Levodopa/carbidopa and entacapone in the treatment of Parkinson's disease: efficacy, safety and patient preference.

Levodopa (LD) is the oldest, most efficacious and best-tolerated drug for dopaminergic substitution of patients with Parkinson's disease (PD). Its main drawback is its short half-life, which supports onset of motor complications in the long term. Therefore well-informed PD patients mostly accept LD therapy as late as possible.

Peripheral COMT inhibition prevents levodopa associated homocysteine increase.

Chronic levodopa (LD)/dopadecarboxylase inhibitor (DDI) increases homocysteine generation as side reaction of O-methylation. Aim was to investigate the impact of the peripheral COMT inhibitor entacapone (EN) on plasma concentrations of homocysteine, LD and 3-O-methyl-dopa (3-OMD). Patients with Parkinson's disease (PD) received on two consecutive days in a standardised fashion one single dose of 200 mg retarded release LD/carbidopa (CD) or of 150 mg LD/CD/EN, since both were shown to have simultaneous pharmacokinetic LD behaviour.

Homocysteine levels after acute levodopa intake in patients with Parkinson's disease.

Levodopa (L-dopa) administered with a dopadecarboxylase inhibitor (DDI) increases homocysteine plasma levels. This may support the onset of atherosclerosis-related disorders and neuropsychiatric complications in patients with Parkinson's disease (PD). This homocysteine elevation is considered as long-term effect of chronic L-dopa/DDI treatment.

Cysteine elevation in levodopa-treated patients with Parkinson's disease.

Homocysteine, cysteine, and cysteinyl-glycine are all metabolically interrelated. Levodopa/decarboxylase inhibitor (LD/DCI) administration increases total homocysteine (tHcy) plasma levels. Objectives were to investigate associations between LD/DCI intake, concentrations of tHcy, cysteine, and cysteinyl-glycine in PD patients and healthy controls.

Entacapone improves absorption of a coadministered salt in patients with Parkinson's disease.

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.