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

Active substanceGlatiramer acetateGlatiramer acetate

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BIOCAD, CJSC Russia

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:

From colorless to light yellow slightly opalescent solution.

Pharmacotherapeutic group:Immunomodulating agent

ATX: & nbsp

L.03.A.X.13 Glatiramer acetate

Pharmacodynamics:

Timexone® (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 the binding sites 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 entering 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 (IL-4, IL-6, IL-10, etc.). These cytokines reduce local inflammation by suppressing the local inflammatory T-cell response, which leads to 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 Th-2 cells and protects brain structures from damage (neuroprotective effect). The drug does not have a generalized effect on the main links of normal immune responses of the body, which fundamentally distinguishes it from nonspecific immunomodulators, including beta interferon preparations. The resulting antibodies to glatiramer acetate 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 dosage, the data on the pharmacokinetics of glatiramer acetate are only indicative. Based on them, as well as on experimental data, it is believed that after a subcutaneous injection the preparation is rapidly hydrolyzed at the site of administration. Products of hydrolysis, 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 that suggests multiple sclerosis) with the severity of the inflammatory process, requiring the use of intravenous glucocorticosteroids (to slow the transition to clinically significant multiple sclerosis).

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

Contraindications:

Hypersensitivity to glatiramer acetate or mannitol; children under 18 years of age (efficacy and safety not studied); pregnancy.

Carefully:

Predisposition to the development of allergic reactions, cardiovascular diseases, impaired renal function.

Pregnancy and lactation:

Data on the use of glatiramer acetate during pregnancy are not available, the possible risk of such use during pregnancy is not established. Glatiramer acetate contraindicated during pregnancy. When treating glatiramer acetate, reliable methods of contraception should be used. It is not known whether glatiramer acetate with breast milk, therefore, if you need to use during lactation, you should evaluate the expected benefit of therapy for the mother and the potential risk to the child.

Dosing and Administration:

In the form of subcutaneous injections of 20 mg glatiramer acetate (one filled with the injection syringe solution) once a day, preferably at the same time of the day. Treatment is long. The decision to discontinue therapy should be made by the attending physician.

Each syringe with the drug glatiramer acetate is intended only for single use.

Recommendations for use in patients:

1. Before administering the drug, make sure that you have everything you need for an injection:

- a syringe filled with the drug solution;

- alcohol napkin.

2. Take one contour mesh package with a filled syringe from the total package that should be stored in the refrigerator and let it sit at room temperature for at least 20 minutes.

3. Before using the preparation, wash your hands thoroughly with soap and water.

4. Before use, inspect the solution in a syringe. In the presence of suspended particles or a change in the color of the solution or damage to the syringe, it should not be used.

5. Select the area of the body for injection (the recommended areas for injections are indicated in Figures 1 and 2):

- Hands (back of the shoulder);

- Hips (anterior thighs other than the groin and knee);

- The abdomen (except for the white line and umbilical region);

- Buttocks.

Do not use painful points, discolored, reddened areas of the skin or areas with seals and nodules for injection.

Every day, choose a new site for the injection, so you can reduce discomfort and pain on the skin area at the injection site. Within each injection area, there are many points for the injection. Constantly change injection points within a specific area.

It is recommended to draw up a scheme for changing injection sites and to have it with you. On the body there are a number of areas in which it is difficult to do injections yourself (buttocks, hands), for this you may need the help of another person.

6. Remove the syringe from the individual contoured package, removing the paper label (strip).

7. Take the syringe in the hand that you are writing. Remove the protective cap from the needle.

8. Preliminarily treating the injection site with an alcoholic napkin, slightly gather the skin into the fold with the thumb and forefinger (Fig. 3).

9. With the syringe perpendicular to the injection site, insert the needle into the skin at an angle of 90 ° (Figure 4); inject the drug, evenly pressing the plunger of the syringe down to the end (until it is completely emptied).

10. Remove the syringe with the needle moving vertically upward, keeping the same angle.

11. A dry sterile cotton ball can be applied to the injection site. If necessary, you can glue it with a band-aid. It is not recommended to rub or massage the injection site after injection.

12. Dispose of used syringes only in a specially designated place, which is inaccessible to children.

If you forget to inject the Timexone® drug, inject immediately as soon as you remember it. Do not administer a double dose of the drug. Use the next syringe only after 24 hours.

Do not stop using Timexone® without consulting your doctor.

Correction of the dosing regimen

Correction of the dosing regimen is not provided. The drug is administered in a dose of 20 mg subcutaneously every day.

Side effects:

Glatiramer acetate is safe and well tolerated by patients. In some cases, the following adverse reactions may occur.

From the side of the blood and lymphatic system: lymphadenopathy, leukocytosis, leukopenia, splenomegaly, thrombocytopenia. change in the structure of lymphocytes.

From the immune system: hypersensitivity reaction, anaphylactoid reaction, angioedema.

From the endocrine system: hyperthyroidism.

From the side of metabolism: anorexia, weight gain, alcohol intolerance, gout, hyperlipidemia, hypernatremia, decreased ferritin concentration in serum.

From the nervous system: headache, anxiety, depression, euphoria, nervousness, pathological dreams, psychosis, hallucinations, hostility, mania, personality disorder, suicidal behavior, taste perversion, migraine, syncope, tunnel syndrome, cognitive disorders, tremor, convulsions, dysgraphia, dyslexia, violation motor functions, myoclonus, neuritis, neuromuscular blockade, paralysis, including peroneal nerve, stupor.

From the side of the organ of vision: diplopia, visual field defect, eye movement disorder, cataract, corneal damage, dryness of sclera and cornea, subconjunctival hemorrhage, age of ptosis, mydriasis, nystagmus, optic nerve atrophy, visual impairment.

From the side of the organ of hearing and balance: headache, hearing loss.

From the cardiovascular system: heart palpitations, tachycardia, extrasystole, sinus bradycardia, paroxysmal tachycardia, increased blood pressure, varicose veins.

From the respiratory system: cough, shortness of breath, seasonal rhinitis, apnea, hyperventilation of the lungs, laryngospasm.

From the digestive system: nausea, vomiting, edema of the tongue, constipation, caries, odontogenic periostitis, salivary gland enlargement, dyspepsia, dysphagia, belching, esophageal ulcer, colitis, enterocolitis, polyposis of the large intestine, anorectal disorders, rectal bleeding.

From the liver and bile ducts: cholelithiasis, hepatomegaly.

From the skin and subcutaneous tissues: ecchymosis, hyperhidrosis, skin rash, itching, urticaria, contact dermatitis, erythema nodosum, cutaneous nodules.

From the side of the musculoskeletal system and connective tissue: arthralgia, pain in the cervical spine, back pain, arthritis, bursitis, pain in the side, muscle atrophy, osteoarthritis.

From the urinary system: imperative urge to urinate, pollakiuria, urinary retention, hematuria, nephrolithiasis.

From the genitals and mammary glands: amenorrhea, mammary gland enlargement, erectile dysfunction, prolapse of pelvic organs, deviation of laboratory parameters in smears from the cervical canal, violation of the menstrual cycle, vulvovaginal disorders.

Infections: otitis media, bronchitis, gastroenteritis, exacerbation of diseases caused by N. simplex, rhinitis, vaginal candidiasis, inflammation of subcutaneous fat, furunculosis, pyelonephritis, herpes zoster.

Other: reactions immediately after the injection *, asthenia, fatigue, chills, fever, nasal bleeding, peripheral edema, a hangover state.

* Reactions immediately after injection

Local reactions: pain, redness, swelling, abscess, hematoma, lipoatrophy, skin necrosis. Systemic reactions: "tides" of blood, chest pain, palpitation, anxiety, shortness of breath, difficulty swallowing, urticaria. These symptoms are temporary and limited and do not require special intervention; they can also begin several months after the initiation of therapy, the patient may experience a symptom occasionally.

Overdose:

There are no data on an overdose of glatiramer acetate. In case of an overdose, careful observation and symptomatic treatment are indicated.

Interaction:

The interaction between glatiramer acetate and other drugs has not been adequately studied. No drug interaction was found, including simultaneous use of glatiramer acetate with drugs that are used to treat multiple sclerosis, including corticosteroids (with combined use for up to 28 days). Very rarely the frequency of local reactions can increase.

Special instructions:

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

Patients should be informed of the possible occurrence of adverse reactions, including those that occur immediately after the injection of Tymexone®.

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 long-term use (within a few months) of Thymexone®, lipoatrophy can develop at injection sites and, in isolated cases, skin necrosis. 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 Timexon ® is an immunomodulating drug and is used in the treatment of autoimmune disease - multiple sclerosis, its use can be accompanied by changes in the functions of the immune system, and therefore the patient's immune system should be periodically monitored. Syringes should be stored in the refrigerator at a temperature of 2-8 ° C.

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

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 vehicle or complex equipment.

Form release / dosage:

A solution for subcutaneous administration of 20 mg / ml.

Packaging:

1 ml per three-component sterile syringes from colorless neutral glass I hydrolytic class.

1 syringe per contour cell pack of polymer film. For 28 contour mesh packages together with instructions for use and napkins alcohol in an amount of 28 pcs. in a pack of cardboard.

Storage conditions:

At a temperature of 2 to 8 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003875

Date of registration:03.10.2016

Expiration Date:03.10.2021

The owner of the registration certificate:BIOCAD, CJSC BIOCAD, CJSC Russia

Manufacturer: & nbsp