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

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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

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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.

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“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

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Lefèvre, G. Y., Sedek, G., Huang, H. A., Saltzman, M. A., Rosenberg, M. A., Kiese, B., & Fordham, P. (2007) · The Journal of Clinical Pharmacology · doi:10.1177/0091270006297748 · Cited by 62
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Sabbagh, M. N., & Cummings, J. L. (2011) · BMC Neurology · doi:10.1186/1471-2377-11-21 · Cited by 61
Oral administration of pyridostigmine bromide and huperzine A protects human whole blood cholinesterases from ex vivo exposure to soman
Gordon, R. K., Haigh, J. R., Garcia, G. E., Feaster, S. R., Riel, M. A., Lenz, D. E., Aisen, P. S. S., & Doctor, B. P. (2005) · Chemico-Biological Interactions · doi:10.1016/j.cbi.2005.10.031 · Cited by 61
Pharmacogenomics of Cognitive Dysfunction and Neuropsychiatric Disorders in Dementia
Cacabelos, R. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21093059 · Cited by 61
Determination of donepezil hydrochloride in human and rat plasma, blood and brain microdialysates by HPLC with a short C30 column
Nakashima, K., Itoh, K., Kono, M., Nakashima, M. N., & Wada, M. (2005) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2005.10.017 · Cited by 60
Pharmacogenetics of cytochrome P450 (CYP) in the elderly
Seripa, D., Pilotto, A., Panza, F., Matera, M. G., & Pilotto, A. (2010) · Ageing Research Reviews · doi:10.1016/j.arr.2010.06.001 · Cited by 59
In vitro formulation optimization of intranasal galantamine leading to enhanced bioavailability and reduced emetic response in vivo
Leonard, A. K., Sileno, A. P., Brandt, G., Foerder, C. A., Quay, S. C., & Costantino, H. R. (2006) · International Journal of Pharmaceutics · doi:10.1016/j.ijpharm.2006.11.013 · Cited by 59
Alzheimer Disease and Its Management
Samanta, M. K., Wilson, B., Santhi, K., Kumar, K. P. S., & Suresh, B. (2006) · American Journal of Therapeutics · doi:10.1097/01.mjt.0000208274.80496.f1 · Cited by 54
Evidence of carrier‐mediated transport in the penetration of donepezil into the rat brain
Kim, M., Maeng, H., Yu, K., Lee, K., Tsuruo, T., Kim, D., Shim, C., & Chung, S. (2009) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.21895 · Cited by 55
Donepezil: a clinical review of current and emerging indications
Román, G. C., & Rogers, S. (2004) · Expert Opinion on Pharmacotherapy · doi:10.1517/14656566.5.1.161 · Cited by 56
Pharmacokinetic and Pharmacodynamic Properties of Cholinesterase Inhibitors Donepezil, Tacrine, and Galantamine in Aged and Young Lister Hooded Rats
Goh, C. W., Aw, C. C., Lee, J. H., Chen, C., & Browne, E. R. (2010) · Drug Metabolism and Disposition · doi:10.1124/dmd.110.035964 · Cited by 53
2-Phenylbenzofuran derivatives as butyrylcholinesterase inhibitors: Synthesis, biological activity and molecular modeling
Delogu, G., Matos, M. J., Fanti, M., Era, B., Medda, R., Pieroni, E., Fais, A., Kumar, A., & Pintus, F. (2016) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2016.03.039 · Cited by 52
Pharmacologists and Alzheimer disease therapy: to boldly go where no scientist has gone before
Mancuso, C., Siciliano, R., Barone, E., Butterfield, D. A., & Preziosi, P. (2011) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.2011.601740 · Cited by 53
Ameliorative effect of rosmarinic acid on scopolamine-induced memory impairment in rats
Hasanein, P., & Kazemian-Mahtaj, A. (2014) · Neuroscience Letters · doi:10.1016/j.neulet.2014.11.027 · Cited by 51
Donepezil Plus Solifenacin (CPC-201) Treatment for Alzheimer's Disease
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Safety and tolerability of transdermal and oral rivastigmine in Alzheimer’s disease and Parkinson’s disease dementia
Darreh-Shori, T., & Jelic, V. (2010) · Expert Opinion on Drug Safety · doi:10.1517/14740330903439717 · Cited by 51
Pharmacological Characterization of RS-1259, an Orally Active Dual Inhibitor of Acetylcholinesterase and Serotonin Transporter, in Rodents: Possible Treatment of Alzheimer’s Disease
Abe, Y., Aoyagi, A., Hara, T., Abe, K., Yamazaki, R., Kumagae, Y., Naruto, S., Koyama, K., Marumoto, S., Tago, K., et al. (2003) · Journal of Pharmacological Sciences · doi:10.1254/jphs.93.95 · Cited by 51
BCHE and CYP2D6 genetic variation in Alzheimer’s disease patients treated with cholinesterase inhibitors
Chianella, C., Gragnaniello, D., Delser, P. M., Visentini, M. F., Sette, E., Tola, M. R., Barbujani, G., & Fuselli, S. (2011) · European Journal of Clinical Pharmacology · doi:10.1007/s00228-011-1064-x · Cited by 50
Pharmacogenetic Considerations in the Treatment of Alzheimer’s Disease
Cacabelos, R., Torrellas, C., Teijido, Ó., & Carril, J. C. (2016) · Pharmacogenomics · doi:10.2217/pgs-2016-0031 · Cited by 50
Current advances in transdermal delivery of drugs for Alzheimer's disease
Nguyen, T. T., Giau, V. V., & Vo, T. K. (2017) · Indian Journal of Pharmacology · doi:10.4103/0253-7613.208143 · Cited by 49
Pharmacogenetic considerations when prescribing cholinesterase inhibitors for the treatment of Alzheimer’s disease
Cacabelos, R. (2020) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1080/17425255.2020.1779700 · Cited by 51
Efficacy and Tolerability of Low-Dose Donepezil in Schizophrenia
Erickson, S. K., Schwarzkopf, S. B., Palumbo, D. R., Badgley-Fleeman, J., Smirnow, A. M., & Light, G. A. (2005) · Clinical Neuropharmacology · doi:10.1097/01.wnf.0000173714.61744.e6 · Cited by 50
Sex influences on cholinesterase inhibitor treatment in elderly individuals with Alzheimer's disease.
Haywood, W. M., & Mukaetova-Ladinska, E. (2006) · The American Journal of Geriatric Pharmacotherapy · doi:10.1016/j.amjopharm.2006.09.009 · Cited by 45
Donepezil—an updated review of challenges in dosage form design
Sutthapitaksakul, L., Dass, C. R., & Sriamornsak, P. (2021) · Journal of Drug Delivery Science and Technology · doi:10.1016/j.jddst.2021.102549 · Cited by 46
Anti-Neurodegenerative Benefits of Acetylcholinesterase Inhibitors in Alzheimer’s Disease: Nexus of Cholinergic and Nerve Growth Factor Dysfunction
Moss, D. E., & Perez, R. G. (2021) · Current Alzheimer Research · doi:10.2174/1567205018666211215150547 · Cited by 48
Pharmacokinetics and Bioavailability of the Novel Rivastigmine Transdermal Patch Versus Rivastigmine Oral Solution in Healthy Elderly Subjects
Lefèvre, G. Y., Pommier, F., Sedek, G., Allison, M. J., Huang, H. A., Kiese, B., Ho, Y., & Appel‐Dingemanse, S. (2008) · The Journal of Clinical Pharmacology · doi:10.1177/0091270007312154 · Cited by 46
Donepezil (Aricept®) for treatment of Alzheimer´s disease and other dementing conditions
Geldmacher, D. (2004) · Expert Review of Neurotherapeutics · doi:10.1586/14737175.4.1.5 · Cited by 45
Use of Cholinesterase Inhibitors in Non-Alzheimer’s Dementias
Noufi, P., Khoury, R., Jeyakumar, S., & Grossberg, G. (2019) · Drugs & Aging · doi:10.1007/s40266-019-00685-6 · Cited by 37

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

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Clinical Pharmacokinetics and Pharmacodynamics of Cholinesterase Inhibitors

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