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Old 11-08-2015, 09:27 AM
ashleyk ashleyk is offline
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Join Date: Oct 2006
Location: New England
Posts: 262
15 yr Member
ashleyk ashleyk is offline
Member
 
Join Date: Oct 2006
Location: New England
Posts: 262
15 yr Member
Default Allithiamine

Hi BreezyRacer, could you provide more details on how allithiamine has helped you with your PD?
I started to do a search on allithiamine and PD. It seems to behave as a Prodrug which, from what I can understand, is a molecule that when combined with a med like Sinemet can greatly enhances the ability of L-dopa to cross the BBB.
Never heard of prodrugs before but it is interesting and may be a great improvement in the effectiveness of Sinemet, meaning that more L-dopa goes to the brain and less to the body with less side effects. I guess I'll buy some.

http://www.sciencedirect.com/science...78517394002716

The plasma levels of DOPA demonstrated no significant differences between DOPA and the prodrugs. In contrast, however, brain levels of DOPA were remarkably elevated following administration of the prodrugs. Among the prodrugs examined, ZiPr-DOPA(P)2 was found to most efficiently facilitate delivery of DOPA to brain and this compound showed 30- and 3.7-fold greater increases in the AUC and MRT of DOPA in brain, respectively, than did DOPA itself. These findings suggest that a redox ring-closure system to a quaternary thiazolium can be used as an alternative chemical delivery system to the brain.

http://www.researchgate.net/publication/51790350

Abstract: L-Dopa is the mainstay of Parkinson’s disease therapy; this drug is usually administered orally, but it is extensively metabolized
in the gastrointestinal tract, so that relatively little arrives in the bloodstream as intact L-Dopa. The peripheral conversion of L-Dopa
by amino acid decarboxylase to dopamine is responsible for the typical gastrointestinal and cardiovascular side effects. To minimize the
conversion to dopamine outside the central nervous system, L-Dopa is usually given in combination with peripheral inhibitors of amino
acid decarboxylase. In spite of that, other central nervous side effects such as dyskinesia, on-off phenomenon and end-of-dose deterioration
still remain. The main factors responsible for the poor bioavailability are the drug’s physical-chemical properties
: low water and lipid
solubility, resulting in unfavorable partition, and the high susceptibility to chemical and enzymatic degradation. Starting from these considerations
the prodrug approach has been applied to L-Dopa in order to overcome its metabolism problems and to improve its bioavailability.
The goal of this paper is to provide the reader with a critical overview on L-Dopa prodrugs here classified according to the nature
of the main chemical modification on L-Dopa backbone that led to the formation of the desired derivative.

http://www.ncbi.nlm.nih.gov/pubmed/15328496
http://www.ncbi.nlm.nih.gov/pubmed/21150770
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