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Liptruzet (Ezetimibe and Atorvastatin Tablets)(二十一)
2013-06-16 15:35:39 来源: 作者: 【 】 浏览:19759次 评论:0
eractions (7) for clinical significance.
‡ The dose of saquinavir plus ritonavir in this study is not the clinically used dose. The increase in atorvastatin exposure when used clinically is likely to be higher than what was observed in this study. Therefore, caution should be applied and the lowest dose necessary should be used.
§ Greater increases in AUC (up to 2.5 fold) and/or Cmax (up to 71%) have been reported with excessive grapefruit consumption (≥ 750 mL -- 1.2 liters per day).
¶ Single sample taken 8-16 h post-dose.
# Due to the dual interaction mechanism of rifampin, simultaneous coadministration of atorvastatin with rifampin is recommended, as delayed administration of atorvastatin after administration of rifampin has been associated with a significant reduction in atorvastatin plasma concentrations.
Cyclosporine 5.2 mg/kg/day, stable dose † 10 mg QD for 28 days ↑8.7 fold ↑10.7 fold
Tipranavir 500 mg BID/ritonavir 200 mg BID, 7 days † 10 mg, SD ↑9.4 fold ↑8.6 fold
Telaprevir 750 mg q8h, 10 days † 20 mg, SD ↑7.88 fold ↑10.6 fold
   
Saquinavir 400 mg BID/ritonavir 400 mg BID, 15 days †, ‡ 40 mg QD for 4 days ↑3.9 fold ↑4.3 fold
Clarithromycin 500 mg BID, 9 days † 80 mg QD for 8 days ↑4.4 fold ↑5.4 fold
Darunavir 300 mg BID/ritonavir 100 mg BID, 9 days † 10 mg QD for 4 days ↑3.4 fold ↑2.25 fold
Itraconazole 200 mg QD, 4 days † 40 mg, SD ↑3.3 fold ↑20%
Fosamprenavir 700 mg BID/ritonavir 100 mg BID, 14 days † 10 mg QD for 4 days ↑2.53 fold ↑2.84 fold
Fosamprenavir 1400 mg BID, 14 days † 10 mg QD for 4 days ↑2.3 fold ↑4.04 fold
Nelfinavir 1250 mg BID, 14 days † 10 mg QD for 28 days ↑74% ↑2.2 fold
Grapefruit Juice, 240 mL QD †, § 40 mg, SD ↑37% ↑16%
Diltiazem 240 mg QD, 28 days 40 mg, SD ↑51% No change
Erythromycin 500 mg QID, 7 days 10 mg, SD ↑33% ↑38%
Amlodipine 10 mg, single dose 80 mg, SD ↑15% ↓12%
Cimetidine 300 mg QD, 4 weeks 10 mg QD for 2 weeks ↓Less than 1% ↓11%
Colestipol 10 mg BID, 28 weeks 40 mg QD for 28 weeks Not determined ↓26%¶
Maalox TC® 30 mL QD, 17 days 10 mg QD for 15 days ↓33% ↓34%
Efavirenz 600 mg QD, 14 days 10 mg for 3 days ↓41% ↓1%
Rifampin 600 mg QD, 7 days (coadministered) †, # 40 mg, SD ↑30% ↑2.7 fold
Rifampin 600 mg QD, 5 days (doses separated) †, # 40 mg, SD ↓80% ↓40%
Gemfibrozil 600 mg BID, 7 days † 40 mg, SD ↑35% ↓Less than 1%
Fenofibrate 160 mg QD, 7 days † 40 mg, SD ↑3% ↑2%
Boceprevir 800 mg TID, 7 days 40 mg, SD ↑2.30 fold ↑2.66 fold

Data given as x-fold change represent a simple ratio between coadministration and atorvastatin alone (i.e., 1-fold = no change). Data given as % change represent % difference relative to atorvastatin alone (i.e., 0% = no change).
† See Warnings and Precautions (5.1) and Drug Interactions (7) for clinical significance.
‡ The dose of saquinavir plus ritonavir in this study is not the clinically used dose. The increase in atorvastatin exposure when used clinically is likely to be higher than what was observed in this study. Therefore, caution should be applied and the lowest dose necessary should be used.
§ Greater increases in AUC (up to 2.5 fold) and/or Cmax (u

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