Preparations for insulin therapy

Insulin preparations are necessary for patients with type 1 diabetes and for 40% of patients with a second form of 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 depends directly on the site of the injection, muscle activity, the characteristics of the blood flow and the technique of performing the injection.

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

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

Preparations for insulin therapy are classified by their origin:

1. 1. Animals (pigs) - Insulrap GPP, Ultralente, Ultralente MS, Monodar Ultralong, Monodar Long, Monodar K, Monosuynsulin.
2. 2. Human (semi-synthetic and genetically engineered) - Actrapid, Novorapid, Lantus, Humulin, Humalog, Novomix, Protafan.
3. 3. Synthetic analogues - Lizpro, Aspart, Glargin, Detemir.

The medications are divided according to the duration of the action:

Insulins of ultrashort action

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

Lispro

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

Equimolaren to human insulin. Penetrating into muscle tissue accelerates the transition of glucose and amino acids into fat. It starts to act 15 minutes after the injection. High suction speed allows you to apply the medicine immediately before eating.

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

Treatment of adverse symptoms and overdose consists of subcutaneous, / m or / in the introduction of glucagon, IV injection of hypertonic solution of dextrose. With the development of hypoglycemic coma, an intravenous jet injection of 40 ml of a 40% dextrose solution is shown before the patient leaves the coma.

Aspart

An analogue of the human hormone with an ultrashort action. The preparation was obtained by recombinant DNA technology using the strain Saccharomyces cerevisiae. Has hypoglycemic action. It starts to act 10-20 minutes after subcutaneous injection and reaches the maximum therapeutic effect in 1-3 hours.

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

In case of an overdose, there are signs of hypoglycemia, seizures and there is a risk of developing hypoglycemic coma. To eliminate mild hypoglycemia and normalize the state, it is sufficient to take sugar or foods rich in easily digestible carbohydrates. In other cases, intravenous administration of a 40% dextrose solution is necessary.

[1], [2], [3], [4], [5]

Aphidra

Solution for subcutaneous administration. It is an analog of human insulin, corresponding to him in terms of the strength of the action. Has increased activity, but shorter duration of action in comparison with human hormone.

• It is used to compensate for carbohydrate metabolism in the body with insulin deficiency. It is allowed to use for treatment of children over 6 years old. It is administered subcutaneously 15 minutes before meals or after eating. Dosage and treatment is determined by the attending physician, individually for each patient.
• Contraindications: hypersensitivity to glulisin or other components of the drug. With special care is used for pregnant and sick in the period of breastfeeding.
• Side effects: hypoglycemia and other metabolic disorders, nausea and vomiting, decreased concentration, visual impairment, allergic reactions at the injection site. In rare cases, it is possible to develop allergic dermatitis, a feeling of tightness in the chest, anaphylactic reactions.
• Overdose is manifested by symptoms of hypoglycemia of mild or severe form. In the first case, the treatment shows the intake of glucose or sugar-containing products. In the second case, the patient is given an intramuscular or intravenous drip 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.

[6], [7], [8]

Soluble human genetic engineering

Biosulin

A solution for injections that includes human genetically engineered insulin, glycerol, meta-cresol and other components. Has a short hypoglycemic effect. Penetrating into the body interacts with a specific receptor of the outer cytoplasmic membrane of cells.

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

• Indications: Type 1 diabetes mellitus and insulin-independent form of the disease, intercurrent diseases, conditions requiring decompensation of carbohydrate metabolism.
• Dosage and administration: subcutaneously, intramuscularly or intravenously 30 minutes before meals with increased carbohydrate content. The daily dosage is from 0.5 to 1 IU / kg body weight.
• Contraindications: hypersensitivity to the components of the medication, hypoglycemia, pregnancy and lactation.
• Side effects: increased sweating and agitation, palpitations, tremor of limbs, hunger, paresthesia in the mouth and other hypoglycemic symptoms. Local reactions: puffiness at the injection site, itching, lipodystrophy, allergic reactions, puffiness.
• Overdose: it has a similar symptomatology with adverse reactions. With the development of hypoglycemic state, a carbohydrate-rich diet is recommended, and in severe cases - the administration of a solution of dextrose or glucagon.

Biosulin is produced in vials of 10 ml each and in cartridges of 3 ml.

[9]

Insumman

Drug replenishing the deficiency of endogenous insulin in diabetes mellitus. It has several forms, which differ in the percentage ratio of a neutral solution of insulin and protamine. Each species has its own pharmacokinetics, that is, features of distribution in the body. All forms are characterized by a rapid onset and an average duration of action.

• Insuman Comb 15/85 - shows activity 30-45 minutes after administration, the maximum therapeutic effect develops in 3-5 hours. The duration of the action is 11-20 hours.
• Insuman Comb 25/75 - starts 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 - effective 30 minutes after administration, maximum effect observed after 1-1.5 hours, duration of action is 10-16 hours.

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

Side effects: skin allergic reactions, lipodystrophy, insulin resistance, pronounced renal impairment, hyperglycemic reactions. Overdose has a similar but more pronounced symptomatology. Contraindications: hypersensitivity to the components of the drug, diabetic coma. It is available in the form of a suspension for injection in 10 ml bottles 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. Therapeutic effect persists for 6-8 hours.

• Indications for use: diabetes insulin-dependent, treatment of patients with intolerance to other forms of medication, forthcoming surgery in patients with a second form of diabetes, lipodystrophy.
• Method of application: if the drug is administered in its pure form, it is administered 3 times a day subcutaneously, intramuscularly or intravenously. After 30 minutes after the injection you need to take food. The dosage is determined by the endocrinologist, individually for each patient.
• Side effects: a sharp decrease in blood sugar, redness at the injection site and itching, skin allergic reactions.
• Contraindications: hormonal tumors of the pancreas, hypoglycemia. Application during pregnancy and lactation is possible only with medical appointment.

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

Soluble human semisynthetic

Brinsulppi

The drug is of short action, it shows its activity 30 minutes after subcutaneous injection. The maximum therapeutic effect develops within 1-3 hours and lasts about 8 hours.

• Indications for use: Type 1 and type 2 diabetes in children and adults, resistance to oral hypoglycemic drugs.
• Method of application: dosage of the hormone for subcutaneous administration is determined by the attending physician, individually for each patient. The solution is injected immediately after typing in the syringe. If the daily dose is more than 0.6 U / kg, then the drug is divided into two injections and injected into different parts of the body.
• Side effects: skin rashes, angioedema, anaphylactic shock, lipodystrophy, transient refractive failure, hyperemia of tissues at the site of injection.
• Contraindications: individual intolerance to the components of the drug, hypoglycemic conditions. Treatment during pregnancy and lactation is possible only for medical purposes. With special care is used for increased physical or mental performance.

[10],

Humor R100

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

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

• Indications for use: diabetes of the first and second type. Partial or complete resistance to oral hypoglycemic medications, diabetic ketoacidosis, gestational diabetes, metabolic disorders in switching to long-acting insulin.
• Dosage and administration: the drug is intended for subcutaneous, intramuscular and intravenous administration. On average, the dosage is 0.5 to 1 IU / kg body weight. The hormone is used 30 minutes before a meal rich in carbohydrates. The solution to be injected must be at room temperature. If the agent is prescribed for monotherapy, the frequency of administration is 3-5 times a day.
• Contraindications: individual intolerance of the components of the drug, signs of hypoglycemia. Use during pregnancy is prohibited, injections during breastfeeding are possible only for medical purposes.
• Side effects: blanching of the skin, increased sweating, palpitations, tremor of the extremities, agitation, nausea and vomiting, headaches. Also, allergic reactions at the injection site are possible.
• Overdose: a hypoglycemic state of varying severity. Treatment consists of eating sugar or carbohydrate-rich foods. In severe cases, a 40% solution of dextrose or glucagon is indicated.

Humodar P100 is produced in bottles of 10 ml and in cartridges of 3 ml of solution each.

Berlinulinsulin H normal U-40

Medication with hypoglycemic effect. Refers to preparations of fast and short action. The maximum therapeutic effect develops after 1-3 hours and persists for 6-8 hours.

It is used to treat all forms of diabetes and diabetic coma. 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 hypersensitivity to the drug, the dosage is reduced, with a decreased sensitivity, it is increased.

The drug is contraindicated for intolerance of its components and signs of hypoglycemia. Adverse symptoms are manifested by local skin reactions, deterioration of general well-being.

Insulin of medium duration

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 the action is 12-24 hours.

Isolan

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

The drug is used for subcutaneous and intramuscular injection. Dosage and frequency of injections is determined by the attending physician, individually for each patient. Isophane is contraindicated in hypoglycemic and coma. Side effects are manifested by the sensation of hunger, overfatigue, tremor of extremities, allergic reactions.

Monotard MS

An insulin preparation with an average duration of action. Contains 30% amorphous and 70% crystalline hormone. The active ingredient is a suspension of monocomponent pig insulin. It begins to act 2.5 hours after the injection, the maximum effect develops after 7-15 hours and persists for 24 hours.

• Indications for use: all forms of diabetes mellitus, resistance to oral hypoglycemic agents, various complications of diabetes mellitus, surgery, pregnancy and lactation.
• Method of application: the dose is selected by the doctor individually for each patient. The medicine is injected deep subcutaneously, each time changing the site of the injection. If the dosage exceeds 0.6 U / kg, then it should be divided into two injections in different places. Patients who receive more than 100 units of medicine per day are hospitalized.
• Side effects: different in severity of hypoglycemia, 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

Hypoglycemic agent of medium duration of action. It is used for the treatment of diabetes 1 and 2 forms. The drug is used for subcutaneous injection into the thigh area, it is also permissible to administer the drug to the anterior abdominal wall, buttock, deltoid shoulder muscle. Dosing is calculated by the endocrinologist, focusing on the level of glucose in the patient's blood and other features of his body.

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

Long-acting insulins

Begins to act 1-6 hours after administration. Evenly lowers blood glucose levels. Has a pronounced peak action and remains effective for 24 hours. Allows you to make injections 1 time per day.

Lantus

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

• Indications for use: insulin-dependent form of diabetes in adults and children over 6 years.
• Method of application: prolonged action is based on the introduction of the active component in the subcutaneous fat. This effect of the drug allows you to apply it once a day. Dosage is calculated for each patient individually.
• Side effects: metabolic disorders of varying severity. Most often there is a decrease in visual acuity, lipoatrophy, lipogypertrophy, dysgeusia, local allergic reactions. In rare cases, there is anaphylactic shock, myalgia, bronchospasm.
• 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: non-compliance with the dosage threatens the development of long-term forms of severe hypoglycemia, which is dangerous for the patient. Weak symptomatology is stopped by taking carbohydrates. In severe cases, intravenous administration of a concentrated solution of glucose is indicated.

Lantus is available in the form of a solution for injection, in cartridges of 3 ml.

Levemir Penfill

Antidiabetic remedy, analogue of human basal hormone with prolonged action. The long-term effect is based on the interaction of the molecules of the active substance with albumins through the chains of fatty acids at the site of administration of the drug. Hypoglycemic action persists for 24 hours, but may vary depending on the dosage. Prolonged action allows you to use the medicine 1-2 times a day.

• It is used for the treatment of type 1 diabetes. The solution is administered subcutaneously, the dosage is selected individually for each patient, depending on the needs of his organism and the characteristics of the disease.
• Side effects: pale skin, tremors of the extremities, increased nervousness, anxiety, drowsiness, palpitations, impaired orientation and vision, paresthesia. Local reactions are also possible in the form of edema of the tissues, itching, lipodystrophy, and hyperemia of the skin. Overdose has a similar symptomatology. Treatment consists in the use of carbohydrate-containing products.
• Contraindications: intolerance of the constituents of the medicine. Use during pregnancy and lactation is possible only for medical purposes and under the strict control of the endocrinologist.

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

Trevisa FlexTach

The analogue of the human hormone is extremely long-acting. The mechanism of action of the drug is based on interaction with the receptors of human endogenous insulin. Hypoglycemic effect is due to increased utilization of glucose by tissues after the hormone binds to the receptors of fat and muscle cells.

• The drug is used to treat diabetes in adults and adolescents, as well as children older than 1 year. The solution is used for subcutaneous administration, the dosage is calculated by the attending physician, individually for each patient.
• Contraindications: intolerance of the components of the drug, pregnancy and lactation.
• Side effects: hypoglycemia, allergic reactions at the injection site, lipodystrophy. Also, there are possible violations by the immune system, peripheral edema, convulsions. Overdose has similar symptoms. To eliminate the painful symptoms, it is recommended to take sugar-containing foods inside. If hypoglycemia is severe, then a dextrose solution is necessary.

Tresiba Flex Tach is produced in syringes-pens for subcutaneous injection at 100 and 200 U / ml.

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