Onglyza is indicated in adult patients with type II diabetes as a supplement to diet and exercise to improve glycemic control: as monotherapy, when metformin is impractical due to contraindications or intolerance; in combination with other drugs for the treatment of diabetes mellitus, including insulin, if they do not provide adequate glycemic control.
active substance: saxagliptin;
1 film-coated tablet contains saxagliptin hydrochloride in terms of saxagliptin 5 mg;
excipients: lactose monohydrate; microcrystalline cellulose, croscarmellose sodium, magnesium stearate and dyes for 5 mg: Opadray II white, Opadray II pink, Opakod blue.
Saxagliptin is a high-potency (Ki: 1.3 nM) selective reversible competitive inhibitor of DPP-4. In patients with type II diabetes, the use of saxagliptin inhibits the enzymatic activity of DPP-4 for a period of 24 hours. Following oral glucose loading, such inhibition of DPP-4 resulted in a 2–3-fold increase in circulating active hormone-incretin levels, including glucagon-like peptide-1 (GPP-1) and glucose-dependent insulinotropic polypeptide (GIC concentration and increase). glucose-dependent reactivity of beta cells, which resulted in increased concentrations of insulin and C-peptide. Increased insulin release by beta cells and decreased glucagon synthesis by pancreatic alpha cells have been associated with lower fasting glucose concentrations and decreased fluctuations in glucose levels after oral glucose loading or ingestion. Saxagliptin improves glycemic control by lowering fasting glucose and postprandial glycemia in patients with type 2 diabetes.
Onglyza is indicated in adult patients with type II diabetes as a supplement to diet and exercise to improve glycemic control:
- as monotherapy, when metformin is impractical due to contraindications or intolerance;
- in combination with other drugs for the treatment of diabetes mellitus, including insulin, if they do not provide adequate glycemic control.
Hypersensitivity to the active substance or to any of the excipients or a history of severe hypersensitivity reactions, including anaphylactic reaction, anaphylactic shock and angioneurotic edema to any dipeptidyl peptidase 4 inhibitor (DPP-4).
Safety and effectiveness in children have not been established, so the drug should not be used in children. No data available.
Use during pregnancy or breastfeeding
The use of saxagliptin in pregnant women has not been studied. The results of animal studies have shown reproductive toxicity when the drug is used in high doses. The potential risk for humans is unknown. The drug should not be prescribed during pregnancy, unless there is an urgent need.
It is unknown whether saxagliptin is excreted in human breast milk. Animal studies have shown excretion of saxagliptin and / or its metabolite in milk. The risk to the infant cannot be ruled out. Decisions to discontinue breastfeeding or drug therapy should be made taking into account the benefits of breastfeeding for the child and the benefits of therapy for the woman.
Method of application and dosage
The recommended dose of Onglyza is 5 mg once a day. When Onglyza is used in combination with insulin or a sulphonylurea, a lower dose of insulin or a sulphonylurea may be needed to reduce the risk of hypoglycaemia.
The drug has no clinically significant effect on the QTc interval or heart rate when administered orally in doses up to 400 mg per day for 2 weeks (80 times higher than the recommended dose). In case of overdose, appropriate maintenance treatment should be prescribed according to the patient’s clinical condition. Saxagliptin and its major metabolite can be removed by hemodialysis (23% of the dose within 4 hours).
- Infections and invasions: upper respiratory tract infections, urinary tract infections, gastroenteritis, sinusitis, nasopharyngitis;
- Metabolism and nutrition disorders: hypoglycemia;
- Nervous system disorders: dizziness, headache;
- Disorders of the gastrointestinal tract: abdominal pain, diarrhea, dyspepsia, flatulence, gastritis, nausea, vomiting;
- Disorders of the skin and subcutaneous tissue: rash, dermatitis, itching;
- General disorders and administration site conditions: fatigue.
Store at a temperature not exceeding 30 ° C. Keep out of reach of children.