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1 milliliter of drug of Apidr Solostar includes 100 PIECES (3,49 mg) of insulin of a glulizin.
In addition: Acidum hydrochloricum, metacresol, sodium chloride, trometamin, polysorbate 20, sodium hydroxide, water for infection.
Apidra Solostar is issued in the form of injection (for p / to introduction) solution in cartridges on 3 ml which are built in in the syringe handle on 5 pieces in secondary packaging.
Pharmacodynamics and pharmacokinetics
Insulin glulizin, being active ingredient of drug of Apidr, in fact — recombinant analog of insulin of the person, on force of the action equivalent to endogenous human insulin. In comparison with soluble insulin of the person action of this analog develops quicker, and duration of its influence is slightly shorter.
Fundamental effect of insulin, as well as its drugs of analogs including insulin of a glulizin, regulation of a glucosic exchange is. Effects of this group of drugs are directed to lowering of concentration of plasma glucose, activation of its assimilation by peripheral fabrics (in particular fatty tissue and skeletal muscles), and also to suppression of forming of glucose in hepatic fabric. In adipocytes drug oppresses a lipolysis, slows down process of proteolysis and increases protein synthesis. The conducted researches with involvement of patients with a diabetes mellitus and healthy volunteers confirmed faster occurrence of effects of Apidra at p / to introduction, and also her less long action, in comparison with soluble human insulin. At p / to a way of introduction hypoglycemic efficiency of this drug is observed in 10-20 minutes. When comparing in/in injections of soluble insulin of the person and insulin of a glulizin effects of both drugs remain at one level. Glyukozoponizhayushchy activity of one unit of both drugs completely matches.
In the 1st phase of the conducted researches with involvement of patients with an insulin-dependent diabetes mellitus the assessment of glyukozoponizhayushchy abilities of soluble insulin of the person and insulin of a glulizin was carried out at p / to injections in a dose of 0,15 PIECES/kg entered into various time concerning standard 15-minute meal. Following the results of researches it was found out that Apidra's introduction in 2 minutes prior to food rendered the same glycemic effect, as well as administration of human insulin for half an hour before meal. In case of administration of both of these drugs in 2 minutes prior to food, the best indicators of glycemic control were observed concerning insulin of a glulizin. Apidra's injection which is carried out in 15 minutes after the beginning of food yielded the same glycemic result that introduction of human analog in 2 minutes prior to meal.
In the 1st phase of the conducted researches between insulin lizpro, insulin gluliziny and soluble insulin of the person with involvement of patients with obesity proved preservation of fast efficiency of Apidra. In the course of carrying out this research, the period of achievement of 20% of a threshold of full AUC respectively for insulin glulizina / insulin lizpro / human insulin made 114/121/150 minutes, an AUC (0-2 hours) which is also displaying early glyukozoponizhayushchy action equaled respectively 427мг/кг/354мг/кг/197мг/кг.
In the 3rd phase of the conducted 26-week clinical trial between insulin gluliziny and insulin lizpro which were entered p / to shortly (0-15 minutes) to food to patients with the juvenile diabetes applying as background drug – insulin glargin, it is found out that effects of both of these medicines were comparable concerning the control of a glycemia which is estimated on rejections of the contents of HbA1C (glikozilirovanny hemoglobin) in a final stage of research compared with an initial stage. The comparable parameters of plasma glucose fixed by self-checking were noted. In case of insulin injections glulizin, in comparison with administration of insulin lizpro, increase in dosages of background drug was not required.
In the 3rd phase of the conducted 12-week clinical trial at the patients with an insulin-dependent diabetes mellitus passing background treatment by insulin glargin the efficiency of insulin of the glulizin entered right after food, which is not conceding that at its introduction before itself (0-15 minutes) or the injection of soluble insulin of the person which is carried out in 30-45 minutes prior to food is proved meal.
In the studied group of patients which received insulin glulizin before food, more significant decrease in HbA1C, in comparison with the patients who were in group of use of human analog was noted.
In the 3rd phase of the conducted 26-week clinical trial with the subsequent 26-week testing of safety, compared insulin glulizin, the entered p / to in 0-15 minutes prior to food and soluble insulin of the person entered p / to in 30-45 minutes prior to meal to involvement of the patients with insulinonezavisimy diabetes receiving in addition as background drug – insulin isophanes. Indicators of an average index of weight of patients equaled 34,55 kg/sq.m. More significant decrease in maintenance of HbA1C (-0,46%) was observed at patients from group insulin of a glulizin, in comparison with group of human insulin (-0,30%). In this research most of patients (79%) just before introduction combined the short-range drug with insulin isofan. 58 studied people at the time of randomization accepted peroral hypoglycemic means and continued their reception in an invariable dose.
In case of carrying out continuous p / to infusional injection of insulin with use of the pompovy device (rather juvenile diabetes) at 59 patients using drugs Apidra or Aspart noted the low frequency of occlusion of a catheter, for Apidr's drug – 0,08 occlusions in 30 days, for drug Aspart – 0,15 occlusions for the same period, and also similar frequency of negative reactions in the place of an injection, respectively 10,3% and 13,3%.
In a children's age group with achrestic diabetes, when comparing safety and efficiency of introduction as background drug – insulin of a glargin (once at 24 o'clock in the evening) or insulin isophane (twice a day in the morning and in the evening) with p / to administration of insulin lizpro and insulin of a glulizin (in 15 minutes prior to food), in both groups comparable indicators of glycemic control, frequency of serious hypoglycemic episodes and frequency of forming of the hypoglycemia demanding foreign intervention were revealed. Thus after carrying out therapy for 26 weeks, in group of use of Apidra, receiving glycemic control required significantly smaller increase of daily dosages of high-speed insulin, background drug and the total insulin dose, in comparison with group using insulin lizpro.
When carrying out clinical testings at adult patients, any distinctions in efficiency and safety of use of Apidra by patients of different floors and various races it was not revealed.
At Apidra's use amino acid replacement processes asparagine of insulin of the person on a lysine in VZ position, and also a lysine on glutaminic acid in a B29 position, promote the fastest absorption of drug.
AUC drug in all groups of patients (the healthy volunteers and patients suffering from the 1 and 2 type of a diabetes mellitus) showed the absorption exceeding twice and Apidra's Cmax in comparison with soluble insulin of the person.
When carrying out researches with involvement of patients with juvenile diabetes, after p / to an injection of 0,15 PIECES/kg of Apidra of his Cmax it was reached for 55 minutes and equaled 82±1,3 mked/ml whereas these parameters for human analog respectively made 46±1,3 mked/ml and 82 minutes. The average duration of finding of insulin of a glulizin in a system blood-groove was less (98 min.), than at insulin of the person (161 min.).
When carrying out researches with involvement of patients with non-insulin-dependent diabetes, after p / to an injection of 0,2 PIECES/kg of Apidra, average Cmax of its active ingredient equaled 91 mked/ml (in the range of 78-104 mked/ml).
Drug absorption, in a case p / to an injection of Apidra led to the area of a hip was the lowest and increased at administration of drug to the area of a shoulder. The highest absorption was observed at injection introduction to the region of a front abdominal wall. At p / to introduction absolute bioavailability of drug Apidra equaled about 70% (a hip – 68%; a shoulder – 71%; the abdominal wall – 73%) was also characterized by low variability at different patients.
At in introduction distribution of insulin of a glulizin and its subsequent removal is similar to those parameters for soluble insulin of the person and makes respectively: Vd – the 13th liter and 22 liters; T1/2 – 13 minutes and 18 minutes. At p / to an injection removal of insulin of a glulizin happens quicker (to T1/2 – 42 minutes) in comparison with human analog (with T1/2 – 86 minutes). When carrying out the cross analysis of results of researches and testings of insulin of a glulizin, including healthy volunteers and patients with the 1 and 2 type of diabetes, the seeming T1/2 of this drug was in an interval of 37-75 minutes.
The conducted research with involvement of the persons without diabetes mellitus but having renal pathologies of various degree of manifestation (at KK it is more than 80 ml/min., 30-50 ml/min. and less than 30 ml/min.) showed preservation of average parameter of speed of action of Apidra. However at pathologies of kidneys allow reduced need for insulin use.
At liver pathologies studying of pharmacokinetic indicators of Apidra was not carried out.
Influence of advanced age of the patient on pharmacokinetic features Apidra is up to the end not studied.
The pharmacodynamics and Apidra's pharmacokinetics were investigated in children's age groups of patients with achrestic diabetes of 7-11 years and 12-16 years. Indicators of absorption, Tmax and Cmax of drug in both of these groups were comparable to those for adult patients. At Apidra's injection just before testing with meal, the best control of plasma glucose after food in comparison with human insulin is observed. Increase in content of plasma glucose after food (AUC0-6 of hours) equaled for Apidra – 641 мг/ч×дл, for soluble insulin of the person – 801 мг/ч×дл.
Indications to use
Purpose of insulin of Apidr is shown to patients is more senior than 6 years at juvenile (insulin-dependent) diabetes.
Use of drug of Apidr Solostar is contraindicated at a hypoglycemia and personal hypersensitivity.
Noted negative manifestations when using drug of Apidr were the reactions characteristic of this pharmacological class of drugs, so and for all existing insulin.
The most significant negative manifestation of an insulin therapy observed from system of a metabolism is the hypoglycemia which most often arises at unreasonable use of the overestimated insulin dosages.
The hypoglycemia symptomatology, as a rule, appears suddenly. Nevertheless, to the disturbances of psychoneurological character which are formed against a neuroglycopenia (unusual weakness or fatigue, headaches, feeling of fatigue, decrease in concentration, visual frustration, drowsiness, a convulsive syndrome, nausea, a confusion/loss of consciousness) precede manifestation of adrenergic counterregulation (irritability, feeling of hunger, nervous excitement, pallor of skin, a tremor, cold sweat, concern, tachycardia, strong heartbeat). Weight of this symptomatology depends on speed and weight of the developing hypoglycemia.
The repeating heavy episodes of a hypoglycemia can become the reason of defeat or frustration of a nervous system. The expressed and long hypoglycemia can be life-threatening patients as increase of its symptoms can lead to death.
Reactions of immune system can be shown by the local phenomena of personal hypersensitivity to Apidra (including a hyperemia, feeling of an itch and puffiness in an injection venue). These phenomena, as a rule, are independently leveled after several days after carrying out an injection. In certain cases the similar symptomatology is shown not from insulin influence, and from irritation of integuments, owing to their preinjection antiseptic processing, and also because of the wrong carrying out p / to an injection.
System manifestations of personal hypersensitivity on Apidr's drug can be followed by forming of rash (perhaps with an itch) on all body, feeling of constraint in a breast, decrease in the ABP, asthma, increase of pulse or a hyperhidrosis. Heavy episodes of a generalized allergy including the anaphylactic phenomena, can be life-threatening.
Negative reactions from integuments are usually limited to the lipodystrophy capable, nevertheless, to reduce absorption of insulin of a glulizin. To forming of a lipodystrophy can bring frequent injections into the same place, without change of areas of administration of drug in this connection frequent change of venues of an injection (a hip, an abdominal wall, a shoulder), for the purpose of the prevention of development of a lipodystrophy is recommended.
Apidra, application instruction
Apidr Solostar's insulin is intended for p / to the introduction which is carried out shortly before (0-15 minutes) or right after food.
This drug has to be used in the therapeutic schemes including sharing of insulin long (perhaps analog) or average long efficiency, and also in parallel with peroral drugs of hypoglycemic action.
Dosing regime of Apidra is defined individually.
Apidra Solostar's introduction is carried out by means of carrying out p / to an injection, or by means of the continuous infusion which is carried out in a hypodermic fatty tissue with use of pompovy system.
Injection p / to introduction carry out to the area of a shoulder, an abdominal wall (front part) or a hip. Infusional introduction is carried out in a hypodermic fatty tissue to the region of an abdominal wall (front part). Places p / to introduction (a hip, an abdominal wall, a shoulder) should be alternated at each subsequent injection. Factors of the carried-out exercise stress, the other changing conditions, and also an injection site can influence speed of absorption and duration of influence of drug. The injection in an abdominal wall differs in faster time of absorption in comparison with introduction to a hip or a shoulder.
When carrying out an injection it is necessary to observe all possible precautionary measures for the purpose of an exception of administration of drug directly in vessels of circulatory system. After carrying out an injection it is forbidden to carry out massage in areas of introduction. All patients using Apidra Solostar are obliged to pass consultation on carrying out the correct technology of administration of insulin.
Apidra Solostar's mixing is allowed only with human insulin isofan. In process mixing of these drugs Apidra needs to be taken in the syringe first of all. P / to introduction it is necessary to carry out at once after mixing process. It is impossible to carry out to injections of the mixed drugs.
If necessary solution of drug can be extracted from the cartridge included in the syringe handle and to use in the pompovy device intended for continuous carrying out p / to infusion. In case of Apidra Solostar's introduction by means of pompovy infusional system, his mixing with any other drugs is not allowed.
When using infusional the set and the reservoir used with Apidr's drug them should be changed at least in 48 hours with observance of all rules of an asepsis. These recommendations can be excellent from stated in the general instructions to pompovy devices, nevertheless, their execution is very important for the correct carrying out infusion and the prevention of forming of serious negative consequences.
The patients undergoing procedure of introduction of Apidra p / to infusional in the continuous way have to have at themselves alternative injection systems of administration of drug, and also to be trained in the correct methods of its use (for a case of damage of the pompovy device).
When carrying out continuous infusion by Apidr's drug, malfunction of an infusional pompovy set, disturbance of its work, and also a mistake in manipulations with them can become very quickly the reason of forming of a hyperglycemia, diabetic ketoacidosis and a ketosis. In case of detection of these manifestations it is necessary to establish urgently the reason of their development and to eliminate it.
Use the syringe handle Solostar with Apidr's drug
Before the first use, Solostar it is necessary to take the syringe handle 1-2 hours at the room temperature.
Just before use the syringe handle it is necessary to examine attentively the cartridge placed in it which contents have to be colourless, transparent and not include visible firm foreign inclusions (to remind water on a consistence).
Used the syringe handle Solostar cannot repeatedly be applied and have to be utilized.
For the prevention of possible infection only one person can use one syringe handle, without giving her to other person.
At each new use the syringe handle needs to be connected carefully to it a new needle (exclusively compatible about Solostar) and to hold testing for safety.
At manipulations with a needle it is necessary to be extremely careful in order to avoid traumatizing and a possibility of infectious transfer.
It is necessary to avoid use the syringe handles at existence at them of damages, and also in cases of uncertainty in their work properly.
Always it is necessary to have in a stock reserve the syringe handle, on a case of loss or damage of the first.
The syringe handle it has to be protected from dirt and dust, it is admissible to wipe its external parts with wet fabric. Do not recommend to immerse the syringe handle in liquid, to wash or grease as it can lead to its damage.
Operational the syringe handle Solostar it is safe in work, differs in exact dosing of solution and demands the careful address. When carrying out all manipulations about the syringe handle it is necessary to avoid any situations which can lead to its damage. In case of any suspicions of its operability it is necessary to use another the syringe handle.
Just before carrying out an injection it is necessary to make sure of compliance of the recommended insulin, having checked marking on a label the syringe handle. After removal of a cap about the syringe handle it is necessary to carry out direct vision of its contents then to establish a needle. Only the colourless, transparent, reminding water on a consistence and not including any foreign firm inclusions insulin solution is allowed to introduction. For each subsequent introduction it is necessary to use a new needle which has to be sterile and correspond the syringe handle.
Before carrying out an injection surely carry out testing for safety, check correctness of work the syringe handle and the needle established on it, and also delete from solution vials of air (at their existence).
For this purpose at removed outside and internal caps of a needle measure a dose of solution, equal 2 PIECES. Directing a needle the syringe handle strictly up, accurately tap with a finger on a cartridge, trying to displace all vials of air to the established needle. Press on the button intended for administration of drug. In case of its emergence on a tip of a needle it is possible to consider that the syringe handle works as it is necessary. If it does not occur, repeat the above described manipulations up to achievement of desirable result.
After carrying out testing for safety the dosing window of the syringe handle has to show 0 value then it is possible to establish a necessary dosage. The entered dose of drug has to be measured with an accuracy of 1 PIECE, in the range of dosages from 1 PIECE (minimum) to 80 PIECES (maximum). In need of introduction of a dose over 80 PIECES carry out two or more injections.
When carrying out an injection the needle installed on the syringe handle needs to be entered accurately under skin. The button the syringe handle intended for administration of solution has to be completely pressed and before extraction of a needle to remain in such situation for 10 seconds that provides full introduction of the established drug dose.
After carrying out an injection it is necessary to remove and throw out a needle. Thus, the prevention of introduction of an infection and/or pollution of the syringe handle, and also leak of drug and hit in an air cartridge is provided. After removal of the used needle, the syringe handle Solostar should be closed a cap.
During removal and utilization of a needle it is necessary to be guided by special rules and methods (for example, technology of installation of a cap of a needle one hand), for the purpose of decrease in risk of possible accidents, and also prevention of infection.
In case of excess administration of insulin there can be a hypoglycemia.
At an easy hypoglycemia, its negative manifestations can be stopped the use in food of sacchariferous products or glucose. To patients with a diabetes mellitus recommend to have always at themselves cookies, candies, pieces of sugar or sweet juice.
Heavy symptoms of a hypoglycemia (including neurologic frustration, spasms, a loss of consciousness, coma) have to be stopped by the second (specially trained) persons carrying out in oil or p / to injections of a glucagon or in/in administration of solution of the Dextrose. If use of a glucagon did not yield result for 10-15 minutes, turn on into maintaining a dextrose.
To the patient who recovered consciousness recommend to eat food carbohydrate-rich, racks to avoid repetition of a hypoglycemia.
For definition of origins of a heavy hypoglycemia and the prevention of its development further, it is necessary to observe the patient in a hospital.
Purposeful researches of pharmacokinetic interaction of insulin of a glulizin were not conducted. Considering the available stock of empirical knowledge which is saved up in the course of use of other similar drugs, forming of any clinically significant medicinal interactions is improbable. There are substances which can influence a glucosic metabolism and demand correction of dosages of insulin of a glulizin, and also further careful control over therapy.
Treat the substances increasing hypoglycemic efficiency of insulin and increasing risk of emergence of a hypoglycemia: fibrata, APF inhibitors, peroral hypoglycemic HP, salicylates, Disopyramidum, Fluoxetine, Pentoksifillin, monoaminoxidase inhibitors, Propoksifen, streptocides.
Treat the substances reducing hypoglycemic effects of insulin: glucocorticoids, Diazoxide, Danazol, diuretics, derivative Fenotiazina, Isoniazid, Somatropin, hormones of a thyroid gland, sympathomimetics (Salbutamol, Epinephrinum, Terbutalin), progestins (oral contraceptives), antipsychotic drugs (Clozapine, Olanzapine), estrogen, protease inhibitors.
Lithium salts, beta adrenoblockers, ethanol, Clonidine can change hypoglycemic action of Apidra in this or that party. Parallel use of Pentamidine can lead to a hypoglycemia, and further to a hyperglycemia.
Under the influence of the medicines possessing sympatholytic activity (A clonidine, Reserpinum, beta adrenoblockers, Guanetidin), manifestations of adrenergic activation (reflex) can be expressed less or be absent completely.
Due to the lack of researches on compatibility, Apidra should not mix up with any other drugs except insulin isophane (human).
When using an infusional pomp Apidra's mixing with other drugs is not allowed.
Terms of sale
All insulin, including Apidr's drug, is prescription.
Range of temperatures of long-term storage of insulin of a glulizin has to correspond to 2-8 °C. Used the syringe handle it is possible to store at a temperature up to 25 °C, in the dark room.
Period of validity
Apidra Solostar can remain for 2 years from the moment of her production. Apidra period of validity, in applied at the moment the syringe handle, is equal to 4 weeks in this connection recommend to apply date of its first use on a syringe handle label.
The patient of insulin of other manufacturing plant or alternative insulin should carry out appointment under strict supervision of medical personnel, in connection with possible need of change of the dosing mode, owing to deviations in concentration of insulin, its type (insulin isophanes, soluble and so forth), a look (human, animal) and/or a production method. Also there can be a need of changes in in parallel the carried-out hypoglycemic therapy by peroral forms. The termination of treatment or use of inadequate dosages of insulin, in particular at patients with juvenile diabetes, can become the reason of forming of diabetic ketoacidosis and the hyperglycemia posing hazard to life of the patient.
The time interval of development of a hypoglycemia is caused by the speed of forming of insulin effect of the used drugs and so it can change at adjustment of the therapeutic scheme. To the circumstances changing harbingers of forming of a hypoglycemia or doing them less expressed, carry: insulin therapy intensification, long existence of a diabetes mellitus, existence of diabetic neuropathy, change of the insulin, reception of some HP (for example, beta adrenoblockers).
Correction of insulin dosages can be necessary at increase in exercise stresses by the patient or change of a daily diet. The physical exercises which are carried out right after food increase risk of emergence of a hypoglycemia. When using high-speed insulin development of a hypoglycemia happens quicker.
Noncompensated hyper — or hypoglycemic manifestations can become the reason of development of a coma, a loss of consciousness or even death.
Need for use of insulin can fluctuate at emotional overloads or diseases.
At performance by the patient of exact, dangerous works, and also driving of transport it is necessary to consider a possibility of forming hyper — or a hypoglycemia and to be careful.
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