Apidra

Apidra – a recombinant analog of insulin human, equal to it on action force, but the rendering more bystry and less long effect.

Form of release and structure

Dosage form of Apidra – solution for hypodermic (п / to) introductions: almost colourless or colourless transparent liquid (on 10 ml in bottles, 1 bottle in a cardboard pack; on 3 ml in cartridges, in packaging of planimetric cell: 5 cartridges for the syringe handle "Optipen" or 5 cartridges which are built in in one-time the syringe handle "Optiset", or 5 cartridge Optiklik systems).

Contains in 1 ml of solution:

• active ingredient: insulin глулизин – 3,49 mg (100 ME insulin human is equivalent);
• auxiliary components: трометамол, m cresol, polysorbate 20, sodium chloride, Acidum hydrochloricum concentrated sodium hydroxide, water for injections.

Indications to use

Apidra is applied to treatment of the diabetes mellitus demanding insulin therapy, at children 6 years are more senior, than teenagers and adult patients.

Contraindications

• hypoglycemia;
• children's age up to 6 years (clinical information on use is limited);
• hypersensitivity to insulin to a glulizin or to any other component of drug.

With care Apidra is recommended to be applied at pregnancy.

The insulin dose decline owing to reduction of a gluconeogenesis and delay of metabolism of insulin can be required by patients with a liver failure.

Decrease in need for insulin is also possible at a renal failure and at advanced age (for a cause of infringement of function of kidneys).

Route of administration and dosage

Apidr's insulin is entered just before meal (in 0-15 min.) or right after food by п / to an injection or continuous infusion into a hypodermic fatty tissue with use of pompovy system.

The dose and the mode of administration of drug are selected individually.

Apidr's solution is applied in complex schemes of therapy with insulin of average duration of action or with an insulin/analogue of insulin of long action, the combined use with peroral hypoglycemic drugs is allowed.

The recommended body parts for administration of drug:

• п / to an injection – make to the area of a shoulder, hip or stomach, at the same time introduction to an abdominal wall gives a little more bystry absorption;
• continuous infusion – is made in a hypodermic fatty tissue in a stomach.

It is necessary to alternate places of infusions and injections at each subsequent administration of drug.

As the dosage form of Apidra – solution, before its use of carrying out resuspending is not required.

Speed of absorption and, respectively, the beginning and duration of effect of drug can change under the influence of an exercise stress, depending on an injection site of solution and other changing factors.

It is required to be careful at administration of drug to exclude probability of its hit directly in blood vessels. After the procedure it is not necessary to mass area of introduction.

Patients it is necessary to teach technique of carrying out injections.

At administration of drug by means of pompovy system for insulin infusion solution cannot be mixed with any other medicinal substances / means.

Apidr's solution does not mix up with any other drugs except for human isophanes insulin. At the same time Apidra is taken in the syringe of the first, and the injection is carried out right after mixing. Data on use of the solutions mixed long before carrying out an injection no.

Cartridges it is necessary to use with insulin the syringe handle "Optipen Pro1" or similar devices in strict accordance with the recommendations about loading of a cartridge, accession of a needle and carrying out an injection of insulin provided in the instruction from the producer. Before use of a cartridge it is necessary to carry out a visual inspection of drug. Only the transparent, colourless, not containing visible firm inclusions solution suits for injections. Before installation the cartridge needs previously to be sustained within 1-2 hours at the room temperature, and before administration of solution it is necessary to remove vials of air from a cartridge.

The used cartridges cannot be filled repeatedly. Damaged the syringe handle "Optipen Pro1" it is impossible to use.

In case of malfunction the syringe handle solution can be gathered from a cartridge in the plastic syringe suitable for insulin in concentration of 100 ME/ml then to enter to the patient.

The syringe handle of reusable use is used to injections only to one patient (in order to avoid infection).

Also it is necessary to follow all above-mentioned recommendations and rules when using for administration of solution of Apidr of cartridge system and the syringe handle "Optiklik", representing glass cartridge with the attached piston mechanism fixed in a transparent plastic container and containing 3 ml of solution of insulin of a glulizin.

Side effects

The most frequent undesirable side effect of an insulin therapy – a hypoglycemia; usually it arises when using insulin in the doses considerably exceeding required.

The side adverse reactions connected with administration of drug, from bodies and systems of patients, registered during clinical trials (the list is given with use of the following gradation of frequency of occurrence: more than 10% – are very frequent; more than 1%, but less than 10% – are frequent; more than 0,1%, but less than 1% – sometimes; more than 0,01%, but less than 0,1% – are rare; less than 0,01% – are very rare):

• metabolism: very often – the hypoglycemia accompanied with the following suddenly arising symptoms: cold sweat, pallor of integuments, fatigue, concern, a tremor, nervous arousing, weakness, confusion of consciousness, drowsiness, difficulty of concentration of attention, visual frustration, nausea, excessive feeling of hunger, a headache, the expressed heartbeat; increase of a hypoglycemia can be effects: a loss of consciousness and/or emergence of spasms, temporary or continuous deterioration in function of a brain, in extreme cases the lethal outcome is possible;
• skin and hypodermic fabrics: often – allergic manifestations, such as puffiness, a hyperemia, an itch in an injection site, at therapy continuation usually passing independently; seldom – a lipodystrophy, generally owing to disturbance of alternation of injection sites of insulin in any of areas / repeated administration of drug to the same place;
• hypersensitivity reactions: sometimes – suffocation, feeling of constraint in a breast, urticaria, an itch, allergic dermatitis; in hard cases of generalized allergic reactions (including anaphylactic) the threat of life is possible.

Special data on studying of symptoms of overdose of insulin of a glulizin are absent, but owing to long use of high doses of Apidra development of varying severity of a hypoglycemia is possible.

Therapy of a state depends on disease degree:

• episodes of an easy hypoglycemia – are stopped by means of the use of glucose or products containing sugar in this connection patients with a diabetes mellitus are recommended to have constantly at themselves cookies, candies, refined sugar pieces, sweet fruit juice;
• episodes of a heavy hypoglycemia (with a loss of consciousness) – are stopped in oil (intramuscular) or п / to introduction of 0,5-1 mg of a glucagon, or in/in (intravenous) administration of glucose (dextrose) in case of lack of response to introduction of a glucagon for 10-15 min. After consciousness recovery the patient is recommended to give carbohydrates inside for the purpose of prevention of a repeated attack of a hypoglycemia then for establishment of the reason of a heavy hypoglycemia, and also prevention of development of similar episodes of the patient it is necessary to observe some time in a hospital.

Special instructions

In case of transfer of the patient into insulin from other producer or new type of insulin strict medical observation as correction of the carried-out therapy in general can be required is necessary.

Use of insulin in inadequate doses or the unreasonable termination of therapy, especially at patients with a diabetes mellitus of 1 type, can become the reason of development of a hyperglycemia and diabetic ketoacidosis – potentially life-threatening states. Time of probable development of a hypoglycemia directly depends on the speed of effect of the applied insulin and can change in this regard at correction of the scheme of therapy.

The main conditions which can change or make less expressed symptoms of development of a hypoglycemia:

• long existence of a diabetes mellitus at the patient;
• diabetic neuropathy;
• insulin therapy intensification;
• concomitant use of some medicines, for example, β-adrenoblockers;;;;;;;;;;
• transition to human insulin from insulin of animal origin.

Correction of doses of insulin can be also necessary in case of change of the modes of a physical activity or food. The strengthened exercise stress received directly after meal can increase probability of development of a hypoglycemia. In comparison with effect of soluble human insulin the hypoglycemia can develop rather after introduction of high-speed analogs of insulin.

Owing to noncompensated hypo - or hyper glycemic reactions are possible a loss of consciousness, development of a coma or a lethal outcome.

Associated diseases or emotional overloads can also change need of the patient for insulin.

Medicinal interaction

Researches on pharmacokinetic medicinal interaction of drug of Apidr were not conducted, but on the basis of the data which are available concerning similar medicines it is possible to draw a conclusion that clinically significant pharmacokinetic interaction is improbable.

Some medicinal substances / drugs are capable to exert impact on glucose metabolism owing to what correction of doses of insulin of a glulizin and more careful control of the carried-out therapy and a condition of the patient can be required.

So at combined use with Apidr's solution:

• peroral hypoglycemic drugs, inhibitors of an angiotensin-converting enzyme, Disopyramidum, fluoxetine, fibrata, monoamine oxidase inhibitors, the propoxyhair dryer, пентоксифиллин, sulfanamide antimicrobic means, salicylates – are capable to strengthen hypoglycemic effect of insulin and to increase predisposition to a hypoglycemia;
• glucocorticosteroids, diuretics, даназол, diazoxide, an isoniazid, соматропин, derivatives of a fenotiazin, sympathomimetics (Epinephrinum/adrenaline, тербуталин, salbutamol), estrogen, hormones of a thyroid gland, progestins (oral contraceptives), antipsychotic medicines (olanzapine, clozapine), protease inhibitors – are capable to reduce hypoglycemic effect of insulin;
• the clonidine, β-adrenoblockers, ethanol, lithium salts – potentiate or weaken hypoglycemic influence of insulin;
• pentamidine – is capable to cause a hypoglycemia with the subsequent hyperglycemia;
• drugs with sympatholytic activity (β-adrenoblockers, гуанетидин, a clonidine, Reserpinum) – at a hypoglycemia can reduce expressiveness or mask symptoms of reflex adrenergic activation.

Researches of compatibility of insulin of a glulizin were not conducted therefore Apidr should not mix with any other drugs, an exception – human isophanes insulin.

In case of administration of solution by means of an infusional pomp Apidr cannot mix with other drugs.

Terms and storage conditions

To store in own cardboard packaging, without light access, at a temperature of 2-8 °C. Not to freeze. To protect from children!

After opening of packaging to store in the place protected from light at a temperature up to 25 °C. A drug period of validity after the first use – 4 weeks (on the label it is recommended to celebrate date of the first intake of solution).

Period of validity – 2 years.