Capecitabine
Indications
Capecitabine is used for:
Breast cancer, Colorectal cancer, Gastric cancer, Oesophageal cancer
Adult Dose
Oral
Breast cancer; 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.
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.
Child Dose
Renal Dose
Renal impairment:
CrCl (ml/min)
51-80 No adjustment needed.
30-50 Reduce dose to 950 mg/m2 bid when starting dose is 1.25 g/m2 bid. No dose adjustment is needed when starting dose is 1 g/m2.
<30 Avoid use.
Administration
Swallow with water within 30 min after a meal
Contra Indications
History of severe and unexpected reactions to fluoropyrimidine therapy; severe renal impairment; pregnancy, lactation. Hypersensitivity.
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.
Pregnancy-Lactation
Pregnancy Category: C
Lactation: excretion in milk unknown; use with caution
Interactions
Antacids containing aluminum and magnesium, leucovorin, anticoagulants, phenytoin, allopurinol.
Adverse Effects
Side effects of Capecitabine :
10%
Diarrhea, Nausea, Anemia, Lymphopenia, Hand and foot syndrome, Edema, Fatigue, Fever, Headache, Pain, Paresthesia, Alopecia, Dermatitis, Abdominal pain, Anorexia, Appetite decreased, Constipation, Dyspepsia, Stomatitis, Vomiting, Neutropenia, Thrombocytopenia, Dyspnea, Bilirubin increased, Eye irritation
1-10%
Chest pain, Dermatitis, Pruritus, Rash, Dizziness, Headache, Weakness, Dehydration, Dry mouth, Dyspepsia, Taste disturbance, Back pain
Potentially Fatal: Cardiotoxicity, bone-marrow depression and hyperbilirubinaemia.
Mechanism of Action
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.