Noxafil Posaconazole Oral Suspension

1. Indications and Usage
Prevention: Indicated for the prevention of invasive aspergillus and candida infections in patients 13 years of age and older who are at high risk due to severe immunocompromise (e.g., hematopoietic stem cell transplantation with graft-versus-host disease or hematologic malignancies with prolonged neutropenia).
Treatment: Indicated for the treatment of oropharyngeal candidiasis (OPC), including terbinafine- and/or fluconazole-refractory OPC.
2. Dosage and Administration
Prevention: The recommended dose is 200 mg three times daily. The duration is determined by the recovery from neutropenia or immunosuppression.
Treatment of Oropharyngeal Candidiasis: The loading dose is 100 mg twice daily on Day 1. The maintenance dose is 100 mg once daily for 13 days.
Refractory Oropharyngeal Candidiasis: The recommended dose is 400 mg twice daily. The duration is determined by the severity of the underlying disease and clinical response.
Administration Requirements: The suspension must be administered during a meal or within 20 minutes after a meal to ensure adequate absorption. For patients unable to eat, it should be administered with a nutritional supplement or carbonated beverage. The bottle must be shaken well before each use.
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 is contraindicated due to the risk of sirolimus toxicity. Use with pimozide or quinidine is also contraindicated due to the risk of 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: In patients with severe renal impairment, breakthrough fungal infections must be monitored closely due to higher variability in plasma exposure.
5. Adverse Reactions and Clinical Research
Adverse Reactions: The most common serious adverse reactions include hyperbilirubinemia, elevated liver transaminases, hepatocellular damage, nausea, and vomiting.
Clinical Research: Clinical trials have demonstrated that posaconazole oral suspension effectively prevents invasive fungal infections in high-risk immunocompromised patients and is effective in treating refractory oropharyngeal candidiasis.
6. Drug Interactions
CYP3A4 Substrates: Posaconazole is a strong inhibitor of CYP3A4 and can significantly increase the plasma concentrations of drugs metabolized by this enzyme (e.g., sirolimus, cyclosporine, tacrolimus, certain statins).
Drugs Affecting Absorption: Drugs that increase gastric pH (e.g., cimetidine, omeprazole) can decrease posaconazole plasma concentrations and should generally be avoided.
7. Pharmaceutical Information
Composition: The active ingredient is posaconazole.
Appearance: A white to off-white liquid suspension.
Storage: Store at controlled room temperature. Shake well before each use.