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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.
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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