Saterex tablets 30mg, No. 28

Type 2 diabetes mellitus (in combination with diet and exercise):

• as monotherapy in case of ineffectiveness of diet therapy and exercise in patients with a contraindication to the use of metformin;

• in combination with metformin as a starting therapy, or when diet and exercise in combination with monotherapy with one of the listed drugs does not lead to adequate glycemic control.

SaterexЃ is taken orally 1 time per day in the morning or in the evening, regardless of the meal. The tablets should be swallowed whole without chewing with water. The dosage regimen of the drug should be selected individually, depending on the effectiveness and tolerability. The recommended initial dose of the drug for monotherapy or as part of a two-component combination therapy with metformin is 20 mg per day. In the absence of reaching the target values ??for the concentration of glucose in the blood, the dose of the drug can be increased to 30 mg per day. If the goals of glycemic control are not achieved while using the maximum recommended daily dose of 30 mg, additional administration of metformin is recommended.

The dosage regimen for metformin should be selected based on the recommended doses for metformin. In case of missed intake of SaterexЃ, the usual dose should be taken as soon as possible after the discovery of the missed dose. It is unacceptable to take a double dose of SaterexЃ.

White film-coated tablets, round, biconvex; in cross section, the core of the tablet is white or almost white.

1 tab.

gozogliptin malate 40.986 mg,

which corresponds to the content of gozogliptin 30 mg

Excipients: microcrystalline cellulose - 260.676 mg, calcium hydrogen phosphate - 130.338 mg, sodium carboxymethyl starch - 13.5 mg, magnesium stearate - 4.5 mg.

- Hypersensitivity to gosogliptin or any component of the drug.

- Diabetes mellitus type 1.

- Diabetic ketoacidosis.

- Severe liver dysfunction.

- Chronic renal failure of severe severity.

- Children under 18 years of age (efficacy and safety of use has not been established).

- Pregnancy, breastfeeding period.

pharmachologic effect

Hypoglycemic agent.

Gozogliptin is an active, highly selective inhibitor of the enzyme dipeptidyl peptidase-4, indicated for the treatment of type 2 diabetes mellitus. By inhibiting the activity of DPP-4, gosogliptin increases the concentration of hormones of the incretin family synthesized in the intestine: glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). An increase in the concentration of GLP-1 and GIP causes an increase in the sensitivity of the beta cells of the pancreas to glucose, which leads to an increase in the synthesis and secretion of insulin. An increase in the concentration of GLP-1 causes an increase in the sensitivity of alpha cells of the pancreas to glucose, which leads to an improvement in glucose-dependent regulation of glucagon secretion. A decrease in the increased secretion of glucagon during meals causes a decrease in insulin resistance.A decrease in the concentration of glucagon against the background of an increase in the concentration of insulin, due to an increase in the concentration of GLP-1 and GIP, causes a decrease in the production of glucose by the liver, which leads to a decrease in the content of glucose in the blood. In patients with type 2 diabetes mellitus with hyperglycemia, these changes in insulin and glucagon secretion lead to a decrease in the concentration of glycated hemoglobin HbA1c and a decrease in plasma glucose concentration both on an empty stomach and after a meal.In patients with type 2 diabetes mellitus with hyperglycemia, these changes in insulin and glucagon secretion lead to a decrease in the concentration of glycated hemoglobin HbA1c and a decrease in plasma glucose concentration both on an empty stomach and after a meal.In patients with type 2 diabetes mellitus with hyperglycemia, these changes in insulin and glucagon secretion lead to a decrease in the concentration of glycated hemoglobin HbA1c and a decrease in plasma glucose concentration both on an empty stomach and after a meal.

With the use of gosogliptin in more than 750 patients with type 2 diabetes mellitus for 12 to 36 weeks, as monotherapy or in combination with metformin, there was a significant long-term decrease in the concentration of HbA1c, fasting blood glucose and 2 hours after meals. During treatment with gozogliptin, there was no significant change in body weight; the incidence of hypoglycemic episodes was minimal.

Pharmacokinetics

Gozogliptin is rapidly absorbed when taken orally with an absolute bioavailability of more than 99%. Cmax in blood plasma is reached within 1 hour after administration. Average plasma concentrations increase in proportion to the dose increase. The decrease in the concentration of gosogliptin in the blood plasma after reaching Cmax is biphasic. After taking gosogliptin at a dose of 30 mg, the AUC is, on average, 4800-5200 ng h / ml, the coefficient of individual AUC variability is 11.5-27.2%. Food intake increases the rate of absorption up to 2 hours, but does not significantly affect the degree of absorption and AUC. The combined use of gosogliptin with metformin does not affect the dynamics of their absorption.

The degree of binding of gozogliptin to plasma proteins is 11.5%.

The main metabolic pathway of gosogliptin in humans is associated with hydroxylation of the pyrimidine group. Other metabolites are associated with amide hydrolysis, carabamoyl glucuronidation, formamide conjugation, glucose conjugation, and creatinine conjugation. In in vitro studies using microsomal human liver enzymes, low binding constants and inhibition by gozogliptin of cytochromes CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 were noted.

Gozogliptin is excreted mainly by the kidneys. After oral administration, about 77% of the dose of gozogliptin is excreted by the kidneys, with 48.5% unchanged. 10.5% of the dose is excreted through the intestine, with a significant proportion of the metabolites of gosogliptin. T1 / 2 after oral administration is about 20 hours. Renal clearance of the free fraction of gosogliptin with preserved renal function is about 45 ml / min with a single dose of 20 mg.

Side effect

From the immune system: infrequently - allergic dermatitis.

From the nervous system: infrequently - dizziness, headache, drowsiness.

From the digestive system: infrequently - constipation, diarrhea, dyspepsia, pancreatitis.

From the liver and biliary tract: infrequently - increased activity of liver enzymes (ALT, AST), cholecystitis, steatosis, increased bilirubin, gallbladder polyp.

From the side of the kidneys and urinary tract: infrequently - urinary tract infections.

Systemic disorders: infrequently - asthenia, fatigue, peripheral edema, back pain.

Application during pregnancy and lactation

The use is contraindicated during pregnancy and during breastfeeding.

Application for violations of liver function

The use is contraindicated in severe liver dysfunction.

Application for impaired renal function

The use is contraindicated in chronic renal failure of severe severity.

Application in children

The use is contraindicated in children under 18 years of age.

Use in elderly patients

No dose adjustment is required in elderly patients.

special instructions

Use in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis is contraindicated.

No dose reduction is required in patients with mild chronic renal failure. Due to the possibility of increasing the concentration of gosogliptin in the blood plasma in patients with moderate renal insufficiency, it is recommended to use it with caution in these patients. It is not recommended for use in patients with severe renal insufficiency due to the limited experience of use in this group of patients.

It is not recommended for use in patients with severe liver dysfunction (ALT or AST> 2.5 times higher than ULN) due to limited experience in this category of patients.

Influence on the ability to drive vehicles and mechanisms

While taking the drug, the risk of hypoglycemia must be taken into account. If dizziness develops during treatment, patients should not drive or operate machinery.

Drug interactions

Since gosogliptin is not a substrate for liver microsomal enzymes, nor does it inhibit or induce these enzymes, the interaction of gosogliptin with drugs that are substrates, inhibitors or inducers of liver microsomal enzymes is unlikely.

No clinically significant interaction of gozogliptin with drugs most commonly used in the treatment of type 2 diabetes mellitus has been established.

The combined use of gosogliptin with insulin, sulfonylurea derivatives, thiazolidinediones and other hypoglycemic drugs, with the exception of metformin, has not been studied.