Janumet, 1000 mg+50 mg 28 pcs
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The drug Janumet is a combination of two hypoglycemic drugs with complementary (complementary) mechanism of action, designed to improve glycemic control in patients with type 2 diabetes: sitagliptin, an inhibitor of the dipeptidyl peptidase-4 (DPP-4) enzyme, and metformin, a representative of the biguanide class.
Sitagliptin is an orally active, highly selective DPP-4 inhibitor for the treatment of type 2 diabetes. The pharmacological effects of the class of DPP-4 inhibitor drugs are mediated by the activation of incretins.
Inhibiting DPP-4, sitagliptin increases the concentration of two known active hormones of the incretin family: glucagon-like peptide 1 (GFP-1) and glucose-dependent insulinotropic polypeptide (GIP). Incretins are part of the internal physiological system of glucose homeostasis regulation. At normal or elevated blood glucose concentrations, GFP-1 and GIP contribute to increased insulin synthesis and secretion by pancreatic beta cells. GFP-1 also inhibits glucagon secretion by pancreatic alpha cells, thus reducing glucose synthesis in the liver. This mechanism of action differs from the mechanism of action of sulfonylurea derivatives, which stimulate insulin release even at low blood glucose concentrations, which is fraught with development of sulfonyl-induced hypoglycemia not only in patients with type 2 diabetes but also in healthy individuals.
As a highly selective and effective inhibitor of DPP-4 enzyme, sitagliptin in therapeutic concentrations does not inhibit activity of related enzymes DPP-8 or DPP-9. Sitagliptin differs in chemical structure and pharmacological action from PPP-1 analogues, insulin, sulfonylurea or meglitinide derivatives, biguanides, peroxisome proliferator-activated receptor gamma agonists (PPARy), alpha-glycosidase inhibitors and amylin analogues.
Metformin is a hypoglycemic drug that increases glucose tolerance in patients with type 2 diabetes by reducing basal and postprandial blood glucose concentrations. Its pharmacological mechanisms of action are different from the mechanisms of action of oral hypoglycemic drugs of other classes. Metformin reduces glucose synthesis in the liver, reduces glucose absorption in the intestine and increases insulin sensitivity through glucose capture and utilization.
Indications
Type 2 diabetesThe use of Janumet is indicated as an adjunct to diet and exercise regimen as monotherapy and combined treatment of type 2 diabetes in the following cases:
- Appointment of starter therapy if adherence to diet and exercise regimen does not achieve adequate glycemic control;
- Need to prescribe combination therapy including metformin or sitagliptin.The need to prescribe combination therapy including sitagliptin, metformin, and sulfonylurea derivatives in the absence of adequate glycemic control from combination treatment with only two of these agents;
- the clinical need to prescribe combination therapy including three drugs: sitagliptin, metformin, and thiazolidinediones (PPAR gamma receptor agonists activated by peroxisome proliferator-activated receptor), in the absence of adequate glycemic control from combination treatment with only two of the listed agents;
- the need to use in combination with insulin if insulin monotherapy does not provide adequate glycemic control.
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Active ingredient
Metformin, Sitagliptin
Composition
One tablet contains:
Active ingredients:
Metformin hydrochloride – 1000 mg;
Sitagliptin phosphate monohydrate – 64.25 mg (equivalent to the content of 50 mg sitagliptin).
Auxiliary components:
Sodium stearyl fumarate;
Microcrystalline cellulose;
Sodium lauryl sulfate;
Povidone.
Composition of the shell:
Opadray II Red, 85 F 15464;
Polyvinyl alcohol;
Macrogol-3350;
Titanium dioxide (E171);
Red iron oxide (E172);
Black iron oxide (E172);
Talc.
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How to take, the dosage
Tablets are taken orally, swallowed whole, with meals. The initial dose is prescribed taking into account the current individual hypoglycemic therapy, tolerance and therapeutic effect. The use of Janumet involves taking sitagliptin at a dose of 50 mg and metformin at a dose of 1000 mg twice daily. The maximum daily dose of sitagliptin is 100 mg (50 mg twice daily), the drug dose is adjusted by changing only the dose of metformin. The recommended initial dosage of Janumet as an adjunct to the diet and exercise regimen for patients with type 2 diabetes mellitus:
- lack of adequate glycemic control with diet and exercise regimen: tablets at a dose of 500 mg/50 mg (metformin/sitagliptin) twice daily. If necessary, the single dose may be gradually increased to 1000 mg/50 mg;
- lack of adequate control with metformin monotherapy: the dose should be administered at the current dose of metformin (500 mg, 850 mg, or 1000 mg per 50 mg of sitagliptin), the frequency of administration is 2 times daily;
- lack of adequate control with sitagliptin monotherapy: 500 mg/50 mg 2 times daily. Thereafter, the single dose of metformin may be increased according to clinical appropriateness up to 1000 mg. Patients with renal impairment taking a sitagliptin dose below 100 mg daily on monotherapy are contraindicated in treatment with Janumet;
- transition from sitagliptin and metformin combination therapy: the dose may be consistent with previous doses of each drug;
- transition from taking two of the following hypoglycemic agents – sitagliptin, metformin, sulfonylurea derivatives:the dose of metformin is determined based on glycemic control levels, also if the patient has previously taken metformin, the current dose is considered. It is recommended to increase the dose of metformin gradually, this will minimize its gastrointestinal side effects. If previous combination therapy included a sulfonylurea derivative, its dose should be reduced;
- switching from taking two of the following hypoglycemic agents – sitagliptin, metformin, thiazolidinediones (PPAR gamma receptor agonists): The metformin dose should match the daily dose of previous therapy. If necessary, it may be increased by gradual titration of the drug dose;
- transition from taking two of the following hypoglycemic agents – sitagliptin, metformin, insulin:the dose should match the previously taken daily dose of metformin. To prevent hypoglycemia, it may be necessary to reduce the previously used dose of insulin. The metformin dose may then be gradually increased.
There are no data to evaluate the safety and efficacy of switching to Janumet from treatment with other hypoglycemic drugs. Any changes in the treatment regimen of type 2 diabetes mellitus should be performed with caution, under careful control of the relevant parameters, taking into account possible changes in glycemic control.
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Interaction
Simultaneous administration of multiple doses of sitagliptin (50 mg twice daily) and metformin (1000 mg twice daily) does not cause clinically significant changes in pharmacokinetic parameters of drugs in patients with type 2 diabetes.
Studies on the interaction of Janumet with other drugs have not been conducted. Therefore, when prescribing concomitant therapy, the results of such studies conducted separately for sitagliptin and metformin should be followed.
When concomitant use of sitagliptin:
- rosiglitazone, glibenclamide, simvastatin, warfarin, oral contraceptives: There is no clinically significant change in their pharmacokinetics; sitagliptin does not inhibit cytochrome P450 system isoenzymes CYP3A4, CYP2C8, CYP2C9, does not inhibit CYP1A2, CYP2D6, CYP2B6, CYP2C19 isoenzymes, does not induce CYP3A4;
- fibrates, statins, ezetimibe (hypocholesterolemic agents), clopidogrel, hypotensive agents, including angiotensin II receptor antagonists, angiotensin-converting enzyme inhibitors, beta-adrenoblockers, hydrochlorothiazide, slow calcium channel blockers, Non-steroidal anti-inflammatory drugs (diclofenac, naproxen, celecoxib), analgesics, antidepressants (fluoxetine, sertraline, bupropion), proton pump inhibitors (omeprazole, lansoprazole), antihistamines (cetirizine), sildenafil: Do not affect the pharmacokinetics of sitagliptin;
- digoxin, cyclosporine:clinically significantly increase their AUC and Cmax values.
When metformin is used concomitantly:
- gliburide: causes no clinically significant interaction;
- furosemide: alters its pharmacokinetic parameters, contributing to a 22% increase in metformin Cmax, 15% increase in AUC in whole blood, with no significant change in renal clearance of the drugs;
- nifedipine: leads to increased absorption, plasma concentration, and amount of metformin excreted by the kidneys;
- cationic agents-morphine, amiloride, digoxin, procainamide, quinine, quinidine, trimethoprim, vancomycin, ranitidine, triamterene may compete for use of the renal tubular transport system;
- phenothiazines, diuretics, glucocorticosteroids, thyroid drugs, oral contraceptives, estrogens, nicotinic acid, phenytoin, sympathomimetics, isoniazid, slow calcium channel blockers: having hyperglycemic potential may impair glycemic control; glycemic control parameters should be closely monitored;
- drugs that actively bind to plasma proteins, such as salicylates, sulfonamides, chloramphenicol, probenecid: do not interact with metformin.
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Special Instructions
Because of the risk of acute pancreatitis, when prescribing Janumet, patients should be informed that severe persistent abdominal pain is a characteristic symptom of acute pancreatitis. If pancreatitis is suspected, the drug should be discontinued. Given that renal excretion is the main route of metformin and sitagliptin excretion, the risk of lactoacidosis is directly related to the degree of renal dysfunction.
Contraindications
- Diabetes mellitus type 1;
- .Renal disease or dysfunction with a CKC less than 60 ml/min or with a serum creatinine concentration of 1.5 mg/dL or higher in men and 1.4 mg/dL or higher in women, including disorders resulting from acute myocardial infarction, shock (cardiovascular collapse), septicemia;
- Severe infectious diseases;
- Dehydration (diarrhea, vomiting);
- Fever;
- Hypoxic conditions: Renal infections, shock, sepsis, bronchopulmonary disease; chronic or acute metabolic acidosis, including diabetic ketoacidosis;
- Severe injuries, major surgical procedures; liver dysfunction, liver failure;
- Lactoacidosis (including history);
- Taking pills within 48 hours before and 48 hours after radiological and radioisotopic studies with iodine-containing contrast agent;
- Having a hypocaloric diet with an energy value less than 1000 kcal per 24 hours;
- Acute alcohol poisoning, chronic alcoholism;
- Pregnancy;
- Breastfeeding;
- Age under 18 years; established hypersensitivity to components of the drug.
According to the instructions, Janumet should be prescribed with caution in elderly patients.
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Side effects
- withgastrointestinal tract:metal taste in the mouth; nausea, vomiting, diarrhea, flatulence, anorexia, abdominal pain;
- blood and cardiovascular system: in single cases – megaloblastic anemia against the background of impaired absorption of folic acid and vitamin B12;
- with regard to metabolism: hypoglycemia; in rare cases – lactoacidosis (respiratory disorders, hypothermia, weakness, drowsiness, abdominal pain, resistant bradyarrhythmia, hypotension, myalgia);
- dermatological reactions: rash, dermatitis.
Additional adverse events established during post-registration observations that may occur against the background of Janumet administration:
- from the immune system:hypersensitivity reactions, including anaphylaxis, angioedema;
- dermatological reactions: skin itching, urticaria, Stevens-Johnson syndrome and other exfoliative skin disorders, cutaneous vasculitis;
- digestive system disorders: constipation, acute pancreatitis (including necrotic and hemorrhagic forms, including lethal);
- reversible system disorders: deterioration of renal function, severe acute renal failure;
- with regard to the respiratory system:nasopharyngitis, upper respiratory tract infections;
- nervous system: headache;
- musculoskeletal system: limb pain, arthralgia, myalgia, back pain.
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Overdose
Symptoms of overdose have not been established.
Pregnancy use
Janumet is contraindicated during pregnancy and while breastfeeding.
Similarities
Velmetia
Weight | 0.064 kg |
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Shelf life | 3 years. |
Conditions of storage | Store at a temperature of up to 25 °C. |
Manufacturer | Akrihin HFC JSC, Russia |
Medication form | pills |
Brand | Akrihin HFC JSC |
Other forms…
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