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20-September-2008 09:55:51 - Tolcapone Tolcapone Systematic IUPAC name 2-dihydroxyamino-4- 4-methylbenzoyl- cyclohexa-2,4-diene-1,6-dione Identifiers CAS number 134308-13-7 ATC code N04BX01 PubChem 4659569 DrugBank APRD00445 Chemical data Formula C14H11NO5 Mol. mass 273.241 g/mol Pharmacokinetic data Bioavailability 65% Protein binding 99.9% Metabolism ? Half life 2-3.5 hours Excretion ? Therapeutic considerations Pregnancy cat. CUS Legal status ℞-onlyUS Routes Oral Tolcapone is a drug that inhibits the enzyme catechol-O-methyl transferase COMT. It is used in the treatment of Parkinson's disease as an adjunct to levodopa/carbidopa medication. It is a yellow, odorless, non-hygroscopic, crystalline compound with a relative molecular mass of 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 barrier and thus exerts its COMT inhibitory effects in the CNS as well as in the periphery. Tolcapone has demonstrated significant hepatotoxicity that 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 Disease because 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. Tablets This pharmacology-related article is a stub. v d e Anti-parkinson drugs: dopaminergic agents N04B Dopa and derivatives Droxidopa Levodopa Melevodopa Etilevodopa Adamantane derivatives Amantadine Dopamine agonists A-412,997 Apomorphine Bromocriptine Cabergoline Dihydrexidine Dihydroergocryptine mesylate Fenoldopam Lisuride Pergolide Piribedil Pramipexole Propylnorapomorphine Quinpirole Ropinirole Rotigotine SKF 38393 SKF 82958 MAOIs B Selegiline Rasagiline COMT inhibitors Entacapone Tolcapone Other Budipine dopa decarboxylase inhibitor Carbidopa Retrieved from http://en..org/wiki/Tolcapone Categories: Pharmacology stubs | Antiparkinsonian agents | COMT inhibitors Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 26 June 2008, at 00:20
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