HENTAXEL (Docetaxel)Solution for Injection 20 mg/0.5mL vial and 80mg/2mL vial
Each 0.5 mL contains Docetaxel 20mg
Each 2 mL contains Docetaxel 80mg
It is indicated for the treatment of patients with advanced or metastatic breast cancers after failure of prior chemotherapy including anticancer agents of anthracene ring. It is indicated for the treatment of patients with advanced or metastatic non-small cell lung cancer after administration of cisplatin-based therapy.
Dosage and Administration
Docetaxel is for intravenous infusion. All patients should be premedicated with oral corticosteroids such as dexamethasone 16 mg per day for 3 days starting 1 day prior to docetaxel administration in order to prevent allergic reaction and fluid retention.
Withdraw corresponding diluent of Docetaxel into appropriate solution before use. Shake gently and mix well. Allow the vial to stand at room temperature for 5 minutes. Check whether the solution is clear. Then according to dosage, withdraw mixed solution to a syringe and inject into an infusion bag or bottle of 5% Dextrose solution or 0.9 sodium chloride solutions. The recommended dose for Docetaxel is 75mg/m2 administered in an hour every 3 weeks or 21 days.
It is an antineoplastic agent belonging to paclitaxel family. It acts by disrupting the microtubular network in cells. Such action is essential for mitotic and interphase cellular functions. Docetaxel binds to free tubulin thereby resulting in the formation of stable microtubules and subsequently into microtubule bundles without normal function. This leads to the inhibition of mitosis in cells. Docetaxel's binding to microtubules does not alter the number of protofilaments in the bound microtubules, a characteristic not found in most spindle poisons currently in clinical use.
Docetaxel for injection has been shown to be clastogenic in the in vitro chromosome aberration test in CHO-K1 cells and in the in vivo micronucleus test in the mouse, but it did not induce mutagenicity in the Ames test or the CHO/HGPRT gene mutation assays.
Drug InteractionsReproductive Toxicity
In vitro drug interaction studies revealed that CYP3A4 inhibitors may affect the metabolism of docetaxel, so it should be cautiously co-administrated with this kind of agents, such as ketoconazole, erythromycin, troleandomycin, and nifedipine.
In case of overdosage, the patient should be kept in a specialized unit where vital functions can be closely monitored. There is no known antidote for docetaxel for injection overdosage. Anticipated complications of overdosage include: bone marrow suppression, peripheral neurotoxicity, and mucositis.
Product is stable for two years
Store between 2oC and 8oC
Foods, Drugs and Cosmetics Act prohibits dispensing without prescription.
Docetaxel for injection produces no impairment of fertility in rats when administered at the dose of 0.3mg/kg (about 1/50 the recommended human dose on a mg/m2 basis), but decreased testicular weights were reported. This correlates with the finding of 10-cycle toxicity study (dosing once every 21 days for 6 months) in rats and dogs in which testicular atrophy or degeneration was observed at doses of 5mg/kg in rats and 0.375mg/kg in dogs (about 1/3 and 1/15 the recommended dose on a mg/m2 basis). An increased frequency of dosing in rats produced similar effects at lower dose levels.
Docetaxel for injection can cause fetal harm when administered to pregnant women. Studies in both rats and rabbits at doses > 0.3 and 0.03 mg/kg/day, respectively (about 1/50 and 1/300 the daily maximum recommended human dose on an mg/m2 basis), administered during the period of organogenesis, have shown that docetaxel for injection is embryotoxic and fetotoxic (characterized by intrauterine mortality, increased resorption, reduced fetal weight, and fetal ossification delay). Above dosages may cause maternal toxicity. There are no adequate and well-controlled studies in pregnant women using docetaxel for injection. If docetaxel for injection is used during pregnancy, or if the patient becomes pregnant while receiving this drug, the patient should be apprised of the potential hazard to the fetus or potential risk for loss of the pregnancy. Women of childbearing potential should be advised to avoid becoming pregnant during therapy with docetaxel.
It is not known whether docetaxel is excreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants from docetaxel for injection, mothers should discontinue nursing prior to taking the drug.
The pharmacokinetics of docetaxel have been evaluated in cancer patients after administration of 20-115 mg/m2 in phase I studies. The area under the curve (AUC) was dose proportional following doses of 70-115 mg/m2 with infusion times of 1 to 2 hours. Docetaxel's pharmacokinetic profile is consistent with a three-compartment pharmacokinetic model, with half-lives for the α, β, and γ phases of 4 min, 36 min, and 666 min., respectively. The initial rapid decline represents distribution to the peripheral compartments and the late (terminal) phase is due, in part, to a relatively slow efflux of docetaxel from the peripheral compartment. Intravenous infusion of docetaxel at dose of 100mg/m2 within 1 hour, mean peak concentration is 3.7µg/ml and AUC is 4.6µg/ml·h. Mean values for total body clearance and steady state volume of distribution were 21 L/h/m2 and 113 L, respectively. Docetaxel and its metabolites are eliminated in the urine and feces, 75% and 6%, respectively. Only little amount is excreted in original drug. In vitro studies showed that docetaxel is about 94% to 97% protein bound. Dexamethasone does not affect the protein binding of docetaxel. In vitro studies revealed that docetaxel is metabolized by the CYP3A4 isoenzyme, and its metabolism is inhibited by CYP3A4 inhibitors.
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