Posaconazole
Posaconazole blocks the synthesis of ergosterol, a key component of the fungal cell membrane. It inhibits the cytochrome P-450 dependent enzyme Lanosterol 14-α-demethylase responsible for the conversion of lanosterol to ergosterol in the fungal cell membrane. This results in an accumulation of methylated sterol precursors and a depletion of ergosterol within the cell membrane, thus weakening the structure and function of the fungal cell membrane.
Posaconazole Tablets can be taken with or without food. The tablets should be swallowed whole with water and should not be crushed, chewed, or broken.Loading Dose: 300 mg (3 Tablets) twice a day on the first day.Maintenance Dose: 300 mg (3 Tablets) once a day from the second day.Duration of therapy should be based on the severity of the underlying disease, recovery from immunosuppression and clinical response.
Xpos is an inhibitor of CYP3A4 and should only be used under specific circumstances during treatment with other medicinal products that are metabolized by CYP3A4 like Midazolam, Triazolam, Alprazolam. Xpos concentrations may be significantly lowered in combination with Rifamycin antibacterials (Rifampicin, Rifabutin), certain anticonvulsants (Phenytoin, Carbamazepine, Phenobarbital, Primidone and Efavirenz).
Posaconazole is contraindicated in persons with known hypersensitivity to Posaconazole or other azole antifungal agents. Co-administration with ergot alkaloids, CYP3A4 substrates, Terfenadine, Astemizole, Cisapride, Pimozide, Halofantrine or Quinidine since this may result in increased plasma concentrations of these medicinal products leading to QTc prolongation and rare occurrences of torsades de pointes, HMG-CoA reductase inhibitors simvastatin, lovastatin and atorvastatin is contraindicated.
Common treatment-emergent adverse reactions in studies with Xpos are diarrhea, nausea, fever, vomiting, headache, coughing and hypokalemia.
Posaconazole must not be used during pregnancy unless the benefit to the mother clearly outweighs the potential risk to the fetus. Breast-feeding must be stopped on initiation of treatment with this drug.
Aural Anti-fungal preparations
Store below 25°C. Keep out of the reach of children.
Pediatric Use: Safety and effectiveness in pediatric patients below the age of 13 years has not been established. Therefore, Xpos is not recommended for pediatric patients less than 13 years of age.Geriatric Use: No dose adjustment is necessary for geriatric patients.Hepatic Impairment: Xpos should be used with caution in patients with hepatic impairment due to limited clinical experience and the possibility that Xpos plasma levels may be higher in these patients. Liver function tests should be evaluated at the start of and during the course of Xpos therapy.Renal Impairment: No dose adjustment is required in patients with mild (eGFR: 50-80 mL/min/1.73 m2) to moderate renal impairment (eGFR: 20-49 mL/min/1.73 m2). Patients with severe renal impairment should be monitored closely for breakthrough fungal infections.
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