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fludarabine (Fludara)

Tradename: Fludara. Fludarabine phosphate. (9-b-beta-arabinofuranosyl-2-fluoroadenine) Indications: - treatment of chronic lymphocytic leukemia (B-cell) - patients not responding to other agents - low grade, non-Hodgkin's lymphoma (follicular lymphoma) - acute myeloid leukemia [5] Dosage: 1) 25 mg/m2/day IV for 5 days every 4 weeks 2) 30% reduction if creatinine clearance < 70 mL/min Lyophilized powder for injection: 50 mg Refrigerate: use within 8 hours of reconstitution. Pharmacokinetics: 1) metabolized to 2 active metabolites 2) highly tissue bound 3) eliminated mostly in the urine 4) 1/2life is 10 hours Adverse effects: 1) common (> 10%) a) nausea/vomiting: mild emetic b) fever/chills, fatigue, pain, rash, diarrhea, stomatitis, GI bleeding, urinary tract infection, paresthesia, myalgia, weakness, dyspnea, non-productive cough, pneumonitis, pneumonia, infection c) myelosuppression - nadir: - neutrophils: 3-25, mean: 13 days - platelets: 2-32, mean: 16 days - WBC: 8 days - recovery 5-7 weeks 2) less common (1-10%) - congestive heart failure, malaise, headache, alopecia, hyperglycemia, anorexia, hearing loss 3) uncommon (< 1%) - occur with higher doses, often occurs on rechallenge. - generally accompanied by CNS demyelination - steroid treatment my or may not be helpful - somnolence, blindness, coma, death, severe neurotoxicity, skin rash, metabolic acidosis, metallic taste, autoimmunehemolytic anemia (may be fatal), reversible hepatotoxicity, renal failure, hematuria, tumor lysis syndrome 4) other [3] - peripheral neuropathy - delayed demyelinating CNS syndromes Mechanism of action: 1) antimetabolite 2) interferes with DNA synthesis

Related

chronic lymphocytic leukemia (CLL)

General

antineoplastic agent (chemotherapeutic agent) purine antimetabolite; antimetabolite; purine analog

Properties

MISC-INFO: elimination route KIDNEY 1/2life 10 HOURS

Database Correlations

PUBCHEM correlations

References

  1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  2. AHFS 96 Drug Information, GK McEnvoy et al (ed), American Society of Health-System Pharmacists, Bethesda, MD 1998
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 529
  5. Deprecated Reference