Despite the huge selection of glucose-lowering drugs, the ideal means for glycemic control has not yet been found. Vildagliptin is one of the most advanced antidiabetic drugs. It not only has a minimum of side effects: does not cause weight gain and hypoglycemia, does not impair the function of the heart, liver and kidneys, but also prolongs the ability of beta cells to produce insulin.
Vildagliptin is a means of increasing the lifespan of incretins - natural hormones of the gastrointestinal tract. According to doctors, this substance can be successfully used in case of long-term diabetes mellitus, and in the initial stages of the disease, including in the composition of the combined treatment.
How vildagliptin was discovered
The first information about incretins appeared more than 100 years ago, back in 1902. Substances were isolated from intestinal mucus and called secretins. Then their ability to stimulate the secretion from the pancreas of enzymes necessary for the digestion of food was discovered. A few years later there were suggestions that the secretins can affect the hormonal activity of the gland. It was found that in patients with glucosuria when taking a precursor of incretins, the amount of sugar in the urine significantly decreases, urine volume decreases, and well-being improves.
In 1932, the hormone got its current name - the glucose-dependent insulinotropic polypeptide (HIP). It was found that it is synthesized in the cells of the mucous membrane of the duodenum 12 and jejunum. By 1983, 2 glucagon-like peptides (GLP) had been isolated. It turned out that GLP-1 causes insulin secretion in response to glucose intake, and its secretion is reduced in diabetics.
Diabetes and pressure surges will be a thing of the past.
- Sugar normalization -95%
- Elimination of vein thrombosis - 70%
- Elimination of palpitations -90%
- Excessive Blood Pressure - 92%
- Increased vigor during the day, improved sleep at night -97%
- stimulates insulin release in patients with diabetes mellitus;
- prolongs the presence of food in the stomach;
- reduces the need for food, promotes weight loss;
- has a positive effect on the heart and blood vessels;
- reduces the production of glucagon in the pancreas, a hormone that weakens the action of insulin.
Splits incretin the enzyme DPP-4, which is present on the endothelium of capillaries, penetrating the intestinal mucosa, for this it is enough for 2 minutes.
The clinical use of these discoveries in 1995 began to explore the pharmaceutical company Novartis. Scientists were able to isolate substances that impede the work of the enzyme DPP-4, because of which the lifespan of GLP-1 and HIP increased several times, and insulin synthesis also grew at the same time. Vildagliptin was the first chemically stable substance with such a mechanism of action that passed safety testing. This name has absorbed a lot of information: here there is a new class of hypoglycemic substances "gliptin" and part of the name of its creator Willhauer, and an indication of the ability of the drug to reduce glycemia "gly" and even the abbreviation "yes", or dipeptidyl-peptidase, the same enzyme DPP -four.
The beginning of the era of incretins in the treatment of diabetes mellitus is officially considered to be the year 2000, when at the congress of endocrinologists for the first time the possibilities of inhibiting DPP-4 were demonstrated. In a short period of time, vildagliptin has taken a strong position in the standards of diabetes therapy in many countries around the world. In Russia, the substance was registered in 2008. Now vildagliptin is annually included in the list of essential medicines.
This rapid success is due to the unique properties of vildagliptin, which were confirmed by more than 130 international studies.
With diabetes, the drug allows you to:
- Improve glycemic control. Vildagliptin at a daily dose of 50 mg helps to reduce sugar after a meal by an average of 0.9 mmol / l. Glycated hemoglobin is reduced by an average of 1%.
- Make the glucose curve smoother by eliminating peaks. The maximum postprandial glycemia is reduced by about 0.6 mmol / l.
- Reliably reduce daytime and nighttime blood pressure in the first six months of treatment.
- Improve lipid metabolism mainly due to a decrease in the concentration of low-density lipoprotein. Scientists consider this effect to be additional, not related to improving the compensation of diabetes.
- To reduce the weight and waist size in patients with obesity.
- Vildagliptin is well tolerated and highly safe. Episodes of hypoglycemia when it is used are extremely rare: the risk is 14 times lower than when taking traditional sulfonylurea derivatives.
- The drug is well combined with metformin. In patients taking metformin, the addition to the treatment of 50 mg of vildagliptin makes it possible to further reduce HG by 0.7%, 100 mg - by 1.1%.
According to the instructions, the action of Galvus, the trade name of vildagliptin, directly depends on the viability of the pancreatic beta cells and the level of glucose. In the first type of diabetes and in type 2 diabetics, vildagliptin is powerless with a large percentage of damaged beta cells. In healthy people and in diabetics with normal glucose, it will not cause a hypoglycemic state.
Currently, vildagliptin and its analogues are considered drugs 2 lines after metformin. They can successfully replace the most common now sulfonylurea derivatives, which also enhance insulin synthesis, but are much less safe.
Pharmacokinetics of the drug
Pharmacokinetic parameters of vildagliptin from the instructions for use:
|The time required to reach the peak of blood concentration, min.||fasting||105|
|Ways of elimination from the body,% vildagliptin and its metabolites||kidneys||85, including 23% unchanged|
|The change in sugar-lowering effect in liver failure,%||mild degree||-20|
|Change in action in violation of renal function,%||Increases by 8-66%, does not depend on the degree of violations.|
|Pharmacokinetics in elderly diabetics||Vildagliptin concentration increases to 32%, the effect of the drug does not change.|
|The effect of food on the absorption and effectiveness of tablets||missing|
|Effect of weight, gender, race on drug efficacy||missing|
|Half-life, min.||180, does not depend on food|
All rights to vildagliptin are rightfully owned by Novartis, which invested a lot of manpower and resources in the development and launch of the drug on the market. Tablets are produced in Switzerland, Spain, Germany. The launch of the line in Russia in the Novartis Neva branch is expected soon. The pharmaceutical substance, that is, vildagliptin itself, is of Swiss origin only.
Vildagliptin contains 2 Novartis preparations: Galvus and Galvus Met. The active substance of Galvus is only vildagliptin. Tablets have a single dosage of 50 mg.
Galvus Met is a combination of metformin and vildagliptin in a single pill. Available dosage options: 50/500 (mg of sildagliptin / mg of metformin), 50/850, 50/100. This choice allows you to take into account the peculiarities of diabetes in a particular patient and precisely select the right dose of medication.
According to reviews of diabetics, taking Galvus and metformin in separate tablets is cheaper: the price of Galvus is about 750 rubles, metformin (Glucophage) is 120 rubles, Galvus Meta is about 1600 rubles. However, the combination treatment with Galvus Met has been found to be more effective and convenient.
There are no analogs in Russia containing vildagliptin in Galvus, since a proactive prohibition acts on the substance. Currently, not only the production of any drugs with vildagliptin is prohibited, but also the development of the substance itself. This measure allows the manufacturer to recoup the costs of numerous studies required to register any new medicine.
Indications for admission
Vildagliptin is indicated only for type 2 diabetes. According to the instructions, tablets can be administered:
- In addition to metformin, if its optimal dose is not enough to control diabetes.
- To replace sulfonylurea drugs (PSM) in diabetics who have an increased risk of hypoglycemia. The reason may be old age, especially diet, sports and other physical activities, neuropathy, impaired function of the liver and digestive processes.
- Diabetics with allergies to the group of PSM.
- Instead of sulfonylurea, if the patient seeks to delay the start of insulin therapy as much as possible.
- As monotherapy (only vildagliptin), if metformin is contraindicated or impossible due to pronounced side effects.
Acceptance of vildagliptin must be combined with a diabetic diet and exercise. High insulin resistance due to low loads and uncontrolled carbohydrate intake can become an insurmountable obstacle to achieving compensation for diabetes. The instruction allows to combine vildagliptin with metformin, PSM, glitazones, insulin.
The recommended dosage of the drug is 50 or 100 mg. It depends on the severity of diabetes. The drug mainly affects postprandial glycemia, so a 50 mg dose is advisable to drink in the morning. 100 mg divided equally into the morning and evening receptions.
Frequency of unwanted actions
The main advantage of vildagliptin - low frequency of side effects in its application. The main problem in diabetics using PSM and insulin is hypoglycemia. Despite the fact that more often they pass in a mild form, sugar drops are dangerous for the nervous system, therefore, they are tried to be avoided to the maximum. Instructions for use informs that the risk of hypoglycemia when taking vildagliptin is 0.3-0.5%. For comparison, in the non-drug control group this risk is estimated at 0.2%.
The high safety of vildagliptin is evidenced by the fact that during the study no diabetic required the drug to be discontinued due to its side effects, as evidenced by the same number of refusals of treatment in groups receiving vildagliptin and placebo.
Less than 10% of patients complained of light vertigo, less than 1% had constipation, headache, swelling of the extremities. It was found that long-term use of vildagliptin does not lead to an increase in the frequency of its side effects.
According to the instructions, contraindications to taking the drug are only hypersensitivity to vildagliptin, child age, pregnancy and lactation. Galvus contain lactose as an auxiliary component, therefore, when it is intolerable, these tablets are prohibited. Galvus Met is allowed here, since there is no lactose in its composition.
Possible consequences of vildagliptin overdose according to the instructions:
|Dosage mg / day||Violations|
|up to 200||It is well tolerated, no symptoms. The risk of hypoglycemia does not increase.|
|400||Muscle pain Rarely - a burning sensation or tingling on the skin, fever, peripheral edema.|
|600||In addition to the above disorders, changes in the composition of the blood are possible: growth of creatine kinase, C-reactive protein, AlAT, myoglobin. Laboratory indicators gradually normalized after discontinuation of the drug.|
|more than 600||Impact on the body has not been studied.|
In case of overdose, GI purification and symptomatic treatment are necessary. Vildagliptin metabolites are excreted by hemodialysis.
Note: an overdose of metformin, one of the components of Galvus Meta, increases the risk of lactic acidosis, one of the most dangerous complications of diabetes.
After vildagliptin, several more substances were discovered that could inhibit DPP-4. All of them are analogues:
- Saksagliptin, trade name Angliz, manufacturer Astra Zeneka. The combination of saxagliptin and metformin is called Kombogliz;
- Sitagliptin is contained in the preparations of Januvia from Merck, Xelevia from Berlin-Chemie. Sitagliptin with metformin - active ingredients of two-component tablets Janumet, analogue Galvus Meta;
- Linagliptin has the trade name Trazhent. The medicine is the brainchild of the German company Beringer Ingelheim. Linagliptin plus metformin in one pill is called Gentadueto;
- Aogliptin is an active component of Vipidia tablets, which Takeda Pharmaceuticals produces in the USA and Japan. The combination of alogliptin and metformin is produced under the brand name Vipdomet;
- Gozogliptin is the only domestic analogue of vildagliptin. It plans to release LLC Satreks. The full production cycle, including pharmacological substance, will be carried out in the Moscow region. According to the results of clinical trials, the safety and effectiveness of gozogliptin was close to vildagliptin.
In pharmacies in Russia, it is currently possible to purchase Onglizu (the price for a monthly course is about 1,800 rubles), Kombogliz (from 3,200 rubles), Yanuviya (1,500 rubles), Xselevia (1,500 rubles), Yanumet (from 1800), Trazentu ( 1700 rub.), Vipidia (from 900 rub.). By the number of reviews, it can be argued that the most popular of Galvus analogues is Januvia.
Doctors reviews about vildagliptin
Doctors appreciate vildagliptin. They call the advantages of this medicine the physiological nature of its action, good tolerability, persistent hypoglycemic effect, low risk of hypoglycemia, additional benefits in the form of suppressing the development of microangiopathy and improving the condition of the walls of large vessels.
Vildagliptin, indeed, significantly increases the price of treatment, but in some cases (frequent hypoglycemia) there is no worthy alternative to it. The effect of the drug is considered to be equal to metformin and PSM, with the passage of time, the carbohydrate metabolism indicators slightly improve.
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