Objective: The aim of our paper was to assess if standard physical exercise may change pharmacokinetics of levodopa/benserazide in patients with and without prior exposure to the drug.

Background: Physical exercise is a crucial component of treatment of Parkinson disease (PD). Some patients report however faster wearing off levodopa after increased physical effort. We hypothesized that PE may influence levodopa pharmacokinetics.

Method: 23 patients with diagnosis of PD and 7 healthy controls (HC) were included in the study. PD patients were divided into 2 groups: levodopa- naïve group (LNPD, n= 12), not receiving levodopa treatment previously and advanced PD group (APD, n =11) treated with levodopa, with motor complications of treatment. Patients were administered orally standard release levodopa/benserazide 200/50 mg capsule. Blood samples were collected at 0, 20, 40, 60, 90, 120, 150, 180 and 240 minutes after drug administration. During the rest day (RD) patients were asked to refrain from any physical activity and rest in bed for a total time of sample collection. During physical exercise day (PED) patients were asked to perform spinning sessions on a cycle ergometer with standardized heart rate and duration. UPDRS part III was performed before, and 60, 180 and 240 minutes after oral admission of levodopa. Levodopa concentrations were measured with LC-MS/MS.

Results: Selected pharmacokinetic parameters (T ½, Tmax, AUC, MRT) were compared between three groups (HC, LNPD, APD) between 2 days. Additionally the influence of the exercise within HC, LNPD and APD group was analysed. No differences in AUC, MRT, Tmax was noted between all groups in PED and RD. On the RD we observed tendency to faster drug elimination (T ½,) in HC than LNPD (p=0.021, one tailed test) and APD (p=0.05, non-significant, one tailed test). We also observed that Tmax was reached faster in APD group than in LNPD (p<0.01, one tailed test) and HC group (p=0.048, one tailed test) on the RD. The MRT change due to the exercise and was significantly higher in APD than LNPD group (p=0.023). No significant effect of physical exercise on decrease in UPDRS part III was observed.

Conclusion: The results of performed analysis suggest that physical exercise do not deteriorate bioavailability of levodopa neither in APD nor in LNPD patients. Some pharmacokinetic parameters of levodopa absorption may vary between HC, LNPD and APD.

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MDS Abstracts - https://www.mdsabstracts.org/abstract/exercise-and-levodopa-metabolism-in-parkinson-disease/