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Enzymes are involved in mechanism of Capecitabine a prodrug, get converted into 5 fluorouracil in-vivo. After conversion, 5-FU get turned into 5-fluoro-2’ deoxyuridine monophosphate & 5 fluoro uridine triphosphate in both normal & cancer cells.

This converting metabolites causes cancer cell injuries by two distinct ways; At first, FdUMP & the folate co factor, N5-10 methylenetetrahydrofolate, are binding to an enzyme thymidylate synthase which leads to produce a covalently bound ternary complex.

This binding concludes as inhibition of production of thymidylate from 2’ deoxyuridylate. This thymidylate is essential messenger for thymidine triphosphate required for DNA synthesis. Finally the insufficiency of thymidine triphosphate leads to cause obstruction in cell division.

In second way, the nuclear transcriptional enzymes are falsely inserted FUTP instead of uridine triphosphate which is occurred during RNA synthesis, this concluded as metabolic error and leads to intercede with RNA processing and protein synthesis.



Absorption: Readily absorbed. Food decrease rate and extent of absorption. peak plasma concentration is 1.5hr. Distribution: Plasma protein binding: <60%, mainly to albumin. Metabolism: capecitabine hydrolysed in the liver into 5'-deoxy-5-fluorocytidine (5'-DFCR) then to 5'-deoxy-5-fluorouridine (5'-DFUR), and subsequently in body tissues into 5-fluorouracil by thymidine phosphorylase enzyme. Excretion: Via urine (96%, (<3% as unchanged drug) and faeces (<3%). Elimination half-life is 0.75 hr.

Brand : Xeloda
Ingredients : Capecitabine
Strength : 500mg
Manufactured : Roche
Package : 120 Tablets

Dosage and administrations

Xeloda tablets should be administered on an empty stomach, taken within 30 minutes after the meals.

Dosage regimens of Xeloda

The prescribed dose of Xeloda tablets are 1250mg/m2 should be administered orally as two times a day for the period of 2 weeks pursued by a one week rest time given as 3 weeks cycle. In combination of Xeloda with docetaxel, the prescribed dose is 1250mg/m2 of Xeloda as two times day and the dose of docetaxel are 75mg/m2 given as intravenous infusion over the period of 1 hour for every 3 weeks. Premedication should be provided, based on the docetaxel labeling it should be initiated before starting the docetaxel therapy for the patients getting both Xeloda plus docetaxel. The supporting therapy for the Duke’s C colon cancer patients, the prescribed treatment duration period is 6 months. The usual dose of Xeloda 1250mg/m2 should be taken orally for 2 weeks which is follows as one week rest period and the duration of therapy should be continue for 3 weeks cycle as total cycle is 8 (24 weeks). In case of toxicity occurs due to Xeloda therapy, treatment should be interrupt or discontinue. On the other way, dose adjustment should be suggested to reduce the adverse effect related to toxicity. In any drugs that should be combined with Xeloda , must require dose alteration such as Phenytoin, coumarin derivatives are combined with Xeloda tablets, must undergo dosage adjustment. Depending on the toxicity grade of patients therapy should be followed; At first, patients suspected with grade II toxicity at the time of 14 days of Xeloda therapy; the treatment should be postponed. Therapy should be interrupted until grade changed to I; then therapy with Xeloda should be continuing as same dose. Supporting therapy should be provided if possible, in case of toxicity.

Grade II toxicity sustains in case of combinational therapy of Xeloda with docetaxel; interrupts the therapy and toxicity decreases as grade 1 then continue the treatment at 100% original dose of Xeloda . In grade I toxicity: continue the dose of Xeloda

In grade II

1st appearance: Post pone the treatment until resolved to grade I and continue the therapy with 100% dose of Xeloda 2nd appearance: Post pone the treatment until resolved to grade I and continue the therapy with 75% dose of Xeloda 3rd appearance: Post pone the treatment until resolved to grade I and continue the therapy with 50% dose of Xeloda . 4th appearance: stop the treatment of Xeloda

In grade III

1st appearance: Post pone the treatment until resolved to grade I and continue the therapy with 75% dose of Xeloda . 2nd appearance: Post pone the treatment until resolved to grade I and continue the therapy with 50% dose of Xeloda . 3rd appearance: stop the treatment.

In grade IV

1st appearance: stop the treatment or if toxicity resolved to grade I, then resume the therapy with 50% dose of Xeloda . For hepatic damage patients: No dosage adjustment should be recommended. For renal damage patients: In moderate renal damage, the dose of Xeloda reduced to 75% in both monotherapy & combinational therapy with docetaxel By using Cockroft & Gault equation; 140-age of patients x body weight in Kg used to analysis the kidney function to obtain creatinine clearance value.

The Xeloda caused side effects

Stomatitis, diarrhea, vomiting, abdominal pain, nausea, dyspepsia, hand and foot syndrome, alopecia, rashes, Erythema, fatigue, pyrexia, asthenia, dizziness, headache, eye disorders, conjunctivitis, neutropenia, Epistaxis, elevated ALAT, increased in calcium levels, anemia, decreased platelets, weakness, edema, chest pain

Safety precautions

Cardio toxicity: monitor cardiac toxicity like myocardial infarction, ischemic conditions, or any other cardiac problems during the therapy with Xeloda . Hand foot syndrome: the dose of Xeloda should be reduced to reduce the toxicity. Dihydropyrimidine dehydrogenase insufficiency: adverse reactions related to 5-FU is contributed to this deficiency. Liver insufficiency: mild or moderate liver damage patients administered Xeloda carefully and monitor the adverse effects. Hematological problems: check the blood cell counts regularly before or after the treatment

Embryo fetal toxicity

Xeloda causes fetal harm, which may causes death. Pregnancy: Xeloda is contraindicated; produce carcinogenesis, mutagenesis, and fertility impairments. Diarrhea: anti-diarrheal therapy should be provided.


During the co administration of Xeloda with warfarin, the anti-coagulant response rate should be monitored frequently. This combination may cause severe bleeding effect which leads to death also. By increasing the prothrombin time & INR values, bleeding may occur. This event may appear within several days & also several months after initiation of therapy. In some cases after stopping the therapy of Xeloda , may occurs


drug interaction

Interaction of Xeloda with anti-coagulant: altered coagulation problem and bleeding occurs to control this adverse effect; monitored the prothrombin time frequently Interaction of Xeloda with phenytoin: level of phenytoin should be monitored for reducing the toxicity of phenytoin Interaction of Leucovorin with Xeloda : 5-FU concentration should be increased and toxicity elevated by Leucovorin. Hence leads to death due to diarrhea, enterocolitis, and dehydration in elder patients While concomitant with Xeloda tablets with CYP2C9 substrates: care should be taken Interaction of Food drug occurs in Xeloda tablets, food may interfere with absorption of Xeloda . Reduce the rate and duration of absorption of Xeloda occurs. Xeloda should be taken within 30minutes after meal


Hypersensitivity reaction produce due to patients may contraindicate to component present in Xeloda . Xeloda is contraindicate to the patient who are having hypersensitive to 5-FU Patient who are having insufficient known enzyme like Dihydropyrimidine dehydrogenase are contraindicated to Xeloda . Xeloda is also contraindicating to severe renal damage patients with creatinine clearance less than 30ml/min.

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