Sitagliptin Phosphate Tablets

This product is an oral antihyperglycemic drug in a class of drugs called dipeptidyl peptidase 4 (DPP-4) inhibitors, which can improve blood sugar control in patients with type 2 diabetes by increasing the levels of active incretin hormones. Incretin hormones include glucagon-like polypeptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are released from the intestine throughout the day and increase in levels after meals. Incretin hormones are part of an endogenous system involved in the physiological regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP can increase the synthesis and release of insulin by pancreatic beta cells through intracellular signaling pathways involving cyclic adenosine monophosphate. In animal models of type 2 diabetes, treatment with GLP-1 or DPP-4 inhibitors can improve the responsiveness of pancreatic beta cells to glucose and promote insulin biosynthesis and release. As insulin levels increase, the uptake of glucose by tissues increases. In addition, GLP-1 can also inhibit the secretion of glucagon by pancreatic alpha cells. The reduction in glucagon concentrations and the increase in insulin levels reduce hepatic glucose production, thereby reducing blood glucose levels. The effects of GLP-1 and GIP are glucose-dependent, and when blood glucose concentrations are low, GLP-1 does not promote insulin release or inhibit glucagon secretion. When glucose levels are above normal, the effects of GLP-1 and GIP on insulin release are enhanced. In addition, GLP-1 does not impair the body's normal glucagon release response to low blood glucose. The activity of GLP-1 and GIP is limited by the enzyme DPP-4, which rapidly hydrolyzes incretins to produce inactive products. Sitagliptin prevents DPP-4 from hydrolyzing incretins, thereby increasing plasma concentrations of the active forms of GLP-1 and GIP. By increasing the levels of active incretins, sitagliptin can increase insulin release and reduce glucagon levels in a glucose-dependent manner. These changes in insulin and glucagon levels can reduce glycated hemoglobin A1c (HbA1c) and lower fasting and postprandial blood glucose levels in patients with type 2 diabetes who have hyperglycemia. Sitagliptin's glucose-dependent mechanism of action is different from that of sulfonylureas, which increase insulin secretion even at low glucose levels, thereby causing hypoglycemia in patients with type 2 diabetes and normal subjects.

Sitagliptin phosphate. Chemical name: 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolone[4,3-a]pyrazine phosphate (1:1) monohydrate

Light brown film-coated tablets, appearing white or off-white after removing the coating.

Suitable for patients with type 2 diabetes; this medicine can have a certain therapeutic effect when exercise, diet and medication are not well controlled.

The recommended dose of this product as a monotherapy is 100 mg once daily. This product can be taken with or without food.

The following adverse reactions have been reported during postmarketing use of this drug. Because these adverse reactions are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Hypersensitivity reactions, including anaphylaxis, angioedema, rash, urticaria, cutaneous vasculitis, and exfoliative skin lesions, including Stevens-Johnson syndrome [see CONTRAINDICATIONS AND PRECAUTIONS]. Elevated liver enzymes; upper respiratory tract infection; nasopharyngitis; pancreatitis.

It is contraindicated for those who are allergic to any ingredient in this product.

Precautions for children: At present, the safety and effectiveness of this product in pediatric patients under 18 years of age have not been established. Precautions for pregnancy and lactation: During the period of embryonic organogenesis, oral administration of sitagliptin to rats and rabbits at doses up to 250 mg/kg and 125 mg/kg, respectively, did not produce malformations (32 times and 22 times the human exposure, respectively, based on the recommended daily dose of 100 mg for adults). A slightly increased incidence of embryonic rib malformations (absent, hypoplastic, and wavy ribs) was observed in rats at oral doses up to 1000 mg/kg per day (approximately 100 times the human exposure, based on the recommended daily dose of 100 mg for adults). A slight decrease in the mean pre-weaning body weight of male and female offspring was observed in rats at oral doses up to 1000 mg/kg, and an increase in the body weight of male offspring after weaning. However, the results of animal reproduction studies are not always predictive of human Elderly Precautions: In clinical studies, the safety and effectiveness of this product in elderly patients (65 years) were comparable to those in younger patients (65 years). No dose adjustment is required based on age. Elderly patients are more likely to have renal impairment; as with patients of other ages, dose adjustments are required for patients with severe renal impairment.

If used with other drugs, drug interactions may occur. Please consult your doctor or pharmacist for details.

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25 mg

24 months