Buy Januvia coated tablets 100mg N28

Januvia coated pills 100mg N28

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1 tablet contains: Sitagliptin (in the form of phosphate monohydrate) 100 mg Supplementary substances: microcrystalline cellulose, unground ground calcium phosphate, croscarmelose sodium, magnesium stearate, sodium stearyl fumarate. ) 3350, talc, iron oxide yellow, iron oxide red.

Pharmacological effect

Oral hypoglycemic drug, a highly selective inhibitor of dipeptidyl peptidase 4 (DPP-4) .Sitagliptin differs in chemical structure and pharmacological activity of the analogs of glucagon-like peptide-1 (GLP-1), insulin, sulfonylureas, biguanides, γ-receptor agonist, a peroxisome proliferator-activated (PPAR-γ), alpha-glycosidase inhibitors, amylin analogues. Inhibiting DPP-4, sitagliptin increases the concentration of 2 known hormones of the incretin family: GLP-1 and the glucose-dependent insulinotropic peptide (HIP). Hormones of the family of incretins are secreted in the intestine during the day, their level rises in response to food intake. Incretins are part of the internal physiological system for regulating glucose homeostasis. At normal or elevated blood glucose levels, hormones of the incretin family contribute to an increase in insulin synthesis, as well as its secretion by pancreatic β-cells due to signaling intracellular mechanisms associated with cyclic AMP. HGP-1 also contributes to the suppression of increased glucagon secretion by the pancreatic α-cells. A decrease in glucagon concentration on the background of an increase in insulin levels contributes to a decrease in glucose production by the liver, which ultimately leads to a decrease in glycemia. At low blood glucose concentrations, the listed effects of incretins on insulin release and a decrease in glucagon secretion are not observed. GLP-1 and HIP do not affect the release of glucagon in response to hypoglycemia. Under physiological conditions, the activity of incretins is limited by the enzyme DPP-4, which quickly hydrolyzes the incretins to form inactive products. Sitagliptin prevents the hydrolysis of the incretins by the enzyme DPP-4, thereby increasing plasma concentrations of the active forms of GPP-1 and HIP.By increasing the level of incretins, sitagliptin increases glucose-dependent insulin release and helps to reduce glucagon secretion. In patients with type 2 diabetes mellitus with hyperglycemia, these changes in insulin and glucagon secretion lead to a decrease in glycated hemoglobin НbА1С and a decrease in plasma glucose concentration, determined on an empty stomach and after a stress test. the activity of the enzyme DPP-4 within 24 hours, which leads to an increase in the level of circulating incretin GLP-1 and HIP by 2-3 times, an increase in plasma concentrations of insulin and C-peptide, a decrease in the end tration of glucagon in plasma, decrease in fasting glucose as well as a decrease in blood glucose after glucose load or a load of food.


The pharmacokinetics of sitagliptin was studied in healthy individuals and patients with type 2 diabetes mellitus. Absorption After ingestion of the drug at a dose of 100 mg in healthy individuals, rapid absorption of sitagliptin is observed with reaching Cmax after 1-4 hours. AUC increases in proportion to the dose and in healthy subjects 8.52 μmol h when administered orally at a dose of 100 mg, Cmax was 950 nmol. The absolute bioavailability of sitagliptin is approximately 87%. Intra-and inter-individual AUC of sitagliptin is insignificant. Simultaneous intake of fatty foods does not affect the pharmacokinetics of sitagliptin, so the drug Januvia can be prescribed regardless of food intake. after taking the first dose. After a single dose of the drug in a dose of 100 mg, the average Vd of sitagliptin in healthy volunteers was approximately 198 liters. The binding of sitagliptin to plasma proteins is 38%. Metabolism Only an insignificant part of the drug ingested is metabolized. After the introduction of 14C-labeled sitagliptin inside about 16% of the radioactive drug was excreted in the form of its metabolites. Traces of 6 sitagliptin metabolites, probably not having DPP-4 inhibitory activity, were found.In vitro studies have revealed that CYP3A4 with CYP2C8 is the primary enzyme involved in limited metabolism of sitagliptin. Exemption Approximately 79% of sitagliptin is excreted unchanged in the urine. Within 1 week after the drug was taken by healthy volunteers, 14C-labeled sitagliptin was eliminated: s urine - 87% and feces -13% .T1 / 2 of sitagliptin when taken orally at a dose of 100 mg is approximately 12.4 hours. Renal clearance is approximately 350 ml / min. Excretion of sitagliptin is carried out primarily by excretion by the mechanism of active tubular secretion. Sitagliptin is a substrate for a transporter of organic human anions of the third type (hOAT-3), which may be involved in the process of elimination of sitagliptin by the kidneys. Clinically, hOAT-3 involvement in the transport of sitagliptin has not been studied. Sitagliptin is also a substrate of p-glycoprotein, which can also participate in the process of renal elimination of sitagliptin. However, cyclosporine, an inhibitor of p-glycoprotein, did not reduce the renal clearance of sitagliptin. Pharmacokinetics in special clinical situations Patients with renal insufficiency An open-label study of the drug Januvia at a dose of 50 mg / day was conducted to study its pharmacokinetics in patients with varying degrees of chronic renal insufficiency. The patients included in the study were divided into groups of mild renal failure (CC 50-80 ml / min), moderate (CC 30-50 ml / min) and severe renal failure (CC less than 30 ml / min), as well as patients with end-stage pathology of the kidneys requiring dialysis. In patients with mild renal insufficiency, there was no clinically significant change in the concentration of sitagliptin in the plasma compared to the control group of healthy volunteers. The increase in AUC of sitagliptin is approximately 2 times higher than in the control group chalos patients with moderate renal insufficiency, about 4-fold increase in AUC was observed in patients with severe renal insufficiency, and also in patients with end-stage renal disease when compared to the control group. Sitagliptin was weakly removed from the systemic circulation by hemodialysis: only 13.5% of the dose was removed from the body during the 3-4 hour dialysis session. Thus,To achieve a therapeutic plasma concentration of the drug (similar to that in patients with normal renal function) in patients with moderate to severe renal insufficiency, dose adjustment is required. Patients with hepatic insufficiency In patients with moderate hepatic insufficiency (7–9 points on the Child- I drink) average AUC and Cmax of a sitagliptin at a single dose of 100 mg increase approximately by 21% and 13% respectively. Thus, the dose adjustment of the drug in mild and moderate liver failure is not required. There is no clinical data on the use of sitagliptin in patients with severe liver failure (more than 9 points on the Child-Pugh scale). However, due to the fact that the drug is primarily excreted by the kidneys, one should not expect a significant change in the pharmacokinetics of sitagliptin in patients with severe hepatic impairment. Elderly patients. The age of patients did not have a clinically significant effect on the pharmacokinetic parameters of sitagliptin. Compared with young patients in elderly patients (65-80 years), the concentration of sitagliptin is approximately 19% higher. Correction of the dose of the drug, depending on age is not required.


- monotherapy: as a supplement to diet and exercise to improve glycemia control in type 2 diabetes; - combination therapy: type 2 diabetes to improve glycemic control in combination with metformin or PPAR-γ agonists (for example, thiazolidinedione), when diet and exercise in combination with the monotherapy with the above remedies do not lead to adequate glycemic control.


- diabetes mellitus type 1; - diabetic ketoacidosis; - pregnancy; - lactation period (breastfeeding); - hypersensitivity to the drug components. It is not recommended to prescribe Januvia to children and adolescents under 18 years of age (data on the use of the drug in pediatric practice are not there is).

Precautionary measures

Use with caution in patients with renal insufficiency. In case of moderate and severe renal failure, as well as in patients with end-stage renal failure requiring hemodialysis, correction of the dosing regimen is required.

Use during pregnancy and lactation

Adequate and strictly controlled clinical studies of the safety of the drug Januvia in pregnant women was not conducted. The use of the drug during pregnancy is contraindicated. It is not known whether sitagliptin is excreted in human breast milk. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.
Dosage and administration
When used as monotherapy or in combination with metformin or a PPAR-γ agonist (for example, thiazolidinedione), the recommended dose of Januvia is 100 mg 1 time / day. You can take Januvia regardless of the meal. If the patient missed taking Januvia, the drug should be taken as soon as possible. A double dose of the drug Januvia is not allowed. In case of mildly severe renal failure (CC ≥50 ml / min, approximately corresponding to serum creatinine ≤ 1.7 mg / dl in men, ≤ 1.5 mg / dl in women), no dose adjustment is required. moderate failure (CC ≥30 ml / min, but less than 50 ml / min, approximately corresponding to serum creatinine content greater than 1.7 mg / dL, but ≤3 mg / dL in men, greater than 1.5 mg / dL, but ≤2.5 mg / dl in women) dose of Januvia is 50 mg 1 time / day. In renal insufficiency severe accuracy (QA less than 30 ml / min, approximately corresponding to serum creatinine content greater than 3 mg / dL in men, greater than 2.5 mg / dL in women), for patients with end-stage renal failure and the need for hemodialysis, the dose of Januvia is 25 mg 1 times / day Yanuvia can be used regardless of the schedule of the hemodialysis procedure.

Side effects

Adverse reactions occurring without a causal relationship with taking the drug Januvia at doses of 100 mg and 200 mg per day, but more often than when taking placebo are presented. On the respiratory system: infections of the upper respiratory tract (100 mg - 6.8%, 200 mg - 6.1% , placebo - 6.7%), nasopharyngitis (100 mg - 4.5%, 200 mg - 4.4%, placebo - 3.3%). CNS: headache (100 mg - 3.6%, 200 mg - 3.9%, placebo - 3.6% ). From the digestive system: diarrhea (100 mg - 3%, 200 mg - 2.6%, placebo - 2.3%), abdominal pain (100 mg - 2.3%, 200 mg - 1.3%, placebo - 2.1%), nausea (100 mg - 1.4%, 200 mg - 2.9%, placebo - 0.6%), vomiting (100 mg - 0.8%, 200 mg - 0.7%, placebo - 0.9%), diarrhea (100 mg - 3%, 200 mg - 2.6%,placebo - 2.3%. From the musculoskeletal system: arthralgia (100 mg - 2.1%, 200 mg - 3.3%, placebo - 1.8%). From the endocrine system: hypoglycemia (100 mg - 1.2%, 200 mg - 0.9 %, placebo - 0.9%. On the laboratory side: at doses of 100 mg / day and 200 mg / day - an increase in uric acid by about 0.2 mg / dl compared with placebo (median level 5-5.5 mg / dl) in patients receiving the drug in a dose of 100 mg / day and 200 mg / day. There are no cases of gout development. A slight decrease in total alkaline phosphorus (approximately 5 IU / L compared to placebo, an average level of 56-62 IU / L), partly due to a slight decrease in the AchF bone fraction. A slight increase in leukocyte count (approximately 200 / µl compared with placebo, the average level of 6600 / µl), due to an increase in the number of neutrophils. This observation was noted in most, but not all studies. The listed changes in laboratory parameters are not considered clinically significant. On the background of the use of the drug Januvia, there were no clinically significant changes in vital signs and ECG (including the QTc interval). Januvia is generally well tolerated as monotherapy , and in combination with other hypoglycemic drugs. In clinical studies, the overall incidence of side effects, as well as the frequency of withdrawal of Januvia due to side effects, were similar to those taken with placebo.


Symptoms: During clinical studies on healthy volunteers, good tolerability was observed when taking Januvia in a single dose of 800 mg. Minimal changes in the QTc interval, not considered clinically significant, were noted in one of the studies of the drug at the indicated dose. Clinical studies of the drug in a dose of more than 800 mg / day have not been carried out. Treatment: removal of unabsorbed drug from the gastrointestinal tract, monitoring vital signs, including ECG, if necessary, conducting symptomatic and supportive therapy. Sitagliptin is poorly dialyzed. In clinical studies, only 13.5% of the dose was removed from the body during the 3-4 hour dialysis session. Prolonged dialysis can be prescribed in cases of clinical need. There is no data on the effectiveness of peritoneal dialysis of sitagliptin.

Interaction with other drugs

In studies of the interaction with other drugs, sitagliptin had no 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 CYP3A4, 2C8 or 2C9 isoenzymes. Based on in vitro data, sitagliptin probably does not inhibit CYP2D6, 1A2, 2C19 or 2B6, nor does it induce CYP3A4. There was a slight increase in AUC (11%), as well as an average Cmax (18%) of digoxin when used together with Sitagliptin This increase is not considered clinically significant. It is not recommended to change the dose of either digoxin or Januvia when used simultaneously. An increase in AUC and Сmax of sitagliptin was noted by 29% and 68%, respectively, in patients with a joint use of Januvia in a single dose of 100 mg and cyclosporine (a powerful p-glycoprotein inhibitor) a single dose of 600 mg. These changes in the pharmacokinetic parameters of sitagliptin are not considered clinically significant. Changing the dose of Januvia when combined with cyclosporine and other p-glycoprotein inhibitors (eg, ketoconazole) is not recommended. Population pharmacokinetic analysis in patients and healthy volunteers (n = 858) who received a wide range of concomitant drugs (n = 83, about half of which is excreted by the kidneys), did not reveal any clinically significant effect of drugs on the pharmacokinetics of sitagliptin.

special instructions

In clinical studies of the drug Januvia as monotherapy or as part of a combination therapy with metformin or pioglitazone, the incidence of hypoglycemia with the use of the drug Januvia was similar to the incidence of hypoglycemia with placebo. The combined use of the drug Januvia in combination with drugs that can cause hypoglycemia, such as insulin, sulfonylurea derivatives, has not been studied. For patients with mild and moderate hepatic insufficiency, dose adjustment of the drug Januvia is not required. The drug has not been studied in patients with severe hepatic insufficiency. In clinical studies, the efficacy and safety of Januvia in elderly patients (≥65 years, 409 patients) were comparable with these indicators in patients younger than 65 years. Dose adjustment for age is not required. Elderly patients are more likely to develop renal failure.Accordingly, as in other age groups, dose adjustment is necessary in patients with severe renal insufficiency. Effect on the ability to drive vehicles and control mechanisms There have been no studies to study the effect of the drug Januvia on the ability to drive vehicles. However, the drug is not expected to adversely affect the ability to drive or complex machinery.