cytosine arabinoside; cytarabine (Cytosar, ARA-C, HiDAC, Depocyt)
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Introduction
Tradenames: Cytosar, Depocyt.
Indications
- leukemia
- myelodysplastic syndrome
- Hodgkin's disease & non-Hodgkin's lymphoma
- stem cell transplantation[5]
Dosage
- 60-200 mg/m2 as continuous IV infusion over 5-10 days
- 10-30 mg/m2 intrathecally 2-3 times weekly
- use normal saline or Elliot's B solution for diluent
- 100 mg/m2 IV or SC every 12 hours for 5 days every month
- 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
Pharmacokinetics
- widely distributed to tissues
- deactivated by the liver
- 72% recovered in the urine
- 1/2life is 2-3 hours (plasma); 2-10 hours (CNS)
elimination via liver
elimination via kidney
1/2life = 2-10 hours
Monitor
Adverse effects
- common (> 10%)
- 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
- other[2]
- myelosuppression
- conjunctivitis (most patients need prophylactic glucocorticoid eyedrops)
- cerebellar toxicity
- neurotoxicity
- flu-like syndrome
- hand & foot syndrome[6]
Drug interactions
- cytarabine decreases digoxin bioavailability
- gentamicin
- flucytosine
Test interactions
- increases serum K+
- decreases serum protein
Laboratory
Mechanism of action
- antimetabolite
- affects rapidly dividing cells in G1 to S phase Mechanism of drug resistance:
- defective transport via the nucleoside transporter
- diminished activity of deoxycytidine kinase
- increased drug inactivation via by activation of cytidine deaminase
More general terms
- pyrimidine antimetabolite; antimetabolite; pyrimidine analog
- antineoplastic agent (chemotherapeutic agent)
Additional terms
- cytidine deaminase; cytidine aminohydrolase (CDA, CDD)
- deoxycytidine kinase (DCK)
- Na+/nucleoside cotransporter or nucleoside transporter
Component of
References
- ↑ Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 596
- ↑ 2.0 2.1 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 533
- ↑ 5.0 5.1 Deprecated Reference
- ↑ 6.0 6.1 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015