Glatiramer acetate is a mixture of acetate salt of synthetic polypeptides formed by four natural amino acids: L-glutamic acid, L-alanine, L- tyrosine, and L-lysine and chemical structure has similarities to myelin basic protein.
The consequence of competitive displacement are 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 CNS. Getting into the site of inflammation in the CNS, these T cells are reactivated myelin antigens that leads to the production of inflammatory cytokines (including IL-4, IL-6, IL-10) which reduce the local inflammation by suppressing local inflammatory T -kletochnogo response. This leads to the accumulation of specific inflammatory cells and Th2-type braking system proinflammatory Th1 cells.
Furthermore, glatiramer acetate neurotrophic factor stimulates the synthesis of Th2-type structure and protects the brain from damage cells (neuroprotection). Glatiramer acetate does not have a generalized effect on the main elements of the normal immune response of the body, which distinguishes it from non-specific immunomodulators, including preparations of beta-interferons. The resulting antibodies to glatiramer acetate with prolonged use do not have a neutralizing effect that reduces the clinical effect of the drug.
Due to the nature of the chemical structure of glatiramer acetate is a mixture of polypeptides formed by natural amino acids, as well as a low therapeutic dose pharmacokinetic data have only an indicative value. Based on them, as well as experimental data suggest that after subcutaneous administration of the drug is rapidly hydrolyzed at the injection site. The hydrolysis products, as well as a small portion of unchanged glatiramer acetate may enter the lymphatic system and partly reach the vascular bed. Detectable concentration of glatiramer acetate or its metabolites in the blood is not correlated with the therapeutic effect.
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1 ml solution contains:
active substance: Glatiramer Acetate – 20 mg;
Excipients: Mannitol – 40 mg Water for injection – up to 1 ml.
– Clinically isolated Syndrome (only one clinical episode of demyelination, allowing assume multiple sclerosis) with the severity of the inflammatory process, requires the use of intravenous corticosteroids (to slow transition in clinically definite multiple sclerosis);
– we Are relapsing-remitting multiple sclerosis (to decrease the relapse rate, slowing the development of disabling complications).
– Hypersensitivity to glatiramer acetate or mannitol;
– Children up to age 18 years (due to lack of efficacy and safety data).
– Patients with a predisposition to allergic reactions and cardiovascular diseases;
– in patients with impaired renal function should be regularly monitoring of laboratory parameters.
Glatirat drug is safe and well tolerated by patients. In some cases, there may be side reactions listed below. The frequency of adverse reactions classified as follows: very often (> 1/10); often (> 1/100, but < 1/10): rare (> 1/1000, but < 1/100); rarely (> 1/10000, but < 1/1000).
Infections and infestations: very often – infections, influenza; often – bronchitis, gastroenteritis, otitis media, Herpes simplex, rhinitis, periodontal abscess, vaginal candidiasis *; infrequently – abscess, inflammation of the subcutaneous fat, abrasions, medicine, Herpes zoster.
Neoplasms, including polyps and cysts: often – benign tumors of the skin, tumors; rarely – skin cancer.
From the side of blood and lymphatic system: often – lymphadenopathy *; rarely – leukocytosis, leukopenia, splenomegaly, anemia, changes in the morphology of lymphocytes.
Immune system: often – a hypersensitivity reaction.
From endocrine system: rarely – goiter, hyperthyroidism.
On the part of metabolism and nutrition: often – anorexia, weight gain *; infrequently – alcohol intolerance, gout, hyperlipidemia, hypernatremia, decreased ferritin concentration in serum.
Mental disorders: very often – anxiety *, depression; often – nervousness; infrequently – abnormal dreams, psychosis, euphoria, hallucinations, aggression, delusions, personality disorders, suicide attempts.
From the nervous system: very often – headache; often – dysgeusia, hypertonia of muscles, migraine, speech disorder, fainting, tremor *; infrequently – carpal tunnel syndrome, cognitive disorders, seizures, dysgraphia, dyslexia, dystonia, motor function disorders, myoclonus. neuritis, neuromuscular blockade, nystagmus, paralysis, paralysis of the peroneal nerve, stupor, visual field defect.
From the side of view: often – diplopia, blurred vision *; infrequently – cataract, corneal injury, scleral and corneal dryness, eye hemorrhage, ptosis eyelids. mydriasis, optic atrophy.
For part of the hearing and balance: often – a hearing loss.
Cardio-vascular system: very often – vasodilation *; frequently – * palpitations, tachycardia *; infrequently – beats, sinus bradycardia, paroxysmal tachycardia, increased blood pressure, varicose veins.
The respiratory system: very often – shortness of breath *; often – cough, seasonal rhinitis; infrequently – apnea, choking sensation, epistaxis, hyperventilation, laryngospasm, pulmonary disorders.
Gastro-intestinal tract: often – nausea *; often – rectal disorders, constipation, caries, dyspepsia, dysphagia, incontinence of stool, vomiting *; rarely – colitis, enterocolitis, colonic polyposis, belching, esophageal ulcer disease, periodontitis, rectal hemorrhage, salivary gland enlargement.
Of the liver and biliary tract: often – a deviation of liver function tests; infrequently – cholelithiasis, hepatomegaly.
Skin and subcutaneous tissue: very often – skin rash; often – ecchymosis, hyperhidrosis, pruritus, skin diseases *, urticaria; infrequently – angioneurotic edema, contact dermatitis, erythema nodosum, skin nodules.
On the part of the musculoskeletal system and connective tissue disorders: very often – arthralgia, back pain *; often – pain in the neck; rarely – arthritis, bursitis, flank pain, muscle atrophy, osteoarthritis.
The kidneys and urinary system: often – urinary urgency, pollakiuria. urinary retention; infrequently – hematuria, nephrolithiasis, urinary tract diseases, deviations from standards laboratory urine analysis. Pregnancy. postpartum and perinatal conditions: rarely – spontaneous abortion.
On the part of the genital organs, and breast: infrequently – engorgement, erectile dysfunction, pelvic organ prolapse, priapism, prostatic diseases, laboratory abnormalities in smears of the cervix duct, impaired testicular function, vaginal bleeding, vulvovaginal disorders.
Other: often – fatigue, chest pain *, injection site reactions *** pain *; often – chills *, * swelling of the face, atrophy at the injection site, *** Local reaction *, peripheral edema, swelling, fever; infrequently – hypothermia, immediate Postinjection reaction, inflammation, cyst, hangover, diseases of the mucous membranes, post-vaccination syndrome, necrosis at the injection site.
* The probability of occurrence of such cases in patients taking Glatiramer acetate is greater than 2% (> 2/100) as compared to placebo. Undesired reaction without sign “*” indicates a difference of less than or equal to 2%.
** “reactions at the injection site” (different types) comprises any undesirable phenomena occurring at the injection site, except atrophy and necrosis are given separately.
*** Refers to localized lipoatrophy at the injection site.
Patients with multiple sclerosis treated Glatiramer acetate during uncontrolled clinical studies, and during the post-marketing use rare were fixed (> 1/10 000, but < 1/1000) cases anaphylactoid reactions.
How to accept, acceptance rate and dosage
The recommended dose for adult patients of 18 years and older – 20 mg glatiramer acetate (contained in the same syringe for injection), subcutaneously once daily, preferably in one and the same time, it is long.
The decision on the duration of therapy should take the treating physician on an individual basis.
If you forgot to do injections on time, you must enter the drug immediately, as soon as you remember about it, but you can not double the dose. The next scheduled dose is administered only after 24 hours.
After injection may develop immediate post-injection reactions.
Stored in original package in a dark place at a temperature of 2 to 8 ° C (in a refrigerator). Do not freeze.
Keep out of the reach of children.
The interaction between the drug and Glatirat other drugs studied enough.
Not reveal any drug interaction, including the simultaneous use of the drug Glatirat with drugs that are used for the treatment of multiple sclerosis, including corticosteroids (for combined use for up to 28 days). Extremely seldom the frequency of local reactions may increase.
In the in vitro study, it was assumed that glatiramer acetate has a high level of communication plasma proteins and is not displaced from the connection with plasma proteins on their own, as well as phenytoin and carbamazepine. However, because the drug Glatirat has potential impact on the protein-binding agents, it is necessary to control the simultaneous application of other medicines.
Patients should be informed about possible adverse reactions associated with the use of the drug.
At the beginning of treatment is necessary to monitor Glatirat neurologist and physician who has experience in the treatment of multiple sclerosis.
Patients should be informed of the possibility of adverse reactions, including those arising directly after the injection of the drug Glatirat. Most of these symptoms are short-lived, spontaneously resolved without consequences. With the development of serious adverse reactions should immediately discontinue therapy and contact your doctor or call an ambulance. The decision on the application of symptomatic therapy takes a doctor.
Chest pain occurring immediately after injection (see. The section “Side effect”) usually is transient in nature, continues for several minutes, is not related to other symptoms runs independently without any clinical consequences. The mechanism of development of this symptom is not clear.
With prolonged use (several months) Glatirat drug injection site lipoatrophy may occur and in rare cases – skin necrosis. In order to prevent the development of these local reactions, the patient should be advised to adhere strictly to the sequence of places for injections under the scheme, which should be made mandatory in the daily change of the place of injection.
Patients with impaired renal or cardiovascular disease should be under medical supervision.
Due to the fact that the drug is Glatirat immunomodulatory drug is used in treating autoimmune disease – multiple sclerosis, its use may be accompanied by changes in the immune system, and therefore should periodically monitor the condition of the patient’s immune system.
If the patient is not able to store the syringes with a drug in the refrigerator Glatirat then be stored at 15-25 ° C, but not more than one month.
Based on available data, there is no need for special precautions for persons driving or complicated equipment.
Data on drug overdose are not available.
In case of overdose should be initiated adequate symptomatic treatment.
Do not use beyond the expiration date.