Movement Disorders (revue)

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The effect of peripheral enzyme inhibitors on levodopa concentrations in blood and CSF

Identifieur interne : 001963 ( Main/Exploration ); précédent : 001962; suivant : 001964

The effect of peripheral enzyme inhibitors on levodopa concentrations in blood and CSF

Auteurs : Maria Nord [Suède] ; Peter Zsigmond [Suède] ; Anita Kullman [Suède] ; Kerstin Rstrand [Suède] ; Nil Dizdar [Suède]

Source :

RBID : ISTEX:7411BA85636A057E85FC2CC3CEACEEBF41C3190F

Descripteurs français

English descriptors

Abstract

Levodopa combined with a dopa‐decarboxylase inhibitor, such as carbidopa, shifts the metabolism to the COMT pathway. Adding the peripheral acting COMT inhibitor entacapone provides improvement for patients with PD suffering from motor fluctuations. We studied the effects of the enzyme inhibitors entacapone and carbidopa on the levodopa concentrations in CSF and in blood. Five PD patients with wearing‐off underwent lumbar drainage and intravenous microdialysis. Samples were taken 12 h daily for 3 days. Day 1; intravenous levodopa was given, day 2; additional oral entacapone 200 mg tid, day 3; additional oral entacapone 200 mg tid and carbidopa 25 mg bid. Levodopa in CSF and in dialysates was analysed. The AUC for levodopa increased both in blood and CSF when additional entacapone was given alone and in combination with carbidopa. The Cmax of levodopa in both CSF and blood increased significantly. Additional entacapone to levodopa therapy gives an increase of Cmax in CSF and in blood. The increase is more evident when entacapone is combined with carbidopa. © 2010 Movement Disorder Society

Url:
DOI: 10.1002/mds.22613


Affiliations:


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<term>Antiparkinson Agents (cerebrospinal fluid)</term>
<term>Antiparkinson Agents (therapeutic use)</term>
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<term>COMT</term>
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<term>Nervous system diseases</term>
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<term>Parkinson Disease (drug therapy)</term>
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<term>Inhibiteur enzyme</term>
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<div type="abstract" xml:lang="en">Levodopa combined with a dopa‐decarboxylase inhibitor, such as carbidopa, shifts the metabolism to the COMT pathway. Adding the peripheral acting COMT inhibitor entacapone provides improvement for patients with PD suffering from motor fluctuations. We studied the effects of the enzyme inhibitors entacapone and carbidopa on the levodopa concentrations in CSF and in blood. Five PD patients with wearing‐off underwent lumbar drainage and intravenous microdialysis. Samples were taken 12 h daily for 3 days. Day 1; intravenous levodopa was given, day 2; additional oral entacapone 200 mg tid, day 3; additional oral entacapone 200 mg tid and carbidopa 25 mg bid. Levodopa in CSF and in dialysates was analysed. The AUC for levodopa increased both in blood and CSF when additional entacapone was given alone and in combination with carbidopa. The Cmax of levodopa in both CSF and blood increased significantly. Additional entacapone to levodopa therapy gives an increase of Cmax in CSF and in blood. The increase is more evident when entacapone is combined with carbidopa. © 2010 Movement Disorder Society</div>
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