Description
Release form
Tablets.
Packing
In a blister pack of 14 tablets. In the package 2 blisters.
Pharmacological action of Janduvia
is an oral hypoglycemic drug, a highly selective dipeptidyl peptidase 4 inhibitor (DPP-4).
Sitagliptin differs in chemical structure and pharmacological action from analogues of glucagon-like peptide-1 (GLP-1), insulin, sulfonylureas, biguanides, β-receptor agonists, peroxisome proliferator-activated (PPAR-β), alpha-glycosidase inhibitors, amylin analogues. By inhibiting DPP-4, sitagliptin increases the concentration of 2 known hormones of the incretin family: GLP-1 and glucose-dependent insulinotropic peptide (HIP). Hormones of the incretin family are secreted in the intestine during the day, their level increases in response to food intake. The incretins are part of the internal physiological system for regulating glucose homeostasis. At normal or elevated blood glucose levels, the 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.
GLP-1 also helps suppress increased secretion of glucagon by β-cells of the pancreas. A decrease in glucagon concentration against the background of an increase in insulin levels helps to reduce glucose production by the liver, which ultimately leads to a decrease in glycemia.
With a low concentration of blood glucose, the listed effects of incretins on insulin release and decreased glucagon secretion are not observed. GLP-1 and HIP do not affect glucagon release in response to hypoglycemia. Under physiological conditions, the activity of incretins is limited by the enzyme DPP-4, which rapidly hydrolyzes incretins with the formation of inactive products.
Sitagliptin prevents the hydrolysis of incretins by the enzyme DPP-4, thereby increasing the plasma concentrations of the active forms of GLP-1 and HIP. By increasing the level of incretins, sitagliptin increases the glucose-dependent release of insulin and helps to reduce the secretion of glucagon. In patients with type 2 diabetes mellitus with hyperglycemia, these changes in the secretion of insulin and glucagon lead to a decrease in the level of glycated hemoglobin b 1 ¡ and a decrease in the plasma concentration of glucose, determined on an empty stomach and after a stress test.
In patients with type 2 diabetes mellitus, taking a single dose of Januvia leads to inhibition of the activity of the DPP-4 enzyme for 24 hours, which leads to an increase in the level of circulating incretins GLP-1 and HIP by a factor of 2 3, an increase in the plasma concentration of insulin and C -peptide, a decrease in the concentration of glucagon in blood plasma, a decrease in fasting glycemia, as well as a decrease in glycemia after glucose loading or food loading.
Indications
Monotherapy: as a supplement to diet and exercise to improve glycemic control in type 2 diabetes.
Combination therapy: type 2 diabetes mellitus to improve glycemic control in combination with metformin or PPAR agonists (for example, thiazolidinedione), when diet and exercise combined with monotherapy with the listed drugs do not lead to adequate glycemic control.
Contraindications
Type 1 diabetes mellitus.
Diabetic ketoacidosis.
Pregnancy.
Lactation (breastfeeding).
Hypersensitivity to the drug.
It is not recommended to prescribe the drug Januvia to children and adolescents under the age of 18 (data on the use of the drug in pediatric practice are not available).
Use with caution in patients with renal failure.
In moderate to severe renal failure, as well as in patients with end-stage renal failure, in need of hemodialysis, correction of the dosage regimen is required.
Use during pregnancy and lactation
Adequate and strictly controlled clinical studies of the safety of Januvia in pregnant women have not been conducted.
The use of the drug during pregnancy is contraindicated.
It is not known whether sitagliptin with breast milk is excreted in humans.
If you need to use the drug during lactation, you should decide whether to stop breastfeeding.
Composition
One film-coated tablet contains:
Active ingredient:
Sitagliptin (in the form of phosphate monohydrate) 100 mg.
Excipients:
Microcrystalline cellulose
Calcium hydrogen phosphate
Sodium croscarmellose
Magnesium stearate
Sodium stearyl fumarate.
Shell Composition:
Opadry II beige 85 F17438
Polyvinyl alcohol
Titanium dioxide
Macrogol (polyethylene glycol) 3350
Talc
Iron oxide yellow
Iron oxide red.
Dosage and administration of
When used as monotherapy or in combination with metformin or PPAR- agonist? (for example, thiazolidinedione), the recommended dose of Januvia is 100 mg 1 time / day.
Januvia can be taken without regard to meals. If the patient missed taking Januvia, then the drug should be taken as soon as possible. It is unacceptable to take a double dose of Januvia.
In renal failure of mild severity (CK? 50 ml / min, approximately equivalent to a serum creatinine content of? 1.7 mg / dl in men,? 1.5 mg / dl in women), dose adjustment is not required.
For moderate renal failure (CC> 30 ml / min, but 1.7 mg / dl, but? 3 mg / dl in men,> 1.5 mg / dl, but? 2.5 mg / dl in women), the dose of Januvia is 50 mg 1 time / day
In severe renal failure (KK3 mg / dl in men,> 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 time / day. Januvia can be used regardless of the schedule of the hemodialysis procedure.
Side effects
From the digestive system: abdominal pain, nausea, vomiting, diarrhea. Laboratory indicators: hyperuricemia, decreased activity of the total and partially bone fractions of alkaline phosphatase, leukocytosis due to an increase in the number of neutrophils.
Other (a causal relationship with the drug has not been established): upper respiratory tract infections, nasopharyngitis, headache, arthralgia. The incidence of hypoglycemia is similar to that of a placebo.
Drug Interaction
In studies of interaction with other drugs, sitagliptin had no clinically relevant 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 also 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 mean C max (18%) digoxin when co-administered with sitagliptin. This increase is not considered clinically significant.
It is not recommended to change the dose of either digoxin or Januvia when co-administered. An increase in AUC and C max of sitagliptin was observed by 29% and 68%, respectively, in patients co-administered with Januvia at a single dose of 100 mg and cyclosporine (a potent p-glycoprotein inhibitor) at a single dose of 600 mg. These changes in the pharmacokinetic parameters of sitagliptin are not considered clinically relevant. It is not recommended to change the dose of the drug Yanuvia when used together with cyclosporine and other p-glycoprotein inhibitors (eg, ketoconazole).
A population pharmacokinetic analysis in patients and healthy volunteers (n = 858) receiving a wide range of concomitant drugs (n = 83, about half of which were excreted by the kidneys) did not reveal any clinically relevant effect of the drugs on the pharmacokinetics of sitagliptin.
Overdose
Symptoms: Good tolerability was observed during clinical studies in healthy volunteers when administered Yanuvia at a single dose of 800 mg. Minimal changes in the QTc interval, which were not considered clinically significant, were noted in one study of the drug at the specified dose. Clinical studies of the drug at a dose of more than 800 mg / day were not conducted.
Treatment: removal of unabsorbed drug from the gastrointestinal tract, monitoring of vital signs, including ECG, if necessary – carrying out symptomatic and supportive therapy. Sitagliptin is poorly dialysable. In clinical studies, only 13.5% of the dose was removed from the body during a 3-4 hour dialysis session. Prolonged dialysis can be prescribed with in case of clinical need. There are no data on the effectiveness of peritoneal dialysis of sitagliptin.
Storage conditions
The drug should be stored at a temperature not exceeding 30 ° C.
Expiration
2 years.
Deystvuyuschee substances
Sytahlyptyn
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dosage form
dosage form
tablets
Akrikhin CPC AO, USA
