Estimation of the Absolute Bioavailability of Rivastigmine in Patients with Mild to Moderate Dementia of the Alzheimer???s Type

Hossain, Mohammad; Jhee, Stanford; Shiovitz, Thomas; McDonald, Craig; Sêdek, G; Pommier, F.; Cutler, Neal R.

doi:10.2165/00003088-200241030-00006

Cited by 51 publications

(39 citation statements)

References 20 publications

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“…Our findings following patch application similarly showed nonlinear pharmacokinetics consistent with the observation that bioavailability of rivastigmine increases with rising doses and confirmed earlier findings with the patch 12 . This novel rivastigmine patch formulation demonstrated a much flatter rivastigmine concentration‐time profile compared with the capsule formulation 21 . The fluctuation between maximum (C max ) and minimum (C min ) concentrations, as expressed by the ratio C max /C min , was markedly lower with the patch (around 1.6–2.0 in white and 1.5–1.6 in Japanese participants) than that previously observed with the oral capsule formulation (ratio = 55) 21 .…”

Section: Discussionsupporting

confidence: 89%

Similar Rivastigmine Pharmacokinetics and Pharmacodynamics in Japanese and White Healthy Participants Following the Application of Novel Rivastigmine Patch

Lefèvre

Büche

Sêdek

et al. 2009

The Journal of Clinical Pharma

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The pharmacokinetics and pharmacodynamics of rivastigmine were compared in Japanese and white healthy participants who were given ascending single doses of the novel rivastigmine transdermal patch. Rivastigmine patch strengths were 4.6 mg/24 h (5 cm2, 9 mg rivastigmine loaded dose), 9.5 mg/24 h (10 cm2, 18 mg), and 13.3 mg/24 h (15 cm2, 27 mg) (per label) or 7.0 mg/24 h (7.5 cm2, 13.5 mg) as a fall-back dose. No relevant ethnic differences in the noncompartmental pharmacokinetics (parent and metabolite NAP226-90) and pharmacodynamics (plasma BuChE activity) of the rivastigmine patch were observed between Japanese and whites. However, drug exposure was slightly higher and inhibition of BuChE slightly more pronounced in Japanese participants than in whites, which was attributed to the lower body weight (ca. 11% less on average) of Japanese participants. Treatments were similarly well tolerated in both ethnic groups. In conclusion, no relevant ethnic differences in the intrinsic disposition or effects of rivastigmine delivered via transdermal route are expected between Japanese and white patients. The possible effect of body weight on drug exposure suggests that special attention should be paid to patients with very low body weight during up-titration.

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Section: Discussionsupporting

confidence: 89%

Similar Rivastigmine Pharmacokinetics and Pharmacodynamics in Japanese and White Healthy Participants Following the Application of Novel Rivastigmine Patch

Lefèvre

Büche

Sêdek

et al. 2009

The Journal of Clinical Pharma

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“…Thus, maximum plasma drug concentration (C max ) and area under the concentration-time curve (AUC) increase more than proportionally with an increasing dose, whereas they are low at low dose [2]. Also rivastigmine has a short plasma half-life, so a sensitive bioanalytical method, which can quantify rivastigmine at sub-nanogram level, is required for the determination of pharmacokinetic parameters of rivastigmine.…”

Section: Introductionmentioning

confidence: 99%

“…The techniques used in these methods include LC-MS/MS [1,3] and GC-MS detection [2,[4][5][6]. Although these assays are sufficiently sensitive, these methods require laborious extraction procedures like liquid-liquid extraction or solid-phase microextraction involving time-consuming and error-prone solvent evaporation and reconstitution steps and long run time.…”

Section: Introductionmentioning

confidence: 99%

A rapid and sensitive liquid chromatography–tandem mass spectrometry (LC–MS/MS) method for the estimation of rivastigmine in human plasma

Bhatt

Subbaiah

Kambli

et al. 2007

Journal of Chromatography B

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“…Also, MRS measurements have been shown to be a predictor of cognitive scores at follow-up in AD, but not in vascular dementia (Wahlund et al 2000). Furthermore, few controlled studies have used MRS to monitor treatment effects of muscarinic agonists and AchE inhibitors, demonstrating N -acetylaspartate measured by MRS combined with hippocampal volumetry, to provide a highly useful surrogate marker of AD progression in trials of neuroprotective agents (Hossain et al 2002; Krishnan et al 2003). …”

Section: The State-of-the-art-imagingmentioning

confidence: 99%

Strategies for molecular imaging dementia and neurodegenerative diseases

Schaller¹

2008

NDT

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Dementia represents a heterogeneous term that has evolved to describe the behavioral syndromes associated with a variety of clinical and neuropathological changes during continuing degenerative disease of the brain. As such, there lacks a clear consensus regarding the neuropsychological and other constituent characteristics associated with various cerebrovascular changes in this disease process. But increasing this knowledge has given more insights into memory deterioration in patients suffering from Alzheimer's disease and other subtypes of dementia. The author reviews current knowledge of the physiological coupling between cerebral blood fl ow and metabolism in the light of state-of-the-art-imaging methods and its changes in dementia with special reference to Alzheimer's disease. Different imaging techniques are discussed with respect to their visualizing effect of biochemical, cellular, and/or structural changes in dementia. The pathophysiology of dementia in advanced age is becoming increasingly understood by revealing the underlying basis of neuropsychological changes with current imaging techniques, genetic and pathological features, which suggests that alterations of (neuro)vascular regulatory mechanisms may lead to brain dysfunction and disease. The current view is that cerebrovascular deregulation is seen as a contributor to cerebrovascular pathologies, such as stroke, but also to neurodegenerative conditions, such as Alzheimer's disease. The better understanding of these (patho)physiological mechanisms may open an approach to new interventional strategies in dementia to enhance neurovascular repair and to protect neurovascular coupling.

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Estimation of the Absolute Bioavailability of Rivastigmine in Patients with Mild to Moderate Dementia of the Alzheimer???s Type

Cited by 51 publications

References 20 publications

Similar Rivastigmine Pharmacokinetics and Pharmacodynamics in Japanese and White Healthy Participants Following the Application of Novel Rivastigmine Patch

Similar Rivastigmine Pharmacokinetics and Pharmacodynamics in Japanese and White Healthy Participants Following the Application of Novel Rivastigmine Patch

A rapid and sensitive liquid chromatography–tandem mass spectrometry (LC–MS/MS) method for the estimation of rivastigmine in human plasma

Strategies for molecular imaging dementia and neurodegenerative diseases

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