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Capecitabine information from DrugsUpdate  

See Available Brands of Capecitabine in India

P - Contraindicated in pregnancy
L - Contraindicated in lactation
LI - Lab*

Capecitabine is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers. Capecitabine is a prodrug, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5'-deoxy-5-fluorocytidine (5'-DFCR) and 5'-deoxy-5-fluorouridine (5'-DFUR), to form 5-fluorouracil.

Pharmacodynamics

Pharmacokinetics

Capecitabine is a prodrug that is converted to fluorouracil following oral administration, which in turn inhibits thymidylate synthetase, blocking the methylation of deoxyuridylic acid to thymidylic acid, interfering with DNA, and to a lesser degree, RNA synthesis.

Capecitabine Indications / Capecitabine Uses

Information Not Available

Capecitabine Adverse Reactions / Capecitabine Side Effects

Diarrhoea, nausea and vomiting, stomatitis, palmar-plantar syndrome, dermatitis. Fatigue, mucosal inflammation, pyrexia, asthenia and lethargy; headache, dizziness and insomnia; lower limb oedema, anorexia, dehydration.
Potentially Fatal: Cardiotoxicity, bone-marrow depression and hyperbilirubinaemia.

Precautions

Warnings
Warfarin
Altered coagulation parameters and/or bleeding, including death, have been reported in patients taking capecitabine concomitantly with coumarin-derivative anticoagulants. Increases in INR have occurred within several days to several months after initiating capecitabine and, in some cases, within 1 mo after stopping capecitabine. Risk factors include 60 yr of age and older and cancer diagnosis. Monitor INR or PT frequently; be prepared to adjust anticoagulant dose accordingly.

Renal Function
Patients with moderate renal function impairment at baseline require dosage modification. Carefully monitor patients with mild or moderate renal function impairment for adverse reactions.

Hepatic Function
Carefully monitor patients with mild to moderate hepatic function impairment caused by liver metastases.

Cardiac effects
Cardiotoxicity has been associated with fluorinated pyrimidine therapy.

Contraception

Ensure women of childbearing potential use effective contraception before initiating therapy and for duration of treatment.

Diarrhoea
Capecitabine can induce diarrhea, sometimes severe. If grade 2, 3, or 4 diarrhea occurs, immediately interrupt administration until the diarrhea resolves or decreases in intensity to grade 1. Following grade 3 or 4 diarrhea, decrease subsequent doses of capecitabine. Monitor patient for development of diarrhea. Consider use of antidiarrheal therapy (eg, loperamide) and be prepared to administer fluid and electrolyte replacement if severe.

DPD
Rarely, unexpected, severe toxicity (eg, diarrhea, neurotoxicity, neutropenia, stomatitis) associated with 5-FU has been attributed to a deficiency of DPD activity.

Hand-and-foot syndrome
If grade 2 or 3 hand-and-foot syndrome occurs, interrupt administration of capecitabine until the event resolves or decreases in intensity to grade 1. Following grade 3 hand-and-foot syndrome, decrease subsequent doses of capecitabine. Monitor patient for development of hand-and-foot syndrome (eg, discomfort of the hands and feet, numbness, redness, swelling), nausea, stomatitis, and vomiting. Inform health care provider if noted.

Hematologic
Grade 3 or 4 neutropenia, thrombocytopenia, or decreases in Hgb occur more frequently when capecitabine is used in combination with docetaxel.

Hyperbilirubinemia
If grade 2 to 4 elevations in bilirubin occur, immediately interrupt administration until the hyperbilirubinemia resolves or decreases in intensity to grade 1.

Overdosage

Symptoms
Bone marrow depression, diarrhea, GI irritation and bleeding, nausea, vomiting.

Special Precautions

Hepatic dysfunction, bone marrow suppression, poor nutritional status, warfarin therapy. Child, elderly, prior extensive pelvic radiation or alkylating therapy. Moderate renal impairment; CBC with differential; monitor hepatic and renal function. Discontinue use if intractable diarrhoea, stomatitis, bone marrow suppression or MI develops.

Other Drug Interactions

Antacids containing aluminum and magnesium, leucovorin, anticoagulants, phenytoin, allopurinol.

Other Interactions

Food Interactions: Food reduces rate and absorption. Admin within 30 min after a meal.

Dosage

Oral
Breast cancer
Adult: 1.25 g/m2 bid for 2 wk followed by a 1 wk rest period; therapy to be given in 3-wk cycles. Recommended treatment duration for colorectal cancer: 6 mth. May be used in combination with docetaxel at 75 mg/m2, given as a 1-hr IV infusion once every 3 wk for the treatment of breast cancer.

Oral
Colorectal cancer
Adult: 1.25 g/m2 bid for 2 wk followed by a 1 wk rest period; therapy to be given in 3-wk cycles. Recommended treatment duration for colorectal cancer: 6 mth. May be used in combination with docetaxel at 75 mg/m2, given as a 1-hr IV infusion once every 3 wk for the treatment of breast cancer.
 
Oral
Gastric cancer
Adult: Used in combination with a platinum-based compound, 1 g/m2 bid for 14 days, followed by a 7-day rest period. 1st dose is given on the evening of day 1 and the last dose on the morning of day 15.

Food(before/after)

Should be taken with food. (Take within ½ hr after meals.)

List of Contraindications

Capecitabine and Pregnancy

Contraindicated in pregnancy.
Category D: There is positive evidence of human foetal 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).


 

Capecitabine and Lactation

Contraindicated in lactation

Capecitabine and Children

Information Not Available

Capecitabine and Geriatic

Information Not Available

Capecitabine and Other Contraindications

History of severe and unexpected reactions to fluoropyrimidine therapy; severe renal impairment; pregnancy, lactation. Hypersensitivity.

Storage

Oral: Store at 25°C

Lab interference

Oral: Store at 25°C

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