Sitagliptin | Xelevia tablets coated.pl.ob. 100 mg 28 pcs.
Special Price
$42.14
Regular Price
$50.00
In stock
SKU
BID873175
Release form
Tablets, film-coated
Tablets, film-coated
Release form
Tablets, film-coated
Indications
Monotherapy
Xelevia® is indicated as a supplement to diet and exercise to improve glycemic control in patients with type 2 diabetes.
Combination therapy
Combination with metformin
Xelevia® in combination with metformin is indicated for patients with type 2 diabetes mellitus to improve glycemic control as a starting therapy or when diet and exercise combined with monotherapy with one of the listed drugs do not lead to adequate glycemic control .
Combination with sulfonylurea derivatives
Xelevia® in combination with sulfonylurea derivatives is indicated for patients with type 2 diabetes mellitus to improve glycemic control when diet and exercise combined with monotherapy with one of these drugs do not lead to adequate glycemic control.
Combination with PPAR- agonists
Xelevia® in combination with PPAR- agonists (thiazolidinediones) is indicated for patients with type 2 diabetes mellitus to improve glycemic control, when diet and physical activity in combination with monotherapy with one of the listed drugs do not lead to adequate glycemic control.
Combination with metformin and sulfonylurea derivatives
Xelevia® in combination with metformin and sulfonylurea derivatives is indicated for patients with type 2 diabetes mellitus to improve glycemic control when diet and exercise combined with therapy of two of the above drugs do not lead to adequate glycemic control.
Combination with metformin and PPAR- agonists
Xelevia® in combination with metformin and PPAR- (thiazolidinediones) is indicated for patients with type 2 diabetes mellitus to improve glycemic control, when diet and physical activity combined with therapy with two of these drugs do not lead to adequate glycemic control.
Combination with insulin
Xelevia® is indicated for patients with type 2 diabetes mellitus as a supplement to insulin (with or without metformin) in cases where diet, exercise and a stable dose of insulin do not lead to adequate glycemic control.
Contraindications
- Hypersensitivity to any of the components of the
preparation - pregnancy, the period of breastfeeding
- type 1 diabetes mellitus
- diabetic ketoacidosis
- children under the age of 18 years of moderate severity and more severe dosages - see section Dosage and administration).
Precautions:
Renal failure
The main route of excretion of sitagliptin from the body is renal excretion. To achieve the same plasma concentrations as in patients with normal excretory function of the kidneys, in patients with moderate to severe renal failure, as well as patients with end-stage chronic renal failure, requiring hemodialysis or peritoneal dialysis, it is necessary to carry out correction (reduction) of the dose of Xelevia® (see section Dosage and Administration. Patients with renal failure).
Pancreatitis
Acute pancreatitis, including hemorrhagic or necrotic with fatal and non-fatal outcome, has been reported in patients taking sitagliptin (see section Adverse effects). Patients should be informed about the characteristic symptoms of acute pancreatitis: persistent, severe abdominal pain. Clinical manifestations of pancreatitis disappeared after discontinuation of sitagliptin. In case of suspected pancreatitis, you must stop taking Xelevia® and other potentially dangerous drugs.
Use during pregnancy and lactation
There were no controlled studies of the drug XeleviaВ® in pregnant women, therefore, there is no data on the safety of its use in pregnant women.
XeleviaВ®, like other oral hypoglycemic drugs, is not recommended for use during pregnancy. There is no data on the penetration of sitagliptin into breast milk. Therefore, the drug XeleviaВ® should not be prescribed during breastfeeding.
Special instructions
Hypoglycemia
According to clinical trials of sitagliptin, the incidence of hypoglycemia with monotherapy or combination therapy with drugs that do not cause hypoglycemia (metformin, pioglitazone) was comparable with the incidence of hypoglycemia in the placebo group. As with other hypoglycemic drugs, hypoglycemia was observed with sitagliptin in combination with insulin or sulfonylurea derivatives (see section Side effects). In order to reduce the risk of sulfon-induced hypoglycemia, the dose of sulfonylurea derivative should be reduced (see section Dosage and Administration).
Use in the elderly
In clinical studies, the efficacy and safety of sitagliptin in elderly patients (≥65 years of age, 409 patients) were comparable to those in patients younger than 65 years of age. Dose adjustment based on age is not required. Elderly patients are more likely to develop renal failure. Accordingly, as in other age groups, a dose adjustment is necessary in patients with severe renal failure (see section Dosage and Administration).
Sitagliptin Cardiovascular Safety Assessment Study (TECOS)
Sitagliptin Cardiovascular Safety Assessment Study (TECOS) patients took sitagliptin 100 mg per day (or 50 mg per day if baseline glomerular filtration rate (eGFR) was 30 and <50 ml / min / 1, 73 m2), or placebo, which were added to standard therapy according to existing national standards for determining target levels of HbA1C and monitoring cardiovascular risk factors. At the end of the average follow-up period of 3 years, in patients with type 2 diabetes, taking sitagliptin in addition to standard treatment did not increase the risk of serious adverse events from the cardiovascular system (risk ratio 0.98 95% confidence interval, 0.89 -1.08 p <0.001 to prove the lack of superiority) or the risk of hospitalization due to heart failure (risk ratio 1.00 95% confidence interval, 0.83-1.20 p = 0.98 for difference in the frequency of risks), compared with standard treatment b supplementation of sitagliptin.
Impact on the ability to drive transp. Wed and fur .:
No studies have been conducted to examine the effect of Xelevia® on the ability to drive vehicles and operate machinery. However, Xelevia® is not expected to adversely affect the ability to drive vehicles and operate machinery.
Composition
One film-coated tablet contains:
Active ingredient:
sitagliptin phosphate monohydrate 128.5 mg (equivalent to 100 mg sitagliptin).
Excipients:
microcrystalline cellulose 123.8 mg, calcium
hydrophosphate ground 123.8 mg, croscarmellose sodium
8,000 mg magnesium
4,000 mg
sodium strdylkp stearyl fumarate 12,00 mg srdlp tablet 85, 16438f8, 8rdlp 00 mg) contains:
polyvinyl alcohol 40,000%,
titanium dioxide (E 171) 21,560%,
macrogol 3350 (polyethylene glycol) 20,200%,
talc 14,800%,
iron oxide yellow (E 172) 3,070% iron oxide red, srdl (E 172) 0.370%.
Dosage and administration
The recommended dose of XeleviaΠis 100 mg once daily orally as monotherapy, or in combination with metformin, or sulfonylurea derivatives, or PPAR-? agonists? (thiazolidinediones), or insulin (with or without metformin), or in combination with metformin and a sulfonylurea derivative, or metformin and PPAR-? agonists.
XeleviaΠcan be taken without regard to meals. Metformin dosage regimen sulfonylurea derivatives and PPAR- agonists should be selected based on recommended doses for these drugs.
When combining XeleviaΠwith sulfonylurea derivatives or with insulin, it is advisable to reduce the traditionally recommended dose of sulfonylurea or insulin derivative to reduce the risk of sulfone-induced or insulin-induced hypoglycemia (see Special instructions. Hypoglycemia).
If the patient has missed taking Xeleviaά the drug should be taken as soon as possible after the patient remembers the missed dose.
Do not take a double dose of XeleviaΠon the same day.
Patients with renal failure
Patients with mild renal failure (creatinine clearance (QC)? 50 ml / min, approximately corresponding to a serum creatinine concentration of? 1.7 mg / dl in men and? 1.5 mg / dl in women) dose adjustment of the drug XeleviaΠis not required.
Due to the need to adjust the dose of sitagliptin in patients with moderate to severe renal insufficiency, the use of XeleviaΠis not shown in this category of patients (the absence of risks on a 100 mg tablet and the absence of 25 mg and 50 mg dosages does not allow for its dosage regimen in patients with moderate to severe renal failure).
Due to the need for dose adjustment, it is recommended that patients with renal failure assess renal function before starting treatment with sitagliptin and periodically during treatment.
Patients with liver failure
No dose adjustment of XeleviaΠis required in patients with mild to moderate hepatic failure. The drug has not been studied in patients with severe liver failure.
Elderly patients
No dose adjustment is required for XeleviaΠin elderly patients.
Drug Interactions
In studies involving other drugs, sitagliptin did not have a clinically significant effect on the pharmacokinetics of the following drugs: metformin, rosiglitazone, glibenclamide, simvastatin, warfarin, or oral contraceptives. Based on these data, sitagliptin does not inhibit CYP3A4, 2C8 or 2C9 isoenzymes. Based on in vitro data, sitagliptin also does not inhibit CYP2D6, 1A2, 2C19 and 2B6 isoenzymes and does not induce CYP3A4 isoenzyme. Repeated administration of metformin in combination with sitagliptin did not significantly affect the pharmacokinetic parameters of sitagliptin in patients with type 2 diabetes mellitus.
According to the population pharmacokinetic analysis of type 2 diabetes patients, concomitant therapy did not have a clinically significant effect on the pharmacokinetics of sitagliptin. The study evaluated a number of drugs most commonly used by patients with type 2 diabetes mellitus, including: lipid-lowering drugs (statins, fibrates, ezetimibe), antiplatelet agents (clopidogrel), antihypertensive drugs (ACE inhibitors, angiotensin II receptor antagonists, beta-blockers, blockers slow calcium channels, hydrochlorothiazide), non-steroidal anti-inflammatory drugs (naproxen, diclofenac, celecoxib), antidepressants (bupropion, fluoxetine, sertraline), antihistamines (cetirizi m) proton pump inhibitors (omeprazole, lansoprazole) and drugs for the treatment of erectile dysfunction (sildenafil).
A slight increase in AUC (11%), as well as average Cmax (18%) of digoxin was observed when combined with sitagliptin. This increase is not considered clinically significant. It is not recommended to change the dose of either digoxin or sitagliptin when used together.
An increase in AUC and Cmax of sitagliptin was noted by 29% and 68%, respectively, in patients with the combined use of a single oral dose of 100 mg of sitagliptin and a single oral dose of 600 mg of cyclosporine, a potent inhibitor of p-glycoprotein. The observed changes in the pharmacokinetic characteristics of sitagliptin are not considered clinically significant. A change in the dose of Xelevia® is not recommended when combined with cyclosporine and other p-glycoprotein inhibitors (e.g. ketoconazole).
A population-based pharmacokinetic analysis of patients and healthy volunteers (N = 858) for a wide range of concomitant medications (N = 83, approximately half of which is excreted by the kidneys) did not reveal any clinically significant effects of these substances on the pharmacokinetics of sitagliptin.
Overdose of
During clinical trials in healthy volunteers, a single dose of 800 mg of sitagliptin was generally well tolerated. Minimal changes in the QTc interval, not considered clinically significant, were observed in one of the studies of sitagliptin at a dose of 800 mg per day. A dose of over 800 mg per day in humans has not been studied.
In the first phase of clinical trials, multiple doses of any adverse reactions associated with treatment with sitagliptin were not observed when taking the drug in a daily dose of up to 400 mg for 28 days.
In case of overdose, it is necessary to start standard supportive measures: removal of the unabsorbed drug from the gastrointestinal tract, monitoring of vital signs, including ECG, as well as the appointment of maintenance therapy, if necessary.
Sitagliptin is poorly dialyzed. In clinical studies, only 13.5% of the dose was removed from the body during a 3-4 hour dialysis session. Prolonged dialysis may be prescribed if necessary. There is no evidence of the effectiveness of peritoneal dialysis for sitagliptin.
Storage conditions
Do not store above 25 РC.
Keep out of the reach and sight of children.
Expiration
2 years.
Active thing
substance Sitagliptin
Terms leave through pharmacies
In retseptu
lekarstvennaja form
tablets
Tablets, film-coated
Indications
Monotherapy
Xelevia® is indicated as a supplement to diet and exercise to improve glycemic control in patients with type 2 diabetes.
Combination therapy
Combination with metformin
Xelevia® in combination with metformin is indicated for patients with type 2 diabetes mellitus to improve glycemic control as a starting therapy or when diet and exercise combined with monotherapy with one of the listed drugs do not lead to adequate glycemic control .
Combination with sulfonylurea derivatives
Xelevia® in combination with sulfonylurea derivatives is indicated for patients with type 2 diabetes mellitus to improve glycemic control when diet and exercise combined with monotherapy with one of these drugs do not lead to adequate glycemic control.
Combination with PPAR- agonists
Xelevia® in combination with PPAR- agonists (thiazolidinediones) is indicated for patients with type 2 diabetes mellitus to improve glycemic control, when diet and physical activity in combination with monotherapy with one of the listed drugs do not lead to adequate glycemic control.
Combination with metformin and sulfonylurea derivatives
Xelevia® in combination with metformin and sulfonylurea derivatives is indicated for patients with type 2 diabetes mellitus to improve glycemic control when diet and exercise combined with therapy of two of the above drugs do not lead to adequate glycemic control.
Combination with metformin and PPAR- agonists
Xelevia® in combination with metformin and PPAR- (thiazolidinediones) is indicated for patients with type 2 diabetes mellitus to improve glycemic control, when diet and physical activity combined with therapy with two of these drugs do not lead to adequate glycemic control.
Combination with insulin
Xelevia® is indicated for patients with type 2 diabetes mellitus as a supplement to insulin (with or without metformin) in cases where diet, exercise and a stable dose of insulin do not lead to adequate glycemic control.
Contraindications
- Hypersensitivity to any of the components of the
preparation - pregnancy, the period of breastfeeding
- type 1 diabetes mellitus
- diabetic ketoacidosis
- children under the age of 18 years of moderate severity and more severe dosages - see section Dosage and administration).
Precautions:
Renal failure
The main route of excretion of sitagliptin from the body is renal excretion. To achieve the same plasma concentrations as in patients with normal excretory function of the kidneys, in patients with moderate to severe renal failure, as well as patients with end-stage chronic renal failure, requiring hemodialysis or peritoneal dialysis, it is necessary to carry out correction (reduction) of the dose of Xelevia® (see section Dosage and Administration. Patients with renal failure).
Pancreatitis
Acute pancreatitis, including hemorrhagic or necrotic with fatal and non-fatal outcome, has been reported in patients taking sitagliptin (see section Adverse effects). Patients should be informed about the characteristic symptoms of acute pancreatitis: persistent, severe abdominal pain. Clinical manifestations of pancreatitis disappeared after discontinuation of sitagliptin. In case of suspected pancreatitis, you must stop taking Xelevia® and other potentially dangerous drugs.
Use during pregnancy and lactation
There were no controlled studies of the drug XeleviaВ® in pregnant women, therefore, there is no data on the safety of its use in pregnant women.
XeleviaВ®, like other oral hypoglycemic drugs, is not recommended for use during pregnancy. There is no data on the penetration of sitagliptin into breast milk. Therefore, the drug XeleviaВ® should not be prescribed during breastfeeding.
Special instructions
Hypoglycemia
According to clinical trials of sitagliptin, the incidence of hypoglycemia with monotherapy or combination therapy with drugs that do not cause hypoglycemia (metformin, pioglitazone) was comparable with the incidence of hypoglycemia in the placebo group. As with other hypoglycemic drugs, hypoglycemia was observed with sitagliptin in combination with insulin or sulfonylurea derivatives (see section Side effects). In order to reduce the risk of sulfon-induced hypoglycemia, the dose of sulfonylurea derivative should be reduced (see section Dosage and Administration).
Use in the elderly
In clinical studies, the efficacy and safety of sitagliptin in elderly patients (≥65 years of age, 409 patients) were comparable to those in patients younger than 65 years of age. Dose adjustment based on age is not required. Elderly patients are more likely to develop renal failure. Accordingly, as in other age groups, a dose adjustment is necessary in patients with severe renal failure (see section Dosage and Administration).
Sitagliptin Cardiovascular Safety Assessment Study (TECOS)
Sitagliptin Cardiovascular Safety Assessment Study (TECOS) patients took sitagliptin 100 mg per day (or 50 mg per day if baseline glomerular filtration rate (eGFR) was 30 and <50 ml / min / 1, 73 m2), or placebo, which were added to standard therapy according to existing national standards for determining target levels of HbA1C and monitoring cardiovascular risk factors. At the end of the average follow-up period of 3 years, in patients with type 2 diabetes, taking sitagliptin in addition to standard treatment did not increase the risk of serious adverse events from the cardiovascular system (risk ratio 0.98 95% confidence interval, 0.89 -1.08 p <0.001 to prove the lack of superiority) or the risk of hospitalization due to heart failure (risk ratio 1.00 95% confidence interval, 0.83-1.20 p = 0.98 for difference in the frequency of risks), compared with standard treatment b supplementation of sitagliptin.
Impact on the ability to drive transp. Wed and fur .:
No studies have been conducted to examine the effect of Xelevia® on the ability to drive vehicles and operate machinery. However, Xelevia® is not expected to adversely affect the ability to drive vehicles and operate machinery.
Composition
One film-coated tablet contains:
Active ingredient:
sitagliptin phosphate monohydrate 128.5 mg (equivalent to 100 mg sitagliptin).
Excipients:
microcrystalline cellulose 123.8 mg, calcium
hydrophosphate ground 123.8 mg, croscarmellose sodium
8,000 mg magnesium
4,000 mg
sodium strdylkp stearyl fumarate 12,00 mg srdlp tablet 85, 16438f8, 8rdlp 00 mg) contains:
polyvinyl alcohol 40,000%,
titanium dioxide (E 171) 21,560%,
macrogol 3350 (polyethylene glycol) 20,200%,
talc 14,800%,
iron oxide yellow (E 172) 3,070% iron oxide red, srdl (E 172) 0.370%.
Dosage and administration
The recommended dose of XeleviaΠis 100 mg once daily orally as monotherapy, or in combination with metformin, or sulfonylurea derivatives, or PPAR-? agonists? (thiazolidinediones), or insulin (with or without metformin), or in combination with metformin and a sulfonylurea derivative, or metformin and PPAR-? agonists.
XeleviaΠcan be taken without regard to meals. Metformin dosage regimen sulfonylurea derivatives and PPAR- agonists should be selected based on recommended doses for these drugs.
When combining XeleviaΠwith sulfonylurea derivatives or with insulin, it is advisable to reduce the traditionally recommended dose of sulfonylurea or insulin derivative to reduce the risk of sulfone-induced or insulin-induced hypoglycemia (see Special instructions. Hypoglycemia).
If the patient has missed taking Xeleviaά the drug should be taken as soon as possible after the patient remembers the missed dose.
Do not take a double dose of XeleviaΠon the same day.
Patients with renal failure
Patients with mild renal failure (creatinine clearance (QC)? 50 ml / min, approximately corresponding to a serum creatinine concentration of? 1.7 mg / dl in men and? 1.5 mg / dl in women) dose adjustment of the drug XeleviaΠis not required.
Due to the need to adjust the dose of sitagliptin in patients with moderate to severe renal insufficiency, the use of XeleviaΠis not shown in this category of patients (the absence of risks on a 100 mg tablet and the absence of 25 mg and 50 mg dosages does not allow for its dosage regimen in patients with moderate to severe renal failure).
Due to the need for dose adjustment, it is recommended that patients with renal failure assess renal function before starting treatment with sitagliptin and periodically during treatment.
Patients with liver failure
No dose adjustment of XeleviaΠis required in patients with mild to moderate hepatic failure. The drug has not been studied in patients with severe liver failure.
Elderly patients
No dose adjustment is required for XeleviaΠin elderly patients.
Drug Interactions
In studies involving other drugs, sitagliptin did not have a clinically significant effect on the pharmacokinetics of the following drugs: metformin, rosiglitazone, glibenclamide, simvastatin, warfarin, or oral contraceptives. Based on these data, sitagliptin does not inhibit CYP3A4, 2C8 or 2C9 isoenzymes. Based on in vitro data, sitagliptin also does not inhibit CYP2D6, 1A2, 2C19 and 2B6 isoenzymes and does not induce CYP3A4 isoenzyme. Repeated administration of metformin in combination with sitagliptin did not significantly affect the pharmacokinetic parameters of sitagliptin in patients with type 2 diabetes mellitus.
According to the population pharmacokinetic analysis of type 2 diabetes patients, concomitant therapy did not have a clinically significant effect on the pharmacokinetics of sitagliptin. The study evaluated a number of drugs most commonly used by patients with type 2 diabetes mellitus, including: lipid-lowering drugs (statins, fibrates, ezetimibe), antiplatelet agents (clopidogrel), antihypertensive drugs (ACE inhibitors, angiotensin II receptor antagonists, beta-blockers, blockers slow calcium channels, hydrochlorothiazide), non-steroidal anti-inflammatory drugs (naproxen, diclofenac, celecoxib), antidepressants (bupropion, fluoxetine, sertraline), antihistamines (cetirizi m) proton pump inhibitors (omeprazole, lansoprazole) and drugs for the treatment of erectile dysfunction (sildenafil).
A slight increase in AUC (11%), as well as average Cmax (18%) of digoxin was observed when combined with sitagliptin. This increase is not considered clinically significant. It is not recommended to change the dose of either digoxin or sitagliptin when used together.
An increase in AUC and Cmax of sitagliptin was noted by 29% and 68%, respectively, in patients with the combined use of a single oral dose of 100 mg of sitagliptin and a single oral dose of 600 mg of cyclosporine, a potent inhibitor of p-glycoprotein. The observed changes in the pharmacokinetic characteristics of sitagliptin are not considered clinically significant. A change in the dose of Xelevia® is not recommended when combined with cyclosporine and other p-glycoprotein inhibitors (e.g. ketoconazole).
A population-based pharmacokinetic analysis of patients and healthy volunteers (N = 858) for a wide range of concomitant medications (N = 83, approximately half of which is excreted by the kidneys) did not reveal any clinically significant effects of these substances on the pharmacokinetics of sitagliptin.
Overdose of
During clinical trials in healthy volunteers, a single dose of 800 mg of sitagliptin was generally well tolerated. Minimal changes in the QTc interval, not considered clinically significant, were observed in one of the studies of sitagliptin at a dose of 800 mg per day. A dose of over 800 mg per day in humans has not been studied.
In the first phase of clinical trials, multiple doses of any adverse reactions associated with treatment with sitagliptin were not observed when taking the drug in a daily dose of up to 400 mg for 28 days.
In case of overdose, it is necessary to start standard supportive measures: removal of the unabsorbed drug from the gastrointestinal tract, monitoring of vital signs, including ECG, as well as the appointment of maintenance therapy, if necessary.
Sitagliptin is poorly dialyzed. In clinical studies, only 13.5% of the dose was removed from the body during a 3-4 hour dialysis session. Prolonged dialysis may be prescribed if necessary. There is no evidence of the effectiveness of peritoneal dialysis for sitagliptin.
Storage conditions
Do not store above 25 РC.
Keep out of the reach and sight of children.
Expiration
2 years.
Active thing
substance Sitagliptin
Terms leave through pharmacies
In retseptu
lekarstvennaja form
tablets
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