Janumet (metformin + sitagliptin) coated tablets 50 mg/1000 mg. №56

Description

Janumet Storage:

active substances: sitagliptin, metformin hydrochloride;

1 film-coated tablet contains sitagliptin phosphate monohydrate equivalent to 50 mg sitagliptin and 500 mg or 850 mg or 1000 mg of metformin hydrochloride;

excipients: microcrystalline cellulose, povidone, sodium lauryl sulfate, sodium stearyl fumarate;

tablet shell: dye Opadray II 85F94203 pink (tablets 50 mg / 500 mg) or Opadray II 85F94182 pink (tablets 50 mg / 850 mg), or Opadray II 85F15464 red (tablets 50 mg / 1000 mg);

dye composition: polyvinyl alcohol, titanium dioxide (E 171), polyethylene glycol 3350, talc, iron oxide black (E 172), iron oxide red (E 172).

Janumet Dosage form.

Film-coated tablets.

Basic physical and chemical properties:

50/500 mg tablets: film-coated tablets, light pink engraved with “575” on one side and smooth on the other side;

50/850 mg tablets: film-coated tablets, pink with engraving “515” on one side and smooth on the other side;

50/1000 mg tablets: film-coated tablets, red with “577” engraving on one side and smooth on the other.

Pharmacotherapeutic group.

A combination of oral hypoglycemic drugs. ATX code A10BD07.

Janumet Pharmacological properties.

Pharmacodynamics.

Janumet is a combination of two hypoglycemic drugs with a complementary mechanism of action designed to improve glycemic control in patients with type II diabetes: sitagliptin, a dipeptidyl peptidase 4 (DPP-4) inhibitor, and metformin hydrochloride metformin.

Sitagliptin is active when taken orally, a potent, highly selective inhibitor of the enzyme dipeptidyl peptidase 4 (DPP-4), which is indicated for the treatment of type II diabetes. The pharmacological effects of the class of DPP-4 inhibitors are mediated by the activation of incretins. By inhibiting DPP-4, sitagliptin increases the concentration of two known active hormones of the incretin family: glucagon-like peptide 1 (GPP-1) and glucose-dependent insulinotropic polypeptide (GIP). Incretins are part of the internal physiological system of regulation of glucose homeostasis. At normal or raised level of glucose of blood GPP-1 and GIP promote increase in synthesis and secretion of insulin by beta cells of a pancreas. GLP-1 also inhibits the secretion of glucagon by alpha cells of the pancreas, thus reducing glucose synthesis in the liver. If the blood glucose level is low, insulin release is not enhanced and glucagon secretion is not suppressed. As a highly selective and effective inhibitor of the enzyme DPP-4, sitagliptin in therapeutic concentrations does not inhibit the activity of related enzymes DPP-8 or DPP-9. Sitagliptin differs in chemical structure and pharmacological action from analogues of GPP-1, insulin, sulfonylurea derivatives or meglitinides, biguanides, gamma-receptor agonists, which are activated by peroxisome proliferators (PPAR-), alpha-glycose inhibitors.

In a two-day study in healthy volunteers, sitagliptin increased the concentration of active GLP-1 in mono-mode, whereas metformin in mono-mode increased the concentrations of active and total GPP-1 at a similar level.

Simultaneous administration of sitagliptin and metformin had an additional potentiating effect on the concentration of active GPP-1. Sitagliptin, in contrast to metformin, increased the concentration of active HIP.