Peringatan Keamanan

Symptoms of overdose include photophobia and possible QTc prolongation.L9821, L15571 In case of overdose, supportive care and ECG monitoring are recommended. Activated charcoal may aid in the removal of unabsorbed drug. Voriconazole is cleared by hemodialysis at a rate of 121 mL/min which may be helpful in removing absorbed drug. Carcinogenicity studies found hepatocellular adenomas in female rats at doses of 50 mg/kg and hepatocellular carcinomas found in male rats at doses of 6 and 50 mg/kg. These doses are equivalent to 0.2 and 1.6 times the recommended maintenance dose (RMD). Studies in mice detected hepatocellular carcinomas in males at doses of 100 mg/kg or 1.4 times the RMD. Hepatocellular adenomas were detected in both male and female mice.

Voriconazole

DB00582

small molecule approved

Deskripsi

Voriconazole (Vfend, Pfizer) is a triazole antifungal medication used to treat serious fungal infections.L15571 It is used to treat invasive fungal infections that are generally seen in patients who are immunocompromised. These include invasive candidiasis, invasive aspergillosis, and emerging fungal infections. The increased affinity of voriconazole for 14-alpha sterol demethylase makes it useful against some fluconazole-resistant organisms.A236050

Voriconazole was approved by the FDA under the trade name Vfend on May 24, 2002.L34660

Struktur Molekul 2D

Berat 349.3105
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Voriconazole follows non-linear kinetics and has a terminal half-life of elimination which is dose-dependent.[L9821]
Volume Distribusi The estimated volume of distribution of voriconazole is 4.6 L/kg [L9821]. Population pharmacokinetic studies estimate the median volume of distribution to be 77.6 L with the central compartment estimated at 1.07 L/kg [A227613] Voriconazole is known to achieve therapeutic concentrations in many tissues including the brain, lungs, liver, spleen, kidneys, and heart.
Klirens (Clearance) The clearance of voriconazole is estimated to be a mean of 5.25-7 L/h in healthy adults for the linear portion of the drug's kinetics.[A227613, A187880]

Absorpsi

The oral bioavailability is estimated to be 96% in healthy adultsL9821. Population pharmacokinetic studies report a reduced bioavailability pediatric patients with a mean of 61.8% (range 44.6–64.5%) thought to be due to differences in first-pass metabolism or due to differences in diet A227613. Of note, transplant patients also have reduced bioavailability but this is known to increase with time after transplantation and may be due in part to gastrointestinal upset from surgery and some transplant medications. Tmax is 1-2 hours with oral administration. When administered with a high-fat meal Cmax decreases by 34% and AUC by 24%. pH does not have an effect on absorption of voriconazole. Differences in Cmax and AUC have been observed between healthy adult males and females with Cmax increasing by 83% and AUC by 113% although this has not been observed to significantly impact medication safety profiles.

Metabolisme

Voriconazole undergoes extensive hepatic metabolism through cytochrome enzymes CYP2C9, CYP2C19, and CYP3A4. CYP2C19 mediates N-oxidation with an apparent Km of 14 ?M and an apparent Vmax of 0.22 nmol/min/nmol CYP2C19.A38618 Voriconazole N-oxide is the major circulating metabolite, accounting for 72% of radiolabeled metabolites found.L9821 CYP3A4 contributes to N-oxidation with a Km of 16 ?M and Vmax of 0.05 nmol/min/nmol CYP3A4 as well as 4-hydroxylation with a Km of 11 ?M and a Vmax of 0.10 nmol/min/nmol CYP3A4.A38618 CYP3A5 and CYP3A7 provide minor contributions to N-oxidation and 4-hydroxylation. The N-oxide and 4-hydroxylated metabolites undergo glucuronidation and are excreted through the urine with other minor glucuronidated metabolites.A19483

Rute Eliminasi

Voriconazole is eliminated via hepatic metabolism with less than 2% of the dose excreted unchanged in the urine.L9821

Farmakogenomik

3 Varian
CYP2C19 (rs12248560)

Patients with this genotype in CYP2C19 are ultra fast metabolizers and require higer doses of voriconazole to attain the therapeutic effect.

CYP2C19 (rs4244285)

The presence of this polymorphism in CYP2C19 is associated with poor metabolism of voriconazole.

CYP2C19 (rs4986893)

The presence of this polymorphism in CYP2C19 is associated with reduced or poor metabolism of voriconazole.

Interaksi Makanan

1 Data
  • 1. Take separate from meals. Take voriconazole at least one hour before or after eating for optimal absorption.

Interaksi Obat

1348 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Voriconazole.
Dabrafenib The serum concentration of Voriconazole can be decreased when it is combined with Dabrafenib.
Amphotericin B The therapeutic efficacy of Amphotericin B can be decreased when used in combination with Voriconazole.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Voriconazole.
Didanosine Didanosine can cause a decrease in the absorption of Voriconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Voriconazole.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Voriconazole.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Voriconazole.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Voriconazole.
Ivabradine The risk or severity of QTc prolongation and torsade de pointes can be increased when Voriconazole is combined with Ivabradine.
Ivacaftor The serum concentration of Ivacaftor can be increased when it is combined with Voriconazole.
Lurasidone The serum concentration of Lurasidone can be increased when it is combined with Voriconazole.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Voriconazole.
Olaparib The metabolism of Olaparib can be decreased when combined with Voriconazole.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Voriconazole.
Fluconazole The metabolism of Voriconazole can be decreased when combined with Fluconazole.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Voriconazole.
Pantoprazole The metabolism of Pantoprazole can be decreased when combined with Voriconazole.
Omeprazole The serum concentration of Omeprazole can be increased when it is combined with Voriconazole.
Lansoprazole The metabolism of Lansoprazole can be decreased when combined with Voriconazole.
Esomeprazole The metabolism of Esomeprazole can be decreased when combined with Voriconazole.
Rabeprazole The metabolism of Rabeprazole can be decreased when combined with Voriconazole.
Dexlansoprazole The metabolism of Dexlansoprazole can be decreased when combined with Voriconazole.
Dexrabeprazole The metabolism of Dexrabeprazole can be decreased when combined with Voriconazole.
Ilaprazole The metabolism of Ilaprazole can be decreased when combined with Voriconazole.
Luliconazole The serum concentration of Voriconazole can be increased when it is combined with Luliconazole.
Colchicine The metabolism of Colchicine can be decreased when combined with Voriconazole.
Fentanyl The serum concentration of Fentanyl can be increased when it is combined with Voriconazole.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Voriconazole.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Voriconazole.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Voriconazole.
Glimepiride The serum concentration of Glimepiride can be increased when it is combined with Voriconazole.
Acetohexamide The serum concentration of Acetohexamide can be increased when it is combined with Voriconazole.
Chlorpropamide The serum concentration of Chlorpropamide can be increased when it is combined with Voriconazole.
Tolazamide The serum concentration of Tolazamide can be increased when it is combined with Voriconazole.
Glyburide The serum concentration of Glyburide can be increased when it is combined with Voriconazole.
Glipizide The serum concentration of Glipizide can be increased when it is combined with Voriconazole.
Gliclazide The serum concentration of Gliclazide can be increased when it is combined with Voriconazole.
Tolbutamide The serum concentration of Tolbutamide can be increased when it is combined with Voriconazole.
Gliquidone The serum concentration of Gliquidone can be increased when it is combined with Voriconazole.
Glisoxepide The serum concentration of Glisoxepide can be increased when it is combined with Voriconazole.
Glibornuride The serum concentration of Glibornuride can be increased when it is combined with Voriconazole.
Carbutamide The serum concentration of Carbutamide can be increased when it is combined with Voriconazole.
Metahexamide The serum concentration of Metahexamide can be increased when it is combined with Voriconazole.
Butalbital The serum concentration of Voriconazole can be decreased when it is combined with Butalbital.
Pentobarbital The serum concentration of Voriconazole can be decreased when it is combined with Pentobarbital.
Secobarbital The serum concentration of Voriconazole can be decreased when it is combined with Secobarbital.
Methohexital The serum concentration of Voriconazole can be decreased when it is combined with Methohexital.
Thiopental The serum concentration of Voriconazole can be decreased when it is combined with Thiopental.
Primidone The serum concentration of Voriconazole can be decreased when it is combined with Primidone.
Methylphenobarbital The serum concentration of Voriconazole can be decreased when it is combined with Methylphenobarbital.
Thiamylal The serum concentration of Voriconazole can be decreased when it is combined with Thiamylal.
Phenobarbital The serum concentration of Voriconazole can be decreased when it is combined with Phenobarbital.
Amobarbital The serum concentration of Voriconazole can be decreased when it is combined with Amobarbital.
Hexobarbital The serum concentration of Voriconazole can be decreased when it is combined with Hexobarbital.
Barbital The serum concentration of Voriconazole can be decreased when it is combined with Barbital.
Barbexaclone The serum concentration of Voriconazole can be decreased when it is combined with Barbexaclone.
Butabarbital The serum concentration of Voriconazole can be decreased when it is combined with Butabarbital.
Venlafaxine The risk or severity of adverse effects can be increased when Voriconazole is combined with Venlafaxine.
Vindesine The metabolism of Vindesine can be decreased when combined with Voriconazole.
Vinorelbine The metabolism of Vinorelbine can be decreased when combined with Voriconazole.
Vincristine The metabolism of Vincristine can be decreased when combined with Voriconazole.
Vinblastine The metabolism of Vinblastine can be decreased when combined with Voriconazole.
Vintafolide The metabolism of Vintafolide can be decreased when combined with Voriconazole.
Vinflunine The metabolism of Vinflunine can be decreased when combined with Voriconazole.
Vincamine The metabolism of Vincamine can be decreased when combined with Voriconazole.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Voriconazole.
Oxycodone The risk or severity of adverse effects can be increased when Voriconazole is combined with Oxycodone.
Ritonavir The serum concentration of Voriconazole can be decreased when it is combined with Ritonavir.
Darunavir The serum concentration of Voriconazole can be decreased when it is combined with Darunavir.
Amprenavir The serum concentration of Voriconazole can be increased when it is combined with Amprenavir.
Fosamprenavir The serum concentration of Voriconazole can be increased when it is combined with Fosamprenavir.
Ibuprofen The serum concentration of Ibuprofen can be increased when it is combined with Voriconazole.
Dexibuprofen The serum concentration of Dexibuprofen can be increased when it is combined with Voriconazole.
Lopinavir The serum concentration of Voriconazole can be decreased when it is combined with Lopinavir.
Sirolimus The serum concentration of Sirolimus can be increased when it is combined with Voriconazole.
Temsirolimus The serum concentration of Temsirolimus can be increased when it is combined with Voriconazole.
Sucralfate Sucralfate can cause a decrease in the absorption of Voriconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Telaprevir The serum concentration of Telaprevir can be increased when it is combined with Voriconazole.
R,S-Warfarin alcohol Voriconazole may increase the anticoagulant activities of R,S-Warfarin alcohol.
S,R-Warfarin alcohol Voriconazole may increase the anticoagulant activities of S,R-Warfarin alcohol.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Voriconazole.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Voriconazole.
Ergoloid mesylate The serum concentration of Ergoloid mesylate can be increased when it is combined with Voriconazole.
Methylergometrine The serum concentration of Methylergometrine can be increased when it is combined with Voriconazole.
Lumacaftor The serum concentration of Voriconazole can be decreased when it is combined with Lumacaftor.
St. John's Wort The serum concentration of Voriconazole can be decreased when it is combined with St. John's Wort.
Goserelin The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Goserelin.
Moxifloxacin The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Moxifloxacin.
Sulfisoxazole The metabolism of Voriconazole can be decreased when combined with Sulfisoxazole.
Sulpiride The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Sulpiride.
Droperidol The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Droperidol.
Oxaliplatin The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Voriconazole.
Ciprofloxacin The metabolism of Voriconazole can be decreased when combined with Ciprofloxacin.
Fluorouracil The metabolism of Voriconazole can be decreased when combined with Fluorouracil.
Perflutren The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Perflutren.
Atropine The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Atropine.
Adenosine The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Adenosine.
Gadobenic acid The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Gadobenic acid.
Nalidixic acid The risk or severity of QTc prolongation can be increased when Voriconazole is combined with Nalidixic acid.

Target Protein

Lanosterol 14-alpha demethylase ERG11

Referensi & Sumber

Synthesis reference: Venkataraman Sundaram, Venkata Bhaskara Rao Uppala, Surya Prabhakar Akundi, Venkateswarlu Muvva, Vijayawardhan Chitta, Alekhya Donthula, Manoj Ramesh Kharkar, Surya Narayana Devarakonda, Subba Reddy Peddireddy, "Process For Preparing Voriconazole." U.S. Patent US20080194820, issued August 14, 2008.
Artikel (PubMed)
  • PMID: 12167683
    Herbrecht R, Denning DW, Patterson TF, Bennett JE, Greene RE, Oestmann JW, Kern WV, Marr KA, Ribaud P, Lortholary O, Sylvester R, Rubin RH, Wingard JR, Stark P, Durand C, Caillot D, Thiel E, Chandrasekar PH, Hodges MR, Schlamm HT, Troke PF, de Pauw B: Voriconazole versus amphotericin B for primary therapy of invasive aspergillosis. N Engl J Med. 2002 Aug 8;347(6):408-15.
  • PMID: 16231256
    Patterson TF, Boucher HW, Herbrecht R, Denning DW, Lortholary O, Ribaud P, Rubin RH, Wingard JR, DePauw B, Schlamm HT, Troke P, Bennett JE: Strategy of following voriconazole versus amphotericin B therapy with other licensed antifungal therapy for primary treatment of invasive aspergillosis: impact of other therapies on outcome. Clin Infect Dis. 2005 Nov 15;41(10):1448-52. Epub 2005 Oct 13.
  • PMID: 16243088
    Kullberg BJ, Sobel JD, Ruhnke M, Pappas PG, Viscoli C, Rex JH, Cleary JD, Rubinstein E, Church LW, Brown JM, Schlamm HT, Oborska IT, Hilton F, Hodges MR: Voriconazole versus a regimen of amphotericin B followed by fluconazole for candidaemia in non-neutropenic patients: a randomised non-inferiority trial. Lancet. 2005 Oct 22-28;366(9495):1435-42.
  • PMID: 11577374
    Ally R, Schurmann D, Kreisel W, Carosi G, Aguirrebengoa K, Dupont B, Hodges M, Troke P, Romero AJ: A randomized, double-blind, double-dummy, multicenter trial of voriconazole and fluconazole in the treatment of esophageal candidiasis in immunocompromised patients. Clin Infect Dis. 2001 Nov 1;33(9):1447-54. Epub 2001 Sep 26.
  • PMID: 11807146
    Walsh TJ, Pappas P, Winston DJ, Lazarus HM, Petersen F, Raffalli J, Yanovich S, Stiff P, Greenberg R, Donowitz G, Schuster M, Reboli A, Wingard J, Arndt C, Reinhardt J, Hadley S, Finberg R, Laverdiere M, Perfect J, Garber G, Fioritoni G, Anaissie E, Lee J: Voriconazole compared with liposomal amphotericin B for empirical antifungal therapy in patients with neutropenia and persistent fever. N Engl J Med. 2002 Jan 24;346(4):225-34.
  • PMID: 30687893
    Shi C, Xiao Y, Mao Y, Wu J, Lin N: Voriconazole: A Review of Population Pharmacokinetic Analyses. Clin Pharmacokinet. 2019 Jun;58(6):687-703. doi: 10.1007/s40262-019-00735-7.
  • PMID: 28702763
    Bellmann R, Smuszkiewicz P: Pharmacokinetics of antifungal drugs: practical implications for optimized treatment of patients. Infection. 2017 Dec;45(6):737-779. doi: 10.1007/s15010-017-1042-z. Epub 2017 Jul 12.
  • PMID: 17433262
    Murayama N, Imai N, Nakane T, Shimizu M, Yamazaki H: Roles of CYP3A4 and CYP2C19 in methyl hydroxylated and N-oxidized metabolite formation from voriconazole, a new anti-fungal agent, in human liver microsomes. Biochem Pharmacol. 2007 Jun 15;73(12):2020-6. doi: 10.1016/j.bcp.2007.03.012. Epub 2007 Mar 19.
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Contoh Produk & Brand

Produk: 192 • International brands: 0
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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