Exendin-4

The active ingredient of Exenatide Microspheres for Injection is Exenatide. Excipients: Exenatide Microspheres for Injection: glycolide-lactide copolymer (50:50), sucrose. Solvents for Injection: sodium carboxymethyl cellulose, sodium chloride, polysorbate 20, sodium dihydrogen phosphate monohydrate, sodium dihydrogen phosphate heptahydrate, water for injection.

Acetaminophen After 14 weeks of treatment with exenatide microspheres (2 mg per week), 1000 mg acetaminophen tablets (taken on an empty stomach or with food) were administered, and no significant changes in acetaminophen AUC were observed compared with the control period. Acetaminophen Cmax decreased by 16% (fasting) and 5% (fed), and Tmax increased from approximately 1 hour in the control period to 1.4 hours (fasting) and 1.3 hours (fed). Exenatide injection has been studied for interactions with the following drugs. The potential drug interactions of exenatide microspheres for injection are expected to be similar to those of exenatide injection. Digoxin Co-administration of repeated doses of exenatide injection 30 minutes before oral digoxin (0.25 mg once daily) can reduce the Cmax of digoxin by 17% and delay Tmax by approximately 2.5 hours; however, the overall steady-state pharmacokinetic exposure (such as AUC) is not changed. Lovastatin Compared with lovastatin alone, administration of exenatide injection (10 μg twice daily) 30 minutes before oral administration of lovastatin (40 mg, single dose) reduced lovastatin AUC and Cmax by approximately 40% and 28%, respectively, and delayed Tmax by approximately 4 hours. In a 30-week controlled clinical study of exenatide injection, patients who were already taking HMG-CoA reductase inhibitors did not experience any corresponding changes in blood lipid levels compared to baseline when using exenatide injection. Lisinopril In patients with mild to moderate hypertension taking a constant dose of lisinopril (5-20 mg/day), the co-administration of exenatide injection (10 μg twice daily) did not change the steady-state Cmax or AUC of lisinopril, and Tmax was delayed by 2 hours. The patients' 24-hour average systolic and diastolic blood pressure did not change. Oral contraceptives The effects of exenatide injection (10 μg twice daily) on single-dose and multiple-dose oral contraceptives (30 μg ethinyl estradiol plus 150 μg levonorgestrel) were studied in healthy female subjects. Repeated oral contraceptives (OCs) administered 30 minutes after exenatide injection decreased the Cmax of ethinyl estradiol and levonorgestrel by 45% and 27%, respectively, and delayed the Tmax of ethinyl estradiol and levonorgestrel by 3.0 hours and 3.5 hours, respectively, compared with oral contraceptives alone. Daily repeated administration of the OC 1 hour before exenatide injection decreased the mean Cmax of ethinyl estradiol by 15%, but did not significantly change the mean Cmax of levonorgestrel, compared with OC alone. For both regimens, exenatide injection did not alter the mean trough concentration of levonorgestrel after repeated daily administration of an oral contraceptive. However, when the OC was administered 30 minutes after exenatide injection, the mean trough concentration of ethinyl estradiol was increased by 20%, compared with OC alone. In this study, the possible effect of food on OC interfered with the effect of exenatide injection on OC pharmacokinetics. Warfarin In healthy volunteers, repeated doses of exenatide injection (dosing days 1-2: 5 μg twice daily, days 3-9: 10 μg twice daily) were given 35 minutes after warfarin (25 mg), and warfarin Tmax was delayed by 2 hours. No clinically relevant effects on the Cmax or AUC of warfarin S- and R-enantiomers were observed. Exenatide injection did not significantly change the pharmacodynamic properties of warfarin (assessed by INR response).

The main ingredient of this product is Exenatide.