An update on the pharmacology of galantamine

被引:66
作者
Villarroya, Mercedes [1 ,2 ]
Garcia, Antonio G. [1 ,2 ,3 ,4 ]
Marco-Contelles, Jose [5 ]
Lopez, Manuela G. [1 ,2 ]
机构
[1] Univ Autonoma Madrid, Inst Teofilo Hernando, Madrid 28029, Spain
[2] Univ Autonoma Madrid, Dept Farmacol, Fac Med, Madrid 28029, Spain
[3] Hosp Univ Princesa, Serv Farmacol Clin, Madrid 28006, Spain
[4] Hosp Univ Princesa, Inst Gerontol, Madrid 28006, Spain
[5] CSIC, Lab Radicales Libres, Madrid 28006, Spain
关键词
acetylcholinesterase; Alzheimer's disease; galantamine; pharmacology;
D O I
10.1517/13543784.16.12.1987
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Alzheimer's disease (AD) is associated with a gradual loss of attention and memory that has been related to impairment of brain cholinergic neurotransmission, particularly a deficit of cholinergic neurons. The first therapeutic target that has demonstrated therapeutic efficacy on cognition, behaviour and functional daily activities has been the inhibition of acetylcholinesterase. The acetylcholinesterase inhibitors used to treat AD patients at present are donepezil, rivastigmine and galantamine. This review summarises the current state of the art concerning the pharmacology of galantamine, focusing on the most important details of its possibilities as an acetylcholinesterase inhibitor, an allosteric potentiator of neuronal nicotinic receptors for acetylcholine, a modulator of neurotransmitter release, and an agent causing neuroprotection through an antiapoptotic action. In so doing, galantamine will be discussed in the context of the treatment of dementia, both of AD type and of mixed vascular-Alzheimer type.
引用
收藏
页码:1987 / 1998
页数:12
相关论文
共 104 条
[1]   Galantamine prevents apoptosis induced by β-amyloid and thapsigargin:: involvement of nicotinic acetylcholine receptors [J].
Arias, E ;
Alés, E ;
Gabilan, NH ;
Cano-Abad, MF ;
Villarroya, M ;
García, AG ;
López, MG .
NEUROPHARMACOLOGY, 2004, 46 (01) :103-114
[2]   Unequal neuroprotection afforded by the acetylcholinesterase inhibitors galantamine, donepezil, and rivastigmine in SH-SY5Y neuroblastoma cells:: Role of nicotinic receptors [J].
Arias, E ;
Gallego-Sandín, S ;
Villarroya, M ;
García, AG ;
López, MG .
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2005, 315 (03) :1346-1353
[3]   STUDIES ON NEW, CENTRALLY ACTIVE AND REVERSIBLE ACETYLCHOLINESTERASE INHIBITORS [J].
ARNAL, F ;
COTE, LJ ;
GINSBURG, S ;
LAWRENCE, GD ;
NAINI, A ;
SANO, M .
NEUROCHEMICAL RESEARCH, 1990, 15 (06) :587-591
[4]   THE CHOLINERGIC HYPOTHESIS OF GERIATRIC MEMORY DYSFUNCTION [J].
BARTUS, RT ;
DEAN, RL ;
BEER, B ;
LIPPA, AS .
SCIENCE, 1982, 217 (4558) :408-417
[5]   Central nicotinic receptors, neurotrophic factors and neuroprotection [J].
Belluardo, N ;
Mudò, G ;
Blum, M ;
Fuxe, K .
BEHAVIOURAL BRAIN RESEARCH, 2000, 113 (1-2) :21-34
[6]   Galantamine provides sustained benefits in patients with 'advanced moderate' Alzheimer's disease for at least 12 months [J].
Blesa, R ;
Davidson, M ;
Kurz, A ;
Reichman, W ;
van Baelen, B ;
Schwalen, S .
DEMENTIA AND GERIATRIC COGNITIVE DISORDERS, 2003, 15 (02) :79-87
[7]  
Bodick N, 1997, ALZ DIS ASSOC DIS, V11, P50
[8]  
Bores Gina M., 1996, Drugs of the Future, V21, P621
[9]  
Bores GM, 1996, J PHARMACOL EXP THER, V277, P728
[10]  
Buccafusco JJ, 2000, J PHARMACOL EXP THER, V295, P438