Beilisu Sitagliptin and Metformin Hydrochloride Extended-release Tablets

1. Indications and Usage
Type 2 Diabetes: Adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Treatment Regimen: Not recommended for patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Standard Dosage: The maximum recommended daily dose is 100 mg sitagliptin and 2000 mg metformin.
Critical Administration Instructions:
Meal Timing: Must be taken with meals to reduce metformin-associated gastrointestinal adverse reactions. Usually administered once daily.
Swallowing: Tablets must be swallowed whole. They must not be split, chewed, or crushed.
3. Mechanism of Action
DPP-4 Inhibition: Sitagliptin inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), increasing the levels of active incretin hormones (GLP-1 and GIP). This promotes glucose-dependent insulin secretion and suppresses glucagon release.
Metformin Action: Metformin decreases hepatic glucose production, decreases intestinal glucose absorption, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization.
4. Safety and Warnings
Lactic Acidosis: A rare but serious metabolic complication associated with metformin accumulation. Risk increases with renal impairment, acute hypoxic states, and alcohol abuse.
Renal Impairment: Contraindicated in patients with severe renal impairment (eGFR below 45 mL/min/1.73 m²). Renal function must be assessed prior to initiation and routinely thereafter.
Hypersensitivity: Severe hypersensitivity reactions (e.g., angioedema, exfoliative dermatitis, Stevens-Johnson syndrome) have been reported.
Vitamin B12 Deficiency: Long-term use may decrease vitamin B12 levels; periodic monitoring is recommended.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Diarrhea, nausea, vomiting, headache, and upper respiratory tract infection.
Serious Adverse Reactions: Lactic acidosis, acute pancreatitis, and severe cutaneous adverse reactions.
6. Drug Interations
Alcohol: Increases the risk of lactic acidosis and hypoglycemia.
Iodinated Contrast Media: Renal function must be evaluated prior to imaging procedures. The drug should be discontinued at the time of or prior to the procedure and not restarted until 48 hours later, provided renal function is stable.
Carbonic Anhydrase Inhibitors: Concomitant use may increase the risk of lactic acidosis.
7. Pharmaceutical Information
Chemical Composition: Active Ingredients: Sitagliptin and Metformin Hydrochloride.
Appearance: Film-coated tablets (colors and shapes vary by specific formulation).
Packaging: Available in various strengths (e.g., 50 mg sitagliptin/1000 mg metformin).
Storage: Store at controlled room temperature in a well-closed container.