Go Insulin | Insulin preparations for injection
Go

Insulin

Insulin is a protein hormone produced by the cells of the islets of Langerhans in the pancreas. Insulin increases the penetration of glucose into body tissues and its use by them, accelerates the conversion of carbohydrates to fatty acids , reduces the glycogen content in the liver and increases its amount in muscles. An increase in the blood sugar level (caused, for example, by the introduction of glucose, adrenaline , glucagon) leads to a regulatory release of insulin. When pancreas endocrine dysfunction occurs, diabetes mellitus occurs (see Diabetes mellitus), manifested in an unregulated rise in blood sugar ( hyperglycemia ) and the appearance of sugar in urine (glycosuria). See also Hormones.

Insulin preparations ( Schedule B ) for medical use are obtained from the pancreas of cattle. Insulin activity is determined biologically and is expressed in units of action (AU) or international units (i. E.).

Insulin for injection (Insulinum pro injectionibus) is available as an aqueous solution of crystalline insulin acidified with hydrochloric acid (pH of the solution 3.0-3.5). 1 ml of solution contains 40 or 80 IU of insulin. The action of the drug insulin begins after 30 minutes. after the introduction and reaches a maximum in 2-4 hours; effect duration 6-8 hours.

The drugs are used mainly for the treatment of diabetes. Treatment of diabetes involves the use of insulin on the background of an appropriate diet. Along with the treatment of diabetes, the drug is used in case of nutritional decline, damage to the liver parenchyma (at the same time glucose is prescribed), to eliminate vomiting of pregnant women, in psychiatric practice (insulin shock). Introduce the drug under the skin, intramuscularly, and in diabetic coma and intravenously.

Go

By adding zinc , protamine (protein) and buffer to insulin, prolonged (prolonged) action preparations were obtained. For example, insulin-protamine suspension (Suspensio insulini-protamini) begins to have a sugar-reducing effect in 2-4 hours, the effect reaches a maximum in 8-12 hours. and lasts 18-24 hours; a suspension of protamine zinc insulin (Suspensio protamini-zinci-insulini) and a suspension of crystalline zinc-insulin (Suspensio zinci-insulini crystallisati) begin to have an effect after 3-6 and 6-8 hours, their effect reaches a maximum after 14-20 and 16-20 hours and the whole lasts 24-36 and 30-36 hours.

Long-acting drugs are used only for the treatment of diabetes mellitus in moderate or severe forms of the disease; with diabetic coma, pre-comatose states, tendencies to the appearance of ketoacidosis, prolonged-action drugs are contraindicated - in these cases, regular insulin is used for injections. Introduced drugs prolonged action only under the skin, their injections are less painful than injections of regular insulin (since the pH is close to neutral). These drugs can be administered to patients less often than insulin for injection, which facilitates the treatment of patients with diabetes. Domestic drugs prolonged action in 1 ml contain 40 IU of insulin. See also Insulin Therapy .

Insulin (Insulinurn) is a hormone of β-cells of the pancreatic islets of Langerhans, which has a sugar-lowering property. Molecular weight 6000. Contains, in addition to carbon, oxygen, hydrogen, nitrogen and sulfur, zinc. In the construction of the molecule involved 16 different amino acids. Insulin is the first protein in which structure is established. Optically inactive, rotates the plane of the polarized beam to the left, soluble in a weakly acidic and alkaline medium, as well as in 80% alcohol.

Insulin for therapeutic purposes is obtained from the pancreas glands of cattle and pigs. The glands are crushed, insulin is extracted with acidified ethyl alcohol, which inactivates the proteolytic enzymes of the pancreas, and then the hormone is precipitated from the solution with various reagents. Dried insulin is diluted in water, acidified with hydrochloric acid, preserved with a 0.3% solution of tricresol or phenol.

The sugar-lowering activity of insulin is standardized by lowering the blood sugar level of gray rabbits after subcutaneous administration. For 1 U of insulin they take such a quantity that, after administration to a rabbit weighing 2 kg and starving for 24 hours, causes a decrease in blood sugar for 4 hours from the moment of administration to 45 mg%.
1 U insulin contained in 0,04082 mg drug.

The insulin solution is a clear, colorless liquid with the smell of a preservative, contains 1.6-1.8% glycerin, pH 2.5-3.5.

The drug is administered into the body under the skin or intramuscularly. Intravenous administration does not have any advantages over these methods of administration. The introduction of insulin inside does not cause a decrease in blood sugar levels, since it is destroyed under the influence of proteases of the gastrointestinal tract. The introduction of the drug through the rectum and nasal mucosa is also ineffective.

Pharmacological action . Systematic administration of insulin in diabetes mellitus is a replacement therapy. With subcutaneous administration of the drug, a decrease in blood sugar occurs in 15-30 minutes, the maximum decrease in the amount of sugar in the blood occurs in 2.5-5 hours. After 6-8 hours, blood sugar comes back to the initial level.

The effect of insulin is aimed at enhancing the synthesis of blood glucose into muscle glycogen, at reducing glycogenolysis and glycogenesis in the liver. Insulin causes hypoglycemia by reducing the supply of sugar from the liver to the blood, partly due to an increased transfer of sugar to brain tissue, heart muscle, the intestinal wall. The latter process may be associated with an increase in the permeability of the cellular elements of these organs to carbohydrates under the influence of insulin. In the presence of insulin, a more complete use of glucose occurs. This action may be due to the enhanced formation of a coenzyme carboxylase related to carbohydrate metabolism, since insulin promotes thiamine phosphorylation. Insulin increases glycogen formation in the liver, reduces glycogenolysis and neoglycogenesis. Under the influence of insulin, the secretion of sugar from the liver to the blood sharply decreases and insulin hypoglycemia occurs.

The course of this process is influenced by the initial sugar content in the blood. Insulin leads to the deposition of glycogen in cases where it is injected with a large amount of sugar or under the influence of existing hyperglycemia. Under the influence of insulin, a sharp decrease in the release of ketone bodies by the liver and lungs is noted with the termination of ketonuria.
1 IU insulin contributes to the absorption of about 4.0 grams of sugar.

Go

Indications . Diabetes. Acute and chronic parenchymal hepatitis. Peptic ulcer and duodenal ulcer. Croupous pneumonia. Exhaustion. Furunculosis. The decline of power. Toxicosis of pregnancy. Pituitary dwarf growth.

In the case of a hyperglycemic coma, the administration of insulin is a vital indication. Early insulin therapy (up to 6 hours from the beginning of a coma) can give a 100% favorable outcome.

Vital indication is insulin therapy and with complications of diabetes mellitus with sepsis, local suppurations, furunculosis, gangrene, injuries, as well as with radiotherapy, surgical interventions, childbirth, with a decrease in the patient's nutrition, infections, intoxication, acidosis.

Insulin is used in severe and moderate forms of diabetes. In cases of a mild form of the disease, periodic use of the drug provides temporary support for the pancreas and causes its possible regeneration and rest under conditions of more normal metabolism.

The insulin dose is individualized depending on the patient's condition, sugar content in the urine (from a rough calculation of 1 IU per 3–5 g of sugar excreted in the urine). Doses of insulin in diabetes mellitus usually exceed 20-40 U per day. They are changed under the control of blood sugar and urine. When hyperglycemic coma doses in some cases, exceed 1000 IU per day.

In diabetes, insulin is administered from 1 to 3 times per day. If the daily dose of insulin required to reduce glycosuria and hyperglycemia exceeds 32 U, it is recommended that it be divided into two injections to avoid hypoglycemic events, with daily doses of 60-80 U or more, three injections have to be taken.

The introduction of the drug is made 20-40 minutes before a meal so that the optimum of its action fell at the height of digestion. Before breakfast, when the most carbohydrates are usually injected, it is advisable to prescribe about half of the total dose of insulin; the rest is entered before lunch and dinner.

The effectiveness of insulin in other diseases is manifested in the regulation of metabolic processes, primarily carbohydrate metabolism, better use of carbohydrates introduced from outside, assimilation of food with a maximum caloric coefficient, stimulation of the function of the digestive tract, water retention in tissues as true absorption, because the fluid fixed by tissues becomes part of protoplasm.

The introduction of insulin contributes to weight gain in individuals with constitutional asthenia, who suffer from reduced appetite, in patients with thyrotoxicosis, neurosis, and recovering from past infectious diseases.

At the same time, it is necessary to establish the exact cause of weight loss, since in case of suspected hypofunction of the adrenal cortex, the use of insulin is prohibited.

Treatment usually begins with 4-6 IU for 20-30 minutes before a meal. At the same time, they find out the body's reaction to the introduction of insulin in order to avoid the onset of a hypoglycemic reaction in exhausted persons. In the absence of hypoglycemic phenomena, the dose of the drug can be increased to 12 U per day. In the case of a tendency to hypoglycemia, the dose is 4-8 U twice a day.

Simultaneously with the introduction of insulin is prescribed a copious amount of carbohydrates from food. The course of treatment is on average a month.

In exhausted children, the administration of insulin can normalize impaired metabolic processes, acidosis, so frequent in children suffering from hypotrophy, improve the motor and secretory functions of the digestive tract, increase weight, etc.

With the introduction of insulin in these children there is a weakened or absent feeling of hunger, which can be fixed in them according to the type of conditioned reflex.

In early childhood, hypotrophic children are prescribed 2-6 U of insulin per day. It should provide carbohydrate nutrition of the child in such cases.

For children with physical and sexual underdevelopment, if they do not have a tendency to obesity, especially if there is a decline in nutrition, insulin is prescribed for 4-12 U per day for 6-12 months (in combination with methylandrostendiol). The introduction of insulin improves appetite, causes weight gain, the development of secondary sexual characteristics, stimulates growth.

Insulin is also used in gastric and duodenal ulcers with low acidity, with significant weight loss with concomitant damage to the liver and pancreas. Insulin acts on acidosis as an alkalizer, it favorably acts on the vegetative nervous system and on functional insufficiency of the liver and pancreas, and is an important factor in the fight against emaciation. Introduce it 8-12 IU 1-2 times a day for 3-4 weeks.

Since insulin contributes to an increase in gastric secretion, to eliminate an undesirable increase in the release of hydrochloric acid, insulin therapy is combined with the use of atropine and the administration of large amounts of easily digestible carbohydrates to patients. Insulin should not be administered to persons who have undergone an operation for peptic ulcer, in order to avoid the occurrence of frequent bouts of spontaneous hypoglycemia, which may occur in the years following the operation.

In acute and chronic parenchymal hepatitis with jaundice, insulin is administered 6–12 IU 1–2 times a day in combination with glucose. The accumulation of glycogen with the introduction of small doses of insulin increases, while large doses of the drug complicate glycogen formation.

In croupous pneumonia, marked changes in carbohydrate metabolism and liver function due to acidosis caused by oxygen starvation are noted. At the same time, from the very beginning of the disease, 12–20 IU of insulin is recommended daily until the temperature decreases (in combination with glucose).

In bronchial asthma, asthmatic attacks are stopped during insulin hypoglycemia, probably due to reflex hyperproduction of adrenaline.

In a number of patients, the general condition improves, weight increases, sleep returns to normal, and remission is prolonged. The drug is prescribed in progressive doses - from 10 to 36 IU per day, and in severe cases up to 2 injections per day.

The amount of insulin per course of treatment is 50–400 U (10–12 injections). Hypoglycemia is maintained from 30 minutes to 3 hours.

Insulin treatment is combined with the use of desensitizing drugs.

With anaphylaxis - urticaria, angioedema, serum and drug disease, insulin is administered 12-20 ED 1-2 times a day until the disappearance of painful phenomena (in combination with the introduction of large amounts of easily digestible carbohydrates). In some individuals, a therapeutic effect occurs 30–60 minutes after the administration of insulin.

Introduction of 8–16 U of insulin for 5–10 days before and after surgical interventions (in combination with glucose infusion) helps to eliminate and prevent the development of acidosis, normalizes metabolic processes in operated patients and improves the postoperative process.

Exhausted patients are recommended to conduct insulin-glucose therapy during preparation for surgery. This preparation is especially indicated for functional liver failure.

The introduction of insulin with glucose helps to prevent postoperative acidosis, acidosis with intoxication, heavy vomiting. In the origin of acidosis, the accumulation of organic acids and ketone bodies matters. Oxidation of these products can occur only with the normalization of the flow of carbohydrate metabolism.

With the upcoming surgery with a long anesthesia, it is important to create a certain saturation of organs and tissues with glycogen, which increases the neutralizing function of the liver and the resistance of various organs, especially the heart and central nervous system, to ether, chloroform and other narcotic substances and metabolic products formed during anesthesia .

In psychiatric practice, insulin is used to treat schizophrenia (doses of 20-80 U). The use of insulin causes a hypoglycemic state in which metabolic processes are inhibited in the brain. The way is unsafe.

Contraindications . Renal diabetes. Addison's disease. Hypopituitarism.

The administration of insulin to patients with diabetes mellitus with coronary artery insufficiency and cerebral circulation requires caution. In such cases, insulin is prescribed in fractional doses with sufficient provision of patients with carbohydrates.

Complications . Hypoglycemic reaction (in those cases, if the patient after injecting insulin did not take carbohydrates). Treat it with the introduction of carbohydrates (sugar, honey, jam, biscuits, white bread). At the same time, 40% glucose is injected into the vein, 5% glucose under the skin, and in severe cases, 0.3-0.5-1.0 ml of a 0.1% solution of hydrochloric adrenaline.

Infiltrates, abscesses or suppurations at the site of insulin administration. Infiltrates are treated by applying heating pads, abscesses are prevented by careful sterilization of the syringe and following antiseptic rules when administering insulin.

Lipodystrophy (local atrophy of the subcutaneous layer at the sites of long-term insulin administration due to disturbed trophism of tissues) is treated by frequent changes in the site of the drug.

Allergic phenomena (urticaria, pruritus, edema) are treated with adrenocorticotropic hormone or by boiling an insulin vial for half an hour to destroy ballast proteins. You can also change a series of insulin or replace insulin derived from the pancreas glands of one type of animal with insulin of another type of animal.

Form release . Bottles of 5 ml (200 U). 1 ml contains 40 U. When used, the rubber cap of the bottle is not removed, but after wiping it with a solution of iodine and after a puncture, insulin is collected in a syringe. At the same time negative pressure is set in the bottle. Therefore, a syringe can gain a little insulin and a lot of foam. To avoid this, after iodine lubrication of the rubber stopper of the vial, a needle is put into it, put on an open syringe, and air is forced into the vial. Then the air will slowly push out the piston and the syringe will be filled with fluid without foam and air bubbles.

Keep with precaution in a cool place (not above 10 °). Refers to list B.