Cited by 368Cholinesterase and Neurodegenerative DiseasesAlzheimer's disease research and treatmentsPharmacogenetics and Drug Metabolism

The DOI matches its Crossref record; 101 of the 105 references it cites were found in a registry or an index.

Clinical Pharmacokinetics and Pharmacodynamics of Cholinesterase Inhibitors

Jann, Michael W., Shirley, Kara L., Small, Gary W.·2002·Clinical Pharmacokinetics

DOI 10.2165/00003088-200241100-00003

Open this paper in CoChat — free account

Abstract

Cholinesterase inhibitors are the 'first-line' agents in the treatment of Alzheimer's disease. This article presents the latest information on their pharmacokinetic properties and pharmacodynamic activity. Tacrine was the first cholinesterase inhibitor approved by regulatory agencies, followed by donepezil, rivastigmine and recently galantamine. With the exception of low doses of tacrine, the cholinesterase inhibitors exhibit a linear relationship between dose and area under the plasma concentration-time curve. Cholinesterase inhibitors are rapidly absorbed through the gastrointestinal tract, with time to peak concentration usually less than 2 hours; donepezil has the longest absorption time of 3 to 5 hours. Donepezil and tacrine are highly protein bound, whereas protein binding of rivastigmine and galantamine is less than 40%. Tacrine is metabolised by hepatic cytochrome P450 (CYP) 1A2, and donepezil and galantamine are metabolised by CYP3A4 and CYP2D6. Rivastigmine is metabolised by sulfate conjugation. Two cholinesterase enzymes are present in the body, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Tacrine and rivastigmine inhibit both enzymes, whereas donepezil and galantamine specifically inhibit AChE. Galantamine also modulates nicotine receptors, thereby enhancing acetylcholinergic activity at the synapse. These different pharmacological profiles provide distinctions between these agents. Cholinesterase inhibitors show a nonlinear relationship between dose and cholinesterase inhibition, where a plateau effect occurs. Cholinesterase inhibitors display a different profile as each agent achieves its plateau at different doses. In clinical trials, cholinesterase inhibitors demonstrate a dose-dependent effect on cognition and functional activities. Improvement in behavioural symptoms also occurs, but without a dose-response relationship. Gastrointestinal adverse events are dose-related. Clinical improvement occurs with between 40 and 70% inhibition of cholinesterase. A conceptual model for cholinesterase inhibitors has been proposed, linking enzyme inhibition, clinical efficacy and adverse effects. Currently, measurement of enzyme inhibition is used as the biomarker for cholinesterase inhibitors. New approaches to determining the efficacy of cholinesterase inhibitors in the brain could involve the use of various imaging techniques. The knowledge base for the pharmacokinetics and pharmacodynamics of cholinesterase inhibitors continues to expand. The increased information available to clinicians can optimise the use of these agents in the management of patients with Alzheimer's disease.

Integrity signals

Registry

Crossref · 10.2165/00003088-200241100-00003

Cites

101 of 101 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

This paper’s full text isn’t openly available, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

“Mini-mental state”
Folstein, M. F., Folstein, S. E., & McHugh, P. R. (1975) · Journal of Psychiatric Research · doi:10.1016/0022-3956(75)90026-6 · Cited by 88,282
[Japanese version of the Neuropsychiatric Inventory--a scoring system for neuropsychiatric disturbance in dementia patients].
Hirono, N., Mori, E., Ikejiri, Y., Imamura, T., Shimomura, T., Hashimoto, M., Yamashita, H., & Ikeda, M. (1997) · PubMed · Cited by 21,012
Special Care Units and Traditional Care in Dementia: Relationship with Behavior, Cognition, Functional Status and Quality of Life - A Review
Kok, J. S., Berg, I. J., & Scherder, E. J. A. (2013) · Dementia and Geriatric Cognitive Disorders Extra · doi:10.1159/000353441 · Cited by 20,589
Older Adults' Reasons for Using Technology while Aging in Place
Peek, S. T. M., Luijkx, K. G., Rijnaard, M. D., Nieboer, M. E., van der Voort, C. S., Aarts, S., van Hoof, J., Vrijhoef, H. J., & Wouters, E. (2015) · Gerontology · doi:10.1159/000430949 · Cited by 19,852
Sensitivity and False Alarm Rate of a Fall Sensor in Long-Term Fall Detection in the Elderly
Kangas, M., Korpelainen, R., Vikman, I., Nyberg, L., & Jämsä, T. J. (2014) · Gerontology · doi:10.1159/000362720 · Cited by 19,007
The Neuropsychiatric Inventory: Comprehensive assessment of psychopathology in dementia
Cummings, J. L., Mega, M., Gray, K., Rosenberg-Thompson, S., Carusi, D. A., & Gornbein, J. (1994) · Neurology · doi:10.1212/wnl.44.12.2308 · Cited by 7,568
A new rating scale for Alzheimer's disease
(1984) · American Journal of Psychiatry · doi:10.1176/ajp.141.11.1356 · Cited by 4,175
Psychopharmacology: The Fourth Generation of Progress
Bloom, F. E., & Kupfer, D. J. (1995) · Medical Entomology and Zoology · Cited by 2,985
Statins and the risk of dementia
Jick, H., Zornberg, G. L., Jick, S. S., Seshadri, S. S., & Drachman, D. (2000) · The Lancet · doi:10.1016/s0140-6736(00)03155-x · Cited by 1,764
A 24-week, double-blind, placebo-controlled trial of donepezil in patients with Alzheimer's disease
Rogers, S. L., Farlow, M. R., Doody, R. S., Mohs, R., Friedhoff, L. T., & Donepezil Study Group* (1998) · Neurology · doi:10.1212/wnl.50.1.136 · Cited by 1,618

Show all 105 references

Research works printed but not linked: 12

Cutler, 1990, Psychopharmacol Bull, 26, 231
Schran, 1996, Pharm Res, 13, S
Johansson, 1993, Acta Neurol Scand, 149, 22
Welty, 1993, Pharm Res, 10, S344
Ravic, 2001, Clin Pharmacol Ther, 69, P44
Reyes, 2001, Clin Pharmacol Ther, 69, P44
DeJong, 1989, Clin Ther, 11, 545
Knapp, 1994, JAMA, 271, 985, 10.1001/jama.1994.03510370037029 · DOI
Corey-Bloom, 1999, Int J Geriatr Psychopharmacol, 1, 55
Anand, 2000, Int J Geriatr Psychopharmacol, 2, 68
Farlow, 1992, JAMA, 268, 2523, 10.1001/jama.1992.03490180055026 · DOI
Steele, 1999, J Clin Outcome Management, 6, 52

Sorted by citations

Items 101–200 of 368

Effects of memantine and donepezil on cortical and hippocampal acetylcholine levels and object recognition memory in rats
Ihalainen, J. A., Sarajärvi, T., Rasmusson, D. D., Kemppainen, S., Keski‐Rahkonen, P., Lehtonen, M., Banerjee, P., Semba, K., & Tanila, H. (2011) · Neuropharmacology · doi:10.1016/j.neuropharm.2011.06.008 · Cited by 46
Safety and Tolerability of the Rivastigmine Patch
Grossberg, G. T., Sadowsky, C., Förstl, H., Frölich, L., Nagel, J., Tekin, S., Zechner, S., Ros, J., & Orgogozo, J. (2009) · Alzheimer Disease & Associated Disorders · doi:10.1097/wad.0b013e31818b1c2c · Cited by 44
Pharmacological and Clinical Profile of Newer Antidepressants
Dolder, C. R., Nelson, M., & Stump, A. (2010) · Drugs & Aging · doi:10.2165/11537140-000000000-00000 · Cited by 43
Effect of Cholinesterase Inhibitors on Mortality in Patients With Dementia
Truong, C., Recto, C., Lafont, C., Canouï‐Poitrine, F., Belmin, J., & Lafuente‐Lafuente, C. (2022) · Neurology · doi:10.1212/wnl.0000000000201161 · Cited by 40
Impact of Rivastigmine Use on the Risk of Nursing Home Placement in a US Sample
Beusterien, K. M., Thomas, S. K., Gause, D. O., Kimel, M., Arcona, S., & Mirski, D. F. (2004) · CNS Drugs · doi:10.2165/00023210-200418150-00008 · Cited by 40
Replication Study to Confirm the Role of CYP2D6 Polymorphism rs1080985 on Donepezil Efficacy in Alzheimer's Disease Patients
Albani, D., Boneschi, F. M., Biella, G., Giacalone, G., Lupoli, S., Clerici, F., Benussi, L., Ghidoni, R., Galimberti, D., Squitti, R., et al. (2012) · Journal of Alzheimer s Disease · doi:10.3233/jad-2012-112123 · Cited by 39
Rivastigmine transdermal system for the treatment of mild to moderate Alzheimer’s disease
Grossberg, G. T., Sadowsky, C., & Olin, J. T. (2010) · International Journal of Clinical Practice · doi:10.1111/j.1742-1241.2009.02330.x · Cited by 39
The Effects of Ginkgo biloba Extracts on the Pharmacokinetics and Pharmacodynamics of Donepezil
Yasui‐Furukori, N., Furukori, H., Kaneda, A., Kaneko, S., & Tateishi, T. (2004) · The Journal of Clinical Pharmacology · doi:10.1177/0091270004264161 · Cited by 38
Switching cholinesterase inhibitors in older adults with dementia
Massoud, F., Desmarais, J. E., & Gauthier, S. G. (2010) · International Psychogeriatrics · doi:10.1017/s1041610210001985 · Cited by 38
Pharmacokinetic Changes of Psychotropic Drugs in Patients with Liver Disease
Schlatter, C., Egger, S. S., Tchambaz, L., & Krähenbühl, S. (2009) · Drug Safety · doi:10.2165/00002018-200932070-00003 · Cited by 38
Butyrylcholinesterase: K variant, plasma activity, molecular forms and rivastigmine treatment in Alzheimer's disease in a Southern Brazilian population
Bono, G. F., Simão-Silva, D. P., Batistela, M. S., Josviak, N. D., Dias, P. F. R., do Nascimento, G. A., de Souza, R. L. R., Piovezan, M. R., de Souza, R. K. M., & Alle, L. F. (2015) · Neurochemistry International · doi:10.1016/j.neuint.2014.12.009 · Cited by 37
A threshold model for opposing actions of acetylcholine on reward behavior: Molecular mechanisms and implications for treatment of substance abuse disorders
Grasing, K. (2016) · Behavioural Brain Research · doi:10.1016/j.bbr.2016.06.022 · Cited by 39
Acute cognitive effects of donepezil in young, healthy volunteers
Zaninotto, A. L., Bueno, O. F. A., Pradella‐Hallinan, M., Tufik, S. B., Rusted, J. M., Stough, C. K. K., & Pompéia, S. (2009) · Human Psychopharmacology Clinical and Experimental · doi:10.1002/hup.1044 · Cited by 37
Galantamine blocks delayed rectifier, but not transient outward potassium current in rat dissociated hippocampal pyramidal neurons
Pan, Y., Xu, X.-H., & Wang, X. (2002) · Neuroscience Letters · doi:10.1016/s0304-3940(02)01235-1 · Cited by 37
Predictors of response to acetylcholinesterase inhibitors in dementia: A systematic review
Pozzi, F. E., Conti, E., Appollonio, I., Ferrarese, C., & Tremolizzo, L. (2022) · Frontiers in Neuroscience · doi:10.3389/fnins.2022.998224 · Cited by 36
Identification of human, rat and mouse hydrolyzing enzymes bioconverting amino acid ester prodrug of ketoprofen
Huttunen, K. M. (2018) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2018.09.018 · Cited by 36
Effects of selegiline alone or with donepezil on memory impairment in rats
Takahata, K., Minami, A., Kusumoto, H., Shimazu, S., & Yoneda, F. (2005) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2005.06.024 · Cited by 36
Cholinesterase inhibitors in Alzheimer's disease and Lewy body spectrum disorders: the emerging pharmacogenetic story
Lam, B., Hollingdrake, E., Kennedy, J. L., Black, S. E., & Masellis, M. (2009) · Human Genomics · doi:10.1186/1479-7364-4-2-91 · Cited by 37
Challenges and Approaches of Drugs Such as Memantine, Donepezil, Rivastigmine, and Aducanumab in the Treatment, Control and Management of Alzheimer's Disease
Saeedi, M., & Mehranfar, F. (2022) · Recent Patents on Biotechnology · doi:10.2174/1872208316666220302115901 · Cited by 36
Buccoadhesive films for once-a-day administration of rivastigmine: systematic formulation development and pharmacokinetic evaluation
Kapil, R., Dhawan, S., Beg, S., & Singh, B. (2012) · Drug Development and Industrial Pharmacy · doi:10.3109/03639045.2012.665926 · Cited by 35
Sucrose stearate as a biosurfactant for development of rivastigmine containing nanostructured lipid carriers and assessment of its activity against dementia in C. elegans model
Anand, A., Arya, M., Kaithwas, G., Singh, G., & Saraf, S. A. (2018) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2018.11.021 · Cited by 35
Potential Herb–Drug Interactions in the Management of Age-Related Cognitive Dysfunction
Auxtero, M. D., Chalante, S., Abade, M. R., Jorge, R., & Fernandes, A. I. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13010124 · Cited by 38
Rivastigmine From Capsules to Patch
Sadowsky, C., Micca, J. L., Grossberg, G. T., & Velting, D. M. (2014) · The Primary Care Companion For CNS Disorders · doi:10.4088/pcc.14r01654 · Cited by 34
Pre-clinical pharmacokinetic-pharmacodynamic modelling and biodistribution studies of donepezil hydrochloride by a validated HPLC method
Krishna, K. V., Saha, R. N., Singhvi, G., & Dubey, S. K. (2018) · RSC Advances · doi:10.1039/c8ra03379j · Cited by 34
Genetic Variants and Oxidative Stress in Alzheimer’s Disease
Kowalska, M., Wize, K., Prendecki, M., Lianeri, M., Kozubski, W. P., & Dorszewska, J. (2020) · Current Alzheimer Research · doi:10.2174/1567205017666200224121447 · Cited by 34
Cholinesterase as a Target for Drug Development in Alzheimer’s Disease
Sharma, P. A., Tripathi, M. K., & Shrivastava, S. K. (2019) · Methods in molecular biology · doi:10.1007/978-1-0716-0163-1_18 · Cited by 33
Development of a novel high-concentration galantamine formulation suitable for intranasal delivery
Leonard, A. K., Sileno, A. P., MacEvilly, C., Foerder, C. A., Quay, S. C., & Costantino, H. R. (2005) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.20389 · Cited by 33
A simple and sensitive assay for the quantitative analysis of rivastigmine and its metabolite NAP 226‐90 in human EDTA plasma using coupled liquid chromatography and tandem mass spectrometry
Frankfort, S. V., Ouwehand, M., van Maanen, M. J., Rosing, H., Tulner, L. R., & Beijnen, J. H. (2006) · Rapid Communications in Mass Spectrometry · doi:10.1002/rcm.2737 · Cited by 33
Central Nervous System Medications: Pharmacokinetic and Pharmacodynamic Considerations for Older Adults
Gronich, N. (2024) · Drugs & Aging · doi:10.1007/s40266-024-01117-w · Cited by 41
Opportunities in pharmacogenomics for the treatment of Alzheimer’s disease
Cacabelos, R., Torrellas, C., & Carrera, I. (2015) · Future Neurology · doi:10.2217/fnl.15.12 · Cited by 32
Donepezil plasma concentrations, CYP2D6 and CYP3A4 phenotypes, and cognitive outcome in Alzheimer’s disease
Coin, A., Pamio, M. V., Alexopoulos, C., Granziera, S., Groppa, F., de Rosa, G., Girardi, A., Sergi, G., Manzato, E., & Padrini, R. (2016) · European Journal of Clinical Pharmacology · doi:10.1007/s00228-016-2033-1 · Cited by 32
Transdermal Delivery of Treatment for Alzheimer’s Disease
Chan, A. L. F., Chien, Y. W., & Lin, S. J. (2008) · Drugs & Aging · doi:10.2165/00002512-200825090-00003 · Cited by 32
Modification of motor cortical excitability by an acetylcholinesterase inhibitor
Korchounov, A., Ilic, T. V., Schwinge, T., & Ziemann, U. (2005) · Experimental Brain Research · doi:10.1007/s00221-005-2326-6 · Cited by 32
Distinguishing Lewy body dementias from Alzheimer’s disease
Tarawneh, R. M., & Galvin, J. E. (2007) · Expert Review of Neurotherapeutics · doi:10.1586/14737175.7.11.1499 · Cited by 32
SATURABLE DISTRIBUTION OF TACRINE INTO THE STRIATAL EXTRACELLULAR FLUID OF THE RAT: EVIDENCE OF INVOLVEMENT OF MULTIPLE ORGANIC CATION TRANSPORTERS IN THE TRANSPORT
Sung, J.-H., Yu, K., Park, J., Tsuruo, T., Kim, D., Shim, C., & Chung, S. (2004) · Drug Metabolism and Disposition · doi:10.1124/dmd.104.002220 · Cited by 32
Pharmacologic treatment of adolescent and child schizophrenia
Young, C., & Findling, R. L. (2004) · Expert Review of Neurotherapeutics · doi:10.1586/14737175.4.1.53 · Cited by 31
Drug-induced changes in P450 enzyme expression at the gene expression level: A new dimension to the analysis of drug–drug interactions
Lee, M. D., Ayanoĝlu, E., & Gong, L. (2006) · Xenobiotica · doi:10.1080/00498250600861785 · Cited by 31
Cholinergic modulation of auditory processing, sensory gating and novelty detection in human participants
Klinkenberg, I., Blokland, A., Riedel, W. J., & Sambeth, A. (2012) · Psychopharmacology · doi:10.1007/s00213-012-2872-0 · Cited by 31
Acetylcholinesterase and its Inhibitors
English, B. A., & Webster, A. A. (2011) · Elsevier eBooks · doi:10.1016/b978-0-12-386525-0.00132-3 · Cited by 31
Rivastigmine blocks voltage‐activated K+ currents in dissociated rat hippocampal neurons
Pan, Y., Xu, X., & Wang, X. (2003) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0705503 · Cited by 31
Severe worsening of parkinsonism in Lewy body dementia due to donepezil
Rozzini, L., Ghianda, D., Trabucchi, M., & Padovani, A. (2004) · Neurology · doi:10.1212/wnl.63.8.1543-a · Cited by 31
Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors
Pejchal, V., Štěpánková, Š., Pejchalová, M., Královec, K., Havelek, R., Růžičková, Z., Ajani, H., Lo, R., & Lepšı́k, M. (2016) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2016.02.033 · Cited by 34
Effect of genetic polymorphisms on Alzheimer’s disease treatment outcomes: an update
Sumirtanurdin, R., Thalib, A. Y., Cantona, K., & Abdulah, R. (2019) · Clinical Interventions in Aging · doi:10.2147/cia.s200109 · Cited by 30
Quantitation of donepezil and its active metabolite 6-O-desmethyl donepezil in human plasma by a selective and sensitive liquid chromatography–tandem mass spectrometric method
Patel, B. N., Sharma, N., Sanyal, M., & Shrivastav, P. S. (2008) · Analytica Chimica Acta · doi:10.1016/j.aca.2008.09.048 · Cited by 30
Pharmacogenomics, Nutrigenomics and Therapeutic Optimization in Alzheimer’s Disease
Cacabelos, R. (2005) · Aging Health · doi:10.2217/1745509x.1.2.303 · Cited by 30
Donepezil
Goldsmith, D. R., & Scott, L. J. (2003) · Drugs & Aging · doi:10.2165/00002512-200320150-00005 · Cited by 29
Rosmarinic acid protects against chronic ethanol-induced learning and memory deficits in rats
Hasanein, P., Seifi, R., Hajinezhad, M. R., & Emamjomeh, A. (2016) · Nutritional Neuroscience · doi:10.1080/1028415x.2016.1203125 · Cited by 29
Dihydropyrimidinone-derived selenoesters efficacy and safety in an in vivo model of Aβ aggregation
Pereira, F. S. D. O., Barbosa, F. A. R., Canto, R. F. S., Luchese, C., Pinton, S., Braga, A. L., de Azeredo, J. B., Quines, C. B., & Ávila, D. S. (2021) · NeuroToxicology · doi:10.1016/j.neuro.2021.10.012 · Cited by 29
Follow-on drugs: How far should chemists look?
Giordanetto, F., Boström, J., & Tyrchan, C. (2011) · Drug Discovery Today · doi:10.1016/j.drudis.2011.05.011 · Cited by 30
Association of the Choline Acetyltransferase Gene with Responsiveness to Acetylcholinesterase Inhibitors in Alzheimer’s Disease
Yoon, H. G., Myung, W., Lim, S. W., Kang, H., Kim, S., Won, H., Carroll, B. J., & Kim, D. (2015) · Pharmacopsychiatry · doi:10.1055/s-0035-1545300 · Cited by 29
Improved l-Type amino acid transporter 1 (LAT1)-mediated delivery of anti-inflammatory drugs into astrocytes and microglia with reduced prostaglandin production
Tampio, J., Löffler, S., Guillon, M., Hugele, A., Huttunen, J., & Huttunen, K. M. (2021) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2021.120565 · Cited by 29
Steady-State Pharmacokinetics of Rivastigmine in Patients with Mild to Moderate Alzheimer’s Disease Not Affected by Co-Administration of Memantine
Shua‐Haim, J. R., Smith, J. M., Picard, F., Sedek, G., Athalye, S. N., Pommier, F., & Lefèvre, G. Y. (2008) · Clinical Drug Investigation · doi:10.2165/00044011-200828060-00004 · Cited by 28
Progress in Clinical Neurosciences: Parkinson's Disease with Dementia and Dementia with Lewy Bodies
Camicioli, R. M., & Fisher, N. (2004) · Canadian Journal of Neurological Sciences / Journal Canadien des Sciences Neurologiques · doi:10.1017/s0317167100002791 · Cited by 28
Donepezil, an acetylcholinesterase inhibitor, attenuates nicotine self‐administration and reinstatement of nicotine seeking in rats
Kimmey, B. A., Rupprecht, L. E., Hayes, M. R., & Schmidt, H. D. (2012) · Addiction Biology · doi:10.1111/adb.12014 · Cited by 29
Stereoselective metabolism of donepezil and steady-state plasma concentrations of S-donepezil based on CYP2D6 polymorphisms in the therapeutic responses of Han Chinese patients with Alzheimer's disease
Lu, J., Wan, L., Zhong, Y., Yu, Q., Han, Y., Chen, P., Wang, B., Li, W., Miao, Y., & Guo, C. (2015) · Journal of Pharmacological Sciences · doi:10.1016/j.jphs.2015.10.010 · Cited by 27
Cholinesterase Inhibitors: Cardioprotection in Alzheimer's Disease
Monacelli, F., & Rosa, G. (2014) · Journal of Alzheimer s Disease · doi:10.3233/jad-141089 · Cited by 26
Patients with Alzheimer’s Disease May Be Particularly Susceptible to Adverse Effects of Statins
Algotsson, A., & Winblad, B. G. (2004) · Dementia and Geriatric Cognitive Disorders · doi:10.1159/000076342 · Cited by 25
Low dose of donepezil improves gabapentin analgesia in the rat spared nerve injury model of neuropathic pain: single and multiple dosing studies
Folkesson, A., Honoré, P. H., Andersen, L. M., Kristensen, P., & Bjerrum, O. J. (2010) · Journal of Neural Transmission · doi:10.1007/s00702-010-0494-4 · Cited by 25
The Inhibitory Effect of Rivastigmine and Galantamine on Choline Transport in Brain Capillary Endothelial Cells
Lee, N.-Y., & Kang, Y. (2010) · Biomolecules & Therapeutics · doi:10.4062/biomolther.2010.18.1.065 · Cited by 25
Once-daily transdermal rivastigmine in the treatment of Alzheimer’s disease
Dodel, R. C. (2008) · Drug Design Development and Therapy · doi:10.2147/dddt.s3102 · Cited by 25
Brain Drug Delivery Systems for Neurodegenerative Disorders
Garbayo, E., Ansorena, E., & Blanco‐Prieto, M. J. (2012) · Current Pharmaceutical Biotechnology · doi:10.2174/138920112803341761 · Cited by 25
Similar Rivastigmine Pharmacokinetics and Pharmacodynamics in Japanese and White Healthy Participants Following the Application of Novel Rivastigmine Patch
Lefèvre, G. Y., Büche, M., Sedek, G., Maton, S., Enz, A., Lorch, U., Sagan, C., & Appel‐Dingemanse, S. (2009) · The Journal of Clinical Pharmacology · doi:10.1177/0091270008330161 · Cited by 25
Treatment of behavioural symptoms and dementia in Parkinson's disease
Hanagasi, H. A., & Emre, M. (2005) · Fundamental & Clinical Pharmacology · doi:10.1111/j.1472-8206.2005.00317.x · Cited by 24
Acute effects of donepezil in healthy young adults underline the fractionation of executive functioning
Ginani, G. E., Tufik, S. B., Bueno, O., Pradella-Hallinan, M. L. D. C., Rusted, J. M., & Pompéia, S. (2011) · Journal of Psychopharmacology · doi:10.1177/0269881110391832 · Cited by 26
The Acetylcholinesterase Inhibitors Competitively Inhibited an Acetyl l-Carnitine Transport Through the Blood–Brain Barrier
Lee, N.-Y., Choi, H.-O., & Kang, Y. (2012) · Neurochemical Research · doi:10.1007/s11064-012-0723-3 · Cited by 24
Pharmacogenomics of drugs used to treat brain disorders
Cacabelos, R. (2020) · Expert Review of Precision Medicine and Drug Development · doi:10.1080/23808993.2020.1738217 · Cited by 24
An In Vitro and In Vivo Cholinesterase Inhibitory Activity of Pistacia khinjuk and Allium sativum Essential Oils
Ghajarbeygi, P., Hajhoseini, A., Hosseini, M.-S., & Sharifan, A. (2019) · Journal of pharmacopuncture · doi:10.3831/kpi.2019.22.031 · Cited by 23
Reduction and Scavenging of Chemically Reactive Drug Metabolites by NAD(P)H:Quinone Oxidoreductase 1 and NRH:Quinone Oxidoreductase 2 and Variability in Hepatic Concentrations
den Braver-Sewradj, S. P., den Braver, M. W., Toorneman, R. M., van Leeuwen, S. J. M., Zhang, Y., Dekker, S. J., Vermeulen, N. P. E., Commandeur, J. N. M., & Vos, J. C. (2017) · Chemical Research in Toxicology · doi:10.1021/acs.chemrestox.7b00289 · Cited by 23
Galantamine Extended Release
Robinson, D. M., & Plosker, G. L. (2006) · CNS Drugs · doi:10.2165/00023210-200620080-00006 · Cited by 23
Romidepsin and metformin nanomaterials delivery on streptozocin for the treatment of Alzheimer's disease in animal model
Zeng, H., Xu, L., Zou, Y., & Wang, S. (2021) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2021.111864 · Cited by 22
Determination of therapeutics with growth‐hormone secretagogue activity in human urine for doping control purposes
Thevis, M., Wilkens, F., Geyer, H., & Schänzer, W. (2006) · Rapid Communications in Mass Spectrometry · doi:10.1002/rcm.2758 · Cited by 22
Effects of Cholinesterase Inhibitors on Postoperative Outcomes of Older Adults With Dementia Undergoing Hip Fracture Surgery
Seitz, D. P., Gill, S. S., Gruneir, A., Austin, P. C., Anderson, G., Reimer, C. L., & Rochon, P. A. (2010) · American Journal of Geriatric Psychiatry · doi:10.1097/jgp.0b013e3181ff67a1 · Cited by 22
Salicylanilide diethyl phosphates as cholinesterases inhibitors
Krátký, M., Štěpánková, Š., Vorčáková, K., & Vinšová, J. (2014) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2014.11.005 · Cited by 21
Switching from Oral Cholinesterase Inhibitors to the Rivastigmine Transdermal Patch
Sadowsky, C., Perez, J. A. D., Bouchard, R. W., Goodman, I. J., & Tekin, S. (2010) · CNS Neuroscience & Therapeutics · doi:10.1111/j.1755-5949.2009.00119.x · Cited by 21
Combining CDP-choline and galantamine, an optimized α7 nicotinic strategy, to ameliorate sensory gating to speech stimuli in schizophrenia
Choueiry, J., Blais, C. M., Shah, D. K., Smith, D., Fisher, D. J., Labelle, A., & Knott, V. (2019) · International Journal of Psychophysiology · doi:10.1016/j.ijpsycho.2019.02.005 · Cited by 20
Novel Sulfonamide-Based Carbamates as Selective Inhibitors of BChE
Magar, P., Parravicini, O., Štěpánková, Š., Svrčková, K., Garro, A., Jendrzejewska, I., Pauk, K., Hošek, J., Jampílek, J., Enriz, R. D., et al. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22179447 · Cited by 21
Postulating the possible cellular signalling mechanisms of antibody drug conjugates in Alzheimer's disease
Punyakoti, P., Behl, T., Sehgal, A., Yadav, S., Sachdeva, M., Anwer, M. K., Vargas-De-La-Cruz, C. B., Venkatachalam, T., Naqvi, M., Verma, R., et al. (2022) · Cellular Signalling · doi:10.1016/j.cellsig.2022.110539 · Cited by 20
2-Hydroxy-N-phenylbenzamides and Their Esters Inhibit Acetylcholinesterase and Butyrylcholinesterase
Krátký, M., Štěpánková, Š., Houngbedji, N.-H., Vosátka, R., Vorčáková, K., & Vinšová, J. (2019) · Biomolecules · doi:10.3390/biom9110698 · Cited by 21
Kinetics of acetylcholinesterase inhibition by an aqueous extract of Withania somnifera roots
Kumar, S., Seal, C., & Okello, E. J. (2011) · Newcastle University ePrints (Newcastle Univesity) · doi:10.25405/ncl.34162032 · Cited by 20
Discontinuation of rivastigmine in routine clinical practice
Frankfort, S. V., Appels, B. A., de Boer, A., Tulner, L. R., van Campen, J. P. C. M., Koks, C. H. W., & Beijnen, J. H. (2005) · International Journal of Geriatric Psychiatry · doi:10.1002/gps.1411 · Cited by 20
Consensus Guidelines for Therapeutic Drug Monitoring in Neuropsychopharmacology: Update 2026 – Pharmacokinetic, pharmacogenetic and clinical aspects
Hart, X. M., Gründer, G., Unterecker, S., Schoretsanitis, G., Hiemke, C., Adamovic, I., Amann, F., Baumann, P., Bergemann, N., Brandt, C., et al. (2026) · Pharmacopsychiatry · doi:10.1055/a-2860-7861 · Cited by 20
Schiff Base Derivatives Based on Ampyrone as Promising Acetylcholinesterase Inhibitors: Synthesis, Spectral Characterization, Biological Activity, and SwissADME Predictions
Başaran, E. (2022) · Russian Journal of Bioorganic Chemistry · doi:10.1134/s1068162023010065 · Cited by 19
Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers
Kim, Y. H., Choi, H. Y., Lim, H., Lee, S. H., Jeon, H. S., Hong, D., Kim, S. S., Choi, Y. K., & Bae, K. (2015) · Drug Design Development and Therapy · doi:10.2147/dddt.s78555 · Cited by 19
Rivastigmine Patch in Chinese Patients with Probable Alzheimer's disease: A 24‐week, Randomized, Double‐Blind Parallel‐Group Study Comparing Rivastigmine Patch (9.5 mg/24 h) with Capsule (6 mg Twice Daily)
Zhang, Z., Hong, Z., Wang, Y., He, L., Wang, N., Zhao, Z., Zhao, G., Shang, L., Weisskopf, M., Callegari, F., et al. (2016) · CNS Neuroscience & Therapeutics · doi:10.1111/cns.12521 · Cited by 19
In silico identification of the potential molecular mechanisms involved in protective effects of prolactin on motor and memory deficits induced by 1,2-Diacetylbenzene in young and old rats
Nguyen, H. D., Jo, W. H., Hoang, N. H. M., & Kim, M. (2022) · NeuroToxicology · doi:10.1016/j.neuro.2022.09.002 · Cited by 20
What Is the Rationale for New Treatment Strategies in Alzheimer's Disease?
Rogawski, M. A. (2004) · CNS Spectrums · doi:10.1017/s1092852900024743 · Cited by 19
No association between CYP2D6 polymorphism and Alzheimer's disease in an Italian population
Scordo, M. G., DAHL, M., Spina, E., Cordici, F., & Arena, M. G. (2005) · Pharmacological Research · doi:10.1016/j.phrs.2005.10.005 · Cited by 19
Compliance assessment of ambulatory Alzheimer patients to aid therapeutic decisions by healthcare professionals
Schwalbe, O., Scheerans, C., Freiberg, I., Schmidt‐Pokrzywniak, A., Stang, A., & Kloft, C. (2010) · BMC Health Services Research · doi:10.1186/1472-6963-10-232 · Cited by 18
Epigenetics and Pharmacoepigenetics of Age-Related Neurodegenerative Disorders
Cacabelos, R., Cacabelos, P., & Carril, J. C. (2019) · Elsevier eBooks · doi:10.1016/b978-0-12-813939-4.00038-3 · Cited by 18
Human serum albumin reduces the potency of acetylcholinesterase inhibitor based drugs for Alzheimer's disease
Islam, M. M., Gurung, A. B., Bhattacharjee, A., Aguan, K., & Mitra, S. (2016) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2016.02.012 · Cited by 18
Pleiotropy and Promiscuity in Pharmacogenomics for the Treatment of Alzheimer's Disease and Related risk factors
Cacabelos, R. (2018) · Future Neurology · doi:10.2217/fnl-2017-0038 · Cited by 18
Severe worsening of parkinsonism in Lewy body dementia due to donepezil
ONOFRJ, M. C., & Thomas, A. (2003) · Neurology · doi:10.1212/01.wnl.0000094201.80888.da · Cited by 18
Acetylcholinesterase inhibitors for autistic spectrum disorders
Ure, A. M., Cox, G., Haslam, R., & Williams, K. J. (2023) · Cochrane Database of Systematic Reviews · doi:10.1002/14651858.cd013851.pub2 · Cited by 18
A fluorescent biosensor based on acetylcholinesterase and 5-oxazolone derivative immobilized in polyvinylchloride (PVC) matrix
Öztürk, G., Alp, S., & Tımur, S. (2007) · Journal of Molecular Catalysis B Enzymatic · doi:10.1016/j.molcatb.2007.03.009 · Cited by 17
Cholinergic modulation of auditory steady-state response in the auditory cortex of the freely moving rat
Zhang, J., Ma, L., Li, W., Yang, P., & Qin, L. (2016) · Neuroscience · doi:10.1016/j.neuroscience.2016.03.006 · Cited by 17
The Effect of Choline Acetyltransferase Genotype on Donepezil Treatment Response in Patients with Alzheimer’s Disease
Lee, K. U., Lee, J. H., Lee, D. Y., Youn, J. C., Kim, J. L., Moon, S. W., Kim, B., Ryu, S., Kim, M.-D., Lee, C. U., et al. (2015) · Clinical Psychopharmacology and Neuroscience · doi:10.9758/cpn.2015.13.2.168 · Cited by 17
First‐in‐man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M1‐receptor partial agonist for the treatment of dementias
Bakker, C., Tasker, T. C. G., Liptrot, J., Hart, E. P., Klaassen, E. S., Prins, S., van der Doef, T. F., Brown, G. A., Brown, A., Congreve, M., et al. (2020) · British Journal of Clinical Pharmacology · doi:10.1111/bcp.14710 · Cited by 16
[18F]DPA-714: Effect of co-medications, age, sex, BMI and TSPO polymorphism on the human plasma input function
Peyronneau, M., Kühnast, B., Nguyen, D.-L., Jégo, B., Sayet, G., Caillé, F., Lavisse, S., Gervais, P., Stankoff, B., Sarazin, M., et al. (2023) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-023-06286-1 · Cited by 16
Cholinesterase inhibitors and memantine are associated with a reduced mortality in nursing home residents with dementia: a longitudinal observational study
Havreng‐Théry, C., Oquendo, B., Zolnowski‐Kolp, V., Krolak‐Salmon, P., Bertin‐Hugault, F., Lafuente‐Lafuente, C., & Belmin, J. (2024) · Alzheimer s Research & Therapy · doi:10.1186/s13195-024-01481-0 · Cited by 16
Alzheimer's Disease: Characterization, Evolution and Implications of the Neuroinflammatory Process
Viegas, F. P. D., Simões, M. C. R., da Rocha, M. D., Castelli, M. R., Moreira, M. S., & Junior, C. V. (2011) · Revista Virtual de Química · doi:10.5935/1984-6835.20110034 · Cited by 19

Authors: Jann, M. W., Shirley, K. L., & Small, G. W.
Affiliations: Mercer University (US)
University of California, Los Angeles (US)
Corresponding author: Jann, Michael W.
ORCID: Jann, Michael W.
Small, Gary W.
Venue: Clinical Pharmacokinetics
Publisher: Springer Science and Business Media LLC
Published: 2002
Volume: 41
Issue: 10
Pages: 719-739
ISSN: 0312-5963 (ISSN-L)
DOI: 10.2165/00003088-200241100-00003
OpenAlex: W2016149437
Cited by: 365
References: 105
Citations by year: 2026: 9 · 2025: 10 · 2024: 13 · 2023: 11 · 2022: 10 · 2021: 12 · 2020: 19 · 2019: 23 · 2018: 11 · 2017: 7 · 2016: 17 · 2015: 17 · 2014: 23 · 2013: 11 · 2012: 16
FWCI: 2.09
Type: journal article
Language: en
Open access: closed
Locations: Clinical Pharmacokinetics (publishedVersion)
PubMed (publishedVersion)
Funders: Eli Lilly and Company
Pfizer Pharmaceuticals
Topics: Health Sciences › Medicine › Pharmacology (medical) › Cholinesterase and Neurodegenerative Diseases
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
Keywords: cholinesterase inhibitors, Alzheimer's disease, pharmacokinetics, pharmacodynamics, tacrine, donepezil, rivastigmine, galantamine, acetylcholinesterase inhibition, butyrylcholinesterase, dose-response relationship, plateau effect, drug metabolism, cytochrome P450, protein binding, nicotinic acetylcholine receptors, biomarkers, neuroimaging
MeSH terms: Rivastigmine, Donepezil, Aging, Alzheimer Disease, Biological Availability, Carbamates, Cholinesterase Inhibitors, Drug Interactions, Half-Life, Humans, Indans, Intestinal Absorption, Liver, Piperidines, Protein Binding, Tacrine, Tissue Distribution, Phenylcarbamates

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Clinical Pharmacokinetics and Pharmacodynamics of Cholinesterase Inhibitors

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Citations

Cites

Cited by

Related

Metadata

Record

About these checks