Increased dosage of carbidopa in parkinsonian patients on low carbidopa-levodopa regimen. Effect on levodopa bioavailability

Clin Neuropharmacol. 1989 Feb;12(1):75-81. doi: 10.1097/00002826-198902000-00010.

Abstract

The effect of a 2.5-fold increase in daily carbidopa intake on the bioavailability of levodopa was studied in six patients with Parkinson's disease on a low chronic regimen of carbidopa-levodopa (Sinemet) at the fixed ratio of 1:10. The extent of levodopa absorption, expressed as the area under the 11-h plasma levodopa concentration-time curve (AUC0-11 h), was not enhanced by the higher carbidopa dose. A significant increase in the AUC was found for the levodopa metabolite 3-O-methyldopa at the higher carbidopa intake. Clinical performances of individual patients were identical with both carbidopa-levodopa ratios. From these data, an adequate inhibition of peripheral decarboxylation and hence a good bioavailability of levodopa may be expected in patients taking low doses of carbidopa-levodopa, using currently available commercial preparations.

MeSH terms

  • Aged
  • Aged, 80 and over
  • Biological Availability
  • Carbidopa / administration & dosage*
  • Carbidopa / therapeutic use
  • Dose-Response Relationship, Drug
  • Humans
  • Levodopa / blood
  • Levodopa / pharmacokinetics*
  • Levodopa / therapeutic use
  • Male
  • Middle Aged
  • Parkinson Disease / drug therapy*
  • Tyrosine / analogs & derivatives
  • Tyrosine / blood

Substances

  • Tyrosine
  • Levodopa
  • Carbidopa
  • 3-methoxytyrosine