Buy Taxol solution concentrate 6 mg/ml 16.7 ml (100 mg) bottles 1 pc.
  • Buy Taxol solution concentrate 6 mg/ml 16.7 ml (100 mg) bottles 1 pc.

Paclitaxel

Corden Pharma Latina S.p.A
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2019-09-19
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Clinical Pharmacology

Antitumor drug obtained by biosynthetic. The mechanism of action is associated with the ability to stimulate the “assembly” of microtubules from dimeric tubulin molecules, stabilize their structure by suppressing depolymerization and inhibit dynamic reorganization in the interphase, which disrupts the cell's mitotic function.

In addition, paclitaxel induces the formation of anomalous clusters or "bundles" of microtubules during the cell cycle and causes the formation of multiple microtubule stars during mitosis.

Causes dose-dependent suppression of bone marrow hematopoiesis.

Experimental studies have shown that paclitaxel has mutagenic and embryotoxic properties, causing a decrease in reproductive function.

Pharmacokinetics

The pharmacokinetics of paclitaxel were studied after iv infusion of the drug at doses of 135 mg / m.2 and 175 mg / m2 for 3 and 24 hours

Distribution

After iv administration, the concentration of paclitaxel in the blood plasma decreases in accordance with the two-phase kinetics.

Medium Vd ranges from 198 to 688 l / m2.

The pharmacokinetics of paclitaxel with increasing doses become nonlinear. With an increase in the dose of the drug by 30% (from 135 mg / m2 up to 175 mg / m2) C valuesmax and AUC0-∞ increased by 75% and 81% respectively.

With repeated courses of therapy, there was no indication of the cumulation of paclitaxel.

Protein binding averages 89%.

Metabolism

In vitro studies have shown that paclitaxel is metabolized in the liver with the participation of the CYP2C8 isoenzyme to form the metabolite 6-alpha-hydroxypaclitaxel and with the participation of the isoenzyme CYP3A4 with the formation of the metabolites 3-para-hydroxypaclitaxel and 6-alpha, 3-para-dihydroxypaclitaxel.

Removal

T1/2 and the total clearance of paclitaxel is variable, depends on the dose and duration of administration and is 13-52.7 h and 12.2-23.8 l / h / m2 respectively.

From 1.3% to 12.6% of the administered dose (15-275 mg / m2 in the form of a 1-, 6- or 24-hour infusion) of the drug is excreted in the urine unchanged, which indicates the presence of intensive extrarenal clearance.

Pharmacokinetics in special clinical situations

The effect of impaired renal function on the metabolism of paclitaxel has not been studied. Dialysis does not affect the rate of excretion of the drug from the body.

Indications

Ovarian cancer:

  • 1 line therapy in combination with cisplatin in patients with a common metastatic process or residual tumor (more than 1 cm) after the initial laparotomy;
  • 2 line therapy in patients with advanced metastatic ovarian cancer after standard therapy, which did not lead to a positive result.

Mammary cancer:

  • adjuvant therapy in patients with metastases in the lymph nodes after standard combined treatment;
  • therapy of metastatic cancer 1 line and with the progression of the disease after adjuvant therapy with the use of anthracycline drugs;
  • 2 line therapy for disease progression after combination chemotherapy with anthracycline anti-tumor antibiotics in the absence of contraindications for their use;
  • adjuvant therapy for the treatment of patients after treatment with anthracycline drugs and cyclophosphamide;
  • 1 line therapy of metastatic breast cancer in combination with trastuzumab in patients with a level of 3+ HER-2 expression according to immunohistochemistry and in the presence of contraindications to therapy with anthracycline drugs.

Non-small cell lung cancer:

  • as a line 1 therapy in combination with cisplatin or for monotherapy of non-small cell lung cancer in patients who are not planned to undergo surgical treatment and / or radiation therapy.

Kaposi's sarcoma in AIDS patients:

  • as a 2 line therapy.

Composition

1 ml (1 bottle) contains:

Active substances: paclitaxel 6 mg (100 mg).

Excipients: macrogol glyceryl ricinoleate (Cremofor® EL), ethanol, nitrogen.

Paclitaxel is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Taxol Corden Pharma Latina S.p.A Italy solution concentrate
Syndexel C.K.Sindan-Pharma Romania solution concentrate
Paclitaxel-Lance Lance farm Russia solution concentrate
Paclitaxel-Ebeve Ebeve Pharma Austria solution concentrate
Paclitaxel-Teva Teva Israel solution concentrate

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Paclitaxel

Dosage and Administration

To prevent severe hypersensitivity reactions before administration of the drug Taxol, premedication should be carried out using GCS, histamine H blockers.1-receptors and histamine H blockers2-receptors. Example a dose of 50 mg IV and cimetidine at a dose of 300 mg or ranitidine at a dose of 50 mg IV in 30-60 minutes before the administration of the drug Taxol.

Ovarian cancer

1 line therapy: the recommended dose of Taxol is 175 mg / m2 as an intravenous infusion for 3 hours or 135 mg / m2 in the form of intravenous infusion over 24 hours followed by the administration of cisplatin at a dose of 75 mg / m2; The interval between courses of treatment should be 3 weeks.

Therapy 2 lines: in monotherapy mode, the dose of the drug Taxol is 175 mg / m2 as an intravenous infusion for 3 hours every 3 weeks.

Mammary cancer

Adjuvant therapy is carried out after standard combination therapy. Taxol dose is 175 mg / m2 as an intravenous infusion for 3 hours. A total of 4 courses of therapy are recommended with an interval of 3 weeks.

1 line therapy

In monotherapy mode: the dose of the drug Taxol is 175 mg / m2 as an intravenous infusion for 3 hours every 3 weeks.

In combination therapy mode:

  • In combination with trastuzumab, the recommended dose of Taxol is 175 mg / m2 as an intravenous infusion for 3 hours every 3 weeks. It is possible to start using Taxol the next day, after administration of the first dose of trastuzumab or, with good endurance, on the day of using trastuzumab.
  • In combination with doxorubicin (50 mg / m) Taxol is prescribed at a dose of 220 mg / m2 as an intravenous infusion for 3 hours every 3 weeks. Taxol should be started 24 hours after doxorubicin.

2 line therapy

For the treatment of patients with disseminated disease after combination chemotherapy, which did not give a positive result -175 mg / m2 as an intravenous infusion for 3 hours every 3 weeks.

Non-small cell lung cancer

  • In the combination therapy regimen, the recommended dose of Taxol is 175 mg / m2 as an intravenous infusion for 3 hours or 135 mg / m2 as an intravenous infusion over 24 hours followed by cisplatin, the interval between courses is 3 weeks;
  • in monotherapy mode, the recommended dose of Taxol is from 175 mg / m2 up to 225 mg / m2 as an intravenous infusion for 3 hours every 3 weeks.

Kaposi's sarcoma in AIDS patients

2 line therapy The recommended dose of Taxol is 135 mg / m2 in the form of intravenous infusion for 3 hours every 3 weeks or 100 mg / m2 IV drip for 3 hours every 2 weeks.

Depending on the immunosuppression observed in patients with a developing form of AIDS, it is recommended:

  1. reduce the dose of dexamethasone for oral administration (one of the three components of the premedication) to 10 mg;
  2. enter Taxol only with a neutrophil count of at least 1000 / μl;
  3. in patients with severe neutropenia (less than 500 / mcl for a week or more) in subsequent courses, reduce the dose of the drug Taxol by 20%;
  4. according to clinical indications, simultaneously apply G-CSF.

Terms of preparation of the solution for infusion

Before administration, the concentrate is diluted to a concentration of 0.3-1.2 mg / ml with 0.9% sodium chloride solution, 5% dextrose solution, 5% dextrose solution in 0.9% sodium chloride solution or 5% dextrose solution in Ringer's solution.

Taxol should be introduced through a system with an integrated membrane filter with a pore size of not more than 0.22 microns.

The prepared solutions can opalesce due to the presence of the base carrier in the composition of the dosage form, and after filtering the opalescence of the solution is preserved.

In the preparation, storage and administration of the drug Taxol should use equipment that does not contain parts of polyvinyl chloride.

Adverse reactions

When using the combination of the drug Taxol with platinum preparations, there were no significant clinical changes in the safety profile of the drug, compared with its use in the form of monotherapy.

In patients with Kaposi's sarcoma, which has developed on the background of AIDS, hemorrhage depression, infections (including opportunistic infections) and febrile neutropenia occur more often and are more severe. In these patients, a lower dose of the drug and maintenance therapy is required.

Determination of the frequency of side effects:

  • very often (≥1 / 10);
  • often (≥1 / 100, <1/10);
  • sometimes (≥1 / 1000, <1/100);
  • rarely (≥1 / 10,000, <1/1000);
  • very rarely (<1/10 000).

From the hemopoietic system: very often - myelosuppression, neutropenia, anemia, thrombocytopenia, leukopenia, fever, bleeding; rarely febrile neutropenia; very rarely - acute myeloid leukemia, myelodysplastic syndrome. Neutropenia (90%), depending less on the dose of the drug and more on the duration of the infusion; severe neutropenia (less than 500 / μl) is more often observed with 24-hour infusions than with 3-hour infusions in about half of the patients, while at 1/3 it is accompanied by an increase in temperature; development of infectious complications (30%); in 1% of patients with diagnoses of sepsis, pneumonia, peritonitis, death was registered. Thrombocytopenia (20%) with a platelet count of less than 100,000 / μl; severe thrombocytopenia with a minimum platelet count below 50,000 / μl (7%); anemia (78%); severe anemia with hemoglobin of less than 8 g / dl (16%). The frequency and severity of anemia depended on the initial hemoglobin content and did not depend on the dose and regimen of administration of the drug Taxol.

Allergic reactions: very often - minor manifestations, mainly in the form of a sensation of heat ("hot flashes"), skin rash; sometimes - pronounced hypersensitivity reactions (decrease in blood pressure, angioedema, tachycardia, impaired respiratory function, generalized urticaria), back pain, chills; rarely - anaphylactic reactions (including fatal); very rarely - anaphylactic shock.

Since the cardiovascular system: very often - changes in ECG, lowering blood pressure; often - bradycardia; sometimes - cardiomyopathy, asymptomatic ventricular tachycardia, tachycardia with bigeminia, AV - blockade and syncope, myocardial infarction, increased blood pressure, thrombosis, thrombophleitis; very rarely - atrial fibrillation, supraventricular tachycardia, shock.

On the part of the respiratory system: rarely - shortness of breath, pleural effusion, respiratory failure, interstitial pneumonia, pulmonary fibrosis, pulmonary embolism; very rarely - cough. More frequent development of radiation pneumonitis was noted in patients simultaneously undergoing radiation therapy.

From the side of the central nervous system and peripheral nervous system: very often, peripheral sensory neuropathy; rarely, motor neuropathy (limb weakness); very rarely - autonomic neuropathy, manifested by paralytic intestinal obstruction and orthostatic hypotension, seizures such as grand mal, convulsions, encephalopathy, dizziness, headache, ataxia.

From the musculoskeletal system: very often - arthralgia, myalgia.

On the part of the digestive system: very often - nausea, vomiting, diarrhea, mucositis; often - a significant increase in the level of AST, alkaline phosphatase; sometimes a significant increase in bilirubin; rarely - intestinal obstruction, intestinal perforation, ischemic colitis, pancreatitis; very rarely - mesenteric artery thrombosis, pseudomembranous colitis, esophagitis, constipation, ascites, fatal hepatonecrosis, fatal hepatic encephalopathy.

From the urinary system: in patients with Kaposi's sarcoma and AIDS, cases of renal dysfunction with reversible increases in serum creatinine have been described.

Dermatological reactions: very often - alopecia; rarely - itching, rash, erythema, fibrosis, very rarely - Stevens-Johnson syndrome, epidermal necrolysis, exudative erythema multiforme, exfoliative dermatitis, urticaria, onycholysis.

Local reactions: often - pain, swelling, erythema, induration and pigmentation of the skin at the injection site, rarely - phlebitis, peeling of the skin; extravasation may cause inflammation and necrosis of the subcutaneous tissue.

Other: anorexia, confusion, asthenia and general malaise.

Carefully: the drug should be used for thrombocytopenia (less than 100,000 / mcl), liver failure, acute infectious diseases (including shingles, chicken pox, herpes), severe IHD, myocardial infarction (in history), and arrhythmias.

Drug interactions

Cisplatin reduces the total clearance of paclitaxel by 33% (more pronounced myelosuppression is observed when paclitaxel is administered after cisplatin).

When using Taxol in combination with doxorubicin, it is possible to increase the concentration of doxorubicin (and its active metabolite, doxorubicinol) in the blood plasma. With the administration of the drug Taxol (infusion for 24 hours), before the administration of doxorubicin (infusion for 48 hours), more pronounced neutropenia and cases of stomatitis were observed. However, with jet administration of doxorubicin and administration of the drug Taxol for 3 hours, there were no changes in the nature of the toxic effects associated with the sequence of administration of the drugs.

Simultaneous use with cimetidine, ranitidine, dexamethasone or diphenhydramine does not affect the binding of paclitaxel to plasma proteins.

The metabolism of paclitaxel is catalyzed by CYP2C8 and CYP3A4 isoenzymes, therefore caution is required when using Taxol against the background of treatment with substrates, inducers (for example, rifampicin, carbamazepine, phenobarbital, phenytoin, efavirenz, nevirapine) or inhibitors (for example, erythromycinics, or inhibitors (for example, erythromycinics, or inhibitors (erythromycin), or inhibitors (erythromycin, phenytoin, efavirenz, nevirapine) or inhibitors (erythromycin) CYP2C8 and CYP3A4.

In vitro inhibitors of microsomal oxidation (including ketoconazole, verapamil, diazepam, quinidine, cyclosporine) in concentrations exceeding when used in therapeutic doses in vivo, as well as testosterone, 17α-ethinyl estradiol, retinoic acid and quercetin inhibit the metabolism of paclitaxel.

Macrogol glyceryl ricinoleate, which is a part of the preparation Taxol, can cause extraction of DEHP [di- (2-ethylhexyl) phthalate] from plasticized PVC containers, and the degree of leaching of DEHP increases with increasing solution concentration and with time.

Pregnancy and Lactation

Taxol is contraindicated for use during pregnancy and lactation (breastfeeding).

Patients of childbearing age during treatment with Taxol and for at least 3 months after the end of therapy should use reliable methods of contraception.

Special instructions

Treatment with Taxol should be carried out by a physician with experience in working with anticancer chemotherapy drugs.

When using Taxol in combination with cisplatin, Taxol should be administered first and then cisplatin. During treatment, it is necessary to regularly monitor the picture of peripheral blood, blood pressure, heart rate and the number of breaths (especially during the first hour of infusion), ECG monitoring (and before the start of treatment).

In the case of the development of severe hypersensitivity reactions, the injection of the drug Taxol should be immediately stopped and symptomatic treatment should be started, and it should not be reintroduced.

In cases of development of AV conduction disorders, with repeated administrations, continuous cardiomonitoring should be performed.

Taxol is a cytotoxic substance, which requires careful handling, use gloves and avoid contact with skin or mucous membranes, which in such cases should be thoroughly washed with soap and water, or (eyes) with plenty of water.

Use in Pediatrics

Safety and efficacy of the drug Taxol® in children have not been established.

Impact on the ability to drive vehicles and other mechanisms that require high concentration of attention

During the period of treatment, patients should refrain from practicing potentially hazardous activities that require increased concentration and psychomotor speed.

Overdosage

Symptoms: bone marrow aplasia, peripheral neuropathy, mucositis.

Treatment: conduct symptomatic therapy. The specific antidote for paclitaxel is unknown.

  • Brand name: Taxol
  • Active ingredient: Paclitaxel
  • Dosage form: Concentrate for solution for infusion.
  • Manufacturer: Corden Pharma Latina S.p.A
  • Country of Origin: Italy

Studies and clinical trials of Paclitaxel (Click to expand)

  1. A case of primary refractory Hodgkin's disease treated successfully with paclitaxel
  2. Effectiveness of cisplatin, paclitaxel, and suramin against human malignant mesothelioma xenografts in athymic nude mice
  3. Role of salvage chemotherapy with topotecan and cisplatin in patients with paclitaxel- and platinum-resistant recurrent ovarian or primary peritoneal cancer: A phase II pilot study
  4. Paclitaxel-induced radiation recall dermatitis
  5. Ocular toxicity secondary to paclitaxel in two lung cancer patients
  6. Paclitaxel: An effective antineoplastic agent in the treatment of xenotransplanted hepatoblastoma
  7. Dramatic response of adult Wilms tumor to paclitaxel and cisplatin
  8. Protective effect of liposome encapsulation on paclitaxel developmental toxicity in the rat
  9. Paclitaxel-induced apoptosis in human gastric carcinoma cell lines
  10. In vitro concurrent paclitaxel and radiation of four vulvar squamous cell carcinoma cell lines
  11. Is paclitaxel and cisplatin a cost-effective first-line therapy for advanced ovarian carcinoma?
  12. Phase I study of escalating doses of mitoxantrone and paclitaxel with granulocyte-macrophage colony stimulating factor support
  13. Paclitaxel, carboplatin, and extended schedule etoposide in the treatment of small cell lung carcinoma
  14. CA 125: A valid marker in ovarian carcinoma patients treated with paclitaxel?
  15. Skin ulceration potential of paclitaxel in a mouse skin model in vivo
  16. Phase II study of paclitaxel in patients with previously treated osteosarcoma and its variants
  17. p53 mutations do not predict response to paclitaxel/radiation for nonsmall cell lung carcinoma
  18. Pharmacoeconomic profile of paclitaxel as a first-line treatment for patients with advanced ovarian carcinoma: A lifetime cost-effectiveness analysis
  19. Phase II study of patients with metastatic nonsmall cell carcinoma of the lung treated with paclitaxel by 3-hour infusion
  20. Development of two radioimmunoassays to detect paclitaxel in sera and in cerebrospinal, ascitic, and pleural fluids
  21. Differential activity of cremophor EL and paclitaxel in patients' tumor cells and human carcinoma cell lines in vitro
  22. Erythropoietin reduces anemia and transfusions after chemotherapy with paclitaxel and carboplatin
  23. A Phase I report of paclitaxel dose escalation combined with a fixed dose of carboplatin in the treatment of head and neck carcinoma
  24. Pharmacoeconomic profile of paclitaxel as a first-line treatment for patients with advanced ovarian carcinoma : A lifetime cost-effectiveness analysis

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