Peringatan Keamanan

There is no reported LD50 data of opicapone. As there is no known antidote for opicapone overdose, overdosage should be managed with symptomatic and supportive treatment. Removal of the drug through gastric lavage and/or inactivation by administering activated charcoal should be considered.L2343, L13772

Opicapone

DB11632

small molecule approved investigational

Deskripsi

Opicapone is a potent, reversible, and peripherally-acting third-generation inhibitor of catechol-o-methyltransferase (COMT), an enzyme involved in the breakdown of various catecholamines including dopamine.A36938, A203048 Many patients with Parkinson’s disease treated with levodopa plus a dopa decarboxylase (DDC) inhibitor (eg carbidopa) experience motor complications over time, which calls for the management of these symptoms through the use of a dopamine agonist, a monoamine oxidase B inhibitor (selegiline, rasagiline), a catechol-O-methyl transferase (COMT) inhibitor, or amantadine, or using a modified-release formulation of levodopa.L2336

Opicapone is used for adjunct therapy to levodopa and carbidopa in adult patients with Parkinson's disease and end-of-dose motor fluctuations. Opicapone was approved for use by the European Commission in June 2016 L2339 and the FDA in April 2020.L13772 It is marketed under the brand name Ongentys as once-daily oral capsules. Exhibiting a long duration of action that exceeds 24 hours, opicapone can be administered once-daily L2336 and demonstrates the lowest risk for cytotoxicity compared to other catechol-O-methyltransferase inhibitors.A203048

Struktur Molekul 2D

Berat 413.17
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of opicapone is one to two hours.[L13772] Despite the short half-life, the observed half-life of opicapone-induced COMT inhibition in human red blood cells was 61.6 hours with a standard deviation of 37.6 hours.[A32590]
Volume Distribusi Following oral administration, the apparent V<sub>d</sub> of opicapone at a dose of 50 mg was 29 L with an inter-subject variability of 36%.[L2343] One study showed small systemic accumulation after multiple-dosing.[A32589]
Klirens (Clearance) Following oral administration of 50 mg opicapone, the apparent total body clearance was 22 L/h, with an inter-subject variability of 45%.[L2343]

Absorpsi

Orally administered opicapone demonstrates a linear, dose-dependent absorption profile.A203048 Opicapone is rapidly absorbed,A32589 with an oral bioavailability of about 20%.L2343 Following administration of a single 50 mg dose of opicapone, the median Tmax was two hours, ranging from one to four hours. A moderate fat or moderate calorie meal was shown to decrease the Cmax by 62%, the mean overall plasma exposure (AUC) by 31%, and the Tmax by 4 hours.L13772

Metabolisme

According to clinical and in vitro studies, sulphation is the primary metabolic pathway of opicapone, forming the inactive metabolite. Opicapone can also undergo glucuronidation, COMT-mediated methylation, reduction, and glutathione conjugation.L2343, L13772 As two major circulating metabolites, BIA 9-1103 (3-O-sulphated opicapone) accounts for 67.1% of the total radioactivity and BIA 9-1104 (4-O-methylated opicapone) accounts for 20.5% of the total radioactivity. Other metabolites are generally unquantifiable in plasma samples.L2341, L2343 Opicapone can undergo N-oxide reduction to form BIA 9-1079, which was shown to be an active metabolite in non-clinical studies;A32590 however, it is generally undetectable in humans.L2341 Other inactive metabolites include BIA 9-1100, BIA 9-1101, and BIA 9-1106.A32590

Rute Eliminasi

Following administration of a single 100 mg dose of radiolabeled opicapone in healthy subjects, about 70% of the total dose was recovered in feces, where 22% of the recovered dose was excreted as an unchanged parent drug. About 20% of the total dose was recovered in exhaled air and about 5% was recovered in the urine, where less than 1% of the recovered dose was in an unchanged form.L13772 The primary detectable metabolite in the urine was the glucuronide metabolite.L2343

Interaksi Makanan

1 Data
  • 1. Take separate from meals. Take opicapone at least one hour before or after eating, as a moderate calorie meal decreases Cmax and overall plasma exposure to the drug, and delays Tmax.

Interaksi Obat

357 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Opicapone is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Opicapone is combined with Levodopa.
Risperidone Opicapone may increase the hypotensive activities of Risperidone.
Methylphenidate The risk or severity of adverse effects can be increased when Methylphenidate is combined with Opicapone.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Opicapone.
Metoclopramide The therapeutic efficacy of Opicapone can be decreased when used in combination with Metoclopramide.
Aripiprazole lauroxil The therapeutic efficacy of Opicapone can be decreased when used in combination with Aripiprazole lauroxil.
Nicorandil Nicorandil may increase the hypotensive activities of Opicapone.
Ziprasidone The therapeutic efficacy of Opicapone can be decreased when used in combination with Ziprasidone.
Olanzapine The therapeutic efficacy of Opicapone can be decreased when used in combination with Olanzapine.
Clozapine The therapeutic efficacy of Opicapone can be decreased when used in combination with Clozapine.
Quetiapine The therapeutic efficacy of Opicapone can be decreased when used in combination with Quetiapine.
Aripiprazole The therapeutic efficacy of Opicapone can be decreased when used in combination with Aripiprazole.
Paliperidone The therapeutic efficacy of Opicapone can be decreased when used in combination with Paliperidone.
Bifeprunox The therapeutic efficacy of Opicapone can be decreased when used in combination with Bifeprunox.
Iloperidone The therapeutic efficacy of Opicapone can be decreased when used in combination with Iloperidone.
Cariprazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Cariprazine.
Lumateperone The therapeutic efficacy of Opicapone can be decreased when used in combination with Lumateperone.
Sertindole The therapeutic efficacy of Opicapone can be decreased when used in combination with Sertindole.
Asenapine The therapeutic efficacy of Opicapone can be decreased when used in combination with Asenapine.
Lurasidone The therapeutic efficacy of Opicapone can be decreased when used in combination with Lurasidone.
Perospirone The therapeutic efficacy of Opicapone can be decreased when used in combination with Perospirone.
Brexpiprazole The therapeutic efficacy of Opicapone can be decreased when used in combination with Brexpiprazole.
Blonanserin The therapeutic efficacy of Opicapone can be decreased when used in combination with Blonanserin.
Melperone The therapeutic efficacy of Opicapone can be decreased when used in combination with Melperone.
Zotepine The therapeutic efficacy of Opicapone can be decreased when used in combination with Zotepine.
Brilaroxazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Brilaroxazine.
Amisulpride The therapeutic efficacy of Opicapone can be decreased when used in combination with Amisulpride.
Pipamperone The therapeutic efficacy of Pipamperone can be decreased when used in combination with Opicapone.
Loxapine The therapeutic efficacy of Opicapone can be decreased when used in combination with Loxapine.
Promazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Promazine.
Prochlorperazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Prochlorperazine.
Droperidol The therapeutic efficacy of Opicapone can be decreased when used in combination with Droperidol.
Chlorpromazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Chlorpromazine.
Haloperidol The therapeutic efficacy of Opicapone can be decreased when used in combination with Haloperidol.
Fluphenazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Fluphenazine.
Thioridazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Thioridazine.
Trifluoperazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Trifluoperazine.
Perphenazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Perphenazine.
Mesoridazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Mesoridazine.
Pimozide The therapeutic efficacy of Opicapone can be decreased when used in combination with Pimozide.
Chlorprothixene The therapeutic efficacy of Opicapone can be decreased when used in combination with Chlorprothixene.
Methotrimeprazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Methotrimeprazine.
Periciazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Periciazine.
Molindone The therapeutic efficacy of Opicapone can be decreased when used in combination with Molindone.
Thioproperazine The therapeutic efficacy of Opicapone can be decreased when used in combination with Thioproperazine.
Thiothixene The therapeutic efficacy of Opicapone can be decreased when used in combination with Thiothixene.
Zuclopenthixol The therapeutic efficacy of Opicapone can be decreased when used in combination with Zuclopenthixol.
Azaperone The therapeutic efficacy of Opicapone can be decreased when used in combination with Azaperone.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Opicapone.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Opicapone.
Procaine Procaine may increase the orthostatic hypotensive activities of Opicapone.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Opicapone.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Opicapone.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Opicapone.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Opicapone.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Opicapone.
Clorgiline Clorgiline may increase the orthostatic hypotensive activities of Opicapone.
Safinamide Safinamide may increase the orthostatic hypotensive activities of Opicapone.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Opicapone.
Methylene blue Methylene blue may increase the orthostatic hypotensive activities of Opicapone.
Hydracarbazine Hydracarbazine may increase the orthostatic hypotensive activities of Opicapone.
Pirlindole Pirlindole may increase the orthostatic hypotensive activities of Opicapone.
Toloxatone Toloxatone may increase the orthostatic hypotensive activities of Opicapone.
Benmoxin Benmoxin may increase the orthostatic hypotensive activities of Opicapone.
Mebanazine Mebanazine may increase the orthostatic hypotensive activities of Opicapone.
Octamoxin Octamoxin may increase the orthostatic hypotensive activities of Opicapone.
Pheniprazine Pheniprazine may increase the orthostatic hypotensive activities of Opicapone.
Phenoxypropazine Phenoxypropazine may increase the orthostatic hypotensive activities of Opicapone.
Pivhydrazine Pivhydrazine may increase the orthostatic hypotensive activities of Opicapone.
Caroxazone Caroxazone may increase the orthostatic hypotensive activities of Opicapone.
Harmaline Harmaline may increase the orthostatic hypotensive activities of Opicapone.
Brofaromine Brofaromine may increase the orthostatic hypotensive activities of Opicapone.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Opicapone.
Butabarbital Butabarbital may increase the hypotensive activities of Opicapone.
Butalbital Butalbital may increase the hypotensive activities of Opicapone.
Pentobarbital Pentobarbital may increase the hypotensive activities of Opicapone.
Secobarbital Secobarbital may increase the hypotensive activities of Opicapone.
Methohexital Methohexital may increase the hypotensive activities of Opicapone.
Primidone Primidone may increase the hypotensive activities of Opicapone.
Methylphenobarbital Methylphenobarbital may increase the hypotensive activities of Opicapone.
Thiamylal Thiamylal may increase the hypotensive activities of Opicapone.
Amobarbital Amobarbital may increase the hypotensive activities of Opicapone.
Hexobarbital Hexobarbital may increase the hypotensive activities of Opicapone.
Barbital Barbital may increase the hypotensive activities of Opicapone.
Barbexaclone Barbexaclone may increase the hypotensive activities of Opicapone.
Thiopental Thiopental may increase the hypotensive activities of Opicapone.
Phenobarbital Phenobarbital may increase the hypotensive activities of Opicapone.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Opicapone.
Streptokinase The risk or severity of adverse effects can be increased when Streptokinase is combined with Opicapone.
Valsartan The risk or severity of adverse effects can be increased when Valsartan is combined with Opicapone.
Ramipril The risk or severity of adverse effects can be increased when Ramipril is combined with Opicapone.
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Opicapone.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Opicapone.
Reserpine The risk or severity of adverse effects can be increased when Reserpine is combined with Opicapone.
Methyclothiazide The risk or severity of adverse effects can be increased when Methyclothiazide is combined with Opicapone.
Metoprolol The risk or severity of adverse effects can be increased when Metoprolol is combined with Opicapone.
Ropinirole The risk or severity of adverse effects can be increased when Ropinirole is combined with Opicapone.
Isradipine The risk or severity of adverse effects can be increased when Isradipine is combined with Opicapone.
Olmesartan The risk or severity of adverse effects can be increased when Olmesartan is combined with Opicapone.

Target Protein

Catechol O-methyltransferase COMT

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27498199
    Scott LJ: Opicapone: A Review in Parkinson's Disease. Drugs. 2016 Sep;76(13):1293-1300. doi: 10.1007/s40265-016-0623-y.
  • PMID: 28322896
    Goncalves D, Alves G, Fortuna A, Soares-da-Silva P, Falcao A: Pharmacokinetics of opicapone, a third-generation COMT inhibitor, after single and multiple oral administration: A comparative study in the rat. Toxicol Appl Pharmacol. 2017 May 15;323:9-15. doi: 10.1016/j.taap.2017.03.013. Epub 2017 Mar 16.
  • PMID: 23248072
    Almeida L, Rocha JF, Falcao A, Palma PN, Loureiro AI, Pinto R, Bonifacio MJ, Wright LC, Nunes T, Soares-da-Silva P: Pharmacokinetics, pharmacodynamics and tolerability of opicapone, a novel catechol-O-methyltransferase inhibitor, in healthy subjects: prediction of slow enzyme-inhibitor complex dissociation of a short-living and very long-acting inhibitor. Clin Pharmacokinet. 2013 Feb;52(2):139-51. doi: 10.1007/s40262-012-0024-7.
  • PMID: 17894650
    Bonifacio MJ, Palma PN, Almeida L, Soares-da-Silva P: Catechol-O-methyltransferase and its inhibitors in Parkinson's disease. CNS Drug Rev. 2007 Fall;13(3):352-79. doi: 10.1111/j.1527-3458.2007.00020.x.
  • PMID: 29345156
    Svetel M, Tomic A, Kresojevic N, Kostic V: Pharmacokinetic drug evaluation of opicapone for the treatment of Parkinson's disease. Expert Opin Drug Metab Toxicol. 2018 Mar;14(3):353-360. doi: 10.1080/17425255.2018.1430138. Epub 2018 Jan 24.

Contoh Produk & Brand

Produk: 24 • International brands: 0
Produk
  • Ongentys
    Capsule • 50 mg • Oral • EU • Approved
  • Ongentys
    Capsule • 50 mg • Oral • EU • Approved
  • Ongentys
    Capsule • 50 mg • Oral • EU • Approved
  • Ongentys
    Capsule • 50 mg • Oral • EU • Approved
  • Ongentys
    Capsule • 25 mg • Oral • EU • Approved
  • Ongentys
    Capsule • 25 mg • Oral • EU • Approved
  • Ongentys
    Capsule • 25 mg • Oral • EU • Approved
  • Ongentys
    Capsule • 25 mg/1 • Oral • US • Approved
Menampilkan 8 dari 24 produk.

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