Delving into the Latest Updates on Papaverine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Papaverin Hydrochloride and Sodium Chloride, Papaverine, Papaverine Hydrochloride and Sodium Chloride

+ [9]

Target

PDE10A

Mechanism

PDE10A inhibitors(Phosphodiesterase 10A inhibitors)

Therapeutic Areas

Nervous System DiseasesCardiovascular Diseases

Active Indication

Peripheral ischaemiaVisceral spasms

Inactive Indication-

Originator Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Active Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

CN (01 Jan 1982),

Peripheral ischaemiaVisceral spasms

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC20H21NO4

InChIKeyXQYZDYMELSJDRZ-UHFFFAOYSA-N

CAS Registry58-74-2

View All Structures (2)

Three artificial imine reductases, constructed via supramolecular anchoring utilising Fe^III-azotochelin, a natural siderophore, to bind an iridium-containing catalyst to periplasmic siderophore-binding protein (PBP) scaffolds, have previously been synthesised and subjected to catalytic testing. Despite exhibiting high homology and possessing conserved siderophore anchor coordinating residues, the three artificial metalloenzymes (ArMs) displayed significant variability in turnover frequencies (TOFs). To further understand the catalytic properties of these ArMs, their kinetic behaviour was evaluated with respect to the reduction of three cyclic imines: dihydroisoquinoline, harmaline, and papaverine. Kinetic analyses revealed that all examined ArMs adhere to Michaelis-Menten kinetics, with the most pronounced saturation profile observed for the substrate harmaline. Additionally, molecular docking studies suggested varied hydrogen-bonding interactions between substrates and residues within the artificial binding pocket. Pi-stacking and pi-cation interactions were identified for harmaline and papaverine, corroborating the higher affinity of these substrates for the ArMs in comparison to dihydroisoquinoline. Furthermore, it was demonstrated that multiple cavities are capable of accommodating substrates in close proximity to the catalytic centre, thereby rationalising the moderate enantioselectivity conferred by the unmodified scaffolds.

04 Oct 2024·Medicine

Symmetrical peripheral gangrene caused by urosepsis: Case reports and literature review

Review

Author: Chen, Yuanyuan ; Cheng, Chuji ; Zhu, Lianghua ; Liu, Kai ; Xu, Xiujuan ; Zha, Junjing ; Wu, Gaofei

Rationale:Symmetrical peripheral gangrene (SPG) is a serious and rare complication in patients with urosepsis, characterized by distal limb symmetry impairment.Patient concerns:In this study, 3 cases of SPG caused by urosepsis were reported, and the Chinese and English literature on SPG caused by urosepsis was reviewed. The demographic, clinicopathological, treatment, and follow-up data of the patients were summarized and analyzed.Diagnosis:SPG was diagnosed with clinical symptoms.Interventions:We conducted urological invasive surgery, administered anti-infective therapy, implemented fluid resuscitation and blood product transfusion, provided mechanical ventilation support, optimized myocardial contractility, administered heparin and B vitamins, utilized papaverine for vasodilation, performed hemodialysis and plasma exchange, peripheral skin warming along with other treatment modalities.Outcomes:Two patients died and 1 patient underwent autoamputation.Lessons:Our cases and literature review demonstrate that timely and accurate diagnosis, effective infection control, correction of hypoperfusion, organ function support, early management of disseminated intravascular coagulation, avoidance of premature amputation, and multidisciplinary comprehensive treatment are crucial for the successful treatment of SPG caused by urosepsis.

25 Sep 2024·Sexual Medicine Reviews

Unveiling the science behind erectile dysfunction topical therapy: investigating transdermal papaverine as a novel treatment approach

Review

Author: Langarizadeh, Mohammad Amin ; Rezaiezadeh, Hojjat ; Saeedi Garaghani, Zahra ; Karami-Mohajeri, Somayyeh ; Ranjbar Tavakoli, Marziyeh

AbstractIntroductionErectile dysfunction is among the most prevalent urologic issues affecting men globally and is characterized by a high incidence rate. This condition significantly affects the quality of life of patients and their sexual partners.ObjectivesDue to the interactions, contraindications, and side effects associated with systemic drugs, recent research has increasingly focused on topical and transdermal medications for the treatment of erectile dysfunction.MethodsBased on previous studies, this article examines papaverine in terms of local effectiveness, methods of increasing therapeutic efficiency, possible local side effects, and evaluation of its various formulations.ResultsAmong these approaches, notable strategies include using novel formulations and nanoformulations as compared with classic ones, employing permeation enhancers, and combining treatments with other oral and topical drugs with synergistic mechanisms. These methods aim to improve transdermal papaverine’s bioavailability and therapeutic efficacy while minimizing side effects and enhancing patient compliance.ConclusionTransdermal papaverine may not be as effective as its injectable form, but the treatment path is more pleasant, with less pain and fewer side effects for patients. For this reason, using solutions that remove the penile skin and fascial absorption barrier can be very effective.

100 Deals associated with Papaverine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D02218	Papaverine Hydrochloride	A03AD01 G04BE02	DB01113

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Peripheral ischaemia	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	01 Jan 1982
Visceral spasms	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	01 Jan 1982

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AUA2024	Not Applicable	Spermatic Cord Torsion	-	Papaverine injection	fbbrxvmgxq(kuxfnoxndg) = ikdburqugv desyamfbrf (xagmfsnrzk )	-	01 May 2024
				No papaverine injection	fbbrxvmgxq(kuxfnoxndg) = bleaaplzqs desyamfbrf (xagmfsnrzk )
NCT03894904 (CTgov)	Phase 4	Anesthesia \| Vasospasm	100	Heparin+Papaverine (Papaverine Plus Heparin During Procedure, With Rescue Papaverine as Needed)	gggsigeqkc(edigcypdcx) = zmzobnwdmm fgrtewjuzu (ofzgucddou, mfvjxqkcxm - mfbjclixqe) View more	-	27 Oct 2022
				Heparin+Rescue papaverine, as needed (Heparin During Procedure, With Rescue Papaverine as Needed)	gggsigeqkc(edigcypdcx) = rrpocnlmzx fgrtewjuzu (ofzgucddou, nhmuhphvjk - yjslbdtvsh) View more
NCT00955929 (CTgov)	Not Applicable	Penile Neoplasms \| Erectile Dysfunction	76	sildenafil (PRN Sildenafil)	mprzfjpwzr(pvucqekshj) = cmqtodaerr sshrowhdrh (tngphpssem, qlivmuiwvg - hofswnoobo) View more	-	08 Nov 2021
				questionnaire+Sildenafil (Nightly Sildenafil Arm)	mprzfjpwzr(pvucqekshj) = luquoiwzkr sshrowhdrh (tngphpssem, zfbfvemsjt - yynecuusid) View more