Oral hypoglycemic agents. Antihyperglycemic drugs of a new generation and their classification. Treatment for trematodes
Contraindications to the use of alpha-glucosidase inhibitors:
- Inflammatory bowel disease;
- intestinal ulcers;
- Intestinal strictures;
- Chronic renal failure;
- Pregnancy and lactation.
Thiazolidinedione derivatives (glitazones)
Representatives of this group of tablets pioglitazone (actos), rosiglitazone (avandia), pioglar. The effect of this drug group due to an increase in the sensitivity of target tissues to the action of insulin, thereby increasing the utilization of glucose. Glitazones do not affect insulin synthesis by beta cells. The hypoglycemic effect of thiazolidinedione derivatives begins to appear after a month, and it may take up to three months to obtain a full effect.
Studies have shown that glitazones improve lipid metabolism and also reduce the level of certain factors that play a role in atherosclerotic vascular disease. Large-scale studies are currently underway to determine whether glitazones can be used as a prophylactic agent. diabetes type 2 and reduce the incidence of cardiovascular complications.
However, thiazolidinedione derivatives also have a side effect: an increase in body weight and a certain risk of heart failure.
Glinide derivatives
This group is represented by repaglinide (novonorm) and nateglinide (starlix). These are short-acting drugs that stimulate the secretion of insulin, which allows you to control the level of glucose after eating. With severe hyperglycemia on an empty stomach, glinides are ineffective.
The insulinotropic effect develops quite quickly when taking glinides. So, the production of insulin occurs twenty minutes after taking Novonorm tablets and five to seven minutes after taking Starlix.
Among side effects- weight gain, as well as a decrease in the effectiveness of the drug with prolonged use.
Contraindications include such conditions as:
- insulin dependent diabetes;
- renal, liver failure;
- Pregnancy and lactation.
Incretins
This is a new class of hypoglycemic drugs, which include derivatives of dipeptidyl peptidase-4 (DPP-4) inhibitors and derivatives of glucagon-like peptide-1 (GLP-1) agonists. Incretins are hormones that are released from the intestines when food is eaten. They stimulate insulin secretion and the main role in this process is played by glucose-dependent insulinotropic (GIP) and glucagon-like peptides (GLP-1). This is what happens in a healthy body. And in a patient with type 2 diabetes, the secretion of incretins decreases, respectively, and the secretion of insulin also decreases.
Dipeptidyl peptidase-4 (DPP-4) inhibitors are essentially activators of GLP-1 and GIP. Under the influence of DPP-4 inhibitors, the duration of action of incretins increases. A representative of dipeptidyl peptidase-4 inhibitors is sitagliptin, which is produced under the trade name Januvia.
Januvia stimulates the secretion of insulin, and also suppresses the secretion of the hormone glucagon. This occurs only under the condition of hyperglycemia. At a normal glucose concentration, the above mechanisms are not included, this helps to avoid hypoglycemia, which happens when treated with other groups of hypoglycemic drugs. Januvia is available in the form of tablets.
But derivatives of GLP-1 agonists (Victose, Lyxumia) are available in the form of solutions for subcutaneous administration, which is of course less convenient than using tablets.
Derivatives of SGLT2 inhibitors
Sodium-glucose cotransporter type 2 (SGLT2) inhibitor derivatives are a newer group of hypoglycemic drugs. Its representatives dapagliflozin and canagliflozin were approved by the FDA in 2012 and 2013, respectively. The mechanism of action of these tablets is based on the inhibition of the activity of SGLT2 (sodium-glucose cotransporter type 2).
SGLT2 is the main transport protein involved in the reabsorption (re-absorption) of glucose from the kidneys into the blood. Medications that inhibit SGLT2 lower the concentration of glucose in the blood by reducing its renal reabsorption. That is, the drugs stimulate the excretion of glucose in the urine.
Concomitant effects with the use of SGLT2 inhibitors are a decrease blood pressure, as well as body weight. Among side effects medications may develop hypoglycemia, urinary infections.
Dapagliflozin and canagliflozin are contraindicated in insulin-dependent diabetes, ketoacidosis, renal failure, pregnancy.
Important! The same drug affects people differently. Sometimes it is not possible to achieve the desired effect during therapy with a single drug. In such cases, resort to combined treatment with several oral hypoglycemic drugs. Such a therapeutic regimen makes it possible to influence different parts of the disease, increase insulin secretion, and also reduce tissue insulin resistance.
Grigorova Valeria, medical commentator
Hypoglycemic(hyperlink http://www.*****/fg_index_id_292.htm) or antidiabetic drugs - medicines that lower blood glucose levels and are used to treat diabetes.
Along with insulin, the preparations of which are suitable only for parenteral use, there are a number of synthetic compounds that have a hypoglycemic effect and are effective when taken orally. These drugs are mainly used in type 2 diabetes mellitus.
Oral hypoglycemic (hyperglycemic) agents are classified according to the main mechanism of hypoglycemic action:
Drugs that increase insulin secretion:
- sulfonylurea derivatives(glibenclamide, gliquidone, gliclazide, glimepiride, glipizide, chlorpropamide);
- meglitinides(nateglinide, repaglinide).
Drugs that mainly increase the sensitivity of peripheral tissues to insulin (sensitizers):
- biguanides(buformin, metformin, phenformin);
- thiazolidinediones(pioglitazone, rosiglitazone, ciglitazone, englitazone, troglitazone).
Drugs that disrupt the absorption of carbohydrates in the intestine:
- alpha-glucosidase inhibitors(acarbose, miglitol).
The hypoglycemic properties of sulfonylurea derivatives were discovered by chance. The ability of the compounds of this group to have a hypoglycemic effect was discovered in the 50s, when patients who received antibacterial sulfanilamide drugs for the treatment infectious diseases a decrease in blood glucose was noted. In this regard, the search for derivatives of sulfonamides with a pronounced hypoglycemic effect began in the 50s. the synthesis of the first sulfonylurea derivatives was carried out, which could be used to treat diabetes mellitus. The first such drugs were carbutamide (Germany, 1955) and tolbutamide (USA, 1956). In the early 50s. these sulfonylurea derivatives have begun to be used in clinical practice. In the 60s and 70s. second-generation sulfonylureas appeared. The first representative of the second generation sulfonylurea drugs - glibenclamide - began to be used to treat diabetes mellitus in 1969, in 1970 glibornuride began to be used, and since 1972 - glipizide. Gliclazide and gliquidone appeared almost simultaneously.
In 1997, repaglinide (a group of meglitinides) was approved for the treatment of diabetes.
The history of the use of biguanides dates back to the Middle Ages, when a plant was used to treat diabetes. Galega officinalis(French lily). At the beginning of the 19th century, the alkaloid galegin (isoamylene guanidine) was isolated from this plant, but in its pure form it turned out to be very toxic. In 1918–1920 the first drugs were developed - derivatives of guanidine - biguanides. Subsequently, due to the discovery of insulin, attempts to treat diabetes mellitus with biguanides faded into the background. Biguanides (phenformin, buformin, metformin) were introduced into clinical practice only in 1957–1958. after sulfonylurea derivatives of the first generation. The first drug in this group was phenformin (due to a pronounced side effect - the development of lactic acidosis - withdrawn from use). Buformin, which has a relatively weak hypoglycemic effect and a potential risk of developing lactic acidosis, has also been discontinued. Currently, only metformin is used from the group of biguanides.
Thiazolidinediones (glitazones) entered clinical practice in 1997. The first drug approved for use as a hypoglycemic agent was troglitazone, but in 2000 its use was banned due to high hepatotoxicity. To date, two drugs from this group are used - pioglitazone and rosiglitazone.
Action sulfonylurea derivatives
It is mainly associated with stimulation of pancreatic beta cells, accompanied by mobilization and increased release of endogenous insulin. The main prerequisite for the manifestation of their effect is the presence of functionally active beta cells in the pancreas. On the membrane of beta cells, sulfonylurea derivatives bind to specific receptors associated with ATP-dependent potassium channels. The sulfonylurea receptor gene has been cloned. It has been established that the classic high-affinity sulfonylurea receptor (SUR-1) is a protein with a molecular weight of 177 kDa. Unlike other sulfonylurea derivatives, glimepiride binds to another protein coupled to ATP-dependent potassium channels and has a molecular weight of 65 kDa (SUR-X). In addition, in the K +
-channel includes the intramembrane subunit Kir 6.2 (a protein with a molecular weight of 43 kDa), which is responsible for the transport of potassium ions. It is believed that as a result of this interaction, the "closing" of the potassium channels of beta cells occurs. Increasing the concentration of K ions +
inside the cell contributes to the depolarization of membranes, the opening of voltage-dependent Ca 2+
channels, an increase in the intracellular content of calcium ions. The result of this is the release of insulin stores from beta cells.
With long-term treatment with sulfonylurea derivatives, their initial stimulating effect on insulin secretion disappears. It is believed that this is due to a decrease in the number of receptors on beta cells. After a break in treatment, the reaction of beta cells to taking drugs of this group is restored.
Some sulfonylurea drugs also have an extrapancreatic effect. Extrapancreatic effects are not of great clinical importance, they include an increase in the sensitivity of insulin-dependent tissues to endogenous insulin and a decrease in the formation of glucose in the liver. The mechanism for the development of these effects is due to the fact that these drugs (especially glimepiride) increase the number of insulin-sensitive receptors on target cells, improve insulin-receptor interaction, and restore post-receptor signal transduction.
In addition, there is evidence that derivatives of sulfonylurea stimulate the release of somatostatin and thereby suppress the secretion of glucagon.
Sulfonylureas derivatives:
I generation: tolbutamide, carbutamide, tolazamide, acetohexamide, chlorpropamide.
II generation: glibenclamide, glizoxepide, glibornuril, gliquidone, gliclazide, glipizide.
III generation: glimepiride.
At present, sulfonylurea preparations of the first generation are practically not used in Russia.
The main difference between second generation drugs and first generation sulfonylurea derivatives is greater activity (50–100 times), which allows them to be used at lower doses and, accordingly, reduces the likelihood of side effects. Individual representatives of hypoglycemic sulfonylurea derivatives of the I and II generations differ in activity and tolerability. Thus, the daily dose of drugs of the first generation - tolbutamide and chlorpropamide - 2 and 0.75 g, respectively, and drugs of the second generation - glibenclamide - 0.02 g; gliquidone - 0.06–0.12 g. Second-generation drugs are usually better tolerated by patients.
Sulfonylureas have different severity and duration of action, which determines the choice of drugs in the appointment. Glibenclamide has the most pronounced hypoglycemic effect of all sulfonylurea derivatives. It is used as a standard for assessing the hypoglycemic effect of newly synthesized drugs. The powerful hypoglycemic effect of glibenclamide is due to the fact that it has the highest affinity for ATP-dependent potassium channels of pancreatic beta cells. Currently, glibenclamide is produced both in the form of a traditional dosage form and in the form of a micronized form - a specially crushed form of glibenclamide, which provides an optimal pharmacokinetic and pharmacodynamic profile due to rapid and complete absorption (bioavailability is about 100%) and makes it possible to use drugs in smaller doses.
Gliclazide is the second most commonly prescribed oral hypoglycemic agent after glibenclamide. In addition to the fact that gliclazide has a hypoglycemic effect, it improves hematological parameters, rheological properties of blood, positively affects the system of hemostasis and microcirculation; prevents the development of microvasculitis, including damage to the retina; inhibits platelet aggregation, significantly increases the relative disaggregation index, increases heparin and fibrinolytic activity, increases heparin tolerance, and also exhibits antioxidant properties.
Gliquidone is a drug that can be prescribed to patients with moderately severe renal impairment, since only 5% of metabolites are excreted through the kidneys, the rest (95%) through the intestines.
Glipizide, having a pronounced effect, poses a minimal danger in terms of hypoglycemic reactions, since it does not accumulate and has no active metabolites.
Oral antidiabetic drugs are the main drug therapy diabetes mellitus type 2 (non-insulin dependent) and are usually prescribed to patients over 35 years of age without ketoacidosis, nutritional deficiencies, complications, or comorbidities requiring immediate insulin therapy.
Sulfonylureas are not recommended for patients whose daily insulin requirement exceeds 40 units with a proper diet. Also, they are not prescribed to patients with severe forms of diabetes mellitus (with severe deficiency of beta cells), with a history of ketosis or diabetic coma, with hyperglycemia above 13.9 mmol / l (250 mg%) on an empty stomach and high glucosuria during diet therapy.
Transfer to treatment with sulfonylurea drugs in patients with diabetes mellitus who are on insulin therapy is possible if violations carbohydrate metabolism compensated for at doses of insulin less than 40 IU / day. At doses of insulin up to 10 IU / day, you can immediately switch to treatment with sulfonylurea derivatives.
Long-term use of sulfonylurea derivatives can cause the development of resistance, which can be overcome by combination therapy with insulin preparations. In type 1 diabetes mellitus, the combination of insulin preparations with sulfonylurea derivatives makes it possible to reduce daily requirement in insulin and helps to improve the course of the disease, including slowing down the progression of retinopathy, which is to some extent associated with the angioprotective activity of sulfonylurea derivatives (especially II generation). However, there are indications of their possible atherogenic effect.
In addition to the fact that sulfonylurea derivatives are combined with insulin (this combination is considered appropriate if the patient's condition does not improve with the appointment of more than 100 IU of insulin per day), they are sometimes combined with biguanides and acarbose.
When using sulfonamide hypoglycemic drugs, it should be borne in mind that antibacterial sulfonamides, indirect anticoagulants, butadione, salicylates, ethionamide, tetracyclines, chloramphenicol, cyclophosphamide inhibit their metabolism and increase efficiency (hypoglycemia may develop). When sulfonylurea derivatives are combined with thiazide diuretics (hydrochlorothiazide, etc.) and CCBs (nifedipine, diltiazem, etc.), antagonism occurs in large doses - thiazides interfere with the effect of sulfonylurea derivatives due to the opening of potassium channels, and CCBs disrupt the flow of calcium ions into pancreatic beta cells glands.
Sulfonylureas increase the effect and intolerance of alcohol, probably due to the delay in the oxidation of acetaldehyde. Antabuse-like reactions are possible.
All sulfonamide hypoglycemic drugs are recommended to be taken 1 hour before a meal, which contributes to a more pronounced decrease in postprandial (after a meal) glycemia. In case of severe dyspeptic symptoms, it is recommended to use these drugs after meals.
Undesirable effects of sulfonylurea derivatives, in addition to hypoglycemia, are dyspeptic disorders (including nausea, vomiting, diarrhea), cholestatic jaundice, weight gain, reversible leukopenia, thrombocytopenia, agranulocytosis, aplastic and hemolytic anemia, allergic reactions (including pruritus, erythema, dermatitis).
The use of sulfonylurea drugs during pregnancy is not recommended, since most of them belong to class C according to the FDA (Food and Drug Administration), insulin therapy is prescribed instead.
Elderly patients are not recommended to use long-acting drugs (glibenclamide) due to an increased risk of hypoglycemia. At this age, it is preferable to use short-acting derivatives - gliclazide, gliquidone.
meglitinides
- prandial regulators (repaglinide, nateglinide).
Repaglinide is a derivative of benzoic acid. Despite the difference in chemical structure from sulfonylurea derivatives, it also blocks ATP-dependent potassium channels in the membranes of functionally active beta-cells of the pancreatic islet apparatus, causes their depolarization and the opening of calcium channels, thereby inducing insulin incretion. An insulinotropic response to food intake develops within 30 minutes after application and is accompanied by a decrease in blood glucose levels during the meal period (insulin concentration does not increase between meals). As with sulfonylurea derivatives, the main side effect is hypoglycemia. With caution, repaglinide is prescribed to patients with hepatic and / or renal insufficiency.
Nateglinide is a derivative of D-phenylalanine. Unlike other oral hypoglycemic agents, the effect of nateglinide on insulin secretion is more rapid but less persistent. Nateglinide is used primarily to reduce postprandial hyperglycemia in type 2 diabetes.
biguanides
, which began to be used for the treatment of type 2 diabetes in the 70s, do not stimulate the secretion of insulin by pancreatic beta cells. Their action is mainly determined by the inhibition of gluconeogenesis in the liver (including glycogenolysis) and increased utilization of glucose by peripheral tissues. They also inhibit the inactivation of insulin and improve its binding to insulin receptors (increasing glucose uptake and metabolism).
Biguanides (unlike sulfonylurea derivatives) do not reduce blood glucose levels in healthy people and in patients with type 2 diabetes after an overnight fast, but significantly limit its increase after a meal without causing hypoglycemia.
Hypoglycemic biguanides - metformin and others - are also used in type 2 diabetes mellitus. In addition to the hypoglycemic effect, long-term use of biguanides has a positive effect on lipid metabolism. The drugs of this group inhibit lipogenesis (the process by which glucose and other substances are converted into fatty acids in the body), activate lipolysis (the process of splitting lipids, especially triglycerides contained in fat, into their constituent fatty acids under the action of the lipase enzyme), reduce appetite, promote reduction in body weight. In some cases, their use is accompanied by a decrease in the content of triglycerides, cholesterol and LDL (determined on an empty stomach) in the blood serum. In type 2 diabetes mellitus, carbohydrate metabolism disorders are combined with pronounced changes in lipid metabolism. Thus, 85-90% of patients with type 2 diabetes mellitus have increased body weight. Therefore, when type 2 diabetes mellitus is combined with overweight, drugs that normalize lipid metabolism are indicated.
An indication for the appointment of biguanides is type 2 diabetes mellitus (especially in cases accompanied by obesity) with the ineffectiveness of diet therapy, as well as with the ineffectiveness of sulfonylurea drugs.
In the absence of insulin, the effect of biguanides does not appear.
Biguanides can be used in combination with insulin in the presence of insulin resistance. The combination of these drugs with sulfonamide derivatives is indicated in cases where the latter do not provide a complete correction of metabolic disorders. Biguanides can cause the development of lactic acidosis (lactacidosis), which limits the use of drugs in this group.
Biguanides can be used in combination with insulin in the presence of insulin resistance. The combination of these drugs with sulfonamide derivatives is indicated in cases where the latter do not provide a complete correction of metabolic disorders. Biguanides can cause the development of lactic acidosis (lactacidosis), which limits the use of some drugs in this group.
Biguanides are contraindicated in the presence of acidosis and a tendency to it (provoke and increase the accumulation of lactate), in conditions accompanied by hypoxia (including heart and respiratory failure, acute phase of myocardial infarction, acute insufficiency cerebral circulation, anemia), etc.
Side effects of biguanides are noted more often than those of sulfonylurea derivatives (20% vs. 4%), first of all, these are adverse reactions from the gastrointestinal tract: a metallic taste in the mouth, dyspepsia, etc. Unlike sulfonylurea derivatives, hypoglycemia with the use of biguanides (for example, metformin ) is very rare.
Lactic acidosis, which sometimes appears when taking metformin, is considered a serious complication, therefore, metformin should not be prescribed for renal failure and conditions that predispose to its development - impaired renal and / or liver function, heart failure, lung pathology.
Biguanides should not be administered simultaneously with cimetidine, since they compete with each other in the process of tubular secretion in the kidneys, which can lead to accumulation of biguanides, in addition, cimetidine reduces the biotransformation of biguanides in the liver.
The combination of glibenclamide (second generation sulfonylurea derivative) and metformin (biguanide) optimally combines their properties, allowing you to achieve the desired hypoglycemic effect with a lower dose of each of the drugs and thereby reduce the risk of side effects.
Since 1997, clinical practice has included thiazolidinediones (glitazones),
whose chemical structure is based on a thiazolidine ring. This new group of antidiabetic agents includes pioglitazone and rosiglitazone. Drugs of this group increase the sensitivity of target tissues (muscles, adipose tissue, liver) to insulin, reduce lipid synthesis in muscle and fat cells. Thiazolidinediones are selective agonists of nuclear receptors PPARγ (peroxisome proliferator-activated receptor-gamma). In humans, these receptors are found in the main “target tissues” for the action of insulin: in adipose tissue, in skeletal muscles and in the liver. Nuclear PPARγ receptors regulate the transcription of insulin-responsible genes involved in the control of glucose production, transport, and utilization. In addition, PPARγ-responsive genes are involved in fatty acid metabolism.
In order for the thiazolidinediones to have their effect, the presence of insulin is required. These drugs reduce the insulin resistance of peripheral tissues and the liver, increase the consumption of insulin-dependent glucose and reduce the release of glucose from the liver; reduce average levels of triglycerides, increase the concentration of HDL and cholesterol; prevent hyperglycemia on an empty stomach and after a meal, as well as glycosylation of hemoglobin.
Alpha-glucosidase inhibitors
(acarbose, miglitol) inhibit the breakdown of poly- and oligosaccharides, reducing the formation and absorption of glucose in the intestine and thereby preventing the development of postprandial hyperglycemia. Carbohydrates taken with food in unchanged form enter the lower sections of the small and large intestines, while the absorption of monosaccharides is prolonged up to 3–4 hours. Unlike sulfonamide hypoglycemic agents, they do not increase the release of insulin and, therefore, do not cause hypoglycemia.
An essential role in positive influence acarbose on glucose metabolism belongs to glucagon-like peptide-1 (GLP-1), which is synthesized in the intestine (as opposed to glucagon, synthesized by pancreatic cells) and released into the blood in response to food intake.
It has been shown that long-term therapy with acarbose is accompanied by a significant reduction in the risk of developing cardiac complications of an atherosclerotic nature. Alpha-glucosidase inhibitors are used as monotherapy or in combination with other oral hypoglycemic agents. The initial dose is 25-50 mg immediately before meals or during meals, and subsequently may be gradually increased (maximum daily dose of 600 mg).
Indications for the appointment of alpha-glucosidase inhibitors are type 2 diabetes mellitus with the ineffectiveness of diet therapy (the course of which should be at least 6 months), as well as type 1 diabetes mellitus (as part of combination therapy).
Drugs in this group can cause dyspepsia due to impaired digestion and absorption of carbohydrates, which are metabolized in the large intestine to form fatty acids, carbon dioxide and hydrogen. Therefore, when prescribing alpha-glucosidase inhibitors, strict adherence to a diet with a limited content of complex carbohydrates, including sucrose, is necessary.
Acarbose can be combined with other antidiabetic agents. Neomycin and cholestyramine enhance the action of acarbose, while increasing the frequency and severity of side effects from the gastrointestinal tract. When combined with antacids, adsorbents and enzymes that improve the digestion process, the effectiveness of acarbose decreases.
Thus, the group of hypoglycemic agents includes a number of effective drugs. They have a different mechanism of action, differ in pharmacokinetic and pharmacodynamic parameters. Knowledge of these features allows the doctor to make the most individual and right choice therapy.
Descriptions of drugs of the pharmacological group Hypoglycemic agents(hyperlink http://www.*****/fg_list_id_292.htm)
Information provided by the project “Register medicines Russia".
Website on the Internetwww. *****
Oral hypoglycemic agents
Oral hypoglycemic agents are medicines taken by mouth that lower blood glucose levels. They are used in the treatment of diabetes mellitus, mainly type II.
Depending on the mechanism of action, they are divided into groups:
- drugs that stimulate the production of insulin in the body. These include sulfonylurea derivatives;
- drugs that increase the sensitivity of peripheral tissues to insulin. These include biguanides, thiazolidinediones;
- drugs that impede the absorption of carbohydrates in the intestines. These include inhibitors? -glucosidase.
Sulfonylureas
Medicines of this group are not recommended for patients who receive a daily dose of insulin more than 40 IU, as well as for ketoacidosis. Sulfonylureas differ in strength and duration of action. With long-term use of these drugs, the body may develop resistance to them. Often sulfonylurea derivatives are prescribed in combination with insulin or biguanides.
There are 3 generations of drugs belonging to this group. Sulfonylureas of the first generation are prescribed in large doses and are almost never used at present.
More modern drugs (II and III generations) are used in small doses, while they are well tolerated by patients.
Maninil 5
Active substance: glibenclamide.
Pharmachologic effect: sulfonylurea derivative II generation. It lowers the level of glucose in the blood, increases the production of insulin by the pancreas and increases the sensitivity of peripheral tissues to it. In addition, the drug reduces the level of cholesterol in the body and the tendency to thrombosis.
Indications: type II diabetes mellitus in adults.
Contraindications: hypersensitivity to the drug, type I diabetes mellitus, ketoacidotic states (including coma), impaired renal and hepatic functions, periods of pregnancy and lactation.
Side effects: digestive disorders, in rare cases - impaired liver function and bile outflow, headache, dizziness, allergic rash, excessive decrease in blood glucose levels in case of overdose.
Mode of application: the dose is selected individually. Taken orally 20-30 minutes before meals. The average daily dose of 2.5-15 mg is divided into 1-3 doses. The initial daily dose for elderly patients is 1 mg.
If previously treated with biguanides, then the initial dose of maninil should not exceed 2.5 mg per day. Every 5-6 days it is increased to compensate for metabolic processes. If after 4-6 weeks the desired result has not been achieved, biguanides are also prescribed.
Release form: 5 mg tablets - 120 pieces per pack.
Special instructions: in the treatment of maninil, it is not recommended to take alcohol. Prescribed with caution in diseases of the kidneys and liver, thyroid gland and adrenals.
Glucostabil
Active substance: gliclazide.
Pharmachologic effect: sulfonylurea derivative II generation. Reduces the level of glucose in the blood, enhances the production of insulin by the pancreas, the sensitivity of peripheral tissues to it. Reduces the time between a meal and the start of insulin production. Reduces the ability of platelets to converge and stick together, reduces thrombosis. Reduces cholesterol and increases lipoprotein levels high density in blood. Reduces the sensitivity of blood vessels to adrenaline.
Indications: diabetes mellitus type II, prevention and treatment of initial manifestations of microangiopathy in diabetes mellitus.
Contraindications: hypersensitivity to sulfonamides and sulfonylurea derivatives, type I diabetes mellitus, ketoacidotic states (including coma), renal and hepatic insufficiency, taking imidazole derivatives.
Side effects: pain in the epigastric region, dysfunction of the gastrointestinal tract, anemia, thrombocytopenia, excessive decrease in blood glucose levels in case of overdose.
Mode of application: taken orally, the dose is set depending on the level of glucose in the blood on an empty stomach and 2 hours after a meal. Initial dose - 40 mg of the drug 2 times a day, then 80-160 mg 2 times a day.
Release form: tablets of 40 and 80 mg - 60 and 100 pieces per pack.
Special instructions: therapy is combined with a low-calorie, low-carbohydrate diet. During treatment, it is necessary to monitor the level of glucose in the blood.
Amaril
Active substance: glimepiride.
Pharmachologic effect: sulfonylurea derivative III generation. It lowers the level of glucose in the blood, enhances the production of insulin by the pancreas and the sensitivity of peripheral tissues to it.
Indications: type II diabetes mellitus in the absence of the effect of diet therapy.
Contraindications: hypersensitivity to sulfonylurea derivatives and sulfonamides, type I diabetes mellitus, ketoacidotic states (including coma), impaired renal and hepatic functions, periods of pregnancy and lactation.
Side effects: an excessive decrease in the level of glucose and sodium in the blood, abdominal pain, dysfunction of the gastrointestinal tract and liver, a decrease in the number of red blood cells, platelets and white blood cells in the blood. From allergic reactions, rashes and itching, anaphylactic shock, increased skin sensitivity to ultraviolet rays are possible.
Mode of application: inside 1 time per day before a hearty breakfast, drinking plenty of water. The dose is calculated individually. The initial daily dose is 1 mg, then every 1-2 weeks it is increased by 1 mg and adjusted to 4-6 mg. The maximum allowable dose is 8 mg per day.
Release form: tablets of 1, 2 and 3 mg - 30 pieces per pack.
Special instructions: during treatment, it is necessary to control the level of glucose in the blood. The drug is used with caution in endocrine diseases. When stressed, you may need a temporary appointment of insulin.
Chlorpropamide
Active substance: chlorpropamide.
Pharmachologic effect: reduces the rate of glucose formation by the liver and increases the sensitivity of peripheral tissues to insulin.
Indications: type II diabetes mellitus and diabetes insipidus (with its stable course).
Contraindications: hypersensitivity to the drug, type I diabetes mellitus (insulin-dependent), diabetes mellitus with decompensation of metabolic processes, elevated body temperature against the background of other diseases, impaired liver and kidney function, thyroid disease, and pregnancy.
Side effects: indigestion, varying degrees of lowering blood glucose levels, allergic reactions.
Mode of application: the dosage of the drug is set individually, the minimum initial dose is 250–500 mg per day. Depending on the therapeutic effect, the dosage is slowly increased by 50-125 mg per day with an interval of 3-5 days. The average maintenance dose of the drug is 125-250 mg per day. Take the drug 1 time during the morning meal. If the patient receives 30 units of insulin per day, then insulin therapy should be adjusted during treatment with chlorpropamide. For elderly patients, the drug is prescribed at a dose of 100-125 mg per day.
Release form: tablets of 250 mg, 60 pieces per pack.
Special instructions: the drug is prescribed if exercise stress prevent normalization of blood glucose levels. The effectiveness of the drug in lowering blood glucose levels can be increased by non-steroidal anti-inflammatory drugs, as well as salicylates.
biguanides
Biguanides are mainly used in the treatment of type II diabetes mellitus, they do not affect the production of insulin by the pancreas. The decrease in blood glucose levels occurs due to inhibition of the processes of formation of glucose from fats and proteins. Biguanides promote the binding of insulin to receptors and the uptake of glucose by cells.
The drugs of this group do not affect the level of glucose in the blood in healthy people and in type II diabetes mellitus after a long break in food intake (night sleep). They inhibit the rise in glucose levels after meals. Due to these features, biguanides do not lead to an excessive decrease in blood glucose levels.
In some cases, treatment with biguanides is combined with the appointment of insulin or sulfonylurea derivatives.
metfogamma
Active substance: metformin hydrochloride.
Pharmachologic effect: lowers blood glucose levels. It inhibits the formation of glucose from fats and proteins. The drug does not change the concentration of insulin, but improves its formation from proinsulin and increases the amount of free insulin. Improves the uptake of glucose by the muscles. Promotes the formation of glycogen from glucose in the liver. The drug enhances fibrinolysis.
Indications: type I diabetes mellitus (as an adjunct to insulin therapy), type II diabetes mellitus in the absence of the effect of diet therapy.
Contraindications: hypersensitivity to the drug, respiratory disorders, heart, kidney and liver failure, acidosis, chronic alcoholism, acute period of myocardial infarction, periods of pregnancy and lactation.
Side effects: dysfunction of the gastrointestinal tract at the beginning of treatment, an excessive decrease in blood glucose levels in case of an overdose, an increase in the level of lactic acid in the blood (in this case, the drug is canceled), in rare cases, megaloblastic anemia.
Mode of application: inside during or after a meal with a small amount of water. With monotherapy, Metfogamma is prescribed for the first 3 days at 500 mg 3 times a day or 1 g 2 times a day. In the period from the 4th to the 14th day, 1 g is recommended 3 times a day. Further, the dose is set depending on the level of glucose in the blood and urine, the usual maintenance daily dose is 100–200 mg.
With simultaneous insulin therapy, the dose of insulin is reduced by 4–8 units every 2 days. With a daily dose of insulin more than 40 IU, correction of treatment is carried out in a hospital.
Release form: tablets of 1 g - 10 and 15 pieces in a blister.
Special instructions: during the period of treatment, it is necessary to control the level of lactic acid in the blood (at least 1 time in 6 months).
Buformin
Active substance: buformin.
Pharmachologic effect: lowers the level of glucose in the blood by suppressing its absorption in the intestine and activating the oxygen-free production of glucose in the body. The drug reduces the formation of glucose from fats and proteins, promotes the binding of insulin to the corresponding receptors.
Indications: type II diabetes mellitus, including those accompanied by obesity. In combination with insulin, it can be used to treat type 1 diabetes.
Contraindications: hypersensitivity to the drug, severe renal, hepatic, heart failure, respiratory dysfunction, acute period of myocardial infarction. The drug is not prescribed for febrile conditions, acidosis, chronic alcoholism, as well as during pregnancy and lactation.
Side effects: metallic taste in the mouth, pain in the epigastric region, loss of appetite, nausea and diarrhea.
Mode of application: inside during meals. The dose is selected individually. The maximum daily dose is 300 mg; frequency of administration - 2-3 times a day, for long-acting drugs - 1 time per day.
Release form: 50 mg tablets - 50 pieces per pack.
Special instructions: when using buformin, it is possible to reduce the dose of insulin. Constant monitoring of glucose levels in the blood and urine is necessary.
Thiazolidinediones
Thiazolidinediones increase tissue susceptibility to insulin. The drugs of this group reduce the formation of lipids and their accumulation in muscles and subcutaneous fat, prevent a pronounced increase in blood glucose levels on an empty stomach and after meals, and the formation of glycated hemoglobin. The action of drugs is carried out only in the presence of insulin.
Aktos
Active substance: pioglitazone.
Pharmachologic effect: reduces the level of glucose in the blood, increases the susceptibility of tissues to insulin, which leads to improved absorption of glucose by cells and a decrease in its formation from liver glycogen. Does not affect the production of insulin by the pancreas, improves fat metabolism.
Indications: type II diabetes mellitus, including as part of complex treatment in the absence of the effect of diet therapy and exercise therapy.
Contraindications: hypersensitivity to the drug, type I diabetes mellitus, acidosis, periods of pregnancy and lactation.
Side effects: excessive decrease in blood glucose levels, in rare cases - anemia.
Mode of application: inside once, regardless of the meal. The initial daily dose is 15–30 mg. If necessary, it is gradually increased to a maximum of 45 mg per day. With insufficient therapeutic effect, other oral hypoglycemic drugs are additionally prescribed. When treating with sulfonylurea derivatives, the drug is prescribed at 15–30 mg per day. If treatment with Actos is combined with insulin therapy, then the dose of insulin is gradually reduced.
Release form: tablets of 30 mg - 7 and 30 pieces per pack.
Special instructions: laboratory monitoring of blood glucose levels is required.
?-glucosidase inhibitors
Drugs in this group make it difficult for the breakdown and absorption of carbohydrates in the intestine. Moreover, they do not affect the formation of insulin by the pancreas, so they do not lead to an excessive decrease in blood glucose levels. Reduce the progression of atherosclerosis and its complications from the heart with prolonged use.
Glukobay
Active substance: acarbose.
Pharmachologic effect: reduces blood glucose levels, slows down the breakdown of sucrose and starch in the intestine, reduces changes in blood glucose levels during the day, does not affect the production of insulin by the pancreas.
Indications: type II diabetes mellitus, combined treatment of type I diabetes mellitus.
Contraindications: hypersensitivity to the drug, disease digestive system, accompanied by impaired absorption in the intestine, liver failure, age under 18 years, periods of pregnancy and lactation.
Side effects: increased gas formation in the intestines, diarrhea, abdominal pain, in the treatment of high doses - an increase in the activity of liver enzymes in the blood.
Mode of application: inside, swallowing whole before or during meals, chewing, washing down the drug with a small amount of liquid. The initial single dose is 50 mg 3 times a day. If necessary, the dose is increased to 100-200 mg 3 times a day. The treatment is long.
Release form: tablets of 50 and 100 mg in blisters of 15 pieces.
Special instructions: during treatment, a strict diet recommended for patients with diabetes mellitus is necessary. When prescribing the drug in large doses, constant monitoring of the level of liver enzymes in the blood is required. With combined treatment, the doses of drugs are adjusted.
Combined and fast-acting drugs
There are more modern oral hypoglycemic drugs that do not belong to the previous groups. They increase the production of insulin by the pancreas and provide a quick effect. Combined hypoglycemic drugs can have several effects at once.
Novonorm
Active substance: repaglinide.
Pharmachologic effect: quickly lowers the level of glucose in the blood, increases the production of insulin by the pancreas. The maximum effect after taking the drug and eating food occurs after 30 minutes. Between meals, the level of insulin in the blood does not change. In type II diabetes, the degree of decrease in blood glucose levels depends on the dose of the drug.
Indications: diabetes mellitus type II.
Contraindications: hypersensitivity to the drug, type I diabetes mellitus, ketoacidotic states (including coma), renal and hepatic insufficiency, taking drugs that affect cytochromes (CYP3A4), pregnancy and its planning, lactation period.
Side effects: excessive decrease in blood glucose levels, manifested by pallor, palpitations, increased sweating, trembling. Perhaps a decrease in visual acuity, mainly at the beginning of treatment. More rarely, there are violations of the function of the gastrointestinal tract, skin allergic reactions.
Mode of application: inside 15 minutes before meals. It is permissible to take the drug 30 minutes before or before meals. The dose is selected individually. At the beginning of treatment, 500 mcg is prescribed for 1 dose, after 2 weeks, under the control of glucose levels in the blood and urine, the dose is increased. The maximum single dose is 4 mg, daily - 16 mg. If the patient has previously received another hypoglycemic drug, then the initial single dose corresponds to 1 mg.
Release form: tablets of 500 mcg, 1 and 2 mg - 30 pieces per pack.
Special instructions: with caution prescribed for kidney disease, weakened state and exhaustion. During treatment with the drug, it is not recommended to take alcohol.
Glibomet
Active substance: glibenclamide, metformin hydrochloride.
Pharmachologic effect: combination drug that lowers blood glucose levels. Stimulates the production of insulin by the pancreas, increases tissue susceptibility to insulin, reduces the formation of glucose from non-carbohydrate compounds in the liver. It hinders the absorption of glucose in the intestines, improves fat metabolism, promotes weight loss. The combination of two substances in the preparation at low doses reduces side effects.
Indications: type II diabetes mellitus in the absence of the effect of diet therapy and monotherapy.
Contraindications: hypersensitivity to the components of the drug, type I diabetes mellitus, ketoacidotic states (including coma), liver and kidney failure, oxygen deficiency in the body, periods of pregnancy and lactation.
Side effects: a decrease in blood glucose, an increase in the level of lactic acid in the blood, in rare cases - nausea, vomiting, a violation of the outflow of bile. There may be dizziness, headache, sensory disturbances. Sometimes there are allergic rashes, joint pain, increased skin sensitivity to ultraviolet rays.
Mode of application: inside in the morning and evening with meals. The dose and duration of treatment is determined individually. At the beginning of treatment, 1-3 tablets per day are prescribed, then the dose is adjusted. The maximum allowable dose is 5 tablets per day.
Release form: tablets (2.5 mg glibenclamide, 400 mg metformin hydrochloride) - 40 pieces per pack.
Special instructions: with the appearance of weakness, convulsions, abdominal pain and vomiting, the drug is canceled and appropriate treatment is carried out. During therapy, it is necessary to control the level of glucose in the blood.
From the book Skin and Venereal Diseases author Oleg Leonidovich IvanovPSYCHOTROPIC DRUGS The majority of skin patients, especially chronic ones, have certain disorders in the neuropsychic sphere, there is a clear connection between the onset and exacerbations of the disease with stressful situations. This applies primarily to patients
From the book 1000 secrets of women's health by Denise FoleyCHAPTER 55 ORAL CONTRACEPTIVES Oral contraceptives—artificial hormones that neutralize the effects of reproductive hormones present in the body—are so safe these days that experts say:
From the book Self-healing and cattle treatment among the Russian old-timer population of Siberia author Georgy Semenovich VinogradovX. Household goods X. Household goods (suspended). Saucer. Medicines are prepared in it. Bottles. Some “compositions” and other medicines are prepared and stored in them. Ordinary water is used to prepare decoctions, broths,
From the book Pharmacology: lecture notes authorLECTURE No. 11. Drugs acting on peripheral neurotransmitter systems. Drugs acting on peripheral cholinergic processes 1. Drugs acting primarily on peripheral neurotransmitter systems B
From the book Pharmacology author Valeria Nikolaevna MalevannayaLECTURE No. 15. Means acting in the field of sensitive nerve endings. Means that reduce the sensitivity of nerve endings 1. Local anesthetics The drugs of this group selectively block the process of transmission of excitation in the efferent nerves and
From the book Faceforming. Unique gymnastics for facial rejuvenation author Olga Vitalievna Gaevskaya4. Enveloping agents and adsorbent agents
From the book A course of lectures on resuscitation and intensive care author Vladimir Vladimirovich Spas2. Products containing essential oils. bitterness. Means containing ammonia Means containing essential oils. Eucalyptus leaf (Folium Eucalypti). Application: decoction and infusion of eucalyptus as an antiseptic for rinsing and inhalation with ENT diseases, as well as for treatment
From the book Most Popular Medicines author Mikhail Borisovich Ingerleib47. Enveloping agents and adsorbent agents
From the book Essential Medicines Handbook author Elena Yurievna Khramova48. Products containing essential oils. bitterness. Means containing ammonia Means containing essential oils. Eucalyptus leaf (Folium Eucalypti). Application: decoction and infusion of eucalyptus as an antiseptic for rinsing and inhalation with ENT diseases, as well as for treatment
From the book Healing Apple Cider Vinegar author Nikolai Illarionovich DanikovTransdermals Most effective means for skin care are referred to as transdermal, that is, penetrating into the skin. For a certain period of time, they linger in the skin and thus enable the active substance to have a beneficial effect on
From the book Complete Medical Diagnostic Handbook author P. VyatkinHypoglycemic conditions and hypoglycemic coma in diabetes mellitus Definition. Hypoglycemia is a state of the body caused by a sharp decrease in the level of sugar (glucose) in the blood and insufficient supply of glucose to the cells of the central nervous system. The most severe manifestation
From the book Beauty and Health of a Woman author Vladislav Gennadievich Liflyandsky From the author's bookOral adsorbents In the human body (in particular, in the blood), in case of violations in the functioning of the liver and kidneys, harmful toxic (toxic) substances are formed and accumulate, which leads to the pathology of other internal organs, for example, to organic damage to the head
From the author's bookFortifying agents. Means that regulate metabolism - Take a pinch of blackthorn flowers and dandelion inflorescences, pour 1 glass of boiling water, let it brew, strain, add 1 tbsp. a spoonful of apple cider vinegar. Drink warm before going to bed.- For a restorative bath
From the author's book From the author's bookHand products For chapped skin Boil 5 potatoes, grind into a pulp, add 5 tbsp. l. milk. Apply warm gruel on the skin and hold for 10 minutes, make an energetic massage. Wash the hands cold water and apply cream. You can just dip your hands into this gruel until
Synthetic hypoglycemic agents differ from insulin in their mechanism of action. More convenient for patients - applied inside. Indicated for type II diabetes (non-insulin dependent). Doses are individual.
Sulfonamides (sulfonylurea derivatives)
Preparations: I generation (practically not used) - CARBUTAMIDE, TOLBUTAMIDE, CHLOROPROPAMIDE; II generation - GLIBENCLAMIDE, GLIQUIDON, GLICLAZIDE, GLIPIZID; Glimepiride is considered a third generation drug.
Sulfonamides activate β-cells pancreas, if any. The sensitivity of β-cells to glucose is restored: drugs block the potassium channels of β-cells; the exit of K + from cells and the process of repolarization are disturbed; the resulting membrane depolarization opens voltage-dependent Ca 2+ channels. Ca 2+ activates the release of insulin into the blood. Extrapancreatic effects include an increase in the number of insulin receptors in tissues and increase their sensitivity to insulin. Most of the effects are due to an improvement in carbohydrate metabolism under the influence of the antidiabetic action of sulfonamides.
I generation drugs CARBUTAMIDE (bucarban, diaboral, oranil) and TOLBUTAMID (butamide) are inactive, cause more side effects (allergization, migraine, dyspepsia, cholestasis, leukopenia, agranulocytosis and, rarely, hypoglycemia). Valid until 12 noon. The daily dose is 2.0-3.0. Carbutamide can cause dysbacteriosis. Chlorpropamide (oradian) is more active; action - up to 36 hours. Can accumulate. Daily dose - up to 0.25. The same side effects. Not prescribed for the elderly. All these drugs are incompatible with alcohol - teturam-like action. Contraindicated in children, in adolescence, during pregnancy and lactation, insulin-dependent diabetes, ketoacidosis, liver and kidney dysfunction, with allergic reactions to sulfanyl- and sulfonamides.
Preparations of II and III generations have hypoglycemic, hypolipidemic, antidiuretic, antiarrhythmic and antithrombotic (anticoagulant) effects. More active drugs of the first generation.
GLIBENCLAMIDE (maninil) is prescribed half an hour before meals, up to 0.02 per day. The most active hypoglycemic drug. Well tolerated. Combined with biguanides (glibomet). GLIQVIDON (glurenorm) has a short effect (up to 8 hours); the most well tolerated drug. May be prescribed for diseases of the liver and kidneys. Daily dose - up to 0.12. GLICLAZIDE (glidiab, diabeton) reduces platelet aggregation and adhesion, preventing microcirculation disorders, including diabetic retinopathy. Indicated for obese diabetics. May be combined with biguanides. Daily dose - up to 0.32 (in 2 divided doses). Glipizide (glibenez) is the fastest acting. Faster excretion (less risk of cumulation). Daily dose - up to 0.03.
Hypoglycemia is possible in case of violation of the dosage and non-compliance with the diet, dyspepsia (nausea, diarrhea), migraine, allergization. Contraindicated in pregnancy and lactation, hypersensitivity, insulin-dependent diabetes, diabetic coma.
GLIMEPIRIDE (Amaryl) is a third-generation drug that does not accumulate. Bioavailable regardless of food intake. Assign 1 time per day. The effect is dose-dependent; lasts up to 24 hours. Daily dose - up to 0.06. Complications and contraindications - as in the appointment of other sulfonamides.
Glibenclamidum, pl. by 0.005
Gliquidonum, pl. by 0.03
Gliclazidum, pl. by 0.08
Glipizidum, pl. by 0.005 and 0.01
Glimepiridum, pl. by 0.001; 0.002; 0.003; 0.004 and 0.006
1. Means of choice for the treatment of cytomegalovirus infection:
3.ganciclovir;
2. Remedy for topical treatment of herpes only:
4.idoxuridine.
3. An agent that inhibits the deproteinization of the viral genome:
3.rimantadine;
Which drug is effective against influenza A and B viruses?
3.oseltamivir;
Specify antiretroviral drugs (for the treatment of HIV infection):
1. azidothymidine, saquinavir;
What is the rationale for combined chemotherapy of HIV infection with protease inhibitors and HIV reverse transcriptase inhibitors?
4. all specified;
Antiviral agents (PVAs) are most effective when treated early because:
2. PVA exhibit a vistatic effect;
8. What drugs are effective against respiratory syncytial viruses and influenza viruses?
3.ribavirin, interferon;
Antifungal agents.
1 . Mechanism of fungicidal action of amphotericin:
1.formation of transmembrane pores;
2. The mechanism of the fungicidal action of fluconazole:
3. inhibition of ergosterol synthesis;
3. An agent for the treatment of systemic mycosis from the group of polyene antibiotics:
1. amphotericin;
4. What drug is used to treat systemic mycoses?
3. amphotericin B;
5. What drug is used to treat gastrointestinal candidiasis?
2.nystatin;
What drugs for the treatment of onychomycosis give the lowest recurrence rate?
3.terbinafine and itraconazole;
7. What oral drug is effective for fungal meningitis (eg, cryptococcal)?
4.fluconazole.
8. Specify an antiherpetic agent:
3. acyclovir;
Antiprotozoal agents.
1. Remedy for stopping an attack of malaria:
4.chloroquine.
2. Remedy for the radical treatment of malaria:
2.primaquine;
3. Means of choice for the treatment of amoebic dysentery, giardiasis, trichomoniasis:
2.metronidazole;
4. The effectiveness of primaquine for the radical treatment of malaria is due to the destruction of:
2. paraerythrocyte schizonts;
Antihelminthics.
1. Means of choice for the treatment of cestodosis:
5. praziquantel.
2. The mechanism of antihelminthic action of levamisole is due to:
2. stimulation of nicotinic cholinergic receptors of neuromuscular synapses of helminths;
3. Means for the treatment of trematodosis:
4. praziquantel.
4. Means for the treatment of extraintestinal nematodes:
1.ditrazine.
5. Levamisole is used to treat:
2.intestinal nematodes
Anti-tuberculosis drugs.
1. Means of the main series for the treatment of tuberculosis:
1.isoniazid
2. Reserve agent for the treatment of tuberculosis:
2.kanamycin;
3. The mechanism of the antimicrobial action of rifampicin is due to the inhibition of:
1.RNA polymerase;
4. The mechanism of antimicrobial action of isoniazid is due to inhibition of:
3.synthesis of mycolic acids;
5. The mechanism of the antimicrobial action of lomefloxacin is due to the inhibition of:
5. topoisomerase II.
Antitumor agents.
1. The mechanism of DNA inactivation by cyclophosphamide is due to:
2. the formation of transverse covalent bonds between DNA strands;
2. Vinblastine disrupts the process of cell division:
2.in the phase of mitosis (M);
3. Methotrexate disrupts DNA synthesis by:
1.inhibition of dihydrofolate reductase;
4. Doxorubicin inactivates DNA by:
3. insertion between adjacent DNA base pairs;
5. Phase-specific action has:
2.fluorouracil;
6. Estrogen Antagonist for Breast Cancer Treatment:
2.tamoxifen;
7. Phazon-specific action has:
2. methotrexate;
8. The effectiveness of antitumor chemotherapy is highest when:
2. acute lymphocytic leukemia;
Hormone preparations of steroid structure.
1. Mark the hormonal preparation of the glucocorticoid group:
2. Specify the variant of specific glucocorticoid therapy:
2. hydrocortisone in Addison's disease;
3. Mark the steroid hormonal drug with mineralocorticoid activity:
3. deoxycorticosterone acetate;
4. Indicate the main effect of mineralocorticoid hormone preparations on metabolism:
3.increased reabsorption of sodium and water;
5. Specify an aldosterone receptor blocker:
4.spironolactone.
6. Mark the indications for prescribing estradiol dipropionate as a means of hormone replacement therapy:
1. ovarian hypofunction
7. Mark the indications for the use of clomiphene citrate:
1. infertility in women;
8. Indicate the indication for the appointment of progesterone:
4. the threat of habitual miscarriage.
9. Mark the indication for medical use of nandrolone (retabolil):
3. extensive injuries, fractures;
10. Indicate the indications for the use of hormonal drugs as means of non-specific (pharmacodynamic) hormone therapy:
2.prednisolone for rheumatoid arthritis;
11. What are the indications for the use of estrogen preparations?
2.osteoporosis, primary and secondary hypogonadism in women, condition after oophorectomy;
12. What is NOT an absolute contraindication to the use of estrogen preparations?
5. breast cancer, endometrial cancer.
13. What are the indications for the use of gestagens?
2. dysfunctional uterine bleeding, recurrent miscarriage, endometriosis, contraception ;
14. What is NOT a medical indication for nandrolone (retabolil)?
4.rapid build-up of muscle mass.
15. What are the complications of non-medical use of anabolic steroids?
5. Answers 1 and 2 are correct.
16. What types of pharmacodynamic effects of glucocorticoids are used in medicine?
6. All are correct except 1.
17. What are the most dangerous side effects of systemic corticosteroids with long-term use?
4. all specified;
18. Which inhaled corticosteroid drug has the lowest risk of systemic adverse effects?
3.beclamethasone propionate;
19. Which glucocorticoid drug has low bioavailability when applied topically (on the skin)?
4.prednisolone hemisuccinate.
20. Which GCS drug is preferable for cerebral edema?
Hormonal preparations of amino acid and polypeptide structure.
1. Specify hormonal drug with antidiuretic action:
1.vasopressin;
2. To note the undesirable property of corticotropin, which is less pronounced in synthetic analogues:
1.allergenicity
3. Which of the following is the essence of the normalizing effect of oxytocin on delivery:
4. amplification of rhythmic uterine contractions with controlled administration in small doses.
4. Mark the indication for the use of vasopressin:
4.diabetes insipidus.
5. Specify an antithyroid agent that suppresses the process of hormone synthesis in the thyroid follicles:
4. methimazole (mercasolil);
6. For the treatment of spasmophilia use:
2. parathyroidin;
7. Which of the hormonal drugs is used for osteoporosis?
1.calcitrin;
8. Choose a hormonal drug for the treatment of type 1 diabetes mellitus (insulin-dependent):
5.insulin.
9. Mark the indication for the appointment of oral hypoglycemic agents:
5. Type II diabetes mellitus.
10. Why hypoglycemic sulfoureas are effective only in diabetes mellitusIItype (insulin-dependent)?
3.because they stimulate insulin secretion;
FSH preparations (follitropins) are used for all of the following indications, EXCEPT:
3.ovarian cancer;
Oxytocin has all the properties EXCEPT:
4. The sensitivity of the uterus is constantly high.
In hypothyroidism, as a means of replacement therapy, the following are used:
3. levothyroxine;
Thiamazole (Mercazolil) as a means of primary (long-term) treatment is indicated for:
3. diffuse toxic goiter;
What are the general properties of oral hypoglycemic agents?
1. in different ways potentiate the effects of insulin;
Specify the typical indications for the appointment of glibenclamide:
4. moderate uncomplicated NIDDM.
Which drug belongs to insulin sensitizers?
4. pioglitazone
How to stop a diabetic coma?
2. in / in 0.1 units / hour short-acting insulin;
What is the most common complication of insulin treatment?
2.hypoglycemia;
What are the acceptable criteria for the effectiveness of insulin therapy?
3.euglycemia, aglucosuria;
- Dignities and clothes of Orthodox priests and monasticism
- Healers and fortune tellers - why do people go to them?
- During confession. Preparing for confession. List of sins for confession. How to dress for confession
- Praise of the Most Holy Theotokos Praise of the Mother of God with an akathist what they pray for