Peringatan Keamanan

Oral LD50 of >500 mg/kg in mice L1102.

Blonanserin

DB09223

small molecule investigational

Deskripsi

Blonanserin is an atypical antipsychotic approved in Japan in January, 2008. It offers improved tolerability as it lacks side effects such as extrapyramidal symptoms, excessive sedation, or hypotension. As a second-generation (atypical) antipsychotic, it is significantly more efficacious in the treatment of the negative symptoms of schizophrenia compared to first-generation (typical) antipsychotics.

Struktur Molekul 2D

Berat 367.512
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Blonanserin has a half life of elimination of 10.7-16.2 h [A31487].
Volume Distribusi Blonanserin has a Vc of 9500 L and a Vt of 8560 L for a total Vd of 18060 L [A7841].
Klirens (Clearance) Blonanserin has a clearance of 1230 L/h [A7841].

Absorpsi

Blonanserin has a Tmax of 1.5 h and a bioavailablity of 55% A7841, A31487. Tmax has been observed to be prolonged and relative bioavailability increased when administered with food A7841.

Metabolisme

Blonanserin is mainly metabolized by CYP3A4 A31487. It undergoes hydoxylation of the cyclooctane ring as well as N-oxidation and N-deethylation of the piperazine ring. The N-deethylated and hydroxylated metabolites are active but to a lesser degree than the parent drug.

Rute Eliminasi

57% of blonanserin is excreted in the urine and 30% in the feces A31487. Only 5% of the drug in the feces is the parent drug with no parent drug excreted through the urine.

Interaksi Obat

1461 Data
Buprenorphine Blonanserin 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 Blonanserin.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Blonanserin.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Blonanserin.
Hydrocodone Blonanserin 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 Blonanserin.
Magnesium sulfate The therapeutic efficacy of Blonanserin can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Blonanserin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Blonanserin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Blonanserin.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Blonanserin.
Orphenadrine Blonanserin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Blonanserin 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 Blonanserin.
Rotigotine Blonanserin may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Blonanserin.
Sodium oxybate Blonanserin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Blonanserin 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 Blonanserin.
Thalidomide Blonanserin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Blonanserin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amisulpride Blonanserin may increase the antipsychotic activities of Amisulpride.
Methylphenidate The risk or severity of adverse effects can be increased when Blonanserin is combined with Methylphenidate.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Blonanserin.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Blonanserin.
Sulpiride Blonanserin may increase the antipsychotic activities of Sulpiride.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Blonanserin.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Blonanserin.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Blonanserin.
Mequitazine Blonanserin may increase the arrhythmogenic activities of Mequitazine.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Blonanserin.
Dicoumarol The risk or severity of adverse effects can be increased when Blonanserin is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Blonanserin is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Blonanserin is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Blonanserin is combined with Tioclomarol.
Phenprocoumon The risk or severity of adverse effects can be increased when Blonanserin is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Blonanserin is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Blonanserin is combined with 4-hydroxycoumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Blonanserin is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Blonanserin is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Blonanserin is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Blonanserin is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Blonanserin is combined with Diphenadione.
(S)-Warfarin The risk or severity of adverse effects can be increased when Blonanserin is combined with (S)-Warfarin.
Mirtazapine Blonanserin may increase the serotonergic activities of Mirtazapine.
Ethanol Blonanserin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Blonanserin 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 Blonanserin.
Fluvoxamine The risk or severity of adverse effects can be increased when Blonanserin is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Blonanserin is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Blonanserin is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Blonanserin is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Blonanserin is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Blonanserin is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Blonanserin is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Blonanserin is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Blonanserin is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Blonanserin.
Seproxetine The risk or severity of adverse effects can be increased when Blonanserin is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Blonanserin is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Blonanserin is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Blonanserin is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Blonanserin is combined with Alaproclate.
Carbidopa The therapeutic efficacy of Carbidopa can be decreased when used in combination with Blonanserin.
Cabergoline The therapeutic efficacy of Cabergoline can be decreased when used in combination with Blonanserin.
Tolcapone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Blonanserin.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Blonanserin.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Blonanserin.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Blonanserin.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Blonanserin.
Entacapone The therapeutic efficacy of Entacapone can be decreased when used in combination with Blonanserin.
Lisuride The therapeutic efficacy of Lisuride can be decreased when used in combination with Blonanserin.
Apomorphine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Blonanserin.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Blonanserin.
Progabide The therapeutic efficacy of Progabide can be decreased when used in combination with Blonanserin.
Selegiline The therapeutic efficacy of Selegiline can be decreased when used in combination with Blonanserin.
Memantine The therapeutic efficacy of Memantine can be decreased when used in combination with Blonanserin.
Pergolide The therapeutic efficacy of Pergolide can be decreased when used in combination with Blonanserin.
Levodopa The therapeutic efficacy of Levodopa can be decreased when used in combination with Blonanserin.
3,5-Dinitrocatechol The therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Blonanserin.
Etilevodopa The therapeutic efficacy of Etilevodopa can be decreased when used in combination with Blonanserin.
Safinamide The therapeutic efficacy of Safinamide can be decreased when used in combination with Blonanserin.
Ifenprodil The therapeutic efficacy of Ifenprodil can be decreased when used in combination with Blonanserin.
Dexetimide The therapeutic efficacy of Dexetimide can be decreased when used in combination with Blonanserin.
Opicapone The therapeutic efficacy of Opicapone can be decreased when used in combination with Blonanserin.
Piribedil The therapeutic efficacy of Piribedil can be decreased when used in combination with Blonanserin.
Benserazide The therapeutic efficacy of Benserazide can be decreased when used in combination with Blonanserin.
Tropatepine The therapeutic efficacy of Tropatepine can be decreased when used in combination with Blonanserin.
Melevodopa The therapeutic efficacy of Melevodopa can be decreased when used in combination with Blonanserin.
Dihydroergocryptine The therapeutic efficacy of Dihydroergocryptine can be decreased when used in combination with Blonanserin.
Phenglutarimide The therapeutic efficacy of Phenglutarimide can be decreased when used in combination with Blonanserin.
Mazaticol The therapeutic efficacy of Mazaticol can be decreased when used in combination with Blonanserin.
Etybenzatropine The therapeutic efficacy of Etybenzatropine can be decreased when used in combination with Blonanserin.
Budipine The therapeutic efficacy of Budipine can be decreased when used in combination with Blonanserin.
Bornaprine The therapeutic efficacy of Bornaprine can be decreased when used in combination with Blonanserin.
Etanautine The therapeutic efficacy of Etanautine can be decreased when used in combination with Blonanserin.
Dexpramipexole The therapeutic efficacy of Dexpramipexole can be decreased when used in combination with Blonanserin.
Bromocriptine The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Blonanserin.
Methylene blue Blonanserin may increase the serotonergic activities of Methylene blue.
Disopyramide Disopyramide may decrease the excretion rate of Blonanserin which could result in a higher serum level.

Target Protein

D(2) dopamine receptor DRD2
D(3) dopamine receptor DRD3
5-hydroxytryptamine receptor 2A HTR2A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23417765
    Wen YG, Shang DW, Xie HZ, Wang XP, Ni XJ, Zhang M, Lu W, Qiu C, Liu X, Li FF, Li X, Luo FT: Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake. Hum Psychopharmacol. 2013 Mar;28(2):134-41. doi: 10.1002/hup.2290. Epub 2013 Feb 18.
  • PMID: 20030420
    Deeks ED, Keating GM: Blonanserin: a review of its use in the management of schizophrenia. CNS Drugs. 2010 Jan;24(1):65-84. doi: 10.2165/11202620-000000000-00000.
  • PMID: 24099858
    Zhou Y, Liu M, Jiang J, Wang H, Hu P: Simultaneous determination of blonanserin and its four metabolites in human plasma using ultra-performance liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Nov 15;939:59-66. doi: 10.1016/j.jchromb.2013.09.007. Epub 2013 Sep 18.

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