Investigation of the impact of sarizotan on the pharmacokinetics of levodopa

Krösser, Sonja; Neugebauer, Roland; Chassard, D; Kovar, Andreas

doi:10.1002/bdd.558

Cited by 8 publications

(5 citation statements)

References 18 publications

(30 reference statements)

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“…After the administration of 100 mg levodopa combined with a dopa decarboxylase inhibitor, the values obtained for C max were next to 1000 ng/ml [16–18]. In our study, in the initial situation of patients, the data ranged from 343.1 to 1433.9 ng/ml, so, in some patients the values were similar to that found by other authors and in others it was lower.…”

Section: Discussionsupporting

confidence: 88%

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A randomised clinical trial to evaluate the effects of Plantago ovata husk in Parkinson patients: changes in levodopa pharmacokinetics and biochemical parameters

Fernández

Hernandez-Echevarria

Sierra

et al. 2014

BMC Complement Altern Med

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BackgroundPlantago ovata husk therapy could be used in patients with Parkinson disease to reduce the symptoms of gastrointestinal disorders, but it is important to know whether this compound modifies levodopa pharmacokinetics. The maintenance of constant plasma concentrations of levodopa abolishes the clinical fluctuations in parkinsonian patients. The aim of this randomised clinical trial was to establish the influence of the fiber Plantago ovata husk in the pharmacokinetics of levodopa when administered to Parkinson patients well controlled by their oral medication.MethodsTo evaluate the effects of this fiber on several biochemical parameters. 18 volunteers participated in the study and received alternatively two treatments (Plantago ovata husk or placebo) with their usual levodopa/carbidopa oral dose. On days 0 (initial situation), 14 and 35 of the study, blood samples were taken to assess levodopa pharmacokinetics and to determine biochemical parameters.ResultsLevodopa Cmax was very similar in the initial situation (603.2 ng/ml) and after placebo administration (612.0 ng/ml), being slightly lower (547.8 ng/ml) when Plantago ovata husk was given. AUC was very similar in the three groups: initial situation.- 62.87 μg.min/ml, fiber treatment.- 64.47 μg.min/ml and placebo treatment.- 65.10 μg.min/ml. Fiber reduced significantly the number of peaks observed in the levodopa concentrations, maintaining concentrations more stable. No significant differences were found in total cholesterol, LDL-cholesterol and triglycerides with the administration of Plantago ovata husk.ConclusionsPlantago ovata husk administration caused a smoothing and homogenization of levodopa absorption, providing more stable concentrations and final higher levels, resulting in a great benefit for patients.Trial registrationEudraCT2006-000491-33

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Section: Discussionsupporting

confidence: 88%

“…This parameter ranged from 20 to 90 minutes as in other studies [10, 17, 19]. However, the mean AUC value (62.87 μg.min/ml) was slightly lower than that found by other authors using the same dose of levodopa: 98.9 μg.min/ml [16], 99.7 μg.min/ml [18], 117.0 μg.min/ml [17]. …”

Section: Discussionmentioning

confidence: 50%

A randomised clinical trial to evaluate the effects of Plantago ovata husk in Parkinson patients: changes in levodopa pharmacokinetics and biochemical parameters

Fernández

Hernandez-Echevarria

Sierra

et al. 2014

BMC Complement Altern Med

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“…Recently, it has been demonstrated that sarizotan has no effect on the pharmacokinetics of levodopa (Krösser et al 2007). It has been suggested that the antidyskinetic properties of sarizotan could be mediated via its 5-HT 1A agonist action in the motor cortex, reducing the activity of the corticostriatal glutamate pathway (Antonelli et al 2005).…”

Section: Discussionmentioning

confidence: 99%

Local administration of sarizotan into the subthalamic nucleus attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats

et al. 2009

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“…The 5-HT 1A receptor agonist tandospirone reduced dyskinesia in L-DOPA-treated PD patients [193]. More recently, preclinical and clinical studies suggest that sarizotan, a 5-HT 1A receptor agonist that possesses weak D 3 and D 4 receptor agonist activity, could ameliorate dyskinetic symptoms in association with L-DOPA [194,195].…”

Section: -Ht 1a Receptor Agonists In Pdmentioning

confidence: 99%

Partial Dopamine D2/Serotonin 5-HT1A Receptor Agonists as New Therapeutic Agents~!2009-12-17~!2010-04-07~!2010-07-20~!

Etiévant¹

2010

TONEUROPPJ

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Abstract:The therapeutic efficacy of current antipsychotic or antidepressant agents still present important drawbacks such as delayed onset of action and a high percentage of non-responders. Despite significant advancements in the development of new drugs with more acceptable side-effect profiles, patients with schizophrenia or major depression experience substantial disability and burden of disease. The present review discusses the usefulness of partial dopamine D 2 /serotonin 5-HT 1A receptors agonists in the treatment of schizophrenia, major depression and bipolar disorder as well as in Parkinson's disease. Partial agonists can behave as modulators since their intrinsic activity or efficacy of a partial agonist depends on the target receptor population and the local concentrations of the natural neurotransmitter. Thus, these drugs may restore adequate neurotransmission while inducing less side effects. In schizophrenia, partial DA D 2 /5-HT 1A receptor agonists (like aripiprazole or bifeprunox), by stabilizing DA system via a preferential reduction of phasic DA release, reduce side effects i.e. extrapyramidal symptoms and improve cognition by acting on 5-HT 1A receptors. Aripiprazole appears also as a promising agent for the treatment of depression since it potentiates the effect of SSRIs in resistant treatment depression. Concerning bipolar disorders aripiprazole may have only a benefit effect in the treatment of manic episodes. Conversely, treatment of Parkinson's disease with partial DA D 2 /5-HT 1A receptor agonists remains still experimental. However several studies suggest that these drugs decrease usually observed side effects (dyskinesia, psychoticlike symptoms) in Parkinson's disease treatment. Hence, these relatively recent researches provide an exciting future in the discovery of novel stabilizators agents for the management of the latter diseases.

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Investigation of the impact of sarizotan on the pharmacokinetics of levodopa

Abstract: Coadministration of sarizotan with levodopa, in combination with a dopa-decarboxylase inhibitor had no effect on the pharmacokinetics or adverse event profile of levodopa.

Cited by 8 publications

References 18 publications

A randomised clinical trial to evaluate the effects of Plantago ovata husk in Parkinson patients: changes in levodopa pharmacokinetics and biochemical parameters

A randomised clinical trial to evaluate the effects of Plantago ovata husk in Parkinson patients: changes in levodopa pharmacokinetics and biochemical parameters

Local administration of sarizotan into the subthalamic nucleus attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats

Partial Dopamine D2/Serotonin 5-HT1A Receptor Agonists as New Therapeutic Agents~!2009-12-17~!2010-04-07~!2010-07-20~!

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