Colorectal cancer Adjuvant treatment in Duke’s colon cancer First line therapy in colon-rectal cancer metastasis Breast cancer In metastatic breast cancer: used in combination with docetaxel after failure of anthracycline containing chemotherapy
Xeloda - (fluoropyrimidine carbamate) with anti-tumor activity Xeloda is a prodrug of 5’-deoxy-5-fluorouridine (5’-DFUR) which is changed to 5 fluoro uracil Xeloda is generally administered orally Xeloda is also have anti-metabolite activity
Xeloda reaches the peak plasma level at about 1.5 hours Food decreased both the rate and duration of absorption of Xeloda with mean Cmax and AUC0-∞ reduced by 60% and 35% respectively.
The human plasma protein bound to Xeloda is occurs in less than 60%
Bio-activation and metabolism:
Xeloda is largely metabolized to 5-FU enzymatically. In liver, 60 kDa carboxylesterase hydrolyses to 5’-deoxy-5-fluorocytidine. An enzyme Cytidine deaminase which converts 5’-DFCR to 5’-DFUR. Another an enzyme Thymidine phosphorylase is also that involved in the conversion of 5’-DFUR to 5-FU active drug
The route of elimination of Xeloda is occurred through urine 95.5% The mean terminal half life period of Xeloda is 0.75 hour
First line therapy of patients with advanced colorectal cancer:
The usual dose of Xeloda is 1250mg/m2 should be taken orally as twice daily (morning and evening dose 2500mg/m2); therapy continue for 2 weeks followed by 1 week rest period given as 3 weeks cycle
Adjuvant therapy for Duke’s colon cancer:
The usual dose of Xeloda is 1250mg/m2 orally as twice daily (morning and evening dose 2500mg/m2); for 2 weeks followed by 1 week given as 3 weeks for total 8 cycles (24 weeks)
Recommended dose: 1250mg/m2 should be taken as orally for twice daily. In combination with docetaxel; 1250mg/m2 of Xeloda with 75mg/m2 of docetaxel for 3 weeks After a meal within 30 minutes Xeloda should be administered
The safety and efficacy of the Xeloda tablets in pediatric patients has not been established
Xeloda is a prodrug, it is metabolizes to 5-FU. In both non-cancer and cancer cells, 5-FU is metabolized in to 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP)
These two metabolites causes injury to the tumor cells by two major ways :
• FdUMP and the folate cofactor (N5-10-methylenetetrahydrofolate), which binds to thymidylate synthase (TS) to form covalently bound ternary complex.
• This binding prohibits the production of thymidylate from 2’-deaxyuridylate
• Thymidylate an important messenger of thymidylate triphosphate.
• It is essential for DNA synthesis, therefore insufficiency of this compound leads to inhibit cell division
• Nuclear transcriptional enzymes can falsely inserted FUTP alternative to uridine triphosphate during RNA synthesis. This metabolic failure can hinder with RNA conversion and protein synthesis via assembly of counterfeit RNA
Anticoagulant: Xeloda concomitant with warfarin and phenprocoumon, bleeding occurs. These events occurred within several days and even a month also Phenytoin: combination of phenytoin and Xeloda, toxicity related to elevation of phenytoin levels Leucovorin: the toxicity and concentration of 5-FU increased by Leucovorin. In elderly patients, phenytoin and Leucovorin is administered weekly which may cause; diarrhea, dehydration, enterocolitis which may causes death. CYP2C9 substrate: other than warfarin, there is no drug interaction occurs while concomitant with CYP2C9 substrates Care should be taken while combination of Xeloda with CYP2C9 substrates Drug-food interaction: In case of administering Xeloda with food, it leads to reduce the rate and duration of absorption of Xeloda. Xeloda tablets should be administered within 30 minutes after food
Coagulopathy: concomitant with warfarin, anti-coagulant response should be monitored Diarrhea: patients with severe diarrhea should be monitored Cardio toxicity: while taking Xeloda, cardio toxicity occurs like; myocardial infarction, angina, dyshythmias, cardiac arrest sudden death, Cardiomyopathy, Dihydropyrimidine dehydrogenase deficiency, Dehydration and renal failure, Embryo fetal toxicity, Mucocutaneous and dermatologic toxicity, Hyperbilirubinaemia, Hematological problems, Care should be taken while using in geriatric patients, Hepatic insufficiency.
Diarrhea, nausea, anemia, Lymphopenia, head and foot syndrome, edema, fatigue, fever, headache, pain, paresthesia, alopecia, dermatitis, abdominal pain, anorexia, loss of appetite, constipation, dyspepsia, stomatitis, vomiting, neutropenia, thrombocytopenia, dyspnea, bilirubin decreased, eye irritation Post marketing reports: Toxic leukoencephalopathy
Xeloda should be stored at 200C to 250 F(680F to 770F)
The patient missed to take a single dose of Xeloda, should consult with medical oncologist and follow the suggestions
Do not self medicate. Or missed dose should be swapped and continue the regular dosing schedule Do not double the dose
Xeloda is contraindicated to renal impairment patients Xeloda is contraindicated in patients with hypersensitivity to Xeloda or other components
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