Cholinesterase inhibitors in the treatment of Alzheimer's disease. A comparison of tolerability and pharmacology

Drug Safety

Volumn 19, Issue 6, 1998, Pages 465-480

  Nordberg, Agneta ^a   Svensson, Anne Lie ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINESTERASE; CHOLINESTERASE; CHOLINESTERASE INHIBITOR; CIMETIDINE; CYTOCHROME P450; DONEPEZIL; ESTERASE; GALANTAMINE; HEPTYLSTIGMINE TARTRATE; METRIFONATE; PHYSOSTIGMINE; RIVASTIGMINE; TACRINE; THEOPHYLLINE; WARFARIN;

ABDOMINAL PAIN; ALZHEIMER DISEASE; ANOREXIA; APLASTIC ANEMIA; BRADYCARDIA; CLINICAL TRIAL; COGNITION; DIARRHEA; DISEASE COURSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG TOLERABILITY; DYSPEPSIA; ENZYME INHIBITION; FOOD DRUG INTERACTION; FOOD INTAKE; HEART VENTRICLE EXTRASYSTOLE; HUMAN; LIVER TOXICITY; MUSCLE CRAMP; MUSCLE WEAKNESS; NAUSEA; NEUROPROTECTION; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; REVIEW; SIDE EFFECT; VERTIGO; VOMITING;

ALZHEIMER DISEASE; CHOLINESTERASE INHIBITORS; HUMANS;

EID: 0032439162     PISSN: 01145916     EISSN: None     Source Type: Journal    
DOI: 10.2165/00002018-199819060-00004     Document Type: Review

References (101)

1. Fratiglioni L. Epidemiology of Alzheimer's disease. Acta Neurol Scand 1993; Suppl. 87: 1-70
2. Masters CL, Beyreuther K. Alzheimer's disease. BMJ 1998; 316: 446-8
3. Nordberg A. Pharmacological treatment of cognitive dysfunction in dementia disorders. Acta Neurol Scand 1996; Suppl. 168: 87-92
4. Knopman DS, Morris JC. An update on primary drug therapies for Alzheimer's disease. Arch Neurol 1997; 54: 1406-9
5. Nordberg A. Biological markers and the cholinergic hypothesis in Alzheimer's disease. Acta Neurol Scand 1992; Suppl. 139: 54-8
6. Lawrence AD, Sahakian BJ. Alzheimer's disease, attention and the cholinergic system. Alzheimer Dis Assoc Disord 1995; 9: 43-39
7. Amberla K, Nordberg A, Viitanen M, et al. Long-term treatment with tacrine (THA) in Alzheimer's disease-evaluation of neuropsychological data. Acta Neurol Scand 1993; Suppl. 149: 55-7
8. Maltby N, Broe GA, Creasey H, et al. Efficacy of tacrine and lecithin in mild to moderate Alzheimer's disease: double blind trial. BMJ 1994; 308: 879-83
9. Nordberg A, Amberla K, Shigeta M, et al. Long-term tacrine treatment in three mild Alzheimer patients: effects on nicotinic receptors, cerebral blood flow, glucose metabolism, EEG and cognitive abilities. Alzheimer Dis Assoc Disord 1998; 12: 228-37
10. Knopman DS, Schneider L, Davis K, et al. Long-term tacrine (Cognex) treatment: effect on nursing home placement and mortality. Neurology 1996; 47: 166-77
11. Minthon L, Nilsson K, Edvinsson L, et al. Long-term effect of tacrine on regional cerebral blood flow changes in Alzheimer's disease. Dementia 1995; 6: 245-51
12. Reisberg B, Burns A, Gauthier S, et al., editors. Outcome methodologies for pharmacologic trials in mild, moderate, and severe Alzheimer's disease. Int Psychogeriatr 1996; 8: 155-344
13. Nordberg A. Functional studies of new drugs for the treatment of Alzheimer's disease. Acta Neurol Scand 1996; Suppl. 165: 137-44
14. Arendt T, Brückner MT, Lange M, et al. Changes in acetylcholinesterase and butyrylcholinesterase in Alzheimer's disease resemble embryonic development- a study of molecular forms. Neurochem Int 1992; 3: 381-96
15. Kása P, Bakonczay Z, Gulya K. The cholinergic system in Alzheimer's disease. Prog Neurobiol 1997; 52: 511-35
16. Ogane N, Giacobini E, Struble R. Differential inhibition of acelylcholinesterase molecular forms in normal and Alzheimer disease brain. Brain Res 1992; 589: 307-12
17. Perry EK, Tomlinson BE, Blessed G, et al. Correlation of cholinergic abnormalities with senile plaques and mental test scores in senile dementia. BMJ 1978; 2: 1457-9
18. Atack JR, Perry EK, Bronham JR, et al. Molecular forms of acetylcholinesterase in senile dementia of Alzheimer's type: selective loss of the intermediate (10S) form. Neurosci Lett 1983: 40: 199-204
19. Inestrosa NC, Alvarez A, Perez CA, et al. Acetylcholinesterase accelerates assembly of amyloid-β-peptides into Alzheimer's fibrils: possible role of the peripheral site of the enzyme. Neuron 1996; 16: 881-91
20. Wright CI, Geula C, Mesulam MM. Neuroglial cholinesterases in the normal brain and Alzheimers disease: relationship to plaques, tangles and pattern of selective vulnerability. Ann Neurol 1993; 34: 373-84
21. Appleyard ME, Smith AD, Berman P, et al. Cholinesterase activities in cerebrospinal fluid of patients with senile dementia of Alzheimer type. Brain 1987; 110: 1309-22
22. Sáez-Valero J, McLean CA, Masters C, et al. Glycosylation of acetylcholinesterase as diagnostic marker for Alzheimer's disease. Lancet 1997; 350: 929
23. Navaratnam DS, Priddle JD, McDonald, et al. Anomalous molecular form of acetylcholinesterase in cerebrospinal fluid in histopathological diagnosed Alzheimer's disease. Lancet 1991; 337: 447-50
24. Shen ZX. An CSF anomalous molecular form of acetylcholinesterase in demented and non-demented subjects. Neuroreport 1997; 8: 3229-32
25. Shen ZX. CSF cholinesterase activity in demented and non-demented subjects. Neuroreport 1998; 9: 483-8
26. Pappata S, Tavitian B, Traykov L, et al. In vivo imaging of human acetylcholinesterase. J Neurochem 1996; 67: 876-9
27. Iyo M, Namba H, Fukushi K, et al. Measurement of acelylcholinesterase by positron emission tomography in the brains of healthy controls and patients with Alzheimer's disease. Lancet 1997; 349: 1805-9
28. Nilsson L, Adem A, Hardy J, et al. Do tetrahydroaminoacridine (THA) and physostigmine restore acetylcholine release in Alzheimer brains via nicotinic receptors? J Neural Transm 1987; 70: 357-68
29. Svensson AL, Zhang X, Nordberg A. Biphasic effect of tacrine tin acetylcholine release in rat brain via M1 and M2 receptors. Brain Res 1996; 726: 207-12
30. Wagstaff A, McTavish D. Tacrine: a review of its pharmacological and pharmacokinetic properties and therapeutic potential in Alzheimer's disease. Drugs & Aging 1994; 4: 1-31
31. Pereira EFR, Alkondon M, Reinhardt S, et al. Physostigmine and galanthamine: probes for a novel binding site on the a4β2 subtype of neuronal nicotinic acetylcholine receptors stably expressed in fibroblast cells. J Pharmacol Exp Ther 1994; 270: 768-78
32. Svensson AL, Nordberg A. Tacrine interacts with an allosteric activator site on a4β2 AChRs in M10 cells. Neuroreport 1996; 7: 2201-5
33. Svensson AL, Nordberg A. The acetylcholinesterase inhibitors donepezil, galanlhamine and NXX-066 interact differently with the neuronal a4β2 nicotinic receptors in M10 cells. Br J Pharmacol. In press
34. Lahiri DK, Lewis S, Farlow MR. Tacrine alters the secretion of the beta-amyloid precursor protein in cell lines. J Neurosci Res 1994; 37: 777-87
35. Mori F, Lai CC, Fusi F, et al. Cholinesterase inhibitors increase secretion of APPs in rat brain cortex. Neuroreport 1995; 6: 633-6
36. Haroutunian V, Greig N, Pei XF, et al. Pharmacological modulation of Alzheimer's β-amyloid precursor protein levels in the CSF of rats with forebrain cholinergic system lesions. Soc Neurosci 1996; 22: 1169
37. Chong YH, Suh YH. Amyloidogenic processing of Alzheimer's amyloid precursor protein in vitro and its modulation by metal ion and lacrine. Life Sci 1996; 59: 545-57
38. Svensson AL, Nordberg A. Tacrine and donepezil attenuate the neurotoxic effect of Aβ (25-35) in rat PC12 cells. Neuroreport 1998; 9: 1519-22
39. Freeman SE, Dawson RM. Tacrine: a pharmacological review. Prog Neurobiol 1991; 36: 257-77
40. Johansson M, Hellström-Lindahl E, Nordberg A. Steady-state pharmacokinetics of tacrine in long-term treatment of Alzheimer patients. Dementia 1996; 7: 111-7
41. Hartvig P, Askmark H, Aquilonius SM, et al. Clinical pharmacokinetics of intravenous and oral 9-amino-1,2,3,4-tetrahydroacridine, tacrine. Fur J Clin Pharmacol 1990; 38: 259-63
42. Hartvig P, Pettersson E, Wiklund L, et al. Pharmacokinetics and effects of 9-amino-1,2,3.4-tetrahydroacridine in the immediate postoperative period in neurosurgical patients. J Clin Anesth 1991; 3: 137-42
43. Forsyth DR, Wilcock GK, Morgan RA, et al. Pharmacokinetics of tacrine hydrochloride in Alzheimer's disease. Clin Pharmacol Ther 1989; 46: 634-41
44. Cutler NR, Sedman AJ, Prior P, et al. Steady-state pharmacokinetics of tacrine in patients with Alzheimer's disease. Psychopharmacol Bull 1990; 26: 231-4
45. Ahlin A, Adem A, Junthé T, et al. Pharmacokinetics of tetrahydroaminoacridine: relations to clinical and biochemical effects in Alzheimer patients. Int Clin Psychopharmacol 1992; 7: 29-36
46. Nybäck H, Nyman H, Öhman G, et al. Preliminary experiences and results with THA for the amelioration of symptoms of Alzheimer's disease. In: Giacobini E, Becker R, editors. Current Research in Alzheimer Therapy. New York: Taylor, Francis, 1988: 231-6
47. Selen A, Balogh L, Siedlik P, et al. Pharmacokinetics of tacrine in healthy subjects. Pharmacol Res 1988; 5: S-218
48. Askmark H, Aquilonius S-M, Gillberg P-G, et al. Functional and pharmacokinetic studies of tetrahydroaminoacridine in patients with amyotrophic lateral sclerosis. Acta Neurol Scand 1990; 82: 253-8
49. Ford JM, Truman CA, Wilcock GK, et al. Serum concentrations of tacrine hydrochloride predict its adverse effects in Alzheimer's disease. Clin Pharmacol Ther 1993; 53: 691-5
50. Samuels SC, Davies K. A risk-benefit assessment of tacrine in the treattnenl of Alzheimer's disease. Drug Saf 1997; 16: 66-77
51. Murphy MF, Hardiman ST, Nash RJ, et al. Evaluation of HP 029 (velnacrine maleate) in Alzheimer's disease. Ann N Y Acad Sci 1991; 640: 253-62
52. Knapp MJ, Knopman DS, Solomon PR, et al. A 30-week randomized controlled trial of high-dose tacrine in patients with Alzheimer's disease. JAMA 1994; 271: 985-91
53. Watkins PB, Zimmerman HJ, Knapp MJ, et al. Hepatotoxic effects of tacrine administration in patients with Alzheimer's disease. JAMA 1994; 271: 992-8
54. Gracon SI, Knapp MJ, Berghoff WG, et al. Safety of tacrine: clinical trials, treatment IND, and postmarketing experience. Alzheimer Dis Assoc Disord 1998; 12: 93-101
55. Nochi S, Asakawa N, Saro T. Kinetic study on the inhibition of acetylcholinesterase by 1-benzyl-4-|(5,6-dimethoxy-1-indanon)-2-yl| methylpiperidine hydrochloride (E2020). Biol Pharm Bull 1995; 18: 1145-7
56. Galli A, Mori F, Benini L, et al. Acetylcholinesterase protection and the anti-diisopropylfluorophosphate efficacy of E2020. Eur J Pharmacol Environ Toxicol Pharmacol 1994; 270: 183-93
57. Rogers SL, Walters EJ, Friedhoff LT. The pharmacokinetics (PK) and pharmacodynamics (PD) of E2020 (R,S)-1-benzyl-4-(5,6-dimetho\y-1-indanon)-2-yl)-methylpiperidine hydrochloride) a novel inhibitor of acetylcholinestenise (AChE): implications for use in the treatment of Alzheimer's disease. Neurobiol Aging 1992; 13: 496
58. Barner EL, Gray SL. Donepezil use in Alzheimer disease. Ann Pharmacother 1998; 12: 70-7
59. Bryson HM, Benfield P, Donepezil. Drugs Aging 1997; 10: 234-9
60. Rogers SL, Farlow MR, Doody RS, et al. A 24 week, double-blind, placebo-controlled trial of donepezil in patients with Alzheimer's disease. Neurology 1998; 50: 136-45
61. 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 Neuropharmacol 1998; 8: 67-75
62. Rogers SL, Friedhoff LT. Donepezil Study Group. The efficacy and safety of donepezil in patients with Alzheimer's disease: results of a US multicentre, randomized, double-blind, placebo-controlled trial. Dementia 1996; 7: 293-303
63. Rainer M. Galanthamine in Alzheimer's disease: a new alternative to tacrine? CNS Drugs 1997; 7: 89-97
64. Kewitz H. Pharmacokinetics and metabolism of galanthamine. Drugs Today 1997; 33: 265-72
65. Rainer M. Clinical studies of galanthamine. Drugs Today 1997; 4: 273-9
66. Holmstedt B, Nordgren I, Sandoz M, et al. Metrifonate: summary of toxicological and pharmacological information available. Acta Toxicol 1978; 41: 3-29
67. Hintz VC, Grewig S, Schmidt BH. Metrifonate induces cholinesterase inhibition exclusively via slow release of dichlorvos. Neurochem Res 1996; 21: 331-7
68. Lamb HM, Faulds D. Metrifonate. Drugs Aging 1997; 11: 490-6
69. Becker RE, Colliver JA, Markwell SJ, et al. Effects of metrifonate on cognitive decline in Alzheimer disease: a double-blind, placebo-controlled, 6-months study. Alzheimer Dis Assoc Disord 1998; 12: 54-7
70. Abdi YA, Villén T. Pharmacokinetics of metrifonate and its rearrangement product dichlorvos in whole blood. Pharmacol Toxicol 1991; 68: 137-9
71. Unni LK, Womack C, Hannant ME, et al. Pharmacokinetics and pharmacodynamics of metrifonate in humans. Methods Find Exp Clin Pharmacol 1994; 16: 285-9
72. Becker RE, Moriearty P, Unni L, et al. Cholinesterase inhibitors as therapy in Alzheimer's disease: benefit to risk consideration in clinical application. In: Becker R, Giacobini E, editors. Alzheimer Disease: from molecular biology to therapy. Boston: Birkhäuser 1996; 257-66
73. Morris JC, Cyrus PA, Orazem J, et al. Metrifonate benefits cognitive, behavioural, and global functions in patients with Alzheimer's disease. Neurology 1998; 50: 1222-30
74. Holmstedt B, Nordgren I, Sandoz M, et al. Metrifonate: summary of toxicological and pharmacological infomiation available. Arch Toxicol 1978: 41: 3-29
75. Render SA, Filbert MG, Moore DH, et al. A role for butyrylcholinesterases in respiratory pathophysiology following nerve-agent intoxication. Proceedings of the Sixth Medical Chemical Defense Bioscience Review 1987; 13: 393-6
76. Anon. Bayer suspends metrifonate trials. SCRIP 1998 Sep 30: 2374: 19
77. Somani SM. Pharmacokinetics and pharmacodynamics of physostigmine in the rat after oral administration. Biopharm Drug Dispos 1989: 10: 187-203
78. Thai LJ, Schwartz G, Sano M. et al. A multicenter double-blind study of controlled-release physostigmine for the treatment of symptoms secondary to Alzheimer's disease. Neurology 1946: 47: 1389-95
79. Walter K, Müller M, Barkworth F, et al. Pharmacokinetics of physostigmine in man following a single application of a transdermal system. Br J Clin Pharmacol 1995; 39: 59-63
80. Becker RE, Moriearty P, Unni L. The second generation of cholinesierase inhibitors: clinical and pharmacological effects. In: Becker R, Giacobini E, editors. Cholinergic basis for Alzheimer therapy. Boston: Birkhäuser 1991: 263-96
81. Williams FM. Serum enzymes of drug metabolism. Pharmacol Ther 1987; 34: 99-109
82. Whelpton R, Hurst P. Bioavailability of oral physostigmine. New Engl J Med 1985; 313: 1293-4
83. McClellan KJ, Benfield P. Eptastigmine. CNS Drugs 1997; 9: 69-75
84. Auteri A, Mosca A, Lattuada N, et al. Pharmacodynamics and pharmacokinetics of eptastigmine in elderly subjects. Eur J Clin Pharmacol 1993; 45: 373-6
85. Imbunbo BP, Licini M, Schettino M, et al. Relationship between pharmacokinetics and pharmacodynamics of eptastigmine in young healthy volunteers. J Clin Pharmacol 1995; 35: 285-90
86. Stramek JJ, Block GA, Reines SA, et al. A multiple-dose safety trial of eptastigmine in Alzheimer's disease, with pharmacodynamic observations of red blood cell cholinesterase. Life Sci 1995; 56: 319-26
87. Canal N, Imbimbo BP, Eptastigmine Study Group. Relationship between pharmacodynamic activity and cognitive effects of eptastigmine in patients with Alzheimer's disease. Clin Parmacol Ther 1996; 60: 218-28
88. Unni LK. Beyond tacrine: recently developed cholinesterase inhibitors for the treatment of Alzheimer's disease. CNS Drugs. In press
89. Enz A, Floersheim P. Cholinesterase inhibitors: an overview of their mechanisms of action. In: Becker R, Giacobini E, editors. Alzheimer disease: from molecular biology to therapy. Boston: Birkhauser 1996; 211-5
90. Cutler NR, Polmsky RJ, Sramek JS, et al. Dose-dependent CSF acetylcholinesterase inhibition by SDZ ENA 713 in Alzheimer's disease. Acta Neurol Scand 1998; 97: 244-50
91. Anand R, Hartman D, Hayes P, et al. An overview of the development of SDZ ENA 713, a brain selective cholinesterase inhibitor. In: Becker R, Giacobini E, editors. Boston: Birkhäuser 1996: 239-43
92. IM (ENA-713) in Alzheimer's disease: an overview. J Drug Dev Clin Pract 1996; 8: 1-14
93. Enz A, Armstutz R, Boddeke H, et al. Brain selective inhibition of acetylcholinestciase: a novel approach to therapy for Alzheimer's disease. Prog Brain Res 1993; 98: 431-8
94. Anand R, Gharabawi G. Clinical development of ExelonTM (ENA-713): the adena program. J Drug Dev Clin Pract 1996; 8: 9-14
95. Spencer CS, Noble S. Rivastigmine: review of its use in Alzheimer's disease. Drug & Aging 1998; 13: 391-411
96. Corey-Bloom J, Anand R, Veach J. A randomized trial evaluating the efficacy and safety of HNA 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
97. Cummmgs JL. Changes in Neuropsychiatric symptoms as outcome measures m clinical trials with cholinergic therapies for Alzheimer disease. Alzheimer Dis Assoc Disord 1997; Suppl. 4: S1-9
98. Giacobini H. From molecular structure to Alzheimer therapy. Jpn J Pharmacol 1997; 74: 225-41
99. Troetel WM, Imbimho BP. Overview of the development of eptastigmine, a longacting cholinestesterase inhibitor. In: Iqhal K, Winblad B, Nishimura T, et al., editors. Alzheimer's disease: biology, diagnosis and therapeutics. Chichcster: John Whiley & Sons, 1997: 671-6
100. Kaufer D, Friedman A, Seidman, et al. Acute stress facilitates long-lasting changes in cholinergic gene expression. Nature 1998; 393: 373-6
101. von der Krammer, Mayhaus M, Albrecht C, et al. Musearinic acetylcholine receptors activate expression of the Erg gene family. J Biol Chem 1998; 273: 14538-44