Peringatan Keamanan

The intraperitoneal lowest published toxic dose (TDLo) is 0.03 mg/kg in rats.L50532

In pre-marketing trials, there were eight cases of accidental or intentional overdose of iloperidone from doses ranging from 48 mg to 576 mg taken once and 292 mg taken over three days. There were no deaths from overdose. The largest confirmed single ingestion of iloperidone was 576 mg; however, no adverse physical effects were reported for this patient. The next largest confirmed ingestion of iloperidone was 438 mg over four days: This patient experienced extrapyramidal symptoms and a QTc interval of 507 msec with no cardiac sequelae. In general, reported signs and symptoms were those resulting from an exaggeration of the known pharmacological effects of iloperidone, including drowsiness, sedation, tachycardia, and hypotension. There is no known antidote for iloperidone overdose; thus, treatment should be supportive.L50527

Iloperidone

DB04946

small molecule approved

Deskripsi

Iloperidone is a benzisoxazole A263557 and an atypical antipsychotic agent that was first approved by the FDA on May 6, 2009.A3024 It is considered to be a second-generation antipsychotic drug A263552 with multiple receptor binding profile, although it shows high affinity towards 5-HT2A and dopamine D2 receptors.A263547 Iloperidone is currently used to treat schizophrenia and manic or mixed episodes associated with bipolar disorder.L50527

Struktur Molekul 2D

Berat 426.4806
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The observed mean elimination half-lives for iloperidone, P88, and P95 in CYP2D6 extensive metabolizers (EM) are 18, 26, and 23 hours, respectively. The mean half-lives of iloperidone, P88, and P95 in CYP2D6 poor metabolizers (PM) are 33, 37, and 31 hours, respectively.[L50527]
Volume Distribusi The apparent volume of distribution ranges from 1340 L to 2800 L.[L50527]
Klirens (Clearance) Iloperidone has an apparent clearance of 47 to 102 L/h.[L50527]

Absorpsi

Iloperidone is well-absorbed following oral administration.L50527 Oral bioavailability is approximately 36% in humans.A3024 The relative availability of the tablet formulation compared to the oral solution is 96%.L50527 The Tmax is two to four hours with single dosing and 1.5 hours with multiple dosing.A3024 A high-fat meal can delay the Tmax of iloperidone and its active metabolite, P88, by one and two hours, respectively; however, food has negligible effects on drug Cmax and AUC.L50527

Metabolisme

Iloperidone is mainly metabolized in the liver.L50527 It primarily undergoes three major biotransformation pathways: carbonyl reduction to produce P88, CYP2D6-mediated hydroxylation to produce P95, and CYP3A4-mediated O-demethylation to produce P89.A3024 P88 and P95 are the two major metabolites. P95 represents 47.9% of the AUC of iloperidone and its metabolites in plasma at steady-state for extensive metabolizers (EM) and 25% for poor metabolizers (PM). P88 is an active metabolite with an in vitro receptor binding profile that is comparable to the parent drug: It accounts for 19.5% and 34% of total plasma exposure in EM and PM, respectively.L50527

Rute Eliminasi

The main route of elimination is renal.A3024 About 58.2% and 45.1% of the drug were found in urine in extensive metabolizers (EM) and poor metabolizers (PM), respectively. Feces accounted for 19.9% (EM) to 22.1% (PM) of the dosed radioactivity.L50527

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Alcohol may worsen the CNS effects of iloperidone, such as dizziness.
  • 2. Take with or without food. A high-fat meals may delay the Tmax of iloperidone and its metabolites, without significantly changing the Cmax or AUC.

Interaksi Obat

1716 Data
Valsartan Iloperidone may decrease the antihypertensive activities of Valsartan.
Ramipril Iloperidone may decrease the antihypertensive activities of Ramipril.
Remikiren Iloperidone may decrease the antihypertensive activities of Remikiren.
Torasemide Iloperidone may decrease the antihypertensive activities of Torasemide.
Guanadrel Iloperidone may decrease the antihypertensive activities of Guanadrel.
Olmesartan Iloperidone may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Iloperidone may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Iloperidone may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Iloperidone may decrease the antihypertensive activities of Minoxidil.
Bendroflumethiazide Iloperidone may decrease the antihypertensive activities of Bendroflumethiazide.
Fosinopril Iloperidone may decrease the antihypertensive activities of Fosinopril.
Trandolapril Iloperidone may decrease the antihypertensive activities of Trandolapril.
Metolazone Iloperidone may decrease the antihypertensive activities of Metolazone.
Benazepril Iloperidone may decrease the antihypertensive activities of Benazepril.
Cyclothiazide Iloperidone may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Iloperidone may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Iloperidone may decrease the antihypertensive activities of Mecamylamine.
Lisinopril Iloperidone may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Iloperidone may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Iloperidone may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Iloperidone may decrease the antihypertensive activities of Cryptenamine.
Perindopril Iloperidone may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Iloperidone may decrease the antihypertensive activities of Candesartan cilexetil.
Eprosartan Iloperidone may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Iloperidone may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Iloperidone may decrease the antihypertensive activities of Quinapril.
Telmisartan Iloperidone may decrease the antihypertensive activities of Telmisartan.
Trichlormethiazide Iloperidone may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Iloperidone may decrease the antihypertensive activities of Deserpidine.
Pentolinium Iloperidone may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Iloperidone may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Iloperidone may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Iloperidone may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Iloperidone may decrease the antihypertensive activities of Polythiazide.
Cilazapril Iloperidone may decrease the antihypertensive activities of Cilazapril.
Saprisartan Iloperidone may decrease the antihypertensive activities of Saprisartan.
Spirapril Iloperidone may decrease the antihypertensive activities of Spirapril.
Tienilic acid Iloperidone may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Iloperidone may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Iloperidone may decrease the antihypertensive activities of Temocapril.
Nicorandil Iloperidone may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Iloperidone may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Iloperidone may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Iloperidone may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Iloperidone may decrease the antihypertensive activities of Imidapril.
BQ-123 Iloperidone may decrease the antihypertensive activities of BQ-123.
Dihydralazine Iloperidone may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Iloperidone may decrease the antihypertensive activities of Zofenopril.
Guanoxan Iloperidone may decrease the antihypertensive activities of Guanoxan.
Delapril Iloperidone may decrease the antihypertensive activities of Delapril.
Vincamine Iloperidone may decrease the antihypertensive activities of Vincamine.
Linsidomine Iloperidone may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Iloperidone may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Iloperidone may decrease the antihypertensive activities of Tolonidine.
Endralazine Iloperidone may decrease the antihypertensive activities of Endralazine.
Cadralazine Iloperidone may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Iloperidone may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Iloperidone may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Iloperidone may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Iloperidone may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Iloperidone may decrease the antihypertensive activities of Guanoclor.
Muzolimine Iloperidone may decrease the antihypertensive activities of Muzolimine.
Xipamide Iloperidone may decrease the antihypertensive activities of Xipamide.
Candesartan Iloperidone may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Iloperidone may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Iloperidone may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Iloperidone may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Iloperidone may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Iloperidone may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Iloperidone may decrease the antihypertensive activities of Quinaprilat.
Furosemide Iloperidone may decrease the antihypertensive activities of Furosemide.
Enalapril Iloperidone may decrease the antihypertensive activities of Enalapril.
Captopril Iloperidone may decrease the antihypertensive activities of Captopril.
Bosentan Iloperidone may decrease the antihypertensive activities of Bosentan.
Guanethidine Iloperidone may decrease the antihypertensive activities of Guanethidine.
Pinacidil Iloperidone may decrease the antihypertensive activities of Pinacidil.
Riociguat Iloperidone may decrease the antihypertensive activities of Riociguat.
Macitentan Iloperidone may decrease the antihypertensive activities of Macitentan.
Aliskiren Iloperidone may decrease the antihypertensive activities of Aliskiren.
Selexipag Iloperidone may decrease the antihypertensive activities of Selexipag.
Buthiazide Iloperidone may decrease the antihypertensive activities of Buthiazide.
Azilsartan medoxomil Iloperidone may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Iloperidone 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 Iloperidone.
Dronabinol The metabolism of Iloperidone can be decreased when combined with Dronabinol.
Droperidol The risk or severity of hypotension can be increased when Droperidol is combined with Iloperidone.
Hydrocodone Iloperidone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Iloperidone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine The risk or severity of hypotension can be increased when Methotrimeprazine is combined with Iloperidone.
Metyrosine Iloperidone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Iloperidone.
Paraldehyde Iloperidone 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 Iloperidone.
Rotigotine Iloperidone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Iloperidone.
Sodium oxybate Iloperidone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Iloperidone 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 Iloperidone.
Thalidomide Iloperidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
5-hydroxytryptamine receptor 1A HTR1A
5-hydroxytryptamine receptor 2C HTR2C
5-hydroxytryptamine receptor 6 HTR6
5-hydroxytryptamine receptor 7 HTR7
Alpha-1A adrenergic receptor ADRA1A
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
D(1A) dopamine receptor DRD1
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
D(1B) dopamine receptor DRD5
Histamine H1 receptor HRH1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 21034370
    Citrome L: Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion. Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1551-64. doi: 10.1517/17425255.2010.531259. Epub 2010 Nov 1.
  • PMID: 24600226
    Rado JT, Janicak PG: Long-term efficacy and safety of iloperidone: an update. Neuropsychiatr Dis Treat. 2014 Feb 26;10:409-15. doi: 10.2147/NDT.S37824. eCollection 2014.
  • PMID: 11093363
    Jain KK: An assessment of iloperidone for the treatment of schizophrenia. Expert Opin Investig Drugs. 2000 Dec;9(12):2935-43. doi: 10.1517/13543784.9.12.2935.
  • PMID: 19624791
    Citrome L: Iloperidone for schizophrenia: a review of the efficacy and safety profile for this newly commercialised second-generation antipsychotic. Int J Clin Pract. 2009 Aug;63(8):1237-48. doi: 10.1111/j.1742-1241.2009.02142.x.
  • PMID: 18095919
    Albers LJ, Musenga A, Raggi MA: Iloperidone: a new benzisoxazole atypical antipsychotic drug. Is it novel enough to impact the crowded atypical antipsychotic market? Expert Opin Investig Drugs. 2008 Jan;17(1):61-75. doi: 10.1517/13543784.17.1.61.

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