Use of rivastigmine transdermal patch in the treatment of Alzheimer's disease

Authors: Winblad, Bengt; Machado, João Carlos

Source: Expert Opinion on Drug Delivery, Volume 5, Number 12, December 2008 , pp. 1377-1386(10)

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Abstract:

Cholinesterase inhibitors such as rivastigmine and donepezil exhibit a dose - response relationship, with higher doses of the drugs demonstrating greater efficacy. Transdermal patches provide smooth continuous drug delivery, with the potential to offer efficacious levels of drug exposure while avoiding the peaks and troughs associated with side effects. As a small, lipophilic and hydrophilic molecule, rivastigmine (C₁₄H₂₂N₂O₂) is chemically well-suited to transdermal delivery. The technology underlying the rivastigmine patch allows it to be discreetly small and thin. The target dose 9.5 mg/24 h rivastigmine patch has a diameter of just 3.5 cm and a surface area of 10 cm². A large randomized controlled trial has demonstrated that the target dose 9.5 mg/24 h rivastigmine patch provided similar efficacy to the highest rivastigmine capsule doses, yet with three times fewer reports of nausea and vomiting. Thus, the rivastigmine patch enables quick and easy access to high dose efficacy. The skin tolerability profile is good, and the patch has demonstrated excellent adhesion. 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.

Document Type: Research article

DOI: http://dx.doi.org/10.1517/17425240802542690

Publication date: 2008-12-01

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