Peringatan Keamanan

Rare individual instances of fatal outcomes following overdose with racemic zopiclone have been reported in European postmarketing reports, most often associated with overdose with other CNS-depressant agent. Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing.

Zopiclone

DB01198

small molecule approved

Deskripsi

Zopiclone is a novel hypnotic agent used in the treatment of insomnia. Its mechanism of action is based on modulating benzodiazepine receptors. In addition to zopiclone's benzodiazepine pharmacological properties it also has some barbiturate-like properties.

Struktur Molekul 2D

Berat 388.808
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Rapidly absorbed following oral administration.

Metabolisme

Extensively metabolized in the liver via decarboxylation (major pathway), demethylation, and side chain oxidation. Metabolites include an N-oxide derivative (weakly active; approximately 12% of a dose) and an N-desmethyl metabolite (inactive; approximately 16%). Approximately 50% of a dose is converted to other inactive metabolites via decarboxylation. Hepatic microsomal enzymes are apparently not involved in zopiclone clearance.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Ingesting alcohol may potentiate the CNS depressant actions of zopiclone.
  • 2. Avoid grapefruit products. Grapefruit may reduce the CYP3A4 metabolism of zopiclone, increasing its sedative effects.

Interaksi Obat

1168 Data
Buprenorphine Zopiclone 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 Zopiclone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Zopiclone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Zopiclone.
Hydrocodone Zopiclone 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 Zopiclone.
Magnesium sulfate The therapeutic efficacy of Zopiclone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Zopiclone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Zopiclone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Zopiclone.
Mirtazapine Zopiclone 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 Zopiclone.
Orphenadrine Zopiclone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Zopiclone 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 Zopiclone.
Pramipexole Zopiclone may increase the sedative activities of Pramipexole.
Ropinirole Zopiclone may increase the sedative activities of Ropinirole.
Rotigotine Zopiclone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Zopiclone.
Suvorexant Zopiclone 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 Zopiclone.
Thalidomide Zopiclone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Zopiclone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Viloxazine The metabolism of Zopiclone can be decreased when combined with Viloxazine.
Methylene blue The metabolism of Zopiclone can be decreased when combined with Methylene blue.
Abiraterone The metabolism of Zopiclone can be decreased when combined with Abiraterone.
Dabrafenib The serum concentration of Zopiclone can be decreased when it is combined with Dabrafenib.
Etoposide The metabolism of Zopiclone can be decreased when combined with Etoposide.
Aldesleukin The metabolism of Zopiclone can be decreased when combined with Aldesleukin.
Octreotide The metabolism of Zopiclone can be decreased when combined with Octreotide.
Fluvoxamine The metabolism of Zopiclone can be decreased when combined with Fluvoxamine.
Fluconazole The metabolism of Zopiclone can be decreased when combined with Fluconazole.
Erythromycin The serum concentration of Zopiclone can be increased when it is combined with Erythromycin.
Citalopram The metabolism of Zopiclone can be decreased when combined with Citalopram.
Cabergoline The metabolism of Zopiclone can be decreased when combined with Cabergoline.
Diethylstilbestrol The metabolism of Zopiclone can be decreased when combined with Diethylstilbestrol.
Isradipine The metabolism of Zopiclone can be decreased when combined with Isradipine.
Valproic acid The metabolism of Zopiclone can be decreased when combined with Valproic acid.
Acetaminophen The metabolism of Zopiclone can be decreased when combined with Acetaminophen.
Dihydroergotamine The metabolism of Zopiclone can be decreased when combined with Dihydroergotamine.
Diltiazem The metabolism of Zopiclone can be decreased when combined with Diltiazem.
Methylergometrine The metabolism of Zopiclone can be decreased when combined with Methylergometrine.
Mefloquine The metabolism of Zopiclone can be decreased when combined with Mefloquine.
Clozapine The metabolism of Zopiclone can be decreased when combined with Clozapine.
Sorafenib The metabolism of Zopiclone can be decreased when combined with Sorafenib.
Nitric Oxide The metabolism of Zopiclone can be decreased when combined with Nitric Oxide.
Cerivastatin The metabolism of Zopiclone can be decreased when combined with Cerivastatin.
Teniposide The metabolism of Zopiclone can be decreased when combined with Teniposide.
Chloramphenicol The metabolism of Zopiclone can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Zopiclone can be decreased when combined with Lansoprazole.
Quinine The metabolism of Zopiclone can be decreased when combined with Quinine.
Raloxifene The metabolism of Zopiclone can be decreased when combined with Raloxifene.
Cimetidine The metabolism of Zopiclone can be decreased when combined with Cimetidine.
Erlotinib The metabolism of Zopiclone can be decreased when combined with Erlotinib.
Ciprofloxacin The metabolism of Zopiclone can be decreased when combined with Ciprofloxacin.
Zafirlukast The metabolism of Zopiclone can be decreased when combined with Zafirlukast.
Vinblastine The metabolism of Zopiclone can be decreased when combined with Vinblastine.
Fluticasone propionate The metabolism of Zopiclone can be decreased when combined with Fluticasone propionate.
Thiopental The metabolism of Zopiclone can be decreased when combined with Thiopental.
Imatinib The metabolism of Zopiclone can be decreased when combined with Imatinib.
Nicardipine The metabolism of Zopiclone can be decreased when combined with Nicardipine.
Astemizole The metabolism of Zopiclone can be decreased when combined with Astemizole.
Dextropropoxyphene The metabolism of Zopiclone can be decreased when combined with Dextropropoxyphene.
Verapamil The metabolism of Zopiclone can be decreased when combined with Verapamil.
Epinephrine The metabolism of Zopiclone can be decreased when combined with Epinephrine.
Aprepitant The metabolism of Zopiclone can be decreased when combined with Aprepitant.
Tamoxifen The metabolism of Zopiclone can be decreased when combined with Tamoxifen.
Losartan The metabolism of Zopiclone can be decreased when combined with Losartan.
Midazolam The risk or severity of sedation and CNS depression can be increased when Midazolam is combined with Zopiclone.
Daunorubicin The metabolism of Zopiclone can be decreased when combined with Daunorubicin.
Paroxetine The metabolism of Zopiclone can be decreased when combined with Paroxetine.
Tranylcypromine The metabolism of Zopiclone can be decreased when combined with Tranylcypromine.
Tetracycline The metabolism of Zopiclone can be decreased when combined with Tetracycline.
Roxithromycin The metabolism of Zopiclone can be decreased when combined with Roxithromycin.
Phenelzine The metabolism of Zopiclone can be decreased when combined with Phenelzine.
Propofol The metabolism of Zopiclone can be decreased when combined with Propofol.
Acetazolamide The metabolism of Zopiclone can be decreased when combined with Acetazolamide.
Diazepam The metabolism of Zopiclone can be decreased when combined with Diazepam.
Clofazimine The metabolism of Zopiclone can be decreased when combined with Clofazimine.
Tacrolimus The metabolism of Zopiclone can be decreased when combined with Tacrolimus.
Quinidine The metabolism of Zopiclone can be decreased when combined with Quinidine.
Metronidazole The metabolism of Zopiclone can be decreased when combined with Metronidazole.
Isoniazid The metabolism of Zopiclone can be decreased when combined with Isoniazid.
Dirithromycin The metabolism of Zopiclone can be decreased when combined with Dirithromycin.
Doxorubicin The metabolism of Zopiclone can be decreased when combined with Doxorubicin.
Metyrapone The metabolism of Zopiclone can be decreased when combined with Metyrapone.
Sulfamethoxazole The metabolism of Zopiclone can be decreased when combined with Sulfamethoxazole.
Glyburide The metabolism of Zopiclone can be decreased when combined with Glyburide.
Irbesartan The metabolism of Zopiclone can be decreased when combined with Irbesartan.
Topotecan The metabolism of Zopiclone can be decreased when combined with Topotecan.
Norfloxacin The metabolism of Zopiclone can be decreased when combined with Norfloxacin.
Oxybutynin The metabolism of Zopiclone can be decreased when combined with Oxybutynin.
Mequitazine The metabolism of Zopiclone can be decreased when combined with Mequitazine.
Primaquine The metabolism of Zopiclone can be decreased when combined with Primaquine.
Dimethyl sulfoxide The metabolism of Zopiclone can be decreased when combined with Dimethyl sulfoxide.
Fluvastatin The metabolism of Zopiclone can be decreased when combined with Fluvastatin.
Pimozide The metabolism of Zopiclone can be decreased when combined with Pimozide.
Miconazole The metabolism of Zopiclone can be decreased when combined with Miconazole.
Bicalutamide The metabolism of Zopiclone can be decreased when combined with Bicalutamide.
Rabeprazole The metabolism of Zopiclone can be decreased when combined with Rabeprazole.

Target Protein

Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1
Gamma-aminobutyric acid receptor subunit alpha-2 GABRA2
Gamma-aminobutyric acid receptor subunit alpha-3 GABRA3
Gamma-aminobutyric acid receptor subunit alpha-5 GABRA5
Translocator protein TSPO

Referensi & Sumber

Synthesis reference: Thomas Jerussi, "Compositions comprising zopiclone derivatives and methods of making and using the same." U.S. Patent US20040147521, issued July 29, 2004.
Artikel (PubMed)
  • PMID: 2581904
    Liu HJ, Sato K, Shih HC, Shibuya T, Kawamoto H, Kitagawa H: Pharmacologic studies of the central action of zopiclone: effects on locomotor activity and brain monoamines in rats. Int J Clin Pharmacol Ther Toxicol. 1985 Mar;23(3):121-8.
  • PMID: 2860074
    Sato K, Hong YL, Yang MS, Shibuya T, Kawamoto H, Kitagawa H: Pharmacologic studies of central actions of zopiclone: influence on brain monoamines in rats under stressful condition. Int J Clin Pharmacol Ther Toxicol. 1985 Apr;23(4):204-10.
  • PMID: 15252823
    Dundar Y, Dodd S, Strobl J, Boland A, Dickson R, Walley T: Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis. Hum Psychopharmacol. 2004 Jul;19(5):305-22.
  • PMID: 6298365
    Blanchard JC, Julou L: Suriclone: a new cyclopyrrolone derivative recognizing receptors labeled by benzodiazepines in rat hippocampus and cerebellum. J Neurochem. 1983 Mar;40(3):601-7.
  • PMID: 6142468
    Julou L, Bardone MC, Blanchard JC, Garret C, Stutzmann JM: Pharmacological studies on zopiclone. Pharmacology. 1983;27 Suppl 2:46-58.

Contoh Produk & Brand

Produk: 91 • International brands: 2
Produk
  • Act Zopiclone
    Tablet • 5 mg • Oral • Canada • Approved
  • Act Zopiclone
    Tablet • 7.5 mg • Oral • Canada • Approved
  • Ag-zopiclone
    Tablet • 3.75 mg • Oral • Canada • Generic • Approved
  • Ag-zopiclone
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ag-zopiclone
    Tablet • 7.5 mg • Oral • Canada • Generic • Approved
  • Apo-zopiclone
    Tablet • 7.5 mg • Oral • Canada • Generic • Approved
  • Apo-zopiclone
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ava-zopiclone
    Tablet • 5 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 91 produk.
International Brands
  • Amoban
  • Zimovane

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul