Lipostat Drug Interactions

Inhibitor of CYP 3A4: Concomitant administration of Atorvastatin with inhibitor of CYP 3A4 can lead to increase in plasma concentration of Atorvastatin. The extent of interaction and potentiation of effects depend on the variability of effect on CYP 3A4.
Transporter inhibitors: Atorvastatin and Atorvastatin-metabolites are substrates of the organic aniontransporting polypeptide 1B1 (OATP1B1) transporter. Inhibitors of the OATP1B1 (e.g. cyclosporine) can increase the bioavailability of Atorvastatin.
Macrolide antibiotics: Co-administration of Atorvastatin with clarithromycin or erythromycin, known inhibitors of CYP 3A4, was associated with higher plasma concentration of Atorvastatin. Concomitant use of Atorvastatin and macrolide antibiotics e.g. clarithromycin, erythromycin increases the risk of myopathy or rhabdomyolysis.
Protease inhibitors: Co-administration of Atorvastatin with protease inhibitors, known inhibitors of CYP 3A4, was associated with increased plasma concentrations of Atorvastatin.
Diltiazem hydrochloride: Co-administration of Atorvastatin with diltiazem was associated with higher plasma concentrations of Atorvastatin.
Azole antifungals: Following concomitant use of Atorvastatin and azole antifungal e.g. itraconazole, Atorvastatin peak plasma concentration and area under the plasma concentration-time curve (AUC) were increased.
Grapefruit juice: Contains one or more components that inhibit CYP 3A4 and can increase plasma concentrations of Atorvastatin, especially with excessive grapefruit juice consumption (> 1.2 L/day).
Lomitapide: Following concomitant use of Atorvastatin with lomitapide, peak plasma concentration and AUC of Atorvastatin were increased.
Niacin: Concomitant use of Atorvastatin and antilipemic dosages (1 g daily or higher) of niacin increase the risk of myopathy.
Fibric acid derivatives: Concomitant use of Atorvastatin and fibric acid derivatives e.g. gemfibrozil, fenofibrate increases the risk of myopathy.
Inducer of CYP 3A4: Concomitant administration of Atorvastatin with inducer of CYP 3A4 (e.g. efavirenz, rifampin) can lead to variable reductions in plasma concentration of Atorvastatin. Due to the dual interaction mechanism of rifampin (CYP 3A4 induction and inhibition of hepatocyte uptake transporter OATP1B1), simultaneous co-administration 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.
Antacid: Co-administration of Atorvastatin with an oral antacid suspension containing magnesium and aluminium hydroxides decreased Atorvastatin plasma concentrations (approximate 35%); however, LDL-C reduction was not altered.
Bile acid sequestrants: Plasma concentrations of Atorvastatin were lower by concomitant use with bile acid sequestrants e.g. colestipol. However, lipid effects were greater when co-administered than either drug was given alone.
Digoxin: When multiple doses of digoxin and 10 mg Atorvastatin were co-administered, steady-state plasma digoxin concentration were unaffected. However, digoxin concentrations increased following administration of digoxin with 80 mg Atorvastatin daily. Patients taking digoxin should be monitored appropriately.
Oral contraceptives: Co-administration of Atorvastatin with an oral contraceptive containing norethindrone and ethinyl estradiol increased the AUC of norethindrone and ethinyl estradiol by approximately 30% and 20%. These increases should be considered when selecting an oral contraceptive for woman taking Atorvastatin.
Warfarin: An Atorvastatin interaction study with warfarinwas conducted, and no clinically significant interactions were seen. Monitoring of the International normalized ratio (INR) after initiation of a statin or a change in statin dosage is recommended.
Colchicine: Myopathy, including rhabdomyolysis has been reported in patient receiving Atorvastatin concomitantly with colchicine.
Fusidic acid: Rhabdomyolysis has been reported with this combination.