Caspofungin Data - Uses, Dosage, Drug class, Brand name, Warnings, etc
Pharmacology |
Caspofungin is an echinocandin antifungal, a specific noncompetitive inhibitor of β-(1-3) glucan synthetase in fungal cell membranes. This weakens the cell wall, leading to cell lysis and death. Active against Candida spp., Aspergillus spp., and Pneumocystis carinii with minimal cross-resistance to azoles. |
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Adult Dosage |
IV for refractory invasive aspergillosis: - Day 1: 70 mg loading dose - Then: 50 mg/day - Infuse over 1 hr; do not mix with dextrose-containing solutions - Unresponsive patients: Consider 70 mg/day (some evidence supports) Moderate hepatic impairment: - 35 mg/day after 70 mg loading dose Severe hepatic impairment: - No experience; safety/efficacy not established Under 18 yr: - Safety and efficacy not established |
Dosage Forms | - Injection: 50 mg, 70 mg |
Pharmacokinetics |
Protein Binding: ~97% to plasma proteins Distribution: Extensive in tissues Metabolism: Slow hydrolysis and N-acetylation Excretion: <2% unchanged in urine Half-life: - Primary: 9–11 hr (main elimination) - Secondary: 40–50 hr |
Adverse Reactions |
Common: - Headache, fever, nausea, vomiting, flushing, pruritus, infusion vein complications - Some effects may be histamine-related Rare: - Anaphylaxis (1 case reported) Other: - Elevated liver function tests, especially with cyclosporine |
Drug Interactions |
- Reduces tacrolimus levels by ~20% - Cyclosporine increases caspofungin AUC by 35%, causes transient ALT/AST increases; concomitant use not recommended - Does not inhibit P450 enzymes, not a P450 substrate, does not induce CYP3A4 - Drug metabolism inducers may decrease caspofungin levels; consider 70 mg/day if unresponsive |
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