Table 1.
Overview on pharmacokinetics of antifungals
| Drugs | Protein binding (%) | Vd (L/kg) | Cmax (µg/ml) | T1/2 (h) | Elimination | Dosage |
|---|---|---|---|---|---|---|
| Amphotericin | 95–99 | 0.5–2 | 1.7–2.8 | 15–27 |
Bile, kidney (80%) No metabolite yet identified |
0.3 mg/kg on day 1 + 5 mg per day until 1 mg/kg Tinf > 4 h mandatory |
| Liposomal amphotericin | 95–99 | 0.05–2.2 | 14–29 (90) | 13–24 | Bile, RES long-term disposition, final elimination not yet clear, no metabolites identified |
3–4 mg/kg per day Tinf > 4 h recommended |
| Fluconazole | 12 | 0.7 | 9 | 30 | Mainly unchanged via the kidney, tubular reabsorption |
IV loading dose: 12 mg/kg once Maintenance dose: 6 mg/kg per 24 h |
| Voriconazole | 58 | 4.5 | 4.4 | 6 |
Hepatic metabolism involving 2C9, 2C19, and CYP3A4 Strong inhibitor |
IV loading dose: 6 mg/kg on day 1 Maintenance: 4 mg/kg per 12 h |
| Isavuconazole | 98–99 | 6.5 | 2.6 | 80–120 |
Hepatic metabolism involving UGT, CYP3A4 Moderate inhibitor |
IV loading dose: 200 mg day 1 and day 2 Maintenance dose: 200 mg per 24 h |
| Caspofungin | 92–97 | 0.3–2 | 10 | 8 | Independent from cytochrome P450 |
IV loading dose: 70 mg Maintenance dose 50 mg (70 mg if body weight > 80 kg) |
| Anidulafungin | 99 | 0.6 | 7 | 40–50 | Spontaneous degradation in plasma |
Loading dose: 200 mg (Tinf 180 min) Maintenance dose: 100 mg (Tinf 90 min) |
| Micafungin | 99.9 | 0.3 | 18 | 13–20 | CYP involved | 50 mg for prophylaxis, 100 mg for candidiasis, 150 mg for esophageal candidiasis |
Details and references are displayed in the text
Cmax peak level, T1/2 half-life, Cl clearance, Vd apparent volume of distribution, Tinf infusion time, RES reticuloendothelial system, CYP cytochrome, UGT urindin diphosphate glucuronosyltransferase