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Clinical Pharmacology
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In patients with Child-Pugh A disease, Cmax and AUC were increased by 60% and 5%, respectively, as compared with patients with normal liver function. In patients with Child-Pugh B disease, Cmax and AUC were increased 100% and 21%, respectively, compared with patients with normal liver function
Drug-Drug Interactions
Cytochrome P450 3A4
Rosuvastatin clearance is not dependent on metabolism by cytochrome P450 3A4 to a clinically significant extent.
Table 3. Effect of Co-administered Drugs on Rosuvastatin Systemic Exposure
| Co-administered drug and dosing regimen | Rosuvastatin | ||
| Dose (mg)* | Change in AUC |
Change in Cmax |
|
| Cyclosporine – stable dose required (75 mg – 200 mg BID) | 10 mg QD for 10 days | ↑ 7-fold† | ↑11-fold† |
| Gemfibrozil 600 mg BID for 7 days | 80 mg | ↑1.9-fold† | ↑2.2-fold† |
| Lopinavir/ritonavir combination 400 mg/100 mg BID for 10 days | 20 mg QD for 7 days | ↑5-fold† | ↑2-fold† |
| Fenofibrate 67 mg TID for 7 days | 10 mg | ↑7% | ↑21% |
| Aluminum & magnesium hydroxide combination antacid | |||
| Administered simultaneously | 40 mg | ↓54%† | ↓ 50%† |
| Administered 2 hours apart | 40 mg | ↓ 22% | ↓ 16% |
| Erythromycin 500 mg QID for 7 days | 80 mg | ↓ 20% | ↓ 31% |
| Ketoconazole 200 mg BID for 7 days | 80 mg | ↑ 2% | ↓ 5% |
| Itraconazole 200 mg QD for 5 days | 10 mg | ↑ 39% | ↑ 36% |
| 80 mg | ↑ 28% | ↑15% | |
| Fluconazole 200 mg QD for 11 days | 80 mg | ↑ 14% | ↑ 9% |
| * Single dose unless otherwise noted † Clinically significant [see DOSAGE AND ADMINISTRATION and Warnings and PRECAUTIONS] |
|||
Table 4. Effect of Rosuvastatin Co-Administration on Systemic Exposure To Other Drugs
| Rosuvastatin Dosage Regimen | Co-administered Drug | ||
| Name and Dose | Change in AUC | Change in Cmax | |
| 40 mg QD for 10 days | Warfarin* 25 mg single dose | R-Warfarin ↑4% S-Warfarin ↑6% | R-Warfarin ↓ 1% S-Warfarin 0% |
| 40 mg QD for 12 days | Digoxin 0.5 mg single dose | ↑ 4% | ↑ 4% |
| 40 mg QD for 28 days | Oral Contraceptive (ethinyl estradiol 0.035 mg & norgestrel 0.180, 0.215 and 0.250 mg) QD for 21 Days |
EE ↑ 26% NG ↑ 34% | EE ↑ 25% NG ↑ 23% |
| EE = ethinyl estradiol, NG = norgestrel *Clinically significant pharmacodynamic effects [See Warnings and PRECAUTIONS] |
|||
Animal Toxicology and/or Pharmacology
Embryo-fetal Development
Generic Name: Rosuvastatin Calcium
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