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

Choosing antihypertensive agents that protect patients against cardiovascular and other complications is a growing trend in the treatment of mild to moderate hypertension. Calcium channel blockers and angiotensin-converting enzyme (ACE) inhibitors are favored because they have neutral or positive effects on lipid levels and insulin resistance. The alpha 1 blockers, especially doxazosin mesylate (Cardura), are enjoying a resurgence in popularity because they have a beneficial effect on lipid levels. In terms of preserving patients' quality of life, the ACE inhibitors in particular have been shown to have a positive impact. It has been shown that systolic hypertension in elderly patients should definitely be treated, but the most appropriate agent has yet to be defined. Therapy should be tailored to the individual. The following questions should be considered when choosing an antihypertensive agent: (1) What are its side effects (especially metabolic ones)? (2) Does it require only once- or twice-a-day dosing? (3) Does it cause regression of left ventricular hypertrophy? (4) Does it prevent death from coronary artery disease? (5) How will it affect quality of life? (6) How much does it cost? The goal of therapy should be to provide adequate blood pressure control throughout the day, enhance compliance, and protect the heart, brain, and kidneys without adversely affecting metabolic state.
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PMID:Antihypertensive therapy. Current issues and challenges. 134 44

The physicochemical properties, pharmacology, pharmacokinetics, cardiovascular and metabolic effects, adverse effects, dosage, and administration of doxazosin are described, and comparative clinical studies of doxazosin therapy in patients with mild to moderate hypertension are reviewed. Doxazosin mesylate, an alpha 1-adrenoceptor antagonist, is rapidly absorbed after oral administration and undergoes extensive hepatic metabolism. The drug decreases blood pressure by reducing peripheral resistance. Maximum hypotensive effects occur four to eight hours after the dose. Doxazosin favorably affects serum lipids by increasing concentrations of high-density lipoprotein (HDL) cholesterol, increasing the HDL:total cholesterol ratio, and decreasing concentrations of low-density lipoprotein cholesterol, total cholesterol, and triglycerides. In comparative clinical trials, doxazosin lowered standing and supine systolic and diastolic blood pressures as effectively as other alpha-adrenoceptor antagonists, beta-adrenoceptor antagonists, diuretics, angiotensin-converting-enzyme inhibitors, and calcium-channel-blocking agents. The most frequently reported adverse effects are dizziness, headache, nausea, lethargy, and fatigue. Doxazosin may be used either alone or in combination with a beta-adrenoceptor inhibitor or a diuretic. Orthostatic hypotension after the first dose occurs infrequently and may be minimized by initiating therapy at a dosage of 1 mg/day. The dosage may be increased at two-week intervals as needed, and blood pressure should be closely monitored. Doxazosin has blood-pressure-lowering effects comparable to those of other alpha 1-adrenoceptor inhibitors and to those of antihypertensives in other drug classes.
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PMID:Doxazosin: a new alpha 1-adrenergic antagonist. 134 55

In the present study we investigated the effect of a selective alpha 1-adrenergic blocker (doxazosin), an angiotensin-converting enzyme (ACE) inhibitor (captopril), and a calcium channel antagonist (nifedipine) on renal function in hypertensive non-insulin-dependent diabetic patients. 30 NIDD hypertensive patients (age = 50 +/- 3 years; BMI = 30 +/- 1 kg/m2) (mean +/- SEM) were studied before and after a 12-week period of antihypertensive treatment. Ten patients were treated with doxazosin (Cardura) (2-8 mg once daily or 8 mg b.i.d.), 9 with captopril (Capoten) (25-50 mg b.i.d.), and 11 with nifedipine (Procardia-XL) (30-60 mg once daily). Blood pressure, creatinine clearance, 24-hour urinary protein excretion, fasting plasma glucose concentration and glycosylated hemoglobin were measured before and after drug treatment. Fasting plasma glucose and glycosylated hemoglobin (HbA1c) were similar in all three groups prior to the start of antihypertensive therapy and did not change significantly from baseline in any treatment groups. In the doxazosin group creatinine clearance rose from 99 +/- 8 to 122 +/- 8 ml/1.73 m2.min (p < 0.01), while 24-hour urinary protein excretion declined from 2.66 +/- 0.05 to 1.76 +/- 0.02 mg/day/ml/1.73 m2.min (p < 0.01). In diabetics treated with captopril creatinine clearance rose from 93 +/- 6 to 109 +/- 9 ml/1.73 m2.min (p < 0.05), while the 24-hour urinary protein excretion fell from 2.70 +/- 0.05 to 2.03 +/- 0.04 mg/day/ml/1.73 m2.min (p < 0.05). In patients treated with nifedipine creatinine clearance did not change (97 +/- 6 vs. 94 +/- 7 ml/1.73 m2.min), while 24-hour urinary protein excretion decreased from 2.84 +/- 0.04 to 1.95 +/- 0.03 mg/day/ml/1.73 m2.min. Systolic and diastolic blood pressure were similar in doxazosin (150 +/- 3/95 +/- 2 mm Hg), captopril (153 +/- 3/93 +/- 1), and nifedipine (155 +/- 4/93 +/- 1) groups prior to the start of antihypertensive therapy and declined to 143 +/- 3/84 +/- 3 (doxazosin), 139 +/- 3/82 +/- 3 (captopril), and 141 +/- 3/84 +/- 1 (nifedipine) mm Hg (all p < 0.01 vs. pretreatment). In summary, both doxazosin and captopril treatment were associated with significant rises in GFR, while all three antihypertensive agents caused a significant decline in proteinuria. These results indicate that alpha-adrenergic blockers, ACE inhibitors, and calcium channel antagonists can safely and effectively be used in the clinical management of non-insulin-dependent diabetic patients with hypertension.
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PMID:Effect of alpha-adrenergic blockers, ACE inhibitors, and calcium channel antagonists on renal function in hypertensive non-insulin-dependent diabetic patients. 885 95

Doxazosin (Cardura-Pfizer) is a alpha 1-adrenoreceptor antagonist. This drug significantly decreases the blood pressure in subjects with hypertension. Despite decreasing blood pressure, doxazosin has a beneficial effect on many disorders observed in subjects with diabetes mellitus. Doxazosin 1) improves the regulation of lipids disturbances, 2) improves tissue sensitivity to insulin, 3) decreases the frequency of sexual disorders. In this situation Doxazosin is a good choice in the treatment of hypertension in diabetic subjects, in subjects with hypertension and hypercholesterolemia, with left ventricular hypertrophy, in old male subjects with hypertension and benign prostatic hypertrophy.
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PMID:[Use of doxazosin (Cardura-Pfizer), alpha 1-adrenoreceptor antagonist, in treatment of hypertension in patients with diabetes]. 968 27

Forty-two patients with benign hyperplasia of the prostate were studied for the role of symptomatic therapy with a selective adrenoblocker Cardura in the prophylaxis of progression of such diseases of the cardiovascular system as arterial hypertension, angina pectoris. The obstructive and irritative symptomatology-related uresis has been shown to get normalized. Also recordable in the conducted investigations was an alleviation of arterial hypertension together with a noticeable decrease in the frequency and severity of attacks of angina.
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PMID:[The effect of symptomatic therapy with the alpha 1-adrenoblocker Cardura in patients with benign prostatic hyperplasia on the course of cardiovascular diseases]. 1082

An active component in the tablet Cardura XL is doxazosine. Doxazosine belongs to the third generation of alpha 1-adrenolytics. It is a blocker of post-synaptic alpha 1-receptors both in humans and in animals. It is a long acting preparation. A tablet cover of Cardura XL is built of two layers (GITS system). It has enabled administration of doxazosine once a day. A great advance of the GITS system is a verly slow and systematic release of the drug from the tablet. This release is independent of pH of gastro-intestinal content or peristalsis. After administration of the tablet of Cardura XL, over 85% of the drug is released after 12 hours and the release ends after 12-16 hours. Maximal serum drug level after administration of doxazosine GITS is observed after 14-16 hours. Higher maximal serum drug level is achieved when the drug is administered together with a meal. Using doxazosine in the GITS form, minimal and maximal serum drug levels during the whole 24 hours differ non significantly. GITS technology enabled achieving stable daily serum drug concentration. Introducing doxazosine GITS caused: 1. decrease of Cmax; 2. elongation of Tmax; and 3. decrease of Cmin compared to doxazosine. It became possible due to gradual absorption of the preparation from gastrointestinal tract and improved coefficient of the drug fluctuation. It should be stated that the described pharmacological differences of doxazosine GITS in younger and elderly, in female and male patients do not influence significantly initial dosing of the drug. Stenosis of the gastrointestinal tract or chronic diarrhea affecting bowel passage of the drug, change its therapeutic effect. An effect of doxazosine GITS, doxazosine and placebo on blood pressure was studied in 392 patients with mild and moderate hypertension (< or = 220/95-115 mm Hg). Doxazosine GITS similarly to doxazosine effectively decreases blood pressure. The value of diastolic blood pressure decrease increases together with the therapy duration. Use of the unique GITS technology assures stable daily serum drug concentration. It results in: mild but permanent decrease of the blood pressure, decreased risk of side-effects, including orthostatic hypotony. Based on the performed post-registration studies it should be stated that doxazosine GITS is not only a very effective but also a safe preparation, which may be administered once daily. The treatment should be initialized with a dose of 4 mg daily. In as much as 60% of the patients with mild or moderate arterial hypertension, an initial dose (4 mg of Cardura XL) effectively lowers blood pressure. Taking into consideration unique features of the described preparation, it is worth thinking of Cardura XL while initializing or switching therapy in hypertensive patients. Cardura XL, due to favourable metabolic effects as well as the unique GITS technology seems to be the drug particularly suitable in hypertensive patients with accompanying dyslipidaemia, diabetes mellitus type 2 and/or benign prostata hypertrophy.
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PMID:[Cardura XL--a unique drug formulation--doxazosine administered in a slow-release form (doxazosine GITS)]. 1129 13

alpha-adrenoceptor antagonists have traditionally been used in the treatment of hypertension but in recent years they have become increasingly common in the treatment of benign prostatic enlargement (BPE), where they reduce the 'dynamic' component of bladder outlet obstruction and appear to have additional actions to reduce irritative symptoms of the disease. Prazosin (Hypovase), Alza), doxazosin (Cardura), Pfizer), indoramin (Doralese), Wyeth-Ayerst Pharmaceuticals Inc.) and terazosin (Hytrin), Abbott Laboratories) are currently available in the UK for BPE but these agents have cardiovascular actions in a significant number of patients, inducing effects which must be considered adverse unless the patient also requires treatment for mild-to-moderate hypertension. The uroselective alpha-adrenoceptor antagonists tamsulosin (Flomax), Yamanouchi Pharmaceutical Co. Ltd.) and alfuzosin (Xatral), Sanofi-Synthelabo) have recently been introduced. These agents exert their selectivity via different mechanisms; selective tissue distribution for alfuzosin and alpha-adrenoceptor subtype selectivity for tamsulosin. The incidence of cardiovascular side effects for both drugs is similar to placebo. Several lines of evidence suggest that the alpha-adrenoceptor antagonists may relieve lower urinary tract (LUT) symptoms by other mechanisms additional to those which account for the reduction in bladder outlet obstruction. If correct, these agents may be of use in the treatment of other bladder conditions.
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PMID:The use of alpha-adrenoceptor antagonists in lower urinary tract disease. 1182 30

Fifteen patients with arterial hypertension (AH) were examined. Their peripheral venous hemodynamics, central circulation, systolic and diastolic functions were studied and a course therapy with doxazosin (cardura, Pfizer, USA) was performed for 30 days. Cardura (doxazosin) was found to be the drug of choice for antihypertensive therapy in patients with AH concurrent with baseline systemic venous normo- or hypertension. In patients with baseline venous hypervolemia in the presence of venous hypotension, cardura therapy resulted in deterioration of signs of venous insufficiency and promoted the development (in 38% of the cases) or progression (in 38%) of diastolic dysfunction of the left ventricle (LV). Thus, the venous circulation and LV myocardial function should be originally assessed in order to decide whether cardura (doxazosin) is used in antihypertensive therapy in patients with AH.
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PMID:[Possibility of predicting the use of doxazosin in the treatment of arterial hypertension]. 1466 75

Doxazosin mesylate is an alpha1-adrenoceptor antagonist that was used to treat hypertension until a major study (ALLHAT; Antihypertensive and Lipid Lowering Treatment to Prevent Heart Attack Trial) showed that it increased the risk of progressing to heart failure. Doxazosin is now being used to treat benign prostatic hyperplasia (BPH). Noradrenaline acts on alpha1-adrenoceptors to contract the smooth muscle in the prostate and bladder, and by opposing these actions, doxazosin is beneficial in BPH. Doxazosin also increases apoptosis in the prostate. Although the standard preparation is suitable for once-daily dosing in BPH, it has to be titrated through three steps to its final dose. The controlled-release gastrointestinal therapeutic system (GITS) formulation of doxazosin is more convenient to use as it only has to be titrated through one step. In the treatment of BPH, standard doxazosin reduced both obstructive and irritative symptoms and increased peak urinary flow rate. The main side effects with doxazosin are those commonly associated with lowering blood pressure, although doxazosin lowers blood pressure to a lesser extent in normotensives than hypertensives. There is some evidence that in addition to being easier to use, doxazosin GITS may cause less adverse effects than the standard preparations. The benefits of doxazosin and the 5alpha-reductase inhibitor, finasteride, may be additive in BPH especially in men with large prostates. Further trials are necessary in order to determine whether doxazosin GITS is superior to other alpha1-adrenoceptor antagonists in BPH.
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PMID:After ALLHAT: doxazosin for the treatment of benign prostatic hyperplasia. 1533 Jul 33

Doxazosin mesylate is a selective alpha-adrenoreceptor antagonist for the treatment of hypertension and benign prostatic hyperplasia. A simple high performance liquid chromatographic method has been developed and validated for the quantitative determination of doxazosin in plasma. A reversed phase C18 column was used for the separation of doxazosin and prazosin (internal standard) with a mobile phase composed of water, acetonitrile, triethylamine (68:32:0.2 v/v, pH 5.0) at a flow rate of 1.2 mL/min. The fluorescence detector was operated at 246 (excitation) and 389 nm (emission). Intra- and inter-day precision and accuracy were acceptable for all quality control samples including the lower limit of quantification of 1 ng/mL. Recovery of doxazosin from human plasma was greater than 93.4%. Doxazosin was stable in human plasma under various storage conditions. This method was used successfully for a pharmacokinetic study in plasma after oral administration of multiple 4-mg dose of doxazosin gastrointestinal therapeutic system formulation to 16 healthy volunteers. At steady state the mean area under the curve for a dosing interval and elimination half-life were calculated to be 367.0 +/- 63.5 ng x hr/mL and 29.2 +/- 4.5 hr, respectively. There was no difference in pharmacokinetic parameters between male and female.
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PMID:Pharmacokinetics of doxazosin gastrointestinal therapeutic system after multiple administration in Korean healthy volunteers. 1772 99


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