rivastigmine / Generic mfg. - LARVOL DELTA

Application of acoustic ejection mass spectrometry for plasma protein binding assay using flux dialysis. (PubMed, Drug Metab Dispos) - "Herein, we validated this approach using 10 commercially available compounds with known fu values-imipramine, indomethacin, itraconazole, lapatinib, nicardipine, warfarin, chlorpromazine, rivastigmine, zonisamide, and ritonavir-with a wide fu range covering from very high binding (fu ≤ 0.01) to low binding (fu > 0.10) in human plasma. SIGNIFICANCE STATEMENT: This study bridges the gap between flux dialysis and acoustic ejection mass spectrometry by creating a synergistic analytical framework for plasma protein binding assays, addressing limitations of both methods and enabling high-throughput applications with improved accuracy and efficiency. The combination of flux dialysis and acoustic ejection mass spectrometry will make a positive contribution to the development of high-throughput in vitro absorption, distribution, metabolism and excretion assays in drug discovery."

Journal

Creatine and Taurine as Novel Competitive Inhibitors of Acetylcholinesterase: A Biochemical Basis for Nutritional Modulation of Brain Function. (PubMed, Int J Mol Sci) - "While clinically approved AChE inhibitors such as donepezil, rivastigmine, and galantamine are used in the symptomatic treatment of Alzheimer's disease and related dementias, little is known about the modulatory effects of common dietary compounds on AChE activity. Docking confirmed that both ligands preferentially occupy the active-site region in a manner consistent with competitive inhibition, with CR showing more favorable binding scores than TA. Although markedly weaker than clinical drugs, these findings provide the first biochemical and in silico evidence that CR and TA directly interact with AChE, suggesting subtle cholinergic modulation relevant to cognitive function and neuroprotection."

Journal • CNS Disorders • Dementia • Pain

Emerging of a new neuroprotective isoflavonoid with potent Keap1/Nrf2/ARE pathway activation and AChE inhibition. (PubMed, Bioorg Chem) - "Notably, it markedly upregulated vital antioxidant defense systems and efficiently inhibited the AChE (IC50 = 14.79 μM), surpassing the efficacy of the reference drug rivastigmine (IC50 = 24.5 μM). Furthermore, compound 32 significantly ameliorated memory impairment and the neuroinflammation associated with scopolamine-initiated cognitive dysfunction in a zebrafish model. Collectively, this study identifies compound 32 as a promising dual-acting neuroprotective lead, offering potential value for advancing therapeutic strategies in AD drug development."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Inflammation • Pain

Transdermal Drug Delivery Systems: A Comprehensive Review of Mechanisms, Technologies, and Clinical Applications. (PubMed, Pharm Res) - "Future directions in TDDS research focus on integrating nanotechnology, AI-driven optimization, wearable sensors, and closed-loop smart systems. These integrations aim to achieve greater precision, personalization, and efficiency in transdermal drug delivery, providing valuable insights for future research and translational development."

Journal • Review • Cardiovascular • CNS Disorders • Nicotine Addiction • Pain

Effects of rivastigmine on the pathogenesis of the experimental trypanosomiasis. (PubMed, Parasitol Int) - "In silico analysis revealed that AChE exerts a catalytic role on ACh through the catalytic triad (Ser200; HIS440; Glu327), rivastigmine being associated with the His440 binding site. Rivastigmine reduced parasitemia and mortality in vivo in the acute phase of infection, suggesting a potential modulatory role on the non-neuronal cholinergic pathway, although further studies are required to understand it."

Journal • Infectious Disease • Inflammation • Pain

Chemical Profiling of Gmelina philippensis Cham. Leaf Extract and Its Antioxidant and Anti-Cholinesterase Properties. (PubMed, Plants (Basel)) - "Overall, these findings highlight that G. philippensis as a rich source of multi-target bioactive compounds, supporting that the extract has good anti-acetylcholinesterase activity comparable to the rivastigmine that used in neurodegenerative disease. This study provides a promising foundation for the development of novel therapeutic approaches targeting neurodegenerative diseases."

Journal • Alzheimer's Disease • CNS Disorders

Successful resolution of Capgras syndrome with rivastigmine treatment in Lewy body dementia. (PubMed, BMJ Case Rep) - "Despite initial challenges in management, including thought blocking and word-finding difficulty, the patient experienced complete resolution of symptoms following treatment with rivastigmine, a cholinesterase inhibitor, commonly used in major neurocognitive disorders. This case highlights the potential efficacy of cholinesterase inhibitors in alleviating psychotic symptoms associated with Capgras syndrome, particularly in individuals with LBD."

Journal • CNS Disorders • Cognitive Disorders • Dementia • Developmental Disorders • Lewy Body Disease • Psychiatry

Comparative safety of cholinesterase inhibitors and memantine for dementia: a protocol for a network meta-analysis of randomized controlled trials. (PubMed, Syst Rev) - "By addressing gaps in prior NMAs, this study aims to provide an in-depth evaluation of safety outcomes associated with different ChEI and memantine doses and formulations across various dementia types. The findings will support clinicians in making informed treatment decisions and guide future research and policy development for dementia management."

Journal • Retrospective data • CNS Disorders • Dementia

β-Caryophyllene Ameliorates STZ-Induced Alzheimer's Disease-Like Conditions in Rats via Modulation of Brain-Derived Neurotrophic Factor, Synaptic Plasticity, and Neuroinflammation. (PubMed, Eur J Neurosci) - "Rats received BCP (10, 20 mg/kg, i.p.) or rivastigmine (2.5 mg/kg) for 28 days...Histopathology confirms normal hippocampal neuronal architecture in BCP-treated groups. These findings highlight the ability of BCP to modulate BDNF signaling, synaptic plasticity, and neuroinflammatory pathways, underscoring its potential as a multitarget therapeutic candidate for AD."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Inflammation • BDNF • IL1B • IL6 • NCAM1 • SYP • TNFA

Dementia medications and the use of psychotropic drugs: A cross-sectional study in Saudi healthcare. (PubMed, J Alzheimers Dis) - "The analysis revealed memantine (62.4%) and rivastigmine (37.6%) as the most commonly prescribed medications, with a notable increase in prescriptions among older adults and a higher prevalence in married patients. Among psychotropic medications, quetiapine, lorazepam, and citalopram were the most frequently used, with quetiapine leading in prescription numbers (27%).ConclusionsThis study provides insights into current prescribing patterns for dementia in Saudi Arabia. Future research should address limitations in coding information and long-term outcomes to improve the management of dementia."

Journal • Observational data • Alzheimer's Disease • CNS Disorders • Dementia

Effect of Alzheimer's disease medications on neurocognitive outcomes in children and adolescents with autism spectrum disorder and low IQ: a scoping review. (PubMed, Transl Psychiatry) - "This scoping review identified promising evidence of neurocognitive improvement in children and adolescents with ASD and low IQ following treatment with either a cholinesterase inhibitor or an NMDA receptor antagonist. Considering the lack of FDA-approved treatments for the cognitive deficits associated with ASD and an absence of medications approved to treat core features of ASD, our findings highlight an opportunity for innovative directions in autism research and treatment."

Journal • Review • Alzheimer's Disease • Autism Spectrum Disorder • CNS Disorders • Cognitive Disorders • Developmental Disorders • Genetic Disorders • Mental Retardation

Pyranotacrines as prospective multi-target compounds against Alzheimer's disease. (PubMed, Bioorg Med Chem) - "A series of tacrine-based 4-H-pyran derivatives were synthesized and biologically estimated as multifactorial ligands against Alzheimer's disease...Moreover, its inhibitory activity against BuChE was 8-folds more active than rivastigmine with IC50 = 0.09 ± 0.016 μM...Additionally, it showed higher anti-oxidative activity with 10.36 TE and chelating anchors activity for metal ions. The safety of 6c towards SH-SY5Y normal cells and HepG2 cancer cells was interesting with safety index ratio (Si = 2273), in addition to its BBB permeability and pharmacokinetic profile."

Journal • Alzheimer's Disease • CNS Disorders • Oncology • Pain

Persistence With Antidementia Therapy in Germany: A Retrospective Cohort Study of 212,850 Patients (ISPOR-EU 2025) - "In this large-scale retrospective cohort study, two-thirds of patients discontinued antidementia therapy within three years, with younger age, female sex, and use of rivastigmine, donepezil, or galantamine linked to higher discontinuation risks. Initiation by a neuropsychiatrist was associated with improved persistence among the oldest patients, highlighting the potential impact of prescriber specialty on long-term therapy adherence."

Retrospective data • CNS Disorders • Psychiatry

Economic Evaluation in Alzheimer's Disease: A Systematic Review (ISPOR-EU 2025) - "Earlier studies (pre-2010) frequently evaluated cholinesterase inhibitors such as donepezil, while later studies incorporated memantine, rivastigmine, and non-pharmacologic approaches, including caregiver training and cognitive therapy. Economic evaluations in AD reflect shifting treatment paradigms and methodological innovation. These findings provide essential groundwork for future cost-effectiveness studies of acupuncture and underscore the importance of including caregiver costs and societal perspectives."

HEOR • Review • Alzheimer's Disease • CNS Disorders • Gene Therapies

Care Dependency and Sick Leave Patterns in Early Alzheimer's Disease: A Retrospective Claims Data Analysis in Germany (ISPOR-EU 2025) - "Early AD was defined as de-novo prescriptions of AChE inhibitor (AChEIs: donepezil, galantamine, or rivastigmine) in individuals aged ≥50 years (index), without memantine prescriptions within 100-days. Care dependency emerges early in AD. Sick leave - especially related to psychiatric comorbidities - may serve as early indicators. Earlier recognition and intervention may delay care dependency and preserve independence."

Retrospective data • Alzheimer's Disease • CNS Disorders • Depression • Psychiatry

Hyperhomocysteinemia alters growth factors and neurotrophins in rat hippocampus: Neuroprotective role of ibuprofen and rivastigmine (SSIEM 2023) - No abstract available

Preclinical • Metabolic Disorders

Hyperhomocysteinemia alters growth factors and neurotrophins in rat hippocampus: Neuroprotective role of ibuprofen and rivastigmine (SSIEM 2023) - No abstract available

Preclinical • Metabolic Disorders

Hyperhomocysteinemia alters growth factors and neurotrophins in rat hippocampus: Neuroprotective role of ibuprofen and rivastigmine (SSIEM 2023) - No abstract available

Preclinical • Metabolic Disorders

Hyperhomocysteinemia alters growth factors and neurotrophins in rat hippocampus: Neuroprotective role of ibuprofen and rivastigmine (SSIEM 2023) - "Treatments with rivastigmine and ibuprofen attenuated some of these harmful effects. Reversal of HHcy damage by these compounds may be a potential neuroprotective strategy for brain damage."

IO biomarker • Preclinical • Alzheimer's Disease • CNS Disorders • Metabolic Disorders • Vascular Neurology • CX3CL1 • GFAP • NGFR • NTRK2 • TLR4

Genetic and Functional Dynamics of Butyrylcholinesterase in Alzheimer's Disease: From Mechanisms to Clinical Relevance. (PubMed, Chem Biol Interact) - "Evidence from biochemical, histological, and clinical studies indicates that BChE influences both the pathophysiology of AD and the effectiveness of cholinesterase inhibitor therapy, with rivastigmine providing unique benefits through dual AChE and BChE inhibition...Despite these advances, uncertainties remain regarding the precise dynamics of BChE activity across disease stages, its contribution to plaque maturation and inflammation, and its influence on responses to novel anti-amyloid antibody therapies. Overall, BChE represents a multifaceted factor in AD pathogenesis, therapy, and biomarker development, warranting further genotype-stratified and mechanistic investigations to clarify its clinical utility."

Journal • Alzheimer's Disease • CNS Disorders • Inflammation • Pain

Brexpiprazole-Induced Rhabdomyolysis and Extrapyramidal Symptoms in an Alzheimer Dementia Patient on Rivastigmine. (PubMed, Am J Ther) - No abstract available

Journal • Alzheimer's Disease • CNS Disorders • Dementia

Validation of a highly sensitive assay for the determination of rivastigmine in human plasma for pharmacokinetic studies. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "The internal standard used was atazanavir-d5. The total analysis time per sample was only 3 min. This method was successfully applied to determine the pharmacokinetic parameters of rivastigmine after a single oral dose of 1.5 mg (capsules) in 26 healthy volunteers."

Journal • PK/PD data

Design of N-salicyltryptamines-based highly selective BChE inhibitors to elevate brain acetylcholine, improve learning, and reduce amyloid-β in Alzheimer's disease. (PubMed, Eur J Med Chem) - "Besides, ameliorated scopolamine-induced cognitive deficits superior to rivastigmine. Crucially, 17 demonstrated greater acetylcholine elevation than rivastigmine in mice brain, attributable to its highly selective BChE inhibition. This study identifies 17 as a promising AD therapeutic candidate and validates the potential of the N-Salicyltryptamines-based dual-targeting approach."

Journal • Alzheimer's Disease • CNS Disorders • Cognitive Disorders

From the hive to the brain: synergistic potential of honeybee products with alzheimer's drugs. (PubMed, Metab Brain Dis) - "In conclusion, bee products combined with donepezil and rivastigmine can be considered a potential neuroprotective agent against AD. Further studies are needed to support the preclinical studies and promote the clinical trials."

Journal • Review • Alzheimer's Disease • CNS Disorders • Cognitive Disorders • Dementia

Neuroprotective Effect of Empagliflozin/Rivastigmine in Alzheimer's Disease Rat Model: Optimization of Multifaceted Mechanism of Action. (PubMed, Drug Dev Res) - "Group I served as the control, while groups II, III, IV, and V received the scopolamine plus heavy metal mixture for AD induction. The findings suggest that EMPA may be a viable candidate for future therapeutic exploration in AD, which has a multifaceted mechanism of action encompassing anti-neuroinflammation, antioxidant stress, and enhanced glucose metabolism, as well as decreased acetylcholinesterase activity and phosphorylated tau protein levels. Interestingly, combined treatment showed a superior effect than EMPA alone."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders • Inflammation • IL10