Galantamine: a review of its use in Alzheimer's disease.
Scott LJ, Goa KL
Adis International Limited, Auckland, New Zealand. demail@adis.co.nz
Drugs 2000 Nov;60(5):1095-122
Abstract
Currently, acetylcholinesterase (AChE) inhibitors are the most promising class
of drugs for the treatment of Alzheimer's disease (AD). Galantamine is a
reversible, competitive, tertiary alkaloid AChE inhibitor. The drug is selective
for AChE rather than butyrylcholinesterase. In addition to inhibition of AChE
galantamine interacts allosterically with nicotinic acetylcholine 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 living in these patients and
significantly reduced the requirement for caregiver assistance with activities
of daily living. Moreover, galantamine recipients achieved significantly better
outcomes on behavioural symptoms than placebo recipients. In a long term study
(12 months), galantamine 24 mg/day slowed the progression of symptoms of the
disease and maintained cognitive function and activities of daily living in
patients with mild to moderate AD. Galantamine was generally well
tolerated with the majority of adverse events being mild to moderate in
intensity and transient. Predictably, adverse events were cholinergic in
nature and generally related to the gastrointestinal system. These effects were
reduced in patients receiving the recommended dose escalation regimen.
Galantamine had no clinically relevant effects on vital signs, haematological or
biochemical laboratory parameters and, importantly, there were no reports of
hepatotoxicity. The incidence of serious adverse events was similar between
galantamine (8 to 32 mg/day) and placebo groups (6 to 16% of patients across all
treatment groups).
CONCLUSIONS: Galantamine is an
effective well tolerated symptomatic treatment for Alzheimer's which
improves cognition, function and activities of daily living in the short term
(up to 6 months) in patients with mild to moderate AD. In addition, it delays
the development of behavioural disturbances and psychiatric symptoms, and
reduces caregiver burden (as measured by caregiver time). In the long term
(up to 1 year), galantamine maintains cognition and activities of daily
living. Adverse events associated with galantamine are mainly cholinergic,
usually mild to moderate in intensity and transient. Galantamine has been
evaluated in several large well-designed studies and, given the relative lack of
established treatment options, it may be considered as one of the first-line
pharmacological treatments in patients with mild to moderate Alzheimer's.
BACK
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order
Research
abstracts
Galantamine:
its use in Alzheimer's
Galantamine: in Alzheimer's
patients
Galantamine: acetylcholinesterase
inhibition
Galantamine: therapeutic
effects beyond cognition
Galantamine: benefits to
Alzheimer's patients
Galantamine:
modulation of nicotinic receptors in
Alzheimer's
Galantamine: a study in
Alzheimer's
Galantamine: its
effects on Alzheimer's
Galantamine: a new treatment
for Alzheimer's
Galantamine:
effect on nicotinic receptor binding
Galantamine: an allosterically
potentiating ligant
Galantamine: nicotinic
modulation in older rabbits
Galantamine: effect on memory
& nicotinic receptors in rats
Galantamine: a 6 month study