Peringatan Keamanan

Frequently experienced adverse effects include extrapyramidal symptoms, insomnia, and drowsiness. More serious adverse effect include neuroleptic malignant syndrome A19676. Oral LD50 value in rats is 870 mg/kg MSDS.

Perospirone

DB08922

small molecule experimental

Deskripsi

Perospirone is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist. Dainippon Sumitomo Pharma developed perospirone in Japan in 2001 for the treatment of acute schizophrenia and bipolar mania as well as chronic schizophrenia. It is commonly present as the hydrated hydrochloride salt form. Classified as a neuroleptic agent, perospirone is shown to be effective against positive, negative and general symptoms in patients with schizophrenia A19676. It is also shown to be less associated with extrapyramidal symptoms as a side effect compared to DB00502.

Struktur Molekul 2D

Berat 426.58
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half life is approximately 1.9 hours following oral ingestion of 8mg perospirone [A19677].
Volume Distribusi The mean volume of distribution following oral administration of 32 mg/day of perospirone is 1733L, with values ranging from 356-5246 L. It is shown to cross the placenta and be secreted into milk in pregnant rats [A19676].
Klirens (Clearance) Apparent clearance rate is approximately 425.5 ± 150.3 L/h in patients receiving a single oral dose of 8mg perospirone [A19683].

Absorpsi

Perospirone is rapidly absorbed following oral administration with the time to reach peak plasma concentration of 0.8 to 1.5 hours. A single oral dose of 8mg perospirone results in peak plasma concentration of 5.7 ug/L A19677. Perospirone is not reported to be accumulated after repeated dosing.

Metabolisme

Perospirone undergoes rapid and extensive first-pass metabolism in the liver; the metabolic pathways involve hydroxylation, N-dealkylation, and S-oxidation, which are catalyzed by CYP1A1, 2C8, 2D6, and 3A4. CYP3A4 is reported to have highest level of contribution in perospirone metabolism. Hydroxyperospirone is formed from hydroxylation of the the cyclohexane-1,2-dicarboximide moiety and retains pharmacological action by mediating antiserotonergic effects, although with lower affinity A19676.

Rute Eliminasi

Perospirone is mainly excreted via renal elimination. 0.4% of of total dose is excreted as unchanged drug following oral administration of 8mg perospirone A19677.

Farmakogenomik

1 Varian
HTR1A (rs6295)

The presence of this polymorphism in HTR1A may indicate a higher level of efficacy in improving negative symptoms of schizophrenia when treated with perospirone.

Interaksi Obat

1150 Data
Buprenorphine Perospirone 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 Perospirone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Perospirone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Perospirone.
Hydrocodone Perospirone 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 Perospirone.
Magnesium sulfate The therapeutic efficacy of Perospirone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Perospirone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Perospirone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Perospirone.
Mirtazapine Perospirone 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 Perospirone.
Orphenadrine Perospirone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Perospirone 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 Perospirone.
Rotigotine Perospirone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Perospirone.
Sodium oxybate Perospirone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Perospirone 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 Perospirone.
Thalidomide Perospirone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Perospirone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amisulpride Perospirone may increase the antipsychotic activities of Amisulpride.
Methylphenidate The risk or severity of adverse effects can be increased when Perospirone is combined with Methylphenidate.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Perospirone is combined with Dexmethylphenidate.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Perospirone.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Perospirone.
Sulpiride Perospirone may increase the antipsychotic activities of Sulpiride.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Perospirone.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Perospirone.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Perospirone.
Mequitazine Perospirone may increase the arrhythmogenic activities of Mequitazine.
Mifepristone The serum concentration of Perospirone can be increased when it is combined with Mifepristone.
Mirabegron The serum concentration of Perospirone can be increased when it is combined with Mirabegron.
Ethanol Perospirone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Perospirone 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 Perospirone.
Zimelidine The risk or severity of adverse effects can be increased when Perospirone is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Perospirone is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Perospirone is combined with Seproxetine.
Citalopram The risk or severity of adverse effects can be increased when Perospirone is combined with Citalopram.
Trazodone The risk or severity of adverse effects can be increased when Perospirone is combined with Trazodone.
Sertraline The risk or severity of adverse effects can be increased when Perospirone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Perospirone is combined with Sibutramine.
Milnacipran The risk or severity of adverse effects can be increased when Perospirone is combined with Milnacipran.
Desvenlafaxine The serum concentration of Perospirone can be increased when it is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Levomilnacipran is combined with Perospirone.
Indalpine The risk or severity of adverse effects can be increased when Perospirone is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Perospirone is combined with Alaproclate.
Carbidopa The therapeutic efficacy of Carbidopa can be decreased when used in combination with Perospirone.
Cabergoline The therapeutic efficacy of Cabergoline can be decreased when used in combination with Perospirone.
Tolcapone The therapeutic efficacy of Tolcapone can be decreased when used in combination with Perospirone.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Perospirone.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Perospirone.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Perospirone.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Perospirone.
Entacapone The therapeutic efficacy of Entacapone can be decreased when used in combination with Perospirone.
Lisuride The therapeutic efficacy of Lisuride can be decreased when used in combination with Perospirone.
Apomorphine The therapeutic efficacy of Apomorphine can be decreased when used in combination with Perospirone.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Perospirone.
Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Perospirone.
Memantine The therapeutic efficacy of Memantine can be decreased when used in combination with Perospirone.
Pergolide The therapeutic efficacy of Pergolide can be decreased when used in combination with Perospirone.
Levodopa The therapeutic efficacy of Levodopa can be decreased when used in combination with Perospirone.
Rasagiline The therapeutic efficacy of Rasagiline can be decreased when used in combination with Perospirone.
3,5-Dinitrocatechol The therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Perospirone.
Etilevodopa The therapeutic efficacy of Etilevodopa can be decreased when used in combination with Perospirone.
Ifenprodil The therapeutic efficacy of Ifenprodil can be decreased when used in combination with Perospirone.
Dexetimide The therapeutic efficacy of Dexetimide can be decreased when used in combination with Perospirone.
Opicapone The therapeutic efficacy of Opicapone can be decreased when used in combination with Perospirone.
Piribedil The therapeutic efficacy of Piribedil can be decreased when used in combination with Perospirone.
Benserazide The therapeutic efficacy of Benserazide can be decreased when used in combination with Perospirone.
Tropatepine The therapeutic efficacy of Tropatepine can be decreased when used in combination with Perospirone.
Melevodopa The therapeutic efficacy of Melevodopa can be decreased when used in combination with Perospirone.
Dihydroergocryptine The therapeutic efficacy of Dihydroergocryptine can be decreased when used in combination with Perospirone.
Phenglutarimide The therapeutic efficacy of Phenglutarimide can be decreased when used in combination with Perospirone.
Mazaticol The therapeutic efficacy of Mazaticol can be decreased when used in combination with Perospirone.
Etybenzatropine The therapeutic efficacy of Etybenzatropine can be decreased when used in combination with Perospirone.
Budipine The therapeutic efficacy of Budipine can be decreased when used in combination with Perospirone.
Bornaprine The therapeutic efficacy of Bornaprine can be decreased when used in combination with Perospirone.
Etanautine The therapeutic efficacy of Etanautine can be decreased when used in combination with Perospirone.
Dexpramipexole The therapeutic efficacy of Dexpramipexole can be decreased when used in combination with Perospirone.
Bromocriptine The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Perospirone.
Trospium The metabolism of Perospirone can be decreased when combined with Trospium.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Perospirone.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Perospirone.
Tolterodine The metabolism of Perospirone can be decreased when combined with Tolterodine.
Tiotropium The metabolism of Perospirone can be decreased when combined with Tiotropium.
Solifenacin The metabolism of Perospirone can be decreased when combined with Solifenacin.
Fesoterodine The metabolism of Perospirone can be decreased when combined with Fesoterodine.
Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Perospirone.
Revefenacin The metabolism of Revefenacin can be decreased when combined with Perospirone.
Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Perospirone.
Zopiclone The risk or severity of adverse effects can be increased when Perospirone is combined with Zopiclone.
Zolmitriptan The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Perospirone.
Mazindol The risk or severity of adverse effects can be increased when Mazindol is combined with Perospirone.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Perospirone.
Sumatriptan The risk or severity of adverse effects can be increased when Sumatriptan is combined with Perospirone.
Naratriptan The risk or severity of adverse effects can be increased when Naratriptan is combined with Perospirone.
Rizatriptan The risk or severity of adverse effects can be increased when Rizatriptan is combined with Perospirone.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
5-hydroxytryptamine receptor 1A HTR1A
Histamine H1 receptor HRH1
D(4) dopamine receptor DRD4
Alpha-1 adrenergic receptors ADRA1A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15257064
    Yasui-Furukori N, Furukori H, Nakagami T, Saito M, Inoue Y, Kaneko S, Tateishi T: Steady-state pharmacokinetics of a new antipsychotic agent perospirone and its active metabolite, and its relationship with prolactin response. Ther Drug Monit. 2004 Aug;26(4):361-5.
  • PMID: 11463136
    Onrust SV, McClellan K: Perospirone. CNS Drugs. 2001;15(4):329-37; discussion 338.
  • PMID: 1975278
    Hirose A, Kato T, Ohno Y, Shimizu H, Tanaka H, Nakamura M, Katsube J: Pharmacological actions of SM-9018, a new neuroleptic drug with both potent 5-hydroxytryptamine2 and dopamine2 antagonistic actions. Jpn J Pharmacol. 1990 Jul;53(3):321-9.
  • PMID: 23812802
    Kishi T, Iwata N: Efficacy and tolerability of perospirone in schizophrenia: a systematic review and meta-analysis of randomized controlled trials. CNS Drugs. 2013 Sep;27(9):731-41. doi: 10.1007/s40263-013-0085-7.
  • PMID: 17239041
    Takeuchi T, Furuta K, Hirasawa T, Masaki H, Yukizane T, Atsuta H, Nishikawa T: Perospirone in the treatment of patients with delirium. Psychiatry Clin Neurosci. 2007 Feb;61(1):67-70.
  • PMID: -
    Zou JJ, Liu L, Di B, Ding L, Zhu YB, Fan HW, Xiao DW, Wang GJ: Estimation of Perospirone in Human Plasma by LC–MS–MS and Its Application to Pharmacokinetics Study Chromatographia. 2008 August 1;68(3-4):239–243.
Textbook
  • ISBN: 978-0-7020-3471-8
    45. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 553-563). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Lullan — Dainippon Sumitomo Pharma

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