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 Method to treat Parkinsons disease

Details
Inventors: Chiesi, Paolo;
Assignee: Chiesi Farmaceutici S.p.A. (Parma, IT)
Primary Examiner: Friedman; Stanley J.
Assistant Examiner:
Attorney, Agent or Firm: Bucknam and Archer

Pharmaceutical compositions for the treatment of Parkinson's disease and neurologic syndromes connected with it, containing as the active principle levodopa methyl ester optionally combined with other active principles selected from dopaminergic, anticholinergic, antidepressive drugs, carboxylase and monoaminoxidase inhibitors.

DETAILED DESCRIPTION I claim: 1.
The method of treatment of Parkinson's disease and related neurological syndromes which consists of administering by the oral or sublingual route to a patient in need of said treatment an aqueous solution containing 250 mgs of LDME levodopa methyl ester as the active ingredient and onset of therapeutic effect is produced with a single dose after 20-30 minutes.




Description:
The present invention refers to pharmaceutical compositions for the treatment of Parkinson's disease, containing levodopa methyl ester alone or combined with other active principles.
Parkinson's disease is characterized by a progressive degeneration of the dopaminergic nigrostriatal pathways in the brain.
Biochemical studies carried out in the sixties lead to the discovery of the fundamental role played in the pathogenesis of this disease by the deficit of neurotransmitters, and particularly of dopamine.
This important advance in the comprehension of the neurochemical bases of the pathology brought about a drastic change in the pharmacological approach to the disease, and lead to the introduction in the therapy of an immediate biologic precursor of dopamine, (-)-3-(3,4-dihydroxyphenyl)-L-alanine, more commonly known as levodopa.
The use of levodopa lead to a dramatic improvement in the treatment of parkinsonism, and it is still the treatment of choice of this disease.
Chronic treatment per os, however, often leads to a progressive decrease of the therapeutic effectiveness and to the onset of serious unwanted effects, including abnormal involuntary movements, "end-of-dose deterioration" when efficacy is limited to 3-4 hours, and the "on-off" phenomenon--marked, very abrupt, almost instantaneous, changes in the level of disability.
Pharmacokinetic factors, such as variability in the plasma concentration and interference with intestinal absorption of levodopa due to competition with proteins and amino acids, appear to play a primary role in the origin of the late complications from levodopa therapy, particularly in the "on-off" fluctuations



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