. . " "@en . . . . "Tolcapone"@en . . "* 7 L/h"@en . . . . . "> 99.9% (to serum albumin)"@en . . . . "134308-13-7"@en . . . . "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. Tolcapone is associated with a risk of hepatotoxicity. [Wikipedia]"@en . . "Used as an adjunct to levodopa/carbidopa therapy for the symptomatic treatment of Parkinson's Disease. This drug is generally reserved for patients with parkinsonian syndrome receiving levodopa/carbidopa who are experiencing symptom fluctuations and are not responding adequately to or are not candidates for other adjunctive therapies."@en . "LD₅₀ = 1600 mg/kg (Orally in rats)"@en . "Tolcapone is almost completely metabolized prior to excretion, with only a very small amount (0.5% of dose) found unchanged in urine. The glucuronide conjugate of tolcapone is mainly excreted in the urine but is also excreted in the bile."@en . . "3,4-Dihydroxy-5-nitro-4'-methylbenzophenone"@en . "Tolcaponum"@en . . . "(3,4-dihydroxy-5-nitrophenyl)(4-methylphenyl)methanone"@en . . "withdrawn"@en . "Rapidly absorbed (absolute bioavailability is about 65%)"@en . . . "2-3.5 hours"@en . . . . "approved"@en . . "3,4-Dihydroxy-4'-methyl-5-nitrobenzophenone"@en . . . . "Tolcapone"@en . . "# Guay DR: Tolcapone, a selective catechol-O-methyltransferase inhibitor for treatment of Parkinson's disease. Pharmacotherapy. 1999 Jan;19(1):6-20. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/9917075 # Keating GM, Lyseng-Williamson KA: Tolcapone: a review of its use in the management of Parkinson's disease. CNS Drugs. 2005;19(2):165-84. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/15697329 # Truong DD: Tolcapone: review of its pharmacology and use as adjunctive therapy in patients with Parkinson's disease. Clin Interv Aging. 2009;4:109-13. Epub 2009 May 14. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/19503773 # Forsberg M, Lehtonen M, Heikkinen M, Savolainen J, Jarvinen T, Mannisto PT: Pharmacokinetics and pharmacodynamics of entacapone and tolcapone after acute and repeated administration: a comparative study in the rat. J Pharmacol Exp Ther. 2003 Feb;304(2):498-506. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/12538800 # Kaakkola S: Clinical pharmacology, therapeutic use and potential of COMT inhibitors in Parkinson's disease. Drugs. 2000 Jun;59(6):1233-50. \"Pubmed\":http://www.ncbi.nlm.nih.gov/pubmed/10882160"@en . "Humans and other mammals"@en . . . . . "* 9 L"@en . . "Tolcapon"@en . . "Tolcapona"@en . . . . . . . . "4'-Methyl-3,4-dihydroxy-5-nitrobenzophenone"@en . . . . "The precise mechanism of action of tolcapone is unknown, but it is believed to be related to its ability to inhibit COMT and alter the plasma pharmacokinetics of levodopa, resulting in an increase in plasma levodopa concentrations. The inhibition of COMT also causes a reduction in circulating 3-OMD as a result of decreased peripheral metabolism of levodopa. This may lead to an increase distribution of levodopa into the CNS through the reduction of its competitive substrate, 3-OMD, for transport mechanisms. Sustained levodopa concentrations presumably result in more consistent dopaminergic stimulation, resulting in greater reduction in the manifestations of parkinsonian syndrome."@en . . . . . . .