Anfulike Amphotericin B Cholesteryl Sulfate Complex for Injection

1. Indications and Usage
Treatment of serious, life-threatening fungal infections caused by susceptible strains of Aspergillus, Candida, Cryptococcus, and others. Specific indications include:
Systemic Fungal Infections: Aspergillosis, blastomycosis, coccidioidomycosis, and cryptococcosis.
Leishmaniasis: Treatment of visceral leishmaniasis (kala-azar).
Fever in Neutropenic Patients: Empiric treatment of fever in neutropenic patients suspected to have fungal infections.
2. Dosage and Administration
Route of Administration: For Intravenous (IV) Infusion ONLY. Intrathecal administration is contraindicated.
Recommended Dosage:
Fungal Infections: Typically 0.5 to 1.0 mg/kg/day, titrated up to 1.5 mg/kg/day based on clinical response and tolerance.
Leishmaniasis: 1.0 to 1.5 mg/kg/day for 10 days.
Critical Administration Instructions:
Dilution: Reconstitute and dilute ONLY in 5% Glucose Injection. Do not use 0.9% Sodium Chloride.
Infusion Time: Infuse over 60 to 120 minutes.
Filtration: Use a 5-micron or polyvinyl alcohol inline filter during administration.
Pre-medication: Administer acetaminophen, diphenhydramine, or hydrocortisone prior to infusion to minimize infusion-related reactions.
3. Mechanism of Action
Membrane Disruption: Amphotericin B binds to ergosterol, a key component of fungal cell membranes.
Pore Formation: This binding creates transmembrane pores, leading to leakage of intracellular potassium, magnesium, and other essential molecules, ultimately causing fungal cell death.
Complex Advantage: In this cholesterol sulfate complex formulation, the drug is encapsulated within a lipid bilayer, which reduces its binding to mammalian cell cholesterol, thereby lowering toxicity.
4. Safety and Warnings
Nephrotoxicity: Dose-dependent renal impairment remains the primary concern. Monitor serum creatinine and BUN regularly; hydration with 0.9% Sodium Chloride before infusion is recommended.
Infusion-Related Reactions: Fever, chills, rigors, and nausea are common, especially during the first few infusions.
Electrolyte Abnormalities: Significant hypokalemia and hypomagnesemia frequently occur and require routine monitoring and supplementation.
Hypersensitivity: Anaphylactic reactions can occur; emergency resuscitation equipment must be available.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Nephrotoxicity, hypokalemia, hypomagnesemia, anemia, infusion-related reactions, nausea, and vomiting.
Clinical Research Highlights: Clinical data demonstrate that this lipid complex formulation achieves comparable antifungal efficacy to conventional amphotericin B but with a significantly lower incidence of severe nephrotoxicity and infusion-related toxicity.
6. Drug Interactions
Nephrotoxic Agents: Concomitant use with aminoglycosides, cyclosporine, or other nephrotoxic drugs increases the risk of renal failure.
Cardiac Glycosides: Hypokalemia induced by amphotericin B increases the risk of digitalis toxicity.
Antineoplastic Agents: May exacerbate bone marrow suppression when used with cytotoxic chemotherapy.
7. Pharmaceutical Information
Chemical Composition: Amphotericin B formulated as a complex with cholesterol sulfate.
Appearance: Yellow to orange lyophilized cake or loose body.
Packaging: Single-use vial (50 mg).
Storage: Store in the original carton at 2°C to 8°C. Do not freeze.