Noxafil Posaconazole Injection

1. Indications and Usage
Treatment: Indicated for the treatment of invasive aspergillosis in adult patients.
Prevention: Indicated for the prevention of invasive aspergillus and candida infections in patients 18 years of age and older who are at high risk due to severe immunocompromise (e.g., patients with hematologic malignancies and prolonged neutropenia or graft-versus-host disease following hematopoietic stem cell transplantation).
2. Dosage and Administration
Treatment of Invasive Aspergillosis: The loading dose is 300 mg twice daily on Day 1. The maintenance dose is 300 mg once daily starting on Day 2. The recommended total duration of treatment is 6 to 12 weeks.
Prevention: The loading dose is 300 mg twice daily on Day 1. The maintenance dose is 300 mg once daily starting on Day 2. The duration is determined by the recovery from neutropenia or immunosuppression.
Administration Requirements: Posaconazole injection should be administered via central venous access (central venous catheter or PICC), with each dose slowly infused intravenously over more than 90 minutes. It must not be administered as an intravenous bolus. If central venous access is temporarily unavailable, it may be infused through a peripheral venous catheter over more than 30 minutes, but this is permitted only once.
Dilution: Dilute with compatible diluents (e.g., 0.9% Sodium Chloride or 5% Dextrose) to a final concentration of 1 to 2 mg/mL. The diluted solution should be used immediately or stored at 2-8°C for up to 24 hours.
3. Mechanism of Action
Posaconazole belongs to the triazole antifungal class. It works by inhibiting the biosynthesis of ergosterol, a major component of fungal cell membranes. This inhibition disrupts fungal cell membrane synthesis and function, exerting a broad-spectrum antifungal effect.
4. Safety and Warnings
Serious Drug Interactions: Concomitant use with sirolimus, pimozide, quinidine, or HMG-CoA reductase inhibitors (statins) metabolized by CYP3A4 (e.g., atorvastatin, lovastatin, simvastatin) is contraindicated due to the risk of severe toxicity or QTc prolongation.
Hepatotoxicity: Monitor liver function tests; hepatotoxicity has been reported.
QTc Prolongation: Use with caution in patients with a history of cardiac arrhythmias or electrolyte abnormalities.
Renal Impairment: Avoid use in patients with moderate to severe renal impairment (eGFR <50 mL/min) unless the benefit outweighs the risk, as the excipient sulfobutyl ether beta-cyclodextrin sodium (SBECD) may accumulate.
5. Adverse Reactions and Clinical Research
Adverse Reactions: Common adverse reactions include nausea, vomiting, fever, diarrhea, and infusion site reactions.
Clinical Research: Clinical trials have demonstrated that posaconazole injection effectively prevents invasive fungal infections in high-risk immunocompromised patients and provides a viable treatment option for invasive aspergillosis.
6. Drug Interactions
CYP3A4 Inhibitors: Posaconazole is a strong inhibitor of CYP3A4 and can significantly increase the plasma concentrations of drugs metabolized by this enzyme.
CYP3A4 Inducers/P-gp Modifiers: Drugs that induce CYP3A4 or inhibit P-glycoprotein (P-gp) may significantly decrease posaconazole plasma concentrations.
QTc-Prolonging Agents: Concomitant use with other agents that prolong the QTc interval may increase the risk of arrhythmias.
7. Pharmaceutical Information
Composition: The active ingredient is posaconazole. Excipients include sulfobutyl ether beta-cyclodextrin sodium, disodium edetate, sodium hydroxide, and hydrochloric acid.
Appearance: A clear liquid ranging in color from colorless to yellow.
Storage: Store at controlled room temperature. Protect from light.