An update on the pharmacology of galantamine.
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.
Villarroya
Mercedes
M
Universidad Autónoma de Madrid, Instituto Teófilo Hernando and Departamento de Farmacología, Facultad de Medicina, C/Arzobispo Morcillo, 4; 28029-Madrid, Spain. mercedes.villarroya@uam.es
García
Antonio G
AG
Marco-Contelles
José
J
López
Manuela G
MG
D000110:Acetylcholinesterase / Q000378:metabolism; D000544:Alzheimer Disease / Q000188:drug therapy / Q000201:enzymology; D000818:Animals; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D005702:Galantamine / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D018696:Neuroprotective Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D018697:Nootropic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use
D002800:Cholinesterase Inhibitors; D018696:Neuroprotective Agents; D018697:Nootropic Agents; D005702:Galantamine; D000110:Acetylcholinesterase