Omarigliptin is a long-acting inhibitor of DPP-4, an enzyme that degrades theincretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Thus, Omarigliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation.
Omarigliptin is a long-acting inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent
insulinotropic polypeptide (GIP). Thus, Omarigliptin increases the concentrations of active incretin hormones, stimulating the release of insulin in a glucose-dependent manner and decreasing the levels of glucagon in the circulation. Both incretin hormones are involved in the physiological regulation of glucose homeostasis. Incretin hormones are secreted at a low basal level throughout the day and levels rise immediately after meal intake. GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. Furthermore, GLP-1 also
reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output.
Wikitin 12.5 Tablet: Each film-coated tablet contains Omarigliptin INN 12.5 mg.
Wikitin 25 Tablet: Each film-coated tablet contains Omarigliptin INN 25 mg.
Omarigliptin is a once-weekly DPP-4 inhibitor indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
The usual recommended dose of Omarigliptin is 25 mg once weekly as monotherapy or as add-on therapy for optimization of glycemic control. The
dosage should be reduced to 12.5 mg once weekly in patients with severe renal dysfunction and in patients with end-stage renal failure or in those requiring hemodialysis or peritoneal dialysis according to the following table:
| Renal dysfunction Dose | Serum creatinine values (mg/dL) *eGFR<30 |
Dose |
| Severe end-stage kidney failure |
Men: Cr>1.9 | 12.5 mg once a week |
| Women: Cr>1.4 |
*Conversion value corresponding to the eGFR (60 years of age)
Patients with a history of hypersensitivity to components of this drug. Severeketosis, diabetic coma, or precoma in type 1 diabetes patients. Severe infection in
which glycemic control is desired by insulin injection, before and after surgery. The efficacy and safety of concomitant administration of this drug and insulin preparations have not been studied.
If pancreatitis is suspected, Omarigliptin should promptly be discontinued and appropriate management should be initiated. Dosage adjustment should be recommended in patients with moderate or severe renal insufficiency and in patients with ESRD. Assessment of renal function should be recommended prior to initiating Omarigliptin. When Omarigliptin is used in combination with sulfonylurea or with insulin, medications known to cause hypoglycemia, a lower dose of sulfonylurea or insulin may be required to reduce the risk of hypoglycemia. If a hypersensitivity reaction is suspected, Omarigliptin should be discontinued.
Following patients or conditions that might cause low blood sugar:
1. Pituitary dysfunction or adrenal insufficiency
2. Malnutrition, starvation, irregular dietary intake, lack of dietary intake or
debilitated state
3. Intense muscle movement
4. Excessive alcohol intake
5. The elderly
Hypoglycemia, acute pancreatitis, bowel obstruction, and intestinal obstruction. Other side effects are Gastrointestinal problems, constipation, diarrhea, skin and subcutaneous tissue disorders.
Interaction of Omarigliptin is with the following: Metformin, Glimepride, Oral contraceptives, Atorvastatin
Elderly population: Often renal function is reduced in elderly patients and this drug is mainly excreted via the kidney. Care must be taken especially in patients
with severe renal dysfunction, and end-stage renal failure patients requiring hemodialysis or peritoneal dialysis. Children: The safety and efficacy of this drug in
children have not been established. Pregnant woman: Clinical trials targeting pregnant women have not been performed so its safety cannot be predicted. Breastfeeding should be avoided.
Wikitin 12.5 Tablet: Each box contains 4’s tablets in Alu-Alu blister pack.
Wikitin 25 Tablet: Each box contains 4’s tablets in Alu-Alu blister pack.
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