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For this reason levodopa is usually administered in combination with a DOPA decarboxylase inhibitor (DDCI), in this case carbidopa, which is very polar (and charged at physiologic pH) and cannot cross the blood brain barrier, however prevents peripheral conversion of levodopa to dopamine and thereby reduces the unwanted peripheral side effects ...
COMT inhibitors are indicated for the treatment of Parkinson's disease in combination with levodopa and an aromatic L-amino acid decarboxylase inhibitor (e.g. carbidopa or benserazide). The therapeutic benefit of using a COMT inhibitor is based on its ability to prevent the methylation of levodopa to 3- O -methyldopa , thus increasing the ...
Carbidopa (Lodosyn) is a drug given to people with Parkinson's disease in order to inhibit peripheral metabolism of levodopa.This property is significant in that it allows a greater proportion of administered levodopa to cross the blood–brain barrier for central nervous system effect, instead of being peripherally metabolised into substances unable to cross said barrier.
The side effects of levodopa may include: Hypertension, especially if the dosage is too high; Arrhythmias, although these are uncommon; Nausea, which is often reduced by taking the drug with food, although protein reduces drug absorption. Levodopa is an amino acid, so protein competitively inhibits levodopa absorption. Gastrointestinal bleeding
Administration can prevent common side-effects, such as nausea and vomiting, as a result of interaction with D 2 receptors in the vomiting center (or cheomoreceptor trigger zone) located outside the blood–brain barrier. [2] Examples of extracerebral decarboxylase inhibitors include carbidopa and benserazide.
Researchers have discovered that people who carry the APOE-e4 gene may be at a higher risk of developing a negative reaction to anti-amyloid drugs for Alzheimer's.
Levodopa is the immediate precursor to dopamine. Entacapone is a selective, reversible catechol-O-methyltransferase (COMT) inhibitor that prevents the degradation of levodopa.
Entacapone is a widely used adjunct drug of levodopa therapy. When given with an inhibitor of dopa decarboxylase (carbidopa or benserazide), levodopa is optimally saved. This "triple therapy" is becoming a standard in the treatment of Parkinson's disease. Specific reactions catalyzed by COMT include: L-DOPA (levodopa) → 3-O-methyldopa