Xiliting Fultagliptin Benzoate Tablets

1. Indications and Usage
Type 2 Diabetes Mellitus: The drug is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus. It can be used as monotherapy or in combination with metformin.
Important Usage Limitations: It is not indicated for type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.
2. Dosage and Administration
Recommended Dosage: The recommended dose is 12 mg taken once daily.
Administration: Tablets can be taken with or without food. Swallow whole; do not chew or crush.
Renal Impairment: No dose adjustment is required for mild renal impairment. For moderate renal impairment (GFR ≥30 mL/min but <60 mL/min), the dose should be reduced to 6 mg once daily. There are no clinical data for severe renal impairment or end-stage renal disease.
Hepatic Impairment: There are currently no clinical data for patients with hepatic impairment.
3. Mechanism of Action
DPP-4 Inhibition: Fultagliptin selectively inhibits the enzyme DPP-4.
Hormonal Effect: This inhibition reduces the degradation of endogenous incretins, specifically glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).
Glycemic Regulation: Increased levels of active incretins lead to a glucose-dependent increase in insulin release and a decrease in glucagon secretion, thereby lowering blood glucose levels without causing significant hypoglycemia.
4. Safety and Warnings
Hypersensitivity: Contraindicated in patients with a history of serious hypersensitivity to fultagliptin or any excipients.
Pancreatitis: Cases of acute pancreatitis have been reported with DPP-4 inhibitors. Patients should be monitored for signs and symptoms of pancreatitis if unexplained severe abdominal pain occurs.
Severe Joint Pain: Severe and disabling joint pain has been reported with DPP-4 inhibitors.
Bullous Pemphigoid: Post-marketing reports of bullous pemphigoid requiring hospitalization and systemic treatment have been observed.
5. Adverse Reactions and Clinical Research
Adverse Reactions: The most common adverse reactions include elevated lipase, elevated amylase, and hypoglycemia (particularly when combined with other antidiabetic agents). Other reported reactions include high uric acid, elevated creatine phosphokinase, and hepatic function abnormalities.
Clinical Research: Clinical trials have demonstrated that fultagliptin effectively improves glycemic control when used as monotherapy or in combination with metformin, with a low risk of hypoglycemia and weight gain.
6. Drug Interactions
CYP450 Substrates: Fultagliptin is primarily excreted unchanged in the urine and is not significantly metabolized by CYP450 enzymes; therefore, significant interactions with CYP450 substrates, inducers, or inhibitors are unlikely.
Other Antidiabetic Agents: When used in combination with insulin or sulfonylureas, there is an increased risk of hypoglycemia, and the dose of the concomitant agent may need to be reduced.
7. Pharmaceutical Information
Composition: The active ingredient is fultagliptin benzoate.
Appearance: Typically white or off-white circular or oval tablets.
Storage: Store at controlled room temperature. Protect from moisture.