Mr. Ibrahem/Tolcapone
Clinical data
Trade namesTasmar
AHFS/Drugs.comMonograph
MedlinePlusa698036
License data
Pregnancy
category
  • AU: B3
Routes of
administration
By mouth
Drug classCOMT inhibitor[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU: Rx-only
Pharmacokinetic data
Bioavailability65%
Protein binding>99.9%
MetabolismLiver (mainly glucuronidation)
Elimination half-life2–3 hours
ExcretionUrine (60%), feces (40%);
only 0.5% in unmetabolized form
Identifiers
  • (3,4-Dihydroxy-5-nitrophenyl)(4-methylphenyl)methanone
Chemical and physical data
FormulaC14H11NO5
Molar mass273.244 g·mol−1
3D model (JSmol)
Melting point143 to 146 °C (289 to 295 °F)
Solubility in waternot soluble
  • [O-][N+](=O)c2cc(C(=O)c1ccc(cc1)C)cc(O)c2O
  • InChI=1S/C14H11NO5/c1-8-2-4-9(5-3-8)13(17)10-6-11(15(19)20)14(18)12(16)7-10/h2-7,16,18H,1H3 checkY
  • Key:MIQPIUSUKVNLNT-UHFFFAOYSA-N checkY
  (verify)

Tolcapone, sold under the brand name Tasmar, is a medication used to treat Parkinson's disease (PD).[2] It is taken together with levodopa/carbidopa.[2] It is taken by mouth.[2] If people do not see improvement within 3 weeks it should be stopped.[2]

Common side effects include nausea, loss of appetite, movement disorders, headache, increased dreams, and confusion.[3] Other side effects may include liver problems, which can be severe, and psychosis.[2] It is an inhibitor of catechol-O-methyltransferase (COMT).[1]

Tolcapone was approved for medical use in Europe in 1997 and the United States in 1998.[3][2] It is available as a generic medication.[4] In the United Kingdom 100 tablets of 100 mg costs the NHS about £95 in 2021.[5] This amount in the United States costs about 1,200 USD.[4] It is not commonly used due to side effects.[1]

References edit

  1. ^ a b c Antonini A, Abbruzzese G, Barone P, Bonuccelli U, Lopiano L, Onofrj M, et al. (February 2008). "COMT inhibition with tolcapone in the treatment algorithm of patients with Parkinson's disease (PD): relevance for motor and non-motor features". Neuropsychiatric Disease and Treatment. 4 (1): 1–9. doi:10.2147/NDT.S2404. PMC 2515921. PMID 18728767.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  2. ^ a b c d e f g h "Tolcapone Monograph for Professionals". Drugs.com. Archived from the original on 4 March 2021. Retrieved 5 October 2021.
  3. ^ a b c "Tasmar". Archived from the original on 10 January 2021. Retrieved 6 October 2021.
  4. ^ a b "Tolcapone Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 6 October 2021.
  5. ^ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 433. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)