II. Indications
- Adjuvant Chemotherapy (FDA approved)
- Colorectal Cancer (including metastatic cancer)
- Metastatic Breast Cancer
- Off-Label Use (non-FDA approved)
- Gastrointestinal Cancer (Gastric Cancer, Esophageal Cancer, Pancreatic Cancer, Hepatobiliary cancer, Anal Cancer)
- Gynecologic Cancer (Ovarian Cancer, Fallopian tube cancer, peritoneal cancer)
- Neuroendocrine Tumors
III. Contraindications
- Creatinine Clearance <30 ml/min
IV. Mechanism
- Antimetabolite Chemotherapy (Antineoplastic Agent)
- Fluoropyrimidine Carbamate, acts as a prodrug
- Selectively activated by tumor cells to 5-Fluorouracil (5-FU)
-
5-Fluorouracil (5-FU) is further metabolized by normal cells and tumor cells to 2 active agents
- 5-fluoro-2-deoxyuridine monophosphate (FdUMP)
- Decreases thymidine synthesis
- Inhibits DNA synthesis and cell division
- 5-fluorouridine triphosphate (FUTP)
- Competes with Uridine Triphosphate for incorporation into RNA
- Inhibits RNA and Protein synthesis
- 5-fluoro-2-deoxyuridine monophosphate (FdUMP)
V. Dosing
- See other references for disease specific dosing protocols
VI. Adverse Effects
- Cardiovascular (cardiac toxicity, esp in Overdose)
- Endo
- Impaired future fertility
- Gastrointestinal
- Mucositis
- Severe Diarrhea
- Hyperbilirubinemia
- Typhlitis (RLQ Pain in neutropenic patients)
- Hematologic
- Myelosuppression (peaks at 1 week after dose)
- Neuro
- Headache
- Palmar-Plantar erythrodysesthesia (sensory Neuropathy)
- Encephalopathy
- Skin
- Acral swelling and erythema (hand and foot syndrome)
- Alopecia
VII. Pharmacokinetics
- Oral Bioavailability: 40 to 60%
- Peak serum concentration: 2 hours
- Catabolized by dihydropyrimidine dehydrogenase (DPD) into inactive metabolite
- Variable metabolism in DPD deficiency
- Inactive metabolite excreted in the urine
VIII. Safety
- Avoid in Pregnancy (any trimester)
- Use reliable Contraception
- Avoid in Lactation
- Monitoring
IX. Drug Interactions
- Capecitabine increases level of other drugs
-
Antacids
- Increase Capecitabine levels
-
Allopurinol
- Avoid with Capecitabine
X. Management: Toxicity or Overdose
- Evaluation
- Complete Blood Count (repeated several days after dose)
- Comprehensive metabolic panel
- Consider serum Troponin
- Electrocardiogram (EKG)
- Acute ingestion
- Consider Activated Charcoal
- Indicated if <1 hour after ingestion and intact mentation
- Consider Uridine Triacetate 10 g
- Indicated in severe toxicity or acute Overdose >2 g
- Consider Activated Charcoal
- Other supportive measures
- Intravenous Fluids
- Granulocyte colony stimulation factors if significant myelosuppression
- Disposition
- Patients with mild gastrointestinal symptoms after therapeutic dose may be discharged
- Observe patients with severe symptoms or intentional Overdose
XI. Resources
- Capecitabine Tablet (DailyMed)
XII. References
- Tomaszewski (2024) Crit Dec Emerg Med 38(2): 34
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Related Studies
| capecitabine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| CAPECITABINE 500 MG TABLET | Generic | $0.56 each |