Xeloda500 mg

Xeloda 500 mg is a nucleoside metabolic inhibitor with antineoplastic activity indicated for: Adjuvant Colon Cancer: Patients with Dukes'C colon cancer. Metastatic Colorectal Cancer: First-line as monotherapy when treatment with fluoropyrimidine therapy alone is preferred. ... Read moreXeloda 500 mg is a nucleoside metabolic inhibitor with antineoplastic activity indicated for: Adjuvant Colon Cancer: Patients with Dukes'C colon cancer. Metastatic Colorectal Cancer: First-line as monotherapy when treatment with fluoropyrimidine therapy alone is preferred. Metastatic Breast Cancer: In combination with docetaxel after failure of prior anthracycline containing therapy. As monotherapy in patients resistant to both paclitaxel and an anthracycline-containing regimen.

Cytotoxic Chemotherapy

Xeloda 500 mg is a prodrug of fluorouracil, a pyrimidine antimetabolite, which is metabolised into 5-fluoro-2′-deoxyuridine-5′monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP covalently binds to thymidylate synthase, inhibiting the formation of thymidilate, thus interfering with DNA synthesis. Additionally, FUTP interferes with RNA synthesis.

In case of stage-III colon cancer and locally advanced or metastatic breast cancer: 1.25 gm/m2 twice daily for 14 days, followed by a 7-day interval, given as 3-week cycles for a total 8 cycles .For metastatic colorectal cancer, in combination therapy it is administered as 0.8-1 gm/m2 twice daily for 14 days repeated after 7 days interval.

Monotherapy: 1250 mg/m2 twice daily orally for 2 weeks followed by a one-week rest period in 3-week cyclesAdjuvant treatment: Is recommended for a total of 6 months (8 cycles)In combination with docetaxel: The recommended dose of Xeloda 500 mg is 1250 mg/m2 twice daily for 2 weeks followed by a 7-day rest period, combined with docetaxel at 75 mg/m2 as a 1-hour IV infusion every 3 weeks. Xeloda 500 mg dosage may need to be individualized to optimize patient management. Xeloda 500 mg dosage has to be reduced by 25% in patients with moderate renal impairment.Example: A person whose body weight is 64 kg and height is 1.64 m has a body surface area of 1.7 m2 and should take 4 tablets of 500 mg and 1 tablet of 150 mg two times daily.The tablets should be taken in morning and evening as prescribed by doctor. The tablets should be taken within 30 minutes after the end of a meal (breakfast and dinner) and swallowed whole with water. Tablets should not be cut or crushed. Xeloda 500 mg should only be prescribed by a doctor experienced in the use of anticancer medicines.

Anticoagulants: Anticoagulant response (INR or prothrombin time) should be monitored frequently in order to adjust the anticoagulant dose as needed. Phenytoin: Phenytoin levels should be monitored in patients taking Xeloda 500 mg concomitantly with phenytoin. The phenytoin dose may need to be reduced. Leucovorin: The concentration of 5-fluorouracil is increased and its toxicity may be enhanced by leucovorin. CYP2C9 substrates: Care should be exercised when Xeloda 500 mg is co-administered with CYP2C9 substrates. Food: Reduced both the rate and extent of absorption of Xeloda 500 mg.

Severe Renal Impairment Hypersensitivity leucopenia, neutropenia or thrombocytopenia Severe reactions to fluoropyrimidine therapy Complete DPD deficiency Pregnant or breast-feeding

Abdominal pain, Rash, dry or itchy skin, Tiredness, loss of appetite (anorexia), Diarrhea, Vomiting, Nausea, Stomatitis, Hand-and-foot skin-reaction, Fever, Infection, Chest pain, Steven-Johnson syndrome

Pregnancy Category D. There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Coagulopathy: Anticoagulant response should be monitored (e.g. INR) and anticoagulant dose must be adjusted accordingly. Otherwise may result in bleeding, death.Diarrhea: Xeloda 500 mg treatment should be stopped immediately until diarrhea resolves or decreases to grade 1. Standard antidiarrheal treatments recommended. Otherwise may get severe.Cardiotoxicity: Common in patients with a prior history of coronary artery disease.Increased Risk of Severe or Fatal Adverse Reactions in Patients with Low or Absent Dihydropyrimidine Dehydrogenase (DPD) Activity: Xeloda 500 mg should be withhold or permanently discontinued in patients with evidence of acute early-onset or unusually severe toxicity, which may indicate near complete or total absence of DPD activity.Dehydration and Renal Failure: Xeloda 500 mg treatment should be stopped until dehydration is corrected. Potential risk of acute renal failure secondary to dehydration.Mucocutaneous and Dermatologic Toxicity: Severe mucocutaneous reactions, Steven-Johnson Syndrome. (SJS) and Toxic Epidermal Necrolysis (TEN), have been reported. Xeloda 500 mg should be permanently discontinued in patients who experience a severe mucocutaneous reaction during treatment. Xeloda 500 mg may induce hand-and-foot syndrome. Xeloda 500 mg treatment should be interrupted until the hand-and-foot syndrome event resolves or decreases in intensity.Hyperbilirubinemia: Xeloda 500 mg treatment should be interrupted immediately until the hyperbilirubinemia resolves or decreases in intensity.Hematologic: Patients should not be treated with neutrophil counts <1.5x109/L or thrombocyte counts <100x109/L.

The manifestations of acute overdose include nausea, vomiting, diarrhea, mucositis, gastrointestinal irritation and bleeding, and bone marrow depression. Medical management of overdose should include customary therapeutic and supportive medical interventions aimed at correcting the presenting clinical manifestations and preventing their possible complications.

Keep in a dry place and store below 30°C. Protect from light and keep out of the reach of children.

Cytotoxic Chemotherapy

Xeloda 500 mg is a preparation of Xeloda 500 mg, an orally-administered chemotherapeutic agent used in the treatment of cancers. Xeloda 500 mg is a prodrug, that is enzymatically converted to fluorouracil (antimetabolite) in the tumour, where it inhibits DNA synthesis and slows growth of tumour tissue.Xeloda 500 mg is a prodrug that is selectively tumour-activated to its cytotoxic moiety, fluorouracil, by thymidine phosphorylase, an enzyme found in higher concentrations in many tumours compared to normal tissues or plasma. Fluorouracil is further metabolized to two active metabolites, 5-fluoro-2'-deoxyuridine 5-monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP), within normal and tumour cells. These metabolites cause cell injury by two different mechanisms. First, FdUMP and the folate cofactor, N5-10 methylenetetrahydrofolate, bind to thymidylate synthase (TS) to form a covalently bound ternary complex. This binding inhibits the formation of thymidylate from 2-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, therefore a deficiency of this compound can inhibit cell division. Secondly, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis through the production of fraudulent RNA.

Pregnancy category D. Xeloda 500 mg can cause fetal harm. Women are advised of the potential risk to the fetus. It is not known whether Xeloda 500 mg is excreted in human breast milk.No studies have been conducted to assess the impact of Xeloda 500 mg on milk production or its presence in human breast milk. As the potential for harm to the nursing infant is unknown, breast-feeding should be discontinued while receiving treatment with Xeloda 500 mg and for 2 weeks after the final dose.