Onglisa
Ongliza: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Onglyza
ATX code: A10BH03
Active ingredient: Saxagliptin (Saxagliptin)
Producer: Bristol-Myers Squibb Company (USA), AstraZeneca Pharmaceutical LP (USA), Bristol-Myers Squibb SrL (Italy)
Description and photo update: 2018-24-10
Prices in pharmacies: from 1666 rubles.
Buy
Onglisa is a drug with hypoglycemic action.
Release form and composition
Dosage form of release Ongliza - tablets, film-coated: round, biconvex, the inscriptions are applied with blue dye; 2.5 mg each - from light to pale yellow color, on one side the inscription "2.5", on the other - "4214"; 5 mg - pink, on one side the inscription "5", on the other - "4215" (10 pcs. in blisters, in a cardboard box 3 blisters).
Composition of 1 tablet:
- active substance: saxagliptin (in the form of saxagliptin hydrochloride) - 2.5 or 5 mg;
- auxiliary components: lactose monohydrate - 99 mg; microcrystalline cellulose - 90 mg; croscarmellose sodium - 10 mg; magnesium stearate - 1 mg; 1M hydrochloric acid solution - in sufficient quantity;
- shell: Opadry II white (polyvinyl alcohol - 40%; titanium dioxide - 25%; macrogol - 20.2%; talc - 14.8%) - 26 mg; Opadry II yellow (for 2.5 mg tablets) [polyvinyl alcohol - 40%; titanium dioxide - 24.25%; macrogol - 20.2%; talc - 14.8%; dye iron oxide yellow (E172) - 0.75%] - 7 mg; Opadry II pink (for 5 mg tablets) [polyvinyl alcohol - 40%; titanium dioxide - 24.25%; macrogol - 20.2%; talc - 14.8%; iron dye oxide red (E172) - 0.75%] - 7 mg;
- ink: Opacode blue - (45% shellac in ethyl alcohol - 55.4%; FD&C Blue # 2 / indigo carmine aluminum pigment - 16%; n-butyl alcohol - 15%; propylene glycol - 10.5%; isopropyl alcohol - 3%; 28% ammonium hydroxide - 0.1%) - in sufficient quantity.
Pharmacological properties
Pharmacodynamics
Saxagliptin is a potent selective reversible competitive inhibitor of dipeptidyl peptidase-4 (DPP-4). In type 2 diabetes mellitus, its intake leads to the suppression of the activity of the DPP-4 enzyme for 24 hours. After ingestion of glucose, inhibition of DPP-4 leads to a 2-3-fold increase in the concentration of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1), an increase in the glucose-dependent response of beta cells and a decrease in the concentration of glucagon, which is the cause of an increase in the concentration C-peptide and insulin.
A decrease in the release of glucagon from pancreatic alpha cells and the release of insulin by beta cells of the pancreas leads to a decrease in postprandial and fasting glycemia.
As a result of placebo-controlled studies, it was found that taking Onglisa proceeds with a statistically significant improvement in fasting blood plasma glucose (FPG), glycosylated hemoglobin (HbA 1c) and postprandial glucose (PPG) in blood plasma in comparison with control.
Patients who failed to achieve the target glycemic level while taking saxagliptin as monotherapy are additionally prescribed metformin, thiazolidinediones or glibenclamide. When taking 5 mg of saxagliptin, a decrease in HbA 1c was noted after 4 weeks, HPN - after 2 weeks. Patients who received saxagliptin in combination with metformin, thiazolidinediones, or glibenclamide experienced a similar decrease in performance.
While taking Onglisa, there is no increase in body weight. The effect of saxagliptin on lipid profile is similar to that of placebo.
Pharmacokinetics
In healthy volunteers and in patients with type 2 diabetes mellitus, similar parameters of the pharmacokinetics of saxagliptin and its main metabolite are noted.
The substance is rapidly absorbed after oral administration on an empty stomach. Achievement of C max (maximum concentration of a substance) of saxagliptin and the main metabolite in plasma occurs within 2 hours and 4 hours, respectively. With increasing dose, there is a proportional increase in C max and AUC (area under the concentration-time curve) of both the substance and its main metabolite. After a single dose of 5 mg of saxagliptin in healthy volunteers, the mean values of C max of saxagliptin and its main metabolite in plasma were 24 ng / ml and 47 ng / ml, the AUC values were 78 ng × h / ml and 214 ng × h / ml, respectively.
The average duration of the final T 1/2 (half-life) of saxagliptin and its main metabolite is 2.5 hours and 3.1 hours, respectively, the average value of the plasma DPP-4 inhibition T 1/2 is 26.9 hours. 4 in plasma for at least 24 hours after taking saxagliptin is associated with its high affinity for DPP-4 and long-term binding to it. A noticeable cumulation of the substance and its main metabolite during a long course with a frequency of 1 time per day is not observed. The dependence of the clearance of saxagliptin and its main metabolite on the daily dose and duration of therapy when taking the drug once a day in the dose range of 2.5-400 mg for 14 days was not revealed.
After oral administration, at least 75% of the dose taken is absorbed. Food intake does not significantly affect the pharmacokinetics of saxagliptin. Foods with a high fat content have no effect on the C max of the substance, however, AUC values increase by 27% in comparison with fasting. When taking the drug with food, in comparison with taking on an empty stomach, the time to reach C max increases by about 30 minutes. These changes have no clinical significance.
Saxagliptin and its main metabolite bind only slightly to serum proteins. In this regard, it can be assumed that with changes in the protein composition of the blood serum, observed in renal or hepatic failure, the distribution of saxagliptin will not undergo significant changes.
The substance is metabolized mainly with the participation of cytochrome P450 isoenzymes 3A4 / 5 (CYP 3A4 / 5). In this case, the main active metabolite is formed, the inhibitory effect of which in relation to DPP-4 is 2 times weaker than that of saxagliptin.
Saxagliptin is excreted in bile and urine. The average renal clearance of the substance is approximately 230 ml / min, the average value of glomerular filtration is approximately 120 ml / min. Renal clearance for the major metabolite is comparable to the mean glomerular filtration rate.
The AUC value of saxagliptin and its main metabolite in mild renal failure is 1.2 and 1.7 times higher, respectively, than in patients with intact renal function. This increase in AUC values is not clinically significant, and dose adjustments should not be made.
In moderate / severe renal failure, as well as in patients on hemodialysis, the AUC values of the substance and its main metabolite are 2.1 and 4.5 times higher, respectively. In this regard, the daily dose for this group of patients should not exceed 2.5 mg per dose. With impaired hepatic function, clinically significant changes in the parameters of the pharmacokinetics of Saxagliptin were not identified and, accordingly, there is no need for dose adjustment.
Clinically significant differences in the parameters of the pharmacokinetics of Saxagliptin in patients aged 65–80 years compared with younger patients were not identified. Despite the fact that dose adjustment is not required in this group of patients, it is necessary to take into account the high probability of decreased renal function.
Indications for use
Onglisa is prescribed for the treatment of type 2 diabetes as an adjunct to exercise and diet to improve glycemic control.
The drug can be administered as follows:
- monotherapy;
- starting combination therapy with metformin;
- addition to monotherapy with thiazolidinediones, metformin, sulfonylurea derivatives in cases of lack of adequate glycemic control during such treatment.
Contraindications
Absolute:
- type 1 diabetes mellitus;
- diabetic ketoacidosis;
- congenital galactose intolerance, impaired absorption of galactose and glucose and lactase deficiency;
- combined use with insulin;
- pregnancy and lactation;
- age up to 18 years;
- individual intolerance to any of the components of the drug.
Relative (Ongliza is prescribed under medical supervision):
- moderate / severe renal impairment;
- combined use with sulfonylurea derivatives;
- elderly age.
Instructions for use of Ongliza: method and dosage
Ongliza is taken orally, regardless of the meal.
The recommended dose is 5 mg in 1 dose.
When carrying out combination therapy, Onglisa is used with metformin, sulfonylurea derivatives or thiazolidinediones.
When starting combination therapy with metformin, its initial daily dose is 500 mg. In cases of an inadequate response, it can be increased.
If a dose of Ongliza has been missed, it should be taken as soon as possible, but a double dose should not be taken within 24 hours.
The daily dose for patients with moderate / severe renal failure (with creatinine clearance ≤ 50 ml / min), as well as for patients on hemodialysis, is 2.5 mg in 1 dose. Onglisa should be taken after the end of the hemodialysis session. The use of the drug in patients on peritoneal dialysis has not been studied. It is recommended to assess renal function before / during therapy.
The recommended daily dose of Onglyza in combination with indinavir, nefazodone, ketoconazole, atazanavir, ritonavir, clarithromycin, itraconazole, nelfinavir, saquinavir, telithromycin and other powerful inhibitors of CYP 3A4 / 5 is 2.5 mg in 1 dose.
Side effects
Possible adverse reactions during monotherapy and the addition of Onglisa to therapy with metformin, glibenclamide or thiazolidinedione (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01 % - rarely):
- nervous system: often - headache;
- digestive system: often - vomiting;
- infections and invasions: often - urinary and upper respiratory tract infections, sinusitis, gastroenteritis.
Hypersensitivity reactions were noted in 1.5% of cases. They were assessed as not posing a threat to life and did not require hospitalization.
In a study of the combined use of Onglisa with thiazolidinediones, the development of peripheral edema was observed. They were mild or moderate and did not require discontinuation of therapy. Cases of headache and nasopharyngitis have been reported frequently with initial combination therapy with metformin.
During the post-registration study, the following disorders were recorded: hypersensitivity reactions (including anaphylaxis, angioedema, urticaria and rash) and acute pancreatitis.
Overdose
Symptoms of intoxication with prolonged use of Ongliza in doses up to 80 times higher than recommended have not been described.
In cases of overdose, symptomatic therapy is indicated. Saxagliptin and its main metabolite can be removed from the body by hemodialysis (elimination rate: 23% of the dose in 4 hours).
special instructions
Combined use with insulin, as well as taking Onglisa as part of triple therapy (metformin and thiazolidinediones or metformin and sulfonylurea derivatives) have not been studied.
Before starting treatment / periodically during therapy in patients with functional impairment of the kidneys, it is recommended to assess renal function.
Since sulfonylurea derivatives can lead to the development of hypoglycemia, when combined with Onglisa, in order to reduce the risk of developing this disorder, it is recommended to reduce the dose of sulfonylurea derivatives.
Ongliza should not be prescribed to patients with a history of serious hypersensitivity reactions when using other DPP-4 inhibitors.
Influence on the ability to drive vehicles and complex mechanisms
When driving vehicles, patients should take into account that taking Onglisa can lead to the development of dizziness.
Application during pregnancy and lactation
According to the instructions, Ongliza is not prescribed to pregnant and lactating women, since the effect of the drug on the woman's body and the fetus / child has not been studied.
Pediatric use
For patients under the age of 18, the drug is not prescribed (the effect of Onglisa in this group of patients has not been studied).
With impaired renal function
In moderate / severe renal failure (creatinine clearance <50 ml / min), as well as in patients on hemodialysis, Onglisa is prescribed with caution in a reduced dose.
Use in the elderly
Therapy in elderly patients requires caution, which is associated with an increased risk of impaired renal function.
Drug interactions
As a result of the analysis of data from clinical trials, it can be assumed that the risk of clinically significant interactions of Ongliza with other drugs / substances in their combined use is negligible.
Rifampicin, carbamazepine, phenobarbital, dexamethasone, phenytoin and other inducers of CYP 3A4 / 5 isoenzymes reduce the plasma concentration of saxagliptin and increase the concentration of its main metabolite.
Analogs
Ongliza's analogues are: Trajenta, Nesina, Galvus, Januvia, Komboglyza XR.
Terms and conditions of storage
Store out of the reach of children at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Onglize
According to reviews, Onglisa is an effective drug that allows you to effectively control glucose levels in type 2 diabetes. A convenient dosing regimen and a rare development of adverse reactions are noted. The result of therapy should be assessed no earlier than after 2-4 weeks of admission. The disadvantages usually indicate the high cost of the drug.
Price for Onglisa in pharmacies
The approximate price for Ongliza (in a package of 30 tablets, 5 mg each) is 1,752-2039 rubles.
Onglisa: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Onglisa 5 mg film-coated tablets 30 pcs. 1666 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
