Buy Yanumet tablets 1000mg + 50mg №56
  • Buy Yanumet tablets 1000mg + 50mg №56

Janumet pills 1000mg + 50mg №56

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56 pcs.

Mechanism of action

The drug Janumet is a combination of two hypoglycemic drugs with a complementary (complementary) mechanism of action designed to improve glycemia control in patients with type 2 diabetes: sitagliptin, an inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4), and Metformin, a member of the biguanide class.

Sitagliptin is active when taken orally, a highly selective inhibitor of DPP-4, intended for the treatment of type 2 diabetes. The pharmacological effects of the class of drugs inhibiting DPP-4 are mediated by activation of incretins. Inhibiting DPP-4, sitagliptin increases the concentration of two known active hormones of the incretin family: glucagon-like peptide 1 (GLP-1) and glucose-dependentinsulinotropic polypeptide (HIP). Incretins are part of the internal physiological system for regulating glucose homeostasis. At normal or elevated blood glucose concentrations, GLP-1 and HIP contribute to an increase in insulin synthesis and secretion by pancreatic beta cells. GLP-1 also suppresses glucagon secretion by pancreatic alpha cells, reducing, thus, the synthesis of glucose in the liver. This mechanism of action differs from the mechanism of action of sulfonylurea derivatives, which stimulate insulin release and at low concentrations of blood glucose, which is fraught with the development of sulfonyl-induced hypoglycemia not only in patients with type 2 diabetes, but also in healthy individuals. Being a highly selective and effective inhibitor of the enzyme DPP-4, sitagliptin at therapeutic concentrations does not inhibit the activity of the related enzymes DPP-8 or DPP-9. Sitagliptin differs in chemical structure and pharmacological action from GLP-1 analogues, insulin, sulfonylurea derivatives or meglitinides, biguanides, gamma-receptor-activated gamma receptor agonists (PPARy), alpha-glycosidase inhibitors and amylin analogues.

Metformin is a hypoglycemic drug that increases glucose tolerance in patients with type 2 diabetes, reducing the basal and postprandial glucose concentration in the blood. Its pharmacological mechanisms of action differ from the mechanisms of action of oral hypoglycemic drugs of other classes.Metformin reduces the synthesis of glucose in the liver, reduces the absorption of glucose in the intestine, and increases insulin sensitivity by capturing and utilizing glucose

Indications and usage

Janumet is indicated as an adjunct to diet and exercise regimen to improve glycemic control in patients with type II diabetes who have not achieved adequate control during monotherapy with metformin or sitagliptin, or after unsuccessful combination treatment with two drugs. Janumet is indicated in combination with sulfonylurea derivatives (a combination of three drugs) as an addition to the diet and exercise regimen to improve glycemia control in patients with type 2 diabetes who have not achieved adequate control after treatment with two of the following three drugs: metformin, sitagliptin or derivatives sulfonylureas. Is Janumet shown in combination with PPAR- agonists? (for example, thiazolidinediones) as an adjunct to diet and exercise regimen to improve glycemia control in patients with type 2 diabetes who did not achieve adequate control after treatment with two of the following three drugs: metformin, sitagliptin or a PPAR-он agonist. Janumet is indicated for patients with type 2 diabetes mellitus (a combination of three drugs) as an addition to the diet and exercise regimen to improve glycemic control in combination with insulin.

Contraindications

- hypersensitivity to sitagliptin phosphate, metformin hydrochloride, or to any other component of the drug;
- Acute conditions that may affect kidney function: dehydration, severe infections, shock;
- acute or chronic diseases that can lead to tissue hypoxia, such as cardiac or respiratory failure, recently suffered myocardial infarction, shock;
- moderate or severe renal impairment (creatinine clearance
- abnormal liver function;
- acute alcohol intoxication, alcoholism;
- breastfeeding period;
- diabetes mellitus type I;
- acute or chronic metabolic acidosis, including diabetic ketoacidosis (with or without coma);
- radiological studies (intravascular injection of iodine-containing contrast agents).

Pregnancy and Breastfeeding

An adequately controlled study of the drug Janumet or its components in pregnant women was not conducted, therefore, there are no data on the safety of its use in pregnant women. The drug Janumet, like other oral hypoglycemic drugs, is not recommended for use during pregnancy. No experimental studies have been conducted on the combined Janumet drug to assess its effect on reproductive function. Only available data from studies of sitagliptin and metformin are given.

Dosage and administration

The dosage regimen of Janumet should be selected individually, based on current therapy, efficacy and tolerability, but not exceeding the maximum recommended daily dose of sitagliptin 100 mg. The drug Janumet usually prescribed 2 times a day with meals, with a gradual increase in dose, in order to minimize the possible side effects of the gastrointestinal tract (GIT), characteristic of metformin. The initial dose of Janumet drug depends on the current hypoglycemic therapy.

Special notes

Use in the elderly Janumet: since the main route of elimination of sitagliptin and metformin are the kidneys, and since the renal excretory function decreases with age, precautions when prescribing the drug Janumet increase in proportion to age. Elderly patients are carefully selected and regularly monitored renal function.

Drug Interactions

Sitagliptin and Metformin
Simultaneous administration of multiple doses of sitagliptin (50 mg 2 times a knock) and metformin (1000 mg 2 times a day) was not accompanied by significant changes in the pharmacokinetic parameters of sitagliptin or metformin in patients with type 2 diabetes.
There were no studies of the inter-drug effect on the pharmacokinetic parameters of the drug Janumet, however, a sufficient number of similar studies were carried out for each of the components of the drug, sitagliptin and metformin.
Sitagliptin
In studies on the interaction with other drugs, sitagliptin did not have a clinically significant effect on the pharmacokinetics of the following drugs: metformin, rosiglitazone, glibenclamide, Simvastatin, Warfarin, oral contraceptives. Based on these data, sitagliptin does not inhibit CYP isoenzymes of the cytochrome CYP3A4.2C8 or 2C9 system. In vitro data suggests that sitagliptin also does not inhibit CYP2D6.1A2.2C19 and 2B6 isoenzymes and does not induce CYP3A4. According to the population pharmacokinetic analysis of patients with type 2 diabetes mellitus, concomitant therapy did not have a clinically significant effect on sitagliptin pharmacokinetics. The study evaluated a number of drugs most frequently used by patients with type 2 diabetes, including: cholesterol-lowering drugs (statins, fibrates, ezetimibe), antiplatelet agents (clopidogrel), antihypertensive drugs (ACE inhibitors, antagonists of angitensin II receptors, beta-blockers, blockers “Slow” Calcium channels, hydrochlorothiazide, analgesics and nonsteroidal anti-inflammatory drugs (naproxen, Diclofenac, celecoxib), antidepressants (bupropion, Fluoxetine, sertraline), antihistamines ( cetirizine), proton pump inhibitors (omeprazole, lansoprazole) and drugs for the treatment of erectile dysfunction (sildenafil).
An increase in AUC (11%), as well as an average Cmax (18%) of Digoxin, was observed when used together with sitagliptin.This increase is not considered clinically significant, however, while taking digoxin, patient monitoring is recommended. An increase in AUC and C max of sitagliptin was noted by 29% and 68%, respectively, with a joint single oral dose of the drug Januvia 100 mg and cyclosporine (a powerful p-glycoprotein inhibitor) in a dose of 600 mg. These changes in the pharmacokinetic parameters of sitagliptin are not clinically significant.
Metformin
Glyburide - in the study of the inter-drug interaction of single doses of metformin and glyburide in patients with type 2 diabetes, no changes in the pharmacokinetic and pharmacodynamic parameters of metformin were observed. Changes in the AUC and Stach glyburide values ​​were highly variable. Insufficient information (single dose) and the mismatch of plasma concentration of glyburide with the observed pharmacodynamic effects call into question the clinical significance of this interaction.
Furosemide - in a study of the inter-drug interaction of single doses of metformin and Furosemide in healthy volunteers, a change in the pharmacokinetic parameters of both drugs was observed. Furosemide increased the concentration of C max of metformin in plasma and whole blood by 22%, the AUC value of metformin in whole blood by 15%, without altering the renal clearance of the drug. The values ​​of C max and AUC of furosemide, in turn, decreased by 31% and 12%, respectively, and the half-life decreased by 32%, without significant changes in the kidney clearance of furosemide.Information about the interaction between the two drugs with long-term joint use is not.
Nifedipine - in a study of the interactions between Nifedipine and metformin after a single dose of drugs by healthy volunteers revealed an increase in plasma C max and AUC of metformin by 20% and 9%, respectively, as well as an increase in the amount of metformin excreted by the kidneys. The max and half-life of metformin did not change. The basis is an increase in the absorption of metformin in the presence of nifedipine. The effect of metformin on the pharmacokinetics of nifedipine is minimal.
Cationic drugs - cationic drugs (i.e. amiloride, digoxin, morphine, procainamide, quinidine, quinine, Ranitidine, triamterene, trimethoprim or vancomycin), secreted by tubular secretion, can theoretically interact with metformin, competing for a shared renal tubular transport system. A similar competition was observed with simultaneous administration of metformin and cimetidine by healthy volunteers in single and multiple dose studies, with a 60% increase in the concentration of C max metformin in plasma and whole blood and a 40% increase in the AUC value of metformin in plasma and whole blood. In a single dose study, the half-life of metformin did not change. Metformin did not affect the pharmacokinetics of cimetidine. And although these inter-drug interactions are mainly theoretical value (with the exception of cimetidine), careful monitoring of the patient and dose adjustment of the Janumet drug and / or the above cationic drugs excreted by the proximal renal tubules are recommended, in cases of their simultaneous administration.
Some drugs have hyperglycemic potential and may interfere with established glycemic control. These include thiazide and other diuretics, glucocorticosteroids, phenothiazines, thyroid preparations, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, slow calcium channel blockers and isoniazid. When prescribing these drugs to a patient receiving Janumet, careful monitoring of the glycemic control parameters is recommended. With simultaneous use of metformin and propranolol, or metformin and Ibuprofen by healthy volunteers, no changes in the pharmacokinetic parameters of these drugs were observed.
Only a small proportion of metformin binds to plasma proteins, therefore, the interactions of metformin with drugs actively binding to plasma proteins (salicylates, sulfonamides, chloramphenicol and probenecid) are unlikely, unlike sulfonylurea derivatives, which also actively bind to plasma proteins.

Sitagliptin: in healthy volunteers, single doses up to 800 mg were generally well tolerated.When used in a clinical study of a dose of 800 mg, a slight lengthening of the Q – Tc interval was revealed, which was not considered clinically significant. There is no experience of using the drug in doses exceeding 800 mg. In studies there were no adverse reactions associated with the dose of the drug when using 600 mg / day for 10 days and 400 mg for 28 days. Sitagliptin is poorly dialyzed: according to clinical studies, only a 13.5% dose was removed during a 3–4-hour hemodialysis session. In case of clinical need, prolonged hemodialysis is prescribed. There is no data on the effectiveness of peritoneal dialysis of sitagliptin.Metformin: there have been cases of overdose of metformin, including admission in quantities exceeding 50 g. Hypoglycemia was detected in about 10% of all cases of overdose, but a causal relationship with an overdose of metformin has not been established. The development of lactic acidosis was reported in approximately 32% of all cases of overdose of metformin. Emergency hemodialysis is necessary (metformin is dialyzed at a rate of up to 170 ml / min in conditions of good hemodynamics) to accelerate the removal of excess metformin in case of suspected overdose. In the event of an overdose of Janumet, it is necessary to start standard supporting activities: removal of the remainder of the drug from the gastrointestinal tract, which has not yet been absorbed, monitoring vital signs, including ECG, hemodialysis, as well as the appointment of maintenance therapy if necessary.

Store at a temperature not higher than 25 ° С.

Janumet