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Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review.

Kurz A, Farlow M, Lefèvre G - Int. J. Clin. Pract. (2009)

Bottom Line: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h).The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability.This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.

View Article: PubMed Central - PubMed

Affiliation: Department of Psychiatry and Psychotherapy, Technische Universität München, Munich, Germany. alexander.kurz@lrz.tumuenchen.de

ABSTRACT

Background: Cholinesterase inhibitors have all been available in oral formulations, but a rivastigmine transdermal patch has now been developed and is approved in many countries worldwide for the treatment of mild-to-moderate Alzheimer's disease (AD) (including the USA, Latin America, Europe and Asia).

Objectives: To review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in dementia therapy. This article will also discuss how the patch may alter the treatment paradigm for patients with AD.

Results: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h). In a clinical trial of 1195 AD patients, this translated into similar efficacy with three times fewer reports of nausea and vomiting (7.2% vs. 23.1%, and 6.2% vs. 17.0% respectively). Consequently, more patients in the 9.5 mg/24 h patch group achieved their target therapeutic dose at the end of the study, compared with those in the 12 mg/day capsule group (95.9% vs. 64.4%).

Conclusion: The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability. This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.

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Related in: MedlinePlus

Steady-state rivastigmine plasma levels for a typical patient following administration of the 9.5 mg/24 h rivastigmine patch vs. 6 mg bid capsules, and the 4.6 mg/24 h rivastigmine patch vs. 3 mg bid capsules. The model adjusts for body weight and gender (15)
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fig01: Steady-state rivastigmine plasma levels for a typical patient following administration of the 9.5 mg/24 h rivastigmine patch vs. 6 mg bid capsules, and the 4.6 mg/24 h rivastigmine patch vs. 3 mg bid capsules. The model adjusts for body weight and gender (15)

Mentions: The results from an open-label study of 51 AD patients randomised to rivastigmine patch (4.6–17.4 mg/24 h; 5–20 cm2), or capsules (3–12 mg/day), were used in a compartmental analysis to model rivastigmine plasma levels over a 24-h application period (Figure 1). Drug exposure was assessed by measuring the area under the curve over a 24-h treatment period (AUC24 h), using a specific power model (14).


Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review.

Kurz A, Farlow M, Lefèvre G - Int. J. Clin. Pract. (2009)

Steady-state rivastigmine plasma levels for a typical patient following administration of the 9.5 mg/24 h rivastigmine patch vs. 6 mg bid capsules, and the 4.6 mg/24 h rivastigmine patch vs. 3 mg bid capsules. The model adjusts for body weight and gender (15)
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC2734925&req=5

fig01: Steady-state rivastigmine plasma levels for a typical patient following administration of the 9.5 mg/24 h rivastigmine patch vs. 6 mg bid capsules, and the 4.6 mg/24 h rivastigmine patch vs. 3 mg bid capsules. The model adjusts for body weight and gender (15)
Mentions: The results from an open-label study of 51 AD patients randomised to rivastigmine patch (4.6–17.4 mg/24 h; 5–20 cm2), or capsules (3–12 mg/day), were used in a compartmental analysis to model rivastigmine plasma levels over a 24-h application period (Figure 1). Drug exposure was assessed by measuring the area under the curve over a 24-h treatment period (AUC24 h), using a specific power model (14).

Bottom Line: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h).The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability.This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.

View Article: PubMed Central - PubMed

Affiliation: Department of Psychiatry and Psychotherapy, Technische Universität München, Munich, Germany. alexander.kurz@lrz.tumuenchen.de

ABSTRACT

Background: Cholinesterase inhibitors have all been available in oral formulations, but a rivastigmine transdermal patch has now been developed and is approved in many countries worldwide for the treatment of mild-to-moderate Alzheimer's disease (AD) (including the USA, Latin America, Europe and Asia).

Objectives: To review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in dementia therapy. This article will also discuss how the patch may alter the treatment paradigm for patients with AD.

Results: The 9.5 mg/24 h rivastigmine patch was shown to provide comparable exposure to the highest recommended doses of capsules (12 mg/day) with significantly lower maximum plasma concentration (Cmax 8.7 vs. 21.6 ng/ml) and slower absorption rate (tmax 8.1 vs. 1.4 h). In a clinical trial of 1195 AD patients, this translated into similar efficacy with three times fewer reports of nausea and vomiting (7.2% vs. 23.1%, and 6.2% vs. 17.0% respectively). Consequently, more patients in the 9.5 mg/24 h patch group achieved their target therapeutic dose at the end of the study, compared with those in the 12 mg/day capsule group (95.9% vs. 64.4%).

Conclusion: The rivastigmine patch provides continuous drug delivery over 24 h and similar efficacy to the highest recommended dose of oral rivastigmine with improved tolerability. This may allow patients to achieve optimal therapeutic doses and to benefit from a longer duration of treatment.

Show MeSH
Related in: MedlinePlus