Pharmacological action
Interferon. It is a highly purified sterile protein containing 165 amino acids. Identical to human leukocyte interferon alpha-2a. It possesses antiviral, anticancer and immunomodulatory activity. It is possible that the mechanism of antiviral and antitumor effect associated with changes in the synthesis of RNA, DNA and proteins. Inhibits viral replication in cells infected with viruses. Increases phagocytic activity of macrophages and enhances specific cytotoxic effect of lymphocytes on target cells.
Pharmacokinetics
After i / m administration C max of interferon alfa-2a observed in 3.8 h. After sc administration C max achieved after 7.3 hours after a V d / in the introduction on the background of the equilibrium concentration is approximately 0.4 L / kg. Interferon alfa-2a undergoes rapid metabolism in the kidneys and to a lesser extent - in the liver. Write mainly by the kidneys. T 1 / 2 an average of 5.1 hours
Statement
Tumours of the lymphatic system and the hemopoietic system: volosatokletochny leukemia, myeloma, cutaneous T-cell lymphoma, chronic myelogenous leukemia, thrombocytosis in myeloproliferative diseases, non-Hodgkin's lymphoma low-grade malignancy.
Solid tumors: Kaposi's sarcoma in AIDS patients without a history of opportunistic infections, renal cell carcinoma, running, melanoma metastases, melanoma after surgical resection (tumor thickness of more than 1.5 mm) in the absence of lymph nodes and distant metastases.
Viral diseases: chronic active hepatitis B in adults with markers of viral replication (positive for HBV-DNA, DNA polymerase, HBeAg); chronic active hepatitis C in adults with antibodies to hepatitis C virus or HCV RNA in serum and increased activity of ALT without signs of hepatic decompensation (Child class A Pugh); genital warts, diseases caused by Herpes simplex virus types 1 and 2 and Varicella zoster (including simple and herpes zoster, recurrent herpes face, genitals, herpes gingivitis and stomatitis ).
Dosage regimen
Set individually, depending on the testimony and stage of disease, the state of the hemopoietic system, treatment regimens.
Side effect
Flu-like syndrome: fatigue, fever, chills, muscle aches, headache, joint pain and sweating.
From the side of the central nervous system and peripheral nervous system: dizziness, blurred vision, depression, confusion, nervousness, anxiety, sleep disturbances, paresthesia, neuropathy, tremor, rare - marked drowsiness, convulsions, coma, cerebral circulatory disorders, coronary retinopathy.
On the part of the digestive system: loss of appetite, nausea, rarely - vomiting, diarrhea, weight loss, weak or moderate abdominal pain, increased activity of ALT, alkaline phosphatase, increased bilirubin concentration in serum, constipation, bloating, heartburn, and in some cases - recurrence of peptic ulcer and bleeding from the gastrointestinal tract.
Since the cardiovascular system: changes in blood pressure, edema, cyanosis, arrhythmias, feeling the heartbeat, chest pain, rarely - a little shortness of breath, cough, and in some cases - pulmonary edema, symptoms of chronic heart failure, sudden cardiac arrest, myocardial infarction.
From the urinary system: proteinuria; rarely - increasing urea, creatinine and uric acid in blood plasma.
From the side of hematopoiesis: transient leukopenia, rarely - thrombocytopenia, decrease in hemoglobin and hematocrit.
Dermatological reactions: rash, itching, alopecia, dry skin and mucous membranes.
Other: rhinitis, nasal bleeding.
Contraindications
Severe heart disease (including history), severe renal dysfunction, severe liver problems, severe violations of myeloid germ blood, cramps, and / or dysfunction of the central nervous system, chronic hepatitis with marked decompensation or cirrhosis, chronic hepatitis in patients receiving or recently received immunosuppressant therapy (except for short-term treatment with steroids), the patients with CML (if the patient has an HLA-identical relative, and he will or can be allogeneic bone marrow transplantation in the near future), hypersensitivity to recombinant interferon alfa-2a .
Application of pregnancy and breastfeeding
The use of interferon alfa-2a in pregnancy is only justified if the benefits of the therapy exceeds potential risk to the fetus. If necessary, use during lactation should decide on the termination of breastfeeding.
Women of childbearing age against the use of interferon alfa-2a should use reliable methods of contraception.
Cautions
In mild and moderate renal failure, liver or bone marrow require careful monitoring.
With caution used in chronic hepatitis with autoimmune diseases in history. When a background of treatment of pathological changes in liver function tests patients need careful monitoring and if necessary, removal of therapy.
Patients receiving interferon psychoneurological recommended regular screening, as In rare cases, there were suicide attempts.
With extreme caution to patients with severe myelosuppression.
Prior to and regularly during treatment should be a detailed analysis of the blood.
Patients after transplantation (eg kidney or bone marrow) immunosuppression medication may be less effective as interferon stimulates the immune system.
If symptoms of hyperglycemia is necessary to monitor glucose levels in blood plasma and the corresponding observation. Patients with diabetes may require dosage adjustment hypoglycemic drugs.
Efficacy, safety of children with chronic myeloid leukemia is not installed.
Effects on ability to drive vehicles and management mechanisms
Depending on the dosing regimen and individual patient's sensitivity interferon alfa-2a can affect the reaction rate, the ability to potentially dangerous activities, including driving vehicles, working with machines and mechanisms.
Drug Interactions
In the application of interferon alfa-2a should consider the possibility of drug interactions with both prescribers, by affecting the liver microsomal enzyme system.
Interferon alfa-2a may enhance neurotoxic, cardiotoxic and myelotoxic effect of drugs, were appointed before or simultaneously with it.
Interferon. It is a highly purified sterile protein containing 165 amino acids. Identical to human leukocyte interferon alpha-2a. It possesses antiviral, anticancer and immunomodulatory activity. It is possible that the mechanism of antiviral and antitumor effect associated with changes in the synthesis of RNA, DNA and proteins. Inhibits viral replication in cells infected with viruses. Increases phagocytic activity of macrophages and enhances specific cytotoxic effect of lymphocytes on target cells.
Pharmacokinetics
After i / m administration C max of interferon alfa-2a observed in 3.8 h. After sc administration C max achieved after 7.3 hours after a V d / in the introduction on the background of the equilibrium concentration is approximately 0.4 L / kg. Interferon alfa-2a undergoes rapid metabolism in the kidneys and to a lesser extent - in the liver. Write mainly by the kidneys. T 1 / 2 an average of 5.1 hours
Statement
Tumours of the lymphatic system and the hemopoietic system: volosatokletochny leukemia, myeloma, cutaneous T-cell lymphoma, chronic myelogenous leukemia, thrombocytosis in myeloproliferative diseases, non-Hodgkin's lymphoma low-grade malignancy.
Solid tumors: Kaposi's sarcoma in AIDS patients without a history of opportunistic infections, renal cell carcinoma, running, melanoma metastases, melanoma after surgical resection (tumor thickness of more than 1.5 mm) in the absence of lymph nodes and distant metastases.
Viral diseases: chronic active hepatitis B in adults with markers of viral replication (positive for HBV-DNA, DNA polymerase, HBeAg); chronic active hepatitis C in adults with antibodies to hepatitis C virus or HCV RNA in serum and increased activity of ALT without signs of hepatic decompensation (Child class A Pugh); genital warts, diseases caused by Herpes simplex virus types 1 and 2 and Varicella zoster (including simple and herpes zoster, recurrent herpes face, genitals, herpes gingivitis and stomatitis ).
Dosage regimen
Set individually, depending on the testimony and stage of disease, the state of the hemopoietic system, treatment regimens.
Side effect
Flu-like syndrome: fatigue, fever, chills, muscle aches, headache, joint pain and sweating.
From the side of the central nervous system and peripheral nervous system: dizziness, blurred vision, depression, confusion, nervousness, anxiety, sleep disturbances, paresthesia, neuropathy, tremor, rare - marked drowsiness, convulsions, coma, cerebral circulatory disorders, coronary retinopathy.
On the part of the digestive system: loss of appetite, nausea, rarely - vomiting, diarrhea, weight loss, weak or moderate abdominal pain, increased activity of ALT, alkaline phosphatase, increased bilirubin concentration in serum, constipation, bloating, heartburn, and in some cases - recurrence of peptic ulcer and bleeding from the gastrointestinal tract.
Since the cardiovascular system: changes in blood pressure, edema, cyanosis, arrhythmias, feeling the heartbeat, chest pain, rarely - a little shortness of breath, cough, and in some cases - pulmonary edema, symptoms of chronic heart failure, sudden cardiac arrest, myocardial infarction.
From the urinary system: proteinuria; rarely - increasing urea, creatinine and uric acid in blood plasma.
From the side of hematopoiesis: transient leukopenia, rarely - thrombocytopenia, decrease in hemoglobin and hematocrit.
Dermatological reactions: rash, itching, alopecia, dry skin and mucous membranes.
Other: rhinitis, nasal bleeding.
Contraindications
Severe heart disease (including history), severe renal dysfunction, severe liver problems, severe violations of myeloid germ blood, cramps, and / or dysfunction of the central nervous system, chronic hepatitis with marked decompensation or cirrhosis, chronic hepatitis in patients receiving or recently received immunosuppressant therapy (except for short-term treatment with steroids), the patients with CML (if the patient has an HLA-identical relative, and he will or can be allogeneic bone marrow transplantation in the near future), hypersensitivity to recombinant interferon alfa-2a .
Application of pregnancy and breastfeeding
The use of interferon alfa-2a in pregnancy is only justified if the benefits of the therapy exceeds potential risk to the fetus. If necessary, use during lactation should decide on the termination of breastfeeding.
Women of childbearing age against the use of interferon alfa-2a should use reliable methods of contraception.
Cautions
In mild and moderate renal failure, liver or bone marrow require careful monitoring.
With caution used in chronic hepatitis with autoimmune diseases in history. When a background of treatment of pathological changes in liver function tests patients need careful monitoring and if necessary, removal of therapy.
Patients receiving interferon psychoneurological recommended regular screening, as In rare cases, there were suicide attempts.
With extreme caution to patients with severe myelosuppression.
Prior to and regularly during treatment should be a detailed analysis of the blood.
Patients after transplantation (eg kidney or bone marrow) immunosuppression medication may be less effective as interferon stimulates the immune system.
If symptoms of hyperglycemia is necessary to monitor glucose levels in blood plasma and the corresponding observation. Patients with diabetes may require dosage adjustment hypoglycemic drugs.
Efficacy, safety of children with chronic myeloid leukemia is not installed.
Effects on ability to drive vehicles and management mechanisms
Depending on the dosing regimen and individual patient's sensitivity interferon alfa-2a can affect the reaction rate, the ability to potentially dangerous activities, including driving vehicles, working with machines and mechanisms.
Drug Interactions
In the application of interferon alfa-2a should consider the possibility of drug interactions with both prescribers, by affecting the liver microsomal enzyme system.
Interferon alfa-2a may enhance neurotoxic, cardiotoxic and myelotoxic effect of drugs, were appointed before or simultaneously with it.
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