Syndaxil is a natural anti-cancer drug obtained semi-synthetically from a plant, binding to plasma proteins is 88-98%. The half-life from blood to tissue is 30 minutes. It easily penetrates and is adsorbed by tissues, accumulates mainly in the liver, spleen, pancreas, stomach, intestines, heart and muscles.
It is metabolized in the liver by hydroxylation with the participation of cytochrome P450 isoenzymes CYP2D8 (with the formation of the metabolite-6-alpha-hydroxypaclitaxel) and CYP3CA4 (with the formation of the metabolites 3-para-hydroxypaclitaxel and 6-alpha, 3-para-dihydroxypaclitaxel). T1 / 2 and total clearance are variable and depend on the dose and duration of intravenous administration: 13.1-52.7 h and 12.2-23.8 l / h / m2, respectively. 90% of the drug is excreted in the bile in the form of metabolites. In a small amount (from 1.3 to 12.6%, depending on the level of the administered dose), it is excreted in the urine in an unchanged form.
Indications for use
For ovarian cancer (first-line therapy for patients with a common form of the disease or a residual tumor (more than 1 cm) after laparotomy (in combination with cisplatin) and second-line therapy for metastases after standard therapy, which did not give a positive result);
breast cancer (presence of affected lymph nodes after standard combination therapy (adjuvant treatment); after relapse of the disease within b months after the start of adjuvant therapy-first-line therapy;
metastatic breast cancer after ineffective standard therapy-second-line therapy);
small cell lung cancer (first-line therapy in patients who are not scheduled for surgical treatment and / or radiation therapy (in combination with cisplatin).
In Kaposi's sarcoma in AIDS patients (second-line therapy, after ineffective therapy with liposomal anthracyclines)Syndaxil is administered intravenously as a 3-hour or 24-hour infusion at a dose of 135-175 mg / m2 with an interval between courses of 3 weeks. The drug is used as monotherapy or in combination with cisplatin (ovarian cancer and non-small cell lung cancer) or doxorubicin (breast cancer).
The recommended dose of Syndaxil for the treatment of Kaposi's sarcoma in AIDS patients is 100 mg / m2 as a 3-hour infusion every 2 weeks. The administration of Syndaxil should not be repeated until the neutrophil content is at least 1500/µl of blood, and the platelet content is at least 100,000/µl of blood.
In patients who have experienced severe neutropenia after taking Syndaxil (neutrophil content <500 / µl of blood for 7 days or more) or severe peripheral neuropathy during subsequent courses of treatment, the dose of Syndaxil should be reduced by 20%. The drug solution is prepared immediately before administration by diluting the concentrate with 0.9% sodium chloride solution, or 5% dextrose solution, or 5% dextrose solution in 0.9% sodium chloride solution for injection, or 5% dextrose solution in Ringer's solution to a final concentration of 0.3-1.2 mg / ml. Prepared solutions can opalesce due to the carrier base present in the dosage form, and after filtration, the opalescence of the solution persists.
From the hematopoietic organs: neutropenia, thrombocytopenia, anemia. Suppression of bone marrow function, mainly granulocyte growth, was the main toxic effect limiting the dose of the drug. The maximum decrease in the level of neutrophils is usually observed on the 8th-11th day, normalization occurs on the 22nd day.
Allergic reactions: in the first hours after taking Syndaxel, hypersensitivity reactions may occur, manifested by bronchospasm, decreased blood pressure, pain behind the sternum, flushes of blood to the face, skin rash, generalized urticaria, angioedema. Isolated cases of chills and back pain are described.
From the cardiovascular system: decreased blood pressure, less often increased blood pressure, bradycardia, possible tachycardia, atrioventricular block, ECG changes, vascular thrombosis and thrombophlebitis.
From the respiratory system: interstitial pneumonia, pulmonary fibrosis, pulmonary embolism, as well as more frequent development of radiation pneumonitis in patients undergoing radiation therapy at the same time.
From the nervous system: mostly paresthesia. Rarely - convulsive seizures of the grand mal type, visual disturbances, ataxia, encephalopathy, autonomic neuropathy, manifested by paralytic intestinal obstruction and orthostatic hypotension
|Active ingredient, mg||250|
|1 bottle, ml||1|
|Ampoules per package, pcs||10|
|Packing||Ampoule, Packing (10 ampoules)|