Concentration-effect relationship of levodopa in patients with Parkinson's disease after oral administration of an immediate release and a controlled release formulation.
1. The relationship between plasma concentration of levodopa and motor- response was investigated in 12 patients with Parkinson's disease who showed marked response fluctuations, after a single oral dose of an immediate release (IR) formulation (100 mg levodopa/25 mg genserazide) and a controll...
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| Main Authors: | , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
January 1995
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| In: |
British journal of clinical pharmacology
Year: 1995, Volume: 39, Issue: 1, Pages: 39-44 |
| ISSN: | 1365-2125 |
| DOI: | https://doi.org/10.1111/j.1365-2125.1995.tb04407.x |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://doi.org/https://doi.org/10.1111/j.1365-2125.1995.tb04407.x Verlag, lizenzpflichtig, Volltext: https://bpspubs.onlinelibrary.wiley.com/doi/abs/10.1111/j.1365-2125.1995.tb04407.x 
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| Author Notes: | S. Harder, H. Baas, N. Bergemann, L. Demisch & S. Rietbrock |
| Summary: | 1. The relationship between plasma concentration of levodopa and motor- response was investigated in 12 patients with Parkinson's disease who showed marked response fluctuations, after a single oral dose of an immediate release (IR) formulation (100 mg levodopa/25 mg genserazide) and a controlled release (CR) formulation (300 mg levodopa/75 mg benserazide), using a double-blind, randomized, cross-over design. 2. The sum score of the Columbia University Rating Scale (CURS sigma) was used for pharmacodynamic assessment. A sigmoidal Emax-model was fitted to the data using a semiparametric pharmacokinetic/dynamic approach. 3. The dose-corrected AUC of levodopa after the IR-formulation was 27.5 (+/- 9.1 s.d.) ng ml-1 h per mg and 23.2 (+/- 4.6 s.d.) ng ml-1 h per mg after the CR-formulation. Cmax was 1714 (+/- 1027 s.d.) ng ml-1 after the IR-formulation and 1494 (+/- 383 s.d.) ng ml-1 after the CR- formulation. 4. With both preparations, the maximal response to levodopa (Emax) was a decrease in the CURS sigma rating of about 27 scores. Estimates of the EC50 of levodopa were 495 (+/- 144 s.d.) ng ml- 1 (IR) and 1024 (+/- 502 s.d.) ng ml-1 (CR), respectively (95%-CI: 1.51- 2.66, point estimator 1.95). The mean duration of the motor response was 1.9 (+/- 0.5 s.d.) h (IR) and 2.8 (+/- 0.7 s.d.) h (CR), respectively (95%-CI: 1.12-2.04, point estimator 1.53).(ABSTRACT TRUNCATED AT 250 WORDS) |
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| Item Description: | Gesehen am 14.12.2020 |
| Physical Description: | Online Resource |
| ISSN: | 1365-2125 |
| DOI: | https://doi.org/10.1111/j.1365-2125.1995.tb04407.x |