Types of insulin and their classification. Rules for injections

Why does a person need insulin?

Insulin is directly involved in metabolic processes occurring in the human body:

• Sugar, which a person receives from food, thanks to insulin, can penetrate the cells of the body's tissues. It is insulin that makes their membranes more permeable.
• Insulin stimulates the production of glycogen from glucose, which occurs in muscle cells and liver cells.
• Proteins are able to accumulate, synthesize and not disintegrate in the body also thanks to insulin. The hormone helps fat cells take up glucose and transform it into fat tissue. It is for this reason that excessive consumption of carbohydrate foods leads to fat deposits.
• Insulin has an anabolic effect (increases the activity of enzymes that promote the breakdown of glucose), as well as an anti-catabolic effect (prevents other enzymes from dissolving glycogen and fats).

The body needs insulin; it is involved in all processes that occur in it. However, the basic task of this hormone is to ensure normal carbohydrate metabolism. Insulin is the only hormone that can lower blood sugar levels. All other hormones help increase blood glucose levels. We are talking about adrenaline, glucagon, growth hormone.

Insulin begins to be produced by the pancreas after the level of carbohydrates in the blood rises. This happens when the food a person has eaten enters the stomach. Moreover, the food product may contain carbohydrates in a minimal amount. Thus, any food that enters the stomach causes the level of insulin in the blood to begin to rise. If a person is fasting, the level of this hormone begins to fall.

The process of insulin production is also influenced by other hormones, as well as calcium and potassium (if their values ​​increase), fatty acids (if they are present in large quantities in the blood). Somatotropin (growth hormone), on the contrary, helps reduce insulin levels in the blood. Somatostatin has a similar effect, but to a lesser extent.

Insulin levels directly depend on blood glucose levels, so studies aimed at determining them are almost always carried out in parallel. To implement them, you need to donate blood to the laboratory.

Video: Insulin: why is it needed and how does it work?

The mechanism of action of insulin for gaining muscle mass in bodybuilding

In bodybuilding, insulin is used to increase endurance and build muscle mass.

When we eat something sweet, insulin is released by the pancreas and facilitates the penetration of glucose into cells (including muscle cells) for use as energy.

The anabolic properties of insulin are explained by the fact that, in addition to glucose, it provides better delivery of amino acids (= building materials) and some minerals into muscle cells and enhances the synthesis of muscle proteins.

Glucose is an energy molecule. If its concentration in the blood exceeds the body's current need for energy, then it is converted into glycogen. Glycogen is an energy store that is “opened” by the use of glucose in the blood and is used to fuel muscles during exercise.

Dr Sonksen from St Thomas's Hospital in London, in his article on the use of growth hormone and insulin in sports, says: “Since in most sports the performance is determined by the amount of glycogen in the muscles, increasing its content in them directly affects the result.”

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The action of insulin for gaining muscle mass in bodybuilding is explained by the following mechanisms:

Insulin stimulates muscle protein synthesis

Insulin stimulates protein synthesis (and therefore muscle growth).

Muscles are made up of muscle proteins. These proteins are produced by ribosomes. The mechanism of protein synthesis by ribosomes is triggered by insulin. (Ribosomes, according to Wikipedia, are complex molecular machines in which information on how to create a protein is written like a code.)

One of the scientists gives this explanation of the process:

“It’s not entirely clear how, but insulin triggers the ribosomal protein production machine. In its absence, ribosomes simply stop working; it seems to act as a switch.”

Does this mean that insulin “helps” build muscle? No. This means that without insulin this is impossible.

Insulin doesn't just help stimulate muscle growth... without it, it's basically impossible

Insulin inhibits muscle catabolism

Another useful function of insulin in bodybuilding is that it prevents muscle breakdown. Its anti-catabolic function is just as important for mass gain as its anabolic effect.

Every day our body creates and breaks down proteins. To gain muscle mass, it is necessary that more protein be synthesized than destroyed. Insulin helps shift this ratio in the right direction, promoting more efficient delivery of amino acids inside muscle cells.

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Diabetes mellitus type 1 and 2: relationship with insulin

In type 2 diabetes, there is a change in the normal production and functionality of insulin. Most often, the disease manifests itself in elderly people who suffer from obesity. With excess accumulation of fat in the body, the number of lipoproteins in the blood increases. This helps reduce cell sensitivity to insulin. As a result, the body begins to produce it in smaller quantities. The level of insulin in the blood drops, and the level of glucose begins to rise, because there are not enough hormones to utilize it.

If your blood glucose level is elevated, then you need to start following a diet and get rid of fat deposits. In this case, the risk of developing diabetes mellitus is reduced, which means a person can avoid serious health problems.

Type 1 diabetes develops differently. With this type of disease, there is a lot of glucose around the cells, but they cannot absorb it, since there is not enough insulin in the blood for these purposes.

As a result of such disorders, the following pathological changes begin to occur in the body:

• Fat reserves from the reserve are not utilized in the Krebs cycle, after which they are sent to the liver. There, fat takes part in the formation of ketone bodies.
• The higher the blood glucose level, the more thirsty a person is. At the same time, sugar begins to be excreted in the urine.
• Carbohydrate metabolism begins to occur along the sorbitol pathway, which is an alternative pathway. This entails negative consequences, since excess sorbitol begins to accumulate in the tissues. When it accumulates in the eye lens, a person develops cataracts, when it accumulates in nerve fibers - polyneuritis, and when it accumulates on the walls of blood vessels - atherosclerotic plaques.

The body tries to prevent these disorders and begins to break down fats. This entails an increase in triglycerides in the blood and a drop in good cholesterol. Hyperlipidemia contributes to a decrease in immunity, an increase in fructosamine and glycosylated hemoglobin in the blood, and a change in its electrolyte balance. The person begins to feel worse and worse, while he is constantly tormented by thirst and urinates frequently.

Diabetes mellitus affects the functioning and condition of all internal organs, which explains the variety of clinical manifestations of the disease.

Ultra-short insulin

This type of insulin is the fastest acting of all. Its action begins immediately after subcutaneous administration; after 1 hour, the maximum accumulation of the active substance is noted in the body. Moreover, its effect also ends quickly, that is, 3-4 hours after the injection.

The video will tell our readers in more detail what the insulin injection technique should be. By following the rules for administering the drug, a diabetic will eliminate possible consequences such as the development of hypoglycemia.

Ultra-short-acting insulin injections should be given immediately before meals or immediately after. It should be noted that the time of day does not matter.

The onset of action of the ultra-short drug is a few minutes after the injection. The patient feels the maximum effect within an hour. The duration of exposure occurs during the period of food digestion.

In this case, you should pay attention to the pattern: as the dose of the drug increases, the period of exposure increases, but within the limits specified in the instructions. In fact, the effect of the fast hormone lasts up to 4 hours with an administered dose of insulin up to 12 units.

Attention. It is strictly not recommended to administer insulin in a dose exceeding 20 units. With this option, the risk of hypoglycemia attacks increases, because excess hormone is not absorbed by the body and negatively affects the functioning of the body.

Side effects may occur in the patient if the dose of the medicine was incorrectly calculated. It must be said that when calculating the dosage, the doctor conducts a full examination of the patient’s body; the sugar level must be measured using a special algorithm. If the dose of insulin is calculated correctly, then there is no need to be afraid of the body’s reaction.

Attention. One of the most important disadvantages of this method of therapy is the unpredictability and instability of the drug's response to glucose levels. Due to the high potency of the medication, blood glucose levels may drop sharply. 1 unit of ultra-short-acting insulin reduces sugar concentration 2 times faster than the same dose of other types of insulin.

In what cases are ultra-short insulins recommended?

Due to the characteristics of the body, hormonal metabolism can occur quite rapidly, which in frequent cases, both insulin-dependent and non-insulin-dependent diabetics may experience morning attacks of hyperglycemia. This syndrome is not uncommon and cannot be eliminated, so doctors recommend early morning injections of ultra-short insulin in a dose of up to 6 units.

Also, these types of drugs are used with food, as they have a super-rapid effect. However, ultra-short types force the patient to take injections several times a day, imitating natural hormonal synthesis in the pancreas (up to 6 times a day, depending on the number of meals).

Another important circumstance in which these types of drugs are used is the patient’s pre-comatose or comatose state, when the action of rapid insulin is able to compensate for the critical deficiency of the hormone.

Short insulins can compensate for a critical deficiency of the hormone.

Ultra-short-acting insulin preparations

Table No. 3. The most common drugs with ultra-short effects:

Causes of increased and decreased insulin in the blood

The following pathologies can lead to increased insulin levels in the blood:

• Insulinomas are tumor formations of the islets of Langerhans. They produce insulin in large quantities. At the same time, on an empty stomach the level of glucose in the blood will be reduced. To detect a tumor, doctors use a formula to calculate the ratio of insulin to glucose. In this case, the level of insulin in the blood is divided by the level of glucose in blood taken on an empty stomach.
• Early stage of type 2 diabetes mellitus. As the disease progresses, insulin levels will decrease and glucose levels will increase.
• Excess body weight. Sometimes it is the increased level of insulin in the blood that provokes the development of obesity, as a person’s appetite grows, he overeats and accumulates fat. Although it is not always possible to track the cause of obesity.
• Tumor lesion of the pituitary gland (acromegaly). If a person is healthy, insulin helps lower glucose levels. This, in turn, promotes the production of somatotropin. When acromegaly develops, such production does not occur. This feature is used when conducting stimulation tests aimed at determining hormonal balance. When insulin is administered in the form of intramuscular injections, the level of somatotropin does not increase either one or two hours after the injection.
• Hypercorticism. With this disease, there is an increased production of glucocorticoids in the body, which suppress the processes of glucose utilization. As a result, its values ​​remain elevated despite high levels of insulin in the blood.
• Muscular dystrophy. It develops against the background of metabolic disorders, and the insulin level will be increased.
• The period of pregnancy can lead to an increase in insulin levels if a woman overeats.
• Hereditary diseases associated with fructose and galactose intolerance.

If a patient in a hyperglycemic coma is given an injection of fast-acting insulin, this will bring him out of this state. Insulin injections are also used to treat patients with diabetes, since its administration helps reduce blood glucose levels. In this case, the level of insulin itself will be increased in a person.

You can reduce insulin levels if you focus your efforts on treating the underlying disease that leads to disturbances in metabolic processes.

Low insulin levels are observed in type 1 and type 2 diabetes mellitus. In this case, non-insulin-dependent diabetes causes a relative decrease in insulin in the blood, and insulin-dependent diabetes causes an absolute drop in the hormone in the blood. Serious stress, physical activity and other factors that have an adverse effect on the body can also lead to its decrease.

Insulin[edit | edit code]

Historical background[edit | edit code]

Discovery of insulin

- one of the brightest in medicine. The honor of the discovery belongs to Banting and Best, but without the previous work of many researchers it would have been unthinkable. In 1869, German medical student Paul Langerhans noticed that the pancreas consists of two groups of cells - acinous cells that secrete digestive enzymes, and others collected in the so-called islets. Langerhans suggested that islet cells perform some special function. What this function was was only discovered in 1889, when Oskar Minkowski and Joseph von Mehring described a syndrome similar to diabetes mellitus in pancreatectomized dogs (Minkowski, 1989).

This was followed by many attempts to isolate a substance from the pancreas that regulates blood glucose levels. In the early 1900s. German physician Georg Ludwig Zülzer decided to inject an extract from the pancreas into a patient dying of diabetes. The patient felt better, but not for long: when the supply of the extract ran out, he fell into a coma and died. Another attempt to find an antidiabetic factor was made in 1911 by E. L. Scott, a student at the University of Chicago. He treated dogs with experimental diabetes mellitus using an alcoholic extract of the pancreas (by the way, almost the same as that later used by Banting and Best). However, Scott's supervisor found these experiments inconclusive because he did not measure blood glucose levels. From 1916 to 1920, the Romanian physiologist Nicolae Paulescu conducted a series of experiments in which he showed that administering an extract from the pancreas to dogs with experimental diabetes mellitus reduced the content of glucose and ketone bodies in the urine. Despite the fact that these results were published, Paulescu's work was only appreciated many years later.

Unaware of the work of his predecessors, a young Canadian surgeon from Toronto, Frederick G. Banting, in 1921, begged professor of physiology John J. R. McLeod to let him into the laboratory to isolate antidiabetic factor from the pancreas. Banting hypothesized that the hormone (insulin) secreted by islet cells was rapidly destroyed by proteases during or before extraction. Together with Charles G. Best, a fourth-year medical student, he began ligating the pancreatic ducts to avoid proteolysis. After ligation, the acinar cells underwent degeneration, but the islets remained intact, and the antidiabetic factor was extracted from them using ethanol and acid. The resulting extract reduced blood glucose levels in dogs with experimental diabetes mellitus.

The first patient to receive Banting and Best's extract was fourteen-year-old Leonard Thompson (Banting et al., 1922), admitted to Toronto City Hospital with a blood glucose level of 500 mg% (28 mmol/l) and a daily urine output of 3-5 l. Despite a strict diet (450 kcal/day), glucosuria increased, and without insulin the boy would have died in a few months. A trial administration of pancreatic extract resulted in a reduction in blood and urine glucose levels. Then the researchers began to inject the boy with Zxtracg daily, which was followed by immediate improvement. Daily glucose excretion decreased from 100 to 7.5 g. In addition, “the boy became cheerful, stronger and said that he felt much better.” Thus, replacement therapy with a new hormone, insulin, prevented inevitable death from diabetes (Banting et al., 1922). In the following year, Banting and Best were plagued by failure. They were unable to achieve reproducibility of results, that is, to obtain active extracts of the pancreas from time to time. McLeod got involved in solving this problem, and, in addition, Banting turned for help to James B. Collip, a chemist famous for the isolation and purification of adrenaline. Soon the extraction technique was fine-tuned, and patients in North America were able to be treated with insulin isolated from the pancreas of pigs and cattle. Currently, diabetes mellitus is treated with human insulin obtained using genetic engineering methods.

In 1923, with amazing speed, Banting and MacLeod were awarded the Nobel Prize in Physiology or Medicine, and passions immediately began to boil around it. Bunting said he would share his half of the prize with Best. McLeod shared with Call and Pom. The history of the discovery of insulin is described in detail by Bliss (1982).

Determining the level of insulin in the blood - why is it necessary?

Insulin level, as an independent blood indicator in absolute value, has a low diagnostic value. To make a conclusion about a particular disorder in the body, it is necessary to determine the level of glucose in the blood and correlate these two indicators.

The most informative test is the stimulation of insulin production with glucose, or, as it is also called, a stress test. It allows you to diagnose diabetes that has a latent course. In this case, the body’s response to produce insulin will be delayed, its concentration increases slowly, but in the future the level of the hormone will increase significantly. If a person is healthy, then insulin in the blood will increase smoothly.

There is another study that has diagnostic value in terms of determining disorders in the production of insulin in the body. This is a glucose loading test (fasting test). First, blood is taken from the patient on an empty stomach, which is examined for the level of glucose, insulin and the protein part that is part of the proinsulin molecule. Then the person must fast for 24 hours and drink limited water. Every 6 hours, his blood is taken to determine the indicator that raises doubts among doctors, that is, C-peptide, glucose or insulin, or all three substances at once.

In general, insulin levels in the blood do not increase in a healthy person. The exception is pregnant women, which is a normal physiological phenomenon for this condition. In all other cases, insulin levels should remain within normal limits.

If it increases, then this is a reason to suspect the following pathologies:

• A tumor of the pancreas, which is located in the tissues of the islets of Langerhans.
• Hyperplasia of tissues of the islets of Langerhans.
• Disturbances in the production of glucocorticoids in the body.
• Severe disturbances in liver function.
• Early stage of diabetes mellitus.

In some diseases, for example, hypercortisolism, acromegaly, muscular dystrophy, insulin levels are monitored in order to monitor the functioning of the body's internal systems.

Insulin biosynthesis, regulation of insulin secretion

Insulin is synthesized in basophilic insulinocytes (beta cells) of the islets of Langerhans of the pancreas from its precursor, proinsulin. Proinsulin was first discovered by DF Steiner in the late 60s. Proinsulin is a single-chain polypeptide with a relative mol. weighing approx. 10,000, contains more than 80 amino acids. Proinsulin is a P. molecule, as if closed by a peptide, which was called a connecting, or C-peptide; this peptide makes the molecule biologically inactive. According to the immunological characteristics, proinsulin is close to I. Proinsulin is synthesized on the ribosomes of insulinocytes, then the proinsulin molecule moves through the cisterns of the cytoplasmic reticulum to the lamellar complex (Golgi complex), from which newly formed secretory granules containing proinsulin are separated. In secretory granules, under the action of enzymes, C-peptide is separated from proinsulin and I is formed. The process of enzymatic transformation of proinsulin occurs in. several stages resulting in the formation of insulin, intermediate forms of pro-insulin and C-peptide. All these substances have different biol and immune activity and can participate in the regulation of various types of metabolism. Disruption of the processes of conversion of proinsulin into insulin leads to a change in the ratio of these substances, the appearance of abnormal forms of insulin, and as a result of this, to a shift in the regulation of metabolism.

The flow of hormones into the blood is regulated by several mechanisms, one of which for I. (trigger signal) is an increase in glucose in the blood (see Hyperglycemia); an important role in the regulation of I.'s intake belongs to microelements and hormones. tract (mainly secretin), amino acids, as well as c. n. With. (see Hormones).

Donating blood for insulin

To calculate the level of insulin in the blood, you will need to take it from a vein. If insulin is determined in plasma, then the blood is drawn into a tube containing heparin. If insulin is determined in blood serum, then an anticoagulant is not required. The study must be carried out no later than 15 minutes after taking blood for analysis.

For the results to be reliable, a person must fast for 12 hours, cannot take any medications, and should also refrain from physical activity. Provided that it is not possible to refuse to take medications, this must be reflected in the analysis form.

30 minutes before taking blood from a vein, a person should go to the doctor’s office and lie down. He needs to spend this time in a calm and relaxed state. Otherwise, it will not be possible to obtain reliable data.

Insulin therapy

Insulin therapy is a treatment method aimed at eliminating carbohydrate metabolism disorders and is based on the injection of insulin preparations. It is mainly used in the treatment of type I diabetes mellitus, and in some cases for type II diabetes mellitus. Very rarely, insulin therapy is used in psychiatric practice, as one of the methods of treating schizophrenia (treatment with hypoglycemic comas).

In order to simulate basal secretion, long-acting types of insulin are administered in the morning and evening. Short-acting insulin is administered after each meal containing carbohydrates.

Indications for insulin therapy are:

• diabetes mellitus type I;
• diabetic hyperosmolar, hyperlaccidemic coma, ketoacidosis;
• the inability to achieve compensation for carbohydrate metabolism in patients with type II diabetes mellitus with glucose-lowering drugs, diet and dosed physical activity;
• gestational diabetes mellitus;
• diabetic nephropathy.

Injections are given subcutaneously. They are performed using a special insulin syringe, pen syringe or insulin pump. In Russia and the CIS countries, most patients prefer to administer insulin using pen syringes, which provide accurate dosing of the drug and virtually painless administration.

Insulin is administered subcutaneously with a special insulin syringe.

No more than 5% of patients with diabetes use insulin pumps. This is due to the high price of the pump and the complexity of its use. However, administering insulin using a pump provides an accurate imitation of its natural secretion, provides better glycemic control, and reduces the risk of developing short-term and long-term consequences of diabetes. Therefore, the number of patients using pump dispensers to treat diabetes mellitus is steadily increasing.

In clinical practice, different types of insulin therapy are used.

Combined (traditional) insulin therapy

This method of treating diabetes mellitus is based on the simultaneous administration of a mixture of short- and long-acting insulins, which allows reducing the daily number of injections.

Advantages of this method:

• there is no need to frequently monitor blood glucose concentrations;
• therapy can be carried out under the control of glucose levels in the urine (glucosuric profile).

After eating, the concentration of glucose in the blood increases, in response to this, the secretory activity of β-cells increases.

Main disadvantages:

• the need for strict adherence to the daily routine and physical activity;
• the need for strict adherence to the diet prescribed by the doctor, taking into account the administered dose;
• the need to eat at least 5 times a day and always at the same time.

Traditional insulin therapy is always accompanied by hyperinsulinemia, that is, an increased level of insulin in the blood. This increases the risk of developing complications such as atherosclerosis, arterial hypertension, and hypokalemia.

Basically, traditional insulin therapy is prescribed to the following categories of patients:

• elderly;
• those suffering from mental illness;
• with a low educational level;
• those in need of outside care;
• unable to comply with the daily regimen, diet, and timing of insulin administration recommended by the doctor.

Intensive insulin therapy

Intensified insulin therapy imitates the physiological secretion of insulin in the patient's body.

In order to simulate basal secretion, long-acting types of insulin are administered in the morning and evening. After each meal containing carbohydrates, short-acting insulin is administered (simulating post-meal secretion). The dose constantly changes depending on the food consumed.

The advantages of this method of insulin therapy are:

• imitation of the physiological rhythm of secretion;
• higher quality of life for patients;
• the ability to adhere to a more liberal daily routine and diet;
• reducing the risk of developing late complications of diabetes.

Disadvantages include:

• the need to train patients to count XE (bread units) and select the correct dose;
• the need to exercise self-monitoring at least 5–7 times a day;
• increased tendency to develop hypoglycemic conditions (especially in the first months of therapy).

Insulin injections

Insulin is prescribed to people as a medicine for various diseases, the main one being diabetes mellitus.

Many people need insulin. Patients cope with its administration on their own. However, they first receive medical advice. It concerns the correct use of the device, the rules of antiseptics, and the dosage of the drug. All patients suffering from type 1 diabetes are forced to inject themselves with insulin in order to continue living normally. Sometimes the hormone is administered on an emergency basis; this is required when complications of the disease develop and in some other serious conditions. For type 2 diabetes mellitus, it is possible to replace injections with oral medications. The fact is that this type of disease requires the administration of insulin only when it is severe. Therefore, if complications develop, a person simply does not have the skills to administer insulin intramuscularly. It's easier for him to take a pill.

Insulin solution, which is based on human insulin substance, is a safe and effective remedy that produces a small number of side effects. The hypoglycemic hormone produced by the pig pancreas has the greatest similarity to human insulin. This is what has been used for many years to treat people. Modern medicine offers people insulin, which was obtained through genetic engineering. If a child needs therapy, he will receive exclusively human insulin, not animal insulin.

The introduction of the hormone allows you to maintain a normal level of glucose in the blood, preventing it from rising and falling to critical levels.

Depending on the person’s disease, his age and the presence of concomitant pathologies, the doctor selects the dose for him individually. The patient must be given full instructions on how and at what time he needs insulin injections. In addition, a person must adhere to a special diet, which is also agreed upon with the doctor. The daily routine, nature and intensity of physical activity should be changed. Only if all these conditions are met can therapy be made effective, which will help improve the quality of life.

Are there insulin analogues? Previously, in Russian clinical practice, only original analogues of foreign-made insulin were used, such as, for example, Humalog (Eli Lilly, insulin lispro), Lantus (Sanofi, insulin glargine), Novorapid (Novo Nordisk, insulin aspart) and others, but now analogues have appeared Russian production. So, for example, the following drugs were registered: RinLiz (replaces Humalog), RinLiz Mix 25 (replaces Humalog Mix 25), RinGlar (replaces Lantus).

These drugs are convenient for the patient to use because they provide a stable effect and the required duration of action and have fewer side effects.

Indications for use

The main area of ​​application of insulin is endocrinology. The hormonal drug is prescribed for therapeutic purposes to patients with established type I diabetes mellitus (insulin-dependent). Insulin can also be prescribed in case of autoimmune attacks on the body in type II diabetes mellitus.

Short-acting insulin, which remains active for 6 hours, is prescribed as part of complex therapy to lower blood sugar in certain diseases:

• Schizophrenia.
• Thyrotoxicosis.
• Chronic hepatitis.
• Stages 1-2 of liver cirrhosis.
• Stomach diseases.
• Furunculosis.

A special place is given to the drug in the treatment of general exhaustion, if it is necessary to restore the patient’s normal nutrition. In these cases, the anabolic effect of insulin is important, which helps to gain body weight.

In cardiological practice, insulin is used as part of polarizing mixtures. The solution is administered intravenously for spasm of the coronary vessels, leading to coronary insufficiency.

Insulin in bodybuilding

What happens to a healthy person after an insulin injection? This question can be answered by considering the practice of using hormonal drugs in a sports environment. Athletes use short-acting insulin in combination with anabolic and androgenic agents. The pancreatic hormone helps increase the permeability of cell membranes of muscle tissue. This facilitates easier and faster penetration of anabolic steroids into the muscles. In combination with insulin, lower dosages of steroids are required to achieve a pronounced effect than with solo courses.

To safely use insulin in bodybuilding, it is important to follow certain rules:

1. Don't overeat. In the body, excess nutrients are transformed into fat deposits.
2. Reduce the content of simple carbohydrates in your daily diet.
3. Assess muscle growth using a measuring tape and a mirror, rather than by weighing yourself. Measurements of the volume of the biceps, thighs, and lower legs will indicate the effectiveness of insulin injections. An incorrectly calculated dose of the drug will lead to the formation of fat folds, for example, in the abdominal area.

Contraindications

The use of insulin is prohibited for diseases that are accompanied by hypoglycemia:

• Acute form of hepatitis.
• Cirrhosis of the liver.
• Hemolytic jaundice.
• Pancreatitis.
• Nephritis.
• Amyloidosis.
• Decompensated forms of heart defects.
• Peptic ulcer of the stomach and duodenum.

For some diseases, the prescription of insulin requires additional research in order to minimize possible negative consequences. Certain control and caution must be observed when prescribing the drug to patients with the following pathologies:

1. Forms of diabetes mellitus, accompanied by signs of coronary insufficiency and cerebrovascular accident.
2. Thyroid diseases.
3. Kidney failure.
4. Addison's disease, which affects the adrenal glands, develops adrenocortical insufficiency.

Side effects

Insulin is administered subcutaneously, and therefore the most common negative symptom is lipodystrophy, a pathological condition characterized by atrophy or excessive growth of adipose tissue in the injection area.

The insulin preparations that are currently available go through several levels of purification. These measures significantly reduce the risk of allergy symptoms. If allergic reactions develop, the drug used is discontinued, emergency hyposensitizing therapy is carried out and another type of insulin is selected.

Overdose

Failure to comply with doctor's instructions or exceeding the therapeutic dose always causes the development of hypoglycemia. In this condition, blood sugar levels decrease rapidly, which can lead to the death of the patient. An excessively high dose of insulin requires prompt medical intervention.

Clinical signs of hyperglycemia:

• Thirst.
• Frequent urination.
• Fatigue.
• Dryness of the oral mucosa and skin.
• Itching.
• Visual impairment, feeling of a veil before the eyes.
• Disorder of consciousness.
• Heart rhythm disturbance.
• Prekoma.
• Coma.

An overdose of insulin poses a danger to a person’s brain activity, and this is especially dangerous for older patients. The development of paralysis and paresis is possible. High doses of insulin affect the elasticity of vascular walls, which affects proper cerebral circulation.

At the first signs of a drop in sugar, the patient is offered sweet tea, fruit juice or honey.

For coma, intensive therapy consists of intravenous administration of 10-20 ml of 20% or 40% glucose solution.

Another treatment regimen is allowed:

• 1-2 mg of glucagon (insulin antagonist) - intramuscularly.
• 0.5 ml of 0.1% solution of adrenaline hydrochloride - subcutaneously.
• 150 ml of 10% glucose as an enema.

Interaction with other drugs

The effectiveness of insulin increases with simultaneous treatment with certain medications:

• alpha-blockers.
• Acetylsalicylic acid.
• Clofibrate.
• Fluoxetine.
• MAO inhibitors.
• Cyclophosphamide.
• Tetracycline.
• Ifosfamide.

The ability of insulin to lower blood sugar is observed when it is combined with certain drugs:

• Oral contraceptives.
• Chlorprothixene.
• Glucocorticosteroids.
• Diazoxide.
• Heparin.
• Lithium carbonate.
• Saluretics.
• Nicotinic acid.
• Thyroid hormones.
• Diphenin.
• Symptomimetic agents.
• Tricyclic antidepressants.

Terms of sale

Insulin drugs are available by prescription. The endocrinologist must write a prescription in Latin.

How to store insulin?

The best place to store insulin is in the refrigerator door. Optimal conditions are observed here - darkening, temperature from +2 to +8°C. Insulins of any type must not be frozen or heated. At temperatures above +35°C, the drug loses all medicinal properties. Patients who maintain an active, sporty lifestyle often use a thermal bag to store insulin.

Best before date

The expiration date on the packaging and bottle must match. It is 2 years from the date of release of the drug. If an opened bottle of insulin is stored under all conditions, it can be used for a month.

How can you tell if your insulin is bad?

If storage rules are not followed, the drug cannot be used. It is forbidden to inject an insulin solution that has changed color or in which any suspensions, fibers, or lumps have formed. If, when shaking the bottle with the suspension, no whitish suspension is observed, then the drug should be considered spoiled. Transparency is a sign of quality for ultra-short, short-acting and rapid-acting insulins. Extended-release insulin glargine should remain clear.

Conversion of insulin in the body

When part of the blood enters the bloodstream, it forms complexes with blood plasma proteins—the so-called. bound insulin, the other part remains in the form of free insulin. L.K. Staroseltseva et al. (1972) established that there are two forms of bound I.: one form is a complex of I. with transferrin, the other is a complex of I. with one of the components of blood serum alpha globulins. Free and bound I. differ from each other in biological, immune and physical-chemical properties. properties, as well as the effect on adipose and muscle tissue, which are target organs and are called insulin-sensitive tissues. Free I. reacts with antibodies to crystalline P., stimulates the absorption of glucose by muscle and, to some extent, adipose tissue. Bound glucose does not react with antibodies to crystalline glucose, stimulates the absorption of glucose by adipose tissue and has virtually no effect on this process in muscle tissue. Bound I. differs from free metabolic rate, behavior in the electrophoretic field, during gel filtration and dialysis.

When extracting blood serum with ethanol hydrochloride, a substance was obtained that had biol effects similar to I. However, this substance did not react with antibodies obtained to crystalline Insulin, and therefore was called “unsuppressed insulin-like plasma activity”, or “insulin-like substance”. Great importance is attached to the study of insulin-like activity; “unsuppressed insulin-like plasma activity” is considered by many authors as one of the forms of insulin. Thanks to the processes of binding of insulin to blood serum proteins, its delivery to tissues is ensured. In addition, bound And. is, as it were, a form of storage of the hormone in the blood and creates a reserve of active And. in the bloodstream. A certain ratio of free and bound oxygen ensures the normal functioning of the body.

The amount of iodine circulating in the bloodstream is determined not only by the rate of secretion, but also by the rate of its metabolism in peripheral tissues and organs. The most active metabolic processes occur in the liver. There are several assumptions about the mechanism of these processes in the liver; It has been established that there are two stages: reduction of disulfide bridges in the insulin molecule and proteolysis with the formation of biologically inactive peptide fragments and amino acids. There are several insulin-activating and insulin-degrading enzyme systems involved in the metabolism of insulin. These include the insulin-activating enzyme system [protein disulfide reductase (glutathione)] and the insulin-degrading enzyme system, which is represented by three types of proteolytic enzymes. As a result of the action of protein disulfide reductase, the restoration of S-S bridges and the formation of A- and B-chains of protein occurs, followed by their proteolysis to individual peptides and amino acids. In addition to the liver, I.'s metabolism occurs in muscle and fatty tissues, kidneys, and placenta. The rate of metabolic processes can serve as a control over the level of active insulin and plays a large role in the pathogenesis of diabetes mellitus. The biol half-life of human I. is approx. 30 min.

What types of insulin are there?

There are several types of insulin. It will need to be administered at different times of the day.

• Humalog and Novorapid are ultra-short-acting insulin preparations. Insulin of this type begins to act after 15 minutes, the maximum effect of hormones can be expected after 1-1.5 hours, and 4 hours after its administration there will be no insulin in the blood.
• Insuman Rapid, Actrapid NM, Humulin Regulator are short-acting insulins. The effect of the drug administration occurs within 30-45 minutes. Its effect can last up to 8 hours. The maximum effect should be expected after 2-4 hours.
• Humulin NPH, Insuman Bazal, Protafan NM are medium-duration insulins. The effect of their administration will occur in 1-3 hours, and they will act from 10 to 20 hours. Peak values ​​of the hormone in the blood are reached 6-8 hours after administration.
• Insulin Glargine (Lantus) is a long-acting drug, the effect of which lasts for 20-30 hours. This hormone does not reach peak values, being distributed evenly throughout the entire duration of its action.
• Insulin Degludec is an ultra-long-acting drug whose effect can last for 42 hours. This drug is produced in Denmark.

The last two types of insulin are sufficient to be administered once a day. In emergency cases, they are not used, since their effect does not occur immediately, but after several hours. Therefore, when a coma develops, a person is given ultra-short-acting insulin.

Video: types of insulin used to treat diabetes:

Injections must be administered either under the skin or into the muscle. Information on this matter should be obtained from a doctor. The doctor gives instructions regarding the rules for mixing drugs, as well as the time of their administration, depending on meals. The diet for diabetes mellitus must be strictly followed, since the timing of injections and their dosage directly depends on this.

Introduction[edit | edit code]

This article focuses on the pharmacological actions of insulin, glucagon, somatostatin and oral hypoglycemic agents. The discovery of insulin in 1921 revolutionized medicine by providing a treatment for insulin-dependent diabetes mellitus (type I diabetes mellitus), a disease that was considered incurable. The first part of the chapter describes the physiological effects of insulin and its mechanisms of action; This justifies the role of this hormone in the treatment of diabetes mellitus. The next part describes the pharmacodynamics and pharmacokinetics of insulin preparations, discusses the advantages of intensive insulin therapy and its role in the prevention of chronic complications of diabetes mellitus. The following describes the pharmacological properties of oral hypoglycemic agents, without which it is unthinkable to treat non-insulin-dependent diabetes mellitus (type II diabetes mellitus), the most common form of the disease. The chapter ends with a discussion of the physiology and pharmacology of glucagon and somatostatin. Particular attention is paid to the increasingly widespread use of somatostatin analogues in clinical practice.

Instructions for using insulin

Specifics of insulin administration

Insulin is administered by subcutaneous, intramuscular or intravenous injection. Only short-acting drugs can be injected into a vein for certain medical indications - hyperglycemic coma or pre-comatose state.

Insulin in suspension form is used exclusively intramuscularly. Injecting the drug into a vein is prohibited! Before administration, the insulin ampoule is warmed to room temperature for faster absorption. For insulin injections, a plastic syringe is used, which has virtually no “dead space”, unlike glass instruments. A set of the drug in a plastic syringe ensures that the exact dosage is maintained.

Experienced diabetics prefer syringe pens into which cartridges with insulin solution are installed. The main advantage of these syringes is that the solution does not need to be drawn up before each injection. They can be used for injections of short-, medium- and combined-acting drugs. The needles of insulin syringes are small in size - length 8 -12 mm, thickness 0.3 - 0.4 mm. These features help minimize pain during injections.

Insulin injection areas

With the question: “Where should I inject insulin?” Patients with a newly diagnosed diagnosis and relatives of patients turn to an endocrinologist. The fastest way for the hormonal drug to enter the bloodstream is when administered subcutaneously in the area of ​​the anterior abdomen. The outer upper arm and anterior thigh area are suitable for subcutaneous injections, but absorption is slower here. The slowest absorption occurs when insulin is injected into the subscapular region or into the subcutaneous fat of the buttocks.

The preferred area for subcutaneous insulin injection depends on the type of drug. Short-acting solutions are transparent. They must penetrate the blood quickly, so the front surface of the abdomen is suitable for injections, except for the area around the navel. Long-acting insulin is produced as a cloudy solution. Its slow absorption allows for administration into the surface of the thigh and buttocks.

The patient must follow a strict sequence of changing injection sites. A specific area must correspond to a specific time of day. A morning injection of short-acting insulin can be performed in the abdomen, an afternoon injection in the thigh, and an evening injection subcutaneously in the buttock area. This rule is due to the need to calculate XE (bread units) for different times of the day.

Rules for subcutaneous insulin administration

1. Check the validity period of the drug, type, dosage on the bottle.
2. Wash your hands with soap and treat the injection site with an antiseptic solution.
3. Heat the bottle with the solution in your hands to the optimal temperature. Do not shake the preparation under any circumstances to prevent the formation of air bubbles.
4. Treat the bottle cap with an alcohol solution.
5. Air is drawn into the syringe as much as the required units of the drug. Release it into the bottle and collect the required amount of insulin (in units). Considering the features of the syringe, you can draw a little more solution, about 10 units.
6. Adjust the dose by fixing the syringe at eye level.
7. In order to remove air bubbles, lightly tap the body of the syringe.
8. When injecting the drug, count to 5 or 10 and remove the needle. Massaging the injection site is strictly prohibited! Massage promotes rapid absorption, and too active absorption can cause hypoglycemia.

It is not recommended to treat the surface of the skin with an alcohol solution. Ethyl alcohol destroys insulin, which after its administration can cause lipodystrophy. Before injection, it is enough to wash and dry the corresponding area of ​​skin with a napkin, if necessary. In certain cases, insulin is administered through clothing.

For the injection, choose a place 2.5 cm from the navel or 3 cm from the shoulder, thigh, upper gluteal region. If the injection site is the shoulder or thigh, use your thumb and index finger to form a triangle from the skin, without grasping the muscle. The needle is inserted into the base of the formed triangle with an upward cut at an angle of 45°. It is important to ensure that the needle does not enter the muscle layer, since absorption of the drug here occurs much faster than from subcutaneous fat. For an injection in the stomach or buttock, it is not necessary to form a fold. In this case, the needle is inserted at an angle of 90°

The optimal time for insulin injections is 30 minutes before meals. This is due to the fact that the drug is absorbed into the blood within an hour. The best time to eat is 15-30 minutes after the injection.

How to choose the best insulin?

It is impossible to give a general answer to this question. The selection of insulin, the selection of dosage and the method of its administration is carried out by the treating endocrinologist during the patient’s hospitalization. This takes into account the clinical symptoms of the disease, the severity of the patient’s condition, the time of appearance of signs of a decrease in glucose levels, and the duration of the glucose-lowering effect.

Rules for calculating the dose and administration of insulin

For each patient, the dose of the drug is selected individually. Short-acting insulin begins to act very quickly, but the drug effect lasts for a short time. The solution can be administered both subcutaneously and intramuscularly. In some cases, intravenous injections are indicated.

Short-acting insulin can be injected once or several times a day. The number of injections depends on the clinical picture of diabetes. The injection is given 15-20 minutes before a meal. After this time, a sugar-lowering effect begins to appear, the peak of which is recorded after 2 hours. Its duration is approximately 6 hours.

Scope of application of short-acting insulin:

1. In a hospital setting.

   When selecting the required therapeutic dose in case of hyperglycemic coma, precoma. The precomatose state is urgent to change the patient's insulin activity.

2. In combination with a course of anabolic drugs.

   The dosage in this case is 4-8 units 1-2 times a day. The amount of insulin is minimal and cannot cause any serious consequences.

Long-acting insulins are divided into several types, depending on the duration of the effect:

• Semilong.
• Long.
• Ultralong.

Injections of long-acting drugs are performed much less frequently, due to the fact that the therapeutic effect lasts from 10 to 36 hours.

The long-acting drug is available in the form of a suspension. It is injected only subcutaneously, intramuscularly. Intravenous administration of long-acting insulin is prohibited. Due to its pharmacological characteristics, this type of insulin is not used during coma or precoma.

When selecting a drug, the doctor takes into account the time of maximum glucose-lowering effect. It is at this time that you need to eat. If necessary, mixing two long-acting drugs in one syringe is allowed.

The combined administration of long-acting and short-acting insulin is necessary when the patient needs to maintain optimal sugar levels for a long time. A combination of drugs with different effects is used to quickly normalize blood glucose. Long-acting insulin is usually recommended for morning injections. The injection is given in the morning, before breakfast. In some cases, long-acting medications can be given at other times of the day.

Patients with diabetes must adhere to a special diet. This requirement is mandatory when treating with insulin. The calorie content of food depends on the patient’s weight and lifestyle. If the patient is underweight, but at the same time there is daily physical activity, at least 3000 kcal per day should be supplied to the body along with food. Excess weight and a sedentary lifestyle means consuming no more than 1700-2000 kcal.

How to draw medicine into an insulin syringe?

Correctly drawing one type of insulin into a special syringe is not particularly difficult. To do this, you need to do several sequential steps:

1. Fill the syringe with air until the required number of units of the drug is marked.
2. Puncture the cap of the bottle and release air from the syringe inside.
3. Holding the bottle upside down at eye level, draw a little more than the required amount of the drug into the syringe.
4. In order to remove the formed air bubbles, lightly tap the syringe barrel with your finger and move the piston to the desired mark.

To correctly draw insulin from the bottle, a puncture must be made in the center of the stopper, preferably with a needle from a regular syringe. All subsequent steps are performed with an insulin syringe, inserting a needle into the previously made puncture.

Insulin dose calculation

According to the rules for calculating the drug, the daily dosage should be no more than 1 unit per kilogram of the patient’s weight. The therapeutic dose depends on the type of disease and the characteristics of the clinical picture.

For type I diabetes, the following recommendations have been developed:

• 0.5 IU per 1 kg - in the case of a newly diagnosed disease;
• 0.6 units per 1 kg - with compensation within 12 months;
• 0.7 units per 1 kg - with unstable compensation;
• 0.8 units per 1 kg - for decompensation;
• 0.9 IU per 1 kg - complicated course of the disease, phenomena of ketoacidosis;
• 1.0 units per 1 kg - for women in late pregnancy.

In order not to make a mistake in dosage calculations, you can consider one of the examples. If a patient needs to be administered long-acting insulin at a dose of 0.6 units with a weight of 75 kg, then the volume will be 0.6 x 75 = 45. Half of the resulting amount is taken, rounded down, i.e. the dose is 20 units. In the morning, before breakfast, 12 units are administered, before dinner - 8 units.

Short-acting insulin with the same parameters (weight 75 kg, dose 0.6 units) is calculated according to the rule: 0.6 x 75 = 45, 45 - 20 = 25. For a morning injection, take 9-11 units, before lunch - 6- 8 units, in the evening - 4-6 units.

Medium insulin Protafan, Humulin NPH and others

Types of intermediate-acting insulin that are registered and used in the Russian Federation:

• Protafan HM
• Humulin NPH
• Insuman Bazal GT
• Biosulin N
• Insuran NPH
• Gensulin N
• Rinsulin NPH
• Rosinsulin S
• Khumodar B 100 Rec
• Vozulim-N
• Protamine-insulin ChS.

The source of the list is algorithms for specialized medical care for patients with diabetes mellitus, edited by I.I. Dedova, M.V. Shestakova, A.Yu. Mayorova, 9th issue, 2020.

Average insulin begins to act approximately 2 hours after the injection. Unlike long-acting insulins, it has a pronounced peak after 6-10 hours. This is his flaw. The effect of an average insulin injection ends after 12-16 hours. Diabetics who are on a low-carb diet inject their insulin doses much lower than generally accepted. In such doses, injections of average insulin stop working earlier, after approximately 8 hours.

Dr. Bernstein doesn't recommend using intermediate insulin, but you need to know about these drugs because they are quite popular. Medium insulin is most often called protafan. NPH stands for Neutral Protamine Hagedorn. This is an animal protein that is added to slow down the action. It creates many problems for diabetics.

Why you should not use intermediate insulin:

1. A pronounced peak is a big drawback. The stable and smooth action that long types of insulin have is better.
2. Hagedorn's neutral protamine often causes allergic reactions.
3. Many diabetics sooner or later need to undergo x-rays using a contrast agent to examine blood vessels. During this examination, patients who injected Protafan experience severe allergic reactions, often with loss of consciousness and even death.
4. Diabetics who follow a low-carb diet usually use low doses of insulin. In such low doses, protafan acts for no more than 8-9 hours. It doesn't last all night and all day.

Medium insulin Protafan HM, Humulin NPH, Insuman Basal GT and others should not be injected, even if they are issued with free prescriptions, and other extended-release drugs will have to be purchased at your own expense.

Formation and mechanism of action

The main impetus for the production of insulin by the pancreas is an increase in glucose in the blood plasma. The function of the hormone is quite extensive, mainly affecting metabolic processes in the body, promoting the formation of glycogen and normalizing carbohydrate metabolism. In order to understand the action of insulin, you should familiarize yourself with its formation

Education

The process of hormone formation is a complex mechanism that consists of several stages. First of all, an inactive precursor peptide (preproinsulin) is formed in the pancreatic islets, which, after a series of chemical reactions during maturation, acquires an active form (proinsulin).

Proinsulin, transported to the Golgi complex, is converted to the hormone insulin. Secretion occurs throughout the day in a continuous mode.

Table No. 3. The norm of insulin in the blood, taking into account the age and category of persons:

A stimulating factor for insulin production is food intake (especially sweets). At the same time, additional stimulants appear, such as:

• sugar;
• amino acids (arginine, leucine);
• hormones (cholecystikin, estrogen).

Hyperfunction of insulin production is observed with increasing concentrations in the blood:

• potassium;
• calcium;
• fatty acids.

A decrease in the function of hormone production is observed with an increase in the level of hyperglycemic hormones (glucagon, adrenal hormones, growth hormone), since their excess content contributes to an increase in glucose levels.

Glucose regulation

As we have found out, insulin begins to be intensively produced by β-cells every time food is consumed, that is, when a significant amount of glucose enters the body. Even with a decrease in glucose intake, β-cells never stop normal secretion of the hormone, but when glucose levels drop to critical levels, hyperglycemic hormones are released in the body, which contribute to the entry of glucose into the blood plasma.

Attention. Adrenaline and all other stress hormones significantly suppress the flow of insulin into the blood plasma.

Table No. 4. Normal glucose level:

Plasma glucose levels rise for a short time immediately after eating.

The continuity of the complex mechanism of insulin production and action is considered the main condition for the normal functioning of the body. Prolonged levels of elevated levels of glucose in the blood (hyperglycemia) are the main symptom of diabetes mellitus.

But the concept of hypoglycemia refers to a prolonged level of low glucose in the blood, accompanied by serious complications, for example, hypoglycemic coma, which can lead to death.

The most dangerous consequence of diabetes is hypoglycemic coma.

Action of insulin

Insulin affects all metabolic processes in the body, but its main effect is on carbohydrate synthesis, this is due to an increase in the function of glucose transport through cell membranes. Activation of the action of insulin triggers the mechanism of intracellular metabolism, in which a supply of glucose is transported through cellular tissues into the blood plasma.

Thanks to insulin, glucose is sent in a modified form (glycogen) to two types of tissue:

• muscle (myocytes);
• fat (adipocytes).

Together, these tissues make up 2/3 of the entire cell membrane of the body; they perform the most significant functions. This:

• breath;
• movement;
• energy reserve;
• blood circulation, etc.

Effects of insulin

In the body, insulin is important in metabolic processes and energy reserves. Insulin is the main hormone that helps normalize plasma glucose levels. It has many effects aimed at promoting the activity of certain enzymes.

Table No. 5. Effects of insulin:

Insulin sends glucose into liver cells in a modified form, like glycogen.