黴菌感染 Invasive Aspergillosis: For patients ≥13 years of age) Prophylaxis against invasive fungal infections: For patients ≥2 years of age and >40 kg; Prophylaxis of invasive Aspergillus and Candida infections in severely immunocompromised patients
藥理
Antifungal Agent, Azole Derivative
Interferes with fungal cytochrome P450 (lanosterol-14α-demethylase) activity, decreasing ergosterol synthesis (principal sterol in fungal cell membrane) and inhibiting fungal cell membrane formation.
藥動學
Absorption:
Bioavailability: 54% Distribution:
Protein binding, Albumin: >98% Metabolism:
1. Hepatic: primarily glucuronidation, inhibitor of CYP3A4 (strong); Renal: 13%
2. Elimination Half Life: 26 to 31 hours Excretion:
1. Feces 71% (~66% as unchanged drug)
2. Urine 13% (<0.2% as unchanged drug)
禁忌症
1. Concomitant use with ergot alkaloids, HMG-CoA reductase inhibitors primarily metabolized by CYP3A4 (eg, atorvastatin, lovastatin, and simvastatin), sirolimus, or CYP3A4 substrates that prolong the QT interval (eg, pimozide and quinidine)
2. Hypersensitivity to posaconazole or other azole antifungals
Aspergillosis:
1. Chronic cavitary pulmonary: 300 mg twice daily for 2 doses, then 300 mg once daily; duration ≥6 months, some require prolonged therapy
2. Invasive: 300 mg twice daily for 2 doses, then 300 mg once daily; minimum duration 6-12 weeks Prophylaxis against invasive fungal infections:
300 mg twice daily for 2 doses, then 300 mg once daily
小兒調整劑量
腎功能調整劑量
1. eGFR 20-80 mL/minute/1.73 m2: No dosage adjustment necessary.
2. eGFR <20 mL/minute/1.73 m2: No dosage adjustment necessary; however, monitor for breakthrough fungal infections due to variability in posaconazole exposure.
肝功能調整劑量
1. Child-Pugh class A, B, or C: No dosage adjustment necessary
2. Hepatotoxicity during treatment: There are no dosage adjustments provided in the manufacturer's labeling; consider discontinuing therapy.