Drugs for insulin therapy

Insulin preparations are necessary for patients with type 1 diabetes and for 40% of patients with the second form of the pathology. Insulin is a polypeptide hormone. As a rule, the drug is administered subcutaneously, but in emergency cases, intramuscular or intravenous administration is possible. The rate of its absorption directly depends on the injection site, muscle activity, blood flow characteristics and injection technique.

By binding to cell membrane receptors, the hormone begins to exert its physiological effects:

• Reducing blood glucose levels.
• Activation of glycogen synthesis.
• Suppression of ketone body formation.
• Inhibition of the processes of sugar formation from non-carbohydrate compounds.
• Activation of the formation of triglycerides and low-density lipoproteins.
• Inhibition of fat breakdown due to the formation of fatty acids from carbohydrates.
• Stimulates the production of glycogen, which acts as the body’s energy reserve.

Insulin therapy drugs are classified according to their origin:

1. 1. Animals (pork) – Insulrap GPP, Ultralente, Ultralente MS, Monodar Ultralong, Monodar Long, Monodar K, Monosuinsulin.
2. 2. Human (semi-synthetic and genetically engineered) – Actrapid, Novorapid, Lantus, Humulin, Humalog, Novomix, Protafan.
3. 3. Synthetic analogues – Lispro, Aspart, Glargine, Detemir.

Medicines are divided according to duration of action:

Ultra-short-acting insulins

Absorbed faster than other types of the drug. Begins to act 10-20 minutes after administration, causing a decrease in blood sugar levels. The maximum effect develops within 30-180 minutes and lasts for 3-5 hours.

Lizpro

A two-phase mixture of fast-acting insulin and protamine suspension of medium duration of action. The drug is a DNA recombinant analogue of the human hormone, differing only in the reverse sequence of proline and lysine amino acid residues. Regulates glucose metabolism and has an anabolic effect.

Equimolar to human insulin. Penetrating muscle tissue accelerates the conversion of glucose and amino acids into fat. Begins to act 15 minutes after administration. High absorption rate allows the drug to be used immediately before meals.

• Indications for use: diabetes mellitus type 1, intolerance to other types of drugs, postprandial hyperglycemia (not amenable to correction), accelerated local degradation of pancreatic hormone. Diabetes type 2, resistance to oral hypoglycemic drugs, intercurrent diseases, surgical interventions.
• Method of administration and dosage: determined individually for each patient depending on the level of glycemia in the blood. The drug is administered subcutaneously only. If necessary, it can be combined with prolonged medications or sulfonylurea drugs for oral administration.
• Contraindications: intolerance to the components of the drug, insulinoma.
• Side effects: allergic reactions, lipodystrophy, hypoglycemia, hypoglycemic coma, temporary refractive error.
• Overdose: increased fatigue, drowsiness and lethargy, profuse sweating, increased heart rate, tachycardia, feeling of hunger, paresthesia of the oral area, headaches, vomiting and nausea, irritability and depressive mood. Visual disturbances, convulsions, glycemic coma.

Treatment of side effects and overdose consists of subcutaneous, intramuscular or intravenous administration of Glucagon, intravenous administration of hypertonic dextrose solution. In the event of hypoglycemic coma, intravenous jet injection of 40 ml of 40% dextrose solution is indicated until the patient comes out of the comatose state.

Aspart

An analogue of a human hormone with an ultra-short action. The drug was obtained by recombinant DNA technology using the Saccharomyces cerevisiae strain. It has a hypoglycemic effect. It begins to act 10-20 minutes after subcutaneous administration and reaches its maximum therapeutic effect in 1-3 hours.

It is used for diabetes mellitus of the first and second types. Aspart is used only for subcutaneous administration, the dosage is determined by an endocrinologist. The drug is contraindicated in hypoglycemia and hypersensitivity to its components. It is not used to treat patients under 6 years of age, as well as during pregnancy and lactation.

In case of overdose, signs of hypoglycemia, convulsions and the risk of developing hypoglycemic coma occur. To eliminate mild hypoglycemia and normalize the condition, it is enough to take sugar or foods rich in easily digestible carbohydrates. In other cases, intravenous administration of 40% dextrose solution is necessary.

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Apidra

Solution for subcutaneous administration. It is an analogue of human insulin, corresponding to it in strength of action. It has increased activity, but a shorter duration of action in comparison with the human hormone.

• It is used to compensate for carbohydrate metabolism in the body with a lack of insulin. It is approved for use in the treatment of children over 6 years of age. It is administered subcutaneously 15 minutes before or after meals. The dosage and course of treatment are determined by the attending physician, individually for each patient.
• Contraindications: hypersensitivity to glulisine or other components of the drug. It is used with special caution in pregnant women and patients during breastfeeding.
• Side effects: hypoglycemia and other metabolic disorders, nausea and vomiting, decreased concentration, visual impairment, allergic reactions at the injection site. In rare cases, allergic dermatitis, chest tightness, and anaphylactic reactions may develop.
• Overdose is manifested by symptoms of mild or severe hypoglycemia. In the first case, treatment is indicated by taking glucose or sugar-containing products. In the second case, the patient is given intramuscular or intravenous drip administration of glucagon or dextrose.

Short-acting (simple human insulin) – the therapeutic effect develops within 30-50 minutes after administration. Peak activity lasts 1-4 hours and lasts 5-8 hours.

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Soluble human genetic engineering

Biosulin

Injection solution containing human genetically engineered insulin, glycerol, metacresol and other components. Has a short hypoglycemic effect. When penetrating the body, it interacts with a specific receptor of the outer cytoplasmic membrane of cells.

Promotes the formation of the insulin-receptor complex. Stimulates intracellular processes, synthesis of key enzymes. The onset of action of the drug is noted 30 minutes after administration, and the maximum effect develops within 2-4 hours, the duration of action is 6-8 hours.

• Indications: diabetes mellitus type 1 and insulin-independent form of the disease, intercurrent diseases, conditions requiring decompensation of carbohydrate metabolism.
• Method of administration and dosage: subcutaneously, intramuscularly or intravenously 30 minutes before a meal with a high carbohydrate content. The daily dosage is from 0.5 to 1 IU/kg of body weight.
• Contraindications: hypersensitivity to the components of the drug, hypoglycemia, pregnancy and lactation.
• Side effects: increased sweating and agitation, increased heart rate, tremors of the extremities, hunger, paresthesia in the mouth area and other hypoglycemic symptoms. Local reactions: swelling at the injection site, itching, lipodystrophy, allergic reactions, swelling.
• Overdose: has symptoms similar to side effects. If hypoglycemic state develops, carbohydrate-rich food is recommended, and in severe cases, the introduction of dextrose or glucagon solution.

Biosulin is available in 10 ml vials and 3 ml cartridges.

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Insuman

A drug that replenishes the deficiency of endogenous insulin in diabetes mellitus. It has several forms that differ in the percentage ratio of neutral insulin solution and protamine. Each type has its own pharmacokinetics, i.e., distribution features in the body. All forms are characterized by a rapid onset and medium duration of action.

• Insuman Comb 15/85 – becomes active 30-45 minutes after administration, the maximum therapeutic effect develops after 3-5 hours. The duration of action is 11-20 hours.
• Insuman Comb 25/75 – begins to act 30 minutes after application, the maximum effect begins after 1.5-3 hours, the period of action is 12-18 hours.
• Insuman Comb 50/50 – acts 30 minutes after administration, the maximum effect is observed after 1-1.5 hours, the duration of action is 10-16 hours.

It is used for insulin-dependent forms of diabetes mellitus. The solution is administered subcutaneously one hour before meals. The dosage is determined by the attending physician.

Side effects: skin allergic reactions, lipodystrophy, insulin resistance, severe renal impairment, hyperglycemic reactions. Overdose has similar but more pronounced symptoms. Contraindications: hypersensitivity to the components of the drug, diabetic coma. Available in the form of a suspension for injection in vials of 10 ml each.

Actrapid NM

Insulin-containing drug with a monocomponent structure and short action. The therapeutic effect develops 30 minutes after administration and reaches its maximum within 2-5 hours. The therapeutic effect lasts for 6-8 hours.

• Indications for use: insulin-dependent diabetes, treatment of patients with intolerance to other forms of the drug, upcoming surgery in patients with type 2 diabetes, lipodystrophy.
• Method of administration: if the medicine is prescribed in its pure form, it is administered 3 times a day subcutaneously, intramuscularly or intravenously. 30 minutes after the injection, it is necessary to eat. The dosage is determined by an endocrinologist, individually for each patient.
• Side effects: a sharp decrease in blood sugar, redness at the injection site and itching, allergic skin reactions.
• Contraindications: hormonal tumors of the pancreas, hypoglycemia. Use during pregnancy and lactation is possible only with a doctor's prescription.

Actrapid NM is available in ampoules containing 10 ml of active substance each.

Soluble human semi-synthetic

Brinsulrapi

A short-acting drug, it becomes active 30 minutes after subcutaneous administration. The maximum therapeutic effect develops within 1-3 hours and lasts for about 8 hours.

• Indications for use: diabetes type 1 and 2 in children and adults, resistance to oral hypoglycemic drugs.
• Method of administration: the dosage of the hormone for subcutaneous administration is determined by the attending physician, individually for each patient. The solution is administered immediately after being drawn into the syringe. If the daily dose is more than 0.6 U/kg, the medicine is divided into two injections and injected into different parts of the body.
• Side effects: skin rash, angioedema, anaphylactic shock, lipodystrophy, transient refractive error, tissue hyperemia at the injection site.
• Contraindications: individual intolerance to the components of the drug, hypoglycemic conditions. Treatment during pregnancy and lactation is possible only on doctor's prescription. It is used with special caution in case of increased physical or mental work.

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Humodar P100

Human semisynthetic short-acting insulin. Interacts with receptors of cytoplasmic cell membranes, forming an insulin-receptor complex that stimulates intracellular processes.

Normalization of blood glucose is based on increasing intracellular transport of this hormone, increased absorption and assimilation by tissues. The drug begins to act 30 minutes after administration and reaches its maximum in 1-2 hours, the therapeutic effect lasts for 5-7 hours.

• Indications for use: diabetes type 1 and type 2. Partial or complete resistance to oral hypoglycemic drugs, diabetic ketoacidosis, gestational diabetes, metabolic disorders when switching to prolonged-action insulin.
• Method of administration and dosage: the drug is intended for subcutaneous, intramuscular and intravenous administration. On average, the dosage is from 0.5 to 1 IU/kg of body weight. The hormone is used 30 minutes before a meal rich in carbohydrates. The administered solution should be at room temperature. If the drug is prescribed for monotherapy, the frequency of administration is 3-5 times a day.
• Contraindications: individual intolerance to the components of the drug, signs of hypoglycemia. Use during pregnancy is prohibited, injections during breastfeeding are possible only on doctor's prescription.
• Side effects: pale skin, increased sweating, increased heart rate, tremors of the extremities, agitation, nausea and vomiting, headaches. Allergic reactions at the injection site are also possible.
• Overdose: hypoglycemic state of varying severity. Treatment consists of consuming sugar or carbohydrate-rich foods. In severe cases, administration of 40% dextrose solution or glucagon is indicated.

Humodar P100 is available in 10 ml vials and in cartridges containing 3 ml of solution each.

Berlinsulin H normal U-40

A medicinal product with a hypoglycemic effect. Refers to drugs of fast and short action. The maximum therapeutic effect develops in 1-3 hours and lasts for 6-8 hours.

It is used to treat all forms of diabetes and diabetic coma. The dosage is set individually for each patient. As a rule, the drug is administered subcutaneously 10-15 minutes before meals 3-4 times a day. The daily dose is 6-20 units. For patients with increased sensitivity to the drug, the dosage is reduced, with decreased sensitivity - increased.

The product is contraindicated in case of intolerance to its components and signs of hypoglycemia. Side effects are manifested by local skin reactions, deterioration of general well-being.

Intermediate-acting insulins

It is slowly absorbed and has a therapeutic effect 1-2 hours after a subcutaneous injection. The maximum effect is achieved within 4-12 hours, the duration of action is 12-24 hours.

Isophane

Suspension for subcutaneous administration. Activates the phosphatidylinositol system, changes glucose transport. Increases potassium entry into the cell. 1 ml of suspension contains 40 IU of human insulin of biosynthetic origin. It is used in insulin-dependent diabetes mellitus, in allergies to other types of insulin, and severe vascular complications of diabetes.

The drug is used for subcutaneous and intramuscular administration. The dosage and frequency of injections are determined by the attending physician, individually for each patient. Isophane is contraindicated in hypoglycemic and comatose states. Side effects include a feeling of hunger, fatigue, tremors of the limbs, and allergic reactions.

Monotard MS

A medium-acting insulin preparation. Contains 30% amorphous and 70% crystalline hormone. The active ingredient is zinc suspension of monocomponent porcine insulin. It begins to act 2.5 hours after administration, the maximum effect develops after 7-15 hours and lasts for 24 hours.

• Indications for use: all forms of diabetes mellitus, resistance to oral hypoglycemic agents, various complications of diabetes mellitus, surgical interventions, pregnancy and lactation.
• Method of administration: the dose is selected by the doctor individually for each patient. The medicine is administered deep subcutaneously, changing the injection site each time. If the dosage exceeds 0.6 U/kg, it should be divided into two injections in different places. Patients receiving more than 100 units of the medicine per day are subject to hospitalization.
• Side effects: hypoglycemic states of varying severity, precoma, coma. Hyperemia at the injection site, skin allergic reactions.
• Contraindications: hypoglycemic conditions and hypoglycemic coma.

Monotard MS is available in the form of a suspension for injection in 10 ml vials.

Insulong SPP

A medium-acting hypoglycemic agent. It is used to treat diabetes types 1 and 2. The drug is used for subcutaneous injections into the thigh area, and it is also allowed to administer the drug into the anterior abdominal wall, buttock, and deltoid muscle of the shoulder. The dosage is calculated by an endocrinologist, based on the patient's blood glucose level and other characteristics of his body.

The drug is contraindicated in case of hypersensitivity to its components, hypoglycemia. Side effects are manifested by refraction disorders and swelling of the extremities. In case of nutritional disorders during treatment or use of an increased dosage, hypoglycemia may develop. Also possible local reactions after the injection: redness, swelling and itching.

Long-acting insulins

It starts to act 1-6 hours after administration. It evenly reduces the blood glucose level. It has an indistinct peak of action and remains effective for 24 hours. It allows injections to be made once a day.

Lantus

Hypoglycemic insulin preparation, with the active component glargine (analogue of human hormone). It has low solubility in a neutral medium. When administered subcutaneously, the acid is neutralized and forms microprecipitates that release insulin.

• Indications for use: insulin-dependent diabetes in adults and children over 6 years of age.
• Method of application: prolonged action is based on the introduction of the active component into the subcutaneous fat tissue. This effect of the drug allows it to be used once a day. The dosage is calculated for each patient individually.
• Side effects: metabolic disorders of varying severity. Most often observed are decreased visual acuity, lipoatrophy, lipohypertrophy, dysgeusia, local allergic reactions. In rare cases, anaphylactic shock, myalgia, bronchospasm occur.
• Contraindications: hypersensitivity to the components of the drug, hypoglycemia, diabetic ketoacidosis. The drug is not recommended for the treatment of pregnant women and children.
• Overdose: failure to comply with the dosage may result in the development of prolonged forms of severe hypoglycemia, which is dangerous for the patient. Mild symptoms are relieved by taking carbohydrates. In severe cases, intravenous administration of a concentrated glucose solution is indicated.

Lantus is available as an injection solution in 3 ml cartridges.

Levemir Penfill

An antidiabetic agent, an analogue of human basal hormone with prolonged action. The long-term effect is based on the interaction of the active substance molecules with albumins through fatty acid chains at the injection site. The hypoglycemic effect lasts for 24 hours, but may vary depending on the dosage. The prolonged action allows the drug to be used 1-2 times a day.

• It is used to treat type 1 diabetes. The solution is administered subcutaneously, the dosage is selected individually for each patient depending on the needs of his body and the characteristics of the disease.
• Side effects: paler skin, tremor of the extremities, increased nervousness, anxiety, drowsiness, increased heart rate, impaired orientation and vision, paresthesia. Local reactions in the form of tissue edema, itching, lipodystrophy and hyperemia of the skin are also possible. Overdose has similar symptoms. Treatment consists of eating carbohydrate-containing products.
• Contraindications: intolerance to the components of the medication. Use during pregnancy and lactation is possible only on doctor's prescription and under strict supervision of an endocrinologist.

Levemir Penfill is available in 3 ml cartridges (300 units) as a solution for parenteral administration.

Tresiba FlexTouch

An analogue of the human hormone of ultra-long action. The mechanism of action of the drug is based on the interaction with receptors of human endogenous insulin. The hypoglycemic effect is due to the increase in the utilization of glucose by tissues after the hormone binds to receptors of fat and muscle cells.

• The medicine is used to treat diabetes in adult and adolescent patients, as well as children over 1 year of age. The solution is used for subcutaneous administration, the dosage is calculated by the attending physician, individually for each patient.
• Contraindications: intolerance to the components of the drug, pregnancy and lactation.
• Side effects: hypoglycemia, allergic reactions at the injection site, lipodystrophy. Immune system disorders, peripheral edema, and seizures are also possible. Overdose has similar signs. To eliminate painful symptoms, it is recommended to take sugar-containing products orally. If hypoglycemia is severe, then a dextrose solution must be administered.

Tresiba FlexTouch is available in pens for subcutaneous administration of 100 and 200 U/ml.

In addition to the above-mentioned groups of drugs, there are mixtures of insulins with different durations of action: aspart biphasic NovoMix 30/50, FlexPen, Penfill, Lispro, biphasic Humalog Mix 25/50.