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Clinical Pharmacokinetics

, Volume 42, Issue 15, pp 1383–1392 | Cite as

Clinical Pharmacokinetics of Galantamine

  • Martin R. FarlowEmail author
Review Article

Abstract

Galantamine is the most recently approved cholinergic drug for the treatment of Alzheimers’s disease, the most common type of dementia. Vascular dementia and Alzheimers’s disease with cerebrovascular disease are also common in older patients. Dementia affects cognition, causes losses in ability to perform activities of daily living and often results in the emergence of psychiatric and abnormal behavioural symptoms. Dementia also results in an ever-increasing burden and a decreased quality of life for caregivers. Treatments for dementia, particularly Alzheimers’s disease, have focused on improving function in the cholinergic system. Vascular dementia and diffuse Lewy body dementia are also associated with significant defects in cholinergic function.

Galantamine works by inhibiting acetylcholinesterase and by allosterically modulating nicotinic receptors. In clinical trials, galantamine has shown benefits in the domains of cognition, function in activities of daily living, and behaviour.

Galantamine is about 90% bioavailable and displays linear pharmacokinetics. It has a relatively large volume of distribution and low protein binding. Metabolism is primarily through the cytochrome P450 system, specifically the CYP2D6 and CYP3A4 isoenzymes. Population pharmacokinetic modelling with galantamine has shown that the variables affecting clearance are age, sex, and bodyweight. Model simulations demonstrate the importance of a slower dose-escalation schedule in patients with moderate hepatic impairment.

In several large trials, galantamine has been shown to be well tolerated, with most adverse events being mild-to-moderate and gastrointestinal in nature. Based on the literature and clinical trial experience, galantamine appears to be an excellent treatment option for patients with Alzheimers’s disease, vascular dementia or Alzheimers’s disease with cerebrovascular disease.

Keywords

Vascular Dementia Nicotinic Receptor Rivastigmine Galantamine Extensive Metabolisers 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Notes

Acknowledgements

Dr Farlow has received grants, honoraria, and consultation fees from Janssen Pharmaceutical Products, LP. The author has provided no information on conflicts of interest directly relevant to the content of this review.

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Copyright information

© Adis Data Information BV 2003

Authors and Affiliations

  1. 1.Department of NeurologyIndiana University School of MedicineIndianapolis, CL299USA

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