Release form, composition and packing Betaferon
Valium for a solution for subcutaneous injection in the form of freeze-dried mass of a white enclosed solvent transparent, almost colorless; prepared solution of slightly opalescent to opalescent, colorless or pale yellow. 1 vial. 1 ml of p-pa recombinant interferon beta-1b 9.6 mln.ME (300 mcg) 8 mln.ME (250 mcg). Excipients: human albumin, mannitol. Solvent: sterile rr sodium chloride 0.54% - 1.2 ml.
Clinico-pharmacological group: Interferon. Drug used in multiple sclerosis.
Pharmacological action
Interferon beta-1b, used in multiple sclerosis, has antiviral and immunoregulatory activity. Mechanisms of action of interferon beta-1b in multiple sclerosis is not definitely established. However, it is known that the biological effect of interferon beta-1b is mediated by its interaction with specific receptors that are found on the surface of human cells.
Binding of interferon beta-1b to these receptors induces the expression of a number of substances which are considered as mediators of biological effects of interferon beta-1b. The content of some of these substances were determined in serum and fractions of blood cells of patients treated with interferon beta-1b. Interferon beta-1b decreases the binding capacity and expression of receptors of gamma interferon enhances their dissolution. The drug increases the suppressive activity of peripheral blood mononuclear cells.
As for remitting, and at the secondary-progressive multiple sclerosis treatment Betaferon reduces the frequency (30%) and severity of clinical exacerbations of the disease, the number of hospitalizations and the need for steroid treatment, and lengthens the duration of remission.
In patients with secondary-progressive multiple sclerosis use of Betaseron will delay further progression of disease and disability (including severe when patients are forced to always use a wheelchair) for up to 12 months.
This effect was observed in patients with both acute exacerbations of the disease, with or without exacerbations, as well as with any index of disability (in the study included patients with an estimate from 3.0 to 6.5 points on the expanded disability scale, EDSS).
The results of magnetic resonance imaging (MRI) brain of patients with remitting and secondary-progressive multiple sclerosis patients receiving Betaferon showed a significant positive effect of the drug on the severity of the pathological process, as well as a significant decrease in the formation of new active lesions.
Pharmacokinetics
After subcutaneous injection of Betaseron at a dose of 0.25 mg concentration of interferon beta-1b in serum are low or not determined. In this regard, information on the pharmacokinetics of the drug in patients with multiple sclerosis treated with Betaferon ® at the recommended dose, no.
After subcutaneous injection of 0.5 mg dose to healthy volunteers Cmax is about 40 IU / ml achieved after 8.1 h after injection. The absolute bioavailability of Betaseron when s / c infusion was approximately 50%. With / in the introduction of interferon beta-1b serum clearance, and T1 / 2 are an average of 30 ml / min / kg and 5 h, respectively.
The introduction of Betaseron every other day does not lead to increased concentrations of interferon beta-1b in serum and its pharmacokinetic processes during the course of therapy, apparently, do not change.
When s / c infusion at a dose of Betaseron 0.25 mg a day in healthy volunteers, levels of biological response markers (neopterin, beta2-microglobulin and the immunosuppressive cytokine IL-10) significantly increased compared to benchmarks 6-12 hours after the first dose of the drug.
They reached a peak after 40-124 h and remained elevated throughout the 7-day (168 h) study period.
Statement
clinically isolated syndrome (CIS) (the only clinical demyelinating event suggestive of multiple sclerosis, subject to exclusion of alternative diagnoses) with sufficient severity of the inflammatory process for appointment / to SCS - for slowing the transition to a clinically reliable multiple sclerosis (KDRS) in patients with high risk of KDRS.
Universally accepted definition of high risk do not. According to a study by a group at high risk for KDRS include patients with monoochagovym CIS (clinical manifestations of a lesion in the CNS) and ≥ T2 foci on MRI and / or accumulated contrast agent centers.
Patients with multifocal CIS (clinical manifestations of> 1 lesion in the CNS) are at high risk of developing KDRS regardless of the number of lesions on MRI;
remitting multiple sclerosis - to reduce the frequency and severity of exacerbations of multiple sclerosis in ambulatory patients (ie patients could walk unaided) with a history of at least two exacerbations of the disease over the past 2 years and followed by complete or incomplete recovery of neurological symptoms;
secondary-progressive multiple sclerosis with active disease course characterized by relapses or marked deterioration of neurological functions during the last 2 years - to reduce the frequency and severity of exacerbations, as well as to slow the progression of the disease.
Dosing regimen
Betaseron treatment should be started under the supervision of a physician with experience treating this disease. At present, the question remains about the duration of treatment Betaferon. In clinical studies, the duration of therapy in patients with remitting and secondary-progressive multiple sclerosis as high as 5 and 3 years respectively.
The duration of therapy is determined by your doctor. Recommended dose of Betaseron 0.25 mg (8 mln.ME), which is contained in 1 ml of prepared solution, administered sc every other day. The patient should be informed that in case of missing injections, the drug should be introduced immediately, as soon as he remembers. Following an injection of doing in 48 hours
Rules for preparation of the solution:
A package containing vials and syringes with solvent. To dissolve the lyophilized powder for injection using a syringe attached finished with a solvent and a needle.
A package containing vials, syringes with solvent, the adapter with a needle to the vial and alcohol wipes. To dissolve the lyophilized powder for injection using a syringe made ready with a solvent and an adapter with a needle to the vial. 1.2 ml of solvent (sodium chloride 0.54%) injected into the vial with Betaseron.
The powder should dissolve completely without shaking. Before use, inspect a ready solution. In the presence of particles or changes in color of the solution can not be applied. 1 ml of final solution contains 0.25 mg (8 mln.ME) interferon beta-1b. The drug should be administered sc immediately after the preparation of the solution. If an injection is delayed, the solution should be refrigerated and used within 3 h. The solution must not be frozen.
Side effect
Below are the side effects observed with a frequency of 2% and higher than in the placebo group, patients who in the course of controlled clinical trials received Betaferon dose 0.25 mg / m 2 or 0.16 mg / m 2 every other day for up to 3 years.
From the body as a whole: the reaction at the injection site, fatigue, complex flu-like symptoms, headache, fever, chills, abdominal pain, chest pain, malaise, necrosis at the injection site, pain of various locations.
With the cardiovascular system: peripheral edema, vasodilatation, hypertension, peripheral vascular disease, palpitations, tachycardia.
From the digestive system: nausea, constipation, diarrhea, increased AST and ALT levels 5 times the original level, dyspepsia.
From the hematopoietic system: lymphocytes <1500/mkl, neutrophils <1500/mkl, leukocytes <3000/mkl, lymphadenopathy.
From a metabolism: an increase in body weight.
From the musculoskeletal system: myasthenia, myalgia, arthralgia, leg cramps.
The nervous system: hypertonicity, dizziness, insomnia, loss of coordination, anxiety, nervousness.
With the respiratory system: dyspnea.
Dermatological reactions: rash, skin diseases, increased sweating, alopecia.
With the urinary system: the imperative need to urinate, frequent urination.
From the sexual system: metrorrhagia (acyclic bleeding), menorrhagia, dysmenorrhea, in men - impotence, prostate diseases.
The following side effects are based on postmarketing monitoring the use of Betaferon, grouped by organs and systems are presented with the following frequency of occurrence: Very common (≥ 10%), relatively frequent (<10% - ≥ 1%), infrequent (<1% - ≥ 0.1%), rarely (<0.1% - ≥ 0.01%), very rare (<0.01%). General reaction: very often - flu-like symptoms (fever, chills, myalgia, headache, excessive sweating), the frequency of these symptoms decreased over time, rarely - malaise, chest pain.
From the hematopoietic system: Infrequent - leukopenia, anemia, thrombocytopenia, rarely - lymphadenopathy.
Cardio-vascular system: Infrequent - hypertension, rarely - cardiomyopathy, tachycardia, palpitations.
On the part of the endocrine system: rarely - dysfunction of the thyroid gland, hyperthyroidism, hypothyroidism.
CNS: Infrequent - muscular hypertonicity, depression, rarely - seizures, confusion, agitation, emotional lability, suicidal attempts.
Part of the respiratory system: rarely - dyspnea, bronchospasm.
From the digestive system: Infrequent: - nausea, vomiting, increased activity of ACT, ALT, rarely - increased levels of bilirubin and GGT activity, pancreatitis, anorexia.
From the musculoskeletal system: Infrequent - myalgia.
From the reproductive system: rarely - menstrual irregularities.
Allergic reactions: seldom - anaphylactic reactions.
Local reactions: very common - congestion, local swelling, inflammation, pain, rarely - skin necrosis (with time with continued treatment the frequency of reactions at the site of injection usually decreases).
Valium for a solution for subcutaneous injection in the form of freeze-dried mass of a white enclosed solvent transparent, almost colorless; prepared solution of slightly opalescent to opalescent, colorless or pale yellow. 1 vial. 1 ml of p-pa recombinant interferon beta-1b 9.6 mln.ME (300 mcg) 8 mln.ME (250 mcg). Excipients: human albumin, mannitol. Solvent: sterile rr sodium chloride 0.54% - 1.2 ml.
Clinico-pharmacological group: Interferon. Drug used in multiple sclerosis.
Pharmacological action
Interferon beta-1b, used in multiple sclerosis, has antiviral and immunoregulatory activity. Mechanisms of action of interferon beta-1b in multiple sclerosis is not definitely established. However, it is known that the biological effect of interferon beta-1b is mediated by its interaction with specific receptors that are found on the surface of human cells.
Binding of interferon beta-1b to these receptors induces the expression of a number of substances which are considered as mediators of biological effects of interferon beta-1b. The content of some of these substances were determined in serum and fractions of blood cells of patients treated with interferon beta-1b. Interferon beta-1b decreases the binding capacity and expression of receptors of gamma interferon enhances their dissolution. The drug increases the suppressive activity of peripheral blood mononuclear cells.
As for remitting, and at the secondary-progressive multiple sclerosis treatment Betaferon reduces the frequency (30%) and severity of clinical exacerbations of the disease, the number of hospitalizations and the need for steroid treatment, and lengthens the duration of remission.
In patients with secondary-progressive multiple sclerosis use of Betaseron will delay further progression of disease and disability (including severe when patients are forced to always use a wheelchair) for up to 12 months.
This effect was observed in patients with both acute exacerbations of the disease, with or without exacerbations, as well as with any index of disability (in the study included patients with an estimate from 3.0 to 6.5 points on the expanded disability scale, EDSS).
The results of magnetic resonance imaging (MRI) brain of patients with remitting and secondary-progressive multiple sclerosis patients receiving Betaferon showed a significant positive effect of the drug on the severity of the pathological process, as well as a significant decrease in the formation of new active lesions.
Pharmacokinetics
After subcutaneous injection of Betaseron at a dose of 0.25 mg concentration of interferon beta-1b in serum are low or not determined. In this regard, information on the pharmacokinetics of the drug in patients with multiple sclerosis treated with Betaferon ® at the recommended dose, no.
After subcutaneous injection of 0.5 mg dose to healthy volunteers Cmax is about 40 IU / ml achieved after 8.1 h after injection. The absolute bioavailability of Betaseron when s / c infusion was approximately 50%. With / in the introduction of interferon beta-1b serum clearance, and T1 / 2 are an average of 30 ml / min / kg and 5 h, respectively.
The introduction of Betaseron every other day does not lead to increased concentrations of interferon beta-1b in serum and its pharmacokinetic processes during the course of therapy, apparently, do not change.
When s / c infusion at a dose of Betaseron 0.25 mg a day in healthy volunteers, levels of biological response markers (neopterin, beta2-microglobulin and the immunosuppressive cytokine IL-10) significantly increased compared to benchmarks 6-12 hours after the first dose of the drug.
They reached a peak after 40-124 h and remained elevated throughout the 7-day (168 h) study period.
Statement
clinically isolated syndrome (CIS) (the only clinical demyelinating event suggestive of multiple sclerosis, subject to exclusion of alternative diagnoses) with sufficient severity of the inflammatory process for appointment / to SCS - for slowing the transition to a clinically reliable multiple sclerosis (KDRS) in patients with high risk of KDRS.
Universally accepted definition of high risk do not. According to a study by a group at high risk for KDRS include patients with monoochagovym CIS (clinical manifestations of a lesion in the CNS) and ≥ T2 foci on MRI and / or accumulated contrast agent centers.
Patients with multifocal CIS (clinical manifestations of> 1 lesion in the CNS) are at high risk of developing KDRS regardless of the number of lesions on MRI;
remitting multiple sclerosis - to reduce the frequency and severity of exacerbations of multiple sclerosis in ambulatory patients (ie patients could walk unaided) with a history of at least two exacerbations of the disease over the past 2 years and followed by complete or incomplete recovery of neurological symptoms;
secondary-progressive multiple sclerosis with active disease course characterized by relapses or marked deterioration of neurological functions during the last 2 years - to reduce the frequency and severity of exacerbations, as well as to slow the progression of the disease.
Dosing regimen
Betaseron treatment should be started under the supervision of a physician with experience treating this disease. At present, the question remains about the duration of treatment Betaferon. In clinical studies, the duration of therapy in patients with remitting and secondary-progressive multiple sclerosis as high as 5 and 3 years respectively.
The duration of therapy is determined by your doctor. Recommended dose of Betaseron 0.25 mg (8 mln.ME), which is contained in 1 ml of prepared solution, administered sc every other day. The patient should be informed that in case of missing injections, the drug should be introduced immediately, as soon as he remembers. Following an injection of doing in 48 hours
Rules for preparation of the solution:
A package containing vials and syringes with solvent. To dissolve the lyophilized powder for injection using a syringe attached finished with a solvent and a needle.
A package containing vials, syringes with solvent, the adapter with a needle to the vial and alcohol wipes. To dissolve the lyophilized powder for injection using a syringe made ready with a solvent and an adapter with a needle to the vial. 1.2 ml of solvent (sodium chloride 0.54%) injected into the vial with Betaseron.
The powder should dissolve completely without shaking. Before use, inspect a ready solution. In the presence of particles or changes in color of the solution can not be applied. 1 ml of final solution contains 0.25 mg (8 mln.ME) interferon beta-1b. The drug should be administered sc immediately after the preparation of the solution. If an injection is delayed, the solution should be refrigerated and used within 3 h. The solution must not be frozen.
Side effect
Below are the side effects observed with a frequency of 2% and higher than in the placebo group, patients who in the course of controlled clinical trials received Betaferon dose 0.25 mg / m 2 or 0.16 mg / m 2 every other day for up to 3 years.
From the body as a whole: the reaction at the injection site, fatigue, complex flu-like symptoms, headache, fever, chills, abdominal pain, chest pain, malaise, necrosis at the injection site, pain of various locations.
With the cardiovascular system: peripheral edema, vasodilatation, hypertension, peripheral vascular disease, palpitations, tachycardia.
From the digestive system: nausea, constipation, diarrhea, increased AST and ALT levels 5 times the original level, dyspepsia.
From the hematopoietic system: lymphocytes <1500/mkl, neutrophils <1500/mkl, leukocytes <3000/mkl, lymphadenopathy.
From a metabolism: an increase in body weight.
From the musculoskeletal system: myasthenia, myalgia, arthralgia, leg cramps.
The nervous system: hypertonicity, dizziness, insomnia, loss of coordination, anxiety, nervousness.
With the respiratory system: dyspnea.
Dermatological reactions: rash, skin diseases, increased sweating, alopecia.
With the urinary system: the imperative need to urinate, frequent urination.
From the sexual system: metrorrhagia (acyclic bleeding), menorrhagia, dysmenorrhea, in men - impotence, prostate diseases.
The following side effects are based on postmarketing monitoring the use of Betaferon, grouped by organs and systems are presented with the following frequency of occurrence: Very common (≥ 10%), relatively frequent (<10% - ≥ 1%), infrequent (<1% - ≥ 0.1%), rarely (<0.1% - ≥ 0.01%), very rare (<0.01%). General reaction: very often - flu-like symptoms (fever, chills, myalgia, headache, excessive sweating), the frequency of these symptoms decreased over time, rarely - malaise, chest pain.
From the hematopoietic system: Infrequent - leukopenia, anemia, thrombocytopenia, rarely - lymphadenopathy.
Cardio-vascular system: Infrequent - hypertension, rarely - cardiomyopathy, tachycardia, palpitations.
On the part of the endocrine system: rarely - dysfunction of the thyroid gland, hyperthyroidism, hypothyroidism.
CNS: Infrequent - muscular hypertonicity, depression, rarely - seizures, confusion, agitation, emotional lability, suicidal attempts.
Part of the respiratory system: rarely - dyspnea, bronchospasm.
From the digestive system: Infrequent: - nausea, vomiting, increased activity of ACT, ALT, rarely - increased levels of bilirubin and GGT activity, pancreatitis, anorexia.
From the musculoskeletal system: Infrequent - myalgia.
From the reproductive system: rarely - menstrual irregularities.
Allergic reactions: seldom - anaphylactic reactions.
Local reactions: very common - congestion, local swelling, inflammation, pain, rarely - skin necrosis (with time with continued treatment the frequency of reactions at the site of injection usually decreases).
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