Oral hypoglycemic drugs: list, the principle of their action
Jul 05, 2018
Treatment of type 1 and type 2 diabetes has significant differences.In type 2 diabetes, the function of insulin synthesis is preserved, but it is produced in a reduced amount.In this case, tissue cells become less susceptible to the hormone.Correct these disorders successfully can oral hypoglycemic drugs.Contents: Types of oral hypoglycemic drugs biguanide derivatives Sulfonylureas Inhibitors of alpha-glucosidase derivatives thiazolidinedione derivatives glinides Incretins derivatives inhibitors SGLT2
Types of oral hypoglycemic drugs
hypoglycemic drugs discharged much, they differ in their origin and chemicalFormula. There are such groups of oral hypoglycemic agents:
- derivatives of sulfonylureas;
- α-glucosidase inhibitors;
In addition, a new group of hypoglycemic drugs has recently been synthesized: derivatives of inhibitors of sodium-glucose cotransporter type 2( SGLT2).
Derivatives of biguanides
At present only metformin is used from biguanides.In fact, this medicine does not affect the synthesis of insulin, and therefore it will be absolutely inefficient if insulin is not synthesized at all.The drug realizes its therapeutic effect through an increase in the utilization of glucose, the improvement of its transport through the cell membranes, as well as the reduction of glucose in the blood.
In addition, the drug has an anorexigenic effect, because it can be used in the treatment of obesity under the supervision of a doctor.By the way, some "miracle pills" for losing weight contain this substance, while an unscrupulous manufacturer may not specify it in the composition.The use of such drugs can be really dangerous to health.Metformin is an antidiabetic drug that is prescribed by a doctor, taking into account indications and contraindications.
Contraindications to the use of biguanides:
- Diabetes mellitus type 1;
- Renal failure;
- Heart failure;
- Disturbed liver function;
- Respiratory failure due to lung disease;
- Old age.
If a woman who takes metformin becomes pregnant, she must cancel the use of this medication.The use of metformin will be possible only after the cessation of breastfeeding.
Very often in the treatment of type 2 diabetes resort to the use of sulfonylurea derivatives. There are sulfonylurea preparations of three generations:
- First generation: tolbutamide, tolazamide, chlorpropamide.
- Second generation: glibenclamide, glycoside, glycidone, glipizide.Third generation: glimepiride. .
Preparations of the first generation have actually lost their relevance, and therefore now they are practically not applied.Preparations of the second and third generation are several tens times more active than preparations of the first generation.In addition, the likelihood of developing side effects when using more modern sulfanylurea drugs is much less.The first preparation of the second generation was glibenclamide, which is successfully used now.
Sulfonylurea preparations exhibit varying degrees of effect and duration of action.Among them, the most pronounced hypoglycemic action is glibenclamide.Perhaps, this is the most popular representative among sulfonylurea drugs.The second most frequently used is glycazide.This drug has not only a hypoglycemic effect, but also positively affects the rheological properties of the blood, as well as microcirculation.
Derivatives of sulfonylureas stimulate the secretion of insulin and its release from beta cells, and restore the sensitivity of these cells to glycemia.
- Ineffective with a significant loss of beta cells of the pancreas in the patient;
- Some patients do not have an antidiabetic effect for reasons unknown;
- Effective only when dieting;
- Must be taken half an hour before meals.
The main contraindications for the use of sulfonylurea drugs are type 1 diabetes, the state of ketoacidosis, the period of pregnancy and lactation, serious operations.
Inhibitors of alpha-glucosidases
This group is represented by preparations of acarbose and miglitol.They reduce the absorption in the intestines of most carbohydrates( maltose, sucrose, starch).In the end, this prevents the development of hyperglycemia.The use of alpha-glucosidase inhibitors can cause all kinds of dyspeptic phenomena( flatulence, diarrhea) due to disruption of digestion processes, as well as absorption of carbohydrates.To avoid undesirable phenomena from the digestive tract, treatment starts with small doses, gradually increasing it.The tablet should be taken with food.In addition, it is important to follow a diet and restrict the use of complex carbohydrates.
In case of occurrence of diarrheal phenomena it is impossible to resort to the use of enzyme preparations, antacids, sorbents.This, of course, will improve digestion, eliminate flatulence and diarrhea, but the effectiveness of the alpha-glucosidase inhibitor will decrease markedly.
Acarbose is the only oral preparation that can be used in the complex treatment of insulin-dependent diabetes.In addition, according to modern studies, treatment with acarbose is accompanied by a decrease in the progression of arteriosclerosis of the vessels and a reduction in the risk of developing cardiac complications against the background of atherosclerosis.
Contraindications to the use of α-glucosidase inhibitors:
- Inflammatory bowel disease;
- Cirrhosis of the liver;
- Ulcers of the intestine;
- Intestinal striction;
- Chronic renal failure;
- Pregnancy and lactation.
Derivatives of thiazolidinediones( glitazones)
Representatives of this group of tablets are pioglitazone( actos), rosiglitazone( avandia), pioglar.The effect of this drug group is due to the increased sensitivity of target tissues to the action of insulin, thereby increasing the utilization of glucose.Glitazones do not affect the synthesis of insulin beta cells.Hypoglycemic action of thiazolidinedione derivatives begins to appear after a month, and to obtain the full effect it can take up to three months.
According to the research data, the glitazones improve lipid metabolism and also reduce the level of certain factors that play a role in atherosclerotic vascular lesions.Now extensive studies are being conducted to determine whether it is possible to use glitazones as a means for preventing type 2 diabetes and reducing the incidence of cardiovascular complications.
However, thiazolidinedione derivatives also have side effects: an increase in body weight and a certain risk of heart failure.
Thiazolidinediones are recommended for use with biguanides, sulfonylurea, insulin.
Derived clay species
Representatives of this group are repaglinide( novonorm) and nateglinide( starlix).These are short-acting drugs that stimulate the secretion of insulin, which allows you to keep your glucose levels under control after eating.With severe hyperglycaemia, fasting clay is ineffective.
The insulinotropic effect develops rather quickly with the admission of clay minerals.Thus, the development of insulin occurs twenty minutes after taking the tablets novonorm and after five to seven minutes after taking Starlix.
Among the side effects - gaining weight, as well as a decrease in the effectiveness of the drug with prolonged use.
Contraindications include the following conditions:
- Insulin-dependent diabetes;
- Renal, hepatic impairment;
- Pregnancy and lactation.
This is a new class of hypoglycemic drugs, which include derivatives of inhibitors of dipeptidyl peptidase-4( DPP-4) and derivatives of agonists of glucone-like peptide-1( GLP-1).Increrets are hormones that are released from the intestine when eating.They stimulate the secretion of insulin and the main role in this process is played by glucose-dependent insulinotropic( GUI) and gluconoid-like peptides( GLP-1).It happens in a healthy body.And in patients with type 2 diabetes, the secretion of incretins decreases, and the secretion of insulin decreases accordingly.
Inhibitors of dipeptidyl peptidase-4( DPP-4) are essentially activators of GLP-1 and HIP.Under the influence of DPP-4 inhibitors, the duration of action of incretins increases.Representative of inhibitors of dipeptidyl peptidase-4 is sitagliptin, which is available under the trade name of Yanuvia.
Yanuvia stimulates the secretion of insulin, and suppresses the secretion of the hormone glucagon.This occurs only on condition of hyperglycemia.At normal glucose concentration, the above mechanisms are not included, it helps to avoid hypoglycemia, which happens when treating with sugar-lowering drugs of other groups.Issued Januvia in the form of tablets.
But derivatives of agonists GLP-1( viktose, lyxumium) are available in the form of solutions for subcutaneous administration, which is certainly less convenient than using tablets.
Derivatives of SGLT2 inhibitors
Derived inhibitors of sodium-glucose cotransporter type 2( SGLT2) is the newest group of hypoglycemic drugs.Its representatives dapagliflozin and kanagliflozin were approved by the FDA in 2012 and 2013, respectively.The mechanism of action of these tablets is based on inhibition of the activity of SGLT2( sodium-glucose cotransporter type 2).
SGLT2 is the main transport protein involved in the reabsorption( reabsorption) of glucose from the kidneys into the blood.Medications inhibitors of SGLT2 lower the concentration of glucose in the blood by reducing its renal reabsorption.That is, drugs stimulate the release of glucose in the urine.
Concomitant phenomena with the use of SGLT2 inhibitors are lowering blood pressure, as well as body weight.Among the side effects of the drug may be the development of hypoglycemia, urinary infections.
Dapagliflozin and cannagliflozin are contraindicated in insulin-dependent diabetes, ketoacidosis, renal failure, and pregnancy.
Important! The same medicine affects people in different ways.Sometimes it is not possible to achieve the desired effect on the background of therapy with a single drug.In such cases, resort to combined treatment with several oral hypoglycemic drugs.This therapeutic scheme allows you to work on different parts of the disease, increase the secretion of insulin, and reduce insulin resistance of tissues.
Grigorova Valeria, medical reviewer