Peringatan Keamanan

Patients experiencing an overdose of apomorphine may present with nausea, hypotension, and loss of consciousness.L13919 Treat patients with symptomatic and supportive measures.

The intraperitoneal LD50 in mice is 145µg/kg.L14012

Apomorphine

DB00714

small molecule approved investigational

Deskripsi

Apomorphine is a non-ergoline dopamine D2 agonist indicated to treat hypomobility associated with Parkinson's. It was first synthesized in 1845 and first used in Parkinson's disease in 1884.A203618 Apomorphine has also been investigated as an emetic, a sedative, a treatment for alcoholism, and a treatment of other movement disorders.A203597,A203618

Apomorphine was granted FDA approval on 20 April 2004.L13919

Struktur Molekul 2D

Berat 267.3224
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half life of a 15mg sublingual dose of apomorphine is 1.7h,[L13919] while the terminal elimination half life of an intravenous dose is 50 minutes.[L13922]
Volume Distribusi The apparent volume of distribution of subcutaneous apomorphine is 123-404L with an average of 218L.[L13919] The apparent volume of distribution of sublingual apomorphine is 3630L.[L13922]
Klirens (Clearance) The clearance of a 15mg sublingual dose of apomorphine is 1440L/h,[L13919] while the clearance of an intravenous dose is 223L/h.[L13922]

Absorpsi

Apomorphine has a plasma Tmax of 10-20 minutes and a cerebrospinal fluid Tmax.A203549 The Cmax and AUC of apomorphine vary significantly between patients, with 5- to 10-fold differences being reported.A203549,A203405

Metabolisme

Apomorphine is N-demethylated by CYP2B6, 2C8, 3A4, and 3A5.L13919 It can be glucuronidated by various UGTs,L13919 or sulfated by SULTs 1A1, 1A2, 1A3, 1E1, and 1B1.A203447 Approximately 60% of sublingual apomorphine is eliminated as a sulfate conjugate, though the structure of these sulfate conjugates are not readily available.A203447,L13919 The remainder of an apomorphine dose is eliminated as apomorphine glucuronide and norapomorphine glucuronide.L13919 Only 0.3% of subcutaneous apomorphine is recovered as the unchanged parent drug.A203402

Rute Eliminasi

Data regarding apomorphine's route of elimination is not readily available.L13919,L13922 A study in rats has shown apomorphine is predominantly eliminated in the urine.A203579

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Ingesting alcohol may potentiate hypotension caused by apomorphine.

Interaksi Obat

1441 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Apomorphine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Apomorphine is combined with Levodopa.
Risperidone Apomorphine may increase the hypotensive activities of Risperidone.
Buprenorphine Apomorphine 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 Apomorphine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Apomorphine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Apomorphine.
Hydrocodone Apomorphine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Apomorphine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Apomorphine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Apomorphine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Apomorphine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Apomorphine.
Orphenadrine Apomorphine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Apomorphine 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 Apomorphine.
Pramipexole Apomorphine may increase the sedative activities of Pramipexole.
Ropinirole Apomorphine may increase the sedative activities of Ropinirole.
Rotigotine Apomorphine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Apomorphine.
Sodium oxybate The risk or severity of CNS depression can be increased when Apomorphine is combined with Sodium oxybate.
Suvorexant Apomorphine 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 Apomorphine.
Thalidomide Apomorphine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Apomorphine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Cabergoline The risk or severity of adverse effects can be decreased when Cabergoline is combined with Apomorphine.
Dihydroergotamine The risk or severity of adverse effects can be decreased when Dihydroergotamine is combined with Apomorphine.
Lisuride The risk or severity of adverse effects can be decreased when Lisuride is combined with Apomorphine.
Fenoldopam The risk or severity of adverse effects can be decreased when Apomorphine is combined with Fenoldopam.
Ergoloid mesylate The risk or severity of adverse effects can be decreased when Apomorphine is combined with Ergoloid mesylate.
Pergolide The risk or severity of adverse effects can be decreased when Apomorphine is combined with Pergolide.
Bromocriptine The risk or severity of adverse effects can be decreased when Apomorphine is combined with Bromocriptine.
Aripiprazole The risk or severity of adverse effects can be decreased when Apomorphine is combined with Aripiprazole.
Quinagolide The risk or severity of adverse effects can be decreased when Apomorphine is combined with Quinagolide.
Brexpiprazole The risk or severity of adverse effects can be decreased when Apomorphine is combined with Brexpiprazole.
Dihydroergocornine The risk or severity of adverse effects can be decreased when Apomorphine is combined with Dihydroergocornine.
Dopexamine The risk or severity of adverse effects can be decreased when Apomorphine is combined with Dopexamine.
Piribedil The risk or severity of adverse effects can be decreased when Apomorphine is combined with Piribedil.
Dihydrexidine The risk or severity of adverse effects can be decreased when Apomorphine is combined with Dihydrexidine.
Dihydroergocryptine The risk or severity of adverse effects can be decreased when Apomorphine is combined with Dihydroergocryptine.
Metergoline The risk or severity of adverse effects can be decreased when Apomorphine is combined with Metergoline.
Methylphenidate The risk or severity of adverse effects can be increased when Methylphenidate is combined with Apomorphine.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Dexmethylphenidate is combined with Apomorphine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Apomorphine.
Ondansetron The risk or severity of adverse effects can be increased when Ondansetron is combined with Apomorphine.
Mifepristone The serum concentration of Apomorphine can be increased when it is combined with Mifepristone.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Apomorphine.
Dicoumarol The risk or severity of adverse effects can be increased when Apomorphine is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Apomorphine is combined with Phenindione.
Acenocoumarol The risk or severity of adverse effects can be increased when Apomorphine is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Apomorphine is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Apomorphine is combined with Coumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Apomorphine is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Apomorphine is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Apomorphine is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Apomorphine is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Apomorphine is combined with Tioclomarol.
Warfarin The risk or severity of adverse effects can be increased when Apomorphine is combined with Warfarin.
Mirtazapine The risk or severity of hypotension can be increased when Mirtazapine is combined with Apomorphine.
Nicorandil Nicorandil may increase the hypotensive activities of Apomorphine.
Ethanol Apomorphine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Apomorphine 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 Apomorphine.
Fluvoxamine The risk or severity of adverse effects can be increased when Apomorphine is combined with Fluvoxamine.
Paroxetine The risk or severity of adverse effects can be increased when Apomorphine is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Apomorphine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Apomorphine is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Apomorphine is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Apomorphine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Apomorphine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Apomorphine is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Apomorphine.
Seproxetine The risk or severity of adverse effects can be increased when Apomorphine is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Apomorphine is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Apomorphine is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Apomorphine is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Apomorphine is combined with Alaproclate.
Citalopram The risk or severity of QTc prolongation can be increased when Apomorphine is combined with Citalopram.
Olanzapine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Olanzapine.
Clozapine The risk or severity of QTc prolongation can be increased when Apomorphine is combined with Clozapine.
Bifeprunox The therapeutic efficacy of Apomorphine can be decreased when used in combination with Bifeprunox.
Cariprazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Cariprazine.
Lumateperone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Lumateperone.
Sertindole The therapeutic efficacy of Apomorphine can be decreased when used in combination with Sertindole.
Lurasidone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Lurasidone.
Perospirone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Perospirone.
Blonanserin The therapeutic efficacy of Apomorphine can be decreased when used in combination with Blonanserin.
Melperone The therapeutic efficacy of Apomorphine can be decreased when used in combination with Melperone.
Zotepine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Zotepine.
Brilaroxazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Brilaroxazine.
Amisulpride The therapeutic efficacy of Apomorphine can be decreased when used in combination with Amisulpride.
Methylene blue Apomorphine may increase the serotonergic activities of Methylene blue.
Loxapine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Loxapine.
Promazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Promazine.
Prochlorperazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Prochlorperazine.
Chlorpromazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Chlorpromazine.
Fluphenazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Fluphenazine.
Trifluoperazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Trifluoperazine.
Perphenazine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Perphenazine.
Chlorprothixene The therapeutic efficacy of Apomorphine can be decreased when used in combination with Chlorprothixene.

Target Protein

D(4) dopamine receptor DRD4
D(2) dopamine receptor DRD2
D(3) dopamine receptor DRD3
D(1B) dopamine receptor DRD5
D(1A) dopamine receptor DRD1
Alpha-2C adrenergic receptor ADRA2C
Alpha-2B adrenergic receptor ADRA2B
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2B HTR2B
5-hydroxytryptamine receptor 2C HTR2C
Alpha-2A adrenergic receptor ADRA2A
5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 1B HTR1B

Referensi & Sumber

Synthesis reference: Narayanasamy Gurusamy, "Process for Making Apomorphine and Apocodeine." U.S. Patent US20100228032, issued September 09, 2010.
Artikel (PubMed)
  • PMID: 32104425
    Borkar N, Mu H, Holm R: Challenges and trends in apomorphine drug delivery systems for the treatment of Parkinson's disease. Asian J Pharm Sci. 2018 Nov;13(6):507-517. doi: 10.1016/j.ajps.2017.11.004. Epub 2017 Dec 6.
  • PMID: 14660177
    Thomas NL, Coughtrie MW: Sulfation of apomorphine by human sulfotransferases: evidence of a major role for the polymorphic phenol sulfotransferase, SULT1A1. Xenobiotica. 2003 Nov;33(11):1139-48. doi: 10.1080/00498250310001609192.
  • PMID: 20225277
    Fanali G, Rampoldi V, di Masi A, Bolli A, Lopiano L, Ascenzi P, Fasano M: Binding of anti-Parkinson's disease drugs to human serum albumin is allosterically modulated. IUBMB Life. 2010 May;62(5):371-6. doi: 10.1002/iub.317.
  • PMID: 27979722
    Jenner P, Katzenschlager R: Apomorphine - pharmacological properties and clinical trials in Parkinson's disease. Parkinsonism Relat Disord. 2016 Dec;33 Suppl 1:S13-S21. doi: 10.1016/j.parkreldis.2016.12.003. Epub 2016 Dec 13.
  • PMID: 15037665
    LeWitt PA: Subcutaneously administered apomorphine: pharmacokinetics and metabolism. Neurology. 2004 Mar 23;62(6 Suppl 4):S8-11. doi: 10.1212/wnl.62.6suppl4.s8.
  • PMID: 9617507
    van der Geest R, van Laar T, Kruger PP, Gubbens-Stibbe JM, Bodde HE, Roos RA, Danhof M: Pharmacokinetics, enantiomer interconversion, and metabolism of R-apomorphine in patients with idiopathic Parkinson's disease. Clin Neuropharmacol. 1998 May-Jun;21(3):159-68.
  • PMID: 24780865
    Haberzettl R, Fink H, Bert B: The murine serotonin syndrome - evaluation of responses to 5-HT-enhancing drugs in NMRI mice. Behav Brain Res. 2015 Jan 15;277:204-10. doi: 10.1016/j.bbr.2014.04.033. Epub 2014 Apr 27.
  • PMID: 36471
    Costall B, Naylor RJ, Nohria V: Hyperactivity response to apomorphine and amphetamine in the mouse: the importance of the nucleus accumbens and caudate-putamen. J Pharm Pharmacol. 1979 Apr;31(4):259-61. doi: 10.1111/j.2042-7158.1979.tb13494.x.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 31 • International brands: 3
Produk
  • Apokyn
    Injection • 30 mg/3mL • Subcutaneous • US • Approved
  • Apokyn
    Liquid • 10 mg/1mL • Subcutaneous • US • Approved
  • Apokyn
    Injection • 30 mg/3mL • Subcutaneous • US • Approved
  • Apomorphine Hydrocloride
    Injection • 30 mg/3mL • Subcutaneous • US • Generic • Approved
  • Kynmobi
    Film, soluble • 10 mg/1 • Sublingual • US • Approved
  • Kynmobi
    Film, soluble • 10 mg/1 • Sublingual • US • Approved
  • Kynmobi
    Film, soluble • 15 mg/1 • Sublingual • US • Approved
  • Kynmobi
    Film, soluble • 15 mg/1 • Sublingual • US • Approved
Menampilkan 8 dari 31 produk.
International Brands
  • Ixense — Takeda (discontinued)
  • Spontane
  • Uprima — Abbott (discontinued)

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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