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donepezil hydrochloride (Aricept jelly / donepezil jelly)

✓ Approved

Eisai Co., Ltd. · ACHE · Small Molecule

What is donepezil hydrochloride?

donepezil hydrochloride is a small molecule developed by Eisai Co., Ltd.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesAricept jelly, donepezil jelly
CompanyEisai Co., Ltd.
Drug ClassSmall Molecule
Molecular TargetACHE
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Eisai Co., Ltd.

Mechanism of Action

Molecular Targets

donepezil hydrochloride acts on 1 molecular target:

ACHEacetylcholinesterase (Cartwright blood group) (N-ACHE, ACEE)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

donepezil hydrochloride is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersDementia Alzheimer's type✓ Approved
Nervous system disordersDementia with Lewy bodies✓ Approved

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Isatin derivatives as potent cholinesterase inhibitors: recent developments and future challenges.

Shahzad Muhammad M, Mushtaq Alia A, Rochais Christophe C, Naseer Muhammad Moazzam MM

Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by cognitive decline, memory impairment, and neuronal loss, primarily associated with β-amyloid plaque deposition, tau hyperphosphorylation, and cholinergic dysfunction. Since the disruption of cholinergic neurotransmission is a key pathological feature of AD, the cholinesterase (ChE) inhibitors targeting acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) remain the mainstay of symptomatic treatment by enhancing synaptic acetylcholine levels. However, the currently approved small molecules, including tacrine, donepezil, rivastigmine, and galantamine, are limited by their modest efficacy, poor selectivity, and adverse effects, necessitating the development of improved therapeutic agents. Among emerging scaffolds, isatin (1H-indole-2,3-dione) has attracted considerable research attention owing to its structural versatility, synthetic accessibility, and favorable pharmacological properties. Recent studies have reported diverse isatin-based derivatives, including hydrazones, Schiff bases, thiosemicarbazones, spirooxindoles, and molecular hybrids, exhibiting potent AChE and BChE inhibitory activities, often in the submicromolar or nanomolar ranges. Structure-activity relationship studies have revealed the critical influence of electronic effects, linker optimization, N-substitution, and molecular hybridization on inhibitory potency and selectivity. This review summarizes the most promising isatin-based cholinesterase inhibitors reported from 2020 to the present, highlighting their biological activities, structure-activity relationships, and potential for the development of next-generation anti-Alzheimer therapeutics.

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Ritodrine hydrochloride is a commonly used tocolytic agent for threatened preterm labor in Japan, despite its serious adverse events and limited use in many other countries. National obstetric guidelines have shifted toward restricting its use, but the evidence-practice gap remains unclear. The aim of this study is to determine usage trends for ritodrine at nationwide and prefectural levels and identify factors associated with usage. We conducted an ecological study linking nationwide aggregated medical claims data and statistical survey records across all 47 prefectures. We investigated 10-year trends in ritodrine use from fiscal year (FY) 2014 to 2023. Choropleth maps and spatial statistics illustrated geographic relationships among neighboring prefectures. We also conducted a cross-sectional study to identify factors associated with ritodrine injection use. The usage rate of ritodrine injection per 1000 deliveries decreased by more than 45% over 10 years. Joinpoint regression analysis identified FY2017 as a turning point, after which the decline accelerated. However, prefectural usage varied up to 13.58-fold, with spatial clustering of high-use regions. Factors associated with injection usage included the density of Perinatal Medical Centers (PMCs), hospital admissions for threatened preterm labor and preterm birth per 1000 deliveries, and the proportion of hospitals among delivery facilities. This study showed that nationwide use of ritodrine injection decreased by half over a decade, along with regional disparities among prefectures in Japan. These variations might reflect localized treatment policies influenced by differences in healthcare resources and geographical accessibility.

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Microwave-induced efficient degradation of tetracycline using magnetic ZnFe2O4 nanoparticles anchored on C/SiO2.

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In response to the ecological and health risks posed by Tetracycline Hydrochloride (TCH) residues in the environment, this study develops a microwave-induced catalytic system using ZnFe2O4/C/SiO2 nanocomposites for efficient TCH degradation. The composites were prepared by anchoring ZnFe2O4 nanoparticles onto a rice husk-derived C/SiO2 support, leveraging both the thermal and non-thermal effects of microwave irradiation to synergistically enhance catalytic performance. Our results showed that the porous structure of C/SiO2 effectively dispersed ZnFe2O4 nanoparticles, reduced agglomeration, and significantly improved microwave absorption by balancing dielectric loss and magnetic loss, with a reflection loss reaching -41.97 dB. Under optimized conditions (microwave power: 1000 W, catalyst dosage: 100 mg, reaction time: 21 min), the degradation rate of 60 ppm TCH exceeded 99%. Free radical trapping and EPR analyses confirmed that holes (h+) are the dominant active species responsible for degradation, and oxygen vacancies promote electron-hole separation. Recycling experiments showed that the catalyst maintained a degradation efficiency of over 75% after four cycles, indicating good stability. This study offers an efficient and sustainable microwave catalytic technology for organic wastewater treatment, with the added environmental benefit of utilizing agricultural waste.

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High protein concentrations often lead to high viscosity, necessitating reduced solution viscosity. We investigated the effects of eight anionic excipients commonly used in biopharmaceutical formulations on the solution viscosity of high-concentration monoclonal antibodies using three antibodies with different isoelectric points. The three antibodies exhibited attractive or repulsive protein-protein interaction tendencies in histidine buffer without anionic excipients. The effect of adding anionic excipients on solution viscosity differed by interaction tendencies. Preferential interaction coefficients revealed differences in the extent of interaction between individual anionic excipients and antibodies. Comparison with chloride, positioned in the middle of the Hofmeister series, suggested that the observed viscosity behavior could only be partially explained by the previously reported Hofmeister anion effects on solution viscosity. We examined the effects of combining L-arginine with each anionic excipient as a counter anion. Formulations containing L-arginine and other anionic excipients contributed more strongly to reducing solution viscosity than L-arginine hydrochloride. The effects of anionic excipients on viscosity can be understood in terms of protein-protein interactions of an antibody in the presence of anionic excipients; whether anionic excipients strengthen or weaken the intrinsic protein-protein interactions is important, underscoring the key indicator for selecting the optimal anionic excipients when designing high-concentration formulations with lower viscosities.

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Duan Wenna W, Jiang Qiu Q, Shang Guichun G, Liu Jingbo J et al.

This research explored the bioactive components and therapeutic mechanisms of Qizhi Yishen Capsule (QZC) in managing early-stage diabetic kidney disease (DKD) by integrating network pharmacology with experimental evidence, aiming to support its clinical utility with scientific validation. Network pharmacology and molecular docking were utilized to identify QZC's potential targets in DKD treatment. The therapeutic impact of QZC on renal damage in DKD rats was assessed through in vivo tests, including serum biochemistry, histological staining, and transmission electron microscopy analysis.Potential mechanisms were further explored through metabolomics, in vitro experiments, qRT-PCR, and Western blot analysis. The renal protective effects of QZC in DKD were predicted to be mediated via signaling pathways such as PI3K-Akt, AMPK, and MAPK, based on network pharmacology analysis. In vivo studies confirmed that QZC (509 mg·kg-1), in combination with metformin hydrochloride tablets (MET, 104 mg kg-1), significantly alleviated pathological renal injury and improved podocyte ultrastructure in DKD rats. Metabolomics analysis identified 420 candidate biomarkers, of which 157 were upregulated in the DKD model group and downregulated after QZC treatment, and 263 showed the opposite trend. These metabolites were mainly involved in starch and sucrose metabolism, tyrosine metabolism, phenylalanine metabolism, cysteine and methionine metabolism, and the biosynthesis of phenylalanine, tyrosine, and tryptophan. In vitro assays demonstrated that QZC (300 μg ml-1), gamma-linolenic acid (GLA, 12 μmol L-1), and methyl caffeate (MC, 12 μmol L-1)-two active constituents of QZC-significantly inhibited apoptosis in HK-2 cells, regulated the cell cycle, and reduced reactive oxygen species (ROS) levels. qRT-PCR and Western blot analyses indicated that QZC activated AMPK, SIRT1, and PGC-1α expression at the mRNA and protein levels. QZC improves hyperglycemia-induced tubular injury and metabolic disorders in DKD rats by suppressing oxidative stress and apoptosis through multi-component and multi-target regulation of the AMPK/SIRT1/PGC-1α signaling pathway. This study integrates network pharmacology, metabolomics, and experimental validation to systematically elucidate, for the first time, the multi-component basis and the AMPK/SIRT1/PGC-1α pathway mechanism underlying QZC's efficacy against early DKD.

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Zhang Shuxin S, Li Lin L

Attention deficit hyperactivity disorder (ADHD) is a prevalent childhood disorder with existing treatment challenges, and research on the combined therapy of methylphenidate hydrochloride and sensory integration training for it is inconclusive. Thus, this study explored the clinical efficacy of this combined treatment in children with ADHD, finding it significantly improved relevant scores and reduced adverse reactions, suggesting its potential for wider use. From June 2022 to June 2023, a research sample of 102 individuals diagnosed with ADHD was recruited and allocated into 2 groups at an observation group (n=52) and a control group (n=50). Exclusively methylphenidate hydrochloride extended-release tablets were given to the control group as treatment, whereas the observation group underwent combined therapy with methylphenidate hydrochloride extended-release tablets and sensory integration training. The assessment and comparison of sensory integration and praxis tests, full-scale response control quotient, full-scale attention quotient, Conners' behavior rating scale, and adverse reactions during the treatment period were conducted prior to and following 2 treatment cycles in both the observation and control groups. Prior to treatment, there were no remarkable variations (P > .05) in the scores of sensory integration and praxis tests, Integrated Visual and Auditory Continuous Performance Test (IVA-CPT) scores, and behavior rating scale between the 2 groups. Following the treatment, the observation group exhibited notably superior scores in the sensory integration and praxis test, IVA-CPT, and behavior rating scale, with a notably reduced occurrence of complications, in comparison to the control group (P < .05). To summarize, the utilization of methylphenidate hydrochloride alongside sensory integration training has demonstrated promising effectiveness in treating children diagnosed with ADHD and deserves broader implementation.

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