Contents

Search

cytosine arabinoside; cytarabine (Cytosar, ARA-C, HiDAC, Depocyt)

Tradenames: Cytosar, Depocyt. Indications: 1) leukemia a) acute myeloid leukemia (AML) b) acute lymphocytic leukemia (ALL) c) chronic myeloid leukemia (CML) d) meningial leukemia e) acute non-lymphocytic leukemia 2) myelodysplastic syndrome 3) Hodgkin's disease & non-Hodgkin's lymphoma 4) stem cell transplantation [5] Dosage: 1) 60-200 mg/m2 as continuous IV infusion over 5-10 days 2) 10-30 mg/m2 intrathecally 2-3 times weekly - use normal saline or Elliot's B solution for diluent 3) 100 mg/m2 IV or SC every 12 hours for 5 days every month 4) doses up to 3 g/m2 IV every 12 hours have been given Powder for injection: 100 mg, 200 mg, 1g, 2g. Injection: Liposomal (Depocyt). Caution: - incompatible with 5-fluorouracil, gentamicin, insulin, methylprednisolone, nafcillin, oxacillin, penicillin G Monitor: 1) complete blood count (CBC) 2) liver function tests (LFTs) Pharmacokinetics: 1) widely distributed to tissues 2) deactivated by the liver 3) 72% recovered in the urine 4) 1/2life is 2-3 hours (plasma); 2-10 hours (CNS) Adverse effects: 1) common (> 10%) - oral ulceration, anal ulceration, hepatic dysfunction, fever, rash, thrombophlebitis, bleeding, nausea/vomiting, diarrhea, mucositis 2) less common (1-10%) - dizziness, headache, skin freckles, itching, alopecia, sepsis, pneumonia, cellulitis at injection site, urinary retention, neuritis, cardiomegaly, somnolence, peripheral neuropathy, malaise, confusion, myalgia, bone pain, sudden respiratory depression leading to pulmonary edema 3) other [2] - myelosuppression - conjunctivitis (most patients need prophylactic glucocorticoid eyedrops) - cerebellar toxicity - neurotoxicity - flu-like syndrome - hand & foot syndrome [6] Drug interactions: 1) cytarabine decreases digoxin bioavailability 2) gentamicin 3) flucytosine Test interactions: 1) increases serum K+ 2) decreases serum protein Laboratory: - cytarabine C in serum/plasma - cytarabine U in serum/plasma Mechanism of action: 1) antimetabolite 2) affects rapidly dividing cells in G1 to S phase Mechanism of drug resistance: 1) defective transport via the nucleoside transporter 2) diminished activity of deoxycytidine kinase 3) increased drug inactivation via by activation of cytidine deaminase

Related

cytidine deaminase; cytidine aminohydrolase (CDA, CDD) deoxycytidine kinase (DCK) Na+/nucleoside cotransporter or nucleoside transporter

General

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

Properties

MISC-INFO: elimination route LIVER KIDNEY 1/2life 2-10 HOURS pregnancy-category D

References

  1. Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 596
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 533
  5. Deprecated Reference
  6. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015

Component-of

cytarabine/daunorubicin; CPX-351 (Vyxeos)

Databases & Figures

PUBCHEM correlations Therapeutic Inducers of Apoptosis