AI Article Synopsis

  • Entacapone (EN) enhances the effect of levodopa/dopa decarboxylase inhibitors (LD/DDI) by blocking the enzyme COMT, which helps in producing basic metabolites of levodopa.
  • In a study, parkinsonian patients showed a higher recovery rate of (13)C-sodium-octanoate when taking a combination of levodopa, Carbidopa (CD), and Entacapone (EN) compared to only levodopa and CD.
  • The inhibition of COMT creates a more favorable (basic) environment in the gastrointestinal tract, improving the absorption of acids and salts, which may also lead to better absorption of levodopa itself.

Article Abstract

Entacapone (EN) improves the efficacy of levodopa/dopadecarboxylase inhibitor (LD/DDI) formulations by inhibition of the enzyme catechol-O-methyltransferase (COMT). COMT inhibition also promotes the synthesis of basic LD metabolites, whereas DDI support the composition of acidic LD derivatives. LD metabolism correlates to the one of (13)C-sodium-octanoate, which is employed in breath tests to measure gastric emptying velocity. Objectives were to investigate the impact of COMT inhibition on the recovery rate of (13)C-sodium-octanoate in parkinsonian patients, who received first 100 mg LD/Carbidopa (CD) and the next day 100 mg LD/CD/EN combined with (13)C-sodium-octanoate in each case. The recovery rate of (13)C-sodium-octanoate was significant higher during the LD/CD/EN-compared with the LD/CD condition. COMT inhibition combined with LD/DDI improves absorption of a co-administered salt probably due to a COMT inhibition induced basic environment in gastrointestinal membranes. This improves dissolution and absorption of acids and salts. Thus it may enhance absorption of LD itself.

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http://dx.doi.org/10.1002/mds.22176DOI Listing

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