Antimycotic (approved for adults in Germany since October 2005) from the group of azoles (triazole). Posaconazole inhibits the ergosterol biosynthesis and is considered to be an antimycotic, which is used in severe or in itraconazole- or amphotericin B-resistant fungal infections, especially in immunocompromised patients.
Posaconazole
DefinitionThis section has been translated automatically.
Pharmacodynamics (Effect)This section has been translated automatically.
Posaconazole inhibits the ergosterol biosynthesis and here a fungus-specific cytochrome P450 isoenzyme (CYP51A1), which is responsible for the conversion of lanosterol into ergosterol. Ergosterol precursors are incorporated into the membrane and the permeability for cell components is increased.
IndicationThis section has been translated automatically.
- Onychomycosis(resistance to therapy with terbinafine or itraconazole).
- Invasive aspergillosis in patients whose disease is resistant to therapy with amphotericin B or itraconazole or who are intolerant to these drugs. The preparation is also used as a prophylactic in patients with severe immunosuppression.
- Fusariosis in patients whose disease is resistant to therapy with Amphotericin or intolerance to Amphotericin B.
- Chromoblastomycosis and Myzetom in patients whose disease is resistant to therapy with itraconazole or intolerance to itraconazole.
- Coccidioidomycosis in patients whose disease is resistant to therapy with amphotericin B, itraconazole or fluconazole or intolerance to these drugs.
- Oropharyngeal candidosis.
Dosage and method of useThis section has been translated automatically.
- Therapy-resistant invasive mycosis/patients with intolerance to other systemic antifungal drugs: 2 times/day 400 mg (10 ml) p.o. (daily dose 800 mg) or 4 times/day 200 mg (5 ml) p.o. The duration of therapy depends on the severity of the underlying disease, recovery from immunosuppression if necessary and the clinical response.
- Oropharyngeal candidosis: Initial (initial dose) 1 time / day 200 mg (5 ml) on the first day, then 1 time / day 100 mg (2.5 ml) p.o. for 13 days.
- Prophylaxis of invasive mycoses: 3 times/day 200 mg (5 ml) p.o. The duration of therapy in immunocompromised patients depends on the recovery from neutropenia or immunosuppression.
- Dosage (for therapy-resistant onychomycosis): 1x /day 200 - 400mg p.o.
Remember! To be taken with meals or, in patients who cannot eat a meal, with a food supplement to increase absorption and ensure adequate exposure.
Undesirable effectsThis section has been translated automatically.
Hepatotoxicity: slight to moderate increase in values for ALT, AST, alkaline phosphatase, total bilirubin and/or toxic hepatitis
InteractionsThis section has been translated automatically.
Posaconazole is metabolized via UDP glucuronidation (phase 2 enzymes). Inhibitors (e.g. verapamil, ciclosporin, guinidine, clarithromycin, erythromycin, etc.) or inducers (e.g. rifampicin, rifabutin, certain antiepileptic drugs, etc.) of these enzymes can increase or decrease the plasma concentration of posaconazole. Simultaneous use of posaconazole with H2-receptor antagonists and proton pump inhibitors can lead to a reduction in bioavailability (e.g. terfenadine, astemizole). QTc prolongation may occur .
ContraindicationThis section has been translated automatically.
- Hypersensitivity to the active substance or any of the other ingredients.
- Concomitant use of ergot alkaloids, terfenadine, astemizole, cisapride, pimozide, halofantrine or quinidine (QTc prolongation and in rare cases for the occurrence of torsades de pointes), HMG-coA reductase inhibitors such as simvastatin, lovastatin and atorvastatin.
PreparationsThis section has been translated automatically.
Noxafil
Note(s)This section has been translated automatically.
Close monitoring of blood values (especially leukocytes, neutrophils, liver values).
LiteratureThis section has been translated automatically.
- Schiller DS, Fung HB (2007) Posaconazole: an extended-spectrum triazole antifungal agent. Clin Ther 29: 1862-1886
- Elewski B et al (2012) A randomized, placebo- and active-controlled, parallel-group, multicentre, investigator-blinded study of four treatment regimens of posaconazole in adults with toenail onychomycosis.br J Dermatol 166:389-398.