Cholinesterase inhibitors for the treatment of Alzheimer's disease: Getting on and staying on

Current Therapeutic Research - Clinical and Experimental

Volumn 64, Issue 4, 2003, Pages 216-235

  Grossberg, George T ^a  

^a SAINT LOUIS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Acetylcholinesterase; Alzheimer's disease; Butyrylcholinesterase; Cholinesterase inhibitors; Safety and tolerability

Indexed keywords

ANTIDIABETIC AGENT; ANTIEMETIC AGENT; ANTIINFLAMMATORY AGENT; CARDIOVASCULAR AGENT; CHOLINESTERASE; CHOLINESTERASE INHIBITOR; DONEPEZIL; GALANTAMINE; PAROXETINE; PLACEBO; RIVASTIGMINE;

ALZHEIMER DISEASE; BEHAVIOR; BRAIN REGION; CLINICAL FEATURE; CLINICAL PRACTICE; CLINICAL TRIAL; COGNITION; CONTROLLED CLINICAL TRIAL; DAILY LIFE ACTIVITY; DISEASE COURSE; DISEASE EXACERBATION; DOSE CALCULATION; DOSE RESPONSE; DOSE TIME EFFECT RELATION; DRUG ABSORPTION; DRUG BINDING SITE; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG EFFICACY; DRUG HALF LIFE; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; ENZYME INHIBITION; EXTRAPYRAMIDAL SYMPTOM; FOOD DRUG INTERACTION; HUMAN; INHIBITION KINETICS; LONG TERM CARE; META ANALYSIS; MUSCLE CRAMP; MUSCLE WEAKNESS; NAUSEA; PLASMA PROTEIN BINDING; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; REVIEW; SLEEP DISORDER; SLEEP WAKING CYCLE; VOMITING;

EID: 0037532679     PISSN: 0011393X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0011-393X(03)00059-6     Document Type: Review

References (102)

1. Bartus RT, Dean RL III, Beer B, Lippa AS. The cholinergic hypothesis of geriatric memory dysfunction. Science. 1982;217:408-414.
2. Foster RH, Plosker GL. Donepezil. Pharmacoeconomic implications of therapy. Pharmacoeconomics. 1999;16:99-114.
3. Lamb HM, Goa KL. Rivastigmine: A pharmacoeconomic review of its use in Alzheimer's disease. Pharmacoeconomics. 2001;19:303-318.
4. Rösler M, Anand R, Cicin-Sain A, et al. Efficacy and safety of rivastigmine in patients with Alzheimer's disease: International randomised controlled trial. BMJ. 1999;318:633-638.
5. Corey-Bloom J, Anand R, Veach J. A randomized trial evaluating the efficacy and safety of ENA 713 (rivastigmine tartrate), a new acetylcholinesterase inhibitor, in patients with mild to moderately severe Alzheimer's disease. Int J Geriatr Psychopharmacol. 1998;1:55-65.
6. Rogers SL, Farlow MR, Doody RS, et al, for the Donepezil Study Group. A 24-week, double-blind, placebo-controlled trial of donepezil in patients with Alzheimer's disease. Neurology. 1998;50:136-145.
7. Tariot PN, Solomon PR, Morris JC, et al, for the Galantamine USA-10 Study Group. A 5-month, randomized, placebo-controlled trial of galantamine in AD. Neurology. 2000;54:2269-2276.
8. Wilcock GK, Lilienfeld S, Gaens E, et al, for the Galantamine International-1 Study Group. Efficacy and safety of galantamine in patients with mild to moderate Alzheimer's disease: Multicentre randomised controlled trial. BMJ. 2000;321:1445-1449.
9. Farlow M, Anand R, Messina J Jr, et al. A 52-week study of the efficacy of rivastigmine in patients with mild to moderately severe Alzheimer's disease. Eur Neurol. 2000;44:236-241.
10. Nordberg A, Svensson AL. Cholinesterase inhibitors in the treatment of Alzheimer's disease: A comparison of tolerability and pharmacology. Drug Saf. 1998;19:465-480.
11. Blackard WG Jr, Sood GK, Crowe DR, Fallon MB. Tacrine. A cause of fatal hepatotoxicity? J Clin Gastroenterol. 1998;26:57-59.
12. Sifton DW, ed. Physicians' Desk Reference®. Montvale, NJ: Medical Economics; 2002:1792, 2342, 2665.
13. Svensson AL. Cholinesterase inhibitors in Alzheimer's disease: An experimental study on mechanisms for interaction with muscarinic and nicotinic receptors and neuroprotection [published doctoral dissertation]. Huddinge, Sweden: Division of Nicotine Research, Department of Clinical Neuroscience and Family Medicine, Karolinska Institute, Huddinge University Hospital; 1997: Publication no. B84, S-141 86.
14. Barnes CA, Meltzer J, Houston F, et al. Chronic treatment of old rats with donepezil or galantamine: Effects on memory, hippocampal plasticity and nicotinic receptors. Neuroscience. 2000;99:17-23.
15. Svensson A, Nordberg A. Interaction of tacrine, galantamine, NXX-066 and E2020 with neuronal alpha4beta2 nicotinic receptors expressed in fibroblast cells. In: Iqbal K, Winblad B, Nishimura T, et al, eds. Alzheimer's Disease: Biology, Diagnosis, and Therapeutics. New York: Wiley; 1997:751-756.
16. Bryson HM, Benfield P. Donepezil. Drugs Aging. 1997;10:234-239; discussion 240-241.
17. Kasa P, Papp H, Kasa P Jr, Torok I. Donepezil dose-dependently inhibits acetylcholinesterase activity in various areas and in the presynaptic cholinergic and the postsynaptic cholinoceptive enzyme-positive structures in the human and rat brain. Neuroscience. 2000;101:89-100.
18. Amici S, Lanari A, Romani R, et al. Cerebrospinal fluid acetylcholinesterase activity after long-term treatment with donepezil and rivastigmina. Mech Ageing Dev. 2001;122:2057-2062.
19. Davidsson P, Blennow K, Andreasen N, et al. Differential increase in cerebrospinal fluid-acetylcholinesterase after treatment with acetylcholinesterase inhibitors in patients with Alzheimer's disease. Neurosci Lett. 2001;300:157-160.
20. Parnetti L, Amici S, Lanari A, et al. Cerebrospinal fluid levels of biomarkers and activity of acetylcholinesterase (AChE) and butyrylcholinesterase in AD patients before and after treatment with different AChE inhibitors. Neurol Sci. 2002;23 (Suppl 2):S95-S96.
21. Darreh-Shori T, Almkvist O, Guan ZZ, et al. Sustained cholinesterase inhibition in AD patients receiving rivastigmine for 12 months. Neurology. 2002;59:563-572.
22. Weinstock M. Selectivity of cholinesterase inhibition. CNS Drugs. 1999;12:307-323.
23. Samochocki M, Zerlin M, Jostock R, et al. Galantamine is an allosterically potentiating ligand of the human alpha4/beta2 nAChR. Acta Neurol Scand Suppl. 2000;176:68-73.
24. Albuquerque EX, Alkondon M, Pereira EF, et al. Properties of neuronal nicotinic acetylcholine receptors: Pharmacological characterization and modulation of synaptic function. J Pharmacol Exp Ther. 1997;280:1117-1136.
25. Giacobini E. Selective inhibitors of butyrylcholinesterase: A valid alternative for therapy of Alzheimer's disease? Drugs Aging. 2001;18:891-898.
26. Schegg KM, Harrington LS, Neilsen S, et al. Soluble and membrane-bound forms of brain acetylcholinesterase in Alzheimer's disease. Neurobiol Aging. 1992;13:697-704.
27. Perry EK, Perry RH, Blessed G, Tomlinson BE. Changes in brain cholinesterases in senile dementia of Alzheimer type. Neuropathol Appl Neurobiol. 1978;4:273-277.
28. Mesulam M, Guillozet A, Shaw P, Quinn B. Widely spread butyrylcholinesterase can hydrolyze acetylcholine in the normal and Alzheimer brain. Neurobiol Dis. 2002;9:88-93.
29. Arendt T, Bruckner MK, Lange M, Bigl V. Changes in acetylcholinesterase and butyrylcholinesterase in Alzheimer's disease resemble embryonic development - a study of molecular forms. Neurochem Int. 1992;21:381-396.
30. Giacobini E, Spiegel R, Enz A, et al. Inhibition of acetyl- and butyryl-cholinesterase in the cerebrospinal fluid of patients with Alzheimer's disease by rivastigmine: Correlation with cognitive benefit. J Neural Transm. 2002;109:1053-1065.
31. Massoulie J, Bon S. The molecular forms of cholinesterase and acetylcholine in vertebrates. Annu Rev Neurosci. 1982;37:57-106.
32. Siek GC, Katz LS, Fishman EB, et al. Molecular forms of acetylcholinesterase in subcortical areas of normal and Alzheimer disease brain. Biol Psychiatry. 1990;27:573-580.
33. Poirier J. Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action. Int J Clin Pract Suppl. 2002;6-19.
34. Massoulie J, Pezzementi L, Bon S, et al. Molecular and cellular biology of cholinesterases. Prog Neurobiol. 1993;41:31-91.
35. Inglis F. The tolerability and safety of cholinesterase inhibitors in the treatment of dementia. Int J Clin Pract Suppl. 2002;45-63.
36. Svensson AL. Tacrine interacts with different sites on nicotinic receptor subtypes in SH-SY5Y neuroblastoma and M10 cells. Behav Brain Res. 2000;113:193-197.
37. Jhee SS, Shiovitz T, Hartman RD, et al. Centrally acting antiemetics mitigate nausea and vomiting in patients with Alzheimer's disease who receive rivastigmine. Clin Neuropharmacol. 2002;25:122-123.
38. Cutler N, Hartman R, Messina J, et al. Antiemetics mitigate nausea and vomiting in Alzheimer's patients. Biol Psychiatry. 2000;47:161S.
39. Scali C, Casamenti F, Bellucci A, et al. Effect of subchronic administration of metrifonate, rivastigmine and donepezil on brain acetylcholine in aged F344 rats. J Neural Trans. 2002;109:1067-1080.
40. McRae T, Orazem J. A large-scale, open-label trial of donepezil in the treatment of Alzheimer's disease: Side effects and concomitant medication use. Int J Neuropharmacol. 1999;2(Suppl 1):S176.
41. Shua-Haim JR, Smith JM, Amin S. Safety and tolerability of slow titration of rivastigmine (Exelon) in the treatment of patients with Alzheimer's disease (AD): An overall analysis of two prospective studies. J Am Geriatr Soc. 2001;49:S76. Abstract.
42. Raskind MA, Peskind ER, Wessel T, Yuan W, for the Galantamine USA-1 Study Group. Galantamine in AD: A 6-month, randomized, placebo-controlled trial with a 6-month extension. Neurology. 2000;54:2261-2268.
43. Vellas B, Inglis F, Potkin S, et al. Interim results from an international clinical trial with rivastigmine evaluating a 2-week titration rate in mild to severe Alzheimer's disease patients. Int J Geriatr Psychopharmacol. 1998;1:140-144.
44. Agid Y, Dubois B. Efficacy and tolerability of rivastigmine in patients with dementia of the Alzheimer type. Curr Ther Res Clin Exp. 1998;59:839-843.
45. Schneider LS, Anand R, Farlow MR. Systematic review of efficacy of rivastigmine for patients with Alzheimer's disease. Int J Geriatr Psychopharmacol. 1998;1(Suppl 1):S26-S34.
46. Moretti R, Torre P, Antonello R, et al. An open-label pilot study comparing rivastigmine and low-dose aspirin for the treatment of symptoms specific to patients with subcortical vascular dementia. Curr Ther Res Clin Exp. 2002;63:443-458.
47. Polinsky RJ. Clinical pharmacology of rivastigmine: A new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Clin Ther. 1998;20:634-647.
48. Anand R, Messina J, Hartman R. Dose-response effect of rivastigmine in the treatment of Alzheimer's disease. Int J Geriatr Psychopharmacol. 2000;2:68-72.
49. Cutler NR, Polinsky RJ, Sramek JJ, et al. Dose dependent CSF acetylcholinesterase inhibition by SDZ ENA 713 in Alzheimer's disease. Acta Neurol Scand. 1998;97:244-250.
50. Grossberg GT, Stahelin HB, Messina JC, et al. Lack of adverse pharmacodynamic drug interactions with rivastigmine and twenty-two classes of medication. Int J Geriatr Psychiatry. 2000;15:242-247.
51. Enz A, Amstutz R, Boddeke H, et al. Brain selective inhibition of acetylcholinesterase: A novel approach to therapy for Alzheimer's disease. Prog Brain Res. 1993 ;98:431-438.
52. Barner EL, Gray SL. Donepezil use in Alzheimer disease. Ann Pharmacother. 1998;32:70-77.
53. Pratt RD, Perdomo CA, and the 308 Study Group. Patient populations in clinical trials of the efficacy and tolerability of donepezil in patients with dementia and cerebrovascular disease ('vascular dementia'). Poster presented at the Second International Congress on Vascular Dementia; January 24-27, 2002; Salzburg, Austria.
54. Ancoli-Israel S, Poceta JS, Stepnowsky C, et al. Identification and treatment of sleep problems in the elderly. Sleep Med Rev. 1997;1:3-17.
55. Pollak CP, Perlick D. Sleep problems and institutionalization of the elderly. J Geriatr Psychiatry Neurol. 1991;4:204-210.
56. Schredl M, Weber B, Braus D, et al. The effect of rivastigmine on sleep in elderly healthy subjects. Exp Gerontol. 2000;35:243-249.
57. Riemann D, Gann H, Dressing H, et al. Influence of the cholinesterase inhibitor galanthamine hydrobromide on normal sleep. Psychiatry Res. 1994;51:253-267.
58. Gann H, Feige B, Hohagen F, et al. Sleep and the cholinergic rapid eye movement sleep induction test in patients with primary alcohol dependence. Biol Psychiatry. 2001;50:383-390.
59. Burns A, Rossor M, Hecker J, et al. The effects of donepezil in Alzheimer's disease - results from a multinational trial. Dement Geriatr Cogn Disord. 1999;10:237-244.
60. Enz A, Boddeke H, Gray J, Spiegel R. Pharmacologic and clinicopharmacologic properties of SDZ ENA 713, a centrally selective acetylcholinesterase inhibitor. Ann NY Acad Sci. 1991;640:272-275.
61. Wilkinson DG, Passmore P, Smith R, et al. Comparison of the tolerability, ease of use and efficacy of donepezil and rivastigmine in Alzheimer's disease patients: A 12-week multinational study. Presented at the 53rd Annual Meeting of the American Academy of Neurology; March 29-April 5, 2001; Philadelphia, Pa.
62. Cummings J, Anand R, Koumaras B, Hartman R. Rivastigmine provides behavioural benefits to Alzheimer's disease patients residing in a nursing home: Findings from a 26-week trial. Neurology. 2000;54(Suppl 3):A468. Abstract.
63. Grace J, Daniel S, Stevens T, et al. Long-term use of rivastigmine in patients with dementia with Lewy bodies: An open-label trial. Int Psychogeriatr. 2001;13:199-205.
64. Maclean LE, Collins CC, Byrne EJ. Dementia with Lewy bodies treated with rivastigmine: Effects on cognition, neuropsychiatric symptoms, and sleep. Int Psychogeriatr. 2001;13:277-288.
65. Reading PJ, Luce AK, McKeith IG. Rivastigmine in the treatment of parkinsonian psychosis and cognitive impairment: Preliminary findings from an open trial. Mov Disord. 2001;16:1171-1174.
66. Merello M, Sabe L, Teson A, et al. Extrapyramidalism in Alzheimer's disease: Prevalence, psychiatric, and neuropsychological correlates. J Neurol Neurosurg Psychiatry. 1994;57:1503-1509.
67. Ellis RJ, Caligiuri M, Galasko D, Thal LJ. Extrapyramidal motor signs in clinically diagnosed Alzheimer disease. Alzheimer Dis Assoc Disord. 1996;10:103-114.
68. Sweet RA, Akil M, Mulsant BH, et al. Determinants of spontaneous extrapyramidal symptoms in elderly psychiatric inpatients diagnosed with Alzheimer's disease, major depressive disorder, or psychotic disorders. J Neuropsychiatry Clin Neurosci. 1998;10:68-77.
69. McKeith I, Del Ser T, Spano F, et al. Efficacy of rivastigmine in dementia with Lewy bodies: A randomised, double-blind, placebo-controlled international study. Lancet. 2000;356:2031-2036.
70. Van Laar T, Vries J, Leenders K. Rivastigmine is effective and safe as anti-psychotic treatment in patients with Parkinson's disease. Presented at the 14th International Congress on Parkinson's Disease; November 10-14, 2001; Helsinki, Finland.
71. Weiser M, Rotmensch HH, Korczyn AD, et al. A pilot, randomized, open-label trial assessing safety and pharmacokinetic parameters of coadministration of rivastigmine with risperidone in dementia patients with behavioral disturbances. Int J Geriatr Psychiatry. 2002;17:343-346.
72. Shea C, MacKnight C, Rockwood K. Donepezil for treatment of dementia with Lewy bodies: A case series of nine patients. Int Psychogeriatr. 1998;10:229-238.
73. Sanders J, Newby VJ, Richardson JP, et al. Donepezil in dementia with Lewy bodies: Treatment and withdrawal. Int Psychogeriatr. 2001;13(Suppl 2):224. Abstract.
74. Magnuson TM, Keller BK, Burke WJ. Extrapyramidal side effects in a patient treated with risperidone plus donepezil. Am J Psychiatry. 1998;155:1458-1459.
75. Arai M. Parkinsonism onset in a patient concurrently using tiapride and donepezil. Intern Med. 2000;39:863.
76. Rizzo J. Comparison of adverse reaction reports for rivastigmine and donepezil using the FDA's adverse event reporting system. Poster presented at the 126th Annual Meeting of the American Neurological Association; September 30-October 3, 2001; Chicago, Ill.
77. Giacobini E. Cholinesterase inhibitors: From the Calabar bean to Alzheimer therapy. In: Giacobini E, ed. Cholinesterases and Cholinesterase Inhibitors. London: Martin Dunitz Ltd; 2000:181-226.
78. Singh S, Dudley C. Discontinuation syndrome following donepezil cessation. Int J Geriatr Psychiatry. 2003;18:282-284.
79. Doody RS, Geldmacher DS, Gordon B, et al. Open-label, multicenter, phase 3 extension study of the safety and efficacy of donepezil in patients with Alzheimer disease. Arch Neurol. 2001;58:427-433.
80. Rogers SL, Friedhoff LT. Long-term efficacy and safety of donepezil in the treatment of Alzheimer's disease: An interim analysis of the results of a US multicentre open label extension study. Eur Neuropsychopharmacol. 1998;8:67-75.
81. Rogers SL, Doody RS, Pratt RD, Ieni JR. Long-term efficacy and safety of donepezil in the treatment of Alzheimer's disease: Final analysis of a US multicentre open-label study. Eur Neuropsychopharmacol. 2000;10:195-203.
82. Winblad B, Engedal K, Soininen H, et al. A 1-year, randomized, placebo-controlled study of donepezil in patients with mild to moderate AD. Neurology. 2001;57:489-495.
83. Mohs RC, Doody RS, Morris JC, et al. A 1-year, placebo-controlled preservation of function survival study of donepezil in AD patients. Neurology. 2001;57:481-488.
84. Rosen WG, Mohs RC, Davis KL. A new rating scale for Alzheimer's disease. Am J Psychiatry. 1984;141:1356-1364.
85. Gottfries CG, Brane G, Steen G. A new rating scale for dementia syndromes. Gerontology. 1982;28(Suppl 2):20-31.
86. Cummings JL, Mega M, Gray K, et al. The Neuropsychiatric Inventory: Comprehensive assessment of psychopathology in dementia. Neurology. 1994;44:2308-2314.
87. DeJong R, Osterlund OW, Roy GW. Measurement of quality-of-life changes in patients with Alzheimer's disease. Clin Ther. 1989;11:545-554.
88. Folstein MF, Folstein SE, McHugh PR, et al. "Mini-mental state". A practical method for grading the cognitive state of patients for the clinician. J Psychiatr Res. 1975;12:189-198.
89. Raskind M, Truyen L. Galantamine has long-term cognitive benefits in Alzheimer's disease - an analysis of responder rates at 36 months. Poster presented at the 7th International Geneva/Springfield Symposium on Advances in Alzheimer Therapy; April 3-6, 2003; Geneva, Switzerland.
90. Grossberg G, Gapsar M, Touchon J, et al. Rivastigmine in Alzheimer's disease: Efficacy over 2 years compared with historical controls. Int Psychogeriatr. 2001;13 (Suppl 2):237. Abstract P-238.
91. Stern RG, Mohs RC, Davidson M, et al. A longitudinal study of Alzheimer's disease: Measurement, rate, and predictors of cognitive deterioration. Am J Psychiatry. 1994;151:390-396.
92. Rösler M, Retz W, Retz-Junginger P, Dennler HJ. Effects of two-year treatment with the cholinesterase inhibitor rivastigmine on behavioural symptoms in Alzheimer's disease. Behav Neurol. 1998;11:211-216.
93. Doraiswamy PM, Krishnan KR, Anand R, et al. Long-term effects of rivastigmine in moderately severe Alzheimer's disease: Does early initiation of therapy offer sustained benefits? Prog Neuropsychopharmacol Biol Psychiatry. 2002;26:705-712.
94. Moran MA, Mufson EJ, Gomez-Ramos P. Colocalization of cholinesterases with beta amyloid protein in aged and Alzheimer's brains. Acta Neuropathol (Berl). 1993;85:362-369.
95. Guillozet AL, Smiley JF, Mash DC, Mesulam MM. Butyrylcholinesterase in the life cycle of amyloid plaques. Ann Neurol. 1997;42:909-918.
96. Inestrosa NC, Alvarez A, Perez CA, et al. Acetylcholinesterase accelerates assembly of amyloid-beta-peptides into Alzheimer's fibrils: Possible role of the peripheral site of the enzyme. Neuron. 1996;16:881-891.
97. Inestrosa NC, Alarcon R. Molecular interactions of acetylcholinesterase with senile plaques. J Physiol Paris. 1998;92:341-344.
98. Alvarez A, Bronfman F, Perez CA, et al. Acetylcholinesterase, a senile plaque component, affects the fibrillogenesis of amyloid-beta-peptides. Neurosci Lett. 1995;201:49-52.
99. Alvarez A, Opazo C, Alarcon R, et al. Acetylcholinesterase promotes the aggregation of amyloid-beta-peptide fragments by forming a complex with the growing fibrils. J Mol Biol. 1997;272:348-361.
100. Alvarez A, Alarcon R, Opazo C, et al. Stable complexes involving acetylcholinesterase and amyloid-beta peptide change the biochemical properties of the enzyme and increase the neurotoxicity of Alzheimer's fibrils. J Neurosci. 1998;18:3213-3223.
101. Munoz FJ, Inestrosa NC. Neurotoxicity of acetylcholinesterase amyloid beta-peptide aggregates is dependent on the type of Abeta peptide and the AChE concentration present in the complexes. FEBS Lett. 1999;450:205-209.
102. Barber K, Mesulam M, Krafft G, Klein W. Butyrylcholinesterase alters the aggregation state of Aβ amyloid. Proc Soc Neurosci. 1996;22:1172.