Rivastigmine, a brain-region selective acetylcholinesterase inhibitor for treating Alzheimer’s disease: review and current status

Bibliography

• MCKHANN G, DRACHMAN D, FOLSTEIN M et al.: Clinical diagnosis of Alzheimer's disease: report of the NINCDS-ADRA Work Group under the auspices of the Department of Health and Human Services Task Force on Alzheimer's disease. Neurology (1984) 34:939–944.
   PubMed Web of Science ®Google Scholar
• •Consensus statement on the criteria for the diagnosis of Alzheimer's disease.
   Google Scholar
• EVANS DA, FUNKENSTEIN HH, ALBERT MS et al.: Prevalence of Alzheimer's disease in a community population of older person. Higher than previously reported. JAMA (1989) 262:2551–2556.
   Google Scholar
• GIACOBINI E: From Molecular Structure to Alzheimer Therapy. Jpnj Pharmacol (1997) 74:225–241.
   PubMedGoogle Scholar
• BRUFANI M, FILOCAMO LAPPA S et al.: New acetylcholin-esterase inhibitors. Drugs of the Future (1997) 22:397–410.
   Google Scholar
• BARTUS RT, DEAN RL, BEER et al.: The cholinergic hypothesis of geriatric memory dysfunction. Science (1982) 217:1184–1190.
   Web of Science ®Google Scholar
• Cognex Macrine) package insert. Morris Plains, NJ: Parke-Davis (1996).
   Google Scholar
• FARLOW M, GRACON SI, HERSHEY LA et al.: A controlled trial of tacrine in Alzheimer's disease. JAMA (1992) 268:2523–2529.
   PubMed Web of Science ®Google Scholar
• KNAPP MJ, KNOPMAN DS, SOLOMON PR et al.: A 30-weekrandomized controlled trial of high-dose tacrine in patients with Alzheimer's disease. JAMA (1994) 271 :985–991.
   PubMed Web of Science ®Google Scholar
• Aricept(Donepezil) package insert. New York:Eisai/Pfizer (1996).
   Google Scholar
• ROGERS SL, FRIEDHOFF LT AND THE DONEPEZIL STUDYGROUP: 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.
   PubMedGoogle Scholar
• 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) 50:136–145.
   PubMed Web of Science ®Google Scholar
• ENZ A, AMSTUTZ R, BODDEKE H et al.: Brain selectiveinhibition of acetylcholinesterase: a novel approach to therapy for Alzheimer's disease. Prog. Brain Res. (1993) 98:431–438.
   PubMed Web of Science ®Google Scholar
• •Comparison of brain distribution and acetylcholinesterase binding profiles (G1 and G4) for rivastigmine, tacrine and physostigmine.
   Google Scholar
• ENZ A, FLOERSHEIM P: Cholinesterase Inhibitors: an overview of their mechanisms of action. In: Alzheimer's disease. From Molecular Biology to Therapy Becker R, Giacobini E (Eds.), Birkhauser, Boston (1996):211–215.
   Google Scholar
• •Comparison of pharmacodynamic properties of several acetylcholinesterase inhibitors.
   Google Scholar
• ENZ A, MEIER D, SPIEGEL R: Effects of novel cholines-terase inhibitors based on the mechanism of enzyme inhibition. In: Alzheimer's disease. Therapeutic Strategies. Giacobini E, Becker R, (Eds.), Birkhauser, Boston, USA (1994) :125–130.
   Google Scholar
• ENZ A, BODDEKE H: Pharmacologic and clinicophar-macologic properties of SDZ ENA 713, a centrally selective acetycholinesterase inhibitor. Ann. NY Acad. Sci. (1991) 640:272–275.
   PubMedGoogle Scholar
• •Evaluation of the duration of action of rivastigmine.
   Google Scholar
• WEINSTOCK M: Possible role of the cholinergic system and disease models. J. Neural. Transm. (1997) 49:93–102.
   Google Scholar
• WHITE LR, CARTWRIGHT WS, CORNONI-HUNTLEY et al.: Geriatric epidemiology. Ann. Rev. Gerontol. Geriatr. (1986) 6:215–311.
   PubMedGoogle Scholar
• HEBERT LE, SCHERR PA, BECKETT LA et al.: Age specific incidence of Alzheimer's disease in a community population. JAMA (1995) 273:1354–1359.
   PubMed Web of Science ®Google Scholar
• LI G,SILVERMAN JM, SMITH CJ et al.: Age at onset and familial risk in Alzheimer's disease. Am. J. Psychiatry (1995) 152:424–430.
   Google Scholar
• SELKOE DJ: Translating cell biology into therapeutic advances in Alzheimer's disease. Nature (1999) (Suppl.):A23–A30.
   Google Scholar
• ••Extensive discussion of the proposed molecularmechanisms for the pathogenesis of AD and identification of new pharmacologic targets.
   Google Scholar
• ALLAIN H et al.: Pharmacology of Alzheimer's disease. Prog. Med. Chem. (1997) 34:1–67.
   Google Scholar
• BENZI G, MORETTI A: Is there a rationale for the use ofacetylcholinesterase inhibitors in the therapy of Alzheimer's disease? Eur.J. Pharmacol (1998) 346:1–13.
   Google Scholar
• WEINSTOCK M., RAZIN M, CHOREV M et al.: Pharma-cological evaluation of phenyl-carbamates as CNS-selective acetylcholinesterase inhibitors. J. Neural. Transm. (1994) (Supp1.43):219–225.
   Google Scholar
• PERRY E, PERRY RH, BLESSED G et al.: Changes in brain cholinesterases in senile dementia of Alzheimer's type. Neuropath. Appl. Neurobiol. (1978) 4:273–277.
   PubMed Web of Science ®Google Scholar
• DAVIS K, MOHS R, MARIN D et al.: Cholinergic markers in elderly patients with early signs of Alzheimer's disease. JAMA (1999) 281:1401–1406.
   PubMed Web of Science ®Google Scholar
• GUILLOZET AL, SMILEY JF, MASH DC et al.: Butyrylcho-linesterase in the life cycle of amyloid plaques. Ann. Neurol (1997) 42:909–918.
   PubMed Web of Science ®Google Scholar
• ENZ A, CHAPPUIS A, PROBST A: Different influence ofinhibitors on acetylcholinesterase forms G1 and G4 isolated from Alzheimer's disease and control brains. In: Multidisciplinary Approaches to Cholinesterase Functions. Shafferman A, Velan B, (Eds.) Plenum Press, New York (1992):243–249.
   Google Scholar
• 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.
   PubMed Web of Science ®Google Scholar
• ••Presents evidence for central selectivity and duration ofaction for rivastigmine by evaluation of binding properties and concentrations in the CSF.
   Google Scholar
• SUGIMOTO H, ILIMURA Y, YAMINISHI Y et al.: Synthesis and structure-activity relationships of acetylcholines-terase inhibitors. J. Med. Chem. (1995) 24:4821–4829
   Web of Science ®Google Scholar
• SUGIMOTO H, TSUCHIYA Y, SUGUMI H et al.: Synthesis and structure relationships of acetycholinesterase inhibitors:1 -benzy1-4 -[2 -(N-benzoyl-N-phenylamino)ethyl]piperidine and related deriva-tives. J. Med. Chem. (1992) 35:4542–4548.
   PubMed Web of Science ®Google Scholar
• Data on file: Novartis Pharma AG. Basel, Switzerland (1996).
   Google Scholar
• POLINSKY RJ: Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Clin. Ther. (1998) 20:634–647.
   PubMed Web of Science ®Google Scholar
• ••Comprehensive compilation of pharmacokinetic andpharmacodynamic data for rivastgmine.
   Google Scholar
• SCHRAN HF, HABUCKY K, MANCIONE L et al.: The effectsof renal and hepatic impairment on the disposition of the acetycholinesterase inhibitor SDZ ENA 713. Pharm. Res. (1996) 13\(Suppl. 9) S428. Abstract.
   Google Scholar
• TANAKA K, MIZUKAWA K, OGAWA N: Post-ischemic administration of the acetylcholinesterase inhbitor ENA-713 prevents delayed neuronal death in the gerbil hippocampus. Neurochem. Res. (1995) 20:663–667.
   PubMed Web of Science ®Google Scholar
• TANAKA K, OGAWA N, ASANUMA M eta].: Effects of the acetycholinesterase inhibitor ENA-713 on ischemia-induced changes in acetylcholine and the aromatic amine levels in the gerbil brain. Arch. Int. Pharma-codyn. (1993) 323:85–96.
   Google Scholar
• SADOSHIMA S, IBAYASHI S, FUJII K eta].: Inhibition of acetylcholinesterase modulates the autoregulation of cerebral blood flow and attenuates ischemic brain metabolism in hypertensive rats. J. Cereb. Blood Flow Metab. (1995) 15:845–851.
   Google Scholar
• CHEN Y, SHOHAMI E, BASS R et al.: Cerebro-protective effects of ENA 713, a novel acetylcholinesterase inhibitor, in closed head injury in the rat. Brain Res. (1998) 784:18–24.
   PubMed Web of Science ®Google Scholar
• NIIGAWA H, TANIMUKAI S, TAKEDA M et al.: Effects ofSDZ-713, a novel acetylcholinesterase inhibitor, on learning of rats with basal forebrain lesions. Prog. Neuro. Psychopharmacol. Biol. Psychiatry (1995) 19:171–186.
   PubMed Web of Science ®Google Scholar
• OHHARA T, TANAKA K, FUKUYA H eta].: Effects of SDZ ENA 713 on spatial memory impairment in basal forebrain-lesioned rats. Jpn. J. Pharmacol. (1994) 64 (Supp1.1). Abstract–652.
   Google Scholar
• TANAKA K, OGAWA N, ASANUMA M et al.: Chronic administration of acetycholinesterase inhibitor in the sensescent rat brain. Neurobiol. Aging (1994)15:721–725.
   PubMed Web of Science ®Google Scholar
• HOLSBOER-TRACHSLER E, HATZINGER M, STOHLER R et al.: Effects of novel acetylcholinesterase inhibitor SDZ ENA 713 on sleep in man. Neuropsychopharmacol (1993) 8:87–92.
   PubMed Web of Science ®Google Scholar
• AGID Y, DUBOIS B ANAND R et al.: Efficacy and tolerability of rivastigmine in pateints with dementia of the Alzheimer type. Curr. Ther. Res. (1998) 59:837–845.
   Google Scholar
• •Early clinical study suggesting 3 mg b.i.d. of oral rivastig-mine is relatively well-tolerated and efficacious.
   Google Scholar
• SRAMEK JJ, ANAND R, WARDLE TS et al.: Safety/tolerabilitiy trial of SDZ ENA 713 in patients with probable Alzheimer's disease. Life Sci. (1996) 58:1201–1207.
   PubMed Web of Science ®Google Scholar
• •Compares tolerability of twice versus three times daily dosing of rivastigmine 12 mg/day.
   Google Scholar
• COREY-BLOOM J, ANAND R, VEACH J et al.: A random- ized 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. GeriaL Pharmacol. (1998) 1:55–65.
   Google Scholar
• •United States study of the safety and efficacy of high and low-dose rivastigmine compared to placebo in patients with mild to moderate Alzheimer's disease.
   Google Scholar
• ROSLER M, ANAND R, CICIN-SAIN A, FOR THE EXELON STUDY GROUP. Efficacy and safety of rivastigmine in patients with Alzheimer's disease: International randomised controlled trial. BM./ (1999) 318:633–640.
   Google Scholar
• ••Multinational study of the safety and efficacy of high andlow-dose rivastigmine compared to placebo in patients with mild to moderate Alzheimer's disease.
   Google Scholar
• ANAND R, GHARABAWI G: Clinical development of Exelon® (ENA-713): The Adena® Programme. J. Drug Dev. Clin. PracL (1996) 8:117–122.
   Google Scholar
• •Methodology paper and outline of the large-scale clinical investigation of rivastigmine in human subjects.
   Google Scholar
• CUTLER NR, ANAND R, HARTMAN RD et al.: Antiemetic therapy for Alzheimer's patients receiving the cholin-esterase inhibitor SDZ ENA 713. Clin. Pharm. Ther. (1998):188. Abstract.
   Google Scholar