Delving into the Latest Updates on Naftopidil with Synapse

AbstractAlthough α1‐adrenoceptor (α1‐AR) antagonists used to treat benign prostatic hyperplasia can cause ejaculation disorders, the aetiology of this adverse event is still controversial. Therefore, we investigated the effects of antagonists with different affinities for α1‐AR subtypes on ejaculatory function and their mechanisms of action in normal rats. In the spontaneous seminal emission (SSE) test, systemically administered prazosin, terazosin, tamsulosin and naftopidil decreased the weight of ejaculated seminal material in a dose‐dependent manner; the potency order was as follows: tamsulosin > terazosin > prazosin > naftopidil. The selective α1D‐AR antagonist BMY7378 had no effect on SSE. Intrathecal tamsulosin and naftopidil did not inhibit SSE. Tamsulosin, the most potent, was ineffective as a single dose and significantly increased seminal vesicle fluid in rats treated for 2 weeks but did not significantly change retrograde ejaculation. These results indicated that the difference in inhibitory potency of the five α1‐AR antagonists against SSE was due to the involvement of α1A‐AR subtypes. Our results further suggested that α1‐AR antagonist‐induced ejaculatory dysfunction at the peripheral level was mainly due to the loss of seminal emission, although some retrograde ejaculation may also be involved.

26 Feb 2024·JACS Au

Ligated Pd-Catalyzed Aminations of Aryl/Heteroaryl Halides with Aliphatic Amines under Sustainable Aqueous Micellar Conditions

Article

Author: Iyer, Karthik S. ; Yirak, Jordan R. ; Lammert, Robert M. ; Lipshutz, Bruce H. ; Kavthe, Rahul D.

Sustainable technology for constructing Pd-catalyzed C-N bonds involving aliphatic amines is reported. A catalytic system that relies on low levels of recyclable precious metal, a known and commercially available ligand, and a recyclable aqueous medium are combined, leading to a newly developed procedure. This new technology can be used in ocean water with equal effectiveness. Applications involving highly challenging reaction partners constituting late-stage functionalization are documented, as is a short but efficient synthesis of the drug naftopidil. Comparisons with existing aminations highlight the many advances being offered.

01 Oct 2023·International journal of clinical pharmacy

Association of silodosin, tamsulosin, and naftopidil with delirium: analysis of the pharmacovigilance database in Japan.

Article

Author: Kawakami, Yasuhiro ; Noritake, Yumi ; Kotake, Kazumasa

BACKGROUNDAn association between adrenergic alpha-1 receptor antagonists and delirium has been suggested, but the details are unclear.AIMThis study investigated the association between adrenergic alpha-1 receptor antagonists and delirium in patients with benign prostatic hyperplasia using the Japanese Adverse Drug Event Report database.METHODFirst, disproportionality analysis compared the frequency of delirium in the adrenergic alpha-1 receptor antagonists silodosin, tamsulosin, and naftopidil. Next, multivariate logistic analysis was performed to examine the association between delirium and adrenergic alpha-1 receptor antagonists where disproportionality was detected.RESULTSA disproportionality in delirium was observed in patients receiving tamsulosin (reporting odds ratio [ROR] 1.85, 95% confidence interval [CI] 1.38-2.44, P < 0.01) compared with those who did not, and also in patients receiving naftopidil (ROR 2.23, 95% CI 1.45-3.28, P < 0.01) compared with those who did not. Multivariate logistic analysis revealed that in addition to previously reported risk factors for delirium, delirium in patients receiving tamsulosin was significantly increased with concomitant use of anticholinergics (odds ratio 2.73, 95% CI 1.41-5.29, P < 0.01) and delirium in patients receiving naftopidil was significantly increased with concomitant use of beta3-adrenergic receptor agonists (odds ratio 4.19, 95% CI 1.66-10.6, P < 0.01).CONCLUSIONAnticholinergics or beta3-adrenergic receptor agonists to treat overactive bladder in patients receiving tamsulosin and naftopidil was strongly associated with delirium. Confirming the medical history and concomitant medications of patients receiving tamsulosin or naftopidil may contribute to preventing delirium in patients with benign prostatic hyperplasia and to improving their outcomes.

100 Deals associated with Naftopidil

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External Link

KEGG	Wiki	ATC	Drug Bank
D01674	Naftopidil	G04CA	DB12092

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Dysuria	JP	-	25 Dec 1998
Prostatic Hyperplasia	JP	-	25 Dec 1998

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Medical device discomfort	Phase 1	KR	Dong-A ST Co., Ltd.	01 May 2014
Ureterolithiasis	Phase 1	KR	Dong-A ST Co., Ltd.	01 May 2014
Pain, Postoperative	Phase 1	KR	Dong-A ST Co., Ltd.	25 Oct 2013

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


1297 (AUA2011)	Not Applicable	Prostatic Cancer	212	Naftopidil	(vakjaefeat) = zogfelneaa xricnhumkj (gwfwuxeoez )	Positive	01 Apr 2011
				Tamsulosin	(vakjaefeat) = wihjxzyobp xricnhumkj (gwfwuxeoez )
AUA2011	Not Applicable	Calculus, Ureteral	99	Naftopidil 75mg	xkbzhtmfkr(pabmexjprx) = zatyeikpjv fazrklvuwd (ajfjspwmfr )	Positive	01 Apr 2011
				Flopropione 240mg	xkbzhtmfkr(pabmexjprx) = hwfgkddljd fazrklvuwd (ajfjspwmfr )