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

1 Doxazosin is a quinazoline derivative, related to prazosin, recently developed for the treatment of hypertension. 2 The intravenous administration of doxazosin (12 micrograms/kg) to six healthy normotensive subjects resulted in significant fall in erect blood pressure, with a corresponding increase in heart rate, but there were no significant changes in supine blood pressure or heart rate. 3 The changes in blood pressure and heart rate were maximal at 6 h after intravenous dosing. With prazosin the maximum effects occurred within the first hours. 4 Pressor response studies with phenylephrine confirmed that doxazosin is a relatively selective postsynaptic alpha-adrenoceptor antagonist. 5 The mean elimination half-life of doxazosin was 11 h. This compared with a T1/2 of 2.5 h for prazosin.
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PMID:A pharmacodynamic and pharmacokinetic assessment of a new alpha-adrenoceptor antagonist, doxazosin (UK33274) in normotensive subjects. 612 42

Controlled clinical studies have demonstrated that blockade of alpha 1-adrenergic receptors relaxes prostatic muscle tone and decreases the symptoms of benign prostatic hyperplasia (BPH). Doxazosin, a once-daily quinazoline derivative and postsynaptic alpha 1-adrenoceptor antagonist, proven as treatment for hypertension, was evaluated in the treatment of BPH in dosages of 1-16 mg. 456 BPH patients (287 doxazosin-treated and 169 placebo-treated) were evaluated for efficacy and safety in five double-blind, placebo-controlled clinical studies. Doxazosin treatment resulted in improvements in both urodynamic and symptomatic parameters associated with BPH. Efficacy was only assessed in 1, 2 and 4 mg. Adverse experiences were reported in 127 (44.3%) of the patients treated with doxazosin and in 49 (29%) of the patients treated with placebo. Fifteen (5.2%) doxazosin patients and 4 (2.4%) placebo patients withdrew from the studies due to adverse effects. Results from these five clinical trials demonstrate doxazosin is effective and safe and well tolerated in both normotensive and hypertensive patients with BPH.
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PMID:Efficacy and safety of the alpha-1 blocker doxazosin in the treatment of benign prostatic hyperplasia. Analysis of 5 studies. Doxazosin Study Groups. 750 24

Hypertension and benign prostatic hyperplasia (BPH) have a number of features in common. For example, both occur with increasing frequency in the elderly, and both are a major source of health expenditure worldwide. However, the most striking feature linking hypertension and BPH is the aetiological role of the sympathetic nervous system. Sympathetic tone mediated by the alpha-receptor is vital in the control of blood pressure. By selectively inhibiting the alpha 1-adrenoceptors in the vasculature, thereby inhibiting the response to epinephrine and norepinephrine and thus reducing peripheral resistance, selective alpha 1-inhibitors such as doxazosin produce a physiological reduction in blood pressure. Receptors of the alpha 1 subtype are also found in the prostate, the urethra and bladder neck. Doxazosin, by reducing the tone of the prostatic smooth muscle, has the potential to improve urinary flow rate, as well as the obstructive and irritative symptoms characteristic of BPH.
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PMID:Role of the sympathetic nervous system in hypertension and benign prostatic hyperplasia. 751 36

A number of studies have confirmed the beneficial effects of selective alpha 1-adrenoceptor inhibitors in patients with benign prostatic hyperplasia (BPH). Most produce clinically significant improvements in symptom scores and uroflow, although some of the shorter-acting agents often do so at the expense of adverse events. Doxazosin has a slower onset of action and longer plasma half-life than any other available selective alpha 1-adrenoceptor inhibitor, which may confer advantages in terms of tolerability over the more rapidly absorbed and eliminated selective alpha 1-adrenoceptor inhibitors. Doxazosin produces statistically significant increases in mean and maximum uroflow, as well as small but significant reductions in maximum voiding pressures and statistically significant improvements in symptoms of frequency, urgency, nocturia, reduced uroflow and sensation of incomplete emptying. Changes in uroflow and symptoms are similar in normotensive and hypertensive patients with BPH, and are accompanied in hypertensive patients by a statistically significant fall in blood pressure. Treatment is well tolerated in both normotensive and hypertensive patients. Doxazosin, by virtue of its unique pharmacological profile, is a valuable new treatment option for the many patients with mild to moderate bladder outflow obstruction due to BPH. It may be especially appropriate therapy for those considerable numbers of elderly men who have both hypertension and bladder outflow obstruction due to prostatic enlargement.
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PMID:Profile of doxazosin in the hypertensive man with benign prostatic hyperplasia. 751 38

Doxazosin is a long-acting alpha 1-adrenoceptor antagonist structurally related to prazosin and terazosin. Its antihypertensive effect is produced by a reduction in the smooth muscle tone of peripheral vascular beds resulting in a decrease in total peripheral resistance without significant effect on cardiac output or heart rate. In benign prostatic hyperplasia, doxazosin's effect of relieving bladder outflow obstruction is produced through a reduction in prostatic tone mediated via alpha 1-adrenoceptor blockade. In most comparative trials doxazosin has proven to be equally effective as the comparator drug in the treatment of mild to moderate hypertension. It has been used in a variety of patient populations including the elderly, Blacks, smokers, and patients with concomitant disease states such as renal dysfunction, hypercholesterolaemia, non-insulin dependent diabetes mellitus (NIDDM) and respiratory disease. Doxazosin has also been used successfully in combination with beta-adrenoceptor antagonists, diuretics, calcium channel antagonists, and angiotensin-converting enzyme inhibitors in patients with hypertension that is uncontrolled with monotherapy. Doxazosin has a beneficial effect on some of the risk factors associated with coronary heart disease including elevated serum lipid levels, impaired glucose metabolism, insulin resistance and left ventricular hypertrophy. Modest decreases in total cholesterol, low density lipoprotein cholesterol and triglycerides are seen with doxazosin therapy while small increases in high density lipoprotein cholesterol and the high density lipoprotein cholesterol/total cholesterol ratio are consistently reported. Some studies have reported an improvement in glucose tolerance although this effect has been more consistently seen in nondiabetic patients than in patients with NIDDM. Additionally, doxazosin produces a similar reduction in left ventricular hypertrophy to other antihypertensive agents. Modelling-based calculations suggest that doxazosin significantly reduces the risk of developing coronary heart disease in patients with mild to moderate hypertension, although this remains to be confirmed in long term prospective studies. Doxazosin appears to be a promising agent in the treatment of urinary symptoms associated with benign prostatic hyperplasia. Similar to other alpha 1-adrenoceptor antagonists, doxazosin treatment produces increases in peak and mean urinary flow rates and improves other objective and symptomatic measures.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Doxazosin. An update of its clinical pharmacology and therapeutic applications in hypertension and benign prostatic hyperplasia. 753 94

A total of 248 hypertensive patients 45 years old or older with benign prostatic hyperplasia (BPH) was included in this 16-week, multicenter, double-blind, placebo-controlled, parallel-group dose-response study. Doxazosin, a selective alpha 1-adrenoceptor antagonist, produced a significant increase in maximum urinary flow rate (2.3 to 3.6 ml. per second) at doses of 4 mg., 8 mg. and 12 mg., and in average flow rate (8 mg. and 12 mg.) compared with placebo. The increase in maximum flow rate was significant with doxazosin versus placebo within 1 week of initiating double-blind therapy. Doxazosin compared to placebo significantly decreased patient-assessed total, obstructive and irritative BPH symptoms. Blood pressure was significantly lower with all doxazosin doses compared with placebo. Adverse events, primarily mild to moderate in severity, were reported in 48% of patients on doxazosin and 35% on placebo. Our results strongly support the use of doxazosin as a nonoperative therapeutic alternative in the management of uncomplicated BPH. Doxazosin would also be particularly useful in the management of patients who have BPH and hypertension.
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PMID:Doxazosin for the treatment of benign prostatic hyperplasia in patients with mild to moderate essential hypertension: a double-blind, placebo-controlled, dose-response multicenter study. 753 56

Benign prostatic hyperplasia (BPH) and hypertension are both common conditions in older men. It is estimated that 20 to 41% of middle-aged to elderly men may have both. Alpha-1 adrenoceptor antagonists, such doxazosin, produce significant improvements in urine flow rate and symptoms in patients with BPH. The effect of doxazosin on urine flow rate and symptoms in hypertensive men with BPH is similar to that seen in normotensive men. By contrast, doxazosin produces a significant fall in blood pressure in hypertensive men, but has minimal effect in normotensives. Doxazosin is well tolerated, irrespective of blood pressure status. Thus, it can be concluded doxazosin is an effective and well tolerated treatment for BPH which appears to have additional benefits in the management of patients with concomitant hypertension.
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PMID:Efficacy of doxazosin in normotensive and hypertensive patients with benign prostatic hyperplasia. 754 49

Currently available data and clinical observations which suggest that there is a pathogenetic relationship between hypertension, diabetes mellitus, and atherosclerosis have provided a concept of the X syndrome, by which hypertensive patients, mainly males, have impaired insulin tolerance along with hyperinsulinemia and concurrent atherogenic disorders of lipid metabolism. The paper discussed the specific pathogenetic mechanisms, clinical manifestations, and prospects for drug correction of the metabolic syndrome. The treatment of arterial hypertension with the calcium antagonist Lomir has indicated there are no negative changes as a control of non-insulin-dependent diabetes mellitus in the presence of effective correction of arterial hypertension and atherogenic dyslipidemias. With the monotherapy of essential hypertension concurrent with hypercholesterolemia with the alpha 1-adrenoblocker Doxazosin, in addition to the agent's high antihypertensive effects, the authors noted its favourable action on lipid spectral parameters and platelet functional activity. There is abundant evidence for the use of specific hypolipidemic agents in patients with essential hypertensive refractory to current antihypertensive drugs. The data obtained with the use of Lescol (fluvastatin) in patients with hypertensive disease and hypercholesterolemia suggest that by substantially reducing the levels of total cholesterol, triglycerides, low density lipoprotein cholesterol and its transport protein apo B does not deteriorate the quality of correction of arterial hypertension in this group of patients.
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PMID:[Hypertension, diabetes mellitus, atherosclerosis: clinical manifestations of metabolic syndrome X. Prospects of pharmacological treatment]. 762 78

This is an open non-comparative study to evaluate the efficacy and tolerability of doxazosin mesilate in 540 subjects with either history or newly diagnosed mild/moderate hypertension. In all adult subjects of both sexes enrolled in this study, the diastolic blood pressure (DBP) was in the range of 95-115 mmHg at two different measurements both in clino- and orthostatism, in the absence of any heart pathology. Those patients who, after one-week wash-out period, reported DPB > or = 95 mmHg, were given doxazosin as a single daily dose. The initial dosage was 1 mg for three days; afterwards, patients have been instructed to take a whole 2 mg tablet in the morning up to the following visit (i.e. 14 days after the first administration). In case < or = 90 mmHg DBP control could not be obtained, the dosage has been increased to 4 mg and if after the same interval of time (i.e. 14 days) DPB control could not be achieved, the dosage was increased up to 8 mg (2 x 4 mg tablets) and/or the concomitant administration of another antihypertensive drug was instituted. At the beginning and at the end of the study blood collection for lipid profile determinations (total cholesterol, HDL cholesterol, LDL cholesterol, triglycerides), routine tests and complete urinalysis were performed. The onset of side-effects was reported in 84 (15.5%) subjects and only 13 (2.4%) of them had to discontinue the therapy. A comparative analysis of the incidence of side-effects between the total number of patients and those aged > or = 65 yrs. has not shown a significant difference. At week 24, a total of 540 subjects had completed the treatment. BP value normalization has been achieved with a mean dosage of 3.1 +/- 1.2 mg/day of doxazosin. Doxazosin administration did not produce clinically significant effects on heart rate. Laboratory data have evidenced a statistically significant increase in HDL cholesterol (p < 0.0001) and a significant reduction of mean values of total cholesterol, LDL cholesterol and triglycerides (p < 0.0001) at week 24, with respect to baseline. In the group of patients aged > or = 65 yrs. (116 patients) only a delta/percentage variation of HDL cholesterol with respect to baseline has been evidenced, after 24 weeks of treatment.
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PMID:[Doxazosin in the treatment of light-to-moderate arterial hypertension in a non-comparative multicenter study]. 770 11

Isolated Systolic Arterial Hypertension (ISAH) is the most frequent form of AHT in the aged population, resulting in an increase of the cardiovascular risk, mainly at the cerebrovascular level. In this open non-comparative study, we analyze the effect of doxazosin, an alpha-adrenergic blocker in 40 patients older than 60 years, diagnosed of isolated systolic hypertension. After 2 weeks of lavage, the patients received treatment with doxazosin according to a monotherapy scheme, with progressive increase of the dose, from 1 to 16 mg/day during a period of 14 weeks. Doxazosin significantly reduces the systolic and diastolic arterial pressure (p < 0.001) with a therapeutical response in 86.5% of the cases, using an average dose of 3.4 mg/day and without observing modifications in the heart rate. This drug improves the lipidic profile, with a reduction of the plasmatic levels of total cholesterol and cholesterol linked to low density proteins (LDL) with p < 0.05 and a reduction of triglycerides. Among the 40 patients included in the study, 10 (25%) referred side effects; there were 2 drop-outs (5%) and the dose had to be reduced in 2 patients (5%). In conclusion, doxazosin shows its antihypertensive effectiveness in the treatment of isolated systolic hypertension in patients older than 60 years and it is well tolerated by most of the patients, improving at the same time the lipidic profile. Hence, it contributes to the reduction of the cardiovascular morbidity-mortality in this group of patients.
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PMID:[Efficacy and tolerance of doxazosin in the treatment of isolated systolic hypertension in hypertensive patients over 60 years of age]. 779 18


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