title: Rivastigmine from capsules to patch: therapeutic advances in the management of Alzheimer's disease and Parkinson's disease dementia.
abstract: OBJECTIVE
  To discuss the pharmacology, mechanism of action, and chemical properties of the cholinesterase inhibitor (ChEI) rivastigmine; to provide a rationale for transdermal delivery and supportive clinical data, along with practical guidance on rivastigmine patch use in Alzheimer's disease and Parkinson's disease dementia.
  
  
  METHODS
  Pivotal studies of rivastigmine capsules and patch were identified using PubMed and the rivastigmine US prescribing information. PubMed searches were performed in 2013 using rivastigmine as a keyword.
  
  
  METHODS
  English-language articles related to rivastigmine considered of relevance to primary care physicians were included.
  
  
  RESULTS
  Pharmacologic differences exist between rivastigmine and ChEIs. Clinical studies demonstrate symptomatic efficacy of oral rivastigmine across all stages of Alzheimer's disease and mild-to-moderate Parkinson's disease dementia. However, gastrointestinal adverse events limit access to optimal therapeutic doses. Strategies that lower maximum plasma concentrations (Cmax) and prolong time to Cmax, ie, transdermal delivery, may improve tolerability. Clinical registration studies have demonstrated improved tolerability of rivastigmine 9.5-mg/24-h patch versus 6-mg twice-daily capsules in mild-to-moderate Alzheimer's disease, and a positive benefit-risk profile of 13.3-mg/24-h versus 9.5-mg/24-h patch in patients needing enhanced efficacy. Clinical data comparing 13.3-mg/24-h versus 4.6-mg/24-h patch in severe Alzheimer's disease demonstrated efficacy on cognition and activities of daily living. These data led to approval of rivastigmine patch in severe Alzheimer's disease. Transdermal delivery also has practical advantages, including simple, once-daily administration and a visual indicator of compliance. Potential application site reactions can be minimized and need not be a barrier to treatment.
  
  
  CONCLUSIONS
  In addition to practical advantages, rivastigmine patch may improve clinical outcomes throughout the course of Alzheimer's disease by providing access to high-dose efficacy without compromising tolerability.
authors: Division of Neurology, Nova Southeastern University, Fort Lauderdale, and Premiere Research Institute, Palm Beach Neurology, West Palm Beach, Florida (Dr Sadowsky); Private Practice, Marietta, Georgia (Dr Micca); Department of Neurology and Psychiatry, St Louis University School of Medicine, St Louis, Missouri (Dr Grossberg); and Novartis Pharmaceuticals Corporation, East Hanover, New Jersey (Dr Velting).
authors: Carl H
authors: CH
authors: Sadowsky
authors: Division of Neurology, Nova Southeastern University, Fort Lauderdale, and Premiere Research Institute, Palm Beach Neurology, West Palm Beach, Florida (Dr Sadowsky); Private Practice, Marietta, Georgia (Dr Micca); Department of Neurology and Psychiatry, St Louis University School of Medicine, St Louis, Missouri (Dr Grossberg); and Novartis Pharmaceuticals Corporation, East Hanover, New Jersey (Dr Velting).
authors: Joseph L
authors: JL
authors: Micca
authors: Division of Neurology, Nova Southeastern University, Fort Lauderdale, and Premiere Research Institute, Palm Beach Neurology, West Palm Beach, Florida (Dr Sadowsky); Private Practice, Marietta, Georgia (Dr Micca); Department of Neurology and Psychiatry, St Louis University School of Medicine, St Louis, Missouri (Dr Grossberg); and Novartis Pharmaceuticals Corporation, East Hanover, New Jersey (Dr Velting).
authors: George T
authors: GT
authors: Grossberg
authors: Division of Neurology, Nova Southeastern University, Fort Lauderdale, and Premiere Research Institute, Palm Beach Neurology, West Palm Beach, Florida (Dr Sadowsky); Private Practice, Marietta, Georgia (Dr Micca); Department of Neurology and Psychiatry, St Louis University School of Medicine, St Louis, Missouri (Dr Grossberg); and Novartis Pharmaceuticals Corporation, East Hanover, New Jersey (Dr Velting).
authors: Drew M
authors: DM
authors: Velting