Active substanceDocetaxelDocetaxel
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  • Dosage form: & nbspconcentrate for solution for infusion
    Composition:

    1 bottle 0.5 ml with a concentrate for the preparation of a solution for infusions 40 mg / ml contains:

    active substance: docetaxel anhydrous 20.00 mg;

    Excipients: citric acid anhydrous 5.20 mg, polysorbate-80 514,80 mg.

    1 bottle of 2.0 ml with a concentrate for the preparation of a solution for infusions of 40 mg / ml contains:

    active substance: docetaxel anhydrous 80.00 mg;

    Excipients: citric acid anhydrous 20.80 mg, polysorbate-80 2059.20 mg.

    1 bottle with 1.5 ml of solvent contains:

    ethanol 191.10 mg, water for injection up to 1.5 ml.

    1 flask with solvent 6.0 ml contains:

    ethanol 764.40 mg, water for injection up to 6.0 ml.

    1 ml concentrate for solution for infusions 40 mg / ml contains:

    active substance: docetaxel anhydrous 40.0 mg;

    Excipients: citric acid anhydrous 10.4 mg, polysorbate-80 1029.6 mg.

    Description:Concentrate for the preparation of a solution for infusions 40 mg / ml: yellow or brownish-yellow, viscous, clear solution.

    Solvent: colorless, transparent solution with a weak characteristic alcohol smell.

    The reconstituted solution: solution from pale yellow to yellow, transparent, free of visible sediment or undissolved particles.

    Pharmacotherapeutic group:Antitumor agent - alkaloid
    ATX: & nbsp

    L.01.C.D.02   Docetaxel

    Pharmacodynamics:

    Docetaxel is an antitumor drug of plant origin (from the taxoid group). Accumulates tubulin in microtubules, prevents their disintegration, which disrupts the phase of mitosis and interfacial processes in tumor cells. Docetaxel long time is stored in cells, where its concentration reaches high values. It is active against some, though not all, of cells that produce in excess p-glycoprotein, which is encoded by a gene of multiple resistance.

    Pharmacokinetics:

    The pharmacokinetics of docetaxel is dose-dependent and corresponds to a three-phase pharmacokinetic model with a half-life (T1/2) 4 min, 36 min and 11.4 h respectively.

    Binding to plasma proteins is more than 95%.

    Metabolism and excretion

    Within 7 days docetaxel is excreted by the kidneys and through the intestine after oxidation of the tert-butyl ether group with the participation of the cytochrome P450 isoenzyme system. Kidney excretion is 6% radioactive dose, through the intestine - 75%. Approximately 80% of the radioactive preparation withdrawn through the intestine was detected within 48 hours as a basic inactive metabolite and three less significant inactive metabolites and, in a very small amount, unchanged.

    Pharmacokinetics in special clinical cases

    The pharmacokinetics of docetaxel are independent of age and gender patient.

    At mildly expressed violations of liver function (activity of alanine aminotransferase (ALT) and aspartate aminotransferase (ACT) not more than 1.5 of the upper limit of normal (ULN), coupled with an increase in the activity of alkaline phosphatase (ALP) is not more than 2.5 ULN), total clearance of docetaxel is decreased by 27% compared to the average.

    The clearance of docetaxel did not change in patients with mild or moderate fluid retention. Data on the clearance of the drug in patients with severe fluid retention do not.

    Indications:

    Breast Cancer (BC)

    Adjuvant therapy

    Operational breast cancer (in combination with doxorubicin and cyclophosphamide):

    - operable breast cancer with regional lymph nodes;

    - operable breast cancer without destruction of regional lymph nodes in patients who have shown the chemotherapy according to the established selection criteria for primary chemotherapy early stages of breast cancer [if one or more high risk of recurrence: tumor size of more than 2 cm, a negative status of estrogen and progesterone receptors, high histological degree of tumor malignancy (grade 2 - 3), age less than 35 years].

    Operable breast cancer with tumor overexpression HER2 (doxorubicin and cyclophosphamide with the subsequent use of docetaxel in combination with trastuzumab (scheme AC VT)).

    Metastatic and / or locally advanced breast cancer

    - Locally distributed or metastatic breast cancer (in combination with doxorubicin, 1st line therapy).

    - Metastatic breast cancer with tumor overexpression HER2 (in combination with trastuzumab, first-line therapy).

    - Locally distributed or metastatic breast cancer with ineffectiveness of previous chemotherapy involving anthracyclines (in combination with capecitabine).

    Non-small cell lung cancer

    - Locally distributed or metastatic non-small cell lung cancer with ineffectiveness of previous chemotherapy (docetaxel in monotherapy).

    - Unresectable locally advanced or metastatic non-small cell lung cancer (in combination with cisplatin, in combination with carboplatin represents an alternative treatment option for cisplatin-based therapy, 1st line therapy).

    Ovarian Cancer

    - Metastatic ovarian cancer with ineffectiveness of previous therapy of the 1st line (docetaxel in monotherapy, therapy of the 2nd line).

    Prostate Cancer

    - Metastatic hormone-resistant (androgen-independent) cancer prostate gland (in combination with prednisone or prednisolone).

    Stomach cancer

    - Metastatic stomach cancer, including cancer of the esophageal-gastric junction zone department (in combination with cisplatin and fluorouracil, 1st line therapy).

    Head and neck cancer

    - Locally spread squamous cell carcinoma of the head and neck (in combination with cisplatin and fluorouracil, induction therapy).

    Contraindications:

    - Hypersensitivity to the active substance or any other component of the drug, including polysorbate-80;

    - initial number of neutrophils <1500 / μl;

    - pronounced violations of the liver function;

    - pregnancy and the period of breastfeeding;

    - Children under 18 years.

    Carefully:

    When the liver function is impaired.

    Dosing and Administration:

    To prevent hypersensitivity reactions, and to reduce fluid retention, all patients (except patients with prostate cancer, recommendations for premedication for which see below) in the absence of contraindications prior to docetaxel administration, a glucocorticosteroid premedication, for example, dexamethasone inside at a dose 16 mg / day (8 mg twice daily), for 3 days, starting 1 day before docetaxel administration.

    In patients with prostate cancer receiving concomitant treatment with prednisone or prednisolone, dexamethasone is premedicated at a dose of 8 mg for 12, 3 and 1 hour before the onset of docetaxel administration.

    To reduce the risk of development of hematological complications, preventive administration of granulocyte colony-stimulating factor (G-CSF) is recommended. Docetaxel is administered intravenously drip for 1 hour 1 time per 3 weeks.

    Mammary cancer

    Adjuvant therapy

    With adjuvant therapy of operative breast cancer with regional lymph nodes and operable breast cancer without regional lymph nodes, the recommended dose of docetaxel is 75 mg / m2 1 hour after administration of doxorubicin (50 mg / m2) and cyclophosphamide (500 mg / m2) every three weeks (TAC scheme). A total of 6 cycles (see also "Dose Correction for Chemotherapy").

    With adjuvant therapy of patients with operative breast cancer with tumor overexpression HER2 the following doses of docetaxel are recommended.

    Chemotherapy according to the AC TH

    - AC (cycles 1-4): doxorubicin (A) 60 mg / m2 followed by administration of cyclophosphamide (C) 600 mg / m2 every 3 weeks, 4 cycles.

    - TH (cycles 5-8): docetaxel (T) 100 mg / m2 Once every 3 weeks, 4 cycles and trastuzumab (H), entered weekly according to the following scheme:

    - cycle 5 (starts 3 weeks after the last cycle of the AU):

    day 1: trastuzumab 4 mg / kg (loading dose),

    day 2: docetaxel 100 mg / m2,

    day 8 and 15: trastuzumab 2 mg / kg.

    - cycles 6-8:

    day 1: docetaxel 100 mg / m2 and trastuzumab 2 mg / kg,

    day 8 and 15: trastuzumab 2 mg / kg.

    - Three weeks after day 1 of the cycle, 8: trastuzumab 6 mg / kg every 3 weeks. Trastuzumab is introduced, in total, for 1 year.

    Locally distributed or metastatic breast cancer

    With locally advanced or metastatic breast cancer as first-line therapy docetaxel 75 mg / m2 is administered in combination with doxorubicin 50 mg / m2; as a second-line therapy, the recommended dose of docetaxel in monotherapy is 100 mg / m2.

    When combined with trastuzumab, the recommended dose of docetaxel is 100 mg / m2 every three weeks with a weekly administration of trastuzumab. The initial intravenous infusion of docetaxel is performed the day after the first dose of trastuzumab. Subsequent doses of docetaxel are administered immediately after the end of intravenous infusion of trastuzumab (with good tolerabilityprevious dose of trastuzumab). For information on the doses and route of administration of trastuzumab, see the instructions for the medical use of trastuzumab. When combined with capecitabine, the recommended dose of docetaxel is 75 mg / m2 every 3 weeks, and capecitabine - 1250 mg / m2 inside twice a day (within 30 minutes after eating) for 2 weeks followed by a weekly break. To calculate the dose of capecitabine in accordance with the surface area of ​​the body, see the instructions for the medical use of capecitabine.

    Non-small cell lung cancer

    In patients who have not received previous chemotherapy, the following treatment regimen is recommended: docetaxel 75 mg / m2, immediately following it, the administration of cisplatin 75 mg / m2 for 30-60 minutes or carboplatin (AUC 6 mg / ml / min) for 30-60 minutes. For treatment after ineffectiveness chemotherapy on the basis of platinum preparations, monotherapy with docetaxel at a dose of 75 mg / m is recommended2 1 time in 3 weeks.

    Metastatic ovarian cancer

    For the second-line treatment of ovarian cancer, the recommended dose of docetaxel is 100 mg / m2 every 3 weeks in monotherapy.

    Prostate Cancer

    The recommended dose of docetaxel is 75 mg / m2 1 time in 3 weeks. Prednisone or prednisolone take inside 5 mg twice a day for a long period of the course treatment.

    Stomach cancer

    The recommended dose of docetaxel is 75 mg / m2 in the form of a one-hour intravenous infusion followed by intravenous infusion of cisplatin at a dose of 75 mg / m2 for 1-3 hours (both drugs only on the first day of each cycle of chemotherapy). Upon completion of cisplatin administration, a 24-hour infusion of fluorouracil at a dose of 750 mg / m2/ day for 5 days, starting from the end of the infusion of cisplatin. Treatment is repeated every 3 weeks. Patients should receive premedication with antiemetics and appropriate additional fluid administration (hydration) when cisplatin is administered. To reduce the risk of hematological toxicity (see "Dose Correction for Chemotherapy" below), the introduction of G-CSF is indicated for prophylactic purposes.

    Head and neck cancer

    Patients should receive premedication with antiemetic medications, they should be given appropriate hydration (before and after cisplatin administration). It is necessary to prevent the development of neutropenic infections (preventive use of antibiotics).

    Induction chemotherapy followed by radiotherapy

    For induction therapy with locally disseminated inoperable squamous cell carcinoma of the head and neck, the recommended dose of docetaxel is 75 mg / m2 in the form of a one-hour intravenous infusion with subsequent administration of cisplatin at a dose of 75 mg / m2 for 1 hour (both drugs are administered only on the first day of each cycle of chemotherapy). After this, a continuous intravenous infusion of fluorouracil in a dose of 750 mg / m2/ day for 5 days. This scheme is repeated every three weeks for 4 cycles. After chemotherapy, patients should undergo radiation therapy.

    Induction chemotherapy followed by radiotherapy

    For induction therapy of locally advanced squamous cell carcinoma of the head and neck (technically unresectable, with a low probability of surgical cure or in organ preservation) the recommended dose of docetaxel is 75 mg / m2 in the form of a one-hour intravenous infusion followed by a 0.5-3 hour intravenous infusion cisplatin in a dose of 100 mg / m2 (both drugs are administered only on the first day of each cycle of chemotherapy) and followed by a continuous intravenous infusion of fluorouracil in a dose of 1000 mg / m2/ day from 1 to 4 days.This scheme is repeated every 3 weeks, only 3 cycles. After chemotherapy, patients should undergo radiation therapy. For information on correcting doses of cisplatin and fluorouracil, see the instructions for use of these drugs.

    Correction of doses for chemotherapy

    General recommendations

    Docetaxel should be administered with a neutrophil count in the peripheral blood ≥ 1500 / μl. With a decrease in the number of neutrophils <500 / μL, which was observed for more than a week, or development of febrile neutropenia, or development of severe cutaneous reactions, or severe peripheral neuropathy during docetaxel therapy, the dose of docetaxel for the following administrations should be reduced from 100 mg / m2 up to 75 mg / m2 and / or with 75 mg / m2 up to 60 mg / m2. If similar complications occur with docetaxel at a dose of 60 mg / m2, treatment should be discontinued.

    With combination therapy for breast cancer

    Adjuvant therapy for breast cancer

    Patients with breast cancer receiving adjuvant therapy with docetaxel in combination with doxorubicin and cyclophosphamide (TAC regimen) are recommended for the primary prevention of G-CSF. With the development of febrile neutropenia or neutropenic infection in all subsequent cycles, it is necessary to reduce the dose of docetaxel to 60 mg / m2 and continue to receive G-CSF.In patients with grade 3 or 4 stomatitis, a dose reduction of 60 mg / m2.

    Docetaxel in the chemotherapy scheme AS TH

    With operable breast cancer with tumor overexpression HER2 after an episode of febrile neutropenia or infection with adjuvant therapy according to the AC TH scheme, G-CSF should be used prophylactically for all subsequent cycles, and the dose of docetaxel in AC TH should be reduced from 100 mg / m2 up to 75 mg / m2.

    Since the development of neutropenia in the first cycle of chemotherapy was observed in clinical practice, neutropenic risk and current recommendations should be considered and, if necessary, G-CSF should be used. In case of development of a stomatitis of 3 or 4 severity degree the dose of docetaxel in the AC TH circuit should be reduced from 100 mg / m2 up to 75 mg / m2. To adjust the dose of trastuzumab, see the information in the instructions for use of trastuzumab.

    When combining docetaxel with capecitabine:

    At the first occurrence of toxicity of 2 degrees of severity, which persists until the next cycle of treatment with docetaxel / capecitabine, the next treatment cycle can be postponed until the toxicity is reduced to 0-1 severity, with 100 during the next treatment cycle % the initial dose of docetaxel.

    In patients with a second-degree toxicity re-development or the first development of 3-degree toxicity at any time of the treatment cycle, treatment is postponed until toxicity is reduced to 0-1 severity, then docetaxel treatment is resumed at a dose of 55 mg / m2.

    With any subsequent manifestations of toxicity or the appearance of any type of toxicity of the 4th degree of severity, the administration docetaxel should be discontinued.

    For the correction of the dose of capecitabine when combined with docetaxel, see the instructions for the use of capecitabine.

    When combined treatment of non-small cell lung cancer

    For patients who initially receive docetaxel in a dose of 75 mg / m2 in combination with cisplatin or carboplatin, in which the platelet count in the previous treatment cycle was reduced to 25,000 / μL (with cisplatin) and to 75,000 / μL (with carboplatin), or in patients who developed febrile neutropenia, or in patients with severe manifestations non-hematological toxicity dose of docetaxel in the next cycle should be reduced to 65 mg / m2. For recommendations on correcting the dose of cisplatin and carboplatin,instructions for the use of cisplatin and carboplatin.

    With a combination of docetaxel with cisplatin and fluorouracil (FU) for stomach cancer or head and neck cancer:

    With the development of febrile neutropenia or infection, despite the administration of G-CSF, the dose of docetaxel should be reduced to 60 mg / m2. With the subsequent development of episodes of complicated neutropenia, it is recommended to reduce the dose of docetaxel from 60 mg / m2 up to 45 mg / m2. When developing thrombocytopenia 4 degrees of severity, the dose of docetaxel should be reduced from 75 mg / m2 up to 60 mg / m2. Subsequent cycles using docetaxel are possible with neutrophil counts> 1500 / μL and platelets> 100,000 / μL. If toxicity continues, treatment should be discontinued.

    With the development of other types of toxicity, dose adjustment of docetaxel is carried out in accordance with the recommendations given below.

    Toxicity

    Correction of dose

    Diarrhea 3rd degree

    The first episode: reduce the dose of FU by 20%.

    The second episode: then reduce the dose of docetaxel by 20%.

    Diarrhea of ​​the 4th degree

    The first episode: Reduce the dose of docetaxel and FU by 20%.

    The second episode: stop treatment.

    Stomatitis / mucositis of the 3rd degree

    The first episode: reduce the dose of FU by 20%.

    The second episode: Cancel only the FU for all subsequent cycles.

    Third episode: reduce the dose of docetaxel by 20%.

    Stomatitis / mucositis of the 4th degree

    The first episode: Cancel only the FU for all subsequent cycles.

    The second episode: reduce the dose of docetaxel by 20%.

    For recommendations on correcting doses of cisplatin and FU, see instructions for their use.

    Special patient groups

    Patients with impaired function liver

    In patients with transaminase activity in the blood plasma (ALT and / or ACT), exceeding 1.5 times the level of IGN, or the activity of AP, more than 2.5 times higher than IGN, the recommended dose of docetaxel is 75 mg / m2. In patients with increased bilirubin concentration and / or increased ALT activity and ACT (> 3.5 VGN) in combination with an increase in the activity of AFP more than 6 times that of UGN, docetaxel Not recommended.

    At the moment, there are no data on the use of docetaxel in combination with other drugs in patients with impaired hepatic function.

    Children

    Safety and efficacy of docetaxel in children have not been studied. There is limited experience with docetaxel in children.

    Elderly patients

    Given the analysis of pharmacokinetic data, there are no specific instructions for the use of docetaxel in elderly patients. When combining docetaxel with capecitabine in patients older than 60 years, it is recommended that the starting dose of capecitabine be reduced by 25% (see the instructions for capecitabine).

    Patients with impaired renal function

    Data on the use of docetaxel in patients with severe renal dysfunction are absent.

    Preparation of a solution for infusions

    The required volume of the premixed solution in accordance with the required dose is introduced into the infusion bag or a vial containing 250 ml of a 5% dextrose solution or 0.9% sodium chloride solution. If the required dose of docetaxel is greater than 200 mg, a larger volume of infusion fluid should be used so that the docetaxel concentration is not greater than 0.74 mg / ml.

    Mix the contents of the infusion bag or vial. The pre-mixed docetaxel solution and the infusion solution must be inspected before administration; In the presence of sediment, the solution should be destroyed.

    Contact of undiluted concentrate with equipment or devices covered with polyvinyl chloride (PVC) is not recommended; this allows to reduce the patient's contact with DEHP (di-2-ethylhexyl phthalate), which can be released in packets and devices for infusion, coated with PVC. The diluted docetaxel solution can be stored in glass vials, polypropylene or plastic bags (polypropylene, rololefin) and injected through devices coated with polystyrene.

    Side effects:

    On the part of the hematopoiesis system:

    very often (≥ 10%) - reversible neutropenia (in patients who did not receive G-CSF), in a number of cases accompanied by fever, attachment of infections, and sometimes the development of sepsis and pneumonia. The number of neutrophils is reduced to the minimum values ​​on average after 7 days (in patients who received previous chemotherapy, this period may be shorter), the average duration of severe neutropenia (<500 / μL) is also 7 days;

    often (≥ 1 and <10%) - development of thrombocytopenia (platelet count <100000 / μl); bleeding, combined with thrombocytopenia (platelet count <50000 / μl) and anemia (hemoglobin <11 g / dL), including severe anemia (hemoglobin <8 g / dL).

    From the immune system:

    very often (≥ 10%) - mild or moderately sensitive hypersensitivity reactions usually occur within a few minutes after the onset of infusion (hot flashes, rashes, itching, chest tightness, back pain, dyspnea, drug fever, chills);

    often (≥ 1 and <10%) - possible the development of severe reactions (lowering blood pressure, bronchospasm, generalized rash and erythema), which disappeared after discontinuation of infusion and the appointment of adequate therapy;

    very rarely (<0.01%) - Lyell's syndrome, Stevens-Johnson syndrome.

    From the skin and subcutaneous tissues:

    very often (≥ 10%) - alopecia, mild and moderately expressed skin reactions;

    rarely (≥0.01 and <0.1%) - a pronounced rash accompanied by itching, or limited erythema of the skin of the palms and feet with edema and subsequent desquamation, as well as edema of the hands, face and chest, hypo- or hyperpigmentation of the nails, onycholysis.

    From the side of metabolism:

    very often (≥ 10%) - fluid retention: cases of development of peripheral edema, pleural or pericardial effusion, ascites, weight gain. Peripheral edema usually appears on the lower limbs, and then can become generalized, resulting in an increase in body weight of 3 kg or more.The frequency and severity of fluid retention increases with repeated administration of the drug; the average total docetaxel dose at which fluid retention was observed was 818.9 mg / m3 during premedication2 and 489.7 mg / m2 - without premedication. However, in some cases, swelling occurred during the first course of therapy. The fluid retention was not accompanied by acute episodes of oliguria or arterial hypotension;

    rarely (≥ 0.01 and <0.1%) - In rare cases, it was reported on the development of dehydration and pulmonary edema.

    From the gastrointestinal tract:

    very often (≥ 10%) - nausea, vomiting, diarrhea, anorexia, constipation, stomatitis, taste disorder, esophagitis, epigastric pain; Colitis, including ischemic, enterocolitis, perforation of the stomach or intestines;

    often (≥ 1 and <10%) - for patients receiving monotherapy with docetaxel at a dose of 100 mg / m2, increased activity ACT, ALT, AFP, and serum bilirubin concentrations more than 2.5 times that of UHN are observed in less than 5% of cases;

    infrequently (≥ 0.1 and <1%) - hepatitis (a lethal outcome was observed in patients with liver diseases in the anamnesis);

    rarely (≥0.01 and <0.1%) - Gastrointestinal bleeding, intestinal obstruction.

    From the side of the central nervous system and the peripheral nervous system:

    Often (≥1%) - peripheral neuropathy in the form of easy or moderately expressed paresthesia, hyperesthesia, dysesthesia or pain, including burning. Motor disorders were characterized by muscle weakness. If these symptoms occur, dose adjustment is necessary. If symptoms persist, then treatment should be discontinued;

    very rarely (<0.01%) - convulsions, transient loss of consciousness.

    From the cardiovascular system:

    often (≥ 1 and <10%) - heart rhythm disturbances (sinus tachycardia, atrial fibrillation), unstable angina, heart failure, decreased or increased blood pressure;

    rarely (≥ 0.01 and <0.1%) - venous thromboembolism and myocardial infarction.

    From the respiratory system:

    very rarely (<0.01%) - acute respiratory distress syndrome and interstitial pneumonia, pulmonary fibrosis and increased reaction to irradiation.

    From the musculoskeletal system:

    often (≥ 1 and <10%) - arthralgia, myalgia, muscle weakness.

    From the side of the organ of vision:

    rarely (> 0.01 and <0.1%) - development of lacrimation in combined with conjunctivitis (or without it), transient visual impairment (flashes of light in the eyes, the appearance of cattle), usually occurring during the administration of the drug and combined with development of hypersensitivity reactions, which usually disappear after discontinuation of infusion;

    very rarely (<0.01%), mainly in patients receiving other antitumoral drugs at the same time, the development of occlusion of the lacrimal canal, leading to excessive lacrimation.

    Local reactions:

    often (≥ 1 and <10%) - moderately expressed hyperpigmentation, inflammation, redness, dry skin, phlebitis, hemorrhage, edema of veins.

    Other:

    often (≥ 1 and <10%) - asthenia, dyspnea, generalized or local pain, including chest pain, not related to heart or lung disease.

    When docetaxel is used in combination with doxorubicin In comparison with monotherapy with docetaxel, a high incidence of neutropenia was observed, including severe neutropenia; febrile neutropenia; thrombocytopenia, including severe thrombocytopenia; anemia; infections, including severe infections; nausea; vomiting; diarrhea, including severe diarrhea; constipation; stomatitis, including severe stomatitis; heart failure; alopecia; but a lower incidence of allergic reactions; skin reactions, including severe ones; defeat of nails,including heavy; fluid retention, including heavy; anorexia; neurosensory and neuromotor reactions, including severe forms; lowering blood pressure; heart rhythm disturbances; increased activity of "liver" transaminases, alkaline phosphatase, bilirubin concentration in the blood; myalgia; asthenia.

    When docetaxel is used in combination with doxorubicin and cyclophosphamide (TAC scheme) compared with monotherapy with docetaxel, a lower incidence of neutropenia, severe anemia, febrile neutropenia, infections, allergic reactions,peripheral edema, neurosensory and neuromotor reactions, nail damage, diarrhea, anemia, but there was a high incidence of mild anemia, thrombocytopenia, nausea, vomiting, stomatitis, taste disorders, constipation, asthenia, arthralgia, alopecia. Colitis, enterocolitis, large intestine perforation without lethal outcomes were also observed (two of the four patients required discontinuation of treatment), acute myeloid leukemia / myelodysplastic syndrome. Prophylactic G-CSF reduced incidence of neutropenia (60%) and neutropenic infections 3-4 degrees.

    When docetaxel is used in combinations with capecitabine there was more frequent development of undesirable phenomena from the gastrointestinal tract (stomatitis, diarrhea, vomiting, constipation, abdominal pain, eating disorders); arthralgia; severe thrombocytopenia and anemia; hyperbilirubinemia; palmar-plantar syndrome (hyperemia of the skin of the extremities / palms and feet / with subsequent edema and desquamation); but a more rare development of severe neutropenia; alopecia, disorders of the nails, including onycholysis; asthenia, myalgia, decreased appetite and anorexia. Dyspepsia, dry mouth, sore throat, candidiasis of the mouth, dermatitis, erythematous rash, discoloration of the nails, pyrexia, pain in the extremities, pain, back pain, lethargy (drowsiness, inhibition, stupor), swelling of the lower extremities shortness of breath , cough, nosebleeds, paresthesia, dizziness, headache, peripheral neuropathy, dehydration, lacrimation, weight loss. In patients over the age of 60 who received combination therapy with docetaxel and capecitabine, compared with patients of younger age, there is a more frequent development of toxicity of 3-4 degrees of severity.

    In patients who received combined treatment with trastuzumab, a greater incidence of adverse reactions (nausea, diarrhea, constipation, abdominal pain, taste disorders, febrile neutropenia, arthralgia, anorexia) and a more frequent development of toxicity of 4 degrees of severity compared with monotherapy with docetaxel. There were cases of heart failure, especially when supplementing therapy with anthracyclines (doxorubicin or epirubicin).

    When docetaxel is used according to the scheme AC TH (see the "Application and Dosage" section), the incidence of many side effects increased: alopecia, anemia, including anemia of 3-4 degrees of severity, nausea, including nausea of ​​3-4 degrees of severity, stomatitis, vomiting, diarrhea, constipation were more common , anorexia, abdominal pain, increased activity of ACT, ALT and alkaline phosphatase, myalgia, nail damage, arthralgia, 3-4 grade infections, heart failure. There was no increase in the frequency of neutropenia. Less commonly met neutropenia 3-4 degrees of severity, fluid retention, neurosensory and neuromotor reactions, rash and desquamation, allergic reactions.Insomnia was also observed, an increase in the concentration of creatinine in the blood.

    When docetaxel is used in combination with cisplatin or carboplatin compared with monotherapy with docetaxel, thrombocytopenia appeared more often, including thrombocytopenia of 3-4 degrees of severity (mostly with carboplatin); nausea, including nausea 3-4 degrees of severity; diarrhea 3-4 degrees of severity; anorexia (mostly with cisplatin), including anorexia 3-4 degrees of severity; reaction at the site of administration. Less frequent neutropenia, including neutropenia 3-4 degrees of severity; anemia, including anemia of 3-4 degrees of severity, infections; febrile neutropenia; allergic reactions; skin reactions; defeat of nails; fluid retention, including fluid retention of 3-4 degrees of severity (mostly with carboplatin); stomatitis, neurosensory and, to a lesser extent, neuromotor neuropathy; alopecia and myalgia. Also observed: fever in the absence of infection, including 3-4 degrees of severity; pain.

    When docetaxel is used in combination with prednisolone and prednisone Compared with monotherapy with docetaxel, the incidence of side effects was significantly reduced: anemia, including 3-4 degrees of severity; infections; neutropenia,including those of 3-4 degrees of severity; thrombocytopenia; febrile neutropenia; weakness; allergic reactions; neurosensory and neuromotor reactions; alopecia; rashes; desquamation; nausea, diarrhea; stomatitis; vomiting; anorexia; myalgia; arthralgia; fluid retention; but more often there were taste disorders and heart failure. Also observed: nasal bleeding, cough, shortness of breath, weakness, lacrimation.

    When docetaxel is used in combination with cisplatin and fluorouracil In comparison with monotherapy with docetaxel, anemia was more frequent, including 3-4 degrees of severity; thrombocytopenia, including 3-4 degrees of severity; febrile neutropenia; neutropenic infections (even with the use of G-CSF); nausea, vomiting, anorexia, stomatitis, diarrhea, esophagitis / dysphagia / pain when swallowing; Infection was less common; allergic reactions; fluid retention; neurosensory and neuromotor reactions; myalgia; alopecia, rash, itching; defeat of nails, skin desquamation; disturbance of the rhythm of the heart. Also, fever was observed in the absence of infection; lethargy (drowsiness, confusion, numbness); changes in hearing; dizziness; lacrimation; dry skin; heartburn; myocardial ischemia; underlined venous pattern; cancer pain; decrease in body weight.Prophylactic use of G-CSF reduces the incidence of febrile neutropenia and / or neutropenic infections.

    Data obtained during the application of the drug in the post-registration period

    Benign, malignant and unspecified neoplasms (including cysts and polyps)

    Rarely: acute myeloid leukemia and myelodysplastic syndrome associated with docetaxel, when used in combination with other chemotherapeutic agents and / or irradiation.

    On the part of the hematopoiesis system

    It has been reported that bone marrow hematopoiesis is suppressed and other hematological adverse reactions; development of the syndrome of disseminated intravascular coagulation (DVS-syndrome), often in combination with sepsis or multi-organ failure.

    From the immune system

    Rarely: anaphylactic shock, sometimes fatal. In patients who received premedication, the lethal outcome was very rare.

    From the nervous system

    Rarely: convulsions or transient loss consciousness, sometimes developing during intravenous infusion of the drug.

    From the side of the organ of vision

    Rarely: lacrimation in combination with conjunctivitis (or without it) and in very rare cases with obstruction of the tear duct, leading to its rupture; cases of transient visual disorders ("flashes of light in the eyes," the appearance of cattle), usually occurring during intravenous infusion administration of the drug and combined with the development of hypersensitivity reactions that usually disappeared after the cessation of intravenous infusion. Cases of cystic edema have been reported the macular area.

    From the side of the hearing organ and labyrinthine disorders

    Rarely: cases of ototoxic effect of the drug with hearing impairment and / or hearing loss, including cases associated with other ototoxic drugs.

    From the side of the cardiovascular system

    Rarely: venous thromboembolic complications and myocardial infarction

    On the part of the respiratory system, the organs of the thorax and the mediastinum

    Rarely: acute respiratory distress syndrome, interstitial pneumonia, interstitial lung disease, pulmonary fibrosis, respiratory failure, which could lead to death. With the simultaneous carrying out of irradiation, rare cases of radiation pneumonia.

    From the gastrointestinal tract

    Rarely: dehydration as a consequence development of reactions from the gastrointestinal tract; perforation of the stomach or intestines; colitis, including ischemic; neutropenic enterocolitis; rare cases of ileus (intestinal obstruction) and intestinal obstruction.

    From the liver and biliary tract

    Rarely: hepatitis, sometimes fatal, mainly in patients with concomitant liver disease.

    From the skin and subcutaneous tissues

    Rarely: cutaneous red lupus, bullous rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. It was reported about the development of such scleroderma changes, which preceded the peripheral lymphangiectatic edema. In some cases, the development of these phenomena caused co-infection, simultaneous use of other drugs and accompanying illnesses.

    General disorders and disorders at the site of administration

    Rarely: the phenomenon of the return of the local radiation reaction in the previously irradiated region, pulmonary edema.

    From the side of the kidneys and urinary tract

    Reported deterioration of kidney function and the development of renal failure, in most cases associated with the simultaneous use nephrotoxic drugs.

    From the side of metabolism and nutrition

    There have been reports of the development of cases of hyponatremia, mainly in combination with dehydration, vomiting and pneumonia.

    Overdose:

    Symptoms: suppression of bone marrow function, peripheral neuropathy, inflammation of the mucous membranes.

    Treatment: there is no specific antidote. It shows hospitalization in a specialized department and careful monitoring of the function of vital organs. Assign G-CSF as soon as possible. If necessary, conduct symptomatic therapy.

    Interaction:

    Research in vitro showed that the biotransformation of the drug can change with the simultaneous use of substances inducing or inhibiting cytochrome P450-3A isoenzymes, or metabolized by cytochrome P450-3A isoenzymes such as ciclosporin, terfenadine, ketoconazole, erythromycin and troleandomycin. In this regard, care must be taken with the simultaneous administration of such drugs,taking into account the possibility of pronounced interaction.

    In vitro drugs that bind strongly to proteins, such as erythromycin, diphenhydramine, propranolol, propafenone, phenytoin, salicylate, sulfamethoxazole and valproic acid, do not affect the binding of docetaxel to proteins. Dexamethasone does not affect the degree of binding of docetaxel to plasma proteins. Docetaxel does not affect the binding to the protein digitoxin.

    When docetaxel is used in combination with doxorubicin, the clearance of docetaxel increases while maintaining its effectiveness. At the same time, the clearance of doxorubicin and the concentration of doxorubicinol (doxorubicin metabolite) in plasma do not change.

    Carboplatin clearance in combination therapy with docetaxel is increased by 50% than with carboplatin monotherapy.

    The effects of docetaxel on the pharmacokinetics (CmOh the mean maximum plasma docetaxel concentration, and AUC - the area under the "concentration-time" curve) of the main metabolite of capecitabine (5'-DFUR) and the effect of capecitabine on the pharmacokinetics (Cmax and AUC) docetaxel is not detected.

    Special instructions:

    Treatment with docetaxel should be performed under the supervision of a doctor who has experience of antitumor therapy.

    Neutropenia

    With the development of severe neutropenia (<500 / μL for 7 days or more) during the course of docetaxel therapy, it is recommended to reduce the dose of the drug at subsequent courses or to use adequate symptomatic measures. Continue follow-up treatment docetaxel is possible after the restoration of the number of neutrophils to 1500 / μl. If G-CSF is administered to patients receiving docetaxel in combination with cisplatin and fluorouracil, febrile neutropenia and / or neutropenic infections develop less frequently. Therefore, when this combination is used, the introduction of G-CSF is a preventive goal to reduce the risk of complications of neutropenia (febrile neutropenia, prolonged neutropenia, neutropenic infection). Care should be taken to monitor the condition and laboratory performance of patients receiving this therapeutic regimen. If patients receive primary G-CSF prophylaxis (from the first cycle) with docetaxel in combination with doxorubicin and cyclophosphamide (TAC chemotherapy regimen), febrile neutropenia and / or neutropenic infection develop less frequently.Therefore, with adjuvant therapy for breast cancer according to the TAC scheme, the issue of the preventive administration of G-CSF from the first cycle should be considered in order to reduce the risk of development of complicated neutropenia (febrile neutropenia, prolonged neutropenia, neutropenic infection). Care should be taken to monitor the condition of patients receiving the TAS chemotherapy regimen.

    Hypersensitivity reactions

    To detect reactions of hypersensitivity, patients should be carefully monitored, especially during the first and second infusions. The development of reactions of hypersensitivity is possible during the first minutes of infusion of docetaxel, therefore, when it is administered, it is necessary to have medicines and equipment for the treatment of arterial hypotension and bronchospasm. Light symptoms of hypersensitivity (facial flushing, localized skin reactions) do not require interruption of the drug administration. Despite premedication, patients experienced severe hypersensitivity reactions (lowering blood pressure, bronchospasm, generalized rash, erythema) and very rarely fatal anaphylactic reactions.The appearance of hypersensitivity reactions requires immediate discontinuation of docetaxel administration and appropriate therapy. Re-administration of docetaxel to patients who underwent severe hypersensitivity reactions is not permitted.

    Patients with hepatic insufficiency

    In patients receiving monotherapy with docetaxel at a dose of 100 mg / m2 when the activity of ALT is increased and / or ACT, more than 1.5 times higher than IGN, in combination with increased activity of AFP more than 2.5 times higher than IGN, there is an extremely high risk of developing severe side effects: sepsis, gastrointestinal bleeding, febrile neutropenia, infections, thrombocytopenia, stomatitis, asthenia. In this regard, in such patients, the recommended dose of docetaxel is 75 mg / m2. Functional liver samples should be determined before the start of therapy and before each subsequent cycle of docetaxel therapy. In patients with increased bilirubin concentration and / or increased ALT activity and ACT (> 3.5 VGN) in combination with an increase in activity of AP (> 6 VGN) docetaxel appoint do not recommend.

    Fluid retention

    Patients with severe fluid retention (eg, pleural effusion, pericardial effusion, and ascites) should be closely monitored.When edema appears, there is a restriction on salt intake and drinking regimen and the appointment of diuretics.

    Leukemia

    With combination therapy with docetaxel, doxorubicin and cyclophosphamide, the risk of delayed myelodysplasia and / or myeloid leukemia requires hematological monitoring of patients.

    Heart failure

    In patients who received docetaxel in combination with trastuzumab for metastatic breast cancer with tumor expression HER2, especially after anthracycline-containing therapy (doxorubicin or epirubicin), it is possible to develop heart failure, which can be of medium severity or severe, and lead to death. When a patient is treated with docetaxel in combination with trastuzumab, she should undergo a cardiac examination before starting therapy. Every three months, heart function should be monitored, which will identify patients who may develop heart failure. For more details, see the instructions for use of trastuzumab.

    Disturbances on the part of the organ of sight

    In patients treated with docetaxel, as well as other taxanes,reported the development of cystic edema of the macular area. Patients who have visual impairment should undergo urgent and complete ophthalmological examination. In the case of diagnosing cystic edema of the macular area, docetaxel treatment should be discontinued and the patient should receive appropriate treatment (see the "Side effect" section).

    Elderly patients

    Compared with patients younger than 60 years in patients aged 60 years and older receiving docetaxel in combination with capecitabine, there was an increase in the incidence of treatment-related adverse events of 3 and 4 severity associated with the treatment of serious unwanted adverse reactions (CPD) and early discontinuation of treatment due to development of CPD.

    There are limited data on the use of a combination of docetaxel with doxorubicin and cyclophosphamide in patients older than 70 years.

    There are limited data on the use of a combination of docetaxel with doxorubicin and cyclophosphamide in patients older than 70 years.

    In patients 65 years of age or older who received docetaxel treatment every three weeks for prostate cancer, the incidence of nail changes was ≥ 10% higher,than in younger patients, and in patients 75 years of age and older, the incidence of fever, diarrhea, anorexia and peripheral edema was ≥ 10% higher than in younger patients.

    When using a combination of docetaxel with cisplatin and fluorouracil, the following adverse reactions (all degrees of severity): lethargy (drowsiness, inhibition, stupor), stomatitis, neutropenic infection, in patients older than 65 years were ≥10% more likely than in patients younger. Therefore, patients over 65 years of age who receive this combination need careful monitoring.

    Treatment and precautions for handling the drug

    As with other potentially toxic substances, caution should be exercised when using docetaxel and preparing solutions. It is recommended to use gloves. If you get a concentrate, a premixed solution or a solution for infusions on the skin, immediately wash it with soap and water. If the concentrate, premixed solution or solution for infusion into the mucous membranes comes into contact, immediately rinse with water.

    Control of laboratory indicators

    A systematic control of the peripheral blood pattern is necessary in order to detect myelotoxicity in a timely manner.

    Use in Pediatrics

    The safety and efficacy of docetaxel in children have not been adequately studied. There is limited experience with docetaxel in children.

    Women and men of childbearing age should avoid conception, using reliable methods of contraception, during the use of the drug and at least 3 months after its withdrawal.

    Effect on the ability to drive transp. cf. and fur:

    Special studies were not conducted. However, it is possible to develop adverse reactions from the nervous system, the organ of vision, etc., which can lead to a decrease in the speed of psychomotor reactions and attention. In this regard, it is not recommended to drive vehicles and engage in other potentially hazardous activities during treatment with docetaxel.

    Form release / dosage:

    Concentrate for the preparation of a solution for infusions, 40 mg / ml.

    Packaging:

    0.5 ml or 2.0 ml concentrate in a vial of transparent colorless glass type I with a capacity of 10 ml or 15 ml, sealed with a rubber stopper and covered with an aluminum cap with a blue or red plastic cover.

    1.5 ml or 6.0 ml of solvent in a vial of transparent colorless glass type I with a capacity of 10 ml or 15 ml, sealed with a rubber stopper and covered with an aluminum cap with a blue or red plastic cover.

    1 bottle with concentrate and 1 bottle of solvent in a plastic tray, along with instructions for use in a cardboard bundle.

    Storage conditions:

    Store at a temperature of 2 to 8 ° C.

    The prepared solution can be stored at a temperature of 5 to 25 ° C for 12 hours.

    Keep out of the reach of children!
    Shelf life:

    18 months (concentrate), 36 months (solvent).

    Do not use after expiry date!

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002042
    Date of registration:10.04.2013
    Expiration Date:10.04.2018
    Date of cancellation:2018-04-10
    The owner of the registration certificate:Tolmar, Corp.Tolmar, Corp. Panama
    Manufacturer: & nbsp
    Information update date: & nbsp08.06.2017
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