Pharmacokinetic rationale for the rivastigmine patch

@article{Cummings2007PharmacokineticRF,
  title={Pharmacokinetic rationale for the rivastigmine patch},
  author={Jeffrey L. Cummings and Gilbert Y. Lef{\`e}vre and Gary W. Small and Silke Appel-Dingemanse},
  journal={Neurology},
  year={2007},
  volume={69},
  pages={S10 - S13}
}
The dual cholinesterase inhibitor rivastigmine is approved in capsule form in many countries for the symptomatic treatment of dementia associated with Alzheimer disease (AD) and Parkinson disease (PD). All orally administered cholinesterase inhibitors are associated with central cholinergic gastrointestinal side effects, particularly during the titration phase, which are believed to be caused by a rapid increase in brain acetylcholine levels after effective inhibition of the target enzymes. A… 
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The apparent success of rivastigmine patch, in terms of clinical utility and patient acceptability, suggests that it may mark the next generation of dementia treatment.
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Rivastigmine patches have a tolerability profile similar to that shown by capsules, but are associated with greater patient satisfaction, and therefore need to be considered for optimal dose titration.
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The clinical and pharmacokinetic data that supported the development of the rivastigmine patch are reviewed, and the ways in which the use of a transdermal patch may improve the management of dementia patients in a real-life setting are discussed.
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Rivastigmine is well suited to patch administration because it is a small, potent molecule that is both lipophilic and hydrophilic and may provide a promising new approach to dementia therapy.
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TLDR
Donepezil, rivastigmine and galantamine are the three ChEIs FDA-approved as first-line treatment for AD and the goal for the future would be to optimize the patch formulation to increase both efficacy and safety.
Rivastigmine transdermal system for the treatment of mild to moderate Alzheimer’s disease
TLDR
The aim of this review was to provide a concise, comprehensive overview of the clinically relevant safety, tolerability and efficacy information available for the rivastigmine transdermal system, which provides a viable treatment option for patients with mild to moderate AD.
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