Antihypertensive Therapy with Once‐daily Administration of Terazosin, a New Alpha₁‐adrenergic‐receptor Blocker

Abstract

The antihypertensive activity of terazosin, an investigational alpha 1-adrenergic-receptor blocker, and its effect on blood lipids were compared with placebo in a double-blind study. After a 3-week placebo baseline period, patients were randomized to receive terazosin (n = 22) or placebo (n = 16). The dose of terazosin was titrated over 2 weeks to a maintenance dosage of 10 mg once daily for 4 weeks. Antihypertensive efficacy was assessed: (1) at the end of the 24-hour dosing interval by comparing the average blood pressure (BP) after 3 and 4 weeks of maintenance therapy to the average BP after 2 and 3 weeks of placebo therapy, and (2) for 3 hours after drug ingestion at the final visit in comparison to the predose BP at that visit. At the end of the 24-hour dosing interval, 10 mg of terazosin reduced the mean supine systolic BP from 155.6 to 152.2 mm Hg and mean supine diastolic BP from 101.9 to 99.0 mm Hg (p less than 0.05). During the 3 hours after drug ingestion, mean supine systolic and diastolic pressures decreased maximally from 151.8 to 142.7 mm Hg (p less than 0.05) and from 99.5 to 91.0 mm Hg (p less than 0.05) respectively. No supine BP reduction differed significantly from the placebo response. During terazosin therapy there was a nonsignificant increase in mean body weight of 1.4 +/- 2.9 kg and no change in blood lipids. Thus the drug demonstrated greater antihypertensive activity 1-3 hours after ingestion than at the end of the 24-hour dosing interval.(ABSTRACT TRUNCATED AT 250 WORDS)

ZnO/rGO nanocomposite/carbon paste electrode for determination of terazosin in human serum samples

“…Terazosin hydrochloride, 2-[4-(2-tetrahydrofuranyl)carbonyl]-1piperazinyl-6,7-dimethoxy-4-quinazolinamine monohydro-chloride dehydrate (TR) is classied as a quinazoline (Scheme 1). It is a highly selective adreno-receptor antagonist, which acts an effective drug for hypertension 1,2 by relaxing veins and arteries, whereas for the symptomatic treatment of urinary obstruction caused by benign prostatic hyperplasia (BPH), by relaxing the muscles of the bladder and prostate. [3][4][5][6] TR is rapidly and almost completely adsorbed from the gastro-intestinal tract aer oral administration.…”

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

“…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.…”

Sensitive determination of terazosin by x‐ray fluorescence spectrometry based on the formation of ion‐pair associates with zinc thiocyanate

“…1) is a highly selective, potent 1-adrenoreceptor antagonist. It is an effective drug against hypertension 1 and benign prostatic hyperplasia. 2 Terazosin is presented for oral use in tablets containing 2, 5 and 10 mg as terazosin hydrochloride, for which the quality control of the final product and stability studies require high-sensitivity analytical methods.…”