Description
Saterex Pharmacodynamics
Gozogliptin is an active, highly selective inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4) for the treatment of type 2 diabetes. By inhibiting DPP-4 activity, gozogliptin increases the concentration of the intestinal hormones of the insectin family: glucagon-like peptide-1 (GFP-1) and glucose-dependent insulinotropic polypeptide (GIP). Increased concentration of GFP-1 and GIP causes increased sensitivity of pancreatic beta cells to glucose, which leads to increased synthesis and secretion of insulin. Increased concentration of GFP-1 causes increased sensitivity of pancreatic alpha cells to glucose, which leads to improved glucose-dependent regulation of glucagon secretion. A decrease in increased glucagon secretion during meals causes a decrease in insulin resistance. Decrease of glucagon concentration against the background of increased insulin concentration, caused by increased concentration of GFP-1 and GIP, causes decrease of glucose production by liver, which leads to decrease of glucose content in blood. In patients with type 2 diabetes mellitus with hyperglycemia, these changes in insulin and glucagon secretion lead to a decrease in glycated hemoglobin HbA1c concentration and a decrease in plasma glucose concentration both on an empty stomach and after a meal.
When using gosogliptin in more than 750 patients with type 2 diabetes for 12 to 36 weeks as monotherapy or in combination with metformin, a significant long-term decrease in HbA1c, blood glucose concentration on an empty stomach and 2 hours after a meal was observed. No significant changes in body weight were observed during gosogliptin treatment; the frequency of hypoglycemic episodes was minimal.
Indications
Type 2 diabetes mellitus (in combination with diet therapy and exercise):
– As monotherapy if diet therapy and exercise are ineffective in patients with a contraindication to the use of metformin;
– in combination with metformin as initial therapy, or when diet and exercise in combination with monotherapy with one of the listed drugs does not lead to adequate glycemic control.
Contraindications
– Hypersensitivity to gosogliptin or any component of the drug.
– Diabetes mellitus type 1.
– Diabetic ketoacidosis.
– Severe impairment of liver function.
– Severe chronic renal insufficiency.
– Childhood under 18 years of age (efficacy and safety of use have not been established).
– Pregnancy, breast-feeding period.
Directions for use and dosages
- The preparation Saterex ® is taken orally once a day in the morning or evening, regardless of meals. The tablets should be swallowed whole, without chewing and with water. The drug dosage regimen should be selected individually depending on the efficacy and tolerability.
- Recommended initial dose of the drug during monotherapy or in two-component combination therapy with metformin is 20 mg per day. If target blood glucose values are not achieved, the drug dose may be increased to 30 mg per day. If glycemic control goals are not achieved at the maximum recommended daily dose of 30 mg, additional administration of metformin is recommended. Metformin dosing regimen should be chosen based on the recommended doses for metformin.
- In case of missing a dose of Saterex8′, the usual dose should be taken as soon as possible after discovering the fact of missing the dose. Do not take a double dose of Saterex®.
- Older age.
- No adjustment of the drug dose is required in elderly patients.
- Use in hepatic dysfunction
- As there is limited experience in using gosogliptin in patients with severe hepatic impairment, it is not recommended to use in ALT or ACT > 2.5 times the upper limit of normal (ULN).
- Use in impaired renal function
- In patients with chronic renal insufficiency of mild degree of severity, correction of the drug dose is not required. In patients with moderate chronic renal failure it is recommended to limit the daily dose to 20 mg. It is not recommended to use Satereks in patients with chronic renal failure of severe severity due to limited experience of use in this group of patients.
