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Query: UMLS:C0085580 (essential hypertension)
 14,686 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The antihypertensive efficacy and tolerability of the 5HT2-receptor antagonist ketanserin was investigated in 188 patients aged 41 to 82 years with mild to moderate essential hypertension. Ketanserin was given as monotherapy (n = 107) as well as in combination with either the diuretic hydrochlorothiazide/amiloride (n = 42) or the betablocker atenolol (n = 39) for 12 weeks. Compared to placebo, ketanserin lowered systolic blood pressure by 11 +/- 16 (SD), 9 +/- 13 and 9 +/- 11 mm Hg (p less than 0.01 for all) and diastolic blood pressure by 9 +/- 10, 10 +/- 9 and 7 +/- 9 mm Hg (p less than 0.001 for all), in the three treatment groups; body weight, serum sodium, potassium, uric acid, cholesterol and triglycerides remained unchanged. The incidence of withdrawals due to unwanted effects was 4% on ketanserin monotherapy, and 12% and 10% on the diuretic/ketanserin and the betablocker/ketanserin combination respectively. Well-being during ketanserin therapy was improved in the older patients in particular; sleep disturbances, daytime fatigue and overall weakness decreased. Ketanserin was well tolerated in combination with the diuretic, whereas in combination with the betablocker the occurrence of dry mouth and stuffy nose was slightly higher. - Ketanserin proved to be an effective antihypertensive drug comparable to other blood pressure lowering agents. It can be combined advantageously with a potassium sparing diuretic or a betablocker. The greater efficacy and tolerability in patients greater than or equal to 60 years qualify ketanserin primarily as an antihypertensive agent for older patients.
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PMID:[Blood pressure lowering action and tolerance of ketanserin in mono- or combination therapy]. 271 Nov 55

Serotonin (5HT) has been implicated in thromboembolic complications and blood pressure elevation and both may be reduced with the 5HT2-receptor blocker ketanserin. In 17 patients with essential hypertension (WHO I and II, diastolic pressure V greater than or equal to 100 mmHg) blood pressure, platelet 5HT uptake, content and release as well as 5HT-induced shape change and aggregation were measured before and immediately after 8 weeks oral ketanserin at 20-40 mg twice daily. During ketanserin therapy, platelet 5HT release, shape change reaction and aggregation to 5HT were significantly reduced by more than 50%. These platelet effects were more pronounced in patients responsive to ketanserin (greater than or equal to 10% decrease of diastolic pretreatment pressure) and the fall in diastolic pressure correlated with the inhibition of 5HT-induced aggregation as well as the change in 5-hydroxy-indoleacetic acid (5HIAA) in platelet-rich plasma (PRP; P less than 0.05). Serotonin-receptor-independent platelet events were not affected by ketanserin. Ketanserin corrects 5HT2-receptor-mediated platelet function along with the reduction of blood pressure.
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PMID:Platelet deactivation by 5HT2-receptor blockade parallels the antihypertensive response to ketanserin. 272 27

The effects of ketanserin on blood pressure and well-being were investigated in 188 patients, aged 41-82 years, with mild to moderate essential hypertension. At entry, 107 were untreated, 42 were taking the diuretic combination hydrochlorothiazide (50 mg/day) plus amiloride (5 mg/day) and another 39 were taking the beta-blocker atenolol (100 mg/day). A single-blind, 4-week placebo run-in period was followed by 12 weeks' oral ketanserin treatment at 20 or 40 mg twice a day. This regimen significantly reduced systolic and diastolic blood pressures in each group. Response rates were greater in patients aged over 60 years. Compared with placebo, sleep disturbances, daytime fatigue and overall weakness decreased during ketanserin treatment (P less than 0.05 for all), but the incidence of dry mouth and stuffy nose increased. In patients older than 60 years there was a greater reduction of complaints than in younger patients. Ketanserin proved effective and well tolerated, improving peripheral circulatory symptomatology, particularly in older patients and those with a good blood pressure response.
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PMID:Antihypertensive efficacy and well-being during monotherapy and combination therapy with ketanserin. 280 91

It remains to be established whether ketanserin's antihypertensive effect is caused by blockade of serotonergic type 2 receptors (S2), by blockade of alpha 1-adrenoceptors or by combined effect on both receptors. We therefore performed several clinical studies. Ketanserin, 10 mg i.v., lowered blood pressure in 6 patients with essential hypertension and blocked, at the same time, the contraction of hand veins to exogenous serotonin. In contrast, ketanserin had no effect on the venoconstrictor action of noradrenaline. Ketanserin also did not alter the pressor effect of bolus injections of the alpha 1-agonist phenylephrine. Furthermore, ketanserin had a distinct hypotensive effect in 4 normotensive patients with autonomic insufficiency who were unresponsive to alpha 1-adrenoceptor blockade. Moreover, the ketanserin-induced marked increase in digital blood flow in 7 patients with Raynaud's phenomenon was not blocked by pretreatment with high doses of the alpha 1-adrenoceptor blockade. However, in patients with essential hypertension, the antihypertensive effect of ketanserin was blunted by pretreatment with prazosin. This may be related to S2 blockade of the alleged amplifying effect of serotonin on alpha 1-adrenoceptor mediated vasoconstriction but the data do not exclude concomitant alpha-blockade by ketanserin. We conclude that the mechanism of ketanserin's antihypertensive effect requires further clarification; nevertheless the data cited above do not support the view that ketanserin is nothing more than another alpha-blocker.
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PMID:Mechanism of action of ketanserin in hypertension and vasospastic disease. 282 6

We evaluated the long-term antihypertensive effects of ketanserin, a selective serotonin2-receptor blocker with weak adrenergic receptor blocker properties. Ketanserin was given alone, 40 mg o.d. or b.i.d., for 2 years to 12 patients with essential hypertension. Systolic and diastolic blood pressures (BPs) were significantly reduced 14 days after the start of therapy and remained lowered during the 2-year follow-up period. In a larger group of patients who received ketanserin monotherapy for 2 to 3 months, the response to therapy varied considerably between subjects, with an overall response rate (BP less than 165/95 mm Hg) of 60% to 75%. During steady-state conditions, the maximum and minimum ketanserin plasma concentrations varied from threefold to fourfold between subjects and did not correlate with individual reductions in BP, but for each individual there was a positive correlation between BP reduction and ketanserin plasma concentration throughout a study day. In combination with beta-blockers, ketanserin effectively reduced BP in the supine and standing positions. The plasma concentration profile was not altered as much during combination therapy as when ketanserin was given alone. Side effects were few and tolerable. Ketanserin effectively reduces BP both alone and in combination with beta-blockers and may be still another drug useful in the treatment of essential hypertension.
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PMID:Treatment of arterial hypertension with ketanserin in mono- and combination therapy. 286 30

The purpose of this study was to compare the effects of the serotonin antagonist ketanserin and the post-synaptic alpha-blocker prazosin on blood pressure in patients with essential hypertension. Both drugs lower blood pressure by a reduction in total peripheral vascular resistance and by reducing the pre- and afterload, apparently achieving these haemodynamic effects through different mechanisms. Ketanserin appears to have a greater effect on afterload. Six men and four women (mean age 47.2 years) with diastolic blood pressure greater than or equal to 100 mmHg were treated for 4 weeks with placebo and then randomized and treated for 8 weeks double-blind with either ketanserin or prazosin. A 4-week wash-out phase with placebo was then instituted followed by another 8 weeks of treatment in a crossover fashion with either ketanserin or prazosin. Blood pressure was measured on each occasion in the supine, sitting and standing positions. The results showed that both medications significantly lowered blood pressure (computed sitting values for all patients: ketanserin from 177/104 +/- 5/7 to 158/89 +/- 8/5 mmHg; prazosin from 176/103 +/- 11/8 to 156/88 +/- 6/4 mmHg). The data in this study show that ketanserin as an antihypertensive agent is as effective as prazosin, but in contrast requires no titration of dosage and better compliance can be expected with twice daily rather than three times daily dosing.
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PMID:Moderate essential hypertension control: a double-blind crossover study between a serotonin antagonist and a post-synaptic alpha-blocker. 287 Nov 45

The role of serotonin in the pathogenesis of hypertension is interesting, and its investigation is much in vogue at present. This study compared the hypotensive effect of ketanserin, a specific 5-hydroxytryptamine receptor antagonist, with metoprolol in essential hypertension. On a double-blind basis, one treatment group (19 patients on ketanserin) was compared with another (21 patients on metoprolol). There was a significant reduction in diastolic blood pressure with both ketanserin and metoprolol (P less than 0,001). Side-effects were insignificant. One patient on metoprolol and 2 on ketanserin complained of dizziness. The dose of ketanserin was 40 mg twice a day and that of metoprolol 100 mg twice a day. Ketanserin does not appear to cause abnormal haematological values or biochemical adverse effects. It can be given to hypertensive patients with cardiac failure or bronchial asthma without adverse effects and may improve the peripheral vascular status of a hypertensive patient.
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PMID:A comparative study of ketanserin and metoprolol in essential hypertension. 293 40

Ketanserin, an antagonist highly selective for 5-hydroxytryptamine (serotonin) type 2 (S2) receptors, was given as monotherapy in a dose of 40 mg b.i.d. to 24 subjects with mild to moderate essential hypertension. Its effects were evaluated in a placebo-controlled double-blind crossover study. The effect on blood pressure in 18 subjects was monitored by 24-hour ambulatory intra-arterial measurements. Systolic and diastolic intra-arterial pressures were significantly lowered by ketanserin both during the day and at night, whereas heart rate was unchanged. Cuff pressure readings (triplicate measurements) with the London School of Hygiene sphygmomanometer and an automatic device (12 measurements in 1 hour) in the outpatient clinic also showed a significant effect on both supine and standing pressures. No postural hypotension was noted. Ketanserin had no effect on endogenous creatinine clearance, serum cholesterol levels, and the plasma levels of norepinephrine, renin, and aldosterone. The only side effect that was significantly more common with ketanserin than with placebo treatment was an increase in body weight. Ketanserin may have a place in the treatment of mild to moderate essential hypertension.
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PMID:Chronic effect of ketanserin in mild to moderate essential hypertension. 293 97

This study was designed to compare the antihypertensive effectiveness of ketanserin (K) and metoprolol (M) in a 3-month double-blind treatment, and to assess the long-term efficacy of K in a 1-year open trial. Twenty-four patients with mild to moderate hypertension were randomly placed in two groups: group 1 (n = 11) received K, 40 mg/day, and group 2 (n = 13) received M, 200 mg/day. In the double-blind phase of treatment both K and M significantly lowered blood pressure (BP) (P less than 0.01). The heart rate was significantly decreased by M (P less than 0.01). In the 1-year follow-up, patients were divided into three groups: group I (n = 7) had been previously treated with K and maintained on K; group II (n = 4) was given K plus M (these patients had previously been treated with K, but K had failed to decrease diastolic BP to less than or equal to 90 mmHg); and group III (n = 13) was given K (previously these patients had been treated with M). In group I, the BP lowering effect remained constant throughout the 1-year follow-up. In group III, supine and standing diastolic BP decreased significantly after treatment with K (P less than 0.05). Side effects from K were minimal. Ketanserin appears to be a new alternative approach in the treatment of mild and moderate essential hypertension.
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PMID:Ketanserin versus metoprolol in the treatment of essential hypertension. 293 18

Ketanserin (K), a selective and specific S2-receptor antagonist, has been compared with metoprolol (M), a cardioselective beta-blocker, in a double-blind study in order to assess its efficacy and safety in the treatment of essential hypertension. After a placebo run-in period of 4 weeks, hypertensive patients [supine diastolic blood pressure (DBP) greater than or equal to 100 mmHg] were treated with K, 40 mg twice daily (n = 18), or with M, 100 mg twice daily (n = 14). Systolic pressure (SBP) and DBP, both supine and standing, were significantly reduced from the first month of treatment by both drugs and remained stable for the whole study period (12 weeks). About two-thirds of the patients treated with K responded to the therapy (drop in DBP of at least 10%) and half were normalized (DBP less than or equal to 90 mmHg). In the M group, 50% of patients responded and 30% were normalized. A significant decrease in the heart rate was observed with M, but not with K. Ten patients treated with K were followed for 1 year. The antihypertensive effect of K was maintained throughout the study with evidence of tolerance. No serious adverse reaction was observed.
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PMID:Clinical experience with ketanserin in the treatment of hypertension. 293 19


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