Peringatan Keamanan

LD50 = 1600 mg/kg (Orally in rats)

Tolcapone

DB00323

small molecule approved withdrawn

Deskripsi

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.

Struktur Molekul 2D

Berat 273.2408
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2-3.5 hours
Volume Distribusi * 9 L
Klirens (Clearance) * 7 L/h

Absorpsi

Rapidly absorbed (absolute bioavailability is about 65%)

Metabolisme

The main metabolic pathway of tolcapone is glucuronidation

Rute Eliminasi

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.

Interaksi Makanan

1 Data
  • 1. Take with or without food. There is a 10-20% reduction in oral bioavailability when food is given 1 hour before and 2 hours after tolcapone.

Interaksi Obat

1446 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Tolcapone is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Tolcapone is combined with Levodopa.
Risperidone Tolcapone may increase the hypotensive activities of Risperidone.
Buprenorphine Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Hydrocodone Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Magnesium sulfate The therapeutic efficacy of Tolcapone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Tolcapone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Mirtazapine Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Orphenadrine Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Pramipexole Tolcapone may increase the sedative activities of Pramipexole.
Ropinirole Tolcapone may increase the sedative activities of Ropinirole.
Rotigotine Tolcapone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Tolcapone.
Sodium oxybate Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Thalidomide Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methylphenidate The risk or severity of adverse effects can be increased when Methylphenidate is combined with Tolcapone.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Tolcapone.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Tolcapone.
Nicorandil Nicorandil may increase the hypotensive activities of Tolcapone.
Ethanol Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Tolcapone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Tolcapone.
Fluvoxamine The risk or severity of adverse effects can be increased when Tolcapone is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Tolcapone is combined with Citalopram.
Trazodone The risk or severity of adverse effects can be increased when Tolcapone is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Tolcapone is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Tolcapone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Tolcapone is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Tolcapone is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Tolcapone is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Tolcapone is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Tolcapone is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Tolcapone is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Tolcapone is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Tolcapone is combined with Seproxetine.
Levomilnacipran Tolcapone may decrease the excretion rate of Levomilnacipran which could result in a higher serum level.
Indalpine The risk or severity of adverse effects can be increased when Tolcapone is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Tolcapone is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Tolcapone is combined with Alaproclate.
Olanzapine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Olanzapine.
Clozapine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Clozapine.
Quetiapine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Quetiapine.
Aripiprazole The therapeutic efficacy of Tolcapone can be decreased when used in combination with Aripiprazole.
Paliperidone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Paliperidone.
Bifeprunox The therapeutic efficacy of Tolcapone can be decreased when used in combination with Bifeprunox.
Iloperidone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Iloperidone.
Cariprazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Cariprazine.
Lumateperone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Lumateperone.
Sertindole The therapeutic efficacy of Tolcapone can be decreased when used in combination with Sertindole.
Asenapine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Asenapine.
Lurasidone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Lurasidone.
Perospirone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Perospirone.
Brexpiprazole The therapeutic efficacy of Tolcapone can be decreased when used in combination with Brexpiprazole.
Blonanserin The therapeutic efficacy of Tolcapone can be decreased when used in combination with Blonanserin.
Melperone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Melperone.
Zotepine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Zotepine.
Brilaroxazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Brilaroxazine.
Amisulpride The therapeutic efficacy of Tolcapone can be decreased when used in combination with Amisulpride.
Pipamperone The therapeutic efficacy of Pipamperone can be decreased when used in combination with Tolcapone.
Loxapine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Loxapine.
Promazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Promazine.
Prochlorperazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Prochlorperazine.
Chlorpromazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Chlorpromazine.
Fluphenazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Fluphenazine.
Thioridazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Thioridazine.
Trifluoperazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Trifluoperazine.
Perphenazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Perphenazine.
Mesoridazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Mesoridazine.
Pimozide The therapeutic efficacy of Tolcapone can be decreased when used in combination with Pimozide.
Chlorprothixene The therapeutic efficacy of Tolcapone can be decreased when used in combination with Chlorprothixene.
Periciazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Periciazine.
Molindone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Molindone.
Thioproperazine The therapeutic efficacy of Tolcapone can be decreased when used in combination with Thioproperazine.
Thiothixene The therapeutic efficacy of Tolcapone can be decreased when used in combination with Thiothixene.
Zuclopenthixol The therapeutic efficacy of Tolcapone can be decreased when used in combination with Zuclopenthixol.
Azaperone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Azaperone.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Tolcapone.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Tolcapone.
Procaine Procaine may increase the orthostatic hypotensive activities of Tolcapone.
Tranylcypromine Tranylcypromine may increase the orthostatic hypotensive activities of Tolcapone.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Tolcapone.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Tolcapone.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Tolcapone.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Tolcapone.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Tolcapone.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Tolcapone.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Tolcapone.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Tolcapone.

Target Protein

Catechol O-methyltransferase COMT

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9917075
    Guay DR: Tolcapone, a selective catechol-O-methyltransferase inhibitor for treatment of Parkinson's disease. Pharmacotherapy. 1999 Jan;19(1):6-20.
  • PMID: 15697329
    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.
  • PMID: 19503773
    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.
  • PMID: 12538800
    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.
  • PMID: 10882160
    Kaakkola S: Clinical pharmacology, therapeutic use and potential of COMT inhibitors in Parkinson's disease. Drugs. 2000 Jun;59(6):1233-50.

Contoh Produk & Brand

Produk: 16 • International brands: 1
Produk
  • Tasmar
    Tablet, film coated • 200 mg/1 • Oral • US • Approved
  • Tasmar
    Tablet, film coated • 100 mg/1 • Oral • US • Approved
  • Tasmar
    Tablet • 100 mg / tab • Oral • Canada • Approved
  • Tasmar
    Tablet • 200 mg / tab • Oral • Canada • Approved
  • Tasmar
    Tablet, film coated • 100 mg • Oral • EU • Approved
  • Tasmar
    Tablet, film coated • 100 mg • Oral • EU • Approved
  • Tasmar
    Tablet, film coated • 100 mg • Oral • EU • Approved
  • Tasmar
    Tablet, film coated • 200 mg • Oral • EU • Approved
Menampilkan 8 dari 16 produk.
International Brands
  • Sen De Ning — Dexin Runsheng Pharmaceutical

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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