Clinical ease of using doxazosin in BPH patients with and without hypertension

Abstract

Clinical studies have demonstrated that doxazosin therapy reduced blood pressure (BP) in patients with benign prostatic hyperplasia (BPH) who were hypertensive at baseline but not in patients who were physiologically or pharmacologically normotensive at baseline. In patients with BPH and uncontrolled hypertension, despite treatment with other antihypertensive drugs, the addition of doxazosin resulted in improved control with significant reductions in BP. The new formulation, doxazosin gastrointestinal therapeutic system (GITS), is initiated at a therapeutic dose, simplifying dose titration. Based on its efficacy and pharmacokinetic and tolerability profiles, doxazosin GITS is an effective and welltolerated treatment for normotensive and hypertensive patients with BPH. Prostate Cancer and Prostatic Diseases (2005) 8, 152-157.

Enantioselective Pharmacokinetics of Doxazosin and Pharmacokinetic Interaction Between the Isomers in Rats

“…Doxazosin is a safe and efficacious treatment option for lower urinary tract symptoms (LUTS) in patients with benign prostatic hyperplasia (BPH), [1][2][3] and as an add-on drug in combination therapy to achieve target blood pressures. [4][5][6][7] Doxazosin contains a chiral carbon at the 2-position of the 1, 4-benzodioxan-2-ylcarbonyl ring, consisting of two optical isomers, (+)-(S)-doxazosin and (-)-(R)-doxazosin, and it is used clinically as a racemate. The (+)-(S)-doxazosin and (-)-(R)-doxazosin do not have the same biological activity.…”

Doxazosin selectively potentiates contraction to serotonin via 5-HT2A receptors in longitudinal muscle strips of the rabbit gastric body

“…In preliminary experiments, we have further observed that (±)doxazosin obviously enhances the contractile response to 5-HT in isolated longitudinal muscle strips of the rabbit gastric body. Because doxazosin, alfuzosin, and terazosin are orally administered for the treatment of LUTS/BPH or uncontrolled hypertension (Chung et al 1999;Andersen et al 2000;Steers and Kirby 2005;De Alvaro et al 2006;Fine and Ginsberg 2008;Zhang et al 2011), patients can maintain a higher concentration of these agents in the GI tract before drug absorption.…”

A Genetic-Function-Approximation-Based QSAR Model for the Affinity of Arylpiperazines toward α1 Adrenoceptors

“…Recently, α 1 -AR antagonists have attracted much attention for the treatment of benign prostatic hyperplasia-related lower urinary tract symptoms, sexual dysfunctions, hypertension, and cardiovascular diseases, while α 2 -AR antagonists have been studied for their activity in a variety of diseases such as pain, depression, anxiety, and obesity …”

“…Recently, R 1 -AR antagonists have attracted much attention for the treatment of benign prostatic hyperplasia-related lower urinary tract symptoms, 9 sexual dysfunctions, 10 hypertension, and cardiovascular diseases, 11 while R 2 -AR antagonists have been studied for their activity in a variety of diseases such as pain, 12 depression, 13 anxiety, 14 and obesity. 15 The discovery of a lead candidate or a hit molecule worthy of further development includes characterization of both the affinity/activity and selectivity profiles toward such targets.…”