Sporanox - Itraconazole

Sporanox , itraconazole [package insert]. Titusville, NJ Janssen Pharmaceutical Products, L.P. (package insert revised 1/2004). 

Onychomycosis is a fungal nail infection. In severe cases, oral antifungals are recommended as first-line agents. Oral triazole antifungals such as itraconazole (Sporanox capsules) as well as terbinafine (Lamisil tablets) are recommended. Treatment with itraconazole poses a lesser burden to patients... 

Econazole (Spectazole) Fluconazole (Diflucan) Itraconazole (Sporanox) Ketoconazole (Nizoral)... 

TRIAZOLE ANTIFUNGALS ITRACONAZOLE (SPORANOX ), FLUCONAZOLE (DIFLUCAN ), VORICONAZOLE (VFEND ), AND FOSFLUCONAZOLE (PRODIF )... 

USAN Itraconazole Trade name Sporanox Johnson Johnson Launched 1988 M.W. 705.65... 

Itraconazole (Sporanox), a triazole, is highly lipophilic and concentrates in skin. It is approved for both cutaneous deep fungal infections and dermatophyte nail disease, for which shorter courses of therapy are probably effective. Pulse therapy, whereby the drug is administered for 1 week and then the patient is off treatment for 3 weeks between pulses, may reduce toxicity without compromising antifungal efficacy. 

Although itraconazole and fluconazole are both triazoles, they are chemically and pharmacologically distinct. Itraconazole (Sporanox) is lipophilic and water insoluble and requires a low gastric pH for absorption. Oral bioavailability is variable, only 50 to 60% when taken with food and 20% or less when the drug is taken on an empty stomach. Itraconazole is highly protein bound (99%) and is metabolized in the liver and excreted into the bile. With initial dosing, the plasma half-life is 15 to 20 hours steady-state serum concentrations are reached only after 2 weeks of therapy, when the half-life is extended to 30 to 35 hours. In lipophilic tissues, drug concentration is 2 to 20 times that found in... 

Azole derivatives currently available for oral treatment of systemic mycosis include fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral), and others. As discussed in Chapter 48, imidazole derivatives act by affecting the permeability of the cell membrane of sensitive cells through alterations of the biosynthesis of lipids, especially sterols, in the fungal cell. 

HP5-P-CD Cephalosporin Itraconazole Oral United States, Sporanox ... 

HP-P-CD was developed by Janssen as a proprietary inactive ingredient (Encapsin ) and used in both the oral and IV formulation of their anti-fungal itraconazole (Sporanox ). The preclinical safety studies (9) conducted on HP-P-CD in support of Sporanox are highlighted in Table 3. 

On the basis of Hfft-CD, Janssen developed different formulation for Itraconazole (Sporanox), a broad-spectrum antifungal agent. Currently, capsule, IV, as well as oral solution formulations have been approved into market (http //www.accessdata.fda.gov/scripts/cder/ob/docs/tempai.cfm). 

Itraconazole (Sporanox, 13.11) is an approved antifungal (Figure 13.5). The drug has a log P value of 6.5, so its very low aqueous solubility is no surprise. Early efforts to improve the properties of itraconazole focused on making an acid salt. Because of the very weak basicity of all the nitrogens in itraconazole, the idea of an acid salt was soon abandoned. Cocrystals were then explored. A library of amides and acids were... 

Itraconazole Sporanox capsule, oral 100 mg solution, oral 10 mg/ml injectable 10 mg/ml (generic also available)... 

Itraconazole (Sporanox , Janssen) is solubilized as a molecular inclusion complex using hydro-xypropyl- p-cyclodextrin. 

Itraconazole (Sporanox) rv Infusion after dilution 40% Hydroxypropyl-P-cyclodextrin... 

Itraconazole / Sporanox /Ortho Biotech and Janssen/antifungal... 

Itraconazole, a weakly basic (pKa 3.7) water-insoluble antifungal drug, is solubilized to lOmg/ml using a combination of 40% hydroxypropyl-p-cyclo-dextrin (i.e., 400mg/ml) in water and pH adjustment to approximately 2 in Sporanox oral solution. The relative oral bioavailability of itraconazole from the oral solution is 149%i 68%i compared to capsules from which the oral bioavailability is 55%). Therefore, the oral bioavailability of itraconazole from the oral solution can be estimated to be 45-82%i. The dose of Sporanox oral solution is up to 20 ml once a day, which is 8.0 g of hydroxypropyl-p-cyclodextrin per dose representing the estimated maximum amount administered orally per dose. 

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