Pharmacokinetic rationale for switching from donepezil to galantamine.

Maelicke, A

Laboratory of Molecular Neurobiology
Johannes-Gutenberg University Medical School
 Mainz, Germany. alfred.maelicke@uni-mainz.de

Clin Ther 2001;23 Suppl A:A8-12 

ABSTRACT

Galantamine, the most recently approved acetylcholinesterase inhibitor (AChEI) for use in the United States, has allosteric modulating activity at nicotinic receptors and inhibits acetylcholinesterase.  This dual mechanism of action may make galantamine an attractive option for patients with Alzheimer's disease who have not benefited from their current therapy; thus, methods for switching patients from donepezil or rivastigmine to galantamine are needed.  Protocols for switching patients from one AChEI to another must consider both the time required for washout of the first drug and the rate of dose escalation of the second drug.  Both issues depend on the pharmacodynamics, pharmacokinetics, and pharmacology of the drugs under consideration.  Because the common property of the drugs considered here is their acetylcholinesterase inhibitory activity, it seems reasonable to keep this activity at or below the activity achieved by the first drug at all times.  In addition, the patient's condition should be monitored to avoid deterioration resulting from subtherapeutic drug concentrations during the switch.  The switching protocol proposed here has been based on an analysis of mean plasma concentrations of donepezil following administration of a single dose and on the established pharmacokinetics of galantamine.

BACK                                           to 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:
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 ligand
  Galantamine: nicotinic modulation in an animal model
  Galantamine: memory & nicotinic receptors in rats  
  Galantamine: a 6 month study:

www.AlzheimersTreatments.com
Smart Nutrition
1765 Garnet Ave # 66
San Diego, CA 92109
smart@smart-nutrition.net