The Effect of Finasteride on the Risk of Acute Urinary Retention and the Need for Surgical Treatment Among Men With Benign Prostatic Hyperplasia

McConnell, John D.; Bruskewitz, Reginald C.; Walsh, Patrick C.; Andriole, Gerald L.; Lieber, Michael M.; Holtgrewe, H. Logan; Albertsen, Peter C.; Roehrborn, Claus G.; Nickel, J. Curtis; Wang, D.Z.; Taylor, Allison J.; Waldstreicher, Joanne

doi:10.1016/s0022-5347(01)63115-x

Cited by 186 publications

(291 citation statements)

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“…Lepor et al (1996) have reported that a combination of terazosin, an α 1 -adrenoceptor antagonist, and finasteride has no greater beneficial effect in BPH patients than terazosin alone. However, subsequent studies (McConnell et al 1998;Marberger 1998) have demonstrated that longterm treatment with finasteride offers advantages in patients with very large prostates, suggesting the possibility that Z-350 could be superior to other α 1 -adrenoceptor antagonists for long-term treatment of certain BPH patients.…”

Section: Discussionmentioning

confidence: 99%

Z-350, a new chimera compound possessing α1-adrenoceptor antagonistic and steroid 5α-reductase inhibitory actions

Fukuda

Fukuta

Higashino

et al. 1999

Naunyn-Schmiedeberg's Arch Pharmacol

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The effects of Z-350, (S)-4-[3-(4-{1-(4-methyl-phenyl)-3-[4-(2-methoxyphenyl)piperazine-1-yl]propoxy} benzoyl)indole-1-yl]butyric acid hydrochloride, a newly synthesized compound possessing alpha-adrenoceptor antagonistic and steroid 5alpha-reductase inhibitory actions, were studied in vitro. In functional experiments, Z-350 shifted the concentration/response curve for the phenylephrine-induced contraction of rabbit prostate, urethra and aorta to the right with pA2 values of 8.04, 7.57 and 7.13, respectively. The binding affinity of Z-350 for alpha1-adrenoceptors in rabbit prostate, urethra and aorta were estimated by the displacement of [3H]prazosin. The pKi values for this action of Z-350 were 7.53, 7.95 and 7.62 for the prostate, urethra and aorta, respectively. alpha1-Adrenoceptor subtype selectivities were studied in the submaxillary gland (r(1A) and liver (alpha1B) of rat. Z-350 inhibited the specific binding of [3H]prazosin to alpha1A and (alpha1B-adrenoceptors with pKi values of 7.82 and 7.29, respectively. Z-350 inhibited rat prostatic steroid 5alpha-reductase non-competitively with a pIC50 of 8.42. These results indicate that Z-350 is a alpha1-adrenoceptor antagonist and is a steroid 5alpha-reductase inhibitor. It is expected that Z-350 will be a candidate drug for the treatment of benign prostatic hyperplasia.

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Section: Discussionmentioning

confidence: 99%

Z-350, a new chimera compound possessing α1-adrenoceptor antagonistic and steroid 5α-reductase inhibitory actions

Fukuda

Fukuta

Higashino

et al. 1999

Naunyn-Schmiedeberg's Arch Pharmacol

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“…Several randomized clinical trials have confirmed the tolerability and safety of long-term finasteride treatment [59,77,78]. In particular, the PLESS (Proscar LongTerm Efficacy and Safety) study, which involved 3040 male BPH patients over 4 years reported that the drop-out rate was higher in the placebo group (42 %) in comparison with the finasteride-treated group (34 %) [79].…”

Section: Adverse Effects Of 5α-rs Inhibitorsmentioning

confidence: 98%

“…In a majority of patients, finasteride (5 mg/day) leads to significant reductions in symptom severity, improvement of urinary flow rate, reduction of prostate volume and risk of acute urinary retention, as well as a reduction of the need for surgical intervention [58,59]. Likewise, dutasteride has been shown to result in similar therapeutic effects as finasteride [60][61][62].…”

Section: Therapeutic Efficacy Of 5α-r Inhibitors In Bphmentioning

confidence: 99%

Adverse effects of 5α-reductase inhibitors: What do we know, don’t know, and need to know?

Traish

Melcangi

Bortolato

et al. 2015

Rev Endocr Metab Disord

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Steroids are important physiological orchestrators of endocrine as well as peripheral and central nervous system functions. One of the key processes for regulation of these molecules lies in their enzymatic processing by a family of 5α-reductase (5α-Rs) isozymes. By catalyzing a key rate-limiting step in steroidogenesis, this family of enzymes exerts a crucial role not only in the physiological control but also in pathological events. Indeed, both 5α-R inhibition and supplementation of 5α-reduced metabolites are currently used or have been proposed as therapeutic strategies for a wide array of pathological conditions. In particular, the potent 5α-R inhibitors finasteride and dutasteride are used in the treatments of benign prostatic hyperplasia (BPH), as well as in male pattern hair loss (MPHL) known as androgenetic alopecia (AGA). Recent preclinical and clinical findings indicate that 5α-R inhibitors evoke not only beneficial, but also adverse effects. Future studies should investigate the biochemical and physiological mechanisms that underlie the persistence of the adverse sexual side effects to determine why a subset of patients is afflicted with such persistence or irreversible adverse effects. Also a better focus of clinical research is urgently needed to better define those subjects who are likely to be adversely affected by such agents. Furthermore, research on the non-sexual adverse effects such as diabetes, psychosis, depression, and cognitive function are needed to better understand the broad spectrum of the effects these drugs may elicit during their use in treatment of AGA or BPH. In this review, we will summarize the state of art on this topic, overview the key unresolved questions that have emerged on the pharmacological targeting of these enzymes and their products, and highlight the need for further studies to ascertain the severity and duration of the adverse effects of 5α-R inhibitors, as well as their biological underpinnings.

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“…Aus dieser Präparatgruppe ist sowohl ein selektiver Inhibitor der 5α-Reduktase Typ II (Finasterid) wie auch ein Inhibitor beider Isoenzyme (Typ I und Typ II; Dutasterid) am Markt. Die Effizienz beider Präparate wurde in prospektiven randomisierten Studien untersucht, wobei für Dutasterid Daten über 4 Jahre, für Finasterid über bis zu 4,5 Jahren vorliegen [3,7,10,11,12,13]. Soweit derzeit beurteilbar ist die klinische Effizienz beider Präparate vergleichbar [3,7,10,11,12,13].…”

Section: α-Reduktaseinhibitorenunclassified

“…Abb. 6;[3,7,11,12,13]). Diese Präparate sind demnach in der Lage, in den natürlichen Verlauf der Erkrankung einzugreifen.…”

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Benigne Prostatahyperplasie

Madersbacher

Marszalek

2007

Internist

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A profound knowledge of pathogenesis and natural history enables a differentiated therapy for elderly men with lower urinary tract symptoms due to benign prostatic hyperplasia (BPH). The role of phytotherapy is still controversially discussed and, therefore, not clearly recommended by any BPH-guideline. alpha(1)-blockers are the therapy of choice for symptomatic patients at a low risk of disease progression (prostate volume <30-40 ml). 5alpha-reductase inhibitors (5ARI) reduce the prostate volume by 20-25% and the risk for acute urinary retention/surgery by more than 50% compared to placebo. Combination therapy (alpha(1)-blocker plus 5ARI) is superior to either monotherapy, though this advantage is only demonstrable after a prolonged treatment period (>12 months).

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The Effect of Finasteride on the Risk of Acute Urinary Retention and the Need for Surgical Treatment Among Men With Benign Prostatic Hyperplasia

Cited by 186 publications

References 1 publication

Z-350, a new chimera compound possessing α1-adrenoceptor antagonistic and steroid 5α-reductase inhibitory actions

Z-350, a new chimera compound possessing α1-adrenoceptor antagonistic and steroid 5α-reductase inhibitory actions

Adverse effects of 5α-reductase inhibitors: What do we know, don’t know, and need to know?

Benigne Prostatahyperplasie

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