The pharmacology of donepezil: A new treatment for Alzheimer's disease

Expert Opinion on Pharmacotherapy

Volumn 1, Issue 1, 1999, Pages 121-135

  Wilkinson, David G ^a  

^a UNIVERSITY OF SOUTHAMPTON   (United Kingdom)

Author keywords

Acetylcholinesterase inhibitor; Alzheimer's disease; Alzheimer's disease assessment scale (adas); Donepezil

Indexed keywords

CHOLINESTERASE INHIBITOR; DONEPEZIL; INDAN DERIVATIVE; NOOTROPIC AGENT; PIPERIDINE DERIVATIVE;

ALZHEIMER DISEASE; ANIMAL; CLINICAL TRIAL; DRUG INTERACTION; HUMAN; PATHOPHYSIOLOGY; PSYCHOLOGICAL ASPECT; REVIEW;

ALZHEIMER DISEASE; ANIMALS; CHOLINESTERASE INHIBITORS; CLINICAL TRIALS; DRUG INTERACTIONS; HUMANS; INDANS; NOOTROPIC AGENTS; PIPERIDINES;

EID: 0033224560     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656566.1.1.121     Document Type: Article

References (44)

1. HUFFMAN A, ROCCA WA, I5RAYNE C: The prevalence of dementia in Europe: a collaborative study of 1980-1990 findings. Int.J. EpUlemiol. (1991) 20:736-748.
2. GRAY AM, FENN P: Alzheimer's disease: the burden of illness in England. Health Trends (.1995) 25:31-37.
3. SMALL GW, RABINS PV, BARRY PB et ah Diagnosis and treatment of Alzheimer's disease and related disorders. JAMA (1997) 278:1363-1371.
4. SUMMERS WK, MAJOVSKI, MARSH GM ctal.: Oral tetrahydroaminoacridinc in long term treatment of senile dementia, Alzheimer type. i\'cw Engl. J. Mecl. (1986) 315:1241-12-45. • This study is of interest, although flawed, as it was the catalyst for the current development of AChEI for treatment of AD.
5. KNAPP MJ. KNOPMAN DS, SOLOMAN PR étal.: A 30-week randomised controlled trial of high dose tacrine in patients with Alzheimer's disease. JAMA (1994) 271:985-991. • First pivotal US Phase III study proving efficacy in AD.
6. NOCHI S, ASAKAWA N, SATO T: Kinetic study on the inhibition of acctyl- cholinesterase by l-benzyl-4- [(5,6 dimcthoxy-l-indanon)-2-yl] methylpiperidine hydrochloride (E2020). Blul. Pbarm. Bull. (1995) 18(8):1145-1147.
7. GALLI A, MORI F, BENINI L cl al.-. Acetylcholiiiesterase protection and the anti-diisopropylflurophosphate efficacy of E2020. Ein: J. Pbannacol. Em-iron. Toxicol. Pbannacol. (1994) 270:189-193.
8. NAKAMURA S, YUKAWA M, MIMORI Y: Abnormal properties of acctylcholinesterase inhibitors localised in senile plaque (abs.no.419). Keurobiol. Aging (1994) 15(Suppl. 1):S102.
9. ROGERS S, YAMANISHI Y, YAMATSU K: E2020-thc pharmacology of a piperidinc cholinesterase inhibitor. In: Cbolinergic Basis for Alzheimer's Therapy. Itecker U, Giacobini E (Eds.), Birkliauser, Boston, USA (1991):314-320.
10. FLICKER DM, DEAN RL, WATKINS DL: Behavioral and ncurochcmical effects following ncurotoxic lesions of a major cholinergic input to the cerebral cortex in the rat et al.: Pbannacol. Biocbem. Bebar. (1983) 18:973-981.
11. KAWASHIMA K, SATO A, YOSHIZAWA M et al.: Effects of the centrally acting cholinesterase inhibitors tetrahydroaminoacridinc and E2020 on the basal concentration of extracellular acctylcholinc in the hippocampus of freely moving rats. Nannyn-Schmiecl. Arch. Pharmncol. (1994) 350:523-528.
12. DAWSON GR, IVERSEN SD: The effects of novel cholinesterase inhibitors and selective muscarinic receptor agonists in tests of reference and working memory. Bebai: Brain Res. (1993) 30(57):143-153.
13. VAN DER STAAY FJ, HINTZ VC, SCHMIDT BH: Effects of metrifonate, its transformation product dichlorvos, and other organophosphorus and reference cholinesterase inhibitors on Morris water escape behaviour in young adult rats. J. Pbannacol. ExJ>. Ther. (1996) 278:697-708.
14. ROGERS SL, FRIEDHOFF LT: Pharmacokinctic and pharmacodynamic profile of doncpezil HC1 following single oral doses. Br.J, Clin. Pbannacol. (1998) 46(Suppl. l):l-6.
15. ROGERS SL, WALTERS EJ, FRIEDHOFF LT: The pharmacokinetics (PK) and pharmacodynamics (PD) of E2020 (R S)-I-benzyl-4-(5, 6 dimethoxy-l-indanon)-2-yl) methylpiperidine hydrochloride), a novel inhibitor of acetylcholinestcrasc (AChE): implications for use in the treatment of Alzheimer's disease (abstract). ffcnrobiol. Aging (1992) 13(1):496.
16. MIHARA M, OHNISHI A, TOMONO Y et al.: Pharmacoklnetics of £2020, a new compound for Alzheimer's disease, in healthy male volunteers. Int. J. Clin. Phaniuicol. Tlier. Toxicol. (1993) 31:223-229.
17. OHNISHI A, MIHAUA M, KAMAKURA H et cil.: Comparison of the pharmacokinctics of E2020, a new compound for Alzheimer's disease, in healthy, young and elderly subjects..J. Clin. l'bannacol. (1993) 33:1086-1091.
18. T1SEO PJ, I'EKDOMO CA, FRIEDHOFF LT: Metabolism and elimination of l4C-donepczil in healthy volunteers, a single dose study. Br.J. Clin, l'bannacol. (1998) 46(Suppl. l):19-24.
19. ROGERS S L, COOPER NM, SUKOVATY R et al.: Pharmacokinctic and pharmacodynamic pro flic of donepezil HC1 following multiple doses.J Clin. l'bannacol. (1998) 46(Suppl. 1):7-12.
20. T1SEO PJ, VARGAS R, PERDOMO CA, FRIEDHOFF LT: An evaluation of the pharmacokinctics of donepezil MCI in patients with impaired hepatic function. Br.J. Clin, l'bannacol. (1998) 46(Suppl. l):51-55.
21. EISAI AMERICA, INC.: US Package Insert: Aricept (donepezil hydrochloride tablets). (September 1998).
22. THAL LJ, SWAUTZ G, SANO M et al.: A multicentrc double-blind study of controlled-rclease physostigrninc for the treatment of symptoms secondary to Alzheimer's disease. I\'curolog)'(.l996) 47:1389-1395.
23. CHATELIER G, A, LACOMBLEZ L: Tacrine and Lecithin in senile dementia of the Alzheimer type; a multi-centre trial. Groupe Français et Etude de la Tetrahydroaminoacridine. Br. Med.J. (1990) 300:495-499.
24. MOLLOY GW, GIA'ATT GH, WILSON DU et al.: Effect of Tetrahydroaminoacridine on cognition, function and behaviour in Alzheimer's disease. Can. Meet. Assoc. J. (1991) 144:29-34.
25. LEBER P: Guidelines for the clinical evaluation of anti-dementia drugs. US FDA, Washington DC, USA (1990).
26. ROSEN WG, MOHS RC, DAVIS KL: A new rating scale for Alzheimer's disease. Am. J. Psycbiat. (1984) 141:1356-1364. • The description of the ADAS which has become the standard test of cognition in drug trials in dementia.
27. ROGERS SL, FRIEDHOFF LT, THE DONEPEZIL STUDY GROUP: The efficacy and Safety of Donepezil in patients with Alzheimer's disease: results of the US multicentrc, randomised, double-blind, placebocontrolled trial. Dementia (1996) 7:293-303.
28. SCHNEIDER LS, OLIN JT, DOODY US et al.: The Alzheimer's disease Cooperative Study: validity and reliability of the Alzheimer's disease Cooperative Study-Clinical Global Impression of Change. Alzbcimer Dis. Assoc. Disorel. (1997) IXSuppl. 2):S22-S32.
29. ROGERS SL, DOODY RS, MOHS RC et al.-. Donepezil improves cognition and global function in Alzheimer's disease. A 15 week, double-blind, placebo-controlled study. Arch. Int. Mecl. (1998) 158:1021-1031. The first pivotal study to show efficacy of donepezil in the US with benefits maintained during a 3 week washout.
30. ROGERS SL, FARLOW MD, DOODY RS et ah. A 24 week, double-blind, placebo-controlled trial of donepezil in patients with Alzheiiner's disease. Xeurvlog)- (1998) 50:136-145. A classic study the major pivotal Phase III trial in US.
31. BURNS A, ROSSOR M, HECKER J et al: The Effects of Donepczil in Alzhcimcr's disease-Results from a Multinational Trial. Dement. Geriatr. Cogii.Disord.d999) 10:237-244. The non-US version of [30] using same protocol and producing similar results but demonstrating greater efficacy for 10 mg rather than 5 nig.
32. BERG L, MILLER JP, BATYJ elal.: Mild senile dementia of the Alzheimer type: 4 evaluations of intervention. Ann. Xetiivl. (1992) 31:242-209.
33. TEUNISSE S, DERIX M, VAN CREVEL H: Assessing the severity of dementia, patient and care-giver. Arch. Nciiml. (1991) 48:274-277. • Paper describing the IDDD scale for measuring functional change.
34. FRIEDHOFF LT, ROGERS SL: Doncpczil lengthens time to loss of activities of daily living in patients with mild to moderate Alzhcimer's disease-results of preliminary evaluation. Neurology (1997) 48(S):A100 (P02.026).
35. BLAU TH: Quality of life, social indicators and criteria of change. I'mf. I'sycbol. (1977) 8:464-473.
36. ROGERS S. FRIEDHOFF L: Long-term efficacy and safety of donepezil in the treatment of Alzheimer's disease: an interim analysis of the results of the US multiccntrc open label extension study. Eur. Neuropsycbopbarmacol. (1998)8:67-75. • An open label continuation study of 129] showing maintenance of effects for a furthe 26 weeks.
37. STERN RG, MOMS RC, DAVIDSON M étal.-. A longitudinal study of Alzheimer's disease: measurement, rate and predictors of cognitive deterioration. Am.J. I'sychiat. (1994) 15K3):390-396.
38. PRATT RD, GELDMACHER DS., PERDOMO CA: An evaluation of the long-term efficacy of donepezil in patients from a Phase III clinical extension trial [posterJpresentation]. Annual Meeting of the American Academy of Keiimlog): Toronto, USA (1999).
39. DOODY RS, GELDMACHER DS, PRATT RD et al.: Optimal donepezil efficacy in Alzheimer's disease is dependent on continued administration. J. Neural. (1999) 246(Suppl. 1):P226 (I 52).
40. MCRAE T, ORAZEM J: Donepezil safety and efficacy in a large, community-based, open-label trial. J. Keurol. (1999) 246(Suppl. 1):P224 (152).
41. KAUFER D, CATT K, POLLOCK B et al.: Donepezil in Alzheimer's disease: relative cognitive and neuropsychiatrie response and impact in caregiver distress [posterj American Geriatrics Society. Seattle, USA (1998). Poster 198.
42. MATTHEWS H, KORBEY J, WILKINSON DG et al.: First year results of donepezil use in a UK clinic for AD [Poster]. A7 Congress of World Psychiatrie Association. Hamburg, Germany (1999).
43. RASKIND MA, CYRUS l'A, KUZICKAUI3, GULANSKI DI: The effects of mctrifonate on the cognitive, behavioral, and functional performance of AJzheimer's disease patients. Metrifonatc Study Group. J Clin. Psycbifit. (1999) 60(5):318-25.
44. KAUFER D: Beyond the cholincrgic hypothesis: the effect of metrifonate and other chollnesterasc inhibitors on neuropsychiatrie symptoms in AJzheimer's disease. Dement. Geriatr. Cogn. Disorcl. (1998) 9(Suppl. 21:8-14.