Rosiglitazone hydrochloride

The main ingredient of this product is rosiglitazone hydrochloride, whose chemical name is 5-{4-[2-(N-methyl-N-(2-pyridinyl)-amino)-ethoxy]-benzyl}thiazolidine-2,4-dione hydrochloride monohydrate.

1 Drugs metabolized by cytochrome P450: In vitro drug metabolism studies have shown that rosiglitazone does not inhibit major P450 enzymes at clinically used doses. In vitro test data confirm that rosiglitazone is mainly metabolized by CYP2C8, and a very small part is metabolized by CYP2C9. 2 Nimodipine and oral contraceptives (ethinyl estradiol and norethindrone) are mainly metabolized by the CYP3A4 pathway, so co-administration with this product (4 mg, twice daily) will not produce clinically significant pharmacokinetic effects on the above two drugs. 3 Glibenclamide: For diabetic patients whose condition is stable after taking glibenclamide, co-administration of this product (2 mg/time, twice daily) with glibenclamide (3.75 mg/day to 10 mg/day) for 7 days will not change their 24-hour average steady-state blood glucose level. 4 Metformin: For healthy subjects, the co-administration of this product (2 mg/time, twice daily) and metformin (500 mg/time, twice daily) for 4 days will not change the steady-state pharmacokinetic parameters of this product and metformin. 5 Acarbose: Healthy subjects took acarbose (100 mg/time, 3 times a day) for 7 days, which had no effect on the pharmacokinetic parameters of a single oral dose of this product. 6 Digoxin: Healthy subjects took this product (8 mg/time, once a day) for 14 consecutive days, which had no effect on the steady-state pharmacokinetic parameters of digoxin (0.375 mg/time, once a day). 7 Warfarin: Continuous use of this product has no effect on the steady-state pharmacokinetic parameters of warfarin enantiomers. 8 Ethanol: Drinking a moderate amount of ethanol once does not increase the risk of acute hypoglycemia in patients with type 2 diabetes taking this product. 9 Ranitidine: Ranitidine (150 mg/time, twice daily) was taken by healthy subjects for 4 days, which did not change the pharmacokinetic parameters of rosiglitazone after single oral or intravenous administration. This result indicates that the increase of gastrointestinal pH does not affect the oral absorption of this product.

Rosiglitazone hydrochloride

1 Drugs metabolized by cytochrome P450: In vitro drug metabolism studies have shown that rosiglitazone does not inhibit major P450 enzymes at clinically used doses. In vitro test data have confirmed that rosiglitazone is mainly metabolized by CYP2C8, and a very small part is metabolized by CYP2C9. 2 Nimodipine and oral contraceptives (ethinyl estradiol and norethindrone) are mainly metabolized by the CYP3A4 pathway, so their co-administration with this product (4 mg, twice daily) will not have a clinically significant pharmacokinetic effect on the above two drugs. 3 Glibenclamide: For diabetic patients whose condition has stabilized after taking glibenclamide, this product (2 mg/time, twice daily) is combined with glibenclamide (3.75 mg/time to 10 mg/day).