Ongliza 5mg n30 film-coated tablets
Latin name
Ongliza
Release form
Pills
Package
30 pcs
pharmachologic effect
Onglyza - saxagliptin - is a potent selective reversible competitive inhibitor of dipeptidyl peptidase-4 (DPP-4).
In patients with type 2 diabetes mellitus, taking saxagliptin leads to suppression of the activity of the DPP-4 enzyme within 24 hours. After oral glucose administration, inhibition of DPP-4 leads to a 2-3 fold increase in the concentration of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), a decrease in the concentration of glucagon and an increase in the glucose-dependent response of beta cells, which leads to an increase in the concentration of insulin and C-peptide.
Release of insulin from pancreatic beta cells and decreased release of glucagon from pancreatic alpha cells results in decreased fasting and postprandial glycemia.
The effectiveness and safety of saxagliptin when taken in doses of 2.5 mg, 5 mg and 10 mg once a day were studied in six double-blind, placebo-controlled studies involving 4148 patients with type 2 diabetes mellitus. Taking the drug was accompanied by a statistically significant improvement in glycosylated hemoglobin (HbA1c), fasting plasma glucose (FPG) and postprandial plasma glucose (PPG) compared to the control.
Patients in whom the target glycemic level could not be achieved while taking saxagliptin as monotherapy were additionally prescribed metformin, glibenclamide or thiazolidinediones. When taking saxagliptin at a dose of 5 mg, a decrease in HbA1c was noted after 4 weeks and FPG after 2 weeks. In the group of patients receiving saxagliptin in combination with metformin, glibenclamide or thiazolidinediones, a decrease in HbA1c was also observed after 4 weeks and FPG after 2 weeks.
The effect of saxagliptin on the lipid profile was similar to that of placebo. No weight gain was observed during saxagliptin therapy.
Indications
Type 2 diabetes mellitus in addition to diet and exercise to improve glycemic control as:
— monotherapy;
— initial combination therapy with metformin;
- addition to monotherapy with metformin, thiazolidinediones, sulfonylurea derivatives, in the absence of adequate glycemic control on this therapy.
Contraindications
- type 1 diabetes mellitus (use not studied);
- use in combination with insulin (not studied);
- diabetic ketoacidosis;
- congenital galactose intolerance, lactase deficiency and glucose-galactose malabsorption;
- pregnancy;
- lactation;
- age under 18 years (safety and effectiveness have not been studied);
- increased individual sensitivity to any component of the drug.
Use during pregnancy and breastfeeding
Due to the fact that the use of saxagliptin during pregnancy has not been studied, the drug should not be prescribed during this period.
It is not known whether saxagliptin passes into breast milk. Due to the fact that the possibility of saxagliptin passing into breast milk cannot be excluded, breastfeeding should be stopped during treatment with saxagliptin or therapy should be discontinued, taking into account the balance of risk for the child and benefit for the mother.
special instructions
The use of Ongliza® in combination with insulin, as well as as part of triple therapy with metformin and thiazolidinediones or metformin and sulfonylurea derivatives, has not been studied.
Patients with impaired renal function.
Dose adjustment is recommended for patients with moderate to severe renal impairment, as well as for patients on hemodialysis. Before starting therapy and periodically during treatment with the drug, it is recommended to evaluate renal function.
Use in combination with drugs that can cause hypoglycemia.
Sulfonylureas may cause hypoglycemia; therefore, a reduction in the dose of sulfonylureas may be necessary to reduce the risk of hypoglycemia when used concomitantly with Onglyza.
Hypersensitivity reactions.
The drug should not be prescribed to patients who have had serious hypersensitivity reactions when using other DPP-4 inhibitors.
Elderly patients.
According to clinical studies, efficacy and safety rates in patients aged 65 years and older did not differ from those in younger patients. However, increased individual sensitivity to saxagliptin in some elderly patients cannot be excluded.
Saxagliptin and its main metabolite are partially eliminated by the kidneys, so it must be taken into account that elderly patients are more likely to have decreased renal function. Ongliza® contains lactose. Patients with congenital galactose intolerance, lactase deficiency and glucose-galactose malabsorption should not take this drug.
Influence on the ability to drive vehicles and operate machinery.
No studies have been conducted to study the effect of saxagliptin on the ability to drive vehicles and operate machinery. Please note that saxagliptin may cause dizziness.
Compound
active substance: saxagliptin 5 mg.
excipients: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, hydrochloric acid 1 M or sodium hydroxide solution 1 M, Opadry II white (polyvinyl alcohol, titanium dioxide, macrogol (PEG 3350), talc), Opadry II yellow (alcohol polyvinyl, titanium dioxide, macrogol (PEG 3350), talc, yellow iron oxide dye (E172), Opacode blue ink (shellac in ethyl alcohol, FD&C Blue #2/indigo carmine aluminum pigment (E132), n-butyl alcohol, propylene glycol, isopropyl alcohol, 28% ammonium hydroxide).
Directions for use and doses
The drug is prescribed orally, regardless of food intake.
For monotherapy, the recommended dose of saxagliptin is 5 mg 1 time / day.
In combination therapy, the recommended dose of saxagliptin is 5 mg 1 time / day in combination with metformin, thiazolidinediones or sulfonylurea derivatives.
When starting combination therapy with metformin, the recommended dose of saxagliptin is 5 mg 1 time / day, the initial dose of metformin is 500 mg / day. In case of inadequate response, the dose of metformin may be increased.
If you miss taking Ongliza®, the missed tablet should be taken as soon as the patient remembers, but you should not take a double dose of the drug within one day.
For patients with mild renal failure (creatinine clearance >50 ml/min), no dose adjustment is required. For patients with moderate or severe renal impairment (CR
For mild, moderate and severe liver dysfunction, no dose adjustment is required.
No dose adjustment is required in elderly patients. However, when choosing a dose, it should be taken into account that in this category of patients a decrease in renal function is more likely.
The safety and effectiveness of the drug in patients under 18 years of age have not been studied.
When used concomitantly with strong CYP 3A4/5 inhibitors, such as ketoconazole, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, ritonavir, saquinavir and telithromycin, the recommended dose of Onglyza® is 2.5 mg 1 time / day
Drug interactions
Analysis of data from clinical studies suggests that the risk of clinically significant interactions between saxagliptin and other drugs when used together is low.
The metabolism of saxagliptin is predominantly mediated by the cytochrome P450 3A4/5 isoenzyme system (CYP3A4/5). In vitro studies have shown that saxagliptin and its main metabolite do not inhibit CYP isoenzymes 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 and 3A4 and do not induce CYP isoenzymes 1A2, 2B6, 2C9, and 3A4. In studies involving healthy volunteers, the pharmacokinetic parameters of saxagliptin and its main metabolite were not significantly changed by metformin, glibenclamide, pioglitazone, digoxin, simvastatin, diltiazem, ketoconazole, omeprazole, a combination of aluminum hydroxide, magnesium hydroxide and simethicone, as well as famotidine. Saxagliptin does not significantly change the pharmacokinetic parameters of metformin, glibenclamide, pioglitazone, digoxin, simvastatin, diltiazem or ketoconazole.
The effect of inducers of CYP 3A4/5 isoenzymes on the pharmacokinetics of saxagliptin has not been studied. However, the combined use of saxagliptin and inducers of CYP 3A4/5 isoenzymes, such as carbamazepine, dexamethasone, phenobarbital, phenytoin and rifampicin, may lead to a decrease in the concentration of saxagliptin in plasma and an increase in the concentration of its main metabolite. The effects of smoking, dietary intake, herbal preparations and alcohol consumption on saxagliptin therapy have not been studied.
Overdose
Symptoms of intoxication are not described with long-term use of the drug in doses up to 80 times higher than recommended.
Treatment: in case of overdose, symptomatic therapy should be used. Saxagliptin and its main metabolite are eliminated from the body by hemodialysis (removal rate: 23% of the dose in 4 hours).
Storage conditions
At a temperature not exceeding 30°C
Best before date
3 years
Conditions for dispensing from pharmacies
On prescription
How I learned to manage type II diabetes
I found out that I have diabetes by accident when I was undergoing a medical examination at work. I had no complaints, I felt completely healthy. A blood test revealed an increase in blood sugar - 6.8 mmol/l. I was referred to an endocrinologist. The doctor said that this is higher than normal (normal is less than 6.1 mmol/l) and an additional examination needs to be done: a sugar load test. They measured my fasting sugar (it was again higher than normal - 6.9 mmol/l) and gave me a glass of a very sweet liquid to drink - glucose. When measuring blood sugar after 2 hours, it was also higher than normal - 14.0 mmol/l (should be no more than 7.8 mmol/l). I also took a blood test for glycated hemoglobin (shows the “average” sugar level for 3 months). It was also high - 7% (and no more than 6% is allowed).
And that’s when I heard from the doctor: “You have type 2 diabetes.” It was a shock for me. Yes, I've heard about diabetes before, but it might be someone else's problem, just not mine. At that time, I was 55 years old, I held a leadership position, worked a lot, felt good and had never been seriously ill. And in general, to be honest, I didn’t go to the doctors. At first I took the diagnosis as a death sentence, because diabetes cannot be cured. I remembered everything I had heard about complications - that something terrible was happening to the kidneys and eyes, ulcers appeared on the legs and legs were amputated, that a person with diabetes would definitely be disabled. But I couldn't let that happen! I have a family, children, and a granddaughter will be born soon! I then asked my endocrinologist only one question: “what should I do?” And the doctor answered me: “You and I will learn to manage the disease. If you keep diabetes under control, complications can be avoided.” And on a piece of paper I drew this diagram:
We started with training: you can’t manage what you don’t know.
I chose the form of individual classes (there are also group classes - “diabetes” schools). We studied for 5 days for 1 hour. And even this seemed not enough to me; in addition, at home I read the literature given to me by the doctor. During the classes I learned about what diabetes is, why it occurs, what processes occur in the body. The information was in the form of presentations, everything was extremely accessible and even interesting. Then, I learned to measure blood sugar using a glucometer (it’s not at all difficult and doesn’t hurt), and keep a self-monitoring diary. The most important thing is that I really understood why this was needed, first of all, for myself. After all, I didn’t know that my sugar was high because I didn’t feel anything. The doctor told me that I was lucky that diabetes was detected at an early stage, when my blood sugar was not yet very high. But dry mouth, thirst, frequent urination, weight loss appear when blood sugar is significantly elevated. The most dangerous thing about this is that a person does not know about his illness, does not receive treatment, but destruction occurs in the body and the risk of developing complications is higher, the later the diagnosis is made. This is why it is so important to get tested regularly: if you are over 45 years old, your blood sugar needs to be checked every 3 years. But even if you are under 45 years old, but you are overweight, have low physical activity, one of your relatives had diabetes, you had “borderline” increases in blood sugar levels, hypertension, high cholesterol levels - you also need to take regular blood tests. blood for sugar.
During the classes, I learned one very important concept: “target blood sugar level.” It is different for everyone, depending on age and the presence of other diseases. That is, if you have diabetes, there is no point in striving for the norm, but you need to stay within “your limits” of sugar on an empty stomach, 2 hours after meals and the level of glycated hemoglobin. The target for me was less than 7 mmol/L, less than 9 mmol/L and less than 7%, respectively. In this case, the risk of complications should be minimal. I was recommended to measure my blood sugar once a day at different times and once a week - several measurements, and record all the indicators in a diary. I donate glycated hemoglobin every 3 months. All this is necessary for the doctor to assess the situation and timely change treatment if necessary.
Next, we had a session on lifestyle changes, nutrition and the importance of exercise in managing diabetes. I admit, this is, of course, the most difficult of all. I have always been used to eating what I want, when I want and how much I want. Physical activity: from the 4th floor by elevator, two steps to the car, by car to work, at work in a chair for 8-10 hours, by car home, by elevator to the 4th floor, sofa, TV, that’s all the activity. As a result, by the age of 40 I became a “moderately well-fed man” with a standard “beer” belly. When calculating my body mass index, I heard another unpleasant verdict: “grade 1 obesity.” Moreover, the location of fat on the stomach is the most dangerous. And something had to be done about this. In class, I learned that food is not just “food is tasty and food is tasteless,” but it consists of components, each of which plays a specific role. The most important carbohydrates for controlling diabetes are carbohydrates, which increase blood sugar. There are carbohydrates that quickly increase it - “simple” ones: sugar, honey, juices. They need to be practically eliminated (instead of sugar, I started using stevia, a natural sweetener). There are carbohydrates that slowly increase sugar - “complex”: bread, cereals, potatoes. You can eat them, but in small portions. Also, foods containing a lot of fat (fatty meat, fatty cheeses, mayonnaise, oils, sausages, fast food) were also banned. Fat does not increase sugar, but it does increase the calorie content of food. In addition, during the examination, I was found to have an elevated level of cholesterol, which comes from animal fats. Cholesterol can be deposited inside the vessels and close them, which ultimately leads to heart attack, stroke, and damage to the blood vessels of the legs. In diabetes mellitus, atherosclerosis develops especially quickly, so cholesterol levels should also be “target” (lower than in people without diabetes!).
What can you eat?
Well, of course, these are various vegetables, herbs, lean meat, fish and dairy products. And most importantly, it was a reduction in portion sizes. After all, the pancreas, which produces insulin to lower blood sugar after meals, cannot cope with large amounts of carbohydrates. Therefore, I was recommended to eat often and in small portions. I also had to give up alcohol, especially beer and everything that goes with it. Alcohol, it turns out, contains a lot of calories, plus it increases appetite.
At first, all this seemed impossible to me, and I would not be able to enjoy food with all these prohibitions. However, this turned out to be completely wrong. My doctor compiled an individual diet for me, taking into account my food preferences (from allowed foods, of course) and I brought it home to my wife. My wife organized the technical side of nutrition, for which I thank her very much. All forbidden foods disappeared from the house, and she herself began to eat the same way, so that I would not be tempted to eat something wrong. And you know, proper nutrition can be tasty and you can enjoy it! Everything harmful can be replaced with something useful. Even alcohol - instead of beer or strong drinks, I now choose dry red wine, 1 glass with dinner. I got even more satisfaction when I stepped on the scale after 6 months and saw that I had lost 5 kg! Of course, this was achieved not only by changing the diet. We bought a membership to a fitness club and started going to classes together. Before starting the exercises, we were examined by a sports doctor to exclude diseases in which a sharp increase in physical activity could lead to deterioration. We worked out with a trainer, according to an individual program, because if an untrained person comes to the gym and starts doing exercises on his own, this is not always effective and can even be dangerous to health. In addition, as the doctor explained to me, exercise can lead to hypoglycemia, especially if a person is taking certain glucose-lowering medications. We also discussed how to avoid hypoglycemia (an excessive decrease in blood sugar, a very dangerous condition), why it occurs, and how to deal with it.
At first it’s difficult to find time, after work you get tired, you want to go home and relax, but a goal is a goal. After all, in addition to weight loss, physical exercise lowers blood sugar (I also learned about this in class - muscles use sugar to work, and the more movements, the better the sugar).
At first we went only on weekends, once a week, then we started going more often, and what’s most surprising is that we found time. They say correctly “if only there was a desire.” And exercise really improves your mood and relieves stress after work much more effectively than relaxing at home in front of the TV. In addition, I gave up the elevator both at home and at work, it seems like a small thing, but it’s also a work for the muscles.
So, by organizing my nutrition and adding sports to my life, I managed to reduce my weight by 5 kg and so far I have managed to maintain the achieved result.
What about drugs to lower blood sugar?
Yes, almost immediately (after receiving test results that everything was fine with my liver and kidneys) I was prescribed a drug - metformin, and I still take it, twice a day, morning and evening with meals. As my doctor explained to me, this drug helps the cells of my body sense their insulin better and thereby keep my sugar levels within the chosen goal. Is it possible to do without drugs? In some cases, yes, by following only a diet and leading an active lifestyle. But this happens quite rarely; more often, metformin is prescribed immediately after diagnosis. We also had a class on different medications to lower blood sugar. There are many of them, and they all act differently. Only your doctor should decide which drug to prescribe for you, based on your sugar levels and glycated hemoglobin. What helped your neighbor or was said on television will not always benefit you and may cause harm. We also had a conversation about insulin. Yes, insulin is used for type 2 diabetes, but only in cases where the combination of several tablets in maximum doses no longer helps, that is, in a situation where the pancreas has exhausted its reserves and can no longer produce insulin. Each person has an individual “reserve”, but still, in order not to “strain” the gland, it is necessary to follow the rules of nutrition first of all, because the more carbohydrates we eat at the same time, the more insulin is needed to transport sugar into the cells, and the more intensely the pancreas has to work. There are still some cases when insulin is needed: for example, if the diagnosis is made when the sugar level is very high, when the pills will not help, and insulin is temporarily prescribed. A temporary switch to insulin is also required when planning operations under anesthesia. But even if it becomes necessary to switch to insulin someday, in order to keep my diabetes “under control,” I am ready for this. Yes, this will be a new task, you will have to learn new things, experience a little discomfort from daily injections, count the amount of carbohydrates and insulin doses, but all this is not so important if it helps to avoid serious complications and loss of health.
Did the doctor tell me during our classes about the complications of diabetes? Yes, and quite detailed and openly, not in vague terms “something bad with the kidneys, eyes, blood vessels,” but specifically what happens in the body in various organs with constantly elevated sugar levels. The kidneys, the organs where the blood is cleansed of toxins, are especially insidious in this regard. When they are affected, there are no sensations to suspect that something is wrong, until the stage when these changes are irreversible and the kidneys completely stop working. In such cases, people need blood purification with a special device - dialysis in a special institution several times a week. How can you find out that something is happening to your kidneys? It is necessary to regularly donate blood for creatinine, based on the level of which the doctor will be able to assess the effectiveness of the kidneys in cleansing the blood of toxins. If there are no changes, this is carried out every year. The higher the creatinine level, the worse the kidneys work. Changes can also be seen in urine tests - in a general (regular) urine test there should be no protein, and in a special test for microalbumin - it should not be above a certain level. I take these tests every 6 months, and so far everything is normal.
To prevent damage to the kidneys, it is necessary to have normal blood pressure (about 130/80 mm Hg). As it turned out, my blood pressure was high, and I didn’t know about this either, because I had never measured it. The cardiologist gave me medications to lower my blood pressure. Since then, I have been taking them constantly, and my blood pressure is as it should be. I visit a cardiologist once a year to assess the effectiveness of treatment, conduct an ECG, and bring a self-monitoring diary. During the time that I was observed, I also had an ultrasound of the heart and an ultrasound of the vessels of the neck - so far no abnormalities have been identified. Another organ that can be affected by diabetes is the eyes, or more precisely the vessels of the retina. There will be no sensations here either, and there is no need to focus on how you see good or bad. These changes can only be seen by an ophthalmologist when examining the fundus of the eye. But a person can “feel” on his own only a sharp deterioration in vision, up to absolute loss, which occurs due to retinal detachment. This condition is treated by laser coagulation of the retina - “soldering” it to the eye. However, in advanced stages, this may not be possible, which is why it is so important that an ophthalmologist sees you at least once a year or more often if there are changes, in order to prescribe treatment in a timely manner and save your vision.
The most terrible complication for me seems to be amputation of legs due to the development of gangrene. My doctor told me why this might happen. With constantly elevated sugar levels, the nerves in the legs are slowly but surely affected. At first, unpleasant sensations, burning, and “goosebumps” may appear in the feet, which a person often does not pay attention to. Over time, sensitivity decreases and may disappear completely. A person can step on a nail, stand on a hot surface, rub a callus and not feel anything and walk for a long time with a wound until he sees it. And wound healing in diabetes mellitus is significantly reduced, and even a small wound or abrasion can turn into an ulcer. All this can be avoided if you follow simple foot care rules and, of course, maintain your target blood sugar level. In addition to self-monitoring of the legs, it is necessary for a doctor (endocrinologist or neurologist) to assess sensitivity with special instruments at least once a year. To improve the condition of the nerves, droppers with vitamins and antioxidants are sometimes prescribed.
In addition to the affected nerves, vascular atherosclerosis (deposition of cholesterol plaques), which leads to a decrease in blood flow to the legs, plays an important role in the development of foot ulcers. Sometimes, the lumen of the vessel can close completely, and this will lead to gangrene, in which amputation becomes the only way out. This process can be detected in time by performing an ultrasound scan of the arteries of the legs. In some cases, special operations are performed on the vessels - dilating the vessels with a balloon and installing stents in them - meshes that prevent the lumen from closing again. A timely operation can save you from amputation. In order to reduce the risk of developing atherosclerosis (and the same process is the cause of stroke and heart attack: blockage of blood vessels also occurs, but only those feeding the brain and heart), it is necessary to maintain the “target” level of cholesterol and its “good” and “bad” fractions. To do this, of course, you need to follow a diet, but I was not able to achieve results with this alone, and the cardiologist selected me a drug that controls cholesterol levels. I take it regularly and have my lipid profile tested every six months.
What should I say in conclusion? Yes, I have diabetes. I've been living with him for 5 years. But I have it under control! I hope my example will help those who also encountered this problem. The most important thing is not to despair, not to give up, otherwise it will not be you, but diabetes that will control you, your life, and determine what your future will be like. And, of course, you don’t need to be left alone with the disease, look for treatment methods on the Internet, ask your friends... Seek help from specialists who know their stuff, and they will definitely help you, teach you how to keep diabetes under control, as they taught me.
