Peringatan Keamanan

Side effect include increase the occurrence of orthostatic hypotension, severe rhabdomyolysis, dyskinesia, hallucinations, hyperkinesia, hypokinesia, dizziness, fatigu,e gastrointestinal effects including abdominal pain constipation diarrhea nausea

Entacapone

DB00494

small molecule approved investigational

Deskripsi

Entacapone is a selective, reversible catechol-O-methyl transferase (COMT) inhibitor for the treatment of Parkinson's disease. It is a member of the class of nitrocatechols. When administered concomittantly with levodopa and a decarboxylase inhibitor (e.g., carbidopa), increased and more sustained plasma levodopa concentrations are reached as compared to the administration of levodopa and a decarboxylase inhibitor.

Struktur Molekul 2D

Berat 305.286
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 0.4-0.7 hour
Volume Distribusi * 20 L
Klirens (Clearance) * 850 mL/min

Absorpsi

Entacapone is rapidly absorbed (approximately 1 hour). The absolute bioavailability following oral administration is 35%.

Metabolisme

Metabolized via isomerization to the cis-isomer, followed by direct glucuronidation of the parent and cis-isomer.

Rute Eliminasi

Entacapone is almost completely metabolized prior to excretion, with only a very small amount (0.2% of dose) found unchanged in urine. As only about 10% of the entacapone dose is excreted in urine as parent compound and conjugated glucuronide, biliary excretion appears to be the major route of excretion of this drug.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

827 Data
Buprenorphine Entacapone 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 Entacapone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Entacapone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Entacapone.
Hydrocodone Entacapone 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 Entacapone.
Magnesium sulfate The therapeutic efficacy of Entacapone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Entacapone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Entacapone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Entacapone.
Mirtazapine Entacapone 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 Entacapone.
Orphenadrine Entacapone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Entacapone 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 Entacapone.
Pramipexole Entacapone may increase the sedative activities of Pramipexole.
Ropinirole Entacapone may increase the sedative activities of Ropinirole.
Rotigotine Entacapone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Entacapone.
Sodium oxybate Entacapone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Entacapone 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 Entacapone.
Thalidomide Entacapone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Entacapone 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 Entacapone.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Entacapone.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Entacapone.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Entacapone.
Ethanol Entacapone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Entacapone 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 Entacapone.
Fluvoxamine The risk or severity of adverse effects can be increased when Entacapone is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Entacapone is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Entacapone is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Entacapone is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Entacapone is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Entacapone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Entacapone is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Entacapone is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Entacapone is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Entacapone is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Entacapone is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Entacapone is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Entacapone is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Entacapone is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Entacapone is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Entacapone is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Entacapone is combined with Alaproclate.
Olanzapine The therapeutic efficacy of Entacapone can be decreased when used in combination with Olanzapine.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Entacapone.
Risperidone The therapeutic efficacy of Entacapone can be decreased when used in combination with Risperidone.
Quetiapine The therapeutic efficacy of Entacapone can be decreased when used in combination with Quetiapine.
Aripiprazole The therapeutic efficacy of Entacapone can be decreased when used in combination with Aripiprazole.
Paliperidone The therapeutic efficacy of Entacapone can be decreased when used in combination with Paliperidone.
Bifeprunox The therapeutic efficacy of Entacapone can be decreased when used in combination with Bifeprunox.
Iloperidone The therapeutic efficacy of Entacapone can be decreased when used in combination with Iloperidone.
Cariprazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Cariprazine.
Lumateperone The therapeutic efficacy of Entacapone can be decreased when used in combination with Lumateperone.
Sertindole The therapeutic efficacy of Entacapone can be decreased when used in combination with Sertindole.
Asenapine The therapeutic efficacy of Entacapone can be decreased when used in combination with Asenapine.
Lurasidone The therapeutic efficacy of Entacapone can be decreased when used in combination with Lurasidone.
Perospirone The therapeutic efficacy of Entacapone can be decreased when used in combination with Perospirone.
Brexpiprazole The therapeutic efficacy of Entacapone can be decreased when used in combination with Brexpiprazole.
Blonanserin The therapeutic efficacy of Entacapone can be decreased when used in combination with Blonanserin.
Melperone The therapeutic efficacy of Entacapone can be decreased when used in combination with Melperone.
Zotepine The therapeutic efficacy of Entacapone can be decreased when used in combination with Zotepine.
Brilaroxazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Brilaroxazine.
Amisulpride The therapeutic efficacy of Entacapone can be decreased when used in combination with Amisulpride.
Pipamperone The therapeutic efficacy of Pipamperone can be decreased when used in combination with Entacapone.
Loxapine The therapeutic efficacy of Entacapone can be decreased when used in combination with Loxapine.
Promazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Promazine.
Prochlorperazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Prochlorperazine.
Chlorpromazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Chlorpromazine.
Fluphenazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Fluphenazine.
Thioridazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Thioridazine.
Trifluoperazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Trifluoperazine.
Perphenazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Perphenazine.
Mesoridazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Mesoridazine.
Chlorprothixene The therapeutic efficacy of Entacapone can be decreased when used in combination with Chlorprothixene.
Periciazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Periciazine.
Molindone The therapeutic efficacy of Entacapone can be decreased when used in combination with Molindone.
Thioproperazine The therapeutic efficacy of Entacapone can be decreased when used in combination with Thioproperazine.
Thiothixene The therapeutic efficacy of Entacapone can be decreased when used in combination with Thiothixene.
Zuclopenthixol The therapeutic efficacy of Entacapone can be decreased when used in combination with Zuclopenthixol.
Azaperone The therapeutic efficacy of Entacapone can be decreased when used in combination with Azaperone.
Pimozide The therapeutic efficacy of Entacapone can be decreased when used in combination with Pimozide.
Benzatropine The metabolism of Benzatropine can be decreased when combined with Entacapone.
Terfenadine The metabolism of Terfenadine can be decreased when combined with Entacapone.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Entacapone.
Darifenacin The metabolism of Darifenacin can be decreased when combined with Entacapone.
Propiomazine The risk or severity of CNS depression can be increased when Entacapone is combined with Propiomazine.
Maprotiline The risk or severity of CNS depression can be increased when Entacapone is combined with Maprotiline.
Tolterodine The metabolism of Tolterodine can be decreased when combined with Entacapone.
Tiotropium The metabolism of Tiotropium can be decreased when combined with Entacapone.
Solifenacin The metabolism of Solifenacin can be decreased when combined with Entacapone.
Pizotifen The risk or severity of CNS depression can be increased when Entacapone is combined with Pizotifen.
Fesoterodine The metabolism of Fesoterodine can be decreased when combined with Entacapone.
Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Entacapone.
Revefenacin The metabolism of Revefenacin can be decreased when combined with Entacapone.
Doxepin The risk or severity of CNS depression can be increased when Entacapone is combined with Doxepin.

Target Protein

Catechol O-methyltransferase COMT

Referensi & Sumber

Synthesis reference: Pandurang Deshpande, Parven Luthra, Anand Pandey, Dharmesh Dhameliya, "Process for the preparation of (E)-2-cyano-3-(3, 4-dihydroxy-5-nitrophenyl)-N, N-diethyl-2-propenamide (entacapone)." U.S. Patent US20060258877, issued November 16, 2006.
Artikel (PubMed)
  • PMID: 11440283
    Najib J: Entacapone: a catechol-O-methyltransferase inhibitor for the adjunctive treatment of Parkinson's disease. Clin Ther. 2001 Jun;23(6):802-32; discussion 771.
  • PMID: 10981253
    Chong BS, Mersfelder TL: Entacapone. Ann Pharmacother. 2000 Sep;34(9):1056-65.
  • PMID: 11939936
    Poewe WH, Deuschl G, Gordin A, Kultalahti ER, Leinonen M: Efficacy and safety of entacapone in Parkinson's disease patients with suboptimal levodopa response: a 6-month randomized placebo-controlled double-blind study in Germany and Austria (Celomen study). Acta Neurol Scand. 2002 Apr;105(4):245-55.
  • PMID: 12876237
    Brooks DJ, Sagar H: Entacapone is beneficial in both fluctuating and non-fluctuating patients with Parkinson's disease: a randomised, placebo controlled, double blind, six month study. J Neurol Neurosurg Psychiatry. 2003 Aug;74(8):1071-9.
  • 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: 232 • International brands: 2
Produk
  • Apo-entacapone
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Auro-entacapone
    Tablet • 200 mg • Oral • Canada • Generic • Approved
  • Carbidopa, Levodopa and Entacapone
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Carbidopa, Levodopa and Entacapone
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Carbidopa, Levodopa and Entacapone
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Carbidopa, Levodopa and Entacapone
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Carbidopa, Levodopa and Entacapone
    Tablet, film coated • - • Oral • US • Generic • Approved
  • Carbidopa, Levodopa and Entacapone
    Tablet, film coated • - • Oral • US • Generic • Approved
Menampilkan 8 dari 232 produk.
International Brands
  • Anxopone — Root
  • Comtade — Novartis

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