| Table 3: | ||
|
Antifungal
Agents
|
||
|
Caspofungin
(Cancidas)
|
Voriconazole
(Vfend)
|
|
| Mechanism of action |
Inhibition of 1,3-ß-D-glucan synthase | Inhibition of fungal cyctochrome P-450-dependent 14-α-demethylase |
| Spectrum
of activity |
Aspergillus sp, C albicans, C glabrata, C tropicalis, C krusei, C parapsilosis, and C lusitaniae; not active against Cryptococcus | Aspergillus sp, C albicans, C glabrata, C tropicalis, C krusei, C parapsilosis, and C lusitaniae; may be active against Cryptococcus, endemic fungi, and Fusarium sp |
| Oral absorption | <1% | >80 % |
| Metabolism | Metabolized by hydrolysis and N-acetylation; does not appear to be a substrate for the CYP-450 system | CYP 2C9 and CYP 2C19 |
| Half-life | ß-phase half-life is 9-11 hours; an additional longer-phase half-life of 40-50 hours also occurs | Approximately 6 hours |
| Adverse
reactions |
Fever, rash, nausea, vomiting, and phlebitis at the injection site | Visual changes, increased liver function test results, and rash |
| Potential drug interactions | Contraindicated with cyclosporine; tacrolimus levels decreased by 30% | Rifampin, rifabutin, and phenytoin, carbamazepine may decrease voriconazole levels. Cyclosporine levels are increased. Potential for interaction with any medication metabolized via 2C9, 2C19, or 3A4 |
| Other
considerations |
Pregnancy category C. Do not use diluents containing dextrose | Hepatotoxicity appears to be level-related, and levels can vary greatly between patients at standard doses |
| Approved
indications |
Treatment of invasive aspergillosis in patients who are refractory to or intolerant of other therapies. Caspofungin has not been studied as initial therapy for invasive aspergillosis |
Pending FDA approval |
| Dosage and administration | Day 1: 70 mg IV x 1 dose, then 50 mg IV q24h* |
Aspergillus or
invasive mold infections^ Candida infections^ |
| *Dosage
reduction is for patients with hepatic insufficiency; see package insert;
^Proposed doses, may require dose adjustment based on levels or concurrent medications |
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Copyright
2002 The Cleveland Clinic Foundation
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