Asenapine

DB06216

small molecule approved

Deskripsi

Developed by Schering-Plough after its merger with Organon International, asenapine is a sublingually administered, atypical antipsychotic for treatment of schizophrenia and acute mania associated with bipolar disorder. Asenapine also belongs to the dibenzo-oxepino pyrrole class. It is also for severe post-traumatic stress disorder nightmares in soldiers as an off-label use. FDA approved on August 13, 2009.

Struktur Molekul 2D

Berat 285.77
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 24 hours (range of 13.4 - 39.2 hours)
Volume Distribusi 20-25 L/kg
Klirens (Clearance) -

Absorpsi

Cmax, single 5 mg dose = 4 ng/mL (within 1 hour); Bioavailability, sublingual administration = 35%; Bioavailability, oral administration (swallowed) = <2%; Time to steady state, 5 mg = 3 days; Peak plasma concentration occurs within 0.5 to 1.5 hours. Doubling dose of asenapine results in 1.7-fold increase in maximum concentration and exposure. Drinking water within 2-5 minutes post administration of asenapine results in a decrease in exposure.

Metabolisme

Asenapine is oxidized via CYP1A2 and undergoes direct glucuronidation via UGT1A4. Oxidation via CYP1A2 is asenapine's primary mode of metabolism.

Rute Eliminasi

Urine (50%) and feces (50%)

Interaksi Makanan

1 Data
  • 1. Take separate from meals. Do not have food or water for 10 minutes after administration.

Interaksi Obat

1716 Data
Fluvoxamine The serum concentration of Asenapine can be increased when it is combined with Fluvoxamine.
Deferasirox The serum concentration of Asenapine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Asenapine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Asenapine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Asenapine can be decreased when it is combined with Teriflunomide.
Valsartan Asenapine may decrease the antihypertensive activities of Valsartan.
Ramipril Asenapine may decrease the antihypertensive activities of Ramipril.
Remikiren Asenapine may decrease the antihypertensive activities of Remikiren.
Torasemide Asenapine may decrease the antihypertensive activities of Torasemide.
Guanadrel Asenapine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Asenapine may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Asenapine may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Asenapine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Asenapine may decrease the antihypertensive activities of Minoxidil.
Bendroflumethiazide Asenapine may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Asenapine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Asenapine may decrease the antihypertensive activities of Trandolapril.
Metolazone Asenapine may decrease the antihypertensive activities of Metolazone.
Benazepril Asenapine may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Asenapine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Asenapine may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Asenapine may decrease the antihypertensive activities of Mecamylamine.
Lisinopril Asenapine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Asenapine may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Asenapine may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Asenapine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Asenapine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Asenapine may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Asenapine may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Asenapine may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Asenapine may decrease the antihypertensive activities of Quinapril.
Telmisartan Asenapine may decrease the antihypertensive activities of Telmisartan.
Trichlormethiazide Asenapine may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Asenapine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Asenapine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Asenapine may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Asenapine may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Asenapine may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Asenapine may decrease the antihypertensive activities of Polythiazide.
Cilazapril Asenapine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Asenapine may decrease the antihypertensive activities of Saprisartan.
Spirapril Asenapine may decrease the antihypertensive activities of Spirapril.
Tienilic acid Asenapine may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Asenapine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Asenapine may decrease the antihypertensive activities of Temocapril.
Nicorandil Asenapine may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Asenapine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Asenapine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Asenapine may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Asenapine may decrease the antihypertensive activities of Imidapril.
BQ-123 Asenapine may decrease the antihypertensive activities of BQ-123.
Zofenopril Asenapine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Asenapine may decrease the antihypertensive activities of Guanoxan.
Delapril Asenapine may decrease the antihypertensive activities of Delapril.
Vincamine Asenapine may decrease the antihypertensive activities of Vincamine.
Linsidomine Asenapine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Asenapine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Asenapine may decrease the antihypertensive activities of Tolonidine.
Endralazine Asenapine may decrease the antihypertensive activities of Endralazine.
Cadralazine Asenapine may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Asenapine may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Asenapine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Asenapine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Asenapine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Asenapine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Asenapine may decrease the antihypertensive activities of Muzolimine.
Xipamide Asenapine may decrease the antihypertensive activities of Xipamide.
Candesartan Asenapine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Asenapine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Asenapine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Asenapine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Asenapine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Asenapine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Asenapine may decrease the antihypertensive activities of Quinaprilat.
Furosemide Asenapine may decrease the antihypertensive activities of Furosemide.
Enalapril Asenapine may decrease the antihypertensive activities of Enalapril.
Captopril Asenapine may decrease the antihypertensive activities of Captopril.
Bosentan Asenapine may decrease the antihypertensive activities of Bosentan.
Eplerenone Asenapine may decrease the antihypertensive activities of Eplerenone.
Irbesartan Asenapine may decrease the antihypertensive activities of Irbesartan.
Guanethidine Asenapine may decrease the antihypertensive activities of Guanethidine.
Hydralazine Asenapine may decrease the antihypertensive activities of Hydralazine.
Debrisoquine Asenapine may decrease the antihypertensive activities of Debrisoquine.
Sitaxentan Asenapine may decrease the antihypertensive activities of Sitaxentan.
Ambrisentan Asenapine may decrease the antihypertensive activities of Ambrisentan.
Pinacidil Asenapine may decrease the antihypertensive activities of Pinacidil.
Riociguat Asenapine may decrease the antihypertensive activities of Riociguat.
Macitentan Asenapine may decrease the antihypertensive activities of Macitentan.
Aliskiren Asenapine may decrease the antihypertensive activities of Aliskiren.
Selexipag Asenapine may decrease the antihypertensive activities of Selexipag.
Levamlodipine Asenapine may decrease the antihypertensive activities of Levamlodipine.
Buthiazide Asenapine may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Asenapine may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Asenapine 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 Asenapine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
Hydrocodone Asenapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Asenapine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Asenapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 1B HTR1B
5-hydroxytryptamine receptor 2B HTR2B
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 5A HTR5A
5-hydroxytryptamine receptor 6 HTR6
5-hydroxytryptamine receptor 7 HTR7
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
D(1A) dopamine receptor DRD1
Alpha-1A adrenergic receptor ADRA1A
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
Histamine H1 receptor HRH1
Histamine H2 receptor HRH2
Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18418367
    Huang M, Li Z, Dai J, Shahid M, Wong EH, Meltzer HY: Asenapine increases dopamine, norepinephrine, and acetylcholine efflux in the rat medial prefrontal cortex and hippocampus. Neuropsychopharmacology. 2008 Nov;33(12):2934-45. doi: 10.1038/npp.2008.20. Epub 2008 Apr 16.
  • PMID: 18308814
    Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28.
  • PMID: 17940749
    Franberg O, Wiker C, Marcus MM, Konradsson A, Jardemark K, Schilstrom B, Shahid M, Wong EH, Svensson TH: Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology (Berl). 2008 Feb;196(3):417-29. Epub 2007 Oct 17.
  • PMID: 23356509
    Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29.

Contoh Produk & Brand

Produk: 43 • International brands: 0
Produk
  • Asenapine
    Tablet • 2.5 mg/1 • Sublingual • US • Generic • Approved
  • Asenapine
    Tablet • 5 mg/1 • Sublingual • US • Generic • Approved
  • Asenapine
    Tablet • 10 mg/1 • Sublingual • US • Generic • Approved
  • Asenapine
    Tablet • 5 mg/1 • Sublingual • US • Generic • Approved
  • Asenapine
    Tablet • 10 mg/1 • Sublingual • US • Generic • Approved
  • Asenapine
    Tablet • 5 mg/1 • Sublingual • US • Generic • Approved
  • Asenapine
    Tablet • 10 mg/1 • Sublingual • US • Generic • Approved
  • Asenapine
    Tablet • 5 mg/1 • Sublingual • US • Generic • Approved
Menampilkan 8 dari 43 produk.

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