood Cell Sodium Content in Hypertension

Cree, J. De; Leempoels, J.; B, Demoen; Verhaegen, H.

doi:10.1097/00005344-198500077-00013

Cited by 11 publications

(4 citation statements)

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“…It is also known that in vitro incubation of erythrocytes with serotonin imparis erythrocyte deformability and that ketanserin [26], which shows both an S2-serotoninergic blocking action and an alphal-blocking action, can effectively inhibit this change in vitro [27]. Therefore, the improvement of erythrocyte deformability and inhibition of Y. Nagakawa et al: Effects of carvedilol on common carotid arterial flow erythrocyte aggregation produced by carvedilol might be due to its alpha-blocking and antiserotonin actions.…”

Section: Discussionmentioning

confidence: 99%

Effects of carvedilol on common carotid arterial flow, peripheral hemodynamics, and hemorheologic variables in hypertension

Nagakawa

Akedo

Kaku

et al. 1990

Eur J Clin Pharmacol

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The effects of a beta-blocker, carvedilol, on peripheral hemodynamics and hemorheologic parameters were evaluated in 11 geriatric patients with essential hypertension [3 men and 8 women aged 62-79 years (mean, 68.6 years)]. Carvedilol was given orally after breakfast at a dose of 10 or 20 mg daily for 8 weeks. Peripheral hemodynamics, the common carotid arterial flow, and hemorheologic parameters were determined twice prior to administration and after 4 and 8 weeks of carvedilol treatment. The common carotid arterial flow was determined using the pulsed Doppler method. Peripheral hemodynamics were assessed by venous occlusion plethysmography. The hemorheologic parameters assessed include erythrocyte aggregation, erythrocyte deformability, plasma viscosity, whole-blood hematocrit, and platelet function tests. Erythrocyte aggregation was measured using an Erythrocyte Aggregometer MA-1 (Myrenne, USA), taking a high shear rate of 600 s-1 and a low shear rate of 3 s-1 as the indices. Statistical comparisons of values before and after carvedilol administration were made using the paired Student's t-test. Systolic and diastolic blood pressure were decreased by carvedilol. The common carotid arterial flow was increased, and peripheral hemodynamics were improved by carvedilol. Erythrocyte aggregation (measured at both a high and a low shear rate) and plasma viscosity were decreased, erythrocyte deformability was increased, and levels of circulating platelet aggregates were also improved by carvedilol. This improvement of hemorheologic variables may contribute to prevention of the initiation and progression of thrombosis and atherosclerosis in geriatric patients with essential hypertension.

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Section: Discussionmentioning

confidence: 99%

Effects of carvedilol on common carotid arterial flow, peripheral hemodynamics, and hemorheologic variables in hypertension

Nagakawa

Akedo

Kaku

et al. 1990

Eur J Clin Pharmacol

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“…These changes were attended by a decrease in erythrocyte Na concentration, which was significantly correlated with the fall in mean blood pressure produced by the treatment [8]. Other authors reported that ketanserin, when administered to normal subjects, decreases the intraerythrocyte Na content and the activity of ouabain-sensitive s6 Rubidium uptake (a marker of Na/K-ATPase) [6,7]. Although previous experiments have pointed out that 5HT has a role in the regulation of cation concentration in platelets [11] and in endothelial cells [12], our study did not show any effect upon erythrocyte sodium transport systems.…”

Section: Discussionmentioning

confidence: 99%

“…This study indicates that ketanserin has a direct influence on transmembrane sodium fluxes. If this action were also present in other cells, it might contribute to the actions of the drug at vascular, nervous, and renal tubular levels.tration by affecting the activity of some sodium transport mechanisms [6][7][8][9]. The aim of this studywas to evaluate, in vitro, the effect of the serotonergic system on transmembrane sodium transport.…”

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Evidence for a direct and non-receptor-mediated action of 5HT2 antagonists on transmembrane cation transport systems

Sechi

Tedde

Cassisa

et al. 1990

Cardiovasc Drug Ther

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Changes in transmembrane sodium fluxes have been reported in normotensive and in hypertensive subjects after ketanserin administration. In this study, the effects of the serotonergic system on transmembrane sodium transport mechanisms have been investigated in vitro. In erythrocytes drawn from ten healthy subjects, we studied the effects of serotonin (5HT) on the Na/K pump, Na/K cotransport, Na/Li countertransport, and passive permeability of Na. No significant changes were found. A direct, non-receptor-mediated action of ketanserin was then suspected, and the effects of two concentrations of ketanserin (5 x 10(-8) and 5 x 10(-7) M) were evaluated in erythrocytes from 12 normal volunteers. Both concentrations of ketanserin significantly decreased the activity of the Na/K pump and increased the activity of Na/Li countertransport. Na/K cotransport and passive permeability were not affected. Indirect evidence of the action of ketanserin on sodium transmembrane fluxes came from other experiments. In the red blood cells taken from five normal subjects and incubated for 2 hours in a plasma pool, we evaluated the changes in intracellular sodium concentration induced by the presence of 5HT or ketanserin. A significant decrease in intracellular sodium concentration occurred only with ketanserin. This study indicates that ketanserin has a direct influence on transmembrane sodium fluxes. If this action were also present in other cells, it might contribute to the actions of the drug at vascular, nervous, and renal tubular levels.

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Serotonin and Serotonin Antagonism in Cardiovascular and Non‐Cardiovascular Disease

Frishman

Huberfeld

Okin

et al. 1995

The Journal of Clinical Pharma

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Serotonin, or 5-hydroxytryptamine, is a naturally-occurring vasoactive substance found primarily in the brain, enterochromaffin tissue, and blood platelets. It has diffuse cardiophysiologic effects. The multiple effects of serotonin on blood vessels can be explained by the existence of 2 serotonergic receptor subtypes (the S1 receptor mediates vasodilation, and the S2 receptor vasoconstriction). Serotonin via the S2 receptor also augments the actions of several other vasoconstricting substances. Serotonin may be responsible for causing, or at least perpetuating, some forms of systemic hypertension through peripheral and central nervous system (CNS) actions. Ketanserin is a highly selective S2-serotonergic antagonist with additional alpha-adrenergic blocking activity, which has been proposed as a therapy for various cardiovascular diseases including hypertension. It has been shown to be more effective than placebo in treating hypertension and comparable in effectiveness to other antihypertensive drugs. Its major side effects relate to the CNS, and prolongation of the electrocardiogram QT interval has been described. Caution must be used when using ketanserin in patients receiving potassium- and magnesium-losing agents, because of the risk of torsades de pointes. Ketanserin has potential utility in the treatment of eclampsia, peripheral vascular disease, carcinoid syndrome, and "shock lung." The drug is not yet approved for clinical use in the United States.

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Ketanserin and Red Blood Cell Sodium Content in Hypertension

Cited by 11 publications

References 0 publications

Effects of carvedilol on common carotid arterial flow, peripheral hemodynamics, and hemorheologic variables in hypertension

Effects of carvedilol on common carotid arterial flow, peripheral hemodynamics, and hemorheologic variables in hypertension

Evidence for a direct and non-receptor-mediated action of 5HT2 antagonists on transmembrane cation transport systems

Serotonin and Serotonin Antagonism in Cardiovascular and Non‐Cardiovascular Disease

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