Index of drugs

Treatment of type 2 diabetes to improve glycemic control in adult patients (> 18 years of age).Monotherapy: in patients with insufficient glycemic control who use only diet and exercise, in which Metformin is inappropriate due to contraindications or intolerance.As a component of 2-oral oral therapy: in combination with Metformin, when only metformin alone in combination with diet and exercise is insufficient to achieve adequate glycemic control; or in combination with a sulphonylurea, when the use of only a sulphonylurea compound in combination with diet and exercise is insufficient to achieve adequate glycemic control in patients who are not suited for using metformin; or in combination with a thiazolidinedione, when the use of only thiazolidinedione alone, in combination with diet and exercise, is not sufficient to achieve adequate glycemic control in patients in whom the use of thiazolidinedione is appropriate.As a component of 3-drug oral therapy: in combination with metformin and a sulphonylurea, when the use of only these drugs (metformin and a sulphonylurea) in combination with diet and exercise is not sufficient to achieve adequate glycemic control.In combination therapy with insulin (with or without metformin) when the use of only insulin alone with diet and exercise is not sufficient to achieve adequate glycemic control.

1 tabl contains 5 mg of saxagliptin (as hydrochloride). The preparation contains lactose.

A very strong, selective, reversible, competitive DPP-4 inhibitor. In patients with type 2 diabetes, it inhibits the enzyme activity of DPP-4 for 24 hours. After oral Glucose administration, DPP-4 inhibition caused a 2-3-fold increase in circulating, active incretin hormones, including glucagon-like peptide-1 (GLP-1 ) and glucose-dependent insulinotropic polypeptide (GIP), a decrease in glucagon, and an increase in glucose-dependent beta cell response, which resulted in increased insulin and C-peptide levels. Increased insulin secretion from pancreatic beta cells and decrease in the concentration of glucagon secreted by alpha cells pancreas was associated with lower fasting glucose levels and smaller increases in glycaemia after oral administration of glucose or after a meal. Saxagliptin, in patients with type 2 diabetes, improves glycemic control by reducing fasting and postmeal glucose. Following oral administration on an empty stomach, saxagliptin is rapidly absorbed, and the maximum concentration of the drug and the main metabolite is reached within 2 hours and 4 hours respectively. Binding to the blood proteins of saxagliptin and its major metabolite is negligible. Biotransformation of saxagliptin occurs primarily through CYP3A4 / 5. The major metabolite is also a selective, reversible, competitive DPP-4 inhibitor that has half the strength of saxagliptin. Medium T_0,5 in plasma for saxagliptin and its major metabolite is 2.5 h and 3.1 h, respectively, and the mean T_0,5 inhibition of the DPP-4 receptor was 26.9 h. Saxagliptin is excreted via the kidneys and liver; in 75% with urine (24% saxagliptin, 36% with its metabolite) and in 22% with faeces.

Hypersensitivity to saxagliptin or to any of the excipients or to severe hypersensitivity reactions to any of the other members of the family of dipeptidyl peptidase 4 (DPP4) inhibitors, including anaphylactic reactions, anaphylactic shock and angioedema.

It should not be used in patients with type 1 diabetes mellitus or in the treatment of diabetic ketoacidosis. The drug will not replace insulin in patients who require it. The efficacy and safety of saxagliptin in 3-packet oral therapy in combination with metformin and a thiazolidinedione has not been studied. When used concomitantly with a sulphonylurea or insulin, it may be necessary to reduce the dose of these medicines to reduce the risk of hypoglycaemia.Patients should be monitored for symptoms of acute pancreatitis (including persistent, severe abdominal pain); if pancreatitis is suspected, saxagliptin should be discontinued; if pancreatitis is confirmed, saxagliptin therapy should not be resumed. Special care should be taken in patients with a history of pancreatitis. Monitoring of renal function before starting treatment with saxagliptin and, in accordance with standard medical procedure, regularly during treatment is recommended. The drug should be used with caution in patients with severe renal insufficiency (do not use in end-stage renal failure requiring hemodialysis); with moderate hepatic insufficiency (do not use in severe hepatic insufficiency); with heart failure from group III-IV according to NYHA (limited experience); when concomitant treatment with CYP3A4 inducers (risk of hypoglycaemic effect decreases). The efficacy and safety profile of saxagliptin in patients with impaired immunity, eg organ transplants or acquired immune deficiency syndrome, has not been established. If severe hypersensitivity reactions to saxagliptin are suspected, the drug should be discontinued, other possible causes for adverse effects considered, and another alternative treatment for diabetes should be used. Patients being treated with saxagliptin are also advised to control the condition of the skin, in particular the presence of bullous lesions, ulcers or rashes. The safety and efficacy of this medicine in children <18 years has not been established. Due to the lactose content, the preparation should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.

Do not use during pregnancy unless clearly necessary. Saxagliptin and / or its metabolite are excreted in animal milk (it is not known whether they are excreted in human milk) - it should be decided whether to discontinue breast-feeding or discontinue treatment, taking into account the benefits of breastfeeding and the benefits of treatment for a woman.

Common: upper respiratory tract infections, urinary tract infections, gastrointestinal mucous membrane infections, nasal sinus infections, headache, abdominal pain, diarrhea, nausea, vomiting. Uncommon: pancreatitis, hypersensitivity reactions, dermatitis, pruritus, urticaria, rash. Rare: anaphylactic reactions (including anaphylactic shock), angioneurotic edema. The above actions occurred during saxagliptin monotherapy, as well as during combination therapy with metformin (applies to the use of saxagliptin after its addition to previous metformin therapy and starting treatment with saxagliptin in combination with metformin), combination therapy with sulfonylurea (glibenclamide) and combination therapy with thiazolidinedione. During the combination therapy with metformin there were also - often: nasal and throat infections, indigestion, gastritis, muscle pain; uncommon: joint pain, erectile dysfunction. During concomitant treatment with glibenclamide, there was an additional - very common: hypoglycaemia; uncommon: dyslipidemia, hypertriglyceridaemia. In combination with the thiazolidinedione, there was peripheral edema (common), and during combination therapy with metformin and a sulphonylurea - bloating (common). Dizziness and fatigue may also occur. Hospitalization for heart failure was more frequent with saxagliptin (3.5%) than with placebo (2.8%).

Orally. Adults: 5 mg once a day. If you miss a dose, take it as soon as possible; do not take a double dose on the same day. When using this medicine in combination with insulin or a sulphonylurea, it may be necessary to reduce the dose of insulin or a sulphonylurea.Special groups of patients. The dose adjustment is not recommended based on the patient's age alone. No dose adjustment is required in patients with mild renal impairment; in patients with moderate to severe renal impairment, take 2.5 mg once a day; it is not recommended for patients with end-stage renal disease (ESRD) requiring hemodialysis.No dose adjustment is required in patients with mild to moderate disturbances; use in patients with severe hepatic impairment is not recommended.Way of giving. The tablets can be taken with or without food, at any time of the day. The tablets must not be divided or crushed.