Gikamtin lyophilisate for infusion 4mg N5
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Active ingredients
Topotecan
Release form
Lyophilisate
Composition
1 fl. topotecan (in the form of hydrochloride) 4 mg. Excipients: glacial acetic acid - 4.42 g / l, water d / and - up to 1 l.
Pharmacological effect
An antitumor drug, an inhibitor of topoisomerase-I, an enzyme directly involved in DNA replication. Topotecan inhibits the activity of topoisomerase-I, stabilizing the covalent complex of the enzyme and helically-split DNA, which is an intermediate of the catalytic mechanism. Inhibition of topoisomerase-I leads to single-stranded DNA rupture and arrest of DNA replication.
Indications
- small cell lung cancer. - ovarian cancer. - recurrent or persistent cervical cancer, which is not amenable to surgical treatment and / or radiation therapy (stage IV B), as part of combination therapy with cisplatin.
Contraindications
- pronounced inhibition of bone marrow function (neutrophil count less than 1500 / μl, platelet count less than 100 000 / μl) - anemia (Hb less than 9 g / dL) - pregnancy - lactation (breastfeeding) - children's age (lack of experience) - increased history of sensitivity to topotecan or other components that make up the drug.
Use during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation (breastfeeding). Women of childbearing age and men in the period of taking Gikamtin should use reliable contraception. If pregnancy occurs, you should immediately inform your doctor.
Dosage and administration
Gikamtin is administered as a 30-minute IV infusion. Before the appointment of the first course of therapy with Gikamtin, the number of neutrophils should be & # 8805 .1500 / μl, platelets & # 8805. 100 000 / mkl, level of hemoglobin & # 8805. 9 g / dl (after transfusion, if necessary). The drug is prescribed for adults and elderly patients. In small cell lung cancer and ovarian cancer, 1.5 mg / m2 is prescribed daily for 5 consecutive days with an interval of 3 weeks (21 days) before the start of each course. To achieve the effect, it is recommended to conduct at least 4 courses of therapy (in clinical studies, the average time of onset of effect in patients with ovarian cancer was 7.6-11.7 weeks, in patients with small cell lung cancer - 6.1 weeks.In approximately 18% of patients with ovarian cancer, the effect was achieved after 5 or more courses of therapy). Repeated courses of therapy with Gikamtin can only be performed with the following indicators: neutrophils & # 8805 .1000 / mcl, platelets & # 8805 .100 000 / mcl, hemoglobin & # 8805 .9 g / dl (including after transfusion, if it's necessary). In severe neutropenia (the number of neutrophils is less than 500 / μl) for 7 days or more, or febrile neutropenia, or in case of delay in treatment due to neutropenia, you should either reduce the dose of the drug to 1.25 mg / m2 / day (or later to 1 mg / m2 / day), or follow-up courses with the appointment of prophylactic administration of G-CSF. If neutropenia in the presence of G-CSF persists, the drug doses should be reduced. With a decrease in the number of platelets during the previous course of chemotherapy less than 25 000 / μl, the doses should be reduced in the same way. In clinical studies, therapy with topotecan was discontinued if it was necessary to reduce the dose below 1 mg / m2. In cervical cancer, the recommended dose of Gikamtin is 0.75 mg / m2 on the 1st, 2nd and 3rd day. On the 1st day of therapy, after administration of the Gikamtin drug, cisplatin is administered at a dose of 50 mg / m2. This scheme is repeated every 21 days, only 6 courses. When signs of progression of the disease Gikamtin should be abolished. Repeated courses of therapy with Gikamtin can only be performed with the following indicators: neutrophil count & # 8805 .1500 / μl, platelets - & # 8805 .100 000 / μl, hemoglobin - & # 8805 .9 g / dl (after transfusion, if necessary) . In severe neutropenia (neutrophil count less than 500 / μl) for 7 days or more, or febrile neutropenia, or in case of delay in treatment due to neutropenia, the drug dose for subsequent courses should be reduced by 20% to 600 μg / m2 / day ( or later up to 450 mcg / m2 / day), or follow-up courses with the appointment of prophylactic administration of G-CSF. If neutropenia in the presence of G-CSF persists, the drug doses should be reduced. By reducing the number of platelets less than 25 000 / μl dose should be reduced in a similar way. Appointment Gikamtin for the treatment of children is contraindicated, because current experience with the drug in this category of patients is insufficient. In patients with impaired renal function with monotherapy for QA & # 8805. 40 ml / min correction of the dosing regimen is not required.When QA is from 20 to 39 ml / min, the recommended dose is 750 mcg / m2 / day. recommendations are based on studies including patients with advanced cancer. When QA is less than 20 ml / min, there are no recommendations. In combination therapy with Gikamtin and cisplatin for the treatment of cervical cancer, it is recommended to begin therapy only in patients whose plasma creatinine concentration does not exceed 1.5 mg / dl. If during treatment the plasma creatinine level exceeds 1.5 mg / dl, you should follow the recommendations of cisplatin for reducing or eliminating cisplatin. In the case of cisplatin withdrawal, there is insufficient data regarding the continuation of monotherapy with Gikamtin in patients with cervical cancer. For patients with impaired liver function (bilirubin level from 1.5 to 10 mg / dL), dosage adjustment is not required with monotherapy. In combination therapy with other cytotoxic drugs, dose adjustment may be required. Terms of preparation of the solution The contents of the vial should be dissolved in 4 ml of sterile water for injection to a concentration of 1 mg / ml. The resulting solution must be diluted with a 0.9% solution of sodium chloride or 5% dextrose solution to a concentration of 25-50 μg / ml. The reconstituted solution should be used immediately after preparation or stored in a refrigerator at a temperature of 2 ° to 8 ° C for 24 hours. The prepared solution should be used immediately after preparation or stored in a refrigerator at a temperature of 2 ° to 8 ° C for 24 hours.
Side effects
Prolonged use does not cause an increase in the toxic effect of the drug. Serious manifestations of cardiotoxicity, neurotoxicity, organ toxicity were not observed. The adverse events listed below are listed in accordance with the damage to organs and organ systems and the frequency of occurrence. The frequency of occurrence is determined as follows: very often (& # 8805 .1 / 10), often (& # 8805 .1 / 100, less than 1/10), infrequently (& # 8805 .1 / 1000, less than 1/100), rarely (& # 8805 .1 / 10 000, less than 1/1000), very rarely (less than 1/10 000, including some cases). Frequency categories were formed based on clinical studies of the drug. On the part of the hematopoietic system: very often - neutropenia, febrile neutropenia, leukopenia, thrombocytopenia, anemia1, changes in blood parameters2. often - pancytopenia. very rarely - side effectsaffecting blood test results. frequency is unknown - bleeding, severe and latent bleeding due to thrombocytopenia. From the musculoskeletal system: often - myalgia. On the part of the digestive system: very often - diarrhea3, nausea, vomiting (including severe), abdominal pain4, constipation, stomatitis, anorexia (including severe). often - hyperbilirubinemia. very rarely - intestinal inflammation (colitis). frequency is unknown - intestinal obstruction. On the part of the immune system: often - hypersensitivity reactions, including rashes. On the part of the respiratory system: rarely - interstitial lung disease. From the skin and subcutaneous fat: very often - alopecia. Allergic reactions: very often - anaphylactoid reactions. rarely - urticaria, difficulty breathing. very rarely - angioedema. frequency is unknown - skin rash (including erythematous, maculopapular rash, urticaria, dermatitis, bullous erythema). General disorders and disorders at the injection site: very often - fever, fatigue, asthenia, infections. often - weakness, sepsis. very rarely - extravasation: hematoma or skin hyperemia at the injection site (during extravasation) (reactions associated with extravasation were mild and, as a rule, did not require specific treatment). frequency unknown - shortness of breath, infection. 1 Cases of moderate to severe anemia (grade 3 and 4 - Hb less than 8 g / dL) occurred in 25% of cases (12% of courses). The median time to onset of moderate and severe anemia is the 12th day with an average duration of 7 days. In 46% of courses with moderate and severe degrees of anemia, the duration is more than 7 days. 30% of patients received red blood cell transfusions (13% of courses). Erythropoietin was administered to 10% of patients in 8% of the courses. 2 Low number of cells required for blood coagulation, which can cause bruising, bleeding and, rarely, severe bleeding (hemorrhage). 3 With on / in the introduction of topotecan diarrhea in patients over the age of 65 years occurred in 10% of cases. 4 Cases of neutropenic colitis, including fatal cases, were regarded as complications of drug-induced neutropenia.
special instructions
Prolonged use does not cause an increase in the toxic effect of the drug. Serious manifestations of cardiotoxicity, neurotoxicity, organ toxicity were not observed.The adverse events listed below are listed in accordance with the damage to organs and organ systems and the frequency of occurrence. The frequency of occurrence is determined as follows: very often (& # 8805 .1 / 10), often (& # 8805 .1 / 100, less than 1/10), infrequently (& # 8805 .1 / 1000, less than 1/100), rarely (& # 8805 .1 / 10 000, less than 1/1000), very rarely (less than 1/10 000, including some cases). Frequency categories were formed based on clinical studies of the drug. On the part of the hematopoietic system: very often - neutropenia, febrile neutropenia, leukopenia, thrombocytopenia, anemia1, changes in blood parameters2. often - pancytopenia. very rarely, side effects that affect blood test results. frequency is unknown - bleeding, severe and latent bleeding due to thrombocytopenia. From the musculoskeletal system: often - myalgia. On the part of the digestive system: very often - diarrhea3, nausea, vomiting (including severe), abdominal pain4, constipation, stomatitis, anorexia (including severe). often - hyperbilirubinemia. very rarely - intestinal inflammation (colitis). frequency is unknown - intestinal obstruction. On the part of the immune system: often - hypersensitivity reactions, including rashes. On the part of the respiratory system: rarely - interstitial lung disease. From the skin and subcutaneous fat: very often - alopecia. Allergic reactions: very often - anaphylactoid reactions. rarely - urticaria, difficulty breathing. very rarely - angioedema. frequency is unknown - skin rash (including erythematous, maculopapular rash, urticaria, dermatitis, bullous erythema). General disorders and disorders at the injection site: very often - fever, fatigue, asthenia, infections. often - weakness, sepsis. very rarely - extravasation: hematoma or skin hyperemia at the injection site (during extravasation) (reactions associated with extravasation were mild and, as a rule, did not require specific treatment). frequency unknown - shortness of breath, infection. 1 Cases of moderate to severe anemia (grade 3 and 4 - Hb less than 8 g / dL) occurred in 25% of cases (12% of courses). The median time to onset of moderate and severe anemia is the 12th day with an average duration of 7 days. In 46% of courses with moderate and severe degrees of anemia, the duration is more than 7 days.30% of patients received red blood cell transfusions (13% of courses). Erythropoietin was administered to 10% of patients in 8% of the courses. 2 Low number of cells required for blood coagulation, which can cause bruising, bleeding and, rarely, severe bleeding (hemorrhage). 3 With on / in the introduction of topotecan diarrhea in patients over the age of 65 years occurred in 10% of cases. 4 Cases of neutropenic colitis, including fatal cases, were regarded as complications of drug-induced neutropenia.