Alpha–1–adrenoceptor blockade in the treatment of benign prostatic hyperplasia

Abstract

In light of the growing interest in the concept of`uroselectivity' and in the increased worldwide use of alpha-blockers for benign prostatic hyperplasia (BPH), this review evaluates the relative bene®ts of various alpha-blocking agents in the treatment of BPH. The pharmacological and physiological selectivity as well as the clinical ef®cacy and safety of alfuzosin, doxazosin (Cardura 1 ), tamsulosin (Flomax 1 ), and terazosin (Hytrin 1 ) are compared. In reviewing ef®cacy and safety, emphasis is given to 17 placebo-controlled, doubleblind trials of these alpha-blockers published in peer-reviewed journals. This review also considers long-term data, effects on blood pressure, costs, and dose ranges.

Pharmacologic pupil dilation as a predictive test for the risk for intraoperative floppy-iris syndrome

“…However, prostate binding studies clearly show that these drugs have different receptor-affinity profiles than tamsulosin. 6,31 The mainly mild IFIS in 12% of patients in our no a 1 -ARA group is not surprising when data in the literature are analyzed. For example, 36% of respondents in the ASCRS survey noted IFIS with drugs other than a 1 -ARAs.…”

Modeling of Relationships between Pharmacokinetics and Blockade of Agonist-Induced Elevation of Intraurethral Pressure and Mean Arterial Pressure in Conscious Dogs Treated with α1-Adrenoceptor Antagonists

“…␣ 1 -Adrenoceptor antagonists represent first-line therapy for the pharmacological treatment of benign prostatic hyperplasia (BPH), in part by relaxing prostatic smooth muscle (Lowe, 1999). Fiduxosin (ABT-980) is a novel ␣ 1 -adrenoceptor antagonist.…”

“…nists to ameliorate BPH symptoms and to reduce adverse effects (e.g., decreased blood pressure, postural hypotension, or syncope) observed with nonsubtype-selective ␣ 1 -antagonists such as doxazosin or terazosin (Lowe, 1999). However, REC 15/2739, a compound showing high ␣ 1A -adrenoceptor selectivity, failed to ameliorate BPH symptoms in clinical trials (Lowe, 1999), perhaps the result of poor pharmacokinetic properties (A.…”

“…Tamsulosin, an ␣ 1a -/␣ 1d -subtype selective agent, had an index value approximately 10-fold greater than the nonselective drugs. Based on its pharmacokinetic profile and a relative uroselectivity 29-fold greater than the nonselective drugs, fiduxosin is expected to exhibit greater selectivity for urethral compared with vascular ␣ 1 -adrenoceptors in human and should be a novel, long-acting, uroselective ␣ 1 -adrenoceptor antagonist.␣ 1 -Adrenoceptor antagonists represent first-line therapy for the pharmacological treatment of benign prostatic hyperplasia (BPH), in part by relaxing prostatic smooth muscle (Lowe, 1999). Fiduxosin (ABT-980) is a novel ␣ 1 -adrenoceptor antagonist.…”

Benign Prostat Hiperplazisine Bağlı Alt Üriner Sistem Yakınmalarının Tedavisinde Tamsulosin ve Serenoa repens Ekstresi'nin (Prostagood) Etkinliklerinin Karşılaştırılması

“…BPH tedavisinde günümüzde FDA onayı almış dört α-bloker yaygın olarak kullanılmaktadır. Bunlar doksazosin, terazosin, tamsulosin ve alfuzosindir (27,28). Bu dört ilacın semptom ve akım hızı düzeltmesindeki faydalarının çok yakın olduğu klavuzlarda rapor edilmiştir (29,30).…”