Table 2.
Pharmacokinetics of darunavir in children and adults from the US Package insert12 and other references as noted
| Observation or parameter (adult patients) | ||
|---|---|---|
| Protein binding | 95% | |
| Bioavailability, absolute | ||
| without ritonavir | 37% | |
| with ritonavir | 82% | |
| Bioavailability, relative | ||
| food11 | +30% | |
| Tmaxa, hours | 2.5–4.0 | |
| Terminal half-life, hours | 15 (when co-administered with ritonavir) | |
| Clearance, L/h (intravenous dosing with ritonavir) | 5.9 | |
| Volume of distribution, L (intravenous dosing)51 | 131 | |
| Effect of hepatic impairment | No significant change with moderate impairment (Child-Pugh Class B) | |
| Effect of renal impairment | No significant change with moderate impairment (creatinine clearance 30–60 mL/min) | |
| Typical darunavir | Pooled POWER 1 and 2 | DELPHI |
| concentrationsb | N = 119 adults | N = 74 children |
| AUC0–24, μg·h/mLc median (range) | 123.3 (67.7–213.0) | 127.3 (67.1–230.7) |
| C0h, μg/mLd median (range) | 3.5 (1.3–7.4) | 3.9 (1.8–7.8) |
a
Time to maximum concentration
b
Observed after darunavir 600 mg plus ritonavir 100 mg twice daily in adults, and according to dosing in Table 2 in children.
c
Area under the time-concentration curve from 0 to 24 hours, calculated as 2*AUC0–12.
d
Concentration immediately prior to dosing, ie. trough concentration.