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Paclitaxel
It is administered as infusion. After infusion it undergoes intensive P450-mediated hepatic metabolism. The clearance of Paclitaxel is saturable and decreases with increasing dose or dose rate.
Indication
& Dosage
Metastatic ovarian and breast cancer
Dosage: Adults: 175mg per square metre by i.v. inf. over 3 hrs. Repeat
every week 3 weeks. Pretreat with conticosteroids.
Children: Not recommended.
Naturally occurring antineoplastic agent that promotes the assembly of microtubules from tubulin dimers and stabilizes microtubules by preventing depolymerization. The stabilization results in the inhibition of the normal dynamic reorganization of the microtubule network that is required for vital interphase and mitotic cellular functions. Also induces abnormal “bundles” of microtubules throughout the cell cycle and multiple esters of microtubules during mitosis. Following IV administration, there is a biphasic decline in plasma levels. The initial rapid decline is due to distribution to the peripheral compartment and significant elimination, whereas the second phase is due, in part, to a slow efflux of the drug from the peripheral compartment. Metabolized by the liver with small amounts of unchanged drug excreted in the urine.
Cisplatin / More profound myelosuppression when paclitaxel was
given after cisplatin than when paclitaxel was given before cisplatin,
due to a 1/3 decrease in paclitaxel clearance
Levels of doxorubicin and doxorubicinol
Adverse
Effect & Precautions
Bone marrow depression,
hypersensitivity reactions, myalgia, chest pain, bradycardia, a
stocking-glove sensory neuropathy, mucositis, nausea, vomiting,
diarrhoea, alopecia. Altered liver function tests.
Precaution: Safety and efficacy in children has not been established.
Monitor haematological functions. The drug should be administered under
supervision of a physician experienced in use of cancer chemotherapy
Pregnancy: Use with caution
Breast Feeding: Discontinue nursing
Man: Use with caution