Janumet
Yanumet: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Janumet
ATX code: A10BD07
Active ingredient: metformin (metformin), sitagliptin (sitagliptin)
Manufacturer: Patheon Puerto Rico Inc. (USA)
Description and photo updated: 2018-23-11
Prices in pharmacies: from 1614 rubles.
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Janumet is a combined hypoglycemic drug for oral administration containing dipeptidyl peptidase-4-inhibitor and biguanide, intended for the treatment of patients with type 2 diabetes mellitus.
Release form and composition
Yanumet is available in the form of film-coated tablets: oval, biconvex, in three doses (metformin / sitagliptin): 500 mg / 50 mg - with a light pink film coating, engraved on one side "575", 850 mg / 50 mg - with a pink film sheath, “515” engraved on one side, 1000 mg / 50 mg - with a reddish-brown film sheath, “577” engraved on one side; core - from almost white to white (14 pcs. in blisters, in a cardboard box 1, 2, 4, 6 or 7 blisters).
1 tablet contains:
- active ingredients: metformin hydrochloride - 500 mg, 850 mg or 1000 mg, sitagliptin phosphate monohydrate - 64.25 mg, which is equivalent to 50 mg of sitagliptin;
- auxiliary components: sodium stearyl fumarate, microcrystalline cellulose, sodium lauryl sulfate, povidone;
- shell composition: tablets at a dose of 500 mg / 50 mg (light pink) - Opadrai II Pink, 85 F 94203, at a dose of 850 mg / 50 mg (pink) - Opadrai II Pink, 85 F 94182, at a dose of 1000 mg / 50 mg (reddish brown) - Opadray II Red, 85 F 15464; the shells of all tablets include: polyvinyl alcohol, macrogol-3350, titanium dioxide (E171), iron oxide red (E172), iron oxide black (E172), talc.
Pharmacological properties
Pharmacodynamics
Yanumet is a combined hypoglycemic drug, the active components of which are independent hypoglycemic agents: sitagliptin is an inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4), metformin is a representative of the biguanide class. The mechanism of action of the drug is due to the mutual complementarity of the effect of active ingredients to improve glycemic control in patients with type 2 diabetes mellitus.
Sitagliptin is a highly selective DPP-4 inhibitor intended for oral administration in the treatment of type 2 diabetes mellitus. Its pharmacological effect is mediated by the activation of incretins, which are part of the internal physiological system that regulates glucose homeostasis. As a result of DPP-4 inhibition, sitagliptin increases the concentration of active hormones of the incretin family, such as glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1). GLP-1 and GIP at normal or elevated blood glucose levels potentiate the beta cells of the pancreas to increase the synthesis and secretion of insulin. GLP-1 helps to reduce the synthesis of glucose in the liver, suppressing the secretion of glucagon by alpha cells of the pancreas. Therapeutic concentrations of sitagliptin do not inhibit the activity of the related enzymes DPP-8 or DPP-9. Its pharmacological action and chemical structure differ from analogs of GLP-1, insulin, meglitinides, sulfonylurea derivatives, peroxisome proliferator activated gamma receptor agonists (PPAR gamma), biguanides, alpha-glucosidase inhibitors, amylin analogs.
Metformin - increases glucose tolerance in type 2 diabetes. Its pharmacological mechanism of action to reduce the basal and postprandial blood glucose concentration differs from the mechanisms of action of other classes of oral hypoglycemic agents. It is due to the ability of metformin to reduce the synthesis of glucose in the liver, absorption of glucose in the intestine, which leads to an increase in peripheral capture and utilization of glucose, to an increase in insulin sensitivity. Reception of metformin does not cause changes in insulin secretion, while its concentration on an empty stomach and the value of the daily plasma concentration of insulin may decrease.
Unlike sulfonylurea derivatives, metformin and sitagliptin do not cause hypoglycemia.
The combined administration of sitagliptin and metformin provides a summation of the therapeutic effect, which is accompanied by an increase in the concentration of active GLP-1.
With arterial hypertension, the simultaneous use of diuretics, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor antagonists, slow calcium channel blockers or beta-blockers with sitagliptin does not cause a significant hypotensive effect.
Pharmacokinetics
The use of Janumet in doses of 500 mg / 50 mg, 850 mg / 50 mg and 1000 mg / 50 mg is bioequivalent to the separate administration of the corresponding doses of metformin and sitagliptin.
Absolute bioavailability: sitagliptin - approximately 87%, metformin (when taken in a dose of 500 mg on an empty stomach) - 50-60%. The pharmacokinetics of sitagliptin when taken simultaneously with fatty foods does not change. The rate and amount of absorbed metformin when taken simultaneously with food decreases. The clinical significance of an increase in the time to reach and a decrease in the value of the maximum plasma concentration (C max) of metformin has not been established.
Plasma protein binding: sitagliptin - 38%, metformin - to a very small extent.
Part of metformin is temporarily distributed in erythrocytes, the plasma concentration of the steady state against the background of the recommended dosage regimen is reached after 24–48 hours and is usually less than 0.001 mg / ml.
In the limited metabolism of sitagliptin, isoenzymes of the cytochrome P 450 system CYP3A4 and CYP2C8 are involved. The metabolic transformation of sitagliptin is minimal; about 79% of the dose taken is excreted unchanged through the kidneys.
Metformin is excreted through the kidneys in unchanged form almost completely (90%) within 24 hours.
The half-life (T 1/2) of sitagliptin is approximately 12.4 hours, renal clearance is approximately 350 ml / min.
Renal excretion of sitagliptin is predominantly carried out by active tubular secretion.
T 1/2 of metformin from plasma is about 6.2 hours, from blood - 17.6 hours. Its main route of excretion through the kidneys causes a 3.5-fold excess of renal clearance over creatinine clearance (CC).
Cumulation of metformin during the use of therapeutic doses does not occur.
In patients with varying degrees of impaired renal function, the half-life of Yanumet is lengthened, and the total concentration (AUC) of sitagliptin in the blood plasma increases. You cannot use the drug in case of impaired renal function.
With a moderate degree (7-9 points on the Child - Pugh scale) hepatic failure, a single dose of sitagliptin at a dose of 100 mg leads to an increase in its average C max by 13%, AUC - by 21%. There are no clinical data on the experience of using the drug in severe (more than 9 points on the Child - Pugh scale) liver failure.
Gender, race or weight of the patient does not affect the pharmacokinetic parameters of the active ingredients.
Elderly patients have an increase in T 1/2 and an increase in C max. These changes are associated with an age-related decrease in renal excretory function. Over the age of 80, treatment with Janumet is possible only in patients with normal renal function and CC.
Studies on the effectiveness and safety of taking the drug by children have not been conducted.
Indications for use
The use of Yanumet is indicated as an adjunct to diet and exercise regimen in the form of monotherapy and combined treatment of type 2 diabetes mellitus in the following cases:
- the appointment of starting therapy if adherence to a diet and exercise regimen does not allow achieving adequate glycemic control;
- lack of adequate glycemic control with monotherapy with metformin or sitagliptin, or with combined treatment with these two drugs;
- the need to prescribe combination therapy, including sitagliptin, metformin and sulfonylurea derivatives, in the absence of adequate glycemic control from combined treatment using only two of the listed agents;
- the clinical necessity of prescribing combination therapy, including three drugs: sitagliptin, metformin and thiazolidinediones (PPAR gamma receptor agonists activated by the peroxisome proliferator), in the absence of adequate glycemic control from combined treatment using only two of the listed agents;
- the need for use in combination with insulin if insulin monotherapy does not provide adequate glycemic control.
Contraindications
- type 1 diabetes mellitus;
- diseases or impaired renal function with CC less than 60 ml / min or with a serum creatinine concentration in men of 1.5 mg / dL and above, in women - 1.4 mg / dL and above, including disorders resulting from acute myocardial infarction, shock (cardiovascular collapse), septicemia;
- severe infectious diseases;
- dehydration (diarrhea, vomiting);
- fever;
- states of hypoxia: renal infections, shock, sepsis, bronchopulmonary diseases;
- chronic or acute metabolic acidosis, including diabetic ketoacidosis;
- heart failure, acute myocardial infarction, respiratory failure, other acute and chronic diseases with clinically pronounced manifestations that can contribute to the development of tissue hypoxia;
- severe injuries, extensive surgical operations;
- impaired liver function, liver failure;
- lactic acidosis (including history);
- taking pills within 48 hours before and 48 hours after X-ray and radioisotope studies with the introduction of an iodine-containing contrast agent;
- adherence to a hypocaloric diet with an energy value of less than 1000 kcal in 24 hours;
- acute alcohol poisoning, chronic alcoholism;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- established hypersensitivity to the components of the drug.
According to the instructions, Janumet should be used with caution in elderly patients.
Instructions for the use of Yanumet: method and dosage
The 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.
Yanumet's use involves taking sitagliptin at a dose of 50 mg and metformin at a dose of 500 mg, 850 mg or 1000 mg 2 times a day. The maximum daily dose of sitagliptin is 100 mg (50 mg 2 times a day), the dose of the drug is adjusted by changing only the dose of metformin.
Recommended initial dosage of Yanumet as an adjunct to diet and exercise regimen for patients with type 2 diabetes:
- lack of adequate glycemic control when following a diet and exercise regimen: tablets at a dose of 500 mg / 50 mg (metformin / sitagliptin) 2 times a day. If necessary, a single dose can be gradually increased to 1000 mg / 50 mg;
- lack of adequate control during monotherapy with metformin: the dose should be prescribed in the amount of the current dose of metformin (500 mg, 850 mg or 1000 mg per 50 mg of sitagliptin), the frequency of administration is 2 times a day;
- lack of adequate control with sitagliptin monotherapy: 500 mg / 50 mg 2 times a day. Further, a single dose of metformin can be increased in accordance with clinical feasibility up to 1000 mg. Patients with renal insufficiency taking sitagliptin dosage below 100 mg per day during monotherapy are contraindicated in Yanumet treatment;
- transition from combination therapy with sitagliptin and metformin: the dose may correspond to the previously taken doses of each of the drugs;
- switching from taking two of the following hypoglycemic agents - sitagliptin, metformin, sulfonylurea derivatives: the dose of metformin is determined based on the level of glycemic control, also, if the patient has taken metformin before, his current dose is taken into account. It is recommended to increase the dose of metformin gradually, this will minimize its side effects from the gastrointestinal tract. If the 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 dose of metformin should correspond to the daily dose of the previous therapy. If necessary, it can be increased by gradually titrating the dose of the drug;
- transition from taking two of the following hypoglycemic agents - sitagliptin, metformin, insulin: the dose should correspond to the previously taken daily dose of metformin. To prevent hypoglycemia, it may be necessary to lower the previously used insulin dose. Then the dose of metformin can be gradually increased.
There are no data on assessing the safety and effectiveness of switching to Yanumet from treatment with other hypoglycemic drugs. Any changes in the treatment regimen for type 2 diabetes mellitus should be carried out with caution, under close monitoring of the relevant parameters, taking into account possible changes in glycemic control.
Side effects
- from the gastrointestinal tract: metallic taste in the mouth; at the beginning of use - nausea, vomiting, diarrhea, flatulence, anorexia, abdominal pain;
- on the part of the blood and the cardiovascular system: in isolated cases - megaloblastic anemia against the background of impaired absorption of folic acid and vitamin B 12;
- from the side of metabolism: hypoglycemia; in rare cases - lactic acidosis (respiratory disorders, hypothermia, weakness, drowsiness, abdominal pain, resistant bradyarrhythmia, hypotension, myalgia);
- dermatological reactions: rash, dermatitis.
Additional side effects identified during post-registration observations that may occur against the background of the use of Yanumet:
- from the immune system: hypersensitivity reactions, including anaphylaxis, angioedema;
- dermatological reactions: pruritus, urticaria, Stevens-Johnson syndrome and other exfoliative skin diseases, cutaneous vasculitis;
- from the digestive system: constipation, acute pancreatitis (including necrotic and hemorrhagic forms, including fatal ones);
- from the urinary system: deterioration of renal function, severe acute renal failure;
- from the respiratory system: nasopharyngitis, upper respiratory tract infections;
- from the nervous system: headache;
- from the musculoskeletal system: pain in the limbs, arthralgia, myalgia, back pain.
Overdose
Overdose symptoms have not been established.
Treatment: if you accidentally take a high dose of Yanumet, you must immediately flush the stomach or induce artificial vomiting to remove the drug that has not yet been absorbed. The patient should be provided with control of vital body functions, electrocardiography, the appointment of symptomatic therapy, in case of clinical need - prolonged hemodialysis. The effectiveness of peritoneal dialysis has not been established.
special instructions
Due to the risk of developing acute pancreatitis when prescribing Yanumet, patients should be informed that severe persistent abdominal pain is a symptom characteristic of acute pancreatitis. If you suspect pancreatitis, the drug should be discontinued.
Given that renal excretion is the main route of elimination of metformin and sitagliptin, the risk of developing lactic acidosis is in direct proportion to the degree of renal dysfunction. In this regard, the appointment of Yanumet can only be made to patients with a normal concentration of creatinine in the serum or below the upper age limit of the norm. For the treatment of elderly patients, the minimum effective dose of the drug should be used to achieve adequate glycemic control. The most likely age-related decline in kidney function in patients over 80 years old, so they need to regularly monitor kidney function.
All patients taking Yanumet should undergo an annual examination to confirm normal renal function; patients at risk are prescribed appropriate tests more often.
To reduce the risk of developing insulin-induced or sulfonyl-induced hypoglycemia during triple combination therapy, the dose of insulin or a sulfonylurea derivative must be reduced.
The pill should be discontinued for major surgery requiring limited fluid and food intake.
With a temporary loss of glycemic control, including hyperthermia, trauma, infection or surgery, in patients with previously stable glycemic control, it is allowed to replace Yanumet with insulin for the period of stabilization of the general condition.
The use of metformin can cause the development of lactic acidosis. Upon confirmation of lactic acidosis, the patient needs immediate hospitalization and maintenance therapy, including the use of hemodialysis to remove accumulated metformin and accelerate the correction of acidosis. The drug should be discontinued.
During the period of treatment with Janumet, drinking alcohol in large doses or is often contraindicated, since alcohol potentiates the metabolism of lactic acid (lactate).
The risk of developing hypoglycemia increases in old age, in debilitated patients, with exhaustion, alcohol abuse, adrenal or pituitary insufficiency, and taking beta-blockers.
During the period of taking Yanumet, patients should agree with the attending physician on the use of any concomitant therapy drugs. This will avoid possible negative effects of these drugs on kidney function.
After carrying out radiological studies with intravascular administration of iodine-containing contrast agents, such as intravenous urography, cholangiography, angiography, it is possible to resume taking the drug after 48 hours only after receiving laboratory results confirming the normal state of renal function.
Reception of Yanumet should be stopped immediately when diagnosing such conditions accompanied by the development of hypoxemia as acute heart failure, acute myocardial infarction, shock of any etiology. The development of hypoxia can cause the development of prerenal azotemia and lactic acidosis.
Reception of Yanumet is recommended to be accompanied by control of hematological blood parameters, which is carried out at least 1 time per year. In patients predisposed to the development of vitamin B 12 deficiency, the plasma concentration of vitamin B 12 should be monitored every 2 years.
If, against the background of drug treatment in patients with adequately controlled type 2 diabetes mellitus, abnormalities in laboratory parameters or clinical conditions that cannot be clearly identified, first of all, laboratory studies should be carried out aimed at excluding ketoacidosis or lactic acidosis. If the development of acidosis is confirmed, taking the tablets should be canceled and appropriate measures should be taken to correct the acidosis.
Influence on the ability to drive vehicles and complex mechanisms
Taking sitagliptin can cause drowsiness and dizziness, therefore, during the period of application of Yanumet, care should be taken when working with complex mechanisms and driving vehicles.
Application during pregnancy and lactation
The use of Yanumet is contraindicated during gestation and during breastfeeding.
Pediatric use
The appointment of a combined hypoglycemic drug for the treatment of children under the age of 18 is contraindicated. There are no data on the safety of using Yanumet in patients under 18 years of age.
With impaired renal function
The appointment of Yanumet is contraindicated in patients with type 2 diabetes mellitus with impaired renal function (CC less than 60 ml / min), kidney disease and other conditions that cause the risk of developing impaired renal function.
For violations of liver function
The appointment of the drug is contraindicated in patients with type 2 diabetes mellitus with impaired liver function, hepatic insufficiency.
Use in the elderly
Janumet should be prescribed with caution to elderly patients due to possible age-related renal impairment.
Drug interactions
Simultaneous administration of multiple doses of sitagliptin (50 mg twice a day) and metformin (1000 mg twice a day) does not cause clinically significant changes in the pharmacokinetic parameters of drugs in patients with type 2 diabetes mellitus.
Studies on the interaction of Yanumet with other drugs have not been conducted. Therefore, when prescribing concomitant therapy, one should be guided by the results of similar studies conducted separately for sitagliptin and metformin.
With the simultaneous use of sitagliptin:
- rosiglitazone, glibenclamide, simvastatin, warfarin, oral contraceptives: there is no clinically significant change in their pharmacokinetics, sitagliptin does not inhibit cytochrome P 450 isoenzymes CYP3A4, CYP2C8, CYP2C9, does not suppress CYPA6 isoenzymes, CYP2C6, CYP2C9, does not suppress CYP2C6 isoenzymes, CYP2C6, CYP2C6 does not inhibit CYP2C6, CYP2C6 isoenzymes
- fibrates, statins, ezetimibe (cholesterol-lowering drugs), clopidogrel, antihypertensive drugs, including angiotensin II receptor antagonists, angiotensin-converting enzyme inhibitors, beta-blockers, hydrochlorothiazide, slow calcium channel blockers, nonsteroidal anti-inflammatory drugs, nonsteroidal anti-inflammatory drugs (anti-inflammatory drugs) (fluoxetine, sertraline, bupropion), proton pump inhibitors (omeprazole, lansoprazole), antihistamines (cetirizine), sildenafil: do not affect sitagliptin pharmacokinetics;
- digoxin, cyclosporin: clinically significantly increase their AUC and C max values.
With the simultaneous use of metformin:
- glyburide: does not cause clinically significant interaction;
- furosemide: changes its pharmacokinetic parameters, contributes to an increase in the C max of metformin by 22%, AUC in whole blood - by 15%, the renal clearance of drugs does not change significantly;
- nifedipine: leads to an increase in absorption, plasma concentration and the amount of metformin excreted by the kidneys;
- cationic agents - morphine, amiloride, digoxin, procainamide, quinine, quinidine, trimethoprim, vancomycin, ranitidine, triamterene: can compete for the use of the renal tubular transport system;
- phenothiazines, diuretics, glucocorticosteroids, thyroid medications, oral contraceptives, estrogens, nicotinic acid, phenytoin, sympathomimetics, isoniazid, slow calcium channel blockers: with hyperglycemic potential, they can disrupt glycemic control it is necessary to carefully monitor the parameters of glycemic control;
- drugs that actively bind to blood plasma proteins, such as salicylates, sulfonamides, chloramphenicol, probenecid: do not interact with metformin.
Analogs
The analogues of Yanumet are: Yanumet Long, Velmetia, Amaryl M, Glibomet, Glukovans, Gluconorm, Avandamet, Galvus Met, Douglimax, Tripride.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
Shelf life of Janumet 1000 + 50 mg and 850 + 50 mg tablets is 2 years, 500 + 50 mg tablets - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Yanumet
Reviews about Yanumet are positive. Patients and doctors point to the high efficacy of the drug and characterize it as an excellent addition to diet and exercise in the treatment of type 2 diabetes. Monotherapy and combination therapy, including Yanumet, provide stable glycemic control and the absence of clinically significant side effects.
Doctors advise to be attentive to the list of contraindications for taking Yanumet and strictly follow all the doctor's recommendations.
All consider the disadvantages of the rather high price of the drug, given the need for its constant intake.
The price of Yanumet in pharmacies
The price for Yanumet 1000 + 50 mg - from 3023 rubles for a package containing 56 tablets, at a dose of 850 + 50 mg - from 2860 rubles, at a dose of 500 + 50 mg - from 2827 rubles.
Yanumet: prices in online pharmacies
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Drug name Price Pharmacy |
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Janumet 1000 mg + 50 mg film-coated tablets 28 pcs. 1614 RUB Buy |
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Janumet Long 1000mg + 100mg film-coated tablets 28 pcs. 1832 RUB Buy |
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Yanumet Long 1000 mg + 50 mg film-coated prolonged-release tablets 56 pcs. 1832 RUB Buy |
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Janumet 850 mg + 50 mg film-coated tablets 56 pcs. 2000 RUB Buy |
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Janumet Long tablets p.p. prolonged release 1000mg + 50mg 56 pcs. 2371 RUB Buy |
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Janumet 500 mg + 50 mg film-coated tablets 56 pcs. 2622 RUB Buy |
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Janumet tablets p.o. 500mg + 50mg 56 pcs. RUB 2734 Buy |
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Janumet tablets p.p. 1000mg + 50mg 56 pcs. 2853 RUB Buy |
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Janumet tablets p.p. 850mg + 50mg 56 pcs. RUB 2910 Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!