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Carbidopa
Systematic (IUPAC) name
(2S)-3-(3,4-dihydroxyphenyl)-2-hydrazino-2-methylpropanoic acid
Identifiers
CAS number 28860-95-9
ATC code  ?
PubChem 34359
DrugBank APRD00160
ChemSpider 31640
Chemical data
Formula C 10H14N2O4  
Mol. mass 226.229 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Protein binding 76%
Metabolism decarboxylated to dopamine in extracerebral tissues
Half life 2 hours
Excretion  ?
Therapeutic considerations
Licence data

US FDA:link

Pregnancy cat.  ?
Legal status POM (UK)
Routes  ?
 Yes check.svgY(what is this?)  (verify)

Carbidopa (Lodosyn) is a drug given to people with Parkinson's disease in order to inhibit peripheral metabolism of levodopa.

Contents

Pharmacology

Carbidopa inhibits aromatic-L-amino-acid decarboxylase (DOPA Decarboxylase or DDC),[1] an enzyme important in the biosynthesis of L-tryptophan to serotonin and in the biosynthesis of L-DOPA to Dopamine (DA).

Along with carbidopa, other DDC inhibitors are benserazide (Ro-4-4602), difluromethyldopa, and α-methyldopa.

Uses

Used in tandem with L-DOPA (trade name levodopa, a dopamine precursor converted in the body to dopamine), it increases the plasma half-life of levodopa from 50 minutes to 1 1/2 hours. CarbiDOPA cannot cross the blood brain barrier, so it inhibits only peripheral DDC. It thus prevents the conversion of L-DOPA to dopamine peripherally. This reduces the side effects caused by dopamine on the periphery, as well as increasing the concentration of L-DOPA and dopamine in the brain.

The combination of carbidopa/levodopa) carries the brand names of Sinemet, Parcopa and Atamet; whilst Stalevo is a combination with entacapone, which enhances the bioavailability of carbidopa and levodopa.

Carbidopa is also used in combination with 5-HTP, a naturally occurring amino acid which is a precursor to the neurotransmitter serotonin and an intermediate in tryptophan metabolism. Carbidopa prevents 5-HTP's metabolism in the liver, which can lead to elevated levels of serotonin in the bloodstream. Research shows that co-administration of 5-HTP and carbidopa greatly increases plasma 5-HTP levels. Without the use of carbidopa, there is a significant risk of heart valve disease when taking 5-HTP, due to serotonin's affect on the heart.[2][3] In Europe, 5-HTP is prescribed with carbidopa to prevent the conversion of 5-HTP into serotonin until it reaches the brain.[4]

References

  1. ^ Gilbert JA, Frederick LM, Ames MM (November 2000). "The aromatic-L-amino acid decarboxylase inhibitor carbidopa is selectively cytotoxic to human pulmonary carcinoid and small cell lung carcinoma cells". Clinical cancer research : an official journal of the American Association for Cancer Research 6 (11): 4365–72. PMID 11106255. http://clincancerres.aacrjournals.org/cgi/pmidlookup?view=long&pmid=11106255.  
  2. ^ Gustafsson BI, Tømmerås K, Nordrum I, Loennechen JP, Brunsvik A, Solligård E, Fossmark R, Bakke I, Syversen U, Waldum H (March 2005). "Long-term serotonin administration induces heart valve disease in rats". Circulation 111 (12): 1517–22. doi:10.1161/01.CIR.0000159356.42064.48. PMID 15781732.  
  3. ^ Xu J, Jian B, Chu R, Lu Z, Li Q, Dunlop J, Rosenzweig-Lipson S, McGonigle P, Levy RJ, Liang B (December 2002). "Serotonin mechanisms in heart valve disease II: the 5-HT2 receptor and its signaling pathway in aortic valve interstitial cells". Am. J. Pathol. 161 (6): 2209–18. PMID 12466135. PMC 1850896. http://ajp.amjpathol.org/cgi/content/abstract/161/6/2209.  
  4. ^ http://www3.interscience.wiley.com/journal/119498636/abstract?CRETRY=1&SRETRY=0

External links








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