Peringatan Keamanan

The possibility of obtundation, seizures, or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis.

Paliperidone

DB01267

small molecule approved

Deskripsi

Paliperidone is the primary active metabolite of risperidone. The mechanism of action is unknown but it is likely to act via a similar pathway to risperidone. It has been proposed that the drug's therapeutic activity in schizophrenia is mediated through a combination of central dopamine Type 2 (D2) and serotonin Type 2 (5HT2A) receptor antagonism. Paliperidone is also active as an antagonist at alpha 1 and alpha 2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. Paliperidone was approved by the FDA for treatment of schizophrenia on December 20, 2006. It is available as an extended-release tablet, a once-monthly intramuscular injection, an every-three-month intramuscular injection, and a twice-yearly gluteal injection.L16168,L37744,L4137,L37749

Struktur Molekul 2D

Berat 426.4839
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of paliperidone is approximately 23 hours.
Volume Distribusi * 487 L
Klirens (Clearance) -

Absorpsi

The absolute oral bioavailability of paliperidone following paliperidone administration is 28%.

Metabolisme

Although in vitro studies suggested a role for CYP2D6 and CYP3A4 in the metabolism of paliperidone, in vivo results indicate that these isozymes play a limited role in the overall elimination of paliperidone. Four primary metabolic pathways have been identified in vivo, none of which could be shown to account for more than 10% of the dose: dealkylation, hydroxylation, dehydrogenation, and benzisoxazole scission. Paliperidone does not undergo extensive metabolism and a significant portion of its metabolism occurs in the kidneys.

Rute Eliminasi

One week following administration of a single oral dose of 1 mg immediate-release 14C-paliperidone to 5 healthy volunteers, 59% (range 51% – 67%) of the dose was excreted unchanged into urine, 32% (26% – 41%) of the dose was recovered as metabolites, and 6% – 12% of the dose was not recovered.

Interaksi Makanan

1 Data
  • 1. Avoid alcohol.

Interaksi Obat

2169 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Paliperidone.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Paliperidone.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Paliperidone.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Paliperidone.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Paliperidone.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Paliperidone.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Paliperidone.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Paliperidone.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Paliperidone.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Paliperidone.
Silodosin The excretion of Silodosin can be decreased when combined with Paliperidone.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Paliperidone.
Valsartan Paliperidone may decrease the antihypertensive activities of Valsartan.
Ramipril Paliperidone may decrease the antihypertensive activities of Ramipril.
Remikiren Paliperidone may decrease the antihypertensive activities of Remikiren.
Guanadrel Paliperidone may decrease the antihypertensive activities of Guanadrel.
Olmesartan Paliperidone may decrease the antihypertensive activities of Olmesartan.
Minoxidil Paliperidone may decrease the antihypertensive activities of Minoxidil.
Trandolapril Paliperidone may decrease the antihypertensive activities of Trandolapril.
Benazepril Paliperidone may decrease the antihypertensive activities of Benazepril.
Candoxatril Paliperidone may decrease the antihypertensive activities of Candoxatril.
Nitroglycerin Paliperidone may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Paliperidone may decrease the antihypertensive activities of Cryptenamine.
Eprosartan Paliperidone may decrease the antihypertensive activities of Eprosartan.
Quinapril Paliperidone may decrease the antihypertensive activities of Quinapril.
Deserpidine Paliperidone may decrease the antihypertensive activities of Deserpidine.
Pentolinium Paliperidone may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Paliperidone may decrease the antihypertensive activities of Trimethaphan.
Saprisartan Paliperidone may decrease the antihypertensive activities of Saprisartan.
Spirapril Paliperidone may decrease the antihypertensive activities of Spirapril.
Diethylnorspermine Paliperidone may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Paliperidone may decrease the antihypertensive activities of Temocapril.
Rauwolfia serpentina root Paliperidone may decrease the antihypertensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Paliperidone may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Paliperidone may decrease the antihypertensive activities of Imidapril.
BQ-123 Paliperidone may decrease the antihypertensive activities of BQ-123.
Dihydralazine Paliperidone may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Paliperidone may decrease the antihypertensive activities of Zofenopril.
Guanoxan Paliperidone may decrease the antihypertensive activities of Guanoxan.
Delapril Paliperidone may decrease the antihypertensive activities of Delapril.
Vincamine Paliperidone may decrease the antihypertensive activities of Vincamine.
Linsidomine Paliperidone may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Paliperidone may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Paliperidone may decrease the antihypertensive activities of Tolonidine.
Endralazine Paliperidone may decrease the antihypertensive activities of Endralazine.
Cadralazine Paliperidone may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Paliperidone may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Paliperidone may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Paliperidone may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Paliperidone may decrease the antihypertensive activities of Guanoclor.
Tocopherylquinone Paliperidone may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Paliperidone may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Paliperidone may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Paliperidone may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Paliperidone may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Paliperidone may decrease the antihypertensive activities of Quinaprilat.
Bosentan Paliperidone may decrease the antihypertensive activities of Bosentan.
Irbesartan Paliperidone may decrease the antihypertensive activities of Irbesartan.
Sitaxentan Paliperidone may decrease the antihypertensive activities of Sitaxentan.
Pinacidil Paliperidone may decrease the antihypertensive activities of Pinacidil.
Riociguat The serum concentration of Riociguat can be increased when it is combined with Paliperidone.
Aliskiren Paliperidone may decrease the antihypertensive activities of Aliskiren.
Enalapril Paliperidone may decrease the antihypertensive activities of Enalapril.
Candesartan cilexetil Paliperidone may decrease the antihypertensive activities of Candesartan cilexetil.
Telmisartan Paliperidone may decrease the antihypertensive activities of Telmisartan.
Captopril Paliperidone may decrease the antihypertensive activities of Captopril.
Cilazapril Paliperidone may decrease the antihypertensive activities of Cilazapril.
Candesartan Paliperidone may decrease the antihypertensive activities of Candesartan.
Azilsartan medoxomil Paliperidone may decrease the antihypertensive activities of Azilsartan medoxomil.
Diazoxide Paliperidone may decrease the antihypertensive activities of Diazoxide.
Buprenorphine Paliperidone 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 Paliperidone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Paliperidone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Paliperidone.
Hydrocodone Paliperidone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Paliperidone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Paliperidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Paliperidone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Paliperidone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Paliperidone.
Orphenadrine Paliperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Paliperidone 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 Paliperidone.
Rotigotine Paliperidone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Paliperidone.
Sodium oxybate Paliperidone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Paliperidone 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 Paliperidone.
Thalidomide Paliperidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Paliperidone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Paliperidone.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Paliperidone.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Paliperidone.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Paliperidone.
Omapatrilat Paliperidone may decrease the antihypertensive activities of Omapatrilat.
Rescinnamine Paliperidone may decrease the antihypertensive activities of Rescinnamine.
Epicaptopril The risk or severity of hypertension can be increased when Paliperidone is combined with Epicaptopril.
Taxifolin The risk or severity of hypertension can be increased when Paliperidone is combined with Taxifolin.
1-benzylimidazole The risk or severity of hypertension can be increased when Paliperidone is combined with 1-benzylimidazole.
Saralasin The risk or severity of hypertension can be increased when Paliperidone is combined with Saralasin.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
D(2) dopamine receptor DRD2
D(4) dopamine receptor DRD4
D(3) dopamine receptor DRD3
5-hydroxytryptamine receptor 2C HTR2C
Histamine H1 receptor HRH1
Alpha-1A adrenergic receptor ADRA1A
Alpha-1B adrenergic receptor ADRA1B
5-hydroxytryptamine receptor 1D HTR1D
Alpha-2A adrenergic receptor ADRA2A
Alpha-2B adrenergic receptor ADRA2B
Alpha-2C adrenergic receptor ADRA2C
5-hydroxytryptamine receptor 1A HTR1A
D(1A) dopamine receptor DRD1
5-hydroxytryptamine receptor 7 HTR7

Referensi & Sumber

Synthesis reference: Santiago Ini, Naama Chasid, Kobi Chen, Osnat Porter-Kleks, "Pure paliperidone and processes for preparing thereof." U.S. Patent US20080171876, issued July 17, 2008.
Artikel (PubMed)
  • PMID: 20497747
    Jones MP, Nicholl D, Trakas K: Efficacy and tolerability of paliperidone ER and other oral atypical antipsychotics in schizophrenia. Int J Clin Pharmacol Ther. 2010 Jun;48(6):383-99.
  • 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.

Contoh Produk & Brand

Produk: 256 • International brands: 1
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International Brands
  • Invega Hafyera — Janssen Pharmaceutical Companies of Johnson & Johnson

Sekuens Gen/Protein (FASTA)

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