Buy Janumet pills 1000 mg + 50 mg 28 pcs

Metformin, Sitagliptin

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Clinical Pharmacology

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. By inhibiting DPP-4, sitagliptin increases the concentration of two known active hormones of the incretin family: glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (HIP). Incretins are part of the internal physiological system for regulating glucose homeostasis. At normal or elevated blood glucose, 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 blood glucose concentrations, 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

The use of Janumet is shown as an addition to the diet and exercise regime in the form of monotherapy and combined treatment of type 2 diabetes in the following cases:

the appointment of starting therapy, if the diet and exercise regime do not allow to achieve adequate control over blood glucose;
lack of adequate glycemic control with monotherapy with metformin or sitagliptin, or with combined treatment with these two drugs;
the need for the appointment of a combination therapy, including sitagliptin, metformin and sulfonylurea derivatives, in the absence of adequate glycemic control from the combined treatment using only two of the listed agents;
the clinical necessity of prescribing a combination therapy, including three drugs: sitagliptin, metformin and thiazolidinediones (PPAR gamma receptor agonists, activated by a peroxisome proliferator), in the absence of adequate glycemic control from the combined treatment using only two of the listed remedies;
the need to use in combination with insulin, if insulin monotherapy does not provide adequate glycemic control.

Composition

1 tablet contains: active ingredients: Metformin hydrochloride - 1000 mg, sitagliptin phosphate monohydrate - 64.25 mg, which is equivalent to 50 mg of sitagliptin; Auxiliary components: sodium fumarate, microcrystalline cellulose, sodium lauryl sulfate, povidone;
Shell composition: Opadry II Red, 85 F 15464, polyvinyl alcohol, macrogol-3350, titanium dioxide (E171), ferric oxide red (E172), ferric oxide black (E172), talc.

Metformin, Sitagliptin is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Janumet	Merck Sharp & Dohme	USA	pills
Janumet Long	Merck Sharp & Dohme	USA	pills

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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 during 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.

Adverse reactions

On the part of the gastrointestinal tract: at the beginning of the course of treatment - anorexia, diarrhea, nausea, vomiting, flatulence, abdominal pain (reduced when taken during meals); metallic taste in the mouth (3%).

Since the cardiovascular system and blood (hematopoiesis, hemostasis): in rare cases - megaloblastic anemia (the result of a violation of the absorption of vitamin B12 and folic acid).

Metabolism: hypoglycemia; in rare cases - lactic acidosis (weakness, drowsiness, hypotension, resistant bradyarrhythmia, respiratory disorders, abdominal pain, myalgia, hypothermia).

For the skin: rash, dermatitis.

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).

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-pharmacological 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 of interactions 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 assessed a number of drugs most commonly used by patients with type 2 diabetes, including: cholesterol-lowering drugs (statins, fibrates, ezetimibe), antiplatelet agents (clopidogrel), antihypertensive drugs (ACE inhibitors, angitensin II receptor antagonists, beta-blockers, blockers "Slow" calcium channels, hydrochlorothiazide, analgesics and nonsteroidal anti-inflammatory drugs (naproxen, diclofenac, celecoxib), antidepressants (bupropion, fluoxetine, sertraline), antihistamine (ceti Rezin), 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 glyburide concentration 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, and 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 Cmax of 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 of theoretical importance (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 can interfere with the established control of glycemia. 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 that actively bind to plasma proteins (salicylates, sulfonamides, chloramphenicol and probenecid) are unlikely, unlike sulfonylurea derivatives, which also actively bind plasma proteins.

Pregnancy and Lactation

There were no adequately controlled studies of Janumet or its components in pregnant women, 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.

Special instructions

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.

Overdosage

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 prolongation of the Q – Tc interval was revealed, which was not considered clinically significant. 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 has been reported in approximately 32% of all cases of metformin overdose. Emergency hemodialysis is necessary (metformin is dialyzed at a rate of up to 170 ml / min in conditions of good hemodynamics) in order 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.