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Silodosin, a novel selective alpha 1A-adrenoceptor selective antagonist for the treatment of benign prostatic hyperplasia. 2007

Masaki Yoshida, and Yukio Homma, and Kazuki Kawabe
Graduate School of Kumamoto University, Department of Urology, Graduate School of Medical Sciences, Honjo, Kumamoto 860-8556, Japan. akkomaki@kumamoto-u.ac.jp

Silodosin is a novel selective alpha(1A)-adrenoceptor (AR) antagonist generated by Kissei Pharmaceutical Co. Ltd. This drug selectively binds to alpha(1A)-AR, which is widely distributed in the prostate, urethra and bladder trigone, involved in their contraction, located at the lower urinary tract. This high selectivity for alpha(1A)-AR contributes to inhibition of sympathetic nerve stimulation and relaxation of smooth muscle tone of the lower urinary tract tissues, resulting in suppression of increase in intraurethral pressure. Clinical data suggested that silodosin showed significant improvement in lower urinary tract symptoms associated with benign prostatic hyperplasia, as well as in quality of life. The improvements were observed in both voiding and storage symptoms. In addition, the clinical effects occurred in the early treatment phase, and were observed not only in mild cases, but also in cases with severe symptoms. Long-term study revealed that the efficacy and safety was sustained for 1 year. Although silodosin showed relatively high incidence rate of abnormal ejaculation, the adverse events associated with lowering of blood pressure were low. This article reviews preclinical and clinical data of silodosin, and introduces the usefulness of the drug for treatment of benign prostatic hyperplasia patients.

UI MeSH Term Description Entries
D007211 Indoles Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
D008297 Male Males
D011470 Prostatic Hyperplasia Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both. Adenoma, Prostatic,Benign Prostatic Hyperplasia,Prostatic Adenoma,Prostatic Hyperplasia, Benign,Prostatic Hypertrophy,Prostatic Hypertrophy, Benign,Adenomas, Prostatic,Benign Prostatic Hyperplasias,Benign Prostatic Hypertrophy,Hyperplasia, Benign Prostatic,Hyperplasia, Prostatic,Hyperplasias, Benign Prostatic,Hypertrophies, Prostatic,Hypertrophy, Benign Prostatic,Hypertrophy, Prostatic,Prostatic Adenomas,Prostatic Hyperplasias, Benign,Prostatic Hypertrophies
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D058668 Adrenergic alpha-1 Receptor Antagonists Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS. Adrenergic alpha-1 Antagonists,Adrenergic alpha-1 Receptor Blockers,Adrenergic alpha1-Antagonists,alpha-1 Adrenergic Blocking Agents,alpha1-Adrenergic Antagonists,alpha1-Adrenoceptor Blocker,Adrenergic alpha 1 Antagonists,Adrenergic alpha 1 Receptor Antagonists,Adrenergic alpha 1 Receptor Blockers,Adrenergic alpha1 Antagonists,Antagonists, alpha1-Adrenergic,alpha 1 Adrenergic Blocking Agents,alpha-1 Antagonists, Adrenergic,alpha1 Adrenergic Antagonists,alpha1 Adrenoceptor Blocker,alpha1-Antagonists, Adrenergic
D018340 Receptors, Adrenergic, alpha-1 A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS. Adrenergic alpha-1 Receptors,Receptors, alpha-1 Adrenergic,alpha-1 Adrenergic Receptors,Adrenergic Receptor, alpha-1,Adrenergic alpha-1A Receptors,Adrenergic alpha-1B Receptors,Adrenergic alpha-1D Receptors,Receptor, Adrenergic, alpha-1,Receptor, Adrenergic, alpha-1A,Receptor, Adrenergic, alpha-1B,Receptor, Adrenergic, alpha-1D,Receptors, Adrenergic, alpha-1A,Receptors, Adrenergic, alpha-1B,Receptors, Adrenergic, alpha-1D,alpha 1 Adrenergic Receptor,alpha-1A Adrenergic Receptor,alpha-1B Adrenergic Receptor,alpha-1C Adrenergic Receptor,alpha-1D Adrenergic Receptor,Adrenergic Receptor, alpha 1,Adrenergic Receptor, alpha-1A,Adrenergic Receptor, alpha-1B,Adrenergic Receptor, alpha-1C,Adrenergic Receptor, alpha-1D,Adrenergic Receptors, alpha-1,Adrenergic alpha 1 Receptors,Adrenergic alpha 1A Receptors,Adrenergic alpha 1B Receptors,Adrenergic alpha 1D Receptors,Receptor, alpha-1 Adrenergic,Receptor, alpha-1A Adrenergic,Receptor, alpha-1B Adrenergic,Receptor, alpha-1C Adrenergic,Receptor, alpha-1D Adrenergic,Receptors, Adrenergic alpha-1,Receptors, Adrenergic alpha-1A,Receptors, Adrenergic alpha-1B,Receptors, Adrenergic alpha-1D,Receptors, alpha 1 Adrenergic,alpha 1 Adrenergic Receptors,alpha 1A Adrenergic Receptor,alpha 1B Adrenergic Receptor,alpha 1C Adrenergic Receptor,alpha 1D Adrenergic Receptor,alpha-1 Adrenergic Receptor,alpha-1 Receptors, Adrenergic,alpha-1A Receptors, Adrenergic,alpha-1B Receptors, Adrenergic,alpha-1D Receptors, Adrenergic

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