Glatirate - instructions for use, dose, side effects, contraindications

Active substanceGlatiramer acetateGlatiramer acetate

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Dosage form: & nbsphypodermic solution

Composition:

1 ml of the solution contains:

active substance: glatiramer acetate 20 mg;

Excipients: Mannitol - 40 mg, water for injection - up to 1 ml.

Description:

The clear or slightly opalescent solution from colorless to pale yellow.

Pharmacotherapeutic group:Immunomodulating agent

ATX: & nbsp

L.03.A.X.13 Glatiramer acetate

Pharmacodynamics:

Glatiramer acetate is an acetic acid salt of a mixture of synthetic polypeptides formed by 4 natural amino acids: L-glutamic acid, L-alanine, L- tyrosine and L-lizinom and on the chemical structure has elements of similarity with the basic protein of myelin.

Glatiramer acetate alters the course of the pathological process in demyelinating central nervous system (CNS) disease - multiple sclerosis, which refers to autoimmune diseases that alter the ratio of T-suppressors in the body. Glatiramer acetate performs immunomodulatory action at the injection site.Its therapeutic effect is mediated through the systemic spread of activated T-suppressors. Glatiramer acetate has a specific mechanism of action, which is based on the ability to competitively replace the myelin antigens - myelin basic protein, myelin oligodendrocyte glycoprotein and proteolipid protein in places of binding with molecules of the main histocompatibility complex of class 2 located on antigen-presenting cells.

The consequence of competitive displacement is two reactions: stimulation of antigen-specific suppressor T-lymphocytes (Th2-type) and inhibition of antigen-specific effector T-lymphocytes (Th1-type). Activated T-suppressor lymphocytes enter the systemic circulation and penetrate the central nervous system. When they reach the site of inflammation in the central nervous system, these T-lymphocytes are reactivated with myelin antigens, which leads to the production of anti-inflammatory cytokines (including IL-4, IL-6, IL-10), which reduce local inflammation by suppressing local inflammatory T cell response. This results in the accumulation of specific anti-inflammatory cells Th2-type and inhibition of the proinflammatory system Th1-cells.

Besides, glatiramer acetate stimulates the synthesis of the neurotrophic factor by T cellsh2-type and protects brain structures from damage (neuroprotective effect). Glatiramer acetate does not have a generalized effect on the main links of normal immune reactions of the body, which fundamentally distinguishes it from nonspecific immunomodulators, including interferon-beta preparations. The resulting antibodies to glatiramer acetate in long-term use do not have a neutralizing effect, which reduces the clinical effect of the drug.

Pharmacokinetics:

Due to the peculiarities of the chemical structure of glatiramer acetate, which is a mixture of polypeptides formed by natural amino acids, as well as a low therapeutic dose, the pharmacokinetics data are only indicative. Based on them, as well as on experimental data, it is believed that, after subcutaneous administration, the drug is rapidly hydrolyzed at the site of administration. Hydrolysis products, as well as a small part of unchanged glatiramer acetate, can enter the lymphatic system and partially reach the vascular bed.The determined concentration of glatiramer acetate or its metabolites in the blood does not correlate with the therapeutic effect.

Indications:

- Clinically isolated syndrome (the only clinical episode of demyelination, suggesting multiple sclerosis) with the severity of the inflammatory process, requiring the use of intravenous glucocorticosteroids (to slow the transition to clinically significant multiple sclerosis);

- Rescidivating-remitting multiple sclerosis (to reduce the frequency of exacerbations, slowing the development of disabling complications).

Contraindications:

- Hypersensitivity to glatiramer acetate or mannitol;

- pregnancy;

- children under 18 years of age (due to lack of data on effectiveness and safety).

Carefully:

- Ppatients who are predisposed to allergic reactions and with cardiovascular diseases;

- patients with impaired renal function should regularly monitor laboratory indicators.

Pregnancy and lactation:

Adequate and well-controlled studies of the safety of glatiramer acetate in pregnancy have not been carried out, therefore the use of glatiramer acetate is contraindicated in pregnancy.Therefore, during the treatment with the drug it is recommended to use reliable methods of contraception.

It is not known whether glatiramer acetate with breast milk, so if you need to use the drug during lactation, you should correlate the expected benefit of therapy for the mother and the potential risk for the child.

Dosing and Administration:

The recommended dose for adult patients 18 years of age and older is 20 mg of glatiramer acetate (contained in a single injection syringe), subcutaneously once a day, preferably at the same time, for a long time.

The decision on the duration of therapy should be made by the attending physician on an individual basis.

Recommendations for patients on the independent use of the drug

Selecting a site for injection:

- for injection, remove one blister from the package. The remaining blisters with syringes should be stored in their original packaging in the refrigerator. If it is not possible to store syringes in the refrigerator, they can be temporarily stored at room temperature (15-25 ° C) for not more than a month, while the drug in the syringe retains its properties only on condition of an unopened blister.In this case, the date of withdrawal of the drug from the refrigerator is placed on a pack of syringes in a specially designated place.

- soak the syringe with the drug for about 20 minutes at room temperature;

- Wash your hands thoroughly with soap and water;

- Select the injection site (see Figure 1) - one of the seven recommended areas that allow the drug to be administered most painlessly. Do not inject in the same area for two consecutive days, to avoid the possible development of irritation and pain at the injection site. Also alternate skin segments within one area, marking them in a special diary. The skin site chosen for injection should be non-palpable, without swelling, redness, and rash.

Introduction of the drug:

- remove the syringe from the blister;

- remove the additional polypropylene cover and protective cap from the needle; - Gently grasp the skin in the crease between the thumb and forefinger of the free hand (see Figure 2);

- Insert the needle into the skin fold perpendicular to the skin surface, as shown in Figure 3;

- enter the entire volume of the drug, evenly pressing the plunger of the syringe;

- pull out the needle by pulling the syringe back vertically to the surface of the skin;

- throw the syringe into a special container with impenetrable walls.

Immediately notify your doctor of an excess of your prescribed dose and any unusual sensations after the injection.

If you forgot to do the injections on time, you should inject the drug as soon as you remember it, but you can not double the dose. The next dose is administered only after 24 hours.

After the injection, it is possible to develop immediate post-injection reaction (see section "Side effect").

In case of incomplete administration of the drug, a syringe with residual solutions is discarded.

Use in children

The drug is not recommended for use in children and adolescents under the age of 18, since adequate and strictly controlled clinical studies of the safety of the drug in this contingent of patients have not been conducted.

Side effects:

Glatirate is safe and well tolerated by patients. In some cases, the following adverse reactions may occur. The frequency of unwanted reactions is classified as follows: very often (> 1/10); often (> 1/100, but <1/10): infrequently (> 1/1000, but <1/100); rarely (> 1/10000, but <1/1000).

Infections and invasions: very often - infections, influenza; often - bronchitis, gastroenteritis, otitis media, Herpes simplex, rhinitis, periodontal abscess, vaginal candidiasis *; infrequently - abscess, inflammation of subcutaneous fat, furunculosis, pyelonephritis, Herpes zoster.

Neoplasms, including polyps and cysts: often - benign neoplasms of the skin, neoplasms; infrequently - skin cancer.

From the hematopoietic and lymphatic systems: often - lymphadenopathy *; infrequently - leukocytosis, leukopenia, splenomegaly, thrombocytopenia, a change in the morphology of lymphocytes.

From the immune system: often - hypersensitivity reactions.

From the endocrine system: infrequently - goitre, hyperthyroidism.

From the side of metabolism and nutrition: often - anorexia, weight gain *; infrequent alcohol intolerance, gout, hyperlipidemia, hypernatremia, decreased ferritin concentration in serum.

Mental disturbance: very often - anxiety *, depression; often - nervousness; infrequent - unusual dreams, psychosis, euphoria, hallucinations, aggressiveness, mania, personality disorders, suicidal attempts.

From the nervous system: very often - headache; often - perversion of taste, hypertension of muscles, migraine, speech disorders, fainting, tremor *; infrequently - tunnel wrist syndrome, cognitive disorders, convulsions, dysgraphia, dyslexia, dystonia, motor function disorders, myoclonus. neuritis, neuromuscular blockade, nystagmus, paralysis, peroneal nerve palsy, stupor, visual field defect.

From the side of the organs of sight: often - diplopia, impaired vision *; infrequently - cataract, corneal damage, dryness of sclera and cornea, hemorrhage in the eye, ptosis of the eyelids. mydriasis, atrophy of the optic nerve.

From the organs of hearing and balance: often - hearing impairment.

From the side of the cardiovascular system: very often - vasodilation *; often - a feeling of palpitations *, tachycardia *; infrequently - extrasystole, sinus bradycardia, paroxysmal tachycardia, increased blood pressure, varicose veins.

From the respiratory system: very often - shortness of breath *; often - cough, seasonal rhinitis; infrequently - apnea, sensation of suffocation, epistaxis, hyperventilation of the lungs, laryngospasm, pulmonary disorders.

From the gastrointestinal tract: very often - nausea *; often - rectal disorders, constipation, caries, dyspepsia, dysphagia, incontinence, vomiting *; infrequently - colitis, enterocolitis, polyposis of the large intestine, belching, peptic ulcer disease, periodontitis, rectal bleeding, enlargement of the salivary glands.

From the liver and bile ducts: often - deviation of liver function tests; infrequently - cholelithiasis, hepatomegaly.

From the skin and subcutaneous fat: very often - skin rash; often - ecchymosis, hyperhidrosis,, skin itching, skin diseases *, urticaria; infrequently - angioedema, contact dermatitis, erythema nodosum, cutaneous nodules.

From the musculoskeletal system and connective tissue: very often - arthralgia, back pain *; often - pain in the neck; infrequently - arthritis, bursitis, pain in the side, muscle atrophy, osteoarthritis.

From the side of the kidneys and the urinary system: often imperative urges, pollakiuria. retention of urine; infrequently - hematuria, nephrolithiasis, urinary tract diseases, deviations from laboratory norms of urinalysis. Pregnancy. postpartum and perinatal conditions: infrequent - spontaneous abortion.

From the genitals and the breast: infrequent breast engorgement, erectile dysfunction, prolapse of pelvic organs, priapism, prostate diseases, deviation of laboratory parameters in smears from the cervical canal, dysfunction of the testicles, vaginal bleeding, vulvovaginal disorders.

Other: very often - asthenia, chest pain *, reactions at the injection site ***, pain *; often - chills *, face swelling *, atrophy at the injection site ***, local reactions *, peripheral edema, edema, fever; infrequently - hypothermia, immediate postinjection reaction, inflammation, cyst, hangover syndrome, mucosal diseases, post-vaccination syndrome, necrosis at the injection site.

* The probability of occurrence of such cases in patients taking Glatiramer acetate is more than 2% (> 2/100) compared with the placebo group. An undesired reaction without a "*" sign indicates a difference of less than or equal to 2%.

** "Reactions at the injection site" (various types) includes any undesirable events occurring at the injection site, with the exception of atrophy and necrosis, which are given separately.

*** Refers to localized lipoatrophy at the injection site.

In patients with multiple sclerosis, who received Glatiramer acetate During uncontrolled clinical trials, as well as during postmarketing use, rare cases of anaphylactoid reactions (> 1/10 000 but <1/1000) were recorded.

Overdose:

Data on drug overdose are not available.

In case of an overdose, adequate symptomatic treatment should be started.

Interaction:

The interaction between Glatirate and other drugs has not been studied enough.

No drug interaction was found, including the simultaneous use of Glatirate with drugs that are used to treat multiple sclerosis, including those with glucocorticosteroids (with combined use for up to 28 days). Very rarely the frequency of local reactions can increase.

In the study in vitro it was assumed that glatiramer acetate has a high level of communication with blood plasma proteins and is not displaced from the connection with the protein of the blood plasma alone, as well as phenytoin and carbamazepine. However, since Glatirate has a potential effect onprotein-binding substances, it is necessary to control its simultaneous use with other drugs.

Special instructions:

Patients should be informed of possible adverse reactions associated with the use of the drug.

At the beginning of treatment with Glatirat, control of a neurologist and a doctor with experience in the treatment of multiple sclerosis is necessary.

Patients should be informed of the possibility of the occurrence of adverse reactions, including those that occur immediately after the injection of Glatirate. Most of these symptoms are brief, spontaneously resolved without consequences. If serious adverse reactions develop, stop treatment immediately and consult your doctor or call for emergency medical attention. The decision to use symptomatic therapy is taken by a doctor.

Pain in the chest that occurs immediately after injection (see section "Side effect"), as a rule, is transient, lasts several minutes, has no connection with other symptoms, passes by itself without any clinical consequences. The mechanism of development of this symptom is unclear.

With prolonged use (for several months) of the Glatirate drug at the injection site, lipoatrophy may develop and in some cases - necrosis of the skin. In order to prevent the development of these local reactions, it is necessary to recommend the patient strictly follow the sequence of injection sites according to a scheme in which a mandatory daily change in the site for injection should be provided.

Patients with impaired renal function or cardiovascular disease should be under the supervision of a physician.

Due to the fact that Glatirate is an immunomodulating medication and is used in the treatment of autoimmune disease - multiple sclerosis, its application can be accompanied by changes in the functions of the immune system, and therefore the patient's immune system should be periodically monitored.

If the patient is unable to store syringes with Glatirate in the refrigerator, storage at a temperature of 15-25 ° C, but not more than one month, is allowed.

Effect on the ability to drive transp. cf. and fur:

Based on the available data, there is no need for special precautions for persons,driving a car or a complicated technique.

Form release / dosage:A solution for subcutaneous administration, 20 mg / ml.

Packaging:

1 ml of the drug in a disposable syringe of colorless glass type I with a bromobutyl plastic piston and the seal piston, a fixed needle, protected by a plastic cap and the additional polypropylene lid.

1 syringe is placed in an unmarked contoured cell pack of PVC / paper.

For 14 double contour mesh packages containing 1 syringe each, together with the instruction for use are placed in a cardboard pack.

Storage conditions:

Store in the original packaging in a dark place at a temperature of 2 to 8 ° C (in the refrigerator). Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003567

Date of registration:14.04.2016 / 16.03.2017

Expiration Date:14.04.2021