Galantamine - A review of its use in Alzheimer's disease

Currently, acetylcholinesterase (AChE) inhibitors are the most promising cl ass of drugs for the treatment of Alzheimer's disease (AD). Galantamine is a reversible, competitive, tertiary alkaloid AChE inhibitor. The drug is se lective for AChE rather than butyrylcholinesterase. In addition to inhibiti on of AChE galantamine interacts allosterically with nicotinic acetylcholin e receptors to potentiate the action of agonists at these receptors. Recipients of galantamine 16 or 24 mg/day achieved significant improvements in cognitive and global symptoms relative to placebo recipients in large ( n = 285 to 978 patients with mild to moderate AD) well-designed trials of 3 to 6 months' duration. Galantamine also improved activities of daily livin g in these patients and significantly reduced the requirement for caregiver assistance with activities of daily living. Moreover, galantamine recipien ts achieved significantly better outcomes on behavioural symptoms than plac ebo recipients. In a long term study (12 months), galantamine 24 mg/day slowed the progress ion of symptoms of the disease and maintained cognitive function and activi ties of daily living in patients with mild to moderate AD. Galantamine was generally well tolerated with the majority of adverse event s being mild to moderate in intensity and transient. Predictably, adverse e vents were cholinergic in nature and generally related to the gastrointesti nal system. These effects were reduced in patients receiving the recommende d dose escalation regimen. Galantamine had no clinically relevant effects o n vital signs, haematological or biochemical laboratory parameters and, imp ortantly, there were no reports of hepatotoxicity. The incidence of serious adverse events was similar between galantamine (8 to 32 mg/day) and placeb o groups (6 to 16% of patients across all treatment groups). Conclusions: Galantamine is an effective well tolerated symptomatic treatme nt for AD which improves cognition, function and activities of daily living in the short term (up to 6 months) in patients with mild to moderate AD. I n addition, it delays the development of behavioural disturbances and psych iatric symptoms, and reduces caregiver burden (as measured by caregiver tim e). In the long term (up to 1 year), galantamine maintains cognition and ac tivities of daily living. Adverse events associated with galantamine are ma inly cholinergic, usually mild to moderate in intensity and transient. Gala ntamine has been evaluated in several large well-designed studies and, give n the relative lock of established treatment options, it may be considered as one of the first-line pharmacological treatments in patients with mild t o moderate AD.