Trajenta pills 5mg №30
$79.81
-
All payments are encrypted via SSL
-
Full Refund if you haven't received your order
Indications
Type 2 diabetes:
- as monotherapy in patients with inadequate control of glycemia only on the background of diet and exercise, with intolerance to Metformin, or when contraindicated for its use due to renal failure;
- as a two-component combination therapy with metformin, sulfonylurea derivatives or thiazolidinedione in case of failure of diet therapy, exercise and monotherapy with these drugs;
- as a three-component combination therapy with metformin and sulfonylurea derivatives in the case of the ineffectiveness of diet therapy, exercise and combination therapy with these drugs;
- as a two-component combination therapy with insulin or multicomponent therapy with insulin, metformin and / or pioglitazone and / or sulfonylurea derivatives in case of failure of diet therapy, exercise and combination therapy with these drugs.
Dosage and administration
The drug is taken orally, at any time of the day, regardless of the meal.
The recommended dose is 5 mg (1 tab.) 1 time / day.
When you skip the next admission, the patient should take the drug as soon as he remembers. You should not take a double dose in one day.
Dose adjustment when applied to patients with impaired renal function, the liver and u elderly patients not required.
Adverse effects
The frequency of side effects when using linagliptin at a dose of 5 mg was similar to the frequency of side effects when using placebo.
Termination of therapy due to adverse events was higher in the group of patients receiving placebo (4.4%) than in the group receiving linagliptin 5 mg (3.5%).
At linagliptin monotherapy The following side effects were observed:
Immune system: hypersensitivity reactions.
Respiratory: cough.
Gastrointestinal: pancreatitis.
Infectious diseases: nasopharyngitis.
At use of linagliptin with metformin:
Immune system: hypersensitivity reactions.
Respiratory: cough.
Gastrointestinal: pancreatitis.
Infectious diseases: nasopharyngitis.
At use of linagliptin with sulfonylurea derivatives:
Immune system: hypersensitivity reactions.
Metabolic disorders: hypertriglyceridemia.
Respiratory: cough.
Gastrointestinal: pancreatitis.
Infectious diseases: nasopharyngitis.
At use of linagliptin with pioglitazone:
Immune system: hypersensitivity reactions.
Metabolic disorders: hyperlipidemia.
Respiratory: cough.
Gastrointestinal: pancreatitis.
Infectious diseases: nasopharyngitis.
Other: weight gain.
At use of linagliptin with insulin:
Immune system: hypersensitivity reactions.
Respiratory: cough.
Gastrointestinal: pancreatitis, constipation.
Infectious diseases: nasopharyngitis.
At use of linagliptin with metformin and sulfonylurea derivatives:
Immune system: hypersensitivity.
Metabolic disorders: hypoglycemia.
Respiratory: cough.
Gastrointestinal: pancreatitis.
Infectious diseases: nasopharyngitis.
At use of linagliptin with metformin and pioglitazone:
Immune system: hypersensitivity reactions.
Metabolic disorders: hyperlipidemia.
Respiratory: cough.
Gastrointestinal: pancreatitis.
Infectious diseases: nasopharyngitis.
Other: weight gain.
Post-marketing application experience:
Immune system: angioedema, urticaria.
Gastrointestinal: ulceration of the oral mucosa.
From the skin: rash.
Contraindications
- diabetes mellitus type 1;
- diabetic ketoacidosis;
- pregnancy;
- lactation period (breastfeeding);
- children's and teenage age up to 18 years;
- hypersensitivity to any component of the drug.
Use during pregnancy and lactation
The use of linagliptin during pregnancy and during breastfeeding is contraindicated.
The data obtained in preclinical studies in animals, indicate the release of linagliptin and its metabolite in breast milk. The risk of exposure to newborns and children during breastfeeding is not excluded.
If necessary, use linagliptin during lactation lactation should be discontinued.
Application for violations of the liver
Dose adjustment when used in patients with impaired liver function is not required.
Application for violations of kidney function
Dose adjustment for use in patients with impaired renal function is not required.
Use in children
The drug is contraindicated in children and adolescents under 18 years of age.
Use in elderly patients
Dose adjustment when used in elderly patients is not required.
Special notes
The use of the drug Trazhent® contraindicated in patients with type 1 diabetes mellitus or for the treatment of diabetic ketoacidosis.
Hypoglycemia
The incidence of hypoglycemia in the case of using linagliptin as monotherapy was comparable to placebo.
In clinical studies, it was reported that the incidence of hypoglycemia when using linagliptin in combination with drugs that are not believed to cause hypoglycemia (metformin, thiazolidinedione derivatives) was similar to the corresponding placebo effect.
Sulfonylurea derivatives are known to cause hypoglycemia. Therefore, if linagliptin is used in combination with sulfonylurea derivatives, caution should be exercised. If necessary, reduce the dose of sulfonylurea derivatives.
The use of linagliptin does not increase the risk of developing cardiovascular diseases.
Linagliptin in combination therapy with other oral hypoglycemic drugs was used in patients with severe renal failure.
Linagliptin provided a significant decrease in the concentration of glycated hemoglobin and the fasting glucose concentration.
Use of linagliptin in patients over the age of 70
The use of linagliptin resulted in a significant decrease in glycated hemoglobin A (HbA1c) (0.64% compared with placebo; baseline HbA1c accounted for about 7.8%). The use of linagliptin also led to a significant decrease in fasting plasma glucose.
Cardiovascular risk
Linagliptin treatment does not lead to an increase in cardiovascular risk. The primary endpoint (a combination of incidence or time before the first occurrence of cardiovascular death, nonfatal myocardial infarction, nonfatal stroke, or hospitalization due to unstable angina) was significantly less common in patients treated with linagliptin than in the combined group of patientsreceiving active comparison drugs and placebo (relative risk 0.78; 95% confidence interval 0.55; 1.12).
Post-marketing experience
In patients taking linagliptin, cases of acute pancreatitis have been reported. If pancreatitis is suspected, use of the drug should be discontinued.
Influence on ability to drive vehicles and mechanisms
Studies on the effect of the drug on the ability to drive vehicles and mechanisms have been conducted. However, due to the possible development of vertigo, caution should be exercised when driving vehicles and machinery.
Overdosage
During controlled clinical trials in healthy volunteers, a single dose of 600 mg of linagliptin (120 times the recommended dose) was well tolerated. Experience using linagliptin dose greater than 600 mg, no.
Treatment: in case of overdose, it is recommended to use usual supportive measures, for example, removal of unabsorbed drug from the gastrointestinal tract, implementation of clinical control and symptomatic therapy.
Drug interaction
Evaluation of in vitro drug interactions
Linagliptin is a weak competitive inhibitor of the isoenzyme CYP3A4 .
Linagliptin does not inhibit other CYP isoenzymes and is not their inducer.
Linagliptin is a substrate for P-glycoprotein and inhibits the transport of Digoxin to a small extent mediated by P-glycoprotein.
Evaluation of drug interactions in vivo
Linagliptin has no clinically significant effect on the pharmacokinetics of metformin, glibenclamide, Simvastatin, pioglitazone, Warfarin, digoxin, and oral contraceptive drugs, which has been proven in vivo, and is based on the low ability of linagliptin to cause drug interactions with substrates for CYP3A4, CYP2C9, CYP2C8, P-glycoprotein and organic cation transport molecules.
Metformin. The combined use of metformin (repeated daily dose of 850 mg 3 times / day) and linagliptin at a dose of 10 mg 1 time / day (higher than the therapeutic dose) in healthy volunteers did not lead to clinically significant changes in the pharmacokinetics of linagliptin or metformin. Thus, linagliptin is not an inhibitor of the transport of organic cations.
Sulfonylurea derivatives. The pharmacokinetics of linagliptin (5 mg) did not change when combined with glibenclamide (a single dose of glyburide 1.75 mg) and repeated intake of linagliptin orally (5 mg). However, a clinically insignificant decrease in AUC and C values was noted.max glibenclamide by 14%. Since glibenclamide is metabolized primarily by CYP2C9, this data also supports the conclusion that linagliptin is not a CYP2C9 inhibitor. No clinically significant interactions are expected with other sulfonylurea derivatives (for example, glipizide and glimepiride), which, like glibenclamide, are mainly metabolized by CYP2C9.
Thiazolidinedione. The combined use of multiple doses of linagliptin at 10 mg / day (higher than the therapeutic dose) and pioglitazone at 45 mg / day (repeated administration), which is a substrate for CYP2C8 and CYP3A4, did not have a clinically significant effect on the pharmacokinetics of linagliptin or pioglitazone, or active pioglitase metabolites . This indicates that linagliptin is in vivo is not an inhibitor of metabolism mediated by CYP2C8, and confirms the conclusion that there is no significant inhibitory effect of linagliptin in vivo on CYP3A4.
Ritonavir The combined use of linagliptin (single dose in a dose of 5 mg) and ritonavir (repeated intake of 200 mg), an active inhibitor of P-glycoprotein and the isoenzyme CYP3A4, increased the values of AUC and Cmax linagliptin, approximately 2 times and 3 times, respectively. However, these changes in linagliptin pharmacokinetics were not considered significant. Therefore, a clinically significant interaction with other inhibitors of P-glycoprotein and CYP3A4 is not expected, and a dose change is not required.
Rifampicin. Repeated combined use of linagliptin and rifampicin, the active inducer of P-glycoprotein and CYP3A4 isoenzyme, led to a decrease in AUC and C valuesmax linagliptin, by 39.6% and 43.8%, respectively, and to a decrease in the inhibition of the basal activity of dipeptidyl peptidase-4, by approximately 30%. Thus, it is expected that the clinical efficacy of linagliptin, which is used in combination with active inducers of P-glycoprotein, will be maintained, although it may not manifest fully.
Digoxin. The combined repeated use of linagliptin (5 mg / day) and digoxin (0.25 mg / day) in healthy volunteers did not affect the pharmacokinetics of digoxin. Thus, linagliptin in vivo is not an inhibitor of transport mediated by P-glycoprotein.
Warfarin. Linagliptin, administered repeatedly at a dose of 5 mg / day, did not change the pharmacokinetics of warfarin, which is a substrate for CYP2C9, which indicates that linagliptin does not have the ability to inhibit CYP2C9.
Simvastatin. Linagliptin, which was used repeatedly in healthy volunteers at a dose of 10 mg / day (above the therapeutic dose), had a minimal effect on the pharmacokinetic parameters of simvastatin, which is a sensitive substrate for CYP3A4. After taking linagliptin at a dose of 10 mg together with simvastatin, used at a daily dose of 40 mg for 6 days, the AUC value of simvastatin increased by 34%, and the C valuemax - on 10%. Thus, linagliptin is a weak inhibitor of CYP3A4-mediated metabolism. Changes in dose while taking with drugs that are metabolized with the participation of CYP3A4, is considered impractical.
Oral contraceptive drugs. The combined use of linagliptin 5 mg with levonorgestrel or ethinyl estradiol did not change the pharmacokinetics of these drugs.
Terms and conditions of storage
The drug should be stored out of the reach of children at a temperature not higher than 25 ° C.