Saterex pills 30mg, 28pcs

Composition

Active ingredient: Gosogliptin malate 40,986 mg (based on Gosogliptin 30 mg). Auxiliary substances: microcrystalline cellulose,260.676 mg, calcium hydrophosphate,130.338 mg, sodium carboxymethyl starch,13,500 mg, magnesium stearate,4,500 mg, polyvinyl alcohol,7,200 mg, titanium dioxide,4,500 mg, macrogol 4000,3,636 mg, talc,2,664 mg

Pharmacological action

Gosogliptin is an active, highly selective inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4), intended for the treatment of type 2 diabetes mellitus. By inhibiting the activity of DPP-4, gosogliptin increases the concentration of incretin family hormones 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 pancreatic beta cells to glucose, which leads to an increase in the synthesis and secretion of insulin. An increase in the GLP-1 concentration causes an increase in the sensitivity of pancreatic alpha cells to glucose, which leads to an improvement in the glucose-dependent regulation of glucagon secretion. A decrease in increased glucagon secretion 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 glucose production by the liver, which leads to a decrease in blood glucose. 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 the concentration of glucose in blood plasma both on an empty stomach and after meals. When using 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. No significant changes in body weight were observed during treatment with gosogliptin; the frequency of episodes of hypoglycemia was minimal.

Indications

Type 2 diabetes mellitus (combined with diet therapy and exercise): · as monotherapy in case of ineffectiveness of diet therapy and exercise in patients with contraindications 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 do not lead to adequate glycemic control.

Contraindications

-Hypersensitivity to gosogliptin or any component of the drug. — Type 1 diabetes mellitus. – Diabetic ketoacidosis. – Severe liver function disorders. — Severe chronic renal failure. – Children under 18 years of age (the effectiveness and safety of use has not been established). – Pregnancy, breast-feeding period. With caution In patients with a history of pancreatitis. It is recommended to use Saterex® with caution in patients with moderate chronic renal failure.

Side effects

When using Saterex® alone or in combination with metformin, most adverse events (AES) were mild, temporary, and did not require discontinuation of therapy. No correlation was found between the incidence of AE and age, gender, ethnicity, duration of use, or dosage regimen. The following criteria were used to assess the incidence of AE: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10000, When using Gosogliptin at doses of 20 mg and 30 mg once a day, the frequency of discontinuation of therapy due to the development of AE was 1.3%. According to the results of clinical studies, the frequency of episodes of symptomatic hypoglycemia in patients treated with Gosogliptin did not exceed 1% and, as a rule, was associated with dietary disorders and increased physical activity. There were no cases of severe hypoglycemia in the Gosogliptin treatment groups. When using the drug Saterex® at a dose of 20 mg and 30 mg once a day as monotherapy against the background of monotherapy with gosogliptin, associated or possibly associated AES were observed in 2.7% of patients. No severe AES were reported in clinical trials. The following AES were observed: Immune system disorders: infrequently-allergic dermatitis. Nervous system disorders: infrequently – dizziness, headache, drowsiness. Gastrointestinal disorders: infrequently-constipation. Liver and biliary tract disorders: infrequently-increased activity of “liver” enzymes (ALT, AST). General disorders and disorders at the injection site: infrequently-asthenia, fatigue. When combining the drug Saterex® at a dose of 20 mg and 30 mg 1 time per day with metformin On the background of combination therapy with metformin with unmodified release (1000-2000 mg/day), AES associated or possibly associated with the drug were observed in 3.3% of patients. The following AES were observed: Nervous system disorders: infrequently-headache. Gastrointestinal disorders: infrequently – diarrhea, dyspepsia, pancreatitis. Liver and gallbladder disorders: infrequently-cholecystitis, steatosis, increased activity of “liver” enzymes (ALT, AST), increased bilirubin, gallbladder polyp. Renal and urinary tract disorders: infrequently-urinary tract infections. General disorders and disorders at the injection site: infrequently-peripheral edema, back pain.

Interaction

Gosogliptin has a low potential for drug interaction. Since gosogliptin is not a substrate of microsomal liver enzymes, nor does it inhibit or induce these enzymes, the interaction of gosogliptin with drugs that are substrates, inhibitors or inducers of microsomal liver enzymes is unlikely. No clinically significant interaction of gosogliptin with drugs most commonly used in the treatment of type 2 diabetes mellitus has been established. Concomitant use of gosogliptin with insulin, sulfonylurea derivatives, thiazolidinediones, and other hypoglycemic drugs, with the exception of metformin, has not been studied.

How to take, course of use and dosage

Saterex® is taken orally once a day in the morning or evening, regardless of food intake. Tablets should be swallowed whole, without chewing, washed down with water. The dosage regimen of the drug should be selected individually, depending on the effectiveness and tolerability. The recommended starting 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 achieving the target blood glucose concentration, the dose of the drug can be increased to 30 mg per day. If the goals of glycemic control are not achieved with the maximum recommended daily dose of 30 mg, additional use of metformin is recommended. The metformin dosage regimen should be selected based on the recommended doses for metformin. If you miss taking Saterex®, the usual dose should be taken as soon as possible after the fact of the omission is detected. It is unacceptable to take a double dose of Saterex®. Elderly No dose adjustment is required in elderly patients. Use in patients with hepatic dysfunctionas the experience of using gosogliptin in patients with severe hepatic impairment is limited, the drug is not recommended for use with an increase in ALT or AST > 2.5 times higher than the upper limit of normal (ULN). Use in patients with impaired renal function in patients with mild chronic renal failure, no dose adjustment is required. In patients with moderate chronic renal failure, it is recommended to limit the daily dose to 20 mg. Saterex® is not recommended for use in patients with severe chronic renal failure due to limited experience in this group of patients.

Overdose

Clinical studies of Saterex® in healthy volunteers have shown good tolerability of gosogliptin at a dose of up to 300 mg. A dose of more than 300 mg has not been studied. With a single use of the drug in a dose of 300 mg, dizziness, muscle pain, dry mouth may occur. All symptoms of overdose and changes in laboratory parameters disappear after discontinuation of the drug. In case of overdose, it is necessary to carry out generally accepted measures: gastric lavage, monitoring of vital signs, symptomatic therapy if necessary. It is possible to remove the drug from the body with a 3-4-hour dialysis.

Special instructions

The use of Saterex® 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 blood plasma in patients with moderate renal insufficiency, it is recommended to use the drug with caution in these patients. It is not recommended to use the drug in patients with severe renal insufficiency due to the limited experience of use in this group of patients. The drug is not recommended for use in patients with severe hepatic impairment (ALT or AST > 2.5 times higher than ULN) due to the limited experience of using the drug in this category of patients.

Storage conditions

In a dark place at a temperature not exceeding 30 °C. Keep out of reach of children.

Shelf

life is 4 years. The drug should not be used after the expiration date

Active ingredient

Gosogliptin

Conditions of release from pharmacies

By prescription

Dosage form

Tablets