With increasing doses of saxagliptin it was observed a proportional increase in dianabol before and after the value of area under the curve “concentration-time» (AUC) saxagliptin and its major metabolite.
A notable accumulation of saxagliptin and its major metabolite with a long reception of the drug 1 time per day was observed. There were no clearance depending saxagliptin and its main metabolite of the dose and duration of therapy for receiving saxagliptin once daily at doses ranging from 2.5 mg to 400 mg over 14 days. Absorption after oral administration is absorbed at least 75% of the dose saxagliptin . Eating does not have a significant effect on the pharmacokinetics of saxagliptin in healthy volunteers. Ingestion of high fat had no effect on C max saxagliptin, while AUC increased by 27% compared to fasting. The time to reach C max (T max ) for saxagliptin increased by approximately 0.5 hours while taking the drug with meals compared to fasting. However, these changes are not clinically significant.
Distribution The binding of saxagliptin and its major metabolite with serum proteins slightly, so it can be assumed that saxagliptin distribution for changes in protein composition of blood serum, have been reported with hepatic or renal failure, will not be subject to significant changes. Metabolismsaxagliptin metabolized mainly by involvement of cytochrome P450 isoenzymes to form an active primary metabolite, an inhibitory effect is in respect of a DPP-4 is expressed in 2-fold weaker than that of saxagliptin. excretion saxagliptin is excreted in urine and bile. After receiving a single dose of 50 mg labeled with 14 C-saxagliptin 24% of the dose excreted by the kidneys as unchanged saxagliptin and 36% – in the form of the main metabolite saxagliptin. Total radioactivity was detected in urine corresponded to 75% of the dose of the drug. Middle renal clearance saxagliptin was about 230 ml / min, mean glomerular filtration -. Approximately 120 ml / min . For the main metabolite renal clearance were comparable with mean values of glomerular filtration About 22% of the radioactivity was found in the faeces.
This increase in AUC values is not clinically significant, so dose adjustment is required. Patients with renal insufficiency of moderate to severe, and in hemodialysis patients AUC values of saxagliptin and its major metabolite were respectively 2.1 and 4.5 times higher , than those in patients with normal renal function. For patients with moderate and severe renal impairment and for patients on hemodialysis, the dose should be saxagliptin 2.5 mg 1 time a day (cm. Sections “Dosage and Administration” and “Cautions”). Abnormal liver function Patients with light, moderate and severe liver dysfunction showed no clinically significant changes in dianabol before and after parameters saxagliptin, so correction dose for such patients is not required. elderly patients 65-80 years showed no clinically significant differences in pharmacokinetic parameters saxagliptin compared with patients younger (18-40 years), so that the dose adjustment in elderly patients is not required. However, it should be noted that this category of patients more likely to decline in renal function (see. Sections “Dosage and Administration” and “Cautions”).
Type 2 diabetes mellitus in addition to diet and exercise to improve glycemic control as:
- starting the combined therapy with metformin;
- add to monotherapy with metformin, thiazolidinediones, sulfonilomocheviny derivatives, in the absence of adequate glycemic control on this therapy.
- Individual hypersensitivity to any component of the formulation;
- Type 1 diabetes (application not known);
- Application together with insulin (not examined);
- Diabetic ketoacidosis;
- Congenital galactose intolerance, lactase deficiency and glucose-galactose malabsorption;
- Pregnancy, lactation;
- Age 18 years (safety and efficacy not studied).
Precautions : renal impairment, and moderate to severe; elderly patients; concomitant use with sulfonylureas.
During pregnancy and lactation
Due to the fact that the use of saxagliptin in pregnancy is not known, should not be given the drug during pregnancy.
It is unknown whether saxagliptin passes into breast milk. Due to the fact that there is a possibility of penetration of saxagliptin in breast milk, breast-feeding should be discontinued during treatment saxagliptin or cancel the therapy, taking into account the ratio of risk to the child and the benefit for the mother.
DOSAGE AND ADMINISTRATION:
Inside, regardless of meals. Monotherapy : the recommended dose of saxagliptin is 5 mg 1 time per day. Combination therapy : The recommended dose of saxagliptin is 5 mg I once daily in combination with metformin, thiazolidinediones or sulfonylureas. With a starting Combining therapy with metformin, the recommended dose of saxagliptin is 5 mg 1 time a day, the initial dose of metformin – 500 mg per day. In case of inadequate response metformin dose can be increased. When the missed doses dianabol before and after missed tablet should be taken as soon as the patient has to remember it, but it should not take a double dose of the drug for one day. Use in specific patient populations Patients with impaired function kidney for patients with renal insufficiency, mild (creatinine clearance> 50 ml / min) dose adjustment is required. for patients with moderate or severe renal impairment (creatinine clearance < 50 mL / min) and in patients on hemodialysis the recommended dose Ongliza drug ® is 2.5 mg 1 time per day. The drug should be taken at the end of hemodialysis. The use of saxagliptin in patients on peritoneal dialysis has not been studied. Before therapy saxagliptin and during treatment is recommended to evaluate renal function. Patients with impaired liver function If abnormal liver function mild, moderate and severe dose adjustment is not needed. elderly patients no dose adjustment in elderly patients is not required.However, when choosing the dose should be considered that in these patients more likely to decline in kidney function. Children The safety and efficacy of the drug in patients under 18 years of age has not been studied. Concomitant use with potent inhibitorsWhile the use of potent inhibitors , such as ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir, and telithromycin, the recommended dose of the drug dianabol before and after is 2.5 mg 1 time per day. Buy steroids online, steroids for beginners buy steroids online uk!