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PubMed1988

Prolonged serum levodopa levels with controlled-release carbidopa-levodopa in the treatment of Parkinson's disease.

Twenty parkinsonian patients (Hoehn and Yahr scale, I through III) were treated with controlled-release carbidopa-levodopa (CR-2 or CR-3) and standard carbidopa-levodopa (Sinemet, 25 mg/100 mg) in a double-blind, crossover pharmacokinetic and clinical efficacy study. The controlled-release agents had a slower rise to peak plasma values and flatter pharmacokinetic curves than did the standard. The area under the curve for CR-3 was significantly increased by 55.5% as compared with standard agent and by 84.2% as compared with CR-2. No differences in clinical efficacy were found between controlled-release agents and the standard agent for this group of parkinsonian patients with mild to moderate severity. The dissociation between the prolonged serum levodopa levels and unimproved clinical efficacy may have resulted from the absence of patients with prominent motor fluctuations and/or substantial serum levodopa variability that was especially prominent with CR-3.

Adult↗
PubMed1975

Fluorescence reactions of fluorescamine with levodopa and its derivatives: fluorescence assay of 3-methoxy-4-hydroxyphenylalanine in levodopa dosage forms.

A simple fluorometric method for the quantitation of 3-methoxy-4-hydroxyphenylalanine, either alone or in the presence of levodopa, is presented. Fluorescence is developed by reaction with fluorescamine. The interactions of this reagent with levodopa and a number of its derivatives under various experimental conditions were studied. Negligible fluorescence was obtained with levodopa, dopamine, levodopa benzyl ester, and 6-hydroxydopamine.

Chemical Phenomena↗
PubMed1980

Dosage form design for improvement of bioavailability of levodopa III: Influence of dose on pharmacokinetic behavior of levodopa in dogs and Parkinsonian patients.

The relationship between the dose of levodopa and its pharmacokinetic behavior following intravenous and oral administration was investigated in dogs and parkinsonian patients. Six beagle dogs received single doses of 2.4, 4.8, and 9.6 mg of levodopa/kg iv and single doses of 4.8, 9.6, and 19.2 mg of levodopa/kg po in a crossover fashion on separate occasions. Three parkinsonian patients received single oral doses of approximately 3.8, 7.7, and 15.4 mg of levodopa/kg in a crossover test. Plasma samples were analyzed for intact levodopa and total dopamine. The relationship between the area under the plasma concentration-time curve (AUC) of levodopa and the intravenous dose to dogs was linear. However, in both dogs and patients, the relationship after oral dosing was nonlinear, with the relative AUC increasing with increasing dose. Therefore, the pharmacokinetic behavior of levodopa after oral administration to dogs and patients was dose dependent.

Administration, Oral↗
PubMed1996

[Levodopa and malignant melanoma--case report and review of the literature. A contribution to causal relationship between levodopa and the development of malignant melanoma].

A 72-years old man with Parkinson's disease was treated with levodopa for 14 years. A superficial spreading melanoma (Breslow depth 1,8 mm Clark level IV) was diagnosed, developing on the back from a pigment lesion which had present for more than 10 years. Other case reports suggest a relationship between the administration of levodopa and the growth of malignant melanoma. On the other hand, epidemiological studies found no correlation. Furthermore, in vitro and in vivo studies have shown a possible anti-tumor effect of levodopa. Critical analysis of the literature leads to the conclusion, that there is no increased melanoma risk from levodopa.

Aged↗
PubMed2003

Efficacy and safety of levodopa with entacapone in Parkinson's disease patients suboptimally controlled with levodopa alone, in daily clinical practice: an international, multicentre, open-label study.

The combination of entacapone with levodopa is effective in the treatment of Parkinson's disease (PD), providing significant improvements in 'on' time and Unified Parkinson's Disease Rating Scale (UPDRS) motor and ADL scores in controlled clinical trials. This multicentre, open-label study was designed to further evaluate the effectiveness of levodopa combined with entacapone 200 mg in routine clinical practice. Patients experiencing end-of-dose wearing-off were treated for 8 weeks (treatment phase), with an optional extension phase up to 20 weeks. The primary efficacy parameter was the Investigators' Global Assessment of Change; secondary efficacy parameters included UPDRS, 'off' time (from patient diaries), Patients' Global Assessment of Change, quality of life (QoL), SF-36 Health Assessment Questionnaire and Parkinson's Disease Questionnaire 39 (PDQ-39). Of the 479 patients who entered this study, 427 (89.1%) completed the treatment phase and 374 (78.1%) continued into the extension phase. Based on the Investigators' Assessment of Change, 380 (79.7%) patients showed an improvement with entacapone during the treatment phase. This improvement was maintained into the extension phase, and at Week 20, 301 (82.2%) patients continued to show an improvement. A positive treatment effect with entacapone was also seen with all secondary efficacy parameters, including QoL. Mean change in the total PDQ-39 scores showed improvements from baseline of -4.0 score points to the end of the treatment phase (n=182) and -3.1 score points at the end of the extension phase (n=152). Entacapone in combination with levodopa was generally well tolerated: 40 patients (8.4%) discontinued treatment due to adverse events (AEs) by the end of the extension phase. This study in a daily clinical practice setting confirmed the efficacy of coadministering entacapone with levodopa shown in controlled clinical trials and suggests that the combination is useful in improving the disability and QoL in patients with PD.

Administration, Oral↗
PubMed1990

Simultaneous high-performance liquid chromatographic analysis of carbidopa, levodopa and 3-O-methyldopa in plasma and carbidopa, levodopa and dopamine in urine using electrochemical detection.

Two assay procedures are described for the analysis of levodopa, carbidopa and 3-O-methyldopa in plasma and levodopa, carbidopa and dopamine in urine. The methods are suitable for quantifying the analytes following therapeutic administration of levodopa and carbidopa. Both were based on reversed-phase high-performance liquid chromatography (HPLC) with electrochemical detection and with methyldopa as the internal standard. Plasma samples were prepared by perchloric acid precipitation followed by the direct injection of the supernatant. Urine was prepared by alumina adsorption, and the analytes were desorbed with perchloric acid solution containing disodium EDTA and sodium metabisulfite prior to injection into the HPLC system. The methods have been utilized to evaluate the pharmacokinetics and bioavailability of oral dosage forms containing levodopa and carbidopa.

Carbidopa↗
PubMed1986

Abnormal eye-head coordination in Parkinson's disease patients after administration of levodopa: a possible substrate of levodopa-induced dyskinesia.

Head oscillations in response to whole body oscillation of Parkinsonian patients before and after administration of levodopa were compared with those of normal subjects. Parkinsonian patients developed large increases in the amplitude of their head movements while fixating a stationary target after administration of levodopa. This increase was proportional to disease severity and was maximal in stage IV patients with levodopa induced dyskinesias. These findings indicate a fundamental yet reversible change in the strategy of eye-head coordination in Parkinsonian patients after administration of levodopa which may be due to release of normally inhibited visuo-vestibular reflexes.

Aged↗
PubMed2004

Clinical experience with the novel levodopa formulation entacapone + levodopa + carbidopa (Stalevo).

Levodopa is the main pharmacologic treatment for Parkinson's disease. However, the long-term administration of levodopa is associated with the development of motor complications which can seriously compromise patient function. Increasing evidence indicates that such problems are related to abnormal pulsatile stimulation of striatal dopamine receptors and that treatments providing more continuous stimulation reduce the risk of motor complications. It is possible that administering levodopa with a reversible catechol-O-methyl transferase inhibitor at frequent intervals might reduce the risk of these complications. Stalevo (Orion) combines levodopa, the dopa-decarboxylase inhibitor carbidopa and the catechol-O-methyl transferase inhibitor entacapone in a single tablet. This review provides an overview of the initial clinical experience gained with Stalevo during clinical trials, including several case studies.

Antiparkinson Agents↗
PubMedDate not supplied

Liquid chromatographic determination of levodopa, levodopa-carbidopa, and related impurities in solid dosage forms.

A rapid reverse phase liquid chromatographic method was developed for the determination of levodopa and levodopa-carbidopa in tablets and capsules. The method also separates these drugs from 3-(3,4,6-trihydroxyphenyl)alanine and methoxytyrosine, impurities of levodopa, and from methyldopa and 3-O-methylcarbidopa, impurities of carbidopa. The mobile phase was 3% acetic acid and the detection wavelength was 280 nm. The method was linear over the concentration range 0.05-0.40 mg levodopa/mL, 0.01-0.06 mg carbidopa/mL, 0.9-12.8 micrograms 3-(3,4,6-trihydroxyphenyl)alanine/mL, 0.7-3.1 micrograms methyldopa/mL, 5-20 micrograms methoxytyrosine/mL, and 0.5-3.3 micrograms 3-O-methylcarbidopa/mL. Mean recoveries (%) for spiked commercial tablets were: levodopa 100.3, carbidopa 100.4, 3-(3,4,6-trihydroxyphenyl)alanine 99.1, methoxytyrosine 100.0, methyldopa 100.0, and 3-O-methylcarbidopa 99.4.

Acetaminophen↗
PubMed1979

Comparison of enteric-coated levodopa with levodopa-carbidopa combination. A double-blind crossover trial.

Twenty-seven patients with idiopathic Parkinson's disease completed a double-blind crossover trial which compared enteric-coated levodopa (Prodopa) with levodopa-carbidopa combination (Sinemet). It was easy to stabilize the patients' condition with either drug, and the dose-sparing effect both of the enteric-coated preparation, and of the levodopa-carbidopa combination was again noted. At the dosages used, the levodopa-carbidopa combination was objectively shown to be more effective in 71% of the patients investigated, although there was no clear personal preference for either preparation when patients compared the two parts of the trial. Both drugs play a valuable role in the treatment of Parkinson's disease.

Adult↗
PubMed1997

Central levodopa metabolism in Parkinson's disease after administration of stable isotope-labeled levodopa.

We report the use of a new stable isotope-labeled form of levodopa (LD) to examine in vivo central LD metabolism in Parkinson's disease (PD). Eight patients representing a wide spectrum of disease severity were administered 50 mg of carbidopa orally followed in 1 hour by an intravenous bolus of 150 mg of stable isotope-labeled LD (ring-1',2',3',4',5',6'-(13)C6). Serial blood samples were taken every 30 to 60 minutes and a lumbar puncture was performed 6 hours after the infusion. The average percentage of labeled homovanillic acid (HVA) in lumbar cerebrospinal fluid (CSF) was 54% (SD, 9%; range, 34-67%). The mean CSF labeled HVA concentration was 34.7 ng/ml (SD, 20.2 ng/ml; range, 11.3-67.9 ng/ml). Area under the curve for labeled serum LD closely predicted CSF labeled HVA concentrations (r = 0.747, p = 0.033). Labeled CSF HVA levels did not significantly correlate with either quality or duration of response to the labeled LD dose. In a similar manner, labeled CSF HVA concentrations were not influenced by duration of disease or previous daily LD dosage. These findings support the hypothesis that levodopa-induced benefit in PD is not severely limited by a defect in central levodopa metabolism.

Adult↗
PubMed1993

Does tolerance develop to levodopa? Comparison of 2- and 21-H levodopa infusions.

To determine if acute tolerance to levodopa develops, we compared the response to 2- and 21-h levodopa infusions with the rate adjusted during the long infusion to yield the same plasma concentration as at the end of the 2-h infusion. The duration of response after discontinuing the long infusions was briefer than after discontinuing the short infusion, suggesting the development of tolerance. Furthermore, dyskinesia severity was greater during long infusions. We conclude that continuous dopaminergic stimulation with levodopa may not offer optimal control of parkinsonism in patients with response fluctuations.

Aged↗
PubMed1980

Plasma levodopa, dopamine and therapeutic response following levodopa therapy of Parkinsonian patients.

In a double blind placebo controlled study of 6 Parkinsonian patients given a single dose of oral levodopa, the plasma levodopa and dopamine as measured by a radioenzymatic method both correlated with clinical improvement. There was a closer correlation with plasma dopamine than with plasma levodopa and it is proposed that peripheral decarboxylation may reflect central decarboxylation.

Aged↗
PubMed1982

Sleep disruption in the course of chronic levodopa therapy: an early feature of the levodopa psychosis.

Sleep disruption is a common complaint in levodopa-treated parkinsonian patients. A survey of 100 parkinsonian patients revealed prominent sleep complaints in 74%. Sleep complaints were unrelated to patient age and the duration of disease but increased in prevalence with longer periods of levodopa therapy. Sleep abnormalities tended to increase in severity with continued treatment and insomnia tended to be followed by daytime somnolence, altered dream events, and episodic nocturnal vocalization and myoclonus. While dyskinetic side effects and on-off syndrome were encountered in patients with and without sleep complaints, 98% of patients experiencing psychiatric side effects also reported sleep disruption. It is suggested that sleep-related symptoms constitute an early stage of levodopa-induced dopaminergic psychiatric toxicity in the parkinsonian population. Clinical and experimental observations suggest that serotonergic mechanisms are important in this symptom complex.

Aged↗
PubMed1990

A comparison of the effects of controlled-release levodopa (Madopar CR) with conventional levodopa in late Parkinson's disease.

In this multicentre study a controlled-release formulation of levodopa and the decarboxylase inhibitor benserazide (Madopar CR) was evaluated in patients with Parkinson's disease exhibiting dose-related fluctuations in motor performance in response to conventional levodopa preparations. The effect of Madopar CR, with or without conventional levodopa/benserazide, on the proportion of time spent "on", "off" or "intermediate" was compared with that of previous conventional levodopa/decarboxylase inhibitor therapy. Evaluation of the two periods of optimum therapy was based on both patient diary data and investigator opinion. Forty seven patients completed the study but full patient diaries were available for only 37. The mean optimum total daily dosage of conventional Madopar was 820 mg taken in a mean of 6.4 doses, compared with a mean optimum daily dosage of combined Madopar CR and conventional Madopar of 1088 mg, taken in a mean of 5.2 doses. Conventional Madopar was taken in addition to Madopar CR in all but eight patients. Madopar CR was felt to be advantageous in 83% and disadvantageous in 11% of patients completing the study. Considering the 37 patients for whom diary data were available, Madopar CR therapy resulted in an increase in the mean time spent "on" (p = 0.016) and a decrease in the mean time spent "off" (p = 0.029) compared with conventional Madopar alone. Individually 25 out of 37 had an increase in "on" time and 19 out of 37 experienced a decrease in "off" time. Thus Madopar CR was found to be beneficial in a significant proportion of patients experiencing fluctuations in response to conventional levodopa.

Adult↗
PubMed1990

Sustained enteral administration of levodopa increases and interrupted infusion decreases levodopa dose requirements.

We placed a 60-year-old man with Parkinson's disease and marked therapeutic response fluctuations on a continuous enteral infusion of levodopa. On around-the-clock infusion, motor performance declined, although the infusion rate was progressively increased. We therefore interrupted the infusion each night. The patient could then progressively reduce levodopa intake while remaining continuously "on." Continuous infusion of levodopa downregulates, and interrupted infusion can restore, and even enhance, the sensitivity of striatal dopamine receptors.

Drug Administration Schedule↗
PubMed2000

Quality control of benserazide-levodopa and carbidopa-levodopa tablets by capillary zone electrophoresis.

In modern practice, the treatment of Parkinson's disease and syndrome is carried out using pharmaceutical formulations containing a combination of levodopa and a decarboxylation inhibitor (carbidopa or benserazide). Two pharmaceutical formulations were quantified by capillary zone electrophoresis using two procedures which differed only in the kind of background electrolyte used. One procedure used a 25 mM phosphate buffer, pH 2.5, while the second one used a 25 mM borate buffer, pH 8.5. The electrophoretic analysis was carried out using an uncoated fused- silica capillary, a separation voltage of 20 kV with currents typically less than 60 microA, and spectrophotometric detection at 205 nm. Calibration curves were performed for levodopa (concentration range 1-100 microg/mL), for carbidopa and benserazide (1-50 microg/mL), and the plots of the peak area versus concentration were found to be linear with a correlation coefficient better than 0.9990. Satisfactory results were obtained when commercial tablets were analyzed in terms of accuracy (98-102%), repeatability (0.6-2.0%), and intermediate precision (1.1-2.6%).

Benserazide↗