Upload & Sell: On
I'm working diligently to catch up on this thread, for the time being... then it's back to homework like this:
Research a drug product called Stalevo to identify what is in this product and how it works to provide therapeutic benefit for a patient with PD.
carbidopa, levodopa and entacapone
Discuss the mechanisms of action for each component and how the components interact.
Current evidence indicates that symptoms of Parkinsonís disease are related to depletion of dopamine in the corpus striatum. Administration of dopamine is ineffective in the treatment of Parkinsonís disease because it does not cross the blood-brain barrier. However, levodopa the metabolic precursor of dopamine, does cross the blood-brain barrier, and is presumably converted to dopamine in the brain. This is thought to be the mechanism whereby levodopa relieves the symptoms of Parkinsonís disease.
When levodopa is administered orally, it is rapidly decarboxylated to dopamine in extracerebral tissues so that only a small portion of a given dose is transported unchanged to the central nervous system. Carbidopa inhibits the decarboxylation of peripheral levodopa, making more levodopa available for delivery to the brain.
Entacapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT).
COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure. Physiological substrates of COMT include DOPA, catecholamines (dopamine, norepinephrine, and epinephrine) and their hydroxylated metabolites. When decarboxylation of levodopa is prevented by carbidopa, COMT becomes the major metabolizing enzyme for levodopa, catalyzing its metabolism to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD).
Ken Hill wrote: