Delving into the Latest Updates on Penehyclidine hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Changtuoning, ET, Penehyclidine

+ [4]

Target

M1 receptor x M3 receptor

Action

antagonists

Mechanism

M1 receptor antagonists(Muscarinic acetylcholine receptor M1 antagonists), M3 receptor antagonists(Muscarinic acetylcholine receptor M3 antagonists)

Therapeutic Areas

Other DiseasesNervous System DiseasesDigestive System Disorders+ [2]

Active Indication

AnesthesiaDrug intoxicationBiliary pain+ [3]

Inactive Indication

Parkinson DiseaseShockSmooth muscle spasm

Originator Organization

Chengdu List Pharmaceutical Co., Ltd.

Active Organization

Chengdu List Pharmaceutical Co., Ltd.

Jinzhou Ahon Pharmaceutical Co., Ltd.

Chongqing Xianyang Pharmaceutical Technology Co., Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

China (24 Oct 2002),

AnesthesiaDrug intoxication

Regulation-

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Structure/Sequence

Molecular FormulaC20H30ClNO2

InChIKeyDDTVVMRZNVIVQM-UHFFFAOYSA-N

CAS Registry151937-76-7

View All Structures (2)

BACKGROUNDRenal tubular injury (RTI) is one of the key characteristics of diabetic nephropathy (DN). Penehyclidine hydrochloride (PHC) was an anticholinergic drug with renoprotective effects, but its specific mechanism in the treatment of DN was still unclear.METHODSWe treated different diabetic mouse models and high glucose-induced RTI models by PHC. Histological analyses were performed using flow cytometry and staining, and ELISA evaluated the ROS, apoptosis, and related markers under different treatments. The molecular interactions were analyzed by ChIP, dual-luciferase reporter, and CoIP.RESULTSPHC alleviated RTI by activating mitophagy and inhibiting apoptosis, and the protective effect could be rescued by PARK2 knockdown. Nrf2 bound to the promoter region of PARK2 and promoted its expression. PHC reduced the level of apoptosis by reducing the degree of nuclear translocation of AIFM1, which was rescued by PARK2 knockdown. PARK2 knockdown reduced the non-degradative ubiquitination of AIFM1, thus promoting its nuclear translocation and ultimately facilitating renal tubular cells (RTCs) apoptosis. The over-expression of AIFM1 rescued the RTCs apoptosis antagonized by PHC.CONCLUSIONSPHC activated Nrf2 to up-regulate PARK2 transcription to induce mitophagy and inhibit apoptosis mediated by nuclear translocation of AIFM1 through promoting non-degradative ubiquitination of AIFM1, ultimately rescuing RTI in DN.

01 Feb 2025·Journal of Anesthesia

Study of penehyclidine for the prevention of postoperative nausea and vomiting following laparoscopic sleeve gastrectomy under general anesthesia: a randomized, prospective, double-blind trial

Article

Author: Wang, Min ; Liu, Chen ; Wang, Ting-Ting ; Wu, Zhou-Quan

PURPOSETo investigate the efficacy of penehyclidine (PHC) for preventing postoperative nausea and vomiting (PONV) after laparoscopic sleeve gastrectomy (LSG) under general anesthesia.MATERIALS AND METHODSIn this prospective study, 219 patients who were scheduled to undergo LSG were randomly assigned to three cohorts: the control cohort (received normal saline), the infusion cohort (administered 0.25 mg of PHC intravenously followed by an additional 0.25 mg through an intravenous analgesia pump for 48 h after LSG), and the bolus cohort (received a single intravenous dose of 0.5 mg of PHC). The study outcomes included the incidence of PONV within the first 48 h postoperatively, the severity and intensity of PONV, side effects and postoperative recovery outcomes. Univariate and multivariate logistic analyses were performed to identify independent risk factors associated with PONV.RESULTSCompared with the control cohort, both the infusion and bolus cohorts presented considerably lower incidences of PONV (61.64% vs. 12.33% vs. 38.36%, P < 0.05), as well as significantly decreased PONV severities (P < 0.05) and intensities (P < 0.05). There were no significant differences in side effects and postoperative recovery outcomes among the three cohorts, with the exception of dry mouthand the administration of rescue antiemetic therapy (P < 0.05). Additionally, the Apfel risk score and PHC intervention were identified as independent risk factors associated with PONV incidence following LSG (P < 0.05).RESULTSPHC effectively prevented PONV occurrence and reduced its severity in LSG patients without decreasing postoperative recovery outcomes, particularly in the infusion cohort.

01 Jan 2025·Journal of PeriAnesthesia Nursing

Penehyclidine Hydrochloride: A Promising Antimuscarinic Agent for PONV Prophylaxis in Diverse Surgical Procedures

Review

Author: Alkheder, Ahmad ; El-Nablaway, Mohammad ; Abo Zeid, Mohamed ; Sarhan, Khalid ; AlHussaini, Khalid I ; Elrosasy, Amr ; Khodeer, Dina M ; Saber, Taisir ; Hawas, Yousef ; Abu Salah, Mariam A ; Aissa, Sara Chikh

PURPOSEThe purpose of this meta-analysis is to measure the effectiveness of penehyclidine hydrochloride hydrate (PHC)-an antimuscarinic drug-in preventing postoperative nausea and vomiting (PONV) for different surgeries.DESIGNMeta-analysis.METHODSAccording to the Preferred Reporting Items for Systematic reviews and Meta-Analyses guidelines, we conducted an online literature search using PubMed, Web of Science, Scopus, and Embase databases. Randomized control trials comparing PHC with placebo or any other standard treatments were included.FINDINGSOur systematic review screened 54 articles, and four randomized control trials with 766 patients were included. There was no significant difference between PHC and the control group for the prevention of postoperative vomiting (risk ratio [RR] = 0.43). However, the subgroup analysis showed some promise. At 24 hours, PHC significantly decreased the incidence of postoperative nausea (RR = 0.31), postoperative vomiting (RR = 0.17), and PONV (RR = 0.33). While at 48 hours, PHC showed nonsignificant results for the same outcomes. PHC did not result in significantly higher rates of analgesia use, headache, dizziness, longer durations of stay in the postanesthesia care unit, or longer duration for extubation, but it showed significantly lower results for the use of antiemetics. Furthermore, PHC showed higher rates of dry mouth.CONCLUSIONSThe findings suggest that PHC offers a promising option for PONV prophylaxis, particularly in surgical settings where early PONV are prevalent, with an acceptable safety profile. Further research is recommended to optimize dosing strategies and compare PHC with established antiemetics.

100 Deals associated with Penehyclidine hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	V03AB	DB16287

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Anesthesia	China	Jinzhou Ahon Pharmaceutical Co., Ltd.	24 Oct 2002
Drug intoxication	China	Jinzhou Ahon Pharmaceutical Co., Ltd.	24 Oct 2002

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Biliary pain	Phase 2	China	Chengdu List Pharmaceutical Co., Ltd.	19 May 2017
Spasm biliary	Phase 2	China	Chengdu List Pharmaceutical Co., Ltd.	19 May 2017
Parkinson Disease	Phase 2	China	Chengdu List Pharmaceutical Co., Ltd.	15 Mar 2012
Shock	Phase 2	China	Chengdu List Pharmaceutical Co., Ltd.	15 Mar 2012
Smooth muscle spasm	Phase 2	China	Chengdu List Pharmaceutical Co., Ltd.	15 Mar 2012
Pulmonary Disease, Chronic Obstructive	Phase 2	China	Chengdu List Pharmaceutical Co., Ltd.	21 Jul 2008
Shock, Septic	Phase 1	China	Chengdu List Pharmaceutical Co., Ltd.	11 Jun 2012

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ChiCTR2100050278 (Pubmed \| BMC Anesthesiol)	Phase 4	-	100	Penehyclidine group	wiphidiluu(tudorptksq) = fylstzaexf exnamilkdz (dxgaxksikf )	-	14 Oct 2022
				TIVA group	wiphidiluu(tudorptksq) = pfyfmywrcz exnamilkdz (dxgaxksikf )
Pubmed \| Anesthesiology	Phase 3	-	864	Penehyclidine	lpfibpvwtz(llnwtooxlo) = dry mouth and delirium ohsjapqnjz (vzykgubnks )	Positive	01 Apr 2022
				Placebo
NCT04054479 (Pubmed \| BMC Anesthesiol)	Phase 4	Strabismus	228	Penehyclidine	tbyfrbjsxk(viugzfonwj) = lnchwbezfd qwxlivcaqa (svfdfrqyhk ) View more	-	13 Feb 2021
				Normal saline	tbyfrbjsxk(viugzfonwj) = xjdgyoaafb qwxlivcaqa (svfdfrqyhk ) View more
EULAR2015	Not Applicable	Axial Spondyloarthritis First line	40	90 mg of ET per os 3 times per week	(spnhxdmqll) = dpptuztnbp bffwnximyg (bszrjmslwm, 1 - 8)	-	10 Jun 2015
SICOG 9908 (ASCO2004)	Phase 3	Metastatic breast cancer	132	PET (cisplatin 30 mg/m2/week + epirubicin 50 gm/m2/week + paclitaxel 120 mg/m2/week + G-CSF)	(ynfmsjkyzw) = Anaemia was substantially more frequent in the PET arm eczvioggte (jowanbxtxi ) View more	Positive	15 Jul 2004
				ET (epirubicin 90 mg/m2/ + paclitaxel 175 mg/m2)
SICOG 9908 (ASCO2004)	Phase 3	Locally advanced breast cancer	160	PET (cisplatin 30 mg/m2/week + epirubicin 50 mg/m2/week + paclitaxel 120 mg/m2/week + G-CSF)	ybubrbttku(pidhwihnmk) = substantially more frequent in the PET arm nzqwowbeww (qjgbvdpvwb ) View more	Positive	15 Jul 2004
				ET (epirubicin 90 mg/m2/ + paclitaxel 175 mg/m2)