Peringatan Keamanan

In rats, the oral and intraperitoneal LD50 values were >320 mg/kg and 100 mg/kg, respectively.L50076

There is limited clinical information regarding itraconazole overdoses. Reported toxic trough levels are over 3 mcg/mL.A34257 Itraconazole is not removed by dialysis; thus, supportive measures should be initiated in the event of an overdose.L50051 There is no known antidote to itraconazole poisoning.A34257

Itraconazole

DB01167

small molecule approved investigational

Deskripsi

First synthesized in the early 1980s, itraconazole is a broad-spectrum triazole antifungal agent used to treat a variety of infections.A34257 It is a 1:1:1:1 racemic mixture of four diastereomers, made up of two enantiomeric pairs, each possessing three chiral centers.L50051 Itraconazole was first approved in the US in 1992 L50056 and is available orally. While the intravenous formulation of the drug was formerly available, it was discontinued in the US in 2007.A263232

Struktur Molekul 2D

Berat 705.633
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 half-life of itraconazole generally ranges from 16 to 28 hours after a single dose and increases to 34 to 42 hours with repeated dosing.[L50051] The metabolite of itraconazole is excreted from the plasma more rapidly than the parent compound.[A34257]
Volume Distribusi The volume of distribution is more than 700 L in adults.[A263232, L50051] Itraconazole is lipophilic and extensively distributed into tissues. Concentrations in the lung, kidney, liver, bone, stomach, spleen and muscle were found to be two to three times higher than corresponding concentrations in plasma, and the uptake into keratinous tissues, skin in particular, up to four times higher. Concentrations in the cerebrospinal fluid are much lower than in plasma.[L50051]
Klirens (Clearance) The mean total plasma clearance following intravenous administration is 278 mL/min. Itraconazole clearance decreases at higher doses due to saturable hepatic metabolism.[L50051]

Absorpsi

Itraconazole is rapidly absorbed after oral administration. As oral capsules, peak plasma concentrations of itraconazole are reached within two to five hours. The observed absolute oral bioavailability of itraconazole is about 55%. Itraconazole exposure is lower with the capsule formulation than with the oral solution when the same dose of the drug is given.L50051 Maximal drug absorption is achieved under adequate gastric acidity.A34257, L50051 As a consequence of non-linear pharmacokinetics, itraconazole accumulates in plasma during multiple dosing. Steady-state concentrations are generally reached within about 15 days, with Cmax values of 0.5 ?g/mL, 1.1 ?g/mL and 2.0 ?g/mL after oral administration of 100 mg once daily, 200 mg once daily and 200 mg b.i.d., respectively.L50051

Metabolisme

Itraconazole is extensively metabolized in the liver. In vitro studies have shown that CYP3A4 is the major enzyme involved in the metabolism of itraconazole.L50051 While itraconazole can be metabolized to more than 30 metabolites,A263222 the main metabolite is hydroxyitraconazole. Hydroxyitraconazole has in vitro antifungal activity comparable to itraconazole; trough plasma concentrations of this metabolite are about twice those of the parent compound.L50051 Other metabolites include keto-itraconazole and N-dealkyl-itraconazole.A263232

Rute Eliminasi

Itraconazole is excreted mainly as inactive metabolites in urine (35%) and in feces (54%) within one week of an oral solution dose. Renal excretion of itraconazole and the active metabolite hydroxyitraconazole account for less than 1% of an intravenous dose. Based on an oral radiolabeled dose, fecal excretion of unchanged drug ranges from 3% to 18% of the dose. As the re-distribution of itraconazole from keratinous tissues appears to be negligible, the elimination of itraconazole from these tissues is related to epidermal regeneration. Contrary to plasma, the concentration in skin persists for two to four weeks after discontinuation of a 4-week treatment and in nail keratin – where itraconazole can be detected as early as one week after the start of treatment – for at least six months after the end of a 3-month treatment period.L50051

Interaksi Makanan

2 Data
  • 1. Exercise caution with grapefruit products. While there is inconclusive evidence of the effect of grapefruit products on the systemic exposure to itraconazole, they may affect drug absorption.
  • 2. Take with food. Food promotes maximal absorption of itraconazole.

Interaksi Obat

1300 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Itraconazole.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Itraconazole.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Itraconazole.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Itraconazole.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Itraconazole.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Itraconazole.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Itraconazole.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Itraconazole.
Silodosin The excretion of Silodosin can be decreased when combined with Itraconazole.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Itraconazole.
Amphotericin B The therapeutic efficacy of Amphotericin B can be decreased when used in combination with Itraconazole.
Didanosine Didanosine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Itraconazole.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Itraconazole.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Itraconazole.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Itraconazole.
Sildenafil The serum concentration of Sildenafil can be increased when it is combined with Itraconazole.
Magnesium oxide Magnesium oxide can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium bicarbonate Sodium bicarbonate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminum hydroxide Aluminum hydroxide can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magaldrate Magaldrate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium hydroxide Magnesium hydroxide can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium trisilicate Magnesium trisilicate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium carbonate Magnesium carbonate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Bismuth subnitrate Bismuth subnitrate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium silicate Magnesium silicate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium acetoacetate Aluminium acetoacetate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Hydrotalcite Hydrotalcite can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Magnesium peroxide Magnesium peroxide can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Almasilate Almasilate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium glycinate Aluminium glycinate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aloglutamol Aloglutamol can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium silicate Calcium silicate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Aluminium phosphate Aluminium phosphate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Pantoprazole Pantoprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Omeprazole Omeprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lansoprazole Lansoprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Esomeprazole Esomeprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rabeprazole Rabeprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexlansoprazole Dexlansoprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Dexrabeprazole Dexrabeprazole can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sodium zirconium cyclosilicate Sodium zirconium cyclosilicate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Vonoprazan Vonoprazan can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Itraconazole.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Itraconazole.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Itraconazole.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Itraconazole.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Itraconazole.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Itraconazole.
Indinavir The metabolism of Indinavir can be decreased when combined with Itraconazole.
Nevirapine The serum concentration of Itraconazole can be decreased when it is combined with Nevirapine.
Methadone The serum concentration of Methadone can be increased when it is combined with Itraconazole.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be increased when it is combined with Itraconazole.
Deslanoside The serum concentration of Deslanoside can be increased when it is combined with Itraconazole.
Ouabain The serum concentration of Ouabain can be increased when it is combined with Itraconazole.
Digitoxin The serum concentration of Digitoxin can be increased when it is combined with Itraconazole.
Oleandrin The serum concentration of Oleandrin can be increased when it is combined with Itraconazole.
Cymarin The serum concentration of Cymarin can be increased when it is combined with Itraconazole.
Proscillaridin The serum concentration of Proscillaridin can be increased when it is combined with Itraconazole.
Lanatoside C The serum concentration of Lanatoside C can be increased when it is combined with Itraconazole.
Gitoformate The serum concentration of Gitoformate can be increased when it is combined with Itraconazole.
Peruvoside The serum concentration of Peruvoside can be increased when it is combined with Itraconazole.
Olanzapine Olanzapine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cimetidine Cimetidine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Nizatidine Nizatidine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ranitidine Ranitidine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Famotidine Famotidine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Methantheline Methantheline can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Promethazine Promethazine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Doxepin Doxepin can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Asenapine Asenapine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Metiamide Metiamide can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Roxatidine acetate Roxatidine acetate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lafutidine Lafutidine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lavoltidine Lavoltidine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Niperotidine Niperotidine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Epinastine Epinastine can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ritonavir The serum concentration of Itraconazole can be increased when it is combined with Ritonavir.
Vincristine The metabolism of Vincristine can be decreased when combined with Itraconazole.
Sucralfate Sucralfate can cause a decrease in the absorption of Itraconazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Itraconazole.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Itraconazole.
Midazolam The metabolism of Midazolam can be decreased when combined with Itraconazole.
Meloxicam The serum concentration of Meloxicam can be decreased when it is combined with Itraconazole.
Tadalafil The metabolism of Tadalafil can be decreased when combined with Itraconazole.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Itraconazole.
Triazolam The metabolism of Triazolam can be decreased when combined with Itraconazole.
Tipranavir The metabolism of Itraconazole can be increased when combined with Tipranavir.
Isoniazid The serum concentration of Itraconazole can be decreased when it is combined with Isoniazid.
Telithromycin The metabolism of Telithromycin can be decreased when combined with Itraconazole.
Boceprevir The serum concentration of Boceprevir can be increased when it is combined with Itraconazole.
Cobicistat The metabolism of Cobicistat can be decreased when combined with Itraconazole.
Darunavir The metabolism of Itraconazole can be decreased when combined with Darunavir.
Elvitegravir The metabolism of Elvitegravir can be decreased when combined with Itraconazole.
Amprenavir The serum concentration of Itraconazole can be increased when it is combined with Amprenavir.
Fosamprenavir The serum concentration of Itraconazole can be increased when it is combined with Fosamprenavir.
Lopinavir The metabolism of Itraconazole can be decreased when combined with Lopinavir.
Saquinavir The serum concentration of Saquinavir can be increased when it is combined with Itraconazole.
Telaprevir The serum concentration of Itraconazole can be increased when it is combined with Telaprevir.

Target Protein

Lanosterol 14-alpha demethylase ERG11
Lanosterol 14-alpha demethylase ERG11

Referensi & Sumber

Synthesis reference: Jong-Soo Woo, Hong-Gi Yi, "Antifungal oral composition containing itraconazole and process for preparing same." U.S. Patent US6039981, issued May, 1998.
Artikel (PubMed)
  • PMID: 11249550
    Pierard GE, Arrese JE, Pierard-Franchimont C: Itraconazole. Expert Opin Pharmacother. 2000 Jan;1(2):287-304. doi: 10.1517/14656566.1.2.287 .
  • PMID: 11219548
    De Beule K, Van Gestel J: Pharmacology of itraconazole. Drugs. 2001;61 Suppl 1:27-37. doi: 10.2165/00003495-200161001-00003.
  • PMID: 32491797
    Kurn H, Wadhwa R: Itraconazole. .
  • PMID: 23641752
    Lestner J, Hope WW: Itraconazole: an update on pharmacology and clinical use for treatment of invasive and allergic fungal infections. Expert Opin Drug Metab Toxicol. 2013 Jul;9(7):911-26. doi: 10.1517/17425255.2013.794785. Epub 2013 May 6.

Contoh Produk & Brand

Produk: 43 • International brands: 3
Produk
  • Ciclopirox 3% / Itraconazole 5% / Urea 20%
    Cream • - • Topical • US
  • Fluconazole 4% / Ibuprofen 2% / Itraconazole 1% / Terbinafine HCl 4%
    Solution • - • Topical • US
  • Itraconazole
    Capsule • 100 mg/1 • Oral • US • Approved
  • Itraconazole
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Itraconazole
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Itraconazole
    Solution • 10 mg/1mL • Oral • US • Generic • Approved
  • Itraconazole
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Itraconazole
    Capsule, coated pellets • 100 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 43 produk.
International Brands
  • Itrizole
  • Oriconazole
  • Sporal

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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