Peringatan Keamanan

During the clinical trials, some patients received posaconazole up to 1600 mg/day with no adverse events noted that were different from the lower doses. In addition, accidental overdose was noted in one patient who took 1200 mg BID for 3 days. No related adverse events were noted by the investigator.

Posaconazole

DB01263

small molecule approved investigational vet_approved

Deskripsi

Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients.

Struktur Molekul 2D

Berat 700.7774
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Posaconazole is eliminated with a mean half-life (t½) of 35 hours (range 20 to 66 hours).
Volume Distribusi * 1774 L
Klirens (Clearance) * 32 L/hr * 51 L/hr [Single-Dose Suspension Administration of 200 mg, fasted] * 21 L/hr [Single-Dose Suspension Administration of 200 mg, nonfat meal] * 14 L/hr [Single-Dose Suspension Administration of 200 mg, high fat meal] * 91 L/hr [Single-Dose Suspension Administration of 400 mg, fasted] * 43 L/hr [Single-Dose Suspension Administration of 400 mg with liquid nutritional supplement (14 g fat)]

Absorpsi

Posaconazole is absorbed with a median Tmax of approximately 3 to 5 hours.

Metabolisme

Posaconazole primarily circulates as the parent compound in plasma. Of the circulating metabolites, the majority are glucuronide conjugates formed via UDP glucuronidation (phase 2 enzymes). Posaconazole does not have any major circulating oxidative (CYP450 mediated) metabolites. The excreted metabolites in urine and feces account for ~17% of the administered radiolabeled dose.

Rute Eliminasi

The excreted metabolites in urine and feces account for ~17% of the administered radiolabeled dose.

Interaksi Makanan

1 Data
  • 1. Take with food. Posaconazole suspension can also be taken with a nutritional supplement drink or carbonated beverage if a full meal cannot be consumed.

Interaksi Obat

1101 Data
Amphotericin B The therapeutic efficacy of Amphotericin B can be decreased when used in combination with Posaconazole.
Didanosine Didanosine can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Posaconazole.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Posaconazole.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Posaconazole.
Pantoprazole Pantoprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Omeprazole Omeprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lansoprazole Lansoprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Esomeprazole Esomeprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexlansoprazole Dexlansoprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexrabeprazole Dexrabeprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ilaprazole Ilaprazole can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Posaconazole.
Colchicine The metabolism of Colchicine can be decreased when combined with Posaconazole.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Posaconazole.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Posaconazole.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Posaconazole.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Posaconazole.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Posaconazole.
Vindesine The metabolism of Vindesine can be decreased when combined with Posaconazole.
Vinorelbine The metabolism of Vinorelbine can be decreased when combined with Posaconazole.
Vincristine The metabolism of Vincristine can be decreased when combined with Posaconazole.
Vinblastine The metabolism of Vinblastine can be decreased when combined with Posaconazole.
Vintafolide The metabolism of Vintafolide can be decreased when combined with Posaconazole.
Vinflunine The metabolism of Vinflunine can be decreased when combined with Posaconazole.
Vincamine The metabolism of Vincamine can be decreased when combined with Posaconazole.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Posaconazole.
Cimetidine Cimetidine can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sucralfate Sucralfate can cause a decrease in the absorption of Posaconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Efavirenz The serum concentration of Posaconazole can be decreased when it is combined with Efavirenz.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Posaconazole.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Posaconazole.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Posaconazole.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Posaconazole.
Methysergide The serum concentration of Methysergide can be increased when it is combined with Posaconazole.
Cabergoline The serum concentration of Cabergoline can be increased when it is combined with Posaconazole.
Dihydroergotamine The serum concentration of Dihydroergotamine can be increased when it is combined with Posaconazole.
Methylergometrine The serum concentration of Methylergometrine can be increased when it is combined with Posaconazole.
Lisuride The serum concentration of Lisuride can be increased when it is combined with Posaconazole.
Ergotamine The serum concentration of Ergotamine can be increased when it is combined with Posaconazole.
Ergoloid mesylate The serum concentration of Ergoloid mesylate can be increased when it is combined with Posaconazole.
Pergolide The serum concentration of Pergolide can be increased when it is combined with Posaconazole.
Bromocriptine The serum concentration of Bromocriptine can be increased when it is combined with Posaconazole.
Ergometrine The serum concentration of Ergometrine can be increased when it is combined with Posaconazole.
Lysergic acid diethylamide The serum concentration of Lysergic acid diethylamide can be increased when it is combined with Posaconazole.
Dihydroergocornine The serum concentration of Dihydroergocornine can be increased when it is combined with Posaconazole.
Dihydroergocristine The serum concentration of Dihydroergocristine can be increased when it is combined with Posaconazole.
Dihydroergocryptine The serum concentration of Dihydroergocryptine can be increased when it is combined with Posaconazole.
Terguride The serum concentration of Terguride can be increased when it is combined with Posaconazole.
Atorvastatin The serum concentration of Atorvastatin can be increased when it is combined with Posaconazole.
Metoclopramide The serum concentration of Posaconazole can be decreased when it is combined with Metoclopramide.
Astemizole The serum concentration of Astemizole can be increased when it is combined with Posaconazole.
Boceprevir The serum concentration of Boceprevir can be increased when it is combined with Posaconazole.
Terfenadine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Terfenadine.
Goserelin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Goserelin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Moxifloxacin.
Sulfisoxazole The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Sulfisoxazole.
Sulpiride The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Sulpiride.
Droperidol The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Posaconazole.
Fluorouracil The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Perflutren.
Atropine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Atropine.
Adenosine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Adenosine.
Pentamidine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Pentamidine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Gadobenic acid.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Nalidixic acid.
Cinoxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Cinoxacin.
Levosimendan The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Levosimendan.
Mesoridazine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Mesoridazine.
Desloratadine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Desloratadine.
Lomefloxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Lomefloxacin.
Dimenhydrinate The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Dimenhydrinate.
Papaverine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Papaverine.
Gemifloxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Gemifloxacin.
Ofloxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Ofloxacin.
Flecainide The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Flecainide.
Probucol The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Probucol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Aceprometazine.
Terlipressin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Terlipressin.
Lofexidine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Lofexidine.
Pracinostat The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Pracinostat.
Technetium Tc-99m ciprofloxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Technetium Tc-99m ciprofloxacin.
Garenoxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Garenoxacin.
Tedisamil The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Tedisamil.
Tucidinostat The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Tucidinostat.
Telavancin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Telavancin.
Nemonoxacin The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Nemonoxacin.
Antazoline The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Antazoline.
Butriptyline The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Butriptyline.
Melperone The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Melperone.
Amifampridine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Amifampridine.
Mocetinostat The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Mocetinostat.
Entinostat The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Entinostat.
CUDC-101 The risk or severity of QTc prolongation can be increased when Posaconazole is combined with CUDC-101.
Simendan The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Simendan.
Ricolinostat The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Ricolinostat.
Mizolastine The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Mizolastine.
Abexinostat The risk or severity of QTc prolongation can be increased when Posaconazole is combined with Abexinostat.

Target Protein

Lanosterol 14-alpha demethylase ERG11

Referensi & Sumber

Synthesis reference: Dominic De Souza, "PREPARATION OF POSACONAZOLE INTERMEDIATES." U.S. Patent US20130203994, issued August 08, 2013.
Artikel (PubMed)
  • PMID: 17251531
    Cornely OA, Maertens J, Winston DJ, Perfect J, Ullmann AJ, Walsh TJ, Helfgott D, Holowiecki J, Stockelberg D, Goh YT, Petrini M, Hardalo C, Suresh R, Angulo-Gonzalez D: Posaconazole vs. fluconazole or itraconazole prophylaxis in patients with neutropenia. N Engl J Med. 2007 Jan 25;356(4):348-59.
  • PMID: 17251530
    Ullmann AJ, Lipton JH, Vesole DH, Chandrasekar P, Langston A, Tarantolo SR, Greinix H, Morais de Azevedo W, Reddy V, Boparai N, Pedicone L, Patino H, Durrant S: Posaconazole or fluconazole for prophylaxis in severe graft-versus-host disease. N Engl J Med. 2007 Jan 25;356(4):335-47.
  • PMID: 20622401
    Bhattacharya M, Rajeshwari K, Dhingra B: Posaconazole. J Postgrad Med. 2010 Apr-Jun;56(2):163-7. doi: 10.4103/0022-3859.65281.
  • PMID: 18457464
    Frampton JE, Scott LJ: Posaconazole : a review of its use in the prophylaxis of invasive fungal infections. Drugs. 2008;68(7):993-1016.
  • PMID: 18035188
    Schiller DS, Fung HB: Posaconazole: an extended-spectrum triazole antifungal agent. Clin Ther. 2007 Sep;29(9):1862-86.
  • PMID: 17516880
    Kwon DS, Mylonakis E: Posaconazole: a new broad-spectrum antifungal agent. Expert Opin Pharmacother. 2007 Jun;8(8):1167-78.
  • PMID: 16107193
    Groll AH, Walsh TJ: Posaconazole: clinical pharmacology and potential for management of fungal infections. Expert Rev Anti Infect Ther. 2005 Aug;3(4):467-87.
  • PMID: 18713852
    Rachwalski EJ, Wieczorkiewicz JT, Scheetz MH: Posaconazole: an oral triazole with an extended spectrum of activity. Ann Pharmacother. 2008 Oct;42(10):1429-38. doi: 10.1345/aph.1L005. Epub 2008 Aug 19.
Menampilkan 8 dari 9 artikel.

Contoh Produk & Brand

Produk: 57 • International brands: 1
Produk
  • Apo-posaconazole
    Tablet, delayed release • 100 mg • Oral • Canada • Generic • Approved
  • Gln-posaconazole
    Tablet, delayed release • 100 mg • Oral • Canada • Approved
  • Jamp Posaconazole
    Suspension • 40 mg / mL • Oral • Canada • Generic • Approved
  • Mint-posaconazole
    Tablet, delayed release • 100 mg • Oral • Canada • Generic • Approved
  • Noxafil
    Suspension • 40 mg/1mL • Oral • US • Approved
  • Noxafil
    Tablet, coated • 100 mg/1 • Oral • US • Approved
  • Noxafil
    Solution • 18 mg/1mL • Intravenous • US • Approved
  • Noxafil
    Powder, for suspension • 300 mg/1 • Oral • US • Approved
Menampilkan 8 dari 57 produk.
International Brands
  • Noxafil

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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