28th November 2010 - History


Journal of Neurology [2010] 257 (Supplement 2) : S249-252 (O.Hornykiewicz) Complete text

L-dopa has been used for thousands of years for Parkinson's Disease. An ancient civilisation in India used a tropical legume called Mucuna Pruriens, whose seeds are a natural source of therapeutic quantities of L-dopa. L-dopa was first isolated in 1910-1913 from seedlings of Vicia faba. In 1938, L-dopa decarboxylase was discovered, the enzyme that turns L-dopa into dopamine. In 1957, dopamine was shown to occur in the brain, and in 1959 it was found to be enriched in a specific part of the brain. In 1960, postmortem studies showed that a severe dopamine deficiency occurred in Parkinson's Disease, thereby providing a basis for dopamine replacement therapy using L-dopa. Accordingly, in 1961, the first successful clinical trial with L-dopa was carried out. In 1963, the dopamine deficiency in the substantia nigra in people with Parkinson's Disease was found. In 1967, the chronic, high dose L-dopa regimen was introduced in the treatment of Parkinson's Disease. 

There are now more than a dozen formats of L-dopa. Sinemet consists of L-dopa and Carbidopa (which helps to prevent the metabolism of L-dopa before it reaches the brain). There is a controlled release version, Sinemet CR, that spreads out the effect of the L-dopa. Madopar consists of L-dopa and Benserazide (which helps to prevent the metabolism of L-dopa before it reaches the brain). There is also a controlled release version called Madopar CR.

Parcopa is an orally disintegrating tablet version of Sinemet. Duodopa is a combination of L-dopa and Carbidopa in the form of a gel. It is administered throughout the day using a portable pump directly into the small intestine through a surgically placed tube. AcuForm is being added to a combination of L-dopa and carbidopa. AcuForm helps to deliver a drug like Sinemet over a longer period of time. Dual layer L-dopa combines the immediate release and the controlled release versions of L-dopa.

Stalevo consists of L-dopa, Carbidopa and Entacopone, which inhibits the COMT enzyme, thereby prolonging the effects of L-dopa.  Melevodopa is the methyl ester of L-dopa. Mucuna pruriens and Fava beans are natural sources of L-dopa. For more current news go to Parkinson's Disease News.


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2015-11-05 15:52:52
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