Ketanserin: A novel cardiovascular drug

Symoens, J.; Janssens, Monique

doi:10.1002/ddr.430080119

Cited by 15 publications

(8 citation statements)

References 51 publications

(45 reference statements)

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“…Interestingly, in this trial, both ketanserin and captopril treatment as monotherapy produced similar and highly significant hypotensive effects, without inducing reflex activation of the sympathetic nervous system or sodium retention, with response rates ranging from 50% to 58% and the proportion of normalized patients ranging from 17% to 25%. These findings confirm the clinical efficacy and the known humoral effects of ketanserin and captopril when used as monotherapy [4][5][6]. Furthermore, the findings indicate that combined therapy is often needed to obtain more effective control of blood pressure in patients with moderate hypertension.…”

Section: Discussionsupporting

confidence: 75%

Ketanserin and captopril interaction in the treatment of essential hypertensives

Lavezzaro¹,

Ladetto²,

Valente³

et al. 1990

Cardiovasc Drug Ther

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The aim of the study was to evaluate whether the combination of ketanserin with captopril exerts an additive antihypertensive effect, as compared with single drug treatment. Twelve patients with uncomplicated moderate essential hypertension received, according to a randomized, double-blind, crossover design, ketanserin (40 mg twice daily), captopril (50 mg twice daily), the combination of the two drugs at these dosages, and the corresponding placebo, each treatment being given for 1 month. Both ketanserin and captopril as monotherapy similarly and significantly reduced blood pressure as compared with placebo (p less than 0.001). The combination treatment of ketanserin plus captopril further and significantly reduced blood pressure when compared with single drug treatment (p less than 0.001). Moreover, the percentage of responders and patients whose blood pressure was normalized were significantly greater under the combined treatment than under ketanserin or captopril monotherapy (p less than 0.001). These data indicate that the combination of ketanserin plus captopril exerts a clear additive antihypertensive effect when compared with each treatment as monotherapy, a finding that suggests this combination can be usefully employed in the treatment of hypertensive patients.

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Section: Discussionsupporting

confidence: 75%

Ketanserin and captopril interaction in the treatment of essential hypertensives

Lavezzaro¹,

Ladetto²,

Valente³

et al. 1990

Cardiovasc Drug Ther

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“…Elderly subjects are more vulnerable to these unwanted actions. Ketanserin seems to be a potent antihypertensive agent, with a favorable effect on LVH and no demonstrable serious side effects [10]. Thus, in elderly hypertensives with LVH, ketanserin may be considered as a first-line medication.…”

Section: Discussionmentioning

confidence: 99%

Left ventricular hypertrophy regression and function changes with ketanserin in elderly hypertensives

Vyssoulis

Karpanou

Pitsavos

et al. 1990

Cardiovasc Drug Ther

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Ketanserin is a serotonin antagonist with age-related antihypertensive efficacy. Its effects on left ventricular (LV) function and hypertrophy have not been adequately reported. We studied noninvasively 54 elderly hypertensives before and 6 months after ketanserin monotherapy. Mean blood pressure was controlled (174/101 to 145/86 mmHg, p less than 0.0001) with no heart rate changes. LV dimensions and volumes remained unchanged, as did all LV ejection indices, thus preserving LV output (p = ns). Total peripheral resistances fell (from means of 1986 to 1615 dynes, cm.s-5, p less than 0.0001), as did LV systolic wall stresses. Mean LV mass was reduced (248 to 237 g, p less than 0.0001), mainly due to interventricular septum thinning (11.8 to 11.1 mm, p less than 0.0001), resulting in a decrease in mean LV cross-sectional area (21.3 to 20.5 cm2, p less than 0.0001) and mass/volume ratio (2.14 to 2.01 p = 0.0001). Thus, LV hypertrophy regression did not affect contractility (LV mass index relation to stress/end-systolic volume index, r = -0.558 before and r = -0.564 after ketanserin therapy). It is concluded that ketanserin is an effective antihypertensive agent in the elderly that reduces LV hypertrophy indices and maintains cardiac output, with no concomitant burdening on LV hemodynamics.

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“…137 In a few early studies using higher doses (60 mg or more per intake), side effects, predominantly drowsiness, fatigue, dizziness, and head- Severe Adverse Events A systematic screen in the 1636 patients with essential hypertension for whom individual case record forms were available indicated that the incidence of severe events was not higher with ketanserin than with placebo treatment (Table 6). 236 However, eight cases of reversible ventricular tachycardia, five of the torsade de pointes type, were reported in the approximately 18,000 patients (see Table 2) treated so far with ketanserin. All eight cases had other factors possibly contributing to the development of the arrhythmia (Table 7).…”

Section: Complaints and Adverse Events Complaintsmentioning

confidence: 99%

Serotoninergic mechanisms in hypertension. Focus on the effects of ketanserin.

et al. 1988

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SUMMARY Aggregating platelets release serotonin, which induces contraction of most vascular smooth muscle by activation of Sj-serotoninergic receptors. Serotonin released in the circulation may contribute to the increase in peripheral resistance of hypertension as the responsiveness of blood vessels from hypertensive animals and humans to the vasoconstrictor action of the monoamine is augmented. The data obtained with the new antihypertensive agent ketanserin may favor that interpretation. Ketanserin is a selective S 2 -serotoniiiergic antagonist with additional ai-adrenergic blockmg properties. In humans, it has a terminal half-life of 12 to 25 hours and is eliminated predominantly by the liver. The hemodynamic profile of ketanserin is that of a vasodilator drug with actions on both resistance and capacitance vessels. On short-term intravenous administration, it lowers blood pressure in hypertensive patients with minimal reflex changes In cardiovascular function. When given orally long term to hypertensive patients, ketanserin causes a sustained reduction in arterial blood pressure, comparable to that obtained with either /3-adrenergic biockers or diuretics. Several studies have shown a greater efficacy in older (> 60 years of age) than in younger patients independent of starting pressure. Side effects mainly consist of dizziness, somnolence, and dry mouth, but they are usually not severe. The mechanism underlying the antihypertensive effect of ketanserin is unclear. It cannot be attributed to either S 2 -serotoninergic or a,-adrenergic blockade alone, but an interaction between the two effects appears to be required.

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Ketanserin: A novel cardiovascular drug

Cited by 15 publications

References 51 publications

Ketanserin and captopril interaction in the treatment of essential hypertensives

Ketanserin and captopril interaction in the treatment of essential hypertensives

Left ventricular hypertrophy regression and function changes with ketanserin in elderly hypertensives

Serotoninergic mechanisms in hypertension. Focus on the effects of ketanserin.

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