Peringatan Keamanan

Symptoms of overdose include lethargy, dystonia/spasm, tachycardia, bradycardia, and seizures. LD50=57.7 mg/kg (rat, oral) and 34 mg/kg (rat, intravenous).A1117,A1118,A1119

Risperidone

DB00734

small molecule approved investigational

Deskripsi

Risperidone is a second-generation antipsychotic (SGA) medication used in the treatment of a number of mood and mental health conditions including schizophrenia and bipolar disorder.L12885 It is one of the most widely used SGAs. Paliperidone, another commonly used SGA, is the primary active metabolite of risperidone (i.e. 9-hydroxyrisperidone).L12885

Schizophrenia and various mood disorders are thought to be caused by an excess of dopaminergic D2 and serotonergic 5-HT2A activity, resulting in overactivity of central mesolimbic pathways and mesocortical pathways, respectively. Risperidone is thought to reduce this overactivity through inhibition of dopaminergic D2 receptors and serotonergic 5-HT2A receptors in the brain.L12885

Risperidone binds with a very high affinity to 5-HT2A receptors, approximately 10-20 fold greater than the drug's binding affinity to D2 receptors, and carries lesser activity at several off-targets which may responsible for some of its undesirable effects.L12885

Struktur Molekul 2D

Berat 410.4845
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3 hours in extensive metabolizers[A31772] Up to 20 hours in poor metabolizers[A31772]
Volume Distribusi The volume of distribution of risperidone is approximately 1 to 2 L/kg.[L12885]
Klirens (Clearance) Risperidone is cleared by the kidneys. Clearance is decreased in the elderly and those with a creatinine clearance (ClCr) between 15-59 mL/min, in whom clearance is decreased by approximately 60%.[L1214]

Absorpsi

Well absorbed. The absolute oral bioavailability of risperidone is 70% (CV=25%). The relative oral bioavailability of risperidone from a tablet is 94% (CV=10%) when compared to a solution.L12885

Metabolisme

Extensively metabolized by hepatic cytochrome P450 2D6 isozyme to 9-hydroxyrisperidone (i.e. paliperidone), which has approximately the same receptor binding affinity as risperidone.A1118,A31772 Hydroxylation is dependent on debrisoquine 4-hydroxylase and metabolism is sensitive to genetic polymorphisms in debrisoquine 4-hydroxylase.A1119,A31772 Risperidone also undergoes N-dealkylation to a lesser extent.A1119,A31772

Rute Eliminasi

Risperidone is extensively metabolized in the liver. In healthy elderly subjects, renal clearance of both risperidone and 9-hydroxyrisperidone was decreased, and elimination half-lives are prolonged compared to young healthy subjects.A31772,L1214

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food does not affect the rate or extent of absorption.

Interaksi Obat

1755 Data
Aldesleukin Aldesleukin may increase the hypotensive activities of Risperidone.
Streptokinase Streptokinase may increase the hypotensive activities of Risperidone.
Valsartan Valsartan may increase the hypotensive activities of Risperidone.
Ramipril Ramipril may increase the hypotensive activities of Risperidone.
Esmolol Esmolol may increase the hypotensive activities of Risperidone.
Betaxolol Betaxolol may increase the hypotensive activities of Risperidone.
Reserpine Reserpine may increase the hypotensive activities of Risperidone.
Methyclothiazide Methyclothiazide may increase the hypotensive activities of Risperidone.
Metoprolol Metoprolol may increase the hypotensive activities of Risperidone.
Isradipine Isradipine may increase the hypotensive activities of Risperidone.
Olmesartan Olmesartan may increase the hypotensive activities of Risperidone.
Morphine Morphine may increase the hypotensive activities of Risperidone.
Ropivacaine Ropivacaine may increase the hypotensive activities of Risperidone.
Bupivacaine Bupivacaine may increase the hypotensive activities of Risperidone.
Chlorthalidone Chlorthalidone may increase the hypotensive activities of Risperidone.
Tolcapone Tolcapone may increase the hypotensive activities of Risperidone.
Nitroprusside Nitroprusside may increase the hypotensive activities of Risperidone.
Olanzapine Olanzapine may increase the hypotensive activities of Risperidone.
Atenolol Atenolol may increase the hypotensive activities of Risperidone.
Diltiazem Diltiazem may increase the hypotensive activities of Risperidone.
Minoxidil Minoxidil may increase the hypotensive activities of Risperidone.
Clozapine The risk or severity of QTc prolongation can be increased when Risperidone is combined with Clozapine.
Amlodipine Amlodipine may increase the hypotensive activities of Risperidone.
Triamterene Triamterene may increase the hypotensive activities of Risperidone.
Nimodipine Nimodipine may increase the hypotensive activities of Risperidone.
Nisoldipine Nisoldipine may increase the hypotensive activities of Risperidone.
Spironolactone Spironolactone may increase the hypotensive activities of Risperidone.
Nitric Oxide Nitric Oxide may increase the hypotensive activities of Risperidone.
Bendroflumethiazide Bendroflumethiazide may increase the hypotensive activities of Risperidone.
Prazosin Prazosin may increase the hypotensive activities of Risperidone.
Imipramine Imipramine may increase the hypotensive activities of Risperidone.
Chlorpromazine Chlorpromazine may increase the hypotensive activities of Risperidone.
Nabilone Nabilone may increase the hypotensive activities of Risperidone.
Sotalol Sotalol may increase the hypotensive activities of Risperidone.
Fosinopril Fosinopril may increase the hypotensive activities of Risperidone.
Trandolapril Trandolapril may increase the hypotensive activities of Risperidone.
Metolazone Metolazone may increase the hypotensive activities of Risperidone.
Lercanidipine Lercanidipine may increase the hypotensive activities of Risperidone.
Benazepril Benazepril may increase the hypotensive activities of Risperidone.
Propranolol Propranolol may increase the hypotensive activities of Risperidone.
Enalapril Enalapril may increase the hypotensive activities of Risperidone.
Doxazosin Doxazosin may increase the hypotensive activities of Risperidone.
Amiloride Amiloride may increase the hypotensive activities of Risperidone.
Labetalol Labetalol may increase the hypotensive activities of Risperidone.
Thiopental Thiopental may increase the hypotensive activities of Risperidone.
Bisoprolol Bisoprolol may increase the hypotensive activities of Risperidone.
Nicardipine Nicardipine may increase the hypotensive activities of Risperidone.
Clofarabine Clofarabine may increase the hypotensive activities of Risperidone.
Dexmedetomidine Dexmedetomidine may increase the hypotensive activities of Risperidone.
Mecamylamine Mecamylamine may increase the hypotensive activities of Risperidone.
Losartan Losartan may increase the hypotensive activities of Risperidone.
Thioridazine Thioridazine may increase the hypotensive activities of Risperidone.
Amphotericin B Amphotericin B may increase the hypotensive activities of Risperidone.
Moexipril Moexipril may increase the hypotensive activities of Risperidone.
Phentolamine Phentolamine may increase the hypotensive activities of Risperidone.
Tizanidine Tizanidine may increase the hypotensive activities of Risperidone.
Methazolamide Methazolamide may increase the hypotensive activities of Risperidone.
Tamsulosin Tamsulosin may increase the hypotensive activities of Risperidone.
Sufentanil Sufentanil may increase the hypotensive activities of Risperidone.
Apomorphine Apomorphine may increase the hypotensive activities of Risperidone.
Lisinopril Lisinopril may increase the hypotensive activities of Risperidone.
Nitroglycerin Nitroglycerin may increase the hypotensive activities of Risperidone.
Mannitol Mannitol may increase the hypotensive activities of Risperidone.
Tranylcypromine Tranylcypromine may increase the hypotensive activities of Risperidone.
Isoflurane Isoflurane may increase the hypotensive activities of Risperidone.
Tretinoin The risk or severity of elevated intracranial pressure can be increased when Risperidone is combined with Tretinoin.
Hydroflumethiazide Hydroflumethiazide may increase the hypotensive activities of Risperidone.
Phenelzine Phenelzine may increase the hypotensive activities of Risperidone.
Perindopril Perindopril may increase the hypotensive activities of Risperidone.
Candesartan cilexetil Candesartan cilexetil may increase the hypotensive activities of Risperidone.
Tolazoline Tolazoline may increase the hypotensive activities of Risperidone.
Fenoldopam Fenoldopam may increase the hypotensive activities of Risperidone.
Indapamide Indapamide may increase the hypotensive activities of Risperidone.
Propofol Propofol may increase the hypotensive activities of Risperidone.
Conivaptan Conivaptan may increase the hypotensive activities of Risperidone.
Eprosartan Eprosartan may increase the hypotensive activities of Risperidone.
Chlorothiazide Chlorothiazide may increase the hypotensive activities of Risperidone.
Quinapril Quinapril may increase the hypotensive activities of Risperidone.
Isosorbide dinitrate Isosorbide dinitrate may increase the hypotensive activities of Risperidone.
Remifentanil Remifentanil may increase the hypotensive activities of Risperidone.
Levosimendan Levosimendan may increase the hypotensive activities of Risperidone.
Phenoxybenzamine Phenoxybenzamine may increase the hypotensive activities of Risperidone.
Pindolol Pindolol may increase the hypotensive activities of Risperidone.
Telmisartan Telmisartan may increase the hypotensive activities of Risperidone.
Methyldopa Methyldopa may increase the hypotensive activities of Risperidone.
Dipyridamole Dipyridamole may increase the hypotensive activities of Risperidone.
Hydrochlorothiazide Hydrochlorothiazide may increase the hypotensive activities of Risperidone.
Levobupivacaine Levobupivacaine may increase the hypotensive activities of Risperidone.
Guanfacine Guanfacine may increase the hypotensive activities of Risperidone.
Isosorbide mononitrate Isosorbide mononitrate may increase the hypotensive activities of Risperidone.
Felodipine Felodipine may increase the hypotensive activities of Risperidone.
Irbesartan Irbesartan may increase the hypotensive activities of Risperidone.
Selegiline Selegiline may increase the hypotensive activities of Risperidone.
Nitrendipine Nitrendipine may increase the hypotensive activities of Risperidone.
Iloprost Iloprost may increase the hypotensive activities of Risperidone.
Papaverine Papaverine may increase the hypotensive activities of Risperidone.
Nifedipine Nifedipine may increase the hypotensive activities of Risperidone.
Amiodarone Amiodarone may increase the hypotensive activities of Risperidone.
Diazoxide Diazoxide may increase the hypotensive activities of Risperidone.
Carvedilol Carvedilol may increase the hypotensive activities of Risperidone.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
Alpha-1B adrenergic receptor ADRA1B
Alpha-2B adrenergic receptor ADRA2B
Alpha-1A adrenergic receptor ADRA1A
Alpha-2C adrenergic receptor ADRA2C
Histamine H1 receptor HRH1
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 1D HTR1D
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 7 HTR7
D(1A) dopamine receptor DRD1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 16004936
    Altschuler EL, Kast RE: The atypical antipsychotic agents ziprasidone correction of zisprasidone, risperdone and olanzapine as treatment for and prophylaxis against progressive multifocal leukoencephalopathy. Med Hypotheses. 2005;65(3):585-6.
  • PMID: 19113797
    Bostwick JR, Guthrie SK, Ellingrod VL: Antipsychotic-induced hyperprolactinemia. Pharmacotherapy. 2009 Jan;29(1):64-73. doi: 10.1592/phco.29.1.64.
  • PMID: 15907153
    Fenton C, Scott LJ: Risperidone: a review of its use in the treatment of bipolar mania. CNS Drugs. 2005;19(5):429-44.
  • PMID: 19562274
    Kemp DE, Canan F, Goldstein BI, McIntyre RS: Long-acting risperidone: a review of its role in the treatment of bipolar disorder. Adv Ther. 2009 Jun;26(6):588-99. doi: 10.1007/s12325-009-0039-0. Epub 2009 Jun 26.
  • PMID: 16716128
    Szarfman A, Tonning JM, Levine JG, Doraiswamy PM: Atypical antipsychotics and pituitary tumors: a pharmacovigilance study. Pharmacotherapy. 2006 Jun;26(6):748-58.
  • PMID: 18537577
    Urichuk L, Prior TI, Dursun S, Baker G: Metabolism of atypical antipsychotics: involvement of cytochrome p450 enzymes and relevance for drug-drug interactions. Curr Drug Metab. 2008 Jun;9(5):410-8.
  • PMID: 14610521
    Yamanouchi Y, Iwata N, Suzuki T, Kitajima T, Ikeda M, Ozaki N: Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone. Pharmacogenomics J. 2003;3(6):356-61.
  • PMID: 9725965
    Acri AA, Henretig FM: Effects of risperidone in overdose. Am J Emerg Med. 1998 Sep;16(5):498-501.
Menampilkan 8 dari 14 artikel.

Contoh Produk & Brand

Produk: 787 • International brands: 5
Produk
  • Act Risperidone
    Tablet • 0.25 mg • Oral • Canada • Approved
  • Act Risperidone
    Tablet • 0.5 mg • Oral • Canada • Approved
  • Act Risperidone
    Tablet • 1 mg • Oral • Canada • Approved
  • Act Risperidone
    Tablet • 2 mg • Oral • Canada • Approved
  • Act Risperidone
    Tablet • 3 mg • Oral • Canada • Approved
  • Act Risperidone
    Tablet • 4 mg • Oral • Canada • Approved
  • Ag-risperidone
    Tablet • 0.25 mg • Oral • Canada • Generic • Approved
  • Ag-risperidone
    Tablet • 0.5 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 787 produk.
International Brands
  • Risperidal M-Tab — Janssen
  • Risperin — Gador
  • Rispolept
  • Rispolin
  • Sequinan

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