Antihypertensive effectiveness of terazosin: A new long‐acting alpha‐adrenergic inhibitor

Abstract

Summary:Eighteen patients aged 35-70 years (meanf SEM 58 f2) 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 .O mg/day to 2.0,5.0, 15.0, and 20.0 mg/day, if the supine diastolic pressure was gmter than 90 d g .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 clini- cal or metabolic effects were observed with the administration of either terazosin or placebo. We conclude that: (1) Terazosin is a new effective long-acting alpha blocker given in combination with other antihypertensive drugs, and (2) it is safe and well tolerated by the patients.

Separation of the enantiomers of four chiral drugs by neutral cyclodextrin-mediated capillary zone electrophoresis

“…This is not in contradiction with Wren's theory, because in Wren's equation only mobility difference Ap is taken into account, and this is governed thermodynamically by the guest-host complexation reaction. Resolution, which is used more widely in separation science than the mobility difference ACt or the mobility ratio ACt/Ctav, is affected by more difference, average apparent mobility of the solutes to be separated, and the column efficiency [9,10]. After optimization of the concentration of the CDs, the resolution for the chiral separation of esmolol and terazosin were further increased to 3.1 (60 mM a-CD) and 1.2 (60 mM DM-~-CD), respectively.…”

“…Esmolol is an ultra-short-acting adrenergic [3-receptor blocking agent [8]. Terazosin is an antihypertensive drug [9,10]. …”

Identification, Preparation, and Characterization of Several Polymorphs and Solvates of Terazosin Hydrochloride

“…To 700 g of 2‐chloro‐4‐amino‐6,7‐dimethoxyquinazoline3 in 50 mL methoxyethanol was added 10.8 g tetrahydrofuroyl piperazine, and the mixture was refluxed 3 h. The clear solution was concentrated and an aqueous solution of potassium bicarbonate was added. The resultant solid that formed was filtered and washed with water.…”

“…Terazosin monohydrochloride or 1‐(4‐amino‐6,7‐dimethoxy‐2‐quinazolinyl)‐4‐(tetrahydro‐2‐furoyl) piperzinyl monohydrochloride was initially isolated as an anhydrous crystalline solid. Terazosin is a potent anti‐hypertensive agent marketed as Hytrin 1–6. During the development of a tablet formulation a dihydrate form of the drug was discovered.…”

Direct Vasodilators and Sympatholytic Agents

“…The first studies evaluating terazosin for hypertension date back to 1985, when it was first used as an adjunct to various antihypertensive regimens. 135 Its antihypertensive effect was comparable to prazosin but showed less effect on supine diastolic blood pressure compared to hydrochlorothiazide. 136 As a monotherapy, it was found to be safe for the long-term treatment of up to 2 years for both supine systolic and diastolic blood pressures.…”