Paclitaxel testosterone propionate 100mg is an anticancer drug of natural origin, obtained from the plant by a semisynthetic yew (Taxus Baccata). The mechanism of action is associated with the ability of the drug to stimulate the “assembly” of microtubules from tubulin dimer molecules, stabilize their structure and inhibit the dynamic reorganization in interphase, which violates the mitotic cell function.
Dozozawisimo suppresses bone marrow hematopoiesis. Mutagenic and embryotoxic properties, causes a decrease in reproductive function.
Following intravenous administration of paclitaxel observed a biphasic decline in plasma concentrations of the drug. It is 2170 ng / ml when administered intravenously over 3 hours in a dose of 135 mg / m maximum drug concentration in plasma. By increasing the injected dose at 30% (175 mg / m 2 ), the maximum plasma concentration of the drug is increased by 75%. Repeated infusions are not accumulates. Relationship to plasma proteins – 89-98%. Receiving cimetidine, ranitidine, dexamethasone, diphenhydramine does not affect the binding of paclitaxel to plasma proteins. The volume of distribution amounts to 198-688 l / m 2 . Easily it penetrates tissue accumulates primarily in the liver, spleen, pancreas, stomach, intestine, heart muscle.
It is metabolized in the liver by hydroxylation, with the participation of cytochrome P450 isoenzymes CYP2D8 (with the formation of a metabolite – 6-alpha-gidroksipaklitaksel) and CYP3CA4 (with the formation of metabolites 3-para-gidroksipaklitaksel and 6-alpha, 3-p-digidroksipaklitaksel).
The half-life and the total clearance of paclitaxel are variable and depend on the dose and duration of intravenous: 13-52 hr and 12-23 l / h / m 2 , respectively.After intravenous infusion (1-24 hours) the total excretion by the kidneys is 1,3-12,6% of the dose. Write mainly in the bile – 90%.
Indications for use
- Ovarian cancer testosterone propionate 100mg (first-line therapy in combination with platinum drugs) and second-line therapy for metastases after standard therapy has not yielded positive results.
- Breast cancer (as first- and second-line as well as adjuvant treatment).
- Non-small cell lung cancer (first-line therapy of patients who have not planned surgery and / or radiation therapy (in combination with cisplatin)).
- Kaposi’s sarcoma in patients with AIDS (second-line therapy after failure of treatment with liposomal anthracyclines).
Contraindications for use
- Children’s age (safety and efficacy not established).
- Increased sensitivity to paclitaxel and other drugs, dosage form which includes polyoxyethylated castor oil.
- Pregnancy and lactation.
- Original content neutrophil count less than 1.5 x 10 9 / L in patients with solid tumors.
- Original (or registered in the course of treatment), the neutrophil content of less than 1.0 x 10 9 / L in patients with Kaposi’s sarcoma in patients with AIDS.
Precautions for the use of
used with caution in patients with depression of bone marrow hematopoiesis (including after chemotherapy or radiation therapy), hepatic failure, acute infectious diseases (including herpes zoster, chickenpox, herpes), severe coronary artery disease heart, myocardial infarction (in history), arrhythmias.
Pregnancy and lactation
Controlled trials of paclitaxel in pregnant women have been conducted. Animal studies have shown embryotoxic, teratogenic and mutagenic effects of paclitaxel. Therefore, pregnant women should not use paclitaxel.
It is not known whether paclitaxel penetrates into breast milk, so to avoid the toxic effect of the drug on the baby during the period of treatment should stop breastfeeding.
Dosing and Administration
Paclitaxel can be used both as a monotherapy and in combination with other anticancer drugs. The dose and dosage regimen of the preparation is adjusted individually.
In order to prevent severe hypersensitivity reactions in all patients premedication should be conducted with the use of corticosteroids, antihistamines, and H2 receptor antagonists. Recommended premedication regimen – 20 mg dexamethasone (or its equivalent) into approximately 12 and 6 hours before injection-Paclitaxel Ebewe 50 mg diphenhydramine (or its equivalent) intravenously and cimetidine 300 mg or ranitidine 50 mg testosterone propionate 100mg intravenously 30-60 minutes prior to Paclitaxel injection-Ebewe.
First-line chemotherapy of ovarian cancer
is recommended a combination regimen with paclitaxel and cisplatin.
Paclitaxel is administered at a dose of 175 mg / m 2 body surface within a three-hour intravenous infusion, or at a dose of 135 mg / m 2 body surface area over a 24-hour intravenous infusion, and then introduced cisplatin 75 mg / m 2 body surface. Intervals between courses – 3 weeks.
Second-line chemotherapy of ovarian cancer
Paclitaxel is recommended to be administered at a dose of 175 mg / m 2 body surface area by three-hour intravenous infusion. Intervals between courses – 3 weeks.
Adjuvant chemotherapy for breast cancer
Paclitaxel was administered after chemotherapy with anthracyclines and cyclophosphamide. Paclitaxel recommended dose of 175 mg / m 2 body surface intravenously over three hours. 4-year intervals between courses – 3 weeks.
Chemotherapy is the first breast cancer cell line
in the case of combined use of doxorubicin (50 mg / m 2 body surface area), paclitaxel must be administered 24 hours after doxorubicin. The recommended dose of paclitaxel – 220 mg / m 2 body surface area three hours when administered by intravenous infusion. Intervals between courses – 3 weeks.
In the case of combined use with trastuzumab, paclitaxel recommended dose of 175 mg / m 2 body surface area by intravenous infusion with a three-hour week intervals between courses. Paclitaxel may be administered on the day after the first dose of trastuzumab or immediately after the administration of subsequent doses of trastuzumab if previous dose testosterone propionate 100mg was well tolerated.
Second-line chemotherapy of breast cancer
Paclitaxel recommended dose of 175 mg / m 2 body surface by three-hour intravenous infusion. Intervals between courses – 3 weeks.
Chemotherapy of advanced non-small cell lung cancer
is recommended combination regimen of paclitaxel and cisplatin. Paclitaxel is administered at a dose of 175 mg / m 2 body surface area by intravenous infusion three hours, after which the cisplatin is administered at a dose of 80 mg / m 2 body surface. Intervals between courses – 3 weeks.
Chemotherapy Kaposi’s sarcoma on the background of AIDS.
Paclitaxel is recommended to be administered at a dose of 100 mg / m 2 body surface area by three-hour intravenous infusion. Intervals between courses – 2 weeks.
Subsequent doses of paclitaxel determined individually, depending on tolerability. The next dose of paclitaxel can be administered only after the increase in the neutrophil count to a level of> 1500 cells / mm3 (> 1000 cells / mm 3 in the case of Kaposi’s sarcoma), and platelets – to a level> 100,000 cells / mm 3 (> 75,000 cells / mm 3 in case of Kaposi’s sarcoma). Patients who have had a severe neutropenia (neutrophil count less than 500 cells / mm 3 for 7 days or longer) or severe peripheral neuropathy, the following dose is reduced by 20% (25% in the case of Kaposi’s sarcoma).
Treatment of patients with impaired hepatic function. At present, there are insufficient data to make recommendations for dose adjustment in patients with impaired hepatic function or mild to moderate severity. Patients with severely impaired liver function should not be prescribed paclitaxel. One of the most common clen steroid is muscle cramps as the medication depletes taurine and many already have electrolyte deficits.