Composition, structure and packing Abitaxel
Concentrate for solution for infusion viscous, transparent, colorless or slightly yellow.
1 ml - 1 fl. paclitaxel 6 mg, 30 mg.
Excipients: castor oil polioksietilirovannogo, ethanol, glacial acetic acid.
Concentrate for solution for infusion viscous, transparent, colorless or slightly yellow.
1 ml - 1 fl. paclitaxel 6 mg, 100 mg.
Excipients: castor oil polioksietilirovannogo, ethanol, glacial acetic acid.
Clinico-pharmacological group: antineoplastic drug.
Pharmacological action Abitaxel
Anticancer drugs of plant origin, obtained through a semi-synthetic plant Taxus baccata. The mechanism of action related to the fact that Abitaksel stimulates microtubule assembly defect of tubulin dimer, stabilizes their structure and inhibits the dynamic reorganization of the interphase, which violates the mitotic cell function. It was a dose-dependent suppression of bone marrow hematopoiesis.
The experimental data have mutagenic and embryotoxic properties, causes a decrease in reproductive function.
Pharmacokinetics
Distribution Abitaxel
Following in / introduction of paclitaxel dynamics of its concentration in plasma is described by a two-phase curve. Intensively distributed in the extravascular space. Linking to plasma proteins is 89-98% (depends on the dose).
After the introduction in doses of 170 mg/m2 and above the therapeutic drug concentration in blood plasma determined for 6-12 hours Stain Paclitaxel appears mainly in the form of metabolites with the bile through the gastrointestinal tract and in small quantities (from 1.3 to 12.6% in Depending on the level of the administered dose) as unchanged by the kidneys.
Statement
ovarian cancer;
breast cancer;
non small cell lung cancer of the lungs.
Dosage regimen
The recommended standard dose of 135-175 mg/m2 Abitaksela, which is introduced into / through a 3-hour or 24-hour infusion of 1 every three weeks. When choosing the dose and dosing regimen in each individual case should be guided by these specialized literature.
The introduction of the drug Abitaksel should not repeat so long as the contents of neutrophils did not amount to at least 1500/mkl and platelet count of at least 100 000/mkl. Patients with severe neutropenia (neutrophils less than 500 cells / mm content within 7 days or longer periods of time) or with a severe form of peripheral neuropathy during follow-up courses Abitaksela dose should be reduced by 20%. The drug is used as monotherapy or in combination therapy: with cisplatin - in ovarian cancer and non small cell lung cancer, lung with doxorubicin - in breast cancer. If Abitaksel used in combination with cisplatin, you must first enter Abitaksel, then cisplatin.
Terms of preparations for the introduction and storage solution to prevent severe hypersensitivity reactions in all patients prior to drug administration should be Abitaksel sedation with the use of GCS, blockers of histamine H1 and H2 receptors. Premedication could include dexamethasone (or equivalent) in a dose of 20 mg orally approximately 12 h and 6 h before injection of the drug Abitaksel, diphenhydramine (or equivalent) at a dose of 50 mg / in 30-60 minutes, cimetidine at a dose of 300 mg / in or ranitidine at a dose of 50 mg / in 30-60 minutes prior to drug administration Abitaksel. The solution preparation is prepared immediately prior to the introduction, breeding concentrate 0.9% sodium chloride solution for injection or 5% dextrose (glucose) or 5% dextrose in 0.9% sodium chloride solution or 5% dextrose in Ringer's solution to a final concentration of 0.3- 1.2 mg / ml.
Polioksietilirovannogo castor oil, which is part of the drug Abitaksel may cause extraction DEGP [di-(2-hexyl) phthalate] of plasticized polyvinyl chloride (PVC) containers, and the degree of washout DEGP increases with time and with increasing concentration of the solution. Therefore, when preparing, storing and administration of the drug Abitaksel should use equipment that does not contain parts of polyvinyl chloride. Keep prepared for infusion solution Abitaksela preferably in bottles made of glass or polypropylene, either in bags made of polypropylene or polyolefin, and the introduction to using the system, the inner surface of which is made of polyethylene. Side effect
On the part of the hemopoietic system: neutropenia (Grade 4 neutropenia observed: usually occurs in 8-11 days, the normalization of states in 22 days), thrombocytopenia, anemia. The suppression of bone marrow function mainly granulocytic germ is a major toxic effect.
Since the cardiovascular system: arterial hypotension, rarely - arterial hypertension, bradycardia, tachycardia is possible, AV-block, ECG changes, thrombosis of the upper extremities, thrombophlebitis.
On the part of the respiratory system: pneumonia, pulmonary embolism, pulmonary fibrosis, radiation pneumonitis (in patients undergoing simultaneous course of radiation therapy).
From the side of the central nervous system and peripheral nervous system: paresthesias, seizures type of grand mal, visual disturbances, ataxia, encephalopathy, neuropathy at the level of the autonomic nervous system, leading to paralytic ileus and orthostatic hypotension.
On the part of the digestive system: nausea, vomiting, diarrhea, mucositis, intestinal obstruction, intestinal perforation, mesenteric artery thrombosis, including ischemic colitis, increased activity of AST, alkaline phosphatase and bilirubin levels in serum and in some cases - liver necrosis and hepatic encephalopathy.
The part of the musculoskeletal system: arthralgia, myalgia. Allergic reactions: in the first hours after injection Abitaksela possible hypersensitivity reactions: wheezing, blood pressure reduction, pain behind the breastbone, a rush of blood to the face, skin rash, angioedema, and in some cases - chills and back pain.
Dermatological reactions: alopecia; rarely - violation pigmentation or discoloration of the nail bed. Local reactions: swelling, pain, erythema, induration and pigmentation of the skin at the injection site; extravasations may cause cellulite.
Other: asthenia, general malaise. The frequency and severity of side effects are dose-dependent nature.
Contraindications
the absolute number of neutrophils less 1500/mkl;
Pregnancy
lactation (breastfeeding);
sensitivity to paclitaxel or any other component of the drug, including polioksietilirovannogo to castor oil.
Pregnancy and lactation
Abitaksel contraindicated in pregnancy. When necessary use during lactation should resolve the issue of termination of breastfeeding.
Cautions
Abitaksel should be administered under the supervision of a physician with experience in the use of anticancer drugs. Since usually hypersensitivity reactions occur in the early hours on the background of the introduction Abitaksela is recommended at this time to conduct a careful monitoring of vital functions. In the case of severe hypersensitivity reactions infusion Abitaksel should cease immediately and start symptomatic treatment, and re-enter the drug should not be. Abitaksel a cytotoxic agent, with the work that needs to be careful, use gloves and avoid skin contact and mucous membranes.
After contact with skin Abitaksela should thoroughly wash it with soap and water, mucous membranes (eyes) - with plenty of water. Due to the fact that there are no antidotes to Abitakselu, to avoid an overdose should be carefully calculate the dose.
Use in Pediatrics
The safety and efficacy Abitaksel in children has not been established.
Overdose
Symptoms: may gain manifestations described side effects.
Treatment: No specific antidote. Monitor vital functions, symptomatic therapy, including antihistamines, antiemetics, SCS.
Drug Interactions
Introduction
Abitaksela after the introduction of cisplatin compared with the reverse sequence (Abitaksel to cisplatin), leads to a decrease in paclitaxel clearance and enhance its toxicity. The simultaneous use Abitaksela with cimetidine, ranitidine, dexamethasone or diphenhydramine does not affect the binding of paclitaxel to proteins. Ketoconazole inhibits the metabolism of paclitaxel, and therefore caution should be exercised when it is simultaneous with the appointment Abitakselom.
Terms and Conditions of storage
The drug should be stored in a dry, dark place at temperatures from 15 ° to 25 ° C.
Shelf life - 2 years. Obtained after mixing solutions Abitaksela stable at room temperature for 27 h. Reconstituted solutions may opalestsirovat because of the presence in the dosage form the basis of the carrier, and after filtration solution opalescence persists.
Concentrate for solution for infusion viscous, transparent, colorless or slightly yellow.
1 ml - 1 fl. paclitaxel 6 mg, 30 mg.
Excipients: castor oil polioksietilirovannogo, ethanol, glacial acetic acid.
Concentrate for solution for infusion viscous, transparent, colorless or slightly yellow.
1 ml - 1 fl. paclitaxel 6 mg, 100 mg.
Excipients: castor oil polioksietilirovannogo, ethanol, glacial acetic acid.
Clinico-pharmacological group: antineoplastic drug.
Pharmacological action Abitaxel
Anticancer drugs of plant origin, obtained through a semi-synthetic plant Taxus baccata. The mechanism of action related to the fact that Abitaksel stimulates microtubule assembly defect of tubulin dimer, stabilizes their structure and inhibits the dynamic reorganization of the interphase, which violates the mitotic cell function. It was a dose-dependent suppression of bone marrow hematopoiesis.
The experimental data have mutagenic and embryotoxic properties, causes a decrease in reproductive function.
Pharmacokinetics
Distribution Abitaxel
Following in / introduction of paclitaxel dynamics of its concentration in plasma is described by a two-phase curve. Intensively distributed in the extravascular space. Linking to plasma proteins is 89-98% (depends on the dose).
After the introduction in doses of 170 mg/m2 and above the therapeutic drug concentration in blood plasma determined for 6-12 hours Stain Paclitaxel appears mainly in the form of metabolites with the bile through the gastrointestinal tract and in small quantities (from 1.3 to 12.6% in Depending on the level of the administered dose) as unchanged by the kidneys.
Statement
ovarian cancer;
breast cancer;
non small cell lung cancer of the lungs.
Dosage regimen
The recommended standard dose of 135-175 mg/m2 Abitaksela, which is introduced into / through a 3-hour or 24-hour infusion of 1 every three weeks. When choosing the dose and dosing regimen in each individual case should be guided by these specialized literature.
The introduction of the drug Abitaksel should not repeat so long as the contents of neutrophils did not amount to at least 1500/mkl and platelet count of at least 100 000/mkl. Patients with severe neutropenia (neutrophils less than 500 cells / mm content within 7 days or longer periods of time) or with a severe form of peripheral neuropathy during follow-up courses Abitaksela dose should be reduced by 20%. The drug is used as monotherapy or in combination therapy: with cisplatin - in ovarian cancer and non small cell lung cancer, lung with doxorubicin - in breast cancer. If Abitaksel used in combination with cisplatin, you must first enter Abitaksel, then cisplatin.
Terms of preparations for the introduction and storage solution to prevent severe hypersensitivity reactions in all patients prior to drug administration should be Abitaksel sedation with the use of GCS, blockers of histamine H1 and H2 receptors. Premedication could include dexamethasone (or equivalent) in a dose of 20 mg orally approximately 12 h and 6 h before injection of the drug Abitaksel, diphenhydramine (or equivalent) at a dose of 50 mg / in 30-60 minutes, cimetidine at a dose of 300 mg / in or ranitidine at a dose of 50 mg / in 30-60 minutes prior to drug administration Abitaksel. The solution preparation is prepared immediately prior to the introduction, breeding concentrate 0.9% sodium chloride solution for injection or 5% dextrose (glucose) or 5% dextrose in 0.9% sodium chloride solution or 5% dextrose in Ringer's solution to a final concentration of 0.3- 1.2 mg / ml.
Polioksietilirovannogo castor oil, which is part of the drug Abitaksel may cause extraction DEGP [di-(2-hexyl) phthalate] of plasticized polyvinyl chloride (PVC) containers, and the degree of washout DEGP increases with time and with increasing concentration of the solution. Therefore, when preparing, storing and administration of the drug Abitaksel should use equipment that does not contain parts of polyvinyl chloride. Keep prepared for infusion solution Abitaksela preferably in bottles made of glass or polypropylene, either in bags made of polypropylene or polyolefin, and the introduction to using the system, the inner surface of which is made of polyethylene. Side effect
On the part of the hemopoietic system: neutropenia (Grade 4 neutropenia observed: usually occurs in 8-11 days, the normalization of states in 22 days), thrombocytopenia, anemia. The suppression of bone marrow function mainly granulocytic germ is a major toxic effect.
Since the cardiovascular system: arterial hypotension, rarely - arterial hypertension, bradycardia, tachycardia is possible, AV-block, ECG changes, thrombosis of the upper extremities, thrombophlebitis.
On the part of the respiratory system: pneumonia, pulmonary embolism, pulmonary fibrosis, radiation pneumonitis (in patients undergoing simultaneous course of radiation therapy).
From the side of the central nervous system and peripheral nervous system: paresthesias, seizures type of grand mal, visual disturbances, ataxia, encephalopathy, neuropathy at the level of the autonomic nervous system, leading to paralytic ileus and orthostatic hypotension.
On the part of the digestive system: nausea, vomiting, diarrhea, mucositis, intestinal obstruction, intestinal perforation, mesenteric artery thrombosis, including ischemic colitis, increased activity of AST, alkaline phosphatase and bilirubin levels in serum and in some cases - liver necrosis and hepatic encephalopathy.
The part of the musculoskeletal system: arthralgia, myalgia. Allergic reactions: in the first hours after injection Abitaksela possible hypersensitivity reactions: wheezing, blood pressure reduction, pain behind the breastbone, a rush of blood to the face, skin rash, angioedema, and in some cases - chills and back pain.
Dermatological reactions: alopecia; rarely - violation pigmentation or discoloration of the nail bed. Local reactions: swelling, pain, erythema, induration and pigmentation of the skin at the injection site; extravasations may cause cellulite.
Other: asthenia, general malaise. The frequency and severity of side effects are dose-dependent nature.
Contraindications
the absolute number of neutrophils less 1500/mkl;
Pregnancy
lactation (breastfeeding);
sensitivity to paclitaxel or any other component of the drug, including polioksietilirovannogo to castor oil.
Pregnancy and lactation
Abitaksel contraindicated in pregnancy. When necessary use during lactation should resolve the issue of termination of breastfeeding.
Cautions
Abitaksel should be administered under the supervision of a physician with experience in the use of anticancer drugs. Since usually hypersensitivity reactions occur in the early hours on the background of the introduction Abitaksela is recommended at this time to conduct a careful monitoring of vital functions. In the case of severe hypersensitivity reactions infusion Abitaksel should cease immediately and start symptomatic treatment, and re-enter the drug should not be. Abitaksel a cytotoxic agent, with the work that needs to be careful, use gloves and avoid skin contact and mucous membranes.
After contact with skin Abitaksela should thoroughly wash it with soap and water, mucous membranes (eyes) - with plenty of water. Due to the fact that there are no antidotes to Abitakselu, to avoid an overdose should be carefully calculate the dose.
Use in Pediatrics
The safety and efficacy Abitaksel in children has not been established.
Overdose
Symptoms: may gain manifestations described side effects.
Treatment: No specific antidote. Monitor vital functions, symptomatic therapy, including antihistamines, antiemetics, SCS.
Drug Interactions
Introduction
Abitaksela after the introduction of cisplatin compared with the reverse sequence (Abitaksel to cisplatin), leads to a decrease in paclitaxel clearance and enhance its toxicity. The simultaneous use Abitaksela with cimetidine, ranitidine, dexamethasone or diphenhydramine does not affect the binding of paclitaxel to proteins. Ketoconazole inhibits the metabolism of paclitaxel, and therefore caution should be exercised when it is simultaneous with the appointment Abitakselom.
Terms and Conditions of storage
The drug should be stored in a dry, dark place at temperatures from 15 ° to 25 ° C.
Shelf life - 2 years. Obtained after mixing solutions Abitaksela stable at room temperature for 27 h. Reconstituted solutions may opalestsirovat because of the presence in the dosage form the basis of the carrier, and after filtration solution opalescence persists.
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