Belizofan

General characteristics. Structure:

Active ingredient: 100 ME insulin of human recombinant.

Excipients: protamin sulfate, phosphate dinatrium a dihydrate, zinc chloride, phenol, metacresol, glycerin, Acidum hydrochloricum for finishing рН, sodium hydroxide for finishing рН, water for injections.

Pharmacological properties:

Pharmacodynamics. Belizofan - drug of insulin of average duration of action. The protamin connected with insulin in a protaminovy complex in a stoichiometric (isowaste) ratio with formation of fine-crystalline suspension is a part of drug. Administration of drug in a hypodermic fatty tissue in the form of fine-crystalline suspension causes slow absorption owing to what the effect of prolongation of action is reached.

Pharmacodynamics. Insulin mentions all types of a metabolism in all organism. However first of all effect of insulin concerns exchange of carbohydrates. Insulin increases permeability of plasma membranes for glucose, activates key enzymes of glycolysis, stimulates formation of a glycogen in a liver and muscles from glucose, strengthens synthesis of fats and proteins. Besides, insulin suppresses activity of the enzymes splitting a glycogen and fats.

Pharmacokinetics. Absorption and the beginning of effect of insulin depends on an injection site (a hip, a shoulder), thickness of a hypodermic fatty tissue, volume of an injection, body temperature, physical activity of the patient.

On average, after hypodermic introduction, Belizofan begins to act in 1,5 hours, renders the maximum effect between the 4th and 12th hour; duration of effect of drug - till 24 o'clock.

It is distributed on fabrics unevenly, does not get through a placental barrier and into breast milk. Collapses an insulinase, generally in a liver and kidneys. The elimination half-life makes several minutes. It is removed by kidneys (30-80%).

Indications to use:

• Diabetes mellitus of the 1st type

• The diabetes mellitus of the 2nd type demanding an insulin therapy as addition to a diet and physical exercises for improvement of control of a glycemia.

Route of administration and doses:

Patients have to be taught the correct technique of an injection.

Belizofan is intended for hypodermic introduction. The drug cannot be administered intravenously. The dose of drug is defined by the doctor individually in a kalsdy specific case, on the basis of glucose level in blood. On average the daily dose of drug fluctuates from 0,5 to 1 ME/kg of body weight, depending on specific features of the patient and level of glucose of blood.

Temperature of the entered insulin has to correspond to room.

Belizofan is usually entered podkolsno into a hip. At hypodermic introduction to a hip drug is soaked up more slowly and more evenly, than at injections to other places.

Injections can be done the same to the area of a deltoid muscle of a shoulder.

Performance of an injection pleated of skin reduces risk of hit in a muscle. It is necessary to change places of injections within anatomic area to prevent development of lipodystrophies.

At an intensive care insulin Belizofan it is possible to use as basal insulin 1-2 times a day (evening and/or morning introduction) to combinations with insulin of short action which is entered before meals.

At a diabetes mellitus 2 types Belizofan can be used in a combination with the hypoglycemic drugs accepted inside in cases when independent reception of these drugs does not allow to compensate a diabetes mellitus.

The dose of insulin needs to be korrigirovat at dysfunction of a thyroid gland, Addison's disease, a hypopituitarism.

Use for elderly people. The dose of insulin needs to be korrigirovat at a diabetes mellitus at persons 65 years are more senior.

Use for persons with abnormal liver functions and kidneys. The need for an insulin dose at elderly patients with diabetes can be reduced in the presence of a renal failure.

At patients with a heavy liver failure the need for insulin can be lowered in connection with reduction of ability to a gluconeogenesis and biotransformation of insulin.

Features of use:

Against the background of therapy by insulin constant control of level of glucose in blood is necessary. Can be the hypoglycemia reasons in addition to overdose of insulin: drug replacement, the admission of meal, vomiting, diarrhea, physical tension, the diseases reducing the need for insulin (an abnormal liver function and kidneys, a gipofuktion of bark of adrenal glands, a hypophysis or thyroid gland), change of the place of an injection, and also interaction with other medicines.

The wrong dosing or breaks in administration of insulin, especially at patients with a diabetes mellitus of the I type, can lead to a hyperglycemia. Usually the first symptoms of a hyperglycemia develop gradually, for several hours or days. They include emergence of thirst, increase of an urination, nausea, vomiting, dizziness, reddening and a xeroderma, dryness in a mouth, appetite loss, an acetone smell in expired air. If not to carry out treatment, the hyperglycemia at a diabetes mellitus of the I type can lead to development of life-threatening diabetic ketoacidosis,

Associated diseases, especially the infections and states which are followed dashingly-: a radka, increase the need for insulin.

Dose adjustment of insulin can be also required if the patient increases the level of physical activity or changes a usual diet.

Transition from one type or brand of insulin to another has to take place under strict control of the doctor. Changes in concentration, a trade name (producer), type (insulin short, the average duration and long action, etc.), a look (human insulin, an analog of human insulin) and/or a method of production can demand dose adjustment of the entered insulin. This need for dose adjustment of insulin can appear both after the first use, and for the first several weeks or months.

During good compensation of carbohydrate metabolism, for example, due to the intensified insulin therapy, usual symptoms harbingers of a hypoglycemia can also change what patients have to be warned about.

Use during pregnancy and breastfeeding. Restrictions on use of insulin during pregnancy do not exist as insulin does not get through a placental barrier. Moreover, if not to carry out treatment of a diabetes mellitus during pregnancy, then danger to a fruit is created. Therefore therapy of diabetes needs to be continued also during pregnancy. Both the hypoglycemia, and a hyperglycemia which can develop in cases of insufficiently precisely picked up therapy increase risk of developing of malformations of a fruit and pre-natal death of a fruit. Pregnant women with diabetes during all pregnancy have to be under observation, at them it is necessary to exercise the strengthened control of level of glucose in blood; the same recommendations concern also to women who plan pregnancy. The need for insulin usually decreases in the first trimester of pregnancy and gradually increases in the second and third trimesters. After the delivery the need for insulin quickly is returned to the level which was noted before pregnancy. Also there are no restrictions for drug use Belizofan during breastfeeding. Performing insulin therapy to nursing mothers does not constitute danger to the child. However correction of the mode of a drug dosing Belizofan and/or diets can be required by mother.

Management of transport and work with mechanisms. Ability of patients to concentration of attention and speed of response can be broken during a hypoglycemia and a hyperglycemia that can constitute danger, for example, during the driving or work with cars and mechanisms. Patients need to recommend to undertake measures for the prevention of development of a hypoglycemia and a hyperglycemia during the driving of the car and work with mechanisms. It is especially important for patients with absence or decrease in expressiveness of symptoms harbingers of the developing hypoglycemia or suffering from frequent episodes of a hypoglycemia. In such cases it is necessary to consider expediency of driving.

Side effects:

The most often found undesirable phenomenon at use of insulin is the hypoglycemia. Hypoglycemia symptoms usually develop suddenly. They can include: cold sweat, pallor of integuments, nervousness or a tremor, feeling of alarm, unusual fatigue or weakness, orientation disturbance, concentration disturbance, dizziness, the expressed feeling of hunger, a temporary vision disorder, a headache, nausea, tachycardia. The heavy hypoglycemia can lead to a loss of consciousness and/or spasms, and also to cause temporary or irreversible disturbance of functions of a brain or death.

Disturbances from immune system: syncope/loss of consciousness.

Disturbances from a nervous system: peripheral neuropathy. If improvement of control of concentration of glucose in blood was reached very quickly, the state called "acute painful neuropathy" which is usually reversible can develop.

Disturbances from an organ of sight: disturbance of a refraction, diabetic retinopathy. Disturbance of a refraction is usually observed at the initial stage of an insulin therapy. As a rule, these symptoms have reversible character. If for a long time adequate control of a glycemia is provided, then the risk of progressing of a diabetic retinopathy decreases. However the insulin therapy intensification with sharp improvement of control of a glycemia can lead to temporary strengthening of expressiveness of a diabetic retinopathy.

Disturbances from an organism in general, and also reaction in a drug injection site: reactions in the venue of an injection (erubescence, a swelling, an itch, morbidity, formation of a hematoma). However in most cases, these reactions have passing character and in the course of therapy disappear. Puffiness is usually observed at the initial stage of an insulin therapy. As a rule, this symptom has passing character.

Generalized allergic reactions can sometimes develop. They are more serious and can lead to emergence of skin rash, a skin itch, increase in sweating, disturbances from digestive tract, to a Quincke's disease, difficulty of breath, tachycardia, arterial hypotension. Generalized allergic reactions are life-threatening and demand performing specialized treatment.

If not to change a drug injection site within anatomic area, the lipodystrophy in an insulin injection site can develop.

Interaction with other medicines:

There is a number of medicines which influence the need for insulin.

Hypoglycemic effect of insulin peroral hypoglycemic drugs, MAO inhibitors, APF inhibitors, karboangidraza inhibitors, non-selective beta adrenoblockers, Bromocriptinum, октреотид strengthen, streptocides, anabolic steroids, tetracyclines, Clofibratum, кетоконазол, Mebendazolum, a pyridoxine, theophylline, cyclophosphamide, фенфлурамин, the lithium drugs, drugs containing ethanol.

Hypoglycemic effect of insulin oral contraceptives, glucocorticosteroids, thyroid hormones, thiazide diuretics, heparin, tricyclic antidepressants, antidepressants, sympathomimetics, даназол weaken, a clonidine, antagonists of calcium, diazoxide, morphine, Phenytoinum, nicotine.

Beta-blockers, clonidine can mask symptoms of a hypoglycemia and complicate its elimination. Oktreotid/lanreotid can, both to reduce, and to increase the need for insulin.

Cases of development of heart failure were received at combined use of insulin and tiazolidindion, especially patients with risk factors have development of heart failure. It should be meant at purpose of this combination. If the above-stated combination is appointed, it is necessary to reveal timely signs and symptoms of heart failure, increase in weight, hypostases. At deterioration in symptoms from cordial system use of tiazolidindion needs to be stopped.

Incompatibility. Suspension of insulin cannot add to solutions for infusions.

Contraindications:

• Hypoglycemia

• The increased individual sensitivity to insulin or any of drug components.

Overdose:

At overdose development of a hypoglycemia is possible. The hypoglycemia can cause drowsiness, confusion of consciousness, tachycardia, a headache, perspiration, nausea, vomiting. Soft hypoglycemic episodes are stopped by peroral administration of glucose, reception of sugar or carbohydrate-rich products. Correction of moderately heavy hypoglycemia can be reached by intramuscular or hypodermic introduction of a glucagon, with the subsequent oral administration of carbohydrates, in case of satisfactory condition of the patient.

To patients who do not react to a glucagon intravenously enter 40% glucose solution. If the patient is in coma, the glucagon should be entered intramusculary or subcutaneously. Glucose has to be entered intravenously if the glucagon is unavailable or the patient does not react to a glucagon. After consciousness recovery the patient is recommended to eat food, carbohydrate-rich, for prevention of repeated development of a hypoglycemia.

Storage conditions:

In the place protected from light at a temperature from 2 °C to 8 °C. Not to freeze. To store the opened bottle with insulin no more than 6 weeks in the place protected from light at a temperature not above 25 °C (but not in the refrigerator). To protect drug from light hit. It is not necessary to heat drug to body temperature before introduction. To avoid heating, hit of direct sunshine and freezing. Not to use drug if after rolling of a bottle between palms suspension does not become white and homogeneous (evenly muddy). To store in the place, unavailable to children. Period of validity 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

In bottles on 10 ml. 1 bottle together with the application instruction is placed in a pack from a cardboard.