Overdose of xenobiotics (antihistamines, antipsychotics, or Jimson Weed) with resulting antimuscarinic toxidrome is a common scenario in medical toxicology. The result of antagonism of muscarinic receptors is a constellation of signs and symptoms (toxidrome): mydriasis, decreased sweat, decreased bowel sounds, agitation, delirium, hallucinations, urinary retention, tachycardia, flushed skin and seizures. Two treatment options are physostigmine or benzodiazepines.
Although the antimuscarinic toxidrome occurs commonly, physostigmine has been used sparingly despite evidence of safety and efficacy. To demonstrate the utility and safety of physostigmine, the investigators propose a randomized clinical trial of physostigmine compared to benzodiazepine for antimuscarinic toxicity.

Start Date30 Mar 2017

Sponsor / Collaborator

University of Colorado Denver

[+1]

NCT03013322

/ CompletedNot ApplicableIIT

Anticholium® Per Se a Randomized, Double-blind, Placebo-controlled, Monocentric Trial on the Adjunctive Use of Physostigmine Salicylate (Anticholium®) in Perioperative Sepsis and Septic Shock

Anticholium® per Se is a randomized, double-blind, placebo-controlled, monocentric trial to assess whether the CAP can be transferred from bench to bedside. In this pilot study, 20 patients with perioperative sepsis and septic shock as a result of intra-abdominal infection are enrolled. According to randomization, participants are treated with physostigmine salicylate (verum group) or 0.9% sodium chloride (placebo group) for up to 5 days. The mean Sequential Organ Failure Assessment (SOFA) score during treatment and subsequent intensive care of up to 14 days is used as surrogate outcome (primary endpoint). Secondary outcome measures include 30- and 90-day mortality. An embedded pharmacokinetics and pharmacodynamics study investigates plasma concentrations of physostigmine and its metabolite eseroline. Further analyses will contribute to the understanding of the role of various cytokines in the pathophysiology of human sepsis. A computer-generated list is used for blocked randomization.

Start Date28 Jan 2015

Sponsor / Collaborator

University Hospital Heidelberg

NCT02216266

/ Unknown statusPhase 3IIT

Monocenter, Double Blind, Randomised, Placebo Controlled Study to Evaluate Physostigmine for the Treatment of Delirium in Perioperative Intensive Care Medicine

Evaluation if physostigmine reduces symptoms in patients who has developed a delirium in Intensive care after a surgery

Start Date01 Apr 2014

Sponsor / Collaborator

Hospital of the Johann Wolfgang Goethe University

[+2]

100 Clinical Results associated with Eserine Salicylate

100 Translational Medicine associated with Eserine Salicylate

100 Patents (Medical) associated with Eserine Salicylate

10,427

Literatures (Medical) associated with Eserine Salicylate

01 Jun 2025·Molecular and Biochemical Parasitology

In Silico and in vitro assessment of anti-leishmania infantum activity of a novel cyclohexyl-1,2,4-oxadiazole derivative

Article

Author: Rodrigues, João Pedro Viana ; de Oliveira, Juliana Ramos ; Lourenço, Francisco Dantas ; Nicolete, Roberto ; de Oliveira, Ronaldo Nascimento ; Teixeira, Maria Jânia ; de Moura, Gabriel Acácio ; de Oliveira, Valentina Nascimento Melo ; Rocha, Yasmim Mendes ; de Morais, Selene Maia ; Barbosa, Sara Ingrid Caetano Gomes ; da Silva, Wildson Max Barbosa ; Alves, Daniela Ribeiro ; Pinheiro, Cristian Vicson Gomes

Globally, an estimated 1 billion people reside in endemic areas, and over 12 million individuals are infected with leishmaniasis. Despite its prevalence, leishmaniasis continues to be a neglected disease, mainly affecting underdeveloped countries. In Brazil, the available treatments are pentavalent antimonials and amphotericin B, which are outdated, toxic, require prolonged parenteral administration and have limited efficacy. The heterocyclic ring oxadiazole has been documented in the literature to possess various biological activities, including leishmanicidal properties, thus positioning it as a potential candidate for further investigation. This study aims to evaluate the in vitro leishmanicidal activity of an oxadiazole compound (2i), explore its mechanism of action through enzymatic inhibition and molecular docking, assess its antioxidant activity, and conduct an in silico pharmacokinetic prediction. Pharmacokinetic predictions via ADME/TOX modeling revealed that the 2i molecule exhibits good intestinal absorption (92 %), is water-insoluble (-4 log.mol/L) and demonstrates high permeability in Caco-2 cells (1.35 log.Papp10-6cm/s), suggesting potential for oral administration. Metabolic studies indicated that oxadiazole 2i is an inhibitor of cytochrome P450 enzymes CYP1A2 and CYP2C19, necessitating further evaluation of potential drug interactions. Additionally, it did not exhibit hepatotoxicity or cardiotoxicity; however, it demonstrated mutagenic potential in the salmonella reverse mutation test (AMES), which is a genetic method that detects mutagenic chemical agents, thus justifying more complex confirmatory studies. In vitro assays showed that oxadiazole 2i has DPPH (2,2-diphenyl-1-picrylhydrazyl) radical reducing activity, indicating potential antioxidant properties with an IC₅₀ of 12.10 µg/mL. Concerning its leishmanicidal mechanism of action, molecular docking simulations at the active site of acetylcholinesterase demonstrated that the 2i molecule had superior binding energy values compared to the reference drug physostigmine (-7.39 kcal/mol versus -6.66 kcal/mol, respectively). However, the pharmacophore map revealed that physostigmine had more molecular interactions than oxadiazole 2i. In acetylcholinesterase inhibition assays, the 2i molecule exhibited significant inhibitory activity with an IC₅₀ of 11.91 µg/mL, suggesting a mechanism of action that compromises the parasitic membrane. Moreover, the 2i molecule demonstrated significant leishmanicidal activity against L. infantum with an IC₅₀ of 30.86 μM. Cytotoxicity assays on RAW 264.7 macrophages revealed a high CC₅₀ value of 485.5 µM and a selectivity index (SI) of 17.86. Based on these findings, oxadiazole 2i emerges as a promising candidate for further study, offering prospects for more affordable, selective, and less toxic leishmanicidal agents.

01 Mar 2025·Phytochemical Analysis

Quantification of α‐Acids, β‐Acids, and Phenolic Compounds in Corsican Hops Using LC–MS/MS and Metabolomic Approach Through Molecular Networks

Article

Author: Costa, J. ; Paolini, J. ; Dabbous‐Wach, A. ; Majidi, L. ; Lorenzetti, J. V.

ABSTRACTIntroductionDetermining the bittering profile of hops is a prerequisite for their use in beer making industry. To fully grasp the brewing potential of Corsican hops, it is therefore essential to perform a precise quantification of the molecules responsible for their bittering power.ObjectiveThe aim of this study is highlighting of the bittering profile of Corsican hops.MethodologyA method for the characterization and quantification of α‐acids, β‐acids, and phenolic compounds in Corsican hops using high performance liquid chromatography coupled with tandem mass spectrometry (LC–MS/MS) has been developed. In addition to the six α‐ and β‐acids commonly quantified in hops, seven others hop acids were identified using a new methodology based on the analysis of their fragmentation pattern in full‐scan detection mode. The compounds were then quantified as humulone or lupulone equivalents. Subsequently, a metabolomic analysis of hop cones was conducted using the method of molecular networking.ResultsA total of 28 compounds were quantified. The influence of both annual climate variations and transplantation on the chemical composition of hops extractives was highlighted. The molecular network elucidation led to the identification of 34 compounds. Among them, eight were previously undescribed in hops, including one previously unknown to the literature.ConclusionThe methodologies developed in this study have shed light on the “bittering” potential of Corsican hops which represents a significant economic opportunity for the local brewing industry potentially establishing a new, sustainable, and profitable hops market. This work focuses extensively on the phenolic compounds and the bittering acids of Corsican hops, aiming to highlight their unique organoleptic characteristics and the influence of the Corsican terroir on their chemical composition and abundance.

01 Mar 2025·Pesticide Biochemistry and Physiology

Bioactive flavonoids from Leucosceptrum canum with nematicidal efficacy and mechanistic insights through acetylcholinesterase inhibition and docking study

Article

Author: Rawat, Dharmendra Singh ; Karakoti, Himani ; Dhami, Anamika ; Kumar, Ravendra ; Prakash, Om ; Kumar, Satya

Leucosceptrum canum, a rare Himalayan plant, shows significant bioactive properties, with its nematicidal potential investigated here for the first time. This study isolated and characterized flavonoids from L. canum, assessing their efficacy against the plant-parasitic nematode Meloidogyne incognita. Bioassay-guided fractionation identified three active flavonoids: Pectolinarigenin, 5,6,7-Trihydroxy-4'-methoxyflavone and Acacetin, structurally elucidated using spectroscopic techniques and literature comparisons. The flavonoids exhibited dose-dependent nematicidal activity, with percent mortalities after 96 h of 100 %, 92 %, and 59 %, respectively. LC₅₀ values of Pectolinarigenin (11.79 μg/mL), 5,6,7-Trihydroxy-4'-methoxyflavone (230.54 μg/mL), and Acacetin (679.67 μg/mL) were recorded, comparable to the standard nematicide Nimitz (LC₅₀: 0.01 μg/mL). These flavonoids also showed strong to moderate acetylcholinesterase (AChE) inhibitory activity, with IC₅₀ values of 17.09, 86.72, and 142.2 μg/mL, respectively, nearing the efficacy of standard, physostigmine (IC₅₀: 19.37 μg/mL), suggesting a neuromuscular mechanism of action. The enzyme kinetics analysis of pectolinarigenin revealed it to be a reversible inhibitor of AChE exhibiting mixed-type inhibition, with inhibition constant of 15.94 μg/mL. Molecular docking revealed strong binding affinities (-7.8 to -7.2 kcal/mol) at the AChE active site, highlighting key hydrogen bonds and hydrophobic interactions. ADMET analysis confirmed favorable pharmacokinetic and safety profiles, underscoring the potential of these flavonoids as eco-friendly nematicidal alternatives. This study establishes L. canum as a valuable source of flavonoids with dual nematicidal and AChE inhibitory properties, supported by integrated in vitro and in silico studies. It underscores the untapped phytochemical wealth of Himalayan flora for sustainable nematode management.

News (Medical) associated with Eserine Salicylate

20 Mar 2023

·www.outsourcing-pharma.com

EDSA outlines supply danger to 100 medicines after manufacturer bankruptcy

The End Drug Shortages Alliance (EDSA), a collaboration between healthcare industry stakeholders, has called attention to the risk of drug shortages by publishing a report outlining what treatments could be at risk. The decision to publish the report arrived after Akorn Pharmaceuticals filed for bankruptcy on February 23, 2023, and ceased all manufacturing operations in the US. Prior to the company closing its doors, it possessed a portfolio of over 100 medications. According to EDSA, Akorn was the sole manufacturer for various acute care injectables, including products that are currently in shortage. This includes products such as physostigmine injection, dimercaprol injection, and calcitriol injection. There is currently a mitigation strategy in place for some of the products most at risk, but in the cases where Akorn had less than 100% of the market share for a particular product, such as sufentanil injection, this is not true. “Transparency regarding drug shortages is important to ensure patient care remains uninterrupted,” said Mittal Sutaria, SVP, Vizient pharmacy contract and program services and EDSA board member. “The healthcare system needs time so that pharmaceutical companies can increase manufacturing when possible and providers can develop mitigation strategies to alleviate any potential disruption in supply when a manufacturer exits the market.” EDSA stated that due to the potential for drug shortages, clinicians will need to develop strategies to mitigate the issue, and encouraged them to exercise a ‘stewardship mindset’ when ordering, prescribing and administering medication affected by supply constraints. googletag.cmd.push(function () { googletag.display('text-ad1'); }); Further, the organization advised manufacturers of impacted products to evaluate their ability to maintain or increase product availability for the marketplace. Akorn bankruptcy The problems that Akorn had faced had been ongoing for a number of years. In 2018, the company had attempted to merge with Fresenius Kabi, but the deal had fallen through after the latter company cited operational problems at the former. Following this period, the company looked to sell itself, but could only manage the sale of individual products and brands. Earlier this year , Herald & Review published a letter from Akorn’s then CEO, Douglas Boothe, to employees of the company, announcing that it would file for bankruptcy, As a result of the decision, the company closed all US sites and engaged in a company-wide lay-off of employees.

15 Mar 2023

·www.businesswire.com

End Drug Shortages Alliance Releases Report for Drugs Impacted by Pharmaceutical Plant Closure

IRVING, Texas--( BUSINESS WIRE )--The End Drug Shortages Alliance (EDSA) today released a report assessing the impact to the U.S. market caused by the recent closure of a drug manufacturer. Akorn Pharmaceuticals filed for bankruptcy Feb. 23 and ceased all U.S. manufacturing operations, leaving questions about the impact to the supply of over 100 medications — some essential — including injectable and oral products as well as ophthalmic, otic and topical formulations. The full report may be accessed here . The EDSA report, which was a collaborative effort among Vizient, ASHP, and Children’s Hospital Association (CHA), provides an analysis for products with greatest risk of supply disruption and vulnerability, including four essential medications, that, if not available, would prove the greatest threat to a hospital’s ability to provide immediate and high-quality patient care. As clinicians will need to develop strategies for potential drug shortages, the report offers high-level guidance, including for the impacted essential medications such as adenosine, used in the treatment of supraventricular tachycardia; calcitriol, used to manage hyperparathyroidism in patients undergoing renal dialysis; dimercaprol, an antidote for metal poisoning; mycophenolate mofetil, a prophylaxis for organ rejection; and physostigmine, used in the reversal of anticholinergic syndrome. “Transparency regarding drug shortages is important to ensure patient care remains uninterrupted,” said Mittal Sutaria, senior vice president, Vizient pharmacy contract and program services and EDSA board member. “The healthcare system needs time so that pharmaceutical companies can increase manufacturing when possible and providers can develop mitigation strategies to alleviate any potential disruption in supply when a manufacturer exits the market.” The report assesses data from multiple sources including essential medication status, market share and current ASHP shortage designation to estimate the resilience of a particular product. It also offers recommendations for key stakeholders, including: Manufacturers and wholesalers, to evaluate their ability to maintain or increase product availability or manufacture products for which Akorn was the sole supplier and establish protective allocations to ensure medications are available for patient care. Group purchasing organizations, to pursue novel sourcing strategies and emergency contracting for life-saving medications. Clinicians and providers, to exercise a stewardship mindset and review purchasing and formulary status to determine conservation and mitigation strategies. “The more time providers and the broader health care system have to prepare for a shortage, the better,” said Eric Tichy, division chair, pharmacy supply solutions for Mayo Clinic and EDSA chairperson. “Advance knowledge of supply disruptions is part of the transparency that the End Drug Shortages Alliance has advocated for since forming. Transparency benefits all market participants.” About End Drug Shortages Alliance The End Drug Shortages Alliance is a collaboration of health care industry stakeholders, including providers, group purchasing organizations, manufacturers, distributors and other industry thought leaders dedicated to solving the pharmaceutical supply challenges that disrupt access to essential medications in the U.S. We prioritize initiatives focused on transparency, quality, redundancy and production of additional supply to achieve undisrupted access to essential medications for health care providers and patients.

AHA

100 Deals associated with Eserine Salicylate

External Link

KEGG	Wiki	ATC	Drug Bank
-	Eserine Salicylate	V03AB19 S01EB05	DB00981

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	-	-	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Insulin Resistance	Phase 2	Sweden	AstraZeneca PLC	01 May 2007

Clinical Result

Indication

Phase

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02008292 (nic_physo, CTgov)	Not Applicable	Smoking \| Schizophrenia	80	Physostigmine (ACH Levels in Healthy Controls After Physostigmine Administration)	itwswwwnyv(iuqumplykr) = srlqeruuzj chksvqzmik (rfdterdayb, yorotgcffu - lnamqddigz)	-	06 Feb 2023
				Physostigmine (ACH Levels in Smokers After Physostigmine Administration)	itwswwwnyv(iuqumplykr) = pgfhqclkmv chksvqzmik (rfdterdayb, pctdeiwpca - ryuaomjiop)
NCT03090620 (TAAT, CTgov)	Phase 4	Toxicity	19	Physostigmine (Physostigmine)	uvhfzgqlju(mzxqorzvsg) = fgbrlffsyv qtxctlvoog (akedqqeimt, eerbiebrrm - eoofcslwut) View more	-	23 Aug 2021
				Lorazepam (Lorazepam)	uvhfzgqlju(mzxqorzvsg) = mlhrbtaiwo qtxctlvoog (akedqqeimt, iaglwxpmqz - dtlzbnnoad) View more
SFN2018	Not Applicable	-	-	physostigmine (Ovariectomized rats)	hdvappfkiv(udtzsszwbb) = dqdpovybhz kgioieteuw (hzaprcueph, 3.0)	-	07 Nov 2018
				physostigmine (Intact control rats)	hdvappfkiv(udtzsszwbb) = ymfppqoinn kgioieteuw (hzaprcueph, 3.1)
SFN2002	Not Applicable	-	-	Piribedil	kapnyzhfhr(yfhzboyyll) = bxetlclgdl hrfinoqqym (lmvygwywhu )	-	06 Nov 2002
				Talipexole	kapnyzhfhr(yfhzboyyll) = desqddmmvk hrfinoqqym (lmvygwywhu )

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