Interferons are glycoproteins produced by mammalian cells. Three main classes of interferons have been identified: alpha, beta, and gamma. These classes are not homogeneous and may contain several different types of interferons that differ in molecular weight. Interferon beta is produced from various cell types, including fibroblasts and macrophages. It has antiviral activity, antiproliferative and immunomodulatory effects. It has an effect by connecting with human cells using specific receptors on their surface. Biological indicators of the effects of interferon include, in particular, neopterin and b2-microglobulin. After a single dose, the intracellular activity of serum 2-5A synthetase and neopterin, as well as the concentration of b2-microglobulin in the blood serum, increases during the day. The mechanism of action of the drug in multiple sclerosis has not yet been studied, for example, it may rely on the inhibition of endogenous interferon-gamma, which is an inflammatory mediator in this disease. In most patients, interferon beta reduces the relapse rate, reduces the severity of clinical symptoms and inhibit the development of physical disability. The clinical effects of treatment can only be assessed after using the drug for a year. After intravenous administration, the plasma concentration of the drug decreases according to an exponential curve. t1/2α is several minutes, t1/2β is several hours. Following subcutaneous or intramuscular injection, serum levels of interferon beta-1a are low but measurable within 12 to 24 hours. Methods of administration of the drug subcutaneously or intramuscularly are equivalent. In healthy volunteers, tmax after intramuscular injection is 3-15 hours, t1 / 2 10 hours. Interferon beta-1a is metabolized and excreted from the body through the liver and kidneys. The bioavailability of interferon beta-1a after subcutaneous administration is 50%, and tmax 1-8 h, t1 / 2 - 5 hours. The biological response increases within 6 hours after taking the first dose, reaches a maximum after 40-124 hours and remains elevated in within 7 days.
Interferon beta 1A: instructions for use
Relapsing-remitting multiple sclerosis. Secondary progressive multiple sclerosis in the active stage, with confirmed relapses. Individual demyelinating lesions with active inflammation, if alternative diagnoses have been ruled out, and if these symptoms are determined by a high risk of progression with a clinical diagnosis of multiple sclerosis. Detailed information - see: descriptions relating to individual drugs.
Contraindications
Hypersensitivity to natural or recombinant interferon, human or any ingredient of the drug, initiation of treatment during pregnancy, severe depression and/or suicidal ideation. In case of decompensated liver disease, do not use or use with extreme caution; be careful also in patients with severe liver disease, with clinical symptoms of active liver disease, in patients with alcohol dependence, with elevated ALT levels (> 2.5 x ULN), or taking other drugs that may affect liver function; consideration should be given to discontinuing treatment if the patient develops jaundice or other clinical signs of liver dysfunction. Use caution in patients with uncontrolled epilepsy taking anticonvulsants. Also, be careful in patients with depressive disorders, past or present, especially those with suicidal thoughts; in the event of symptoms of depression or suicidal thoughts, discontinuation of treatment should be considered. In patients with prior monoclonal gammopathy, the use of cytokines has been associated with vascular permeability leading to shock and death. Due to the lack of studies, it is not recommended for use in progressive multiple sclerosis. It is not recommended for the treatment of patients with relapsing multiple sclerosis who have had less than 2 relapses in the last two years or patients with secondary progressive multiple sclerosis who have not had an active phase of the disease in the last two years. Do not use in children under 12 years of age (lack of relevant studies). Caution should be exercised in patients with heart failure or ischemic heart disease, cardiac arrhythmias, renal insufficiency, as well as patients with severe myelosuppression or after treatment with immunosuppressive drugs. If symptoms of cardiomyopathy appear and a causal relationship between the onset of symptoms and treatment with interferon, severe hypersensitivity reactions (bronchospasm, anaphylaxis, urticaria), treatment should be discontinued. Flu-like symptoms associated with the use of interferon beta can worsen the health of people with cardiovascular disease. Monitoring of thyroid function is recommended in patients with thyroid dysfunction or as clinically indicated. In addition to routine laboratory testing, which is usually performed to monitor patients with multiple sclerosis before treatment and regularly during treatment, and then periodically after the disappearance of clinical symptoms, it is advisable to perform blood morphology and liver tests (for example, AST, ALT, and GGT). Patients with anemia, thrombocytopenia, leukopenia may require more intensive monitoring of blood morphology. Neutropenic patients should be closely monitored due to the risk of infection. In order to minimize the risk of necrosis at the injection site, patients should be instructed on the correct technique for administering the drug, patients who self-administer the drug should be periodically monitored, especially in the event of an injection site reaction; if the patient develops inflammatory processes associated with edema or fluid drainage at the injection site, the patient should be instructed to consult with the attending physician before continuing to use the drug. The content of human in the preparation creates the possibility of transmission of viral diseases or Creutzfeldt and Jakob diseases. There is also a risk of immunogenicity. The presence of antibodies that neutralize interferon beta may reduce the clinical efficacy of the drug. Preparations containing benzyl alcohol should not be used in children under 3 years of age.
Interaction with other drugs
Possible interaction with drugs that metabolize cytochrome P-450; Caution should be exercised in the case of simultaneous use of drugs with a low therapeutic index and clearance, which is largely dependent on hepatic cytochrome P-450, for example, antiepileptic drugs and some groups of antidepressants. The benefits and risks associated with the concomitant use of drugs with hepatotoxic effects should be considered. Use with caution with antiepileptic drugs or drugs that affect the circulatory system. The drug can be used with corticosteroids and ACTH. Use with other immunomodulatory drugs is not recommended due to lack of clinical experience in patients with multiple sclerosis.
Interferon beta 1A: side effects
The most common are flu-like symptoms (chills, fever, joint and muscle pain, headache, weakness, nausea), especially after the first dose of the drug, later these symptoms disappear. In addition, very often appear: neutropenia, lymphopenia, leukopenia, thrombocytopenia, anemia, asymptomatic increase in aminotransferase activity, headache, inflammation and other symptoms at the injection site. Often: a significant increase in the activity of aminotransaminases, depression, insomnia, diarrhea, vomiting, nausea, itching, rash, alopecia, muscle or joint pain, pain at the injection site, fatigue, chills, fever. Infrequently: thyroid dysfunction (most often hyperthyroidism or hypothyroidism), hepatitis, convulsions, retinal vascular dysfunction, thromboembolic complications, shortness of breath, urticaria, necrosis, infiltrates or abscesses at the injection site, infection at the injection site, increased sweating. Rare: thrombocytopenic purpura, hemolytic uremic syndrome, pancytopenia, anaphylactic reactions, liver failure, autoimmune hepatitis, suicide attempts, angioedema, erythema, skin reactions such as erythema multiforme, Stevens-Johnson syndrome, systemic lupus erythematosus, connective tissue inflammation in injection site. In addition, at an unknown frequency: transient neurological symptoms (i.e., numbness, muscle cramps, paresthesias, gait disturbance (dysbasia), muscle and joint stiffness), which may mimic symptoms of an exacerbation of multiple sclerosis. Interferons may be associated with anorexia, dizziness, restlessness, arrhythmia, vasodilation and palpitations, heavy menstrual bleeding and vaginal bleeding. During treatment with interferon beta, an increase in the production of autoantibodies may occur. The frequency of adverse reactions at the injection site can be reduced by using an automatic injector. Approximately 8% of patients develop antibodies that neutralize interferon after 12 months of treatment, which can lead to a decrease in the effectiveness of the drug. For detailed information on the side effects of individual drugs, see the registered materials from the manufacturer. In case of overdose, patients should be hospitalized for observation and supportive treatment.
Pregnancy and lactation
Category C. Interferons may increase the risk of miscarriage. Do not start treatment during pregnancy. Do not use while breastfeeding. Women of childbearing age should use effective contraception.
Interferon beta 1A: dosage
Intramuscularly, subcutaneously. Medication regimens - see descriptions of individual drugs
Notes
Some nervous system side effects may affect the ability to drive and operate machinery. The drug should be stored at a temperature of 2-8 ° C.
Preparations on the Polish market containing interferon beta 1A
Avonex 30mcg/ml (lyophilisate)
Rebif 44 mcg/0.5 ml (syringe)
Types of medication, commercial names of analogues, release forms
Interferon is most commonly available as a lyophilisate ( form of release of the drug, in which the active substance is first dried and then frozen). It can also be found as a solution for subcutaneous injection ( injections), solution for inhalation and topical application, ointment, as well as a lyophilisate for preparing a solution for nasal rinsing ( nasal solution).Different types of interferon can be found on sale under other names - Interferal, Interal, Viferon, Altevir, Inferon, Rebif, Extavia, etc.
Interferon manufacturers
| Company manufacturer | Commercial name of the drug | The country | Release form | Dosage |
| immunodrug | Interferon | Russia | The dosage should be selected by the attending physician individually in each case. | |
| Microgen | Interferon | Russia | Lyophilizate for the preparation of intramuscular injections. | |
| Biocard | Interferon beta-1 b | Russia | Solution for the preparation of subcutaneous injections. | |
| Microgen | human leukocyte interferon | Russia | Lyophilizate for the preparation of inhalations and washing the nasal cavity. | |
| Biomed | Interferon human leukocyte liquid | Russia | Solution for inhalation and topical application. | |
| SPbNIIVS FMBA | Interferon human leukocyte dry | Russia | Lyophilizate for preparing a solution for washing the nasal cavity. |
The mechanism of the therapeutic action of the drug
Interferons are small peptide ( protein) molecules that regulate intercellular interactions ( are cytokines). Interferons show their properties quite actively even in very low concentrations. It has been proven that only one molecule of interferon is able to make the cell of the body completely tolerant to the virus. It is also worth noting that some properties of interferon are not yet fully understood. Interferon is able to have the following types of action on the body:
- antiviral action;
- antitumor activity.
Antitumor activity carried out by the action of the p53 protein. This protein becomes active due to DNA damage and can be produced by any cell in the body. Subsequently, the p53 protein stops the cell cycle of the development of a damaged cell, and in case of significant and irreversible defects in the genetic material, causes its apoptosis. It should be noted that in malignant neoplasms ( cancerous tumors) in about half of the cases, there is a violation of the function of the p53 protein.
Regardless of the form of release ( intramuscular or subcutaneous injections) the body absolutely completely assimilates this drug ( bioavailability 100%). Within 4-12 hours after application, the maximum concentration of interferon is observed in the blood.
For what pathologies is it prescribed?
In most cases, interferon is used in the treatment of various viral infections. Also, due to its antitumor effect, it can be prescribed for certain oncological diseases. It is worth noting that single and weekly dosages can be reduced if interferon is poorly tolerated.The use of interferon
| Name of the pathology | Mechanism of action | Dosage |
| Viral diseases | ||
| Chronic hepatitis B | Affects a special enzyme oligoadenylate cyclase. Subsequently, the process of synthesizing virus particles, as well as their release, is almost completely inhibited in the cell. Stimulates the production of proteins of the histocompatibility complex and immunoproteasome, which greatly increases the activity of the body's immune cells that fight viral infection. | Intramuscularly or subcutaneously. The weekly dosage is 30-35 million IU ( international units). The drug is used every day for 5 million IU or every other day for 10 million units ( three times a week). The course of treatment lasts 16 - 24 weeks. |
| Chronic hepatitis C | Intramuscularly. Adults: 3 million units three times a week. When administered subcutaneously, interferon can be used either alone or together with ribavirin. | |
| Chronic hepatitis D (Delta) | 5 million units subcutaneously three times a week. The course of treatment is 12 - 16 months. | |
| Papillomatosis (disease caused by the human papillomavirus) | After removal of the tumor, the drug is administered subcutaneously at 3 million units three times a week. The duration of treatment is 5 - 6 months. Sometimes the doctor may extend the treatment. | |
| Kaposi's sarcoma on the background of AIDS (numerous malignant skin tumors) | Selected individually. | |
| Herpes eye | Instill 2-3 drops in each eye. Do not instill more than 6 - 7 times a day. With a decrease in the severity of symptoms, the number of drops should be reduced to one. The duration of treatment should not exceed 8 - 10 days. | |
| Treatment or prevention of acute respiratory viral infections (SARS) | 2-3 drops of the drug are injected intranasally 4-5 times a day ( 2 - 3 sprays). The course of treatment is selected by the attending physician ( depends on the type and severity of the viral disease). As a prophylactic, it is used in the form of an ointment. Each nasal passage is smeared with ointment twice a day during the entire first and third weeks. In the second week, you need to take a break. Apply the ointment throughout the entire period of the epidemic ( winter season). | |
| Cancer tumors | ||
| Non-Hodgkin's lymphoma (a group of malignant neoplasms that affects the human lymphatic system) | It activates a special protein p53, which inhibits the further development and division of the cell and prevents its transformation into a cancer cell. When the DNA of a cell is significantly damaged, the p53 protein triggers its programmed death ( apoptosis). | In combination with chemotherapy. 5 million units subcutaneously every other day ( 3 times a week). |
| Renal cell carcinoma (kidney cancer) | The weekly dose is 10 - 30 million units of the drug. Take 3-10 million IU three times a week. | |
| multiple myeloma ( a type of blood cancer) | as maintenance therapy. 4 to 5 million units subcutaneously three times a week. The course of treatment is selected by the attending physician. | |
| Hairy cell leukemia (malignant disease of lymphocytes) | The weekly dose is 6 million units. Apply subcutaneously or intramuscularly at 2 million IU three times a week. The duration of treatment is selected in each individual case individually. | |
| Carcinoid tumors (neuroendocrine tumors that most often occur in the gastrointestinal tract) | Subcutaneously 3 - 9 million units three times a week. The treatment regimen should be changed in case of severe disease - 5 million units of interferon every day. | |
| Carcinoid tumors with metastasis | Subcutaneously, 3 to 4 million units daily. The single dose is then increased to 5, 7, and 10 million units ( at intervals of 14 days). | |
| malignant melanoma (a tumor that arises from pigment cells) | Intravenously, 20 million units per day 4 to 5 times a week. The course of treatment lasts one month. In the future, they switch to maintenance therapy - 10 million IU three times a week ( subcutaneously). The duration of maintenance therapy is 12 months. | |
| cervical dysplasia (the presence of abnormal cells in the cervix) | Selected individually. | |
| Damage to the nervous tissue of the brain and spinal cord | ||
| relapsing-remitting multiple sclerosis (characterized by periodic weakening and worsening of symptoms) | It inhibits the process of replacing nerve cells with connective tissue. Slows down the rate of destruction of the myelin sheath of nerve cells ( a special membrane of the processes of nerve cells). | Subcutaneously, 8 million units of interferon-1b. The initial dose is 2 million IU, which is gradually increased to 8 million units. It is necessary to take the drug three times a week ( in one day). The course of treatment is selected by the attending physician. |
| Secondary Progressive Sclerosis | ||
How to apply the medication?
Most often, interferon is used in the form of intramuscular or subcutaneous injections. For the prevention and treatment of acute respiratory viral infections, intranasal use of interferon is used.Interferon is used in the treatment of the following pathologies:
- viral hepatitis;
- tumor diseases;
- diseases of the central nervous system.
Viral hepatitis
Interferon is used to treat chronic hepatitis. It is often prescribed therapeutically for hepatitis B, C, and D ( delta). The drug can be used in the form of subcutaneous or intravenous injections.For the treatment of hepatitis B, a weekly dosage of 30-35 million international units of interferon is provided. It is worth noting that there are two regimens for the treatment of chronic hepatitis B. The first regimen involves the daily administration of the drug at 5 million units, and with the second regimen, interferon is administered at 10 million IU three times a week ( in one day). The duration of therapy is 4 - 6 months.
Treatment of chronic hepatitis C can be carried out together with another antiviral drug - ribavirin or use interferon as monotherapy ( single drug treatment). The weekly dosage is 9-10 million IU. Interferon is administered subcutaneously or intramuscularly at 3 million three times a week. The course of treatment is selected by the attending physician.
It is worth noting that hepatitis D can only occur together with hepatitis B. Treatment of hepatitis D involves the use of 15 million units of the drug per week. One-time subcutaneous injection of 5 million units ( three times a week). Treatment lasts from 3 to 4 months.
Tumor diseases
Quite often, interferon can be prescribed for palliative care ( maintenance therapy) various cancers.Interferon is used in the treatment of the following neoplastic diseases:
- Non-Hodgkin's lymphoma. Treatment of non-Hodgkin's lymphoma must be carried out in combination with chemotherapy. As a rule, interferon is administered subcutaneously at 5 million IU. You need to use the drug 3 times a week ( in one day).
- Hairy cell leukemia. Interferon is used one-time at 3 million units every other day ( three times a week). The drug can be administered both intramuscularly and subcutaneously. The course of treatment is selected by the attending physician.
- Malignant melanoma. The weekly dosage of interferon is 80-100 million units. It is necessary to use the drug 4-5 times a week. The duration of treatment is 30 days, after which they switch to maintenance therapy - 10 million units 3 times a week. The course of treatment when using maintenance therapy, on average, is 11-12 months.
- carcinoid tumors. Interferon is injected subcutaneously at 3-9 million units 3 times a week. If there is no effect, they switch to another treatment regimen - 5 million units of interferon daily ( 35 million IU per week).
- Carcinoid tumors with metastasis. Treatment is carried out daily in the form of subcutaneous injections of 3-4 million units of interferon. Gradually, every two weeks, a single dose is increased to 5, 7, 10 million units. The course of treatment is selected by the doctor.
- Myeloma. 5 million units of interferon subcutaneously three times a week. The duration of treatment can be selected only by the attending physician.
- Renal cell carcinoma. Interferon is taken three times a week for 3-10 million units. The course of treatment is individual.
Diseases of the central nervous system
Interferon may also be used to treat certain types of sclerosis. It is most commonly prescribed for relapsing-remitting multiple sclerosis or secondary progressive sclerosis. Interferon is prescribed 2 million units three times a week. Gradually, a single dosage is increased up to 8 million IU. Depending on the symptoms and severity of the disease, the duration of treatment can vary greatly.For the treatment, as well as the prevention of various acute respiratory viral diseases, interferon is used in the form of a spray or nasal drops. For the treatment of ARVI, a few drops of interferon should be instilled into each nasal passage ( 2 - 3 drops) 3 to 5 times a day. For the prevention of acute respiratory viral infections, interferon is recommended to take the entire winter period of time. To do this, each nasal passage is lubricated with an ointment that contains interferon 2 to 3 times a day. After the first week of treatment, it is necessary to take a seven-day break, and then resume taking interferon again.
Possible side effects
The use of interferon quite often leads to various adverse reactions. Most often, these reactions occur during the first few weeks of treatment and in the future, their intensity and frequency gradually decrease. It is worth noting that the most common adverse reaction is a flu-like condition with severe headache, fever ( 37 - 38.5ºС), general malaise and pain in the joints and muscles.Interferon can lead to the following side reactions:
- disorders of the digestive tract;
- disorders of the nervous system;
- allergic manifestations;
- disorders of the cardiovascular system;
- violations of the hematopoietic system;
- disorders of the upper and lower respiratory tract.
Digestive tract disorders
Interferon is able to irritate the mucous membrane of the organs of the gastrointestinal system, which is most often manifested by nausea.On the part of the digestive system, the following side effects can be observed:
The toxic effect of interferon on the liver tissue is also often observed. This is manifested by an increase in some indicators of biochemical blood tests. As a rule, there is an increase in the level of hepatic transaminases ( enzymes involved in the transformation of certain amino acids).
Nervous System Disorders
Interferon often increases their excitability of cells of the central nervous system ( brain and spinal cord). Also, interferon can have a negative effect on the visual and auditory analyzer.From the side of the nervous system, the following side effects can be observed:
- anxiety;
- headache;
- dizziness;
- disturbance of consciousness;
- suicidal thoughts ( seldom);
- hallucinations ( very rarely).
Interferon can also affect vision. Irritation of the optic nerve leads to visual impairment. Sometimes taking interferon can be accompanied by inflammation of the ocular mucosa ( conjunctivitis). Conjunctivitis is characterized by symptoms such as swelling of the eyelids and the mucous membrane of the eye, itching of the eyes, lacrimation, photophobia ( photophobia), as well as redness of the whites of the eyes.
Allergic manifestations
Allergic manifestations occur due to the increased individual sensitivity of the human body to a particular drug. When it enters the human body for the first time, interferon is perceived as an allergen. With the following injections of the drug, various pathological mechanisms are triggered in the body, during which a large amount of histamine is released ( hypersensitivity reaction). Histamine is directly involved in the development of tissue edema and in the appearance of skin rashes.Taking interferon can lead to the following allergic manifestations:
- erythema;
- Stevens-Johnson syndrome;
- toxic epidermal necrolysis ( Lyell's syndrome).
Erythema is a pronounced redness of the skin. Erythema occurs due to an increase in the permeability of small skin vessels, resulting in a large amount of blood flowing to the surface of the skin.
Quincke's edema is also a fairly common form of drug allergy, in which fatty tissue of the skin is affected ( subcutaneous fat). Most often, swelling can occur on the face ( lips, eyelids, cheeks, as well as the oral cavity). Sometimes limbs and genitals can swell. As a rule, 3-4 hours after the onset, the edema disappears without a trace. A rare complication of Quincke's edema is blockage of the upper respiratory tract. This happens due to the fact that the edema spreads from the oral cavity to the mucous membrane of the larynx, resulting in suffocation. This condition is extremely dangerous and can lead to coma.
Stevens-Johnson syndrome is an extremely severe form of erythema. This syndrome is characterized by the appearance of large blisters on the mucous membranes ( eyes, pharynx, oral cavity) and on the skin. At the first stage of the disease, as a rule, severe pain occurs in large joints. Body temperature, in turn, rises up to 39ºС. After a couple of hours, the general condition deteriorates sharply, and blisters appear on the mucous membrane of the tongue, cheeks, as well as on the lips, larynx and skin. After opening, very painful and bleeding areas with erosions form in their place.
Toxic epidermal necrolysis is a very life-threatening condition. Within 2-4 hours after the introduction of the drug into the body, the general condition of the body deteriorates sharply. Body temperature rises to 39 - 40ºС. A rash appears on the skin in the form of small dots, which resembles a rash with scarlet fever. In the future, instead of these rashes, rather large blisters with transparent contents are formed, which quickly open. In place of the blisters, erosive areas of the skin open, which can merge and form large erosions. It is worth noting that with toxic epidermal necrolysis, internal organs such as the kidneys, liver, heart, and intestines can be affected. If timely medical care is not provided, then people with this pathology very often die.
Disorders of the cardiovascular system
In rare cases, interferon can adversely affect the cardiovascular system. Sometimes symptoms such as high blood pressure ( hypertension), chest pain ( especially behind the sternum), as well as an increase in the number of heartbeats ( tachycardia). This symptomatology occurs due to increased influence of the sympathetic nervous system on the heart.Hematopoietic system disorders
Sometimes interferon is capable of negatively affecting blood cells, and sometimes also on hematopoietic organs.Taking interferon can lead to the following disorders of the hematopoietic system:
- leukopenia.
Thrombocytopenia manifested by a decrease in the total number of platelets ( platelets). Platelets are needed for normal blood clotting ( coagulation). Most often, thrombocytopenia is manifested by bleeding gums. In some cases, thrombocytopenia can lead to severe bleeding in various internal organs ( especially dangerous bleeding in the brain).
Leukopenia is a decrease in the number of white blood cells ( leukocytes). These cells are able to protect the human body from various pathogens. With leukopenia, a person becomes extremely vulnerable to bacterial infections. This pathological condition often leads to an increase in the size of the spleen and tonsils ( hypertrophy).
Upper and lower respiratory disorders
In some cases, the administration of interferon can lead to symptoms such as cough and shortness of breath. Cough appears reflexively due to irritation of the nerve endings of the vagus and glossopharyngeal nerve located in the mucous membrane of the pharynx, larynx, trachea and bronchi. Shortness of breath can most often occur against the background of anemia, with fever, as well as with various pathologies of the respiratory tract and cardiovascular system.Also, interferon can lead to the following respiratory diseases (rarely):
Sinusitis is an inflammation of the mucous membrane of the paranasal sinuses. Sinusitis can occur against the background of a runny nose or SARS ( flu). This pathology is characterized by symptoms such as heaviness in the paranasal sinus, fever, nasal discharge ( thick), pain in the sinus with sharp turns of the head. Most often, the maxillary sinuses are involved in the inflammatory process ( maxillary) and frontal sinuses.
Pneumonia is an inflammation of the tissues of the lungs, in which the alveoli are most often affected ( structural and functional elements of the lung, in which the process of gas exchange occurs). Depending on the volume of damage to the lung tissue, focal ( inflammation of multiple alveoli), segmental ( inflammatory process within one segment of the lung), equity ( damage to one lobe of the lung) and lobar pneumonia ( involvement of both lungs). Pneumonia is characterized by symptoms such as fever, shortness of breath ( occurs when inflammatory fluid accumulates in the alveoli), chest pain, respiratory failure. With croupous pneumonia, severe intoxication is also observed, which is manifested by headache, dizziness, general malaise and confusion. Most often, uncomplicated pneumonia lasts about a month.
Approximate cost of medication
The cost of the drug varies greatly depending on the type of interferon. Below is a table that shows the average cost of this medication in different cities of Russia.| City | The average cost of interferon | |||
| Lyophilisate for solution preparation for intranasal administration ( interferon alfa ) | Solution for local use and inhalation ( interferon alfa) | Solution for subcutaneous or intramuscular injections ( interferon alfa-2b) | Lyophilisate for the preparation of an aqueous solution for intramuscular injection ( interferon beta-1a) | |
| Moscow | 71 ruble | 122 rubles | 1124 rubles | 9905 rubles |
| Kazan | 70 rubles | 120 rubles | 1119 rubles | 9887 rubles |
| Krasnoyarsk | 69 rubles | 119 rubles | 1114 rubles | 9902 rubles |
| Samara | 69 rubles | 119 rubles | 1115 rubles | 9884 rubles |
| Tyumen | 71 ruble | 123 rubles | 1126 rubles | 9917 rubles |
| Chelyabinsk | 74 rubles | 127 rubles | 1152 rubles | 9923 rubles |
It should be noted that for the treatment of relapsing-remitting multiple sclerosis, as well as secondary progressive sclerosis, recombinant interferon beta-1b is used ( created artificially with the help of special biotechnologies). This type of interferon is obtained on the basis of specific fermentation of bacteria ( coli is used, which contains the human gene responsible for the synthesis of interferonbetaser17). The technology for obtaining interferon beta-1b is quite expensive, and therefore the price for it differs significantly from other types of interferon. Recombinant interferon beta-1b can be found in pharmacies at a price of 6,200 rubles to 35,000 rubles ( depends on the number of ampoules in the package).
Russian name
Interferon beta-1aLatin name of the substance Interferon beta-1a
Interferonum beta-1a ( genus. Interferoni beta-1a)Pharmacological group of the substance Interferon beta-1a
Nosological classification (ICD-10)
Characteristics of the substance Interferon beta-1a
Recombinant human interferon beta-1a produced by mammalian cells (Chinese hamster ovary cell culture). Specific antiviral activity - more than 200 million IU / mg (1 ml of solution contains 30 μg of interferon beta-1a, which has 6 million IU of antiviral activity). It exists in a glycosylated form, contains 166 amino acid residues and a complex carbohydrate fragment associated with a nitrogen atom. The amino acid sequence is identical to natural (natural) human interferon beta.
Pharmacology
pharmachologic effect- antiviral, immunomodulatory, antiproliferative.It binds to specific receptors on the cell surface of the human body and triggers a complex cascade of intercellular interactions, leading to interferon-mediated expression of numerous gene products and markers, incl. class I histocompatibility complex, protein M x, 2",5"-oligoadenylate synthetase, beta 2 -microglobulin and neopterin.
Biological activity markers (neopterin, beta 2 -microglobulin, etc.) are determined in healthy donors and patients after parenteral administration of doses of 15-75 mcg. The concentration of these markers increases within 12 hours after administration and remains elevated for 4-7 days. Peak biological activity is typically observed 48 hours after administration. The exact relationship between plasma levels of interferon beta-1a and the concentration of marker proteins, the synthesis of which it induces, is still unknown.
Stimulates the activity of suppressor cells, enhances the production of interleukin-10 and transforming growth factor beta, which have anti-inflammatory and immunosuppressive effects in multiple sclerosis. Interferon beta-1a significantly reduces the frequency of exacerbations and the rate of progression of irreversible neurological disorders in relapsing-remitting multiple sclerosis (the increase in the number and area of focal brain lesions slows down according to MRI). Treatment may be accompanied by the appearance of antibodies to interferon beta-1a. They decrease his activity. in vitro(neutralizing antibodies) and biological effects (clinical efficacy) in vivo. With a duration of treatment of 2 years, antibodies are found in 8% of patients. According to other data, after 12 months of treatment, antibodies appear in the serum in 15% of patients.
No mutagenic activity was found. Data on the study of carcinogenicity in animals and humans are not available. In a reproductive study in rhesus monkeys treated with interferon beta-1a at doses 100 times the MRHD, ovulation cessation and a decrease in serum progesterone levels were observed in some animals (the effects were reversible). In monkeys treated with doses 2 times the recommended weekly dose, these changes were not detected.
The introduction of doses 100 times higher than the MRDH to pregnant monkeys was not accompanied by manifestations of teratogenic effects and a negative effect on fetal development. However, doses 3-5 times the weekly recommended dose caused miscarriage (no miscarriage occurred at 2 times the weekly dose). Information on the effect on reproductive function in humans is not available.
Pharmacokinetic studies of interferon beta-1a in patients with multiple sclerosis have not been conducted.
In healthy volunteers, the pharmacokinetic parameters depended on the route of administration: when administered intramuscularly at a dose of 60 μg, C max was 45 IU / ml and was reached after 3-15 hours, T 1/2 - 10 hours; with s / c administration C max - 30 IU / ml, the time to achieve it - 3-18 hours, T 1/2 - 8.6 hours. Bioavailability with i / m administration was 40%, with s / c - 3 times below. There are no data indicating a possible penetration into breast milk.
Application of the substance Interferon beta-1a
Recurrent multiple sclerosis (if there are at least 2 relapses of neurological dysfunction within 3 years and there is no evidence of continuous progression of the disease between relapses).
Contraindications
Hypersensitivity (including to natural or recombinant interferon beta, human serum albumin), severe depression and / or the presence of suicidal thoughts, epilepsy (with insufficient effectiveness of antiepileptic drugs), pregnancy, breast-feeding.
Application restrictions
Age up to 16 years (safety and effectiveness of use have not been determined).
Use during pregnancy and lactation
Side effects of the substance Interferon beta-1a
According to a placebo-controlled study with a / m administration at a dose of 30 mcg 1 time per week, if observed in 2% of cases or more (% of occurrence in the placebo group is indicated in brackets).
Flu-like syndrome - 61% (40%), usually at the beginning of treatment, incl. headache 67% (57%), myalgia 34% (15%), fever 23% (13%), chills 21% (7%), asthenia 21% (13%).
From the nervous system and sensory organs: insomnia 19% (16%), dizziness 15% (13%), malaise 4% (3%), syncope (usually once at the start of treatment) 4% (2%), suicidal tendencies 4% (1%), seizures 3 %(0%), speech disorder 3%(0%), hearing loss 3%(0%), ataxia 2%(0%).
From the side of the cardiovascular system and blood (hematopoiesis, hemostasis): anemia 8%(3%), eosinophilia 5%(4%), vasodilation 4%(1%), decrease in hematocrit 3%(1%), arrhythmia.
From the respiratory system: development of upper respiratory tract infections 31% (28%), sinusitis 18% (17%), shortness of breath 6% (5%), otitis media 6% (3%).
From the digestive tract: nausea 33%(23%), diarrhea 16%(10%), dyspepsia 11%(7%), anorexia 7%(6%).
Allergic reactions: urticaria 5% (2%), hypersensitivity reactions 3% (0%).
Others: pain syndrome 24% (20%), incl. arthralgia 9%(5%), abdominal pain 9%(6%), chest pain 6%(4%); development of infections 11% (6%) incl. Herpes zoster 3%(2%), Herpes simplex 2%(1%); muscle spasm 7% (6%); local reactions in the injection area 4% (1%), incl. inflammation 3%(0%), ecchymosis 2%(1%); alopecia 4% (1%); vaginitis 4%(2%), increased AST level 3%(1%), ovarian cyst 3%(0%), nevus 3%(0%).
Interaction
Compatible with corticosteroids and ACTH. Simultaneous use with myelosuppressive drugs is not recommended, incl. cytostatics (possible additive effect). Combine with caution with drugs whose clearance is largely dependent on the cytochrome P450 system (antiepileptic drugs, some antidepressants, etc.).
Routes of administration
Interferon beta-1a substance precautions
With caution appoint patients with mild depression, convulsive syndrome, severe renal and hepatic insufficiency, severe myelosuppression. It is necessary to carefully monitor the condition of patients with heart disease, incl. angina pectoris, congestive heart failure, arrhythmia. During treatment, it is recommended to control the cellular composition of the blood, incl. platelet count and leukocyte formula, as well as conduct a biochemical blood test (including the determination of liver enzymes). If there are signs of bone marrow suppression, more careful monitoring of blood counts is necessary.
INSTRUCTIONS for medical use GENFAXON
interferon beta-1a
Registration number: LSR-003037/10
Trade name: Genfaxon®/Genfaxon®
International non-proprietary or grouping name: interferon beta-1a
Dosage form: solution for subcutaneous injection Composition: 1 syringe in 0.5 ml of the solution contains 22 μg (6 million IU) or 44 μg (12 million IU) of interferon beta-1a and excipients: mannitol, human albumin, sodium acetate, acetic acid, water for injection. Description: clear, colorless to slightly yellowish solution, free from foreign particles Pharmacotherapeutic group: cytokine ATC code: Pharmacological properties Genfaxon® (recombinant human interferon beta-1a) is a natural amino acid sequence of human interferon beta, obtained by genetic engineering using cell culture of Chinese hamster ovary. Interferon beta-1a has immunomodulatory, antiviral and antiproliferative properties. The mechanism of action of interferon beta-1a in patients with multiple sclerosis is not fully understood. It has been shown that the drug helps to limit the damage to the central nervous system underlying the disease, reduces the frequency and severity of exacerbations in patients with relapsing-remitting multiple sclerosis. The action of Genfaxon® has not been studied in primary progressive multiple sclerosis.
Pharmacokinetics
When administered subcutaneously, the concentration of interferon beta-1a in the blood serum is determined within 12-24 hours after the injection. After a single injection of a dose of 60 mcg, the maximum concentration determined by immunological methods is 6-10 IU / ml 3 hours after administration. With 4 subcutaneous injections of the same dose every 48 hours, a moderate accumulation of the drug occurs. After a single injection, intracellular and serum activity of 2-5A synthetase and serum concentrations of beta2-microglobulin and neopterin (biological response markers) increase within 24 hours and then decrease within 2 days. Interferon beta-1a is metabolized and excreted by the liver and kidneys.
Indications for use
Relapsing-remitting multiple sclerosis.
Efficacy in patients with secondary progressive multiple sclerosis in the absence of active disease has not been demonstrated.
Contraindications
- Hypersensitivity to natural or recombinant interferon beta-1a, human serum albumin or other components of the drug.
- Pregnancy and lactation (see "Use during pregnancy and lactation")
- Severe depressive disorders and/or suicidal thoughts.
- Epilepsy in the absence of the effect of the use of appropriate therapy.
- Age up to 12 years (the effect of the drug on this age group has not been sufficiently studied).
Carefully
History of depression, history of seizures, angina pectoris, heart failure, cardiac arrhythmias, severe renal or hepatic failure, severe myelosuppression; thyroid disease.
Use during pregnancy and lactation
Pregnancy
Genfaxon® is not prescribed during pregnancy and lactation. Women of childbearing age should use effective methods of contraception. Considering the potential danger to the fetus, patients planning a pregnancy or becoming pregnant 2 during treatment should definitely inform their doctor about this in order to decide whether to continue (cancel) therapy.
Lactation
There are no data on the excretion of Genfaxon in breast milk. Given the likelihood of serious adverse reactions in infants, a choice should be made between discontinuing Genfaxon® and stopping breastfeeding.
Dosage and administration
Subcutaneously.
The drug should be used at the same time (preferably in the evening), on certain days of the week, with an interval of at least 48 hours.
During the first 2 weeks of starting therapy, Genfaxon® should be administered at a dose of 8.8 mcg (0.2 ml from a syringe containing 22 mcg or 0.1 ml from a syringe containing 44 mcg), during the 3rd and 4th - week - at a dose of 22 mcg (0.5 ml from a syringe containing 22 mcg or 0.25 ml from a syringe containing 44 mcg). When prescribing the drug Genfaxon® at a dosage of 44 mcg, starting from the 5th week, a dose of 0.5 ml 44 mcg is administered.
Adults and adolescents over 16 years of age: The maintenance dose is usually 44 micrograms 3 times a week. At a dose of 22 mcg - 3 times a week, Genfaxon® is prescribed to those patients who, in the opinion of the attending physician, do not tolerate a high dose well enough.
Adolescents 12 to 16 years of age: 22 micrograms 3 times a week.
For convenience, the corresponding divisions are applied to the syringe. The drug remaining in the syringe is not subject to further use.
The decision on the duration of treatment should be made individually by the attending physician.
If you miss a dose, continue with the next injection on the schedule. Do not double dose.
Side effect
Flu-like symptoms
Approximately 40% of patients during the first 6 months during treatment with Genfaxon® may experience a typical interferon flu-like syndrome (headache, fever, chills, muscle and joint pain, nausea). These manifestations are usually mild, occur more often at the beginning of treatment and decrease with continued treatment. The patient should be informed that if any of the listed symptoms is severe or persistent, he should inform the doctor. Your doctor may prescribe a pain reliever or temporarily change your dose.
Reactions at the injection site
Injection site reactions (redness, swelling, blanching of the skin, soreness) are also possible, usually mild and reversible. In isolated cases, necrosis is observed at the injection site, which usually resolves on its own. Rarely, infection of the injection site is possible. The skin in this area can become elastic, edematous, soreness is noted.
Reactions from the digestive, nervous, cardiovascular and other body systems
More rare side effects associated with the use of interferon beta-1a include diarrhea, loss of appetite, vomiting, sleep disturbance, dizziness, nervousness, rash, vasodilation symptoms and palpitations, menstrual irregularities / changes.
Hypersensitivity and allergic reactions
In exceptional cases, serious allergic reactions may occur. If, immediately after the injection, the patient feels shortness of breath, which may be accompanied by hives, a feeling of weakness or discomfort, he should immediately seek medical help.
Deviation of laboratory parameters
Possible deviation from the norm of laboratory parameters, manifested by leukopenia, lymphopenia, thrombocytopenia, increased activity of alanine aminotransferase (ALT), γ-glutamyl transferase and alkaline phosphatase. These changes are usually minor and reversible. There may be symptoms of liver disorders, such as loss of appetite, nausea, vomiting, jaundice.
Reactions from the endocrine system
Interferons can affect the function of the thyroid gland both upward and downward. These changes may not be noticeable to the patient, but the doctor may prescribe an additional examination.
Depression
Patients with multiple sclerosis may develop depression. It is necessary to inform the doctor about any of the above side effects of the drug, including those that are not listed in this leaflet. In case of severe adverse reactions or their persistence for a long time, at the discretion of the physician, a temporary reduction in the dose of the drug or interruption of treatment is allowed. Do not stop treatment or change the dose without the advice of your doctor.
Overdose
No case of overdose has yet been described. In case of an overdose, the patient should be hospitalized for observation and, if necessary, symptomatic therapy.
Interaction with other drugs
Specially planned clinical studies to study the interaction of the drug Genfaxon® with other drugs have not been conducted.
However, it is known that in humans and animals, interferons reduce the activity of cytochrome P450-dependent liver enzymes. Therefore, caution should be exercised when prescribing Genfaxon® simultaneously with drugs that have a narrow therapeutic index, the clearance of which is largely dependent on cytochrome P450, for example, antiepileptic drugs and some antidepressants.
A systematic study of the interaction of the drug Genfaxon® with glucocorticosteroids or adrenocorticotropic hormone (ACTH) has not been conducted. Data from clinical studies indicate the possibility of patients with multiple sclerosis receiving Genfaxon® and glucocorticosteroids or ACTH during exacerbations of the disease.
special instructions
There are isolated reports of tissue necrosis at the injection site. To minimize the risk of developing necrosis, strict adherence to the rules of asepsis when performing an injection and a constant change of injection sites is necessary. If there is a violation of the integrity of the skin with the outflow of fluid at the injection site, you should consult a doctor before continuing to administer the drug. With multiple skin lesions, the drug should be discontinued until they heal. With a single lesion, it is possible to continue therapy with Genfaxon®, provided that the lesion is moderately severe.
In clinical trials, an increase in the activity of "liver" transaminases, especially ALT, has been demonstrated. In the absence of symptoms, plasma ALT activity should be determined before starting therapy with Genfaxon® and repeated after 1, 3 and 6 months and periodically with continued treatment. It is necessary to reduce the dose of the drug if the ALT activity exceeds 5 times the upper limit of the norm, and gradually increase the dose after its normalization. Care must be taken when prescribing interferon beta-1a to patients with a history of severe liver failure, with signs of liver disease, with signs of alcohol abuse, ALT activity 2.5 times the upper limit of normal. Therapy should be discontinued if jaundice or other signs of impaired function appear. liver.
Genfaxon®, like other beta interferons, has the potential to cause serious liver damage, up to acute liver failure. The mechanism of these conditions is unknown, and specific risk factors have not been identified.
In addition to laboratory tests, which are always carried out in patients with multiple sclerosis, during the period of treatment with interferon beta-1a, it is recommended to conduct a complete blood count with the calculation of the leukocyte count and platelet count every 1, 3 and 6 months, as well as conduct a biochemical blood test, in particular , liver function tests.
Patients receiving Genfaxon® sometimes develop or worsen thyroid dysfunction. It is recommended to conduct a study of thyroid function before starting treatment and, if abnormalities are detected, every 6-12 months.
In patients receiving beta interferons, the formation of neutralizing antibodies is possible. Their clinical significance has not been established. If the patient does not respond well to therapy with Genfaxon® and antibodies are detected in him, the doctor should evaluate the advisability of continuing therapy.
Subcutaneous self-administration
Because Genfaxon® comes as a pre-filled hypodermic syringe, you can safely use it at home, either on your own or with the help of family or friends. If possible, the first injection should be given under the supervision of a qualified healthcare professional.
Before using Genfaxon®, please read the following instructions carefully:
Wash your hands thoroughly with soap and water.
Choose a site for injection. Your doctor will advise you on possible injection sites (comfortable sites are located in the upper thigh or lower abdomen). It is recommended to alternate injection sites, avoiding frequent injections into the same site.
Do not inject the drug into places where you feel swelling, hard nodules or pain; Tell your doctor or nurse if you have any such areas.
Remove the Genfaxon® syringe from the package. Wipe the skin at the injection site with an alcohol pad. Let the skin dry. If some of the alcohol remains on the skin, you may feel a burning sensation.
Gently squeeze the skin around the selected area so as to lift it slightly (in order to form a skin fold). With your wrist pressed against the skin near the site, insert the needle at a right angle into the skin with a quick and firm motion. Hold the syringe like a pencil or dart.
Inject the drug with slow and constant pressure at the dose (number of ml) prescribed by the doctor.
The drug remaining in the syringe is not subject to further use.
Press down on the injection site with a swab. Remove the needle from the skin.
Gently massage the injection site with a dry cotton ball or gauze.
Throw away the used syringe in the waste area.
Influence on the ability to drive a car and technical means
During the period of treatment, you should refrain from driving or engaging in activities that require the speed of psychomotor reactions.
Release form
Solution for subcutaneous injection 22 mcg (6 million IU) or 44 mcg (12 million IU).
0.5 ml (22 µg) or 0.5 ml (44 µg) each in a colorless, transparent type I glass syringe with a stainless steel needle, closed with a butyl cap, placed in a paper-lined plastic container.
3 or 12 containers in a cardboard box with instructions for use.
Storage conditions
At a temperature of 2 to 8 ºС in a place protected from light. Do not freeze. Keep out of the reach of children.
Best before date
2 years. Do not use after the expiry date stated on the packaging.
Terms of dispensing from pharmacies
On prescription.
Manufacturer:
Laboratory Tutor S.A.S.I.F.I.A., produced by MR Pharma S.A., Argentina
Laboratory Tuteur S.A.C.I.F.I.A., manufactured by MR Pharma S.A., Argentina.
Address: Av. Juan de Garay, 842/48, Buenos Aires, Argentina
Av. Juan de Garay, 842/48, Buenos Aires,Argentina
Consumer claims are accepted at the address of the representative office of the company "Genfa Medica S.A." (Switzerland).
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