metformin hydrochloride, Saksahlyptyn | Combogliz tablets prolong 1000 + 5 mg, 28 pcs.

Release form

Film-release modified release tablets.

Packing

28 pcs.

Pharmacological action

Combogliz Prolong® combines two hypoglycemic drugs with complementary mechanisms of action for improving glycemic control in patients with type 2 diabetes mellitus (DM2): saxagliptin, a dipeptyl peptidase 4 inhibitor (DPP-4), and metformin, a class b representative.

Saxagliptin:

Hormones such as incretins, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (HIP), are released from the small intestine into the bloodstream in response to food intake.

These hormones help release insulin from the pancreatic beta cells, which depends on the concentration of glucose in the blood, but are inactivated by the enzyme DPP-4 for several minutes. GLP-1 also lowers the secretion of glucagon in pancreatic alpha cells, decreasing the production of glucose in the liver. In patients with type 2 diabetes, the concentration of GLP-1 is lowered, but the insulin response to GLP-1 remains. Saxagliptin, being a competitive inhibitor of DPP-4, reduces the inactivation of incretin hormones, thereby increasing their concentration in the bloodstream and leading to a decrease in fasting glucose after eating.

metformin:

Metformin is a hypoglycemic drug that improves glucose tolerance in patients with type 2 diabetes by lowering basal and postprandial glucose concentrations.

Metformin reduces liver glucose production, decreases intestinal glucose absorption, and increases insulin sensitivity, increasing peripheral glucose uptake and utilization. Unlike sulfonylurea preparations, metformin does not cause hypoglycemia in patients with type 2 diabetes or healthy people (except in special situations, see the sections “Precautions” and “Special Instructions”), and hyperinsulinemia. During metformin therapy, insulin secretion remains unchanged, although fasting insulin concentrations and in response to meals during the day may decrease.

Indications

Type 2 diabetes mellitus combined with diet and exercise to improve glycemic control.

Contraindications

- increased individual sensitivity to any component of the

preparation - serious hypersensitivity reactions (anaphylaxis or angioedema) to DPP-4 inhibitors

- type 1 diabetes mellitus (use not studied)

- use not studied

- congenital galactose intolerance, lactase deficiency and glucose-galactose malabsorption

- pregnancy, lactation

- age under 18 years (safety and efficacy not studied)

- naru renal function (serum creatinine 1.5 mg / dL [men], 1.4 mg / dL [women] or decreased creatinine clearance), including those caused by acute cardiovascular failure (shock), acute myocardial infarction and septicemia

- acute diseases, at which there is a risk of developing renal dysfunction: dehydration (with vomiting, diarrhea), fever, severe infectious diseases, conditions of hypoxia (shock, sepsis, kidney infections, bronchopulmonary diseases)

- acute or chronic metabolic acidosis, including diabetic ketoacidosis, with or without coma

- clinically pronounced manifestations of acute and chronic diseases that can lead to the development of tissue hypoxia (respiratory failure, heart failure, acute myocardial infarction)

- serious znye surgery and trauma (as shown holding insulin)

- human liver

- acute and chronic alcoholism, poisoning with ethanol

- lactic acidosis (including history)

- a period of at least 48 hours before and within 48 hours after conducting radioisotope or x-ray studies with the introduction of iodine-containing contrast agents

- adherence to a low-calorie diet (

With caution

In persons over the age of 60 who perform heavy physical work ( increased risk of developing lactic acidosis) and patients with a history of pancreatitis (no connection between taking the drug and an increased risk of developing pancreatitis has been established)

Use during pregnancy and lactation

Due to the fact that the use of the drug Combogliz Prolong during pregnancy has not been studied, the drug should not be prescribed during pregnancy.

It is not known whether saxagliptin or metformin passes into breast milk.

Since the possibility of penetration of the drug Combogliz Prolong into breast milk is not excluded, the use of the drug during lactation is contraindicated.

Special instructions

Lactic acidosis is a rare, serious metabolic complication that can develop as a result of cumulation of metformin during therapy with Combogliz Prolong. With the development of lactic acidosis due to the use of metformin, its concentration in the blood plasma exceeds 5 Ојg / ml.

In patients with diabetes mellitus, lactic acidosis often develops with severe renal failure, including due to congenital kidney disease and insufficient renal perfusion, especially when taking several drugs. In patients with heart failure, in particular, in patients with unstable angina or acute heart failure and a risk of hypoperfusion and hypoxemia, there is an increased risk of lactic acidosis.

The risk of developing lactic acidosis increases in proportion to the degree of renal failure and the age of the patient. Regular monitoring of renal function in patients taking metformin should be carried out and the minimum effective dose of metformin should be prescribed. In elderly patients, monitoring of renal function is necessary.

Metformin should not be prescribed to patients 80 years of age or older if renal function is impaired (according to QC data), as these patients are more prone to develop lactic acidosis. In addition, metformin therapy should immediately be discontinued if conditions accompanied by hypoxemia, dehydration or sepsis develop. Since liver failure can significantly limit the ability to excrete lactate, metformin should not be prescribed to patients with clinical or laboratory signs of liver disease.

Composition

Active ingredients:

metformin - 1000 mg

saxagliptin - 2.5 mg.

Dosage and administration

Inside, once a day during dinner. Tablets should be swallowed whole without chewing, crushing, or breaking. The dose should be selected individually. Typically, with a combination drug containing saxagliptin and metformin, the dose of saxagliptin is 5 mg once a day.

The recommended initial dose of metformin modified release is 500 mg once a day, it can be increased to 2000 mg once a day, which is ensured by taking 2 tablets 2.5 mg / 1000 mg taken once a day. The dose of metformin is increased gradually to reduce the risk of side effects from the gastrointestinal tract. The maximum daily dose: saxagliptin 5 mg and metformin modified release 2000 mg.

No specific studies have been conducted on the safety and efficacy of Combogliz Prolong in patients previously treated with other hypoglycemic agents and transferred to Combogliz Prolong.

Changes in the treatment of T2DM should be carried out with caution and with appropriate control of the concentration of glucose in the blood. When combined with powerful inhibitors of CYP3A4 / 5 isoenzymes (for example, ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir and telithromycin), the dose of saxagliptin should be 2.5 mg once a day.

The inactive ingredients of Combogliz Prolong can be excreted through the intestines as a soft, moist mass that can retain the shape of the pill taken.

Use in special patient groups

Elderly patients

Since saxagliptin and metformin are partially excreted by the kidneys, and in elderly patients, kidney function is likely to decrease, use Combogliz Prolong with caution in the elderly.

Saxagliptin

No differences in safety or efficacy in patients? 65 years old and young patients. Although there are no differences in responses to therapy between elderly patients and young patients, greater sensitivity in some elderly patients cannot be ruled out.

Metformin Controlled clinical trials of metformin did not include a sufficient number of elderly patients to determine differences in response to therapy compared to young patients. although clinical experience has not established differences in response between the elderly and young patients. As you know, metformin is largely excreted by the kidneys, and therefore there is a risk of developing serious adverse events in patients with renal failure. Combogliz Prolong should be prescribed only to patients with normal renal function. Initial and maintenance doses of metformin should be given to elderly patients, taking into account a possible decrease in renal function. Any dose adjustment should be carried out after a careful assessment of renal function.

Children

Safety and efficacy of the drug in patients under 18 years of age have not been studied.

Overdose

Saxagliptin

With long-term administration of the drug in doses up to 80 times the recommended, no symptoms of intoxication have been reported. In case of overdose, symptomatic therapy should be used. Saxagliptin and its major metabolite are eliminated by hemodialysis (excretion rate: 23% dose for 4 h).

Metformin

Metformin overdose has been reported, including over 50 g. Approximately 10% of cases have developed hypoglycemia, but its causal relationship with metformin has not been established. Lactoacidosis was observed in 32% of metformin overdoses. Metformin is excreted in dialysis, with a clearance of 170 ml / min.

Storage conditions

At a temperature not exceeding 30 РC.

Keep out of the reach and sight of children.

Shelf life

3 years.

Active ingredient

Metformin hydrochloride, Saxagliptin

Terms and conditions

prescription

Dosage form prolonged

tablets.

Possible product names

COMBOGLIZ PROLONG 1000MG + 5MG N28 TABL P / O

Combogliz Prolong 1000mg + 5mg Tab. with modif. exp. p / pl / rev X28

Combogliz prolong 1000mg + 5mg No. 28 tab

COMBOGLIZ PROLONG TAB. WITH MODIF. RELEASE. P / O CAPTURE. 1000MG + 5MG No. 28

COMBOGLIZ PROLONG TAB.MODIF.HISF. P.P. About 1000MG + 5MG No. 28

Bristol-Myers Squibb, USA