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TOP
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APTIVUS®(二十三)
ediatric Patients by Age
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Parameter |
2 to <6 years
(n=12) |
6 to <12 years
(n=8) |
12 to 18 years
(n=6) |
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a Population pharmacokinetic parameters reported as mean ± standard deviation |
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Cptrough (μM) |
59.6 ± 23.6 |
66.3 ± 12.5 |
53.3 ± 32.4 |
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Cmax (μM) |
135 ± 44 |
151 ± 32 |
138 ± 52 |
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Tmax (h) |
2.5 |
2.6 |
2.7 |
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AUC0-12h (μM•h) |
1190 ± 332 |
1354 ± 256 |
1194 ± 517 |
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CL/F (L/h) |
0.34 |
0.45 |
0.99 |
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V (L) |
4.0 |
4.7 |
5.3 |
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t1/2 (h) |
8.1 |
7.1 |
5.2 |
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Drug Interactions
Drug interaction studies were performed with APTIVUS capsules co-administered with ritonavir, and other drugs likely to be co-administered and some drugs commonly used as probes for pharmacokinetic interactions. The effects of co-administration of APTIVUS with 200 mg ritonavir on the AUC, Cmax, and Cmin of tipranavir or the co-administered drug, are summarized in Tables 7 and 8, respectively. For information regarding clinical recommendations see Drug Interactions (7.2).
Table 7 Drug Interactions: Pharmacokinetic Parameters for Tipranavir in the Presence of Co-administered Drugs
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Co-administered Drug |
Co-administered Drug Dose (Schedule) |
tipranavir/ritonavir Drug Dose (Schedule) |
n |
PK |
Ratio (90% Confidence Interval) of Tipranavir
Pharmacokinetic Parameters with/without
Co-administered Drug;
No Effect = 1.00 |
|
Cmax |
AUC |
Cmin |
*steady state comparison to historical data (n)
↑ increase, ↓ decrease, ↔ no change, ↕ unable to predict |
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Antacids (Maalox®) |
20 mL
(1 dose) |
500/200 mg
(1 dose) |
23 |
↓ |
0.75 (0.63, 0.88) |
0.73 (0.64, 0.84) |
- |
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Atazanavir/ritonavir |
300/100 mg QD
(9 doses) |
500/100 mg BID
(34 doses) |
13 |
↑ |
1.08 (0.98, 1.20) |
1.20 (1.09, 1.32) |
1.75 (1.39, 2.20) |
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Atorvastatin |
10 mg
(1 dose) |
500/200 mg BID
(14 doses) |
22 |
↔ |
0.96 (0.86, 1.07) |
1.08 (1.00, 1.15) |
1.04 (0.89, 1.22) |
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Clarithromycin |
500 mg BID
(25 doses) |
500/200 mg BID* |
24 (68) |
↑ |
1.40 (1.24, 1.47) |
1.66 (1.43, 1.73) |
2.00 (1.58, 2.47) |
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Didanosine |
400 mg
(1 dose) |
500/100 mg BID
(27 doses) |
5 |
↓ |
1.32 (1.09, 1.60) |
1.08 (0.82, 1.42) |
0.66 (0 |
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