Clinical Efficacy of Single Morning Doses of Different Levodopa Formulations

Stocchi, F.; uggieri, S. R; Monge, A.; Nordera, G. P.; Bolner, P.; Viselli, F.; Bramante, L.; Quinn, Niall; Pandis, Francesca De; Manfredi, M.

doi:10.1097/00002826-199417003-00004

Cited by 11 publications

(4 citation statements)

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“…Although several controlled‐release (CR) formulations of LD (with CD or benserazide) have been developed, these formulations are associated with erratic absorption and variable LD plasma concentrations . In addition, the latency to onset of motor improvement is typically 30–90 minutes for the IR formulation and 60–180 minutes with the CR formulation due to the slower absorption . Thus, CR CD–LD is commonly administered with IR CD–LD in patients with fluctuations to improve the control of PD symptoms, particularly for the first dose in the morning …”

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confidence: 99%

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Population Pharmacodynamics of IPX066: An Oral Extended‐Release Capsule Formulation of Carbidopa–Levodopa, and Immediate‐Release Carbidopa–Levodopa in Patients With Advanced Parkinson's Disease

Mao

Hsu

Gupta

et al. 2013

The Journal of Clinical Pharma

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A pharmacodynamic model is presented to describe the motor effects (tapping rate, Unified Parkinson’s Disease Rating Scale [UPDRS] Part III, and investigator-rating of ON/OFF, including dyskinesia) of levodopa (LD) in patients with advanced idiopathic Parkinson’s disease (PD) treated with immediate-release (IR) carbidopa–levodopa (CD–LD) or an extended-release (ER) formulation of CD–LD (IPX066). Twenty-seven patients participated in this open-label, randomized, single-and multiple-dose, crossover study. The pharmacodynamic models included a biophase effect site with a sigmoid Emax transduction for tapping and UPDRS and an ordered categorical model for dyskinesia. The pharmacodynamics of LD was characterized by a conduction function with a half-life of 0.59 hours for tapping rate, and 0.4 hours for UPDRS Part III and dyskinesia. The LD concentration for half-maximal effect was 1530 ng/mL, 810 ng/mL, and 600 ng/mL for tapping rate, UPDRS Part III, and dyskinesia, respectively. The sigmoidicity of the transduction was 1.53, 2.5, and 2.1 for tapping rate, UPDRS Part III, and dyskinesia, respectively. External validation of the pharmacodynamic model using tapping rate indicated good performance of the model.

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confidence: 99%

“…In addition, the latency to onset of motor improvement is typically 30–90 minutes for the IR formulation and 60–180 minutes with the CR formulation due to the slower absorption . Thus, CR CD–LD is commonly administered with IR CD–LD in patients with fluctuations to improve the control of PD symptoms, particularly for the first dose in the morning …”

mentioning

confidence: 99%

Population Pharmacodynamics of IPX066: An Oral Extended‐Release Capsule Formulation of Carbidopa–Levodopa, and Immediate‐Release Carbidopa–Levodopa in Patients With Advanced Parkinson's Disease

Mao

Hsu

Gupta

et al. 2013

The Journal of Clinical Pharma

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“…The absorption of LD is better from orally disintegrable tablets, such as dispersible, methylester or ethyl-ester preparations [9]. The C max is then earlier reached and the clinical effect more predictable and reliable [10,11].…”

Section: Absorption Of Levodopa and Factors Influencing Itmentioning

confidence: 99%

Clinical implications of irregular ADMET properties with levodopa and other antiparkinson's drugs

Dézsi

Vécsei

2014

Expert Opinion on Drug Metabolism & Toxicology

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“…Water-soluble preparations of L-dopa, such as Madopar dispersible, L-dopa methylester or L-dopa ethylester, are absorbed more rapidly than standard tablet or capsule L-dopa preparations [37,38]. In different studies, L-dopa methylester -a highly soluble prodrug produced by esterification of the carboxylic moiety of the L-dopa molecule -in solution was shown to be absorbed very quickly, producing an earlier plasma peak and inducing a more predictable clinical effect than standard Ldopa preparations [39,40].…”

Section: Optimizing L-dopa Absorptionmentioning

confidence: 99%

Managing the critical problems of advanced Parkinson’s disease

Stocchi

2002

Expert Review of Neurotherapeutics

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The symptoms of Parkinson's disease can become increasingly difficult to control as the disease advances, particularly with the development of motor complications, such as end-of-dose wearing-off and dyskinesias, following long-term therapy. At this stage, the patient is frequently referred to a Parkinson's disease specialist for advice on their disease management. In this review, we provide an overview of the Parkinson's disease specialist's strategies for coping with such problems. This includes establishing the optimum and most rational L-dopa treatment schedule, improving L-dopa absorption, use of catechol-O-methyl transferase inhibition, the addition of oral dopaminergic agonists and the use of subcutaneous injections or infusions of apomorphine or lisuride. The role of new surgical procedures to treat Parkinson's disease is also reviewed. Finally, we highlight the increasing importance of treatment strategies that stimulate dopamine receptors in a more continuous, less pulsatile manner as a way of reducing the risk of developing treatment-associated motor complications.

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Clinical Efficacy of Single Morning Doses of Different Levodopa Formulations

Cited by 11 publications

References 0 publications

Population Pharmacodynamics of IPX066: An Oral Extended‐Release Capsule Formulation of Carbidopa–Levodopa, and Immediate‐Release Carbidopa–Levodopa in Patients With Advanced Parkinson's Disease

Population Pharmacodynamics of IPX066: An Oral Extended‐Release Capsule Formulation of Carbidopa–Levodopa, and Immediate‐Release Carbidopa–Levodopa in Patients With Advanced Parkinson's Disease

Clinical implications of irregular ADMET properties with levodopa and other antiparkinson's drugs

Managing the critical problems of advanced Parkinson’s disease

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