Levofloxacin and Cholestyramine

Levofloxacin and Cholestyramine

PEP Topic 
Chemotherapy-Induced Diarrhea

Levofloxacin is a fluoroquinolone antibiotic. It is used for the treatment of pneumonia, chronic bronchitis, and sinus, urinary tract, kidney, prostate, and skin infections. 

Cholestyramine is a chemical that binds to bile acids in the gastrointestinal (GI) tract to prevent reabsorption of bile acids.  Binding to cholestyramine results in excretion of bile acids in the feces, which results in increased clearance of cholesterol. It has been used to reduce diarrhea in GI diseases.

Cholestyramine and levofloxacin in combination were examined for their efficacy in treating delayed diarrhea in patients with cancer.

Effectiveness Not Established

Research Evidence Summaries

Flieger, D., Klassert, C., Hainke, S., Keller, R., Kleinschmidt, R., & Fischback, W. (2007). Phase II clinical trial for prevention of delayed diarrhea with cholestyramine/levofloxacin in the second-line treatment with irinotecan biweekly in patients with metastatic colorectal carcinoma. Oncology, 72(1–2), 10–16.

doi: 10.1159/000111083

Intervention Characteristics/Basic Study Process:

Patients receiving 250 mg/m2 IV irinotecan over 90 minutes every two weeks were given 500 mg levofloxacin tablets once at 8 pm and 4 g cholestyramine three times per day (not together with other medications) beginning the day before chemotherapy to day +1. Patients with acute cholinergic syndrome, abdominal cramping, and early diarrhea, were given 0.25-1 mg IV atropine. Patients experiencing delayed diarrhea were offered loperaminde.

Sample Characteristics:

  • The study reported on 51 patients with metastatic colorectal cancer (CRC) in second-line treatment.
  • Mean age was 64 with a range of 41–81.
  • Patients had not received prior irinotecan therapy and were refractory or resistant to 5-fluorouracil (5-FU).

Study Design:

This was a phase II trial.

Measurement Instruments/Methods:

  • Patients recorded diarrhea incidence and severity in diaries following each chemotherapy dose.
  • Diarrhea severity was measured using World Health Organization (WHO) grading.


  • Forty patients (78%) did not develop diarrhea, 11 patients (22%) reported WHO grade 1–2 diarrhea, and only one patient (2%) reported WHO grade 3 diarrhea.
  • No patients reported grade 4 diarrhea. 
  • Reported incidence of diarrhea without prophylaxis in the literature is up to 40%.


  • The study sample was small.
  • This was a phase II study.
  • Investigators did not conduct pharmacokinetic analyses of the active metabolites SN-38 and SN-38G in plasma.
  • No information was provided on the effect of cholestyramine on the efficacy of irinotecan efficacy. If cholestyramine decreases the effects of irinotecan, this could account for a decreased incidence of diarrhea.

Nursing Implications:

Combination cholestyramine and levofloxacin is a promising option for prevention of delayed diarrhea caused by irinotecan and may help to escalate the dose of irinotecan in the future.