Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Terazosin is a selective alpha 1-adrenoceptor antagonist; its actions on the serum lipoprotein profile were compared with those of the cardioselective beta-adrenoceptor antagonist atenolol in 40 patients with mild to moderate hypertension. Atenolol and terazosin were titrated over six weeks until blood pressure control (diastolic blood pressure less than 90 mmHg or greater than 10 mmHg fall in blood pressure) or a maximum dose of atenolol 100 mg or terazosin 10 mg had been achieved. Patients not controlled were then prescribed additional diuretic therapy (cyclopenthiazide 0.5 mg and potassium 1200 mg). At each visit blood pressure and adverse events were recorded; plasma lipids were measured at baseline, six and 12 weeks. During titration there was a linear decrease in systolic (-29 mmHg on atenolol and -24 mmHg on terazosin) and diastolic blood pressure (-17 and -12 mmHg) in both groups without subsequent change over the next six weeks; atenolol reduced heart rate (-11 bpm) without change on terazosin. During the initial six weeks the total cholesterol fell in both groups; however, there were significant between-treatment differences in triglyceride responses with a fall on terazosin and a rise on atenolol. Comparing atenolol and terazosin over the total 12 week study (irrespective of thiazide treatment) increased triglyceride levels and reduced cholesterol ratios and HDL were demonstrated on atenolol, contrasting with reduced triglyceride levels and elevated HDL and cholesterol ratios of terazosin.(ABSTRACT TRUNCATED AT 250 WORDS)
 ...
PMID:Comparison of antihypertensive and lipid actions of terazosin and atenolol in essential hypertension. 135 28

Terazosin (Hytrin; Abbott Laboratories, North Chicago, IL) is a new, selective alpha 1-adrenoceptor blocking agent used on once-a-day basis for therapy of mild-to-moderate hypertension. Its pharmacologic properties are similar to those of prazosin. Terazosin however, differs from prazosin in that its water solubility is 25 times greater than that of prazosin and its elimination half-life is about three times that of prazosin. Greater water solubility facilitates intravenous formulation, and longer half-life allows once-daily administration of terazosin. Terazosin is effective in lowering blood pressure and has a beneficial effect on plasma lipid profile. The major advantage of terazosin compared with prazosin, however, is its long duration of action. Terazosin is safe and effective when used in combination with diuretics and other antihypertensive agents, and in the long-term treatment of patients with mild to moderate essential hypertension.
 ...
PMID:Terazosin: a new alpha adrenoceptor blocking drug. 135 83

Terazosin is a new, long-acting, selective, postsynaptic alpha 1-adrenergic receptor antagonist with a chemical structure similar to that of prazosin. In this article the pharmacokinetics of terazosin are reviewed, and the incidence of adverse events in a dose-response study and a meta-analysis of 20 placebo-controlled trials involving a total of 1814 patients is presented. Peak plasma concentrations of terazosin are achieved 1 to 2 hours after oral administration. The relatively long half-life of terazosin (12 hours) enables it to be administered in a once-a-day regimen. Dose and plasma levels of terazosin show a linear relationship. Terazosin is rapidly and completely absorbed after oral administration. The pharmacokinetics of terazosin are not significantly affected by food, age, hypertension, or renal impairment. Adverse events after the administration of terazosin are usually minor and not age related. The incidence of syncope after therapeutic dosages of terazosin is minimal. Terazosin's effectiveness, combined with its pharmacokinetics, safety profile, and potentially favorable lipid effect, makes it a highly appropriate choice for antihypertensive therapy.
 ...
PMID:Terazosin: pharmacokinetics and the effect of age and dose on the incidence of adverse events. 167 20

Terazosin is a selective alpha 1-adrenergic-blocking agent indicated for the treatment of hypertension. The aim of this multicenter study, performed in 256 patients with mild to moderate essential hypertension, was to define the dosing characteristics of terazosin (in the range of 1 to 80 mg) administered once daily. Patients were randomly assigned to placebo or active treatment groups; each group received 3 months of treatment, which comprised three ascending doses of terazosin, each administered for a 1-month period. As determined by conventional office measurements of supine diastolic blood pressure and by automated ambulatory blood pressure monitoring, there was a clear antihypertensive dose-response relationship for terazosin in the range of 1 to 5 mg daily. Except for the 80 mg dose, none of the doses above 5 mg (10 to 40 mg) appeared to provide additional efficacy. Both the office measurements and the monitoring data indicated that the ratio of trough (effect at the end of the dosing interval) to peak (maximum effect during the dosing interval) was at least 50% or greater during treatment with the 5 mg dose. Thus the 5 mg dose appeared to provide meaningful clinical antihypertensive efficacy and to sustain its effects throughout the full 24-hour period.
 ...
PMID:Antihypertensive dose-response relationships: studies with the selective alpha 1-blocking agent terazosin. 167 21

This open, multicenter phase III study was designed to assess the efficacy and long-term safety of terazosin (1 to 40 mg/day), alone or in combination with other antihypertensive drugs, in 364 patients with mild to moderate essential hypertension. Compared with baseline values, long-term terazosin monotherapy or combination therapy resulted in consistent decreases in both systolic and diastolic blood pressures, with a mean reduction in supine diastolic pressure of 12 to 14 mm Hg. The numbers of patients with controlled blood pressure at the last evaluable visit of each therapy period were as follows: terazosin alone, 106 of 245 (43%); terazosin with added diuretic, 70 of 112 (63%); diuretic with added terazosin, 47 of 88 (53%); and terazosin plus diuretic with added beta-blocker, 22 of 32 (69%). Most adverse events were mild or moderate in severity. Only pain in extremities had a higher incidence during long-term treatment (6%, 181 to 360-day period) than during initial short-term treatment (5%, 1 to 90-day period). Three of six syncopal events occurred during the initial 180 days of treatment; this 0.8% (3/364) incidence was comparable with that reported previously for short-term studies. Only one case of syncope occurred during terazosin monotherapy. Terazosin was judged to be a safe and effective long-term medication for the treatment of hypertension.
 ...
PMID:Long-term efficacy and safety of terazosin alone and in combination with other antihypertensive agents. 167 23

The dynamic component of infravesical obstruction in men with symptomatic benign prostatic hyperplasia (BPH) is determined by alpha 1-adrenoceptor-mediated contractions of the prostatic capsule, prostate adenoma, and bladder neck. Since alpha 1-adrenoceptors are sparse in the bladder, medical therapy aimed at blocking the alpha receptor will relieve bladder outlet obstruction without inhibiting bladder function. Numerous clinical studies have evaluated the use of various alpha blockers for the treatment of BPH. Although the majority of these trials involved limited numbers of patients treated for only short periods, their results have consistently shown that alpha blockers improve urinary flow rates. Adverse reactions appear to be more frequent and more serious with the use of nonselective alpha blockers than with selective alpha 1 blockers, such as terazosin or prazosin. Terazosin offers the additional advantage of once-daily dosing. The common association of hypertension, hyperlipidemia, and symptomatic BPH in the aging male population may provide further impetus for initiating treatment with alpha blockers because alpha blockers are effective antihypertensive agents and may favorably alter lipid profiles.
 ...
PMID:Role of alpha-adrenergic blockers in the treatment of benign prostatic hyperplasia. 168 72

Terazosin is a new, selective, alpha 1-adrenoceptor antagonist which is structurally similar to prazosin and of similar therapeutic efficacy in the treatment of mild-to-moderate essential hypertension. Unlike prazosin, the terminal-phase plasma half-life is long, at approximately 12 h, and effective blood pressure control is usually achieved with a once-daily dosing regimen. Once-daily dosing improves patient compliance, and good compliance to the therapeutic regimen is essential to effective treatment and the reduction of cardiovascular morbidity and mortality. Terazosin has generally been well tolerated in short-term and long-term studies. Unlike diuretics and beta-blockers, terazosin does not adversely affect the serum lipid profile. Indeed, beneficial changes in the serum lipid profile have been observed in patients with hypertension. In placebo-controlled trials, total serum cholesterol and the combined low-density plus very-low-density lipoprotein cholesterol fraction were significantly reduced from baseline in the terazosin-treated group when compared with the placebo-treated group. In addition, terazosin tended to produce increases from baseline in the high-density lipoprotein cholesterol fraction and decreases in serum triglyceride levels. Once-daily dosing and a favorable impact on the serum lipid profile support the use of terazosin as first-choice treatment for mild-to-moderate essential hypertension.
 ...
PMID:Terazosin: a new antihypertensive agent with favorable effects on lipids. 257 Jul 58

Eighteen patients ages 35-70 years (mean +/- SEM 58 +/- 2) with poorly controlled hypertension on various regimens, participated in the present studies. After a 4-week placebo-controlled lead-in period, 12 patients were randomized to terazosin treatment and 6 to placebo. They were followed in the clinic every 2 weeks for 13 weeks, where their supine (5 min) and the upright (2 min) arterial pressure and heart rate were measured. In addition, all patients had a complete laboratory evaluation at the beginning and end of the study. Depending on pressure response, the experimental drug was increased at each visit from 1.0 mg/day to 2.0, 5.0, 15.0, and 20.0 mg/day, if the supine diastolic pressure was greater than 90 mmHg. Terazosin decreased the systolic and diastolic pressure in both the supine and upright positions, and had no significant effect on heart rate. Placebo did not exert any effects on either arterial pressure or heart rate. No adverse clinical or metabolic effects were observed with the administration of either terazosin or placebo. We conclude that: Terazosin is a new effective long-acting alpha blocker given in combination with other antihypertensive drugs, and it is safe and well tolerated by the patients.
 ...
PMID:Antihypertensive effectiveness of terazosin: a new long-acting alpha-adrenergic inhibitor. 286 53

The pharmacokinetics of terazosin have been assessed in human volunteers, hypertensive patients, a limited number of elderly volunteers, and a small number of patients with congestive heart failure. Terazosin was administered intravenously and orally in doses ranging up to 7.5 mg. Following intravenous administration, the disposition of terazosin is characteristic of a two-compartment, open model that is linear and independent of dose. Orally administered terazosin is rapidly, consistently, and almost completely absorbed into the bloodstream. Peak plasma drug levels occur within one to two hours after ingestion. Approximately 90 to 94 percent of the drug is bound to plasma proteins, with the volume of distribution estimated to be 25 to 30 liters. Terazosin undergoes extensive hepatic metabolism, and the major route of elimination is via the biliary tract. Small amounts of terazosin are excreted in the urine. Plasma and renal clearances are 80 and 10 ml per minute, respectively. The mean beta-phase half-life is approximately 12 hours. The pharmacokinetics of terazosin were not influenced by age, congestive heart failure, or hypertension (other than plasma clearance). In contrast to prazosin, terazosin is completely and consistently bioavailable and has a half-life that is three to four times longer than that of prazosin. The prolonged half-life of terazosin allows once-daily dosing, which may facilitate patient compliance with drug therapy for hypertension.
 ...
PMID:Pharmacokinetics of terazosin. 287 2

The safety and efficacy of once-daily terazosin as monotherapy were evaluated in five randomized, double-blind, placebo-controlled studies in which 351 patients with mild to moderate hypertension participated. The five studies included two dose-titration studies and three fixed-dose studies. In the dose-titration studies, terazosin doses were titrated at weekly intervals until supine diastolic blood pressure was below 90 mm Hg. In the fixed-dose studies, titration continued until a predetermined dosage level of terazosin or corresponding placebo was reached. The dose of terazosin ranged from 1 to 40 mg once daily, and responses were assessed after a four-week course of therapy at a constant dosage level. Terazosin administration resulted in significantly greater mean decreases in supine diastolic blood pressure in comparison with placebo in four of the five studies. Similar decreases were observed for supine systolic and standing blood pressures in selected studies. In all five studies, terazosin caused a significant decrease in supine and standing blood pressures from baseline to the final visit. Adverse experiences occurring with a significantly greater prevalence rate in terazosin-treated versus placebo-treated patients and 7 percent of placebo-treated patients), asthenia (17 percent of the terazosin group and 4 percent of the placebo group), and peripheral edema (10 percent of the terazosin group and 3 percent of the placebo group). On the basis of these studies, it appears that terazosin, when administered once daily as monotherapy, is both safe and effective for the treatment of mild to moderate hypertension.
 ...
PMID:Terazosin: an effective once-daily monotherapy for the treatment of hypertension. 287 4


1 2 3 Next >>