Peringatan Keamanan

Prucalopride is well tolerated in doses reaching 10 times the recommended therapeutic dose and signs of overdose are thought to be stared by the presence of headaches, nausea and diarrhea.F2384 Carcinogenicity studies in mice indicated an increased incidence of mammary gland adenocarcinoma at a dose of 80 mg/kg/day. In rats, high doses were linked to increased incidence of benign adrenal pheochromocytoma, pituitary adenoma, pancreatic adenoma, hepatocellular adenoma and thyroid follicular tumors.F2386

For genotoxicity, prucalopride showed only one weak positive result in one of the five bacterial strain reverse mutation test at high concentrations.F2386 As well, there is no evidence of adverse effects on fertility, even in high doses.FDA label

Prucalopride

DB06480

small molecule approved

Deskripsi

Prucalopride is a dihydrobenzofurancarboxamide derivative from the benzofurane family that selectively stimulates 5-HT4 receptors and thus, it presents enterokinetic properties.A37348 The high selectivity of prucalopride allowed further development as it prevented the cardiac adverse reactions observed due to non-target effects of precedent therapies.A40254 Prucalopride was developed by Shire Development LLC and approved for use in Europe in 2009,A40250 in Canada on December 7, 2011 and by the FDA on December 17, 2018.L4880

Struktur Molekul 2D

Berat 367.87
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life of prucalopride is of around 18-20 hours.[A40255]
Volume Distribusi The mean volume of distribution of prucalopride is registered to be 623 L.[A40255]
Klirens (Clearance) Prucalopride renal clearance is reported to be of 17 L/h which actually exceeds the glomerular filtration rate of the kidney.[A40255]

Absorpsi

Prucalopride is well absorbed and it reaches maximum plasma concentration of 3.79ng/ml with a tmax of 2.77 hours after initial administration. It presents an AUC of 96.5 mn.h/ml.A40255 The bioavailability of prucalopride is of over 90% and this bioavailability does not get influenced by the ingestion of food.F2384

Metabolisme

Prucalopride is not extensively metabolized in the body and does not interact with the enzymes of the family of the cytochrome P450 enzymes nor the P glycoprotein.A37348 The metabolism of prucalopride only represents 6% of the administered dose and the remaining 94% is found as the unchanged drug.A40255 From studies, it was reported the recovery of 8 metabolites being the major metabolite R107504 which is formed after the O-demethylation and oxidation of the resulting alcohol to a carboxylic acid.F2384

Rute Eliminasi

After maximum plasma concentration, prucalopride concentration decline in a biphasic manner. Prucalopride is mainly excreted by the urine, representing 84% of the administered dose while only 13% of the dose is recovered in feces.A40255

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1308 Data
Fluconazole The serum concentration of Prucalopride can be increased when it is combined with Fluconazole.
Sildenafil The serum concentration of Prucalopride can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Prucalopride can be increased when it is combined with Reserpine.
Ranolazine The serum concentration of Prucalopride can be increased when it is combined with Ranolazine.
Sorafenib The serum concentration of Prucalopride can be increased when it is combined with Sorafenib.
Loxapine The serum concentration of Prucalopride can be increased when it is combined with Loxapine.
Quinine The serum concentration of Prucalopride can be increased when it is combined with Quinine.
Ritonavir The serum concentration of Prucalopride can be increased when it is combined with Ritonavir.
Toremifene The serum concentration of Prucalopride can be increased when it is combined with Toremifene.
Simvastatin The serum concentration of Prucalopride can be increased when it is combined with Simvastatin.
Verapamil The serum concentration of Prucalopride can be increased when it is combined with Verapamil.
Tamoxifen The serum concentration of Prucalopride can be increased when it is combined with Tamoxifen.
Mifepristone The serum concentration of Prucalopride can be increased when it is combined with Mifepristone.
Vardenafil The serum concentration of Prucalopride can be increased when it is combined with Vardenafil.
Tacrolimus The serum concentration of Prucalopride can be increased when it is combined with Tacrolimus.
Conivaptan The serum concentration of Prucalopride can be increased when it is combined with Conivaptan.
Quinidine The serum concentration of Prucalopride can be increased when it is combined with Quinidine.
Zonisamide The serum concentration of Prucalopride can be increased when it is combined with Zonisamide.
Tipranavir The serum concentration of Prucalopride can be increased when it is combined with Tipranavir.
Ketoconazole The serum concentration of Prucalopride can be increased when it is combined with Ketoconazole.
Amiodarone The serum concentration of Prucalopride can be increased when it is combined with Amiodarone.
Carvedilol The serum concentration of Prucalopride can be increased when it is combined with Carvedilol.
Itraconazole The serum concentration of Prucalopride can be increased when it is combined with Itraconazole.
Propafenone The serum concentration of Prucalopride can be increased when it is combined with Propafenone.
Clarithromycin The serum concentration of Prucalopride can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Prucalopride can be increased when it is combined with Saquinavir.
Lapatinib The serum concentration of Prucalopride can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Prucalopride can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Prucalopride can be increased when it is combined with Mibefradil.
Lopinavir The serum concentration of Prucalopride can be increased when it is combined with Lopinavir.
Biricodar The serum concentration of Prucalopride can be increased when it is combined with Biricodar.
Dronedarone The serum concentration of Prucalopride can be increased when it is combined with Dronedarone.
Nilotinib The serum concentration of Prucalopride can be increased when it is combined with Nilotinib.
Elacridar The serum concentration of Prucalopride can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Prucalopride can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Prucalopride can be increased when it is combined with Vandetanib.
Telaprevir The serum concentration of Prucalopride can be increased when it is combined with Telaprevir.
Zosuquidar The serum concentration of Prucalopride can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Prucalopride can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Prucalopride can be increased when it is combined with Temsirolimus.
Simeprevir The serum concentration of Prucalopride can be increased when it is combined with Simeprevir.
Isavuconazonium The serum concentration of Prucalopride can be increased when it is combined with Isavuconazonium.
Brefeldin A The serum concentration of Prucalopride can be increased when it is combined with Brefeldin A.
Ticagrelor The serum concentration of Prucalopride can be increased when it is combined with Ticagrelor.
Ivacaftor The serum concentration of Prucalopride can be increased when it is combined with Ivacaftor.
Lomitapide The serum concentration of Prucalopride can be increased when it is combined with Lomitapide.
Crizotinib The serum concentration of Prucalopride can be increased when it is combined with Crizotinib.
Vemurafenib The serum concentration of Prucalopride can be increased when it is combined with Vemurafenib.
Linagliptin The serum concentration of Prucalopride can be increased when it is combined with Linagliptin.
Mirabegron The serum concentration of Prucalopride can be increased when it is combined with Mirabegron.
Regorafenib The serum concentration of Prucalopride can be increased when it is combined with Regorafenib.
Enzalutamide The serum concentration of Prucalopride can be decreased when it is combined with Enzalutamide.
Ponatinib The serum concentration of Prucalopride can be increased when it is combined with Ponatinib.
Canagliflozin The serum concentration of Prucalopride can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Prucalopride can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Prucalopride can be increased when it is combined with Ledipasvir.
Vorapaxar The serum concentration of Prucalopride can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Prucalopride can be increased when it is combined with Suvorexant.
Netupitant The serum concentration of Prucalopride can be increased when it is combined with Netupitant.
Cobicistat The serum concentration of Prucalopride can be increased when it is combined with Cobicistat.
Palbociclib The serum concentration of Prucalopride can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Prucalopride can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Prucalopride can be increased when it is combined with Niguldipine.
Lumacaftor The serum concentration of Prucalopride can be increased when it is combined with Lumacaftor.
Rolapitant The serum concentration of Prucalopride can be increased when it is combined with Rolapitant.
Venetoclax The serum concentration of Prucalopride can be increased when it is combined with Venetoclax.
Asunaprevir The serum concentration of Prucalopride can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Prucalopride can be increased when it is combined with Velpatasvir.
Isavuconazole The serum concentration of Prucalopride can be increased when it is combined with Isavuconazole.
Neratinib The serum concentration of Prucalopride can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Prucalopride can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Prucalopride can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Prucalopride can be increased when it is combined with Glasdegib.
Voxilaprevir The serum concentration of Prucalopride can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Prucalopride can be increased when it is combined with Sarecycline.
Erdafitinib The serum concentration of Prucalopride can be increased when it is combined with Erdafitinib.
Rucaparib The metabolism of Prucalopride can be decreased when combined with Rucaparib.
Laniquidar The serum concentration of Prucalopride can be increased when it is combined with Laniquidar.
Enasidenib The serum concentration of Prucalopride can be increased when it is combined with Enasidenib.
Pibrentasvir The serum concentration of Prucalopride can be increased when it is combined with Pibrentasvir.
Glecaprevir The serum concentration of Prucalopride can be increased when it is combined with Glecaprevir.
Dexniguldipine The serum concentration of Prucalopride can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Prucalopride can be increased when it is combined with ONT-093.
Ivosidenib The metabolism of Prucalopride can be increased when combined with Ivosidenib.
Methylene blue The serum concentration of Prucalopride can be increased when it is combined with Methylene blue.
Cethromycin The serum concentration of Prucalopride can be increased when it is combined with Cethromycin.
Entrectinib The serum concentration of Prucalopride can be increased when it is combined with Entrectinib.
Fedratinib The serum concentration of Prucalopride can be increased when it is combined with Fedratinib.
Istradefylline The serum concentration of Prucalopride can be increased when it is combined with Istradefylline.
Lasmiditan The serum concentration of Prucalopride can be increased when it is combined with Lasmiditan.
Cyclosporine The serum concentration of Prucalopride can be increased when it is combined with Cyclosporine.
Mefloquine The serum concentration of Prucalopride can be increased when it is combined with Mefloquine.
Clofazimine The serum concentration of Prucalopride can be increased when it is combined with Clofazimine.
Carfilzomib The serum concentration of Prucalopride can be increased when it is combined with Carfilzomib.
Elagolix The serum concentration of Prucalopride can be increased when it is combined with Elagolix.
Everolimus The serum concentration of Prucalopride can be increased when it is combined with Everolimus.
Favipiravir The serum concentration of Prucalopride can be increased when it is combined with Favipiravir.
Arsenic trioxide The serum concentration of Prucalopride can be increased when it is combined with Arsenic trioxide.
Ripretinib The serum concentration of Prucalopride can be increased when it is combined with Ripretinib.
Pralsetinib The serum concentration of Prucalopride can be increased when it is combined with Pralsetinib.

Target Protein

5-hydroxytryptamine receptor 4 HTR4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 24308797
    Shin A, Camilleri M, Kolar G, Erwin P, West CP, Murad MH: Systematic review with meta-analysis: highly selective 5-HT4 agonists (prucalopride, velusetrag or naronapride) in chronic constipation. Aliment Pharmacol Ther. 2014 Feb;39(3):239-53. doi: 10.1111/apt.12571. Epub 2013 Dec 5.
  • PMID: 29147138
    Omer A, Quigley EMM: An update on prucalopride in the treatment of chronic constipation. Therap Adv Gastroenterol. 2017 Nov;10(11):877-887. doi: 10.1177/1756283X17734809. Epub 2017 Oct 16.
  • PMID: 11438309
    Briejer MR, Bosmans JP, Van Daele P, Jurzak M, Heylen L, Leysen JE, Prins NH, Schuurkes JA: The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. Eur J Pharmacol. 2001 Jun 29;423(1):71-83.
  • PMID: 11696108
    Briejer MR, Prins NH, Schuurkes JA: Effects of the enterokinetic prucalopride (R093877) on colonic motility in fasted dogs. Neurogastroenterol Motil. 2001 Oct;13(5):465-72.
  • PMID: 27127190
    Sajid MS, Hebbar M, Baig MK, Li A, Philipose Z: Use of Prucalopride for Chronic Constipation: A Systematic Review and Meta-analysis of Published Randomized, Controlled Trials. J Neurogastroenterol Motil. 2016 Jul 30;22(3):412-22. doi: 10.5056/jnm16004.
  • PMID: 27614912
    Flach S, Scarfe G, Dragone J, Ding J, Seymour M, Pennick M, Pankratz T, Troy S, Getsy J: A Phase I Study to Investigate the Absorption, Pharmacokinetics, and Excretion of (14)CPrucalopride After a Single Oral Dose in Healthy Volunteers. Clin Ther. 2016 Sep;38(9):2106-15. doi: 10.1016/j.clinthera.2016.08.003. Epub 2016 Sep 7.

Contoh Produk & Brand

Produk: 22 • International brands: 1
Produk
  • Apo-prucalopride
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Apo-prucalopride
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • Jamp Prucalopride
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Jamp Prucalopride
    Tablet • 2 mg • Oral • Canada • Generic • Approved
  • Motegrity
    Tablet, film coated • 1 mg/1 • Oral • US • Approved
  • Motegrity
    Tablet, film coated • 2 mg/1 • Oral • US • Approved
  • Nra-prucalopride
    Tablet • 1 mg • Oral • Canada • Approved
  • Nra-prucalopride
    Tablet • 2 mg • Oral • Canada • Approved
Menampilkan 8 dari 22 produk.
International Brands
  • Resolor — Shire Pharmaceuticals Ireland Ltd

Sekuens Gen/Protein (FASTA)

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