IUPAC_name = 2-dihydroxyamino-4- (4-methylbenzoyl)- cyclohexa-2,4-diene-1,6-dione
CAS_number = 134308-13-7
ATC_prefix = N04
ATC_suffix = BX01
PubChem = 4659569
DrugBank = APRD00445
C = 14 | H = 11 | N = 1 | O = 5
molecular_weight = 273.241 g/mol
bioavailability = 65%
protein_bound = >99.9%
elimination_half-life = 2-3.5 hours
pregnancy_US = C
legal_US = Rx-only
routes_of_administration = Oral
Tolcapone is a
drugthat inhibits the enzyme catechol-O-methyl transferase(COMT). It is used in the treatment of Parkinson's diseaseas an adjunct to levodopa/carbidopamedication. It is a yellow, odorless, non-hygroscopic, crystallinecompound with a relative molecular massof 273.25. The chemical name of tolcapone is 3,4-dihydroxy-4’-methyl-5-nitrobenzophenone. Its empirical formula is C14H11NO5.
Tolcapone has the ability to cross the
blood-brain barrierand thus exerts its COMT inhibitory effects in the CNS as well as in the periphery.
Tolcapone has demonstrated significant
hepatotoxicitythat limits the drug's therapeutic utility to a drug of last resort. Entacapone, another COMT inhibitor, is a more popular selection for L-DOPA adjunct therapy in the treatment of Parkinson's Diseasebecause it has a better side effect and toxicity profile.
Normally, administration of levodopa is compromised when COMT converts it to methyldopa. By preventing this effect, more of the levodopa that is administered reaches the CNS. Additionally, levodopa that is in the CNS, after being converted to dopamine, will not be degraded by COMT when tolcapone inhibits COMT activity.
Wikimedia Foundation. 2010.
Look at other dictionaries:
tolcapone — tol·ca·pone (tōlґkə pōn″) [USP] a reversible inhibitor of catechol O methyltransferase; when administered with levodopa and carbidopa or some other aromatic amino acid decarboxylase inhibitor, it produces more sustained… … Medical dictionary
Monoamine oxidase inhibitor — MAOI redirects here. For the Easter Island statues, see Moai. Monoamine oxidase Monoamine oxidase inhibitors (MAOIs) are a class of antidepressant drugs prescribed for the treatment of depression. They are particularly effective in treating… … Wikipedia
Methyldopa — Systematic (IUPAC) name (S) 2 amino 3 (3,4 dihydroxyphenyl) 2 methyl propanoic acid Clinical data … Wikipedia
Benserazide — Systematic (IUPAC) name 2 amino 3 hydroxy N′ (2,3,4 trihydroxybenzyl)propanehydrazide Clinical data AHFS/Drugs.com … Wikipedia
Rotigotine — Transdermal Patch Systematic (IUPAC) name (S) 6 [propyl(2 thiophen 2 ylethyl)amino] 5,6,7,8 tetrahydronaphthalen 1 ol Clinical data AHFS/ … Wikipedia
L-DOPS — Systematic (IUPAC) name (2R,3S) 2 amino 3 (3,4 dihydroxyphenyl) 3 hydroxypropanoic acid Clinical data Pregnancy cat. … Wikipedia
Memoria episódica — La memoria episódica es la memoria relacionada con sucesos autobiográficos (momentos, lugares, emociones asociadas y demás conocimientos contextuales) que pueden evocarse de forma explícita. La memoria episódica y la memoria semántica son los dos … Wikipedia Español
Amphetamine — For other uses, see Amphetamine (disambiguation). Amphetamine Systematic (IUPAC) name … Wikipedia
Dimethyltryptamine — Systematic (IUPAC) name 2 (1H indol 3 yl) N … Wikipedia
Phenothiazine — Phenothiazine … Wikipedia