Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0012833 (dizziness)
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In a double-blind 3-month study in mild-to-moderate essential hypertensive patients over 50 years of age, ketanserin, a selective S2-serotoninergic antagonist with additional alpha 1-adrenergic blocking properties, has been compared with enalapril, an angiotensin-converting enzyme inhibitor. Supine and upright blood pressures and heart rates were recorded for placebo and during active treatment (-4, -2, 0, 2, 4, 6, 8, 10, and 12 weeks). Metabolic profile (plasma glucose, creatinine, sodium, potassium, total and HDL-cholesterol, triglycerides, uric acid) was monitored during treatment with placebo and at the end of the study. Mean blood pressure was equally and significantly (p less than 0.001) lowered by both drugs from 2 weeks of treatment, whereas no changes occurred in mean heart rate or in biochemical variables. Dizziness was observed in three patients on ketanserin and in one patient on enalapril, whereas headache occurred in only one patient on enalapril. These data indicate that ketanserin is as effective and well tolerated as enalapril in hypertensive patients over 50 years of age.
Cardiovasc Drugs Ther 1990 Jan
PMID:Comparison of ketanserin and enalapril in the treatment of mild-to-moderate essential hypertension. 228 42

Seventeen subjects with essential hypertension (14 men, 3 women, 40-69 years of age), 13 of whom continued their previous antihypertensive therapy, completed a double-blind crossover trial of ketanserin 40 mg twice daily versus placebo tablets twice daily. Each treatment phase was 6 weeks in duration. For the group as a whole, blood pressure (BP) was reduced in the ketanserin phase compared with the placebo phase: supine mean BP decrease: 4 +/- 1 mm Hg (p less than 0.05); standing mean BP decrease: 7 +/- 1 mm Hg (p less than 0.001). Heart rate (HR) was also significantly decreased in the ketanserin phase (5 +/- 1 beats/min) (p less than 0.001). When individual subgroups were analysed, the reductions in BP and HR were greater in subjects already receiving antihypertensive therapy, diuretics, and/or beta-adrenergic blockers. Changes were observed in 24-h urine sodium and potassium excretion: Sodium (mmol/day): placebo 137 +/- 17, ketanserin 174 +/- 19 (p less than 0.05); potassium (mmol/day): placebo 74 +/- 8, ketanserin 57 +/- 5. For the group as a whole, there were no significant adverse effects during the ketanserin phase, although two subjects had a dose reduction of ketanserin because of drowsiness and dizziness. Two additional subjects withdrew from the study owing to adverse effects, one in the placebo phase. In conclusion, ketanserin in the dose administered has a modest hypotensive effect, which is best seen in subjects already receiving other antihypertensive agents.
J Cardiovasc Pharmacol 1985
PMID:Effect of ketanserin on blood pressure and biochemical parameters in patients with essential hypertension. 241 43

The clinical experience of 763 medical practitioners who treated 3,708 hypertensive patients (51% men) with indoramin, administered alone or in combination with diuretics and/or beta-adrenergic antagonists, is reported. All patients had baseline diastolic blood pressure (DBP) of 95 mm Hg or greater, even though most of the patients (62%) already were receiving optimum doses of diuretics (20%), beta-adrenergic antagonists (15%), or diuretics and beta-adrenergic antagonists (27%). After 6 to 10 weeks of indoramin therapy, the DBP of 70% of the patients was 90 mm Hg or lower; another 17% had treated DBP between 91 and 95 mm Hg. Response rates were similar among patients treated with indoramin alone and those who received concomitant antihypertensive treatment. Indoramin doses of 50 mg/day or less (dose range, 12.5 to 125 mg/day) were required in approximately 70% of the patients. Weight gain and reflex tachycardia were not observed. The most frequently reported side effects were drowsiness/tiredness, dizziness, and dry mouth. Only 6% of the patients discontinued indoramin treatment because of side effects. The results of this study indicate that indoramin, administered alone or in combination with diuretics and/or beta-adrenergic antagonists, is a safe and effective antihypertensive agent when used in relatively low doses in clinical practice.
J Cardiovasc Pharmacol 1986
PMID:Antihypertensive therapy in the Federal Republic of Germany: clinical practice experience with indoramin (Wydora). 242 96

In a multicenter, prospective study of step II antihypertensive therapy with indoramin, 1,847 hypertensive patients (773 men and 1,074 women) between the ages of 18 and 70 years were treated by 148 general practitioners. Patients whose blood pressure was inadequately controlled after 4 weeks of therapy with cyclopenthiazide (0.25 to 1.0 mg/day) had indoramin (25 to 200 mg/day) added to their treatment regimen. During cyclopenthiazide treatment, mean (+/- SD) blood pressure decreased from 176/105 +/- 20/7 mm Hg at baseline to 164/98 +/- 21/9 mm Hg (p less than 0.001), and only 447 (24%) patients obtained satisfactory blood pressure control. The addition of indoramin produced a further reduction in mean blood pressure from 169/102 +/- 18/6 to 152/89 +/- 18/8 mm Hg during the first 3 months of treatment (p less than 0.001); this response was maintained for up to 2 years. Satisfactory blood pressure reduction was achieved in 79% of the patients who received indoramin (mean dose, 68 mg/day) plus cyclopenthiazide. Only 25 patients (2%) discontinued indoramin treatment because of nonresponse, and 156 (12%) withdrew because of adverse effects, the most common being sedation, dizziness/giddiness, and headache. These results indicate that indoramin provides safe and effective blood pressure control when used as step II treatment for hypertensive patients who fail to respond to single-agent diuretic therapy.
J Cardiovasc Pharmacol 1986
PMID:Antihypertensive therapy with indoramin: risk-benefit profile in clinical practice. 242 97

The safety and efficacy of indoramin and prazosin added to hydrochlorothiazide (HCTZ) were compared in a double-blind trial involving 209 patients with mild to moderately severe essential hypertension. Patients whose supine diastolic blood pressure (SDBP) did not decrease to less than or equal to 90 mm Hg after 6 weeks of HCTZ therapy had indoramin or prazosin added to their regimen. Mean SDBP during 6 months of combination therapy with either regimen decreased by approximately 10 mm Hg from that at the final evaluation during HCTZ therapy (p less than 0.001); differences between the groups were not statistically significant. Mean heart rate was unchanged, whereas mean weight increased (p less than 0.001) above final HCTZ values by approximately 2 kg in both groups. Mean weight increased significantly (p less than 0.01) from baseline values, however, only in the prazosin/HCTZ group. Approximately 95% of the patients in each group had clinically significant decreases in SDBP. Fatigue or tiredness and dizziness were the most commonly reported adverse effects, and their frequencies were not significantly different in the two groups. Cardiac arrhythmias occurred only in patients in the prazosin/HCTZ group and were significantly (p less than 0.05) more frequent than among patients in the indoramin/HCTZ group; less severe adverse experiences, i.e., dry mouth, ejaculatory problems, drowsiness, and sedation, were significantly (p less than 0.05) more frequent in the indoramin/HCTZ group. When added to HCTZ, indoramin and prazosin are equally safe and effective in the treatment of hypertension.
J Cardiovasc Pharmacol 1986
PMID:Antihypertensive effects of indoramin and prazosin in combination with hydrochlorothiazide. 242 99

The antihypertensive efficacy and safety of indoramin, an alpha 1-adrenergic antagonist, were evaluated in 215 elderly patients. Data were collected from patients aged 60 years and older who were treated under similar protocols with indoramin administered alone (n = 58) or in combination with a thiazide diuretic (n = 157). After at least 6 months of treatment, the mean daily dosage of indoramin was higher among patients who received indoramin alone (122 mg/day) than among those who received indoramin plus a diuretic (92 mg/day). Mean supine blood pressure decreased (p less than 0.001) from 174/105 to 152/191 mm Hg in indoramin-treated patients and from 179/101 to 150/91 mm Hg in patients who were treated with indoramin plus a diuretic. Clinically satisfactory blood pressure decreases occurred in the majority of the patients who received indoramin, either alone (69%) or with a diuretic (75%). Both treatments were well tolerated by elderly patients; only 15 patients (7%) discontinued therapy because of adverse effects. Drowsiness, fatigue, and dizziness were the most frequently reported side effects. The results of this analysis indicate that indoramin, administered alone or in combination with a thiazide diuretic, is a safe and effective therapeutic regimen for elderly hypertensive patients.
J Cardiovasc Pharmacol 1986
PMID:Antihypertensive therapy with indoramin in the elderly. 242 7

This study evaluated the 24-h antihypertensive effect of single daily doses of celiprolol, a beta-1 adrenoceptor antagonist. Patients with supine diastolic BP between 95 and 114 mm Hg started on placebo or celiprolol 200 mg daily for 2 weeks; non-responders received 400 mg daily for 2 weeks and then 600 mg daily for another 2 weeks. Response was defined as a reduction of diastolic BP to 90 mm Hg or below. One hundred ninety patients were evaluated for efficacy, 114 in the celiprolol group and 76 in the placebo group, 84 men and 106 women, mean age 52 years. Blood pressure after 6 weeks fell from 165/103 to 149/92 on celiprolol and from 162/103 to 157/97 on placebo. The fall in systolic and diastolic BP after celiprolol is statistically different (p less than 0.001) from that after placebo. The pulse rate was reduced to a similar extent by the two treatments. The percent of patients with supine diastolic BP either reduced by at least 10 mm Hg or to 90 mm Hg or below, was 66% after celiprolol and 38% after placebo (p less than 0.001). The incidence of adverse reactions was comparable in the two groups: 31% during celiprolol, 25% during placebo. The most frequent reactions observed in both groups were gastrointestinal symptoms, dizziness, fatigue, headache. In conclusion, celiprolol proved to be a safe and effective beta-blocker in the treatment of mild and moderate hypertension.
J Cardiovasc Pharmacol 1986
PMID:A placebo-controlled double-blind multicenter study of celiprolol in the treatment of mild and moderate hypertension. 242 40

Ketanserin, the specific S2 serotonin antagonist, is undergoing evaluation for the therapy of hypertension of all degrees of severity. We studied 20 patients with severe hypertension [diastolic blood pressure (DBP) greater than 120 mm Hg after 40 min of supine rest]. In the first dose-ranging study on eight patients, multiple i.v. injections of 5 mg ketanserin were administered every 4 min (mean 38 mg). Only 4 patients responded adequately (DBP less than 100 mm Hg), 2 responded partially, and 2 did not respond to ketanserin. The major adverse effect of ketanserin, found in all patients, was severe dose-dependent sleepiness. A second double-blind crossover study with ketanserin and placebo (12 patients) assessed neural side effects. The supine DBP dropped from a mean of 134 +/- 4 mm Hg to 112 +/- 4 mm Hg 20 min after ketanserin when the sedation score rose from 0 to 1.2 +/- 0.3 (range 1-3) and the dizziness score from 0.1 +/- 0.1 to 1.4 +/- 0.3 (range 1-3; both p less than 0.01 vs. 1-2 min after ketanserin). Only 7 of 12 patients responded adequately to ketanserin. Twelve of the 20 patients were subsequently given nifedipine 10 mg sublingually; the DBP fell from a mean of 128 +/- 3 mm Hg to 101 +/- 4 mm Hg (p less than 0.001) after 40 min without side effects. Ketanserin does not appear to be a suitable agent for the acute therapy of severe hypertension because of: the imperfect and short-lived blood pressure control; the variability of the hypotensive effect; and sleepiness and dizziness as significant side effects.
J Cardiovasc Pharmacol 1987 Jan
PMID:Effects of intravenous ketanserin on severely hypertensive patients with double-blind crossover assessment of central side-effects. 243 87

Prazosin and terazosin are two alpha 1-adrenoceptor blocking agents, their principal difference being the longer half-life of terazosin. The present study was carried out to determine if elderly subjects are different from the young in their pharmacokinetic handling of these two drugs and if age influences the blood pressure response to each drug. Ten young healthy subjects (aged 19-30 years) and five older healthy subjects (aged 54-62 years) received 1 or 2 mg terazosin, 1 or 2 mg prazosin, or placebo 1 week apart according to a 5 X 5 Latin square design. Concentrations of prazosin and terazosin were measured using a high-performance liquid chromatographic procedure with a detection limit of approximately 0.25 ng/ml. Pharmacokinetic parameters of prazosin were virtually the same in both groups, whereas mean terazosin plasma concentrations were higher in the older group and pharmacokinetic analysis revealed higher peak plasma concentrations and a longer terminal elimination half-life. There was no evidence of increased sensitivity to the hypotensive action of the drug, as peak upright blood pressure falls were similar in the two groups. Symptoms of dizziness in the upright position were also less common. In view of their lack of sedative effects and minimal metabolic disturbances, further studies should be conducted to assess the suitability of these drugs as monotherapy for hypertension in elderly patients.
J Cardiovasc Pharmacol 1987 Aug
PMID:Effect of age on pharmacokinetics of and blood pressure responses to prazosin and terazosin. 244 Nov 67

Felodipine lowers blood pressure by reducing peripheral vascular resistance through a highly selective action on smooth muscle in arteriolar resistance vessels. The selective action may be considered a safeguard against untoward effects on cardiac contractility and conduction. Felodipine does not cause orthostatic hypotension since it has no effect in clinical doses on venous smooth muscle. Felodipine has a natriuretic/diuretic effect, which counteracts the salt and water retention that is often seen during treatment with other potent vasodilators. In clinical studies, felodipine has proved more effective than several established antihypertensive drugs. The combination of felodipine and a beta-adrenergic blocker appears to be a good alternative to standard triple treatment, and felodipine is often effective in patients with previously "refractory" hypertension. The antihypertensive effect of felodipine is dose related. In patients with moderate hypertension, a dose regimen of 5 mg twice a day is usually sufficient, and doses greater than 10 mg twice a day are not often required. Felodipine is generally well tolerated. The most common adverse effects are those expected from a potent arteriolar dilator: ankle swelling, headache, dizziness, flushing, etc. Adverse effects are usually transient or diminish in intensity with continued treatment. The overall frequency of adverse effects with felodipine appears to be similar to that for the established antihypertensive drugs, although the adverse effects differ. Felodipine is a potent arteriolar dilator with therapeutic advantages, especially for patients with moderate to severe hypertension.
J Cardiovasc Pharmacol 1987
PMID:Felodipine in hypertension--a review. 244 9


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