The management of symptomatic benign prostatic hyperplasia (BPH) continues to evolve, with new techniques and forms of medical management being introduced and traditional surgical techniques being used less frequently. Medical management of BPH has evolved from nonspecific alpha-adrenoceptor antagonists to uroselective alpha-adrenoceptor antagonists and 5-alpha reductase inhibitors. Traditionally, alpha-adrenoceptor antagonists have been used for relief of lower urinary tract symptoms (LUTS) as a result of BPH and are known for their quick onset of action. 5-alpha Reductase inhibitors have proven useful for the prevention of BPH progression as measured by prostate volume, disease progression, incidence of acute urinary retention and the need for subsequent BPH-related surgery. Recent studies have shown that the combination of an alpha-adrenoceptor antagonist and a 5-alpha reductase inhibitor has significantly better efficacy than either drug alone or placebo. Currently, alpha-adrenoceptor antagonists are used in the acute setting or for short-term relief of LUTS. The combination of an alpha-adrenoceptor antagonist and a 5-alpha reductase inhibitor is used for the longer term management of BPH symptoms and to prevent progression of BPH and perhaps avoid surgical intervention.
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http://dx.doi.org/10.2165/00002512-200522110-00002 | DOI Listing |
Neurogastroenterol Motil
January 2025
Department of Cell Biology, Physiology and Immunology, Universitat Autònoma de Barcelona, Barcelona, Spain.
Background: Inhibitory neuromuscular transmission in the gastrointestinal tract is mediated by intrinsic nitrergic and purinergic neurons. Purines activate G protein-coupled receptor P2Y receptors, increasing intracellular Ca that activates small conductance calcium-activated potassium (SK) channels. Little is known about the effect of adrenergic receptor activation on intestinal smooth muscle.
View Article and Find Full Text PDFPflugers Arch
October 2024
Department of Cell Physiology, Nagoya City University Graduate School of Medical Sciences, 1, Kawasumi, Mizuho-Cho, Mizuho-Ku, Nagoya, 467-8601, Japan.
In the gastrointestinal tract, nitrergic inhibition of the arteriolar contractility has not been demonstrated. Here, we explored whether neurally-released nitric oxide (NO) inhibits sympathetic vasoconstrictions in the rat rectal arterioles. Changes in sympathetic vasoconstrictions and their nitrergic modulation in rats exposed to water avoidance stress (WAS, 10 days, 1 h per day) were also examined.
View Article and Find Full Text PDFHypertension
August 2024
Department of Epidemiology (S.G., M.J.T., Z.L., B.H.C.S., J.W.D., M.A.I., M.K.), Erasmus MC, University Medical Center Rotterdam, The Netherlands.
Background: We investigated the potential impact of antihypertensive drugs for atrial fibrillation (AF) prevention through a drug target Mendelian randomization study to avoid the potential limitations of clinical studies.
Methods: Validated published single-nucleotide polymorphisms (SNPs) that mimic the action of 12 antihypertensive drug classes, including alpha-adrenoceptor blockers, adrenergic neuron blockers, angiotensin-converting enzyme inhibitors, angiotensin-II receptor blockers, beta-adrenoceptor blockers, centrally acting antihypertensive drugs, calcium channel blockers, loop diuretics, potassium-sparing diuretics and mineralocorticoid receptor antagonists, renin inhibitors, thiazides and related diuretic agents, and vasodilators were used. We estimated, via their corresponding gene and protein targets, the downstream effect of these drug classes to prevent AF via systolic blood pressure using 2-sample Mendelian randomization analyses.
Eur J Pharmacol
September 2024
Centro Acadêmico de Vitória, Universidade Federal de Pernambuco - UFPE, Vitória de Santo Antão-PE, Brazil. Electronic address:
Drugs that act on α-adrenoceptors may contain morpholine and pyrimidinone heterocycles. The aim of this study was to synthesize a series of pyrimidinones (S6a-e and S8) and characterize their α-adrenoceptor activity. Cytotoxicity assays (MTT and LDH) were performed in A7r5 and HUVECs.
View Article and Find Full Text PDFHandb Exp Pharmacol
September 2024
Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC, Australia.
The nine G protein-coupled adrenoceptor subtypes are where the endogenous catecholamines adrenaline and noradrenaline interact with cells. Since they are important therapeutic targets, over a century of effort has been put into developing drugs that modify their activity. This chapter provides an outline of how we have arrived at current knowledge of the receptors, their physiological roles and the methods used to develop ligands.
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