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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

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

A persistent pulmonary artery hypertension, increased airways resistance, increased vascular permeability to protein, and hypoxia are characteristic of sepsis-induced ARDS in humans and are present in the late phase injury response seen in sheep after endotoxin. Our purpose was to determine the role of serotonin, 5-HT, in the steady-state pulmonary hypertension and decreased arterial oxygen tension seen beginning approximately 3 h after Escherichia coli endotoxin injury (2 micrograms/kg) in the adult sheep. Plasma 5-HT levels remained constant, whereas lung lymph values increased from a baseline of 60 +/- 40 to 180 +/- 70 and 270 +/- 90 ng/ml at 1-h and at 3- to 5-h periods, respectively, after endotoxin. Platelet count decreased significantly only at the 3-h time period. Ketanserin, a 5-HT antagonist, was infused (0.15 mg/kg/h) in 7 sheep during endotoxin injury. The degree of early pulmonary hypertension and hypoxia was not affected by ketanserin. Mean values for pulmonary artery pressure and arterial oxygen tension were 40 +/- 8 mmHg and 70 +/- 8 torr for endotoxin alone and 38 +/- 7 mmHg and 72 +/- 7 torr for the ketanserin group. Steady-state, protein-rich pulmonary perfusion was also not altered, being increased 3-fold in both groups. Pulmonary hypertension and hypoxia were significantly attenuated, however, at the 3- to 5-h period with ketanserin, compared with endotoxin alone, the pulmonary artery pressure decreasing from 29 +/- 5 to 22 +/- 4 mmHg and the PaO2 increasing from 75 +/- 4 to 83 +/- 5 torr.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Relationship of increased lung serotonin levels to endotoxin-induced pulmonary hypertension in sheep. Effect of a serotonin antagonist. 293 13

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.
Hypertension 1986 Feb
PMID:Chronic effect of ketanserin in mild to moderate essential hypertension. 293 97

Ketanserin is a pure antagonist of serotonin S2-receptors, in blood vessels, platelets and bronchial tissue. Ketanserin has been suggested as hypotensive drug in man, but it shows as well a specific activity on platelet aggregation. An increased incidence of hypertension, of unknown origin, has been found in patients with chronic alcoholism: hypotheses have been made upon an increased incretion of catecholamines and a greater sensitivity of blood vessels' receptors to their action. The data from the present study of eleven patients show that these subjects had an increased platelet activity and ketanserin administration was effective in allowing both the blood pressure levels and platelet activity to resume their normal range. This drug is thus suggested, for its pharmacological properties, as an elective medication for hypertensive patients with chronic alcoholism.
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PMID:Ketanserin (S2-receptor blocking agents), hypertension and chronic alcoholism. 293 47

Ketanserin is a new potent antiserotonergic drug which, unlike previous ones, is selective for S2-serotoninergic receptors and does not have an agonist action. A trial was carried out on medium-term treatment with ketanserin or propranolol in subjects suffering from mild to moderate hypertension. The trial was designed as a double-blind crossover randomized study comparing either ketanserin or propranolol with placebo. Thirteen patients completed the study, which was divided into two groups (A and B). Systolic (SBP), diastolic (DBP) and mean (MBP) blood pressures were measured by non-invasive, intermittent ambulatory monitoring performed using a Pressurometer II, from Del Mar Avionics. Heart rate was measured using a continuous electrocardiogram monitoring. Systolic blood pressure was significantly reduced both after ketanserin (A:11.1%; B:10.8%) and propranolol (A:11.7%; B:11.8%) but in group A its decrease was more pronounced after propranolol (P less than 0.01). Diastolic blood pressure was significantly reduced both after ketanserin (A:11.5%; B:11.1%) and propranolol (A:11.4%; B:11.9%), as was MBP (A:11.9%; B:11.8% for ketanserin and A:11.9%; B:11.9% for propranolol). The heart rate diminished significantly only after propranolol administration (P less than 0.01). Ambulatory monitoring showed a significant 24-h reduction of SBP after administration of propranolol (P less than 0.0025) and ketanserin (A:P less than 0.0025, B: P less than 0.005). Diastolic blood pressure was also significantly reduced after ketanserin (P less than 0.0005) and propranolol (A: P less than 0.0025, B: P less than 0.0005). The heart rate obtained by continuous electrocardiogram monitoring diminished significantly only after propranolol administration (P less than 0.0005). No significant changes of circadian behaviour of blood pressure were observed.
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PMID:Effects of ketanserin on ambulatory blood pressure monitoring in patients with essential hypertension. 293 8

In a randomized double-blind study with parallel design involving 20 hypertensive patients, the antihypertensive activity and effect on platelet function of ketanserin have been compared with those of atenolol. Patients in both treatment groups were matched for age, body weight, duration of hypertension and blood pressure values on placebo. After 12 weeks of oral treatment, both ketanserin and atenolol significantly reduced blood pressure from 183/113 and 187/111 mmHg, at the end of the placebo run-in period, to 159/91 and 169/99 mmHg, respectively (P less than 0.05). No significant differences were noted between the hypotensive effect of both drugs. In contrast to ketanserin, atenolol significantly reduced the heart rate after 12 weeks of therapy (P = 0.025). Ketanserin significantly inhibited serotonin-induced platelet aggregation and serotonin uptake by thrombocytes, whereas atenolol failed to alter these variables. The results indicate that the antihypertensive activity of the serotonin antagonist ketanserin is comparable with that of the beta-receptor blocker atenolol.
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PMID:Double-blind comparison of ketanserin with atenolol: antihypertensive activity and effect on platelet function. 293 16

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

The antihypertensive effects of intravenous injection of ketanserin, a 5-HT2 receptor antagonist, were assessed in conscious rabbits. In intact rabbits, ketanserin lowered blood pressure in a dose-dependent manner. The antihypertensive effects of ketanserin were also observed in rabbits with two-kidney, one clip (2K1C) hypertension and with one-kidney, one clip (1K1C) hypertension. The effect was more marked in the 1K1C rabbits with low plasma renin activity (PRA) and high plasma norepinephrine (PNE) than in 2K1C rabbits with high PRA and normal PNE. The heart rate was not changed. Ketanserin suppressed the pressor response to exogenous norepinephrine (0.6 micrograms/Kg) 15, 30 and 45 min after the injection of ketanserin (1 mg/Kg). It also suppressed the pressor response to phenylephrine (3 micrograms/Kg) 15 min after the injection, but it did not suppress the pressor response to angiotensin II (0.15 micrograms/Kg). In order to investigate baroreceptor function, balloons were placed around the abdominal aorta and the inferior vena cava and inflated alternately. Thus, the mean arterial pressure vs heart period-logistic curve was obtained under steady-state conditions. There were no changes after the drug administration in the range of heart period and the gain (the slope at midpoint of the curve). These results suggest that the inhibition of pressor response of norepinephrine has effects in addition to a direct vasodilatory action and that an alteration of baroreceptor function is not involved in the antihypertensive effects of ketanserin.
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PMID:Cardiovascular effects of ketanserin in conscious rabbits. 294 1

Ketanserin is a new strong antiserotoninergic drug that, unlike the previous ones, is selective for 5-hydroxytryptamine receptors. This drug has been employed successfully in the treatment of arterial hypertension and of some peripheral vascular diseases. The authors are carrying out a trial on medium term treatment with ketanserin (K) or propranolol (P) in comparison with placebo, to evaluate their effects on blood pressure, haemocoagulative parameters and peripheral circulation. The trial is a double-blind cross-over random trial on subjects with mild or moderate hypertension. Until now 13 patients have ended the study; six of them are suffering from arteriosclerosis obliterans of the lower limbs at 1st or 2nd stage according to Fontaine. Both propranolol and ketanserin significantly reduced the blood pressure, although the decrease in systolic blood pressure was more evident after propranolol. Heart rate diminished significantly only after propranolol administration. The noninvasive, intermittent (every 30 min) monitoring of blood pressure showed a significant 24-hour reduction of blood pressure after administration of propranolol or ketanserin without significant changes of circadian behaviour of the blood pressure. After administration of ketanserin a slight improvement in peripheral circulation was demonstrated, evaluated by using strain-gauge plethysmography. As regards the results obtained for platelet function and other haemocoagulative parameters examined, adenosine diphosphate-induced platelet aggregation, adenosine diphosphate slope, collagen lag period, antithrombin III biological activity, and serum fibrinogen did not show noticeable modifications after treatment, while beta-thromboglobulin levels decreased slightly after ketanserin administration.
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PMID:Effects of ketanserin on blood pressure, peripheral circulation and haemocoagulative parameters in essential hypertensives with or without arteriosclerosis obliterans of the lower limbs. 294 85

Ketanserin is an agent whose main pharmacologic action is antagonism of serotonin (5-hydroxytryptamine, 5HT) receptors of the 5HT2 subtype. It also has weak alpha 1-adrenergic blocking properties, which may contribute to the acute blood pressure lowering effects seen in animal models of hypertension. During chronic treatment of hypertension in animals, the 5HT2 antagonistic properties, or a combination of 5HT2 and alpha 1-antagonistic effects, seems to be responsible for ketanserin's hypotensive action. Studies of patients with hypertension have demonstrated the therapeutic effects of ketanserin in monotherapy and combination therapy. In humans, the drug has a terminal half-life of 12-25 hours, and a twice daily dosage will lower blood pressure over the day. Ketanserin is a vasodilator that acts on both resistance and capacitance vessels. Chronic treatment with the drug causes minimal reflex changes in cardiovascular function, as well as sustained blood pressure reduction comparable with the effects of beta-adrenergic blockers or diuretics. In elderly patients, the therapeutic effects of ketanserin appear to be greater, and side effects are less frequent compared with beta-blockers and diuretics. In addition to its antihypertensive action, ketanserin also produces other effects that may be important in reducing cardiovascular morbidity and mortality in patients with hypertension. Some studies have shown a reduction in total and low-density lipoprotein (LDL) cholesterol, and a rise in high-density lipoprotein (HDL) cholesterol. Ketanserin also reduces ex vivo platelet aggregation and inhibits the serotonin-induced platelet release reaction. Worldwide experience with ketanserin in the treatment of hypertension indicates that it is a safe and effective agent for long-term therapy.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Effects of a new serotonin antagonist, ketanserin, in experimental and clinical hypertension. 304 35


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