Indications |
Intravenous Ovarian carcinoma Adult: Primary treatment (in combination with cisplatin or carboplatin): 135 mg/m2 infused over 24 hr followed by cisplatin and repeated at 3 wk intervals. Secondary treatment (as single agent): 135 or 175 mg/m2 infused over 3 hr once every 3 wk. Hepatic impairment: Do not use in severe impairment, increased risk of hepatotoxicity. For detailed dosing recommendations, consult local protocol. Intravenous Breast cancer Adult: Adjuvant therapy; 2nd line monotherapy or 1st line treatment with trastuzumab: 175 mg/m2 infused over 3 hr once every 3 wk for 4 courses; when used with trastuzumab, dose should be given the day after the 1st dose of trastuzumab or immediately after subsequent doses if well-tolerated. 1st line with doxorubicin: 220 mg/m2 over 3 hr every 3 wk, dose to be administered 24 hr after doxorubicin. Hepatic impairment: Do not use in severe impairment, increased risk of hepatotoxicity. For detailed dosing recommendation, consult local protocol. Intravenous Advanced non-small cell lung cancer Adult: 135 mg/m2 over 24 hr or 175 mg/m2 over 3 hr, followed by cisplatin and repeated at 3 wk intervals. Hepatic impairment: Do not use in severe impairment, increased risk of hepatotoxicity. For detailed dosing recommendation, consult local protocol. Intravenous AIDS-related Kaposi's sarcoma Adult: 135 mg/m2 over 3 hr every 3 wk. Alternatively, 100 mg/m2 over 3 hr every 2 wk especially in patients with poor performance status. Hepatic impairment: Do not use in severe impairment, increased risk of hepatotoxicity. For detailed dosing recommendation, consult local protocol. Reconstitution: Paclitaxel must be diluted before infusion. It can be diluted in 0.9% sodium chloride inj, 5% dextrose inj, 5% dextrose and 0.9% sodium chloride inj or 5% dextrose in lactated Ringer's inj to a concentration of 0.3-1.2 mg/ml. Incompatibility: Do not prepare, store or administer in PVC containing equipment; macrogol glycerol ricinolate (an excipient) can cause [di-(2-ethylhexyl)phthalate] (DEHP) leaching. Y-site incompatibility: Amphotericin B, amphotericin B cholesteryl sulfate complex, chlorpromazine, doxorubicin liposome, hydroxyzine, methylprednisolone sodium succinate, mitoxantrone. Variable compatibility when admixed with cisplatin. |
Contraindications |
History of hypersensitivity (especially macrogol glycerol ricinolate). Patients with baseline neutropenia of <1500 cells/mm3 (<1000 cells/mm3 for kaposi's sarcoma). Pregnancy and lactation. In kaposi's sarcoma, contraindicated in patients with concurrent, serious, uncontrolled infections. |
Warnings / Precautions |
Bone marrow suppression during therapy. Monitor cardiac function if conduction abnormalities result. Premedicaton (with corticosteroid, antihistamine and histamine H2-receptor antagonist) may be required to reduce risk of hypersensitivity reaction. Discontinue, if severe reactions e.g. hypotension, dyspnoea, angioedema or urticaria occur. Caution in patients with moderate hepatic impairment. Monitor for reactions of admin. Safety and efficacy in paediatric patients have not been established. Administer before platinum derivatives (cisplatin, carboplatin) if used in combination. Hazardous agent; use appropriate precautions for handling and disposal. |
Adverse Reactions |
Neutropenia, leukopenia, thrombocytopenia, anaemia, bleeding; hypersensitivity reactions (dyspnoea, flushing, chest pain, tachycardia, rash, hypotension, hypertension); bradycardia, abnormal ECG; neurotoxicity (mainly peripheral neuropathy), myalgia, arthralgia; nausea, vomiting, diarrhoea; severe mucositis, alopecia; rarely hepatic necrosis and encephalopathy, inj site reactions e.g. erythema, tenderness, skin discolouration, swelling; interstitial pneumonitis; infections (mainly UTIs and upper respiratory tract); mucosal inflammation, severe elevation in LFTs (aspartate aminotransferase and alkaline phosphatase). Potentially Fatal: Infections and infestations leading to death e.g. pneumonia and peritonitis. |
Overdose Reactions |
Complications: bone marrow suppression, peripheral neurotoxicity and mucositis. There is no known antidote. Treatment is symptom specific and supportive. |
Drug Interactions |
Myelosuppression was more profound when given after cisplatin than with the alternate sequence (e.g., paclitaxel before cisplatin). CYP2C8 inducers e.g. carbamazepine, phenobarbital, phenytoin, rifampicin, rifapentine, and secobarbital may reduce levels or effects. CYP2C8 inhibitors e.g. gemfibrozil, ketoconazole, montelukast, and ritonavir may increase levels or effects. CYP3A4 inducers e.g. aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins may decrease the levels or effects. CYP3A4 inhibitors e.g. azole antifungals, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, telithromycin, and verapamil may increase levels or effects. May increase anthracycline (eg doxorubicin, epirubicin) levels or toxicity; admin of anthracycline at least 24 hr prior to paclitaxel may reduce interaction. May decrease the absorption of cardiac glycosides (may only affect digoxin tablets); levels should be monitored. See Below for More paclitaxel Drug Interactions |
Food Interactions |
Avoid black cohosh, dong quai in estrogen-dependent tumours. Valerian and St John's wort may decrease paclitaxel levels. Kava kava and gotu kola may increase CNS depression. |
Mechanism of Actions |
Paclitaxel promotes microtubule formation by enhancing the action of tubulin dimers, stabilising existing microtubules and preventing their disassembly, thereby disrupting normal cell division in the late G2 mitotic phase of the cell cycle. This results in the inhibition of cell replication. Distribution: Extensive extravascular distribution and/or tissue binding. Volume of distribution affected by dose and duration of infusion. Protein binding: 89-98%. Metabolism: Hepatic via CYP2C8 and 3A4; 6α-hydroxypaclitaxel is the main metabolite. Excretion: For 1-6 hr infusion; mean β half-life: 6.4 hr. For 3 hr infusion: mean terminal half-life: 13.1-20.2 hr. For 24 hr infusion: mean terminal half life:15.7-52.7 hr. 70% excreted via faeces, 14% excreted via urine. Mean total body clearance after 1 hr and 6 hr infusions: 5.8-16.3 l/hr/m2; after 24 hr infusions: 14.2-17.2 l/hr/m2. |
Storage Conditions |
Intravenous: Store at <25°C and protect from light. Once diluted, chemically and physically stable for 24 hr at 25°C (solutions in glucose 5% in water and normal saline are stable for 3 days at 25°C). Do not refrigerate or freeze diluted solution. Once opened, should be used as soon as possible due to risk of microbial contamination, however can be stored for a max of 28 days at 25°C. |
ATC Classification |
L01CD01 - paclitaxel ; Belongs to the class of plant alkaloids and other natural products, taxanes. Used in the treatment of cancer. |
Storage |
Intravenous: Store at <25°C and protect from light. Once diluted, chemically and physically stable for 24 hr at 25°C (solutions in glucose 5% in water and normal saline are stable for 3 days at 25°C). Do not refrigerate or freeze diluted solution. Once opened, should be used as soon as possible due to risk of microbial contamination, however can be stored for a max of 28 days at 25°C. |
Available As |
|
Paclitaxel
Post Review about Paclitaxel Click here to cancel reply.
Paclitaxel Containing Brands
Paclitaxel is used in following diseases
Drug - Drug Interactions of Paclitaxel
Latest News
- FDA approves Ruconest for treatment of hereditary angioedema
- FDA recommend against aspirin to prevent First Heart Attacks
- FDA approves Pomalyst (pomalidomide) for advanced multiple myeloma
- FDA approves three new drug treatments for type 2 diabetes
- Long-term consequences of vaginal delivery on the pelvic floor
No comments yet.