Adult: 5-75 mg/m2 or 30-100 mg once every 2-7 days to once daily for 4 or 5 days. For lymphomatous meningitis: 50 mg every 2 wk for 5 doses, then every 4 wk for 5 doses.
Parenteral Induction and maintenance of remission in acute leukaemias
Adult: As monotherapy: 200 mg/m2 daily by continuous IV infusion for 5 days, at intervals of approx 2 wk. In combination therapy: 100 mg/m2 bid by rapid IV inj or 100 mg/m2 daily by continuous IV infusion both for 7 days. Maintenance: 1-1.5 mg/kg once or twice wkly via IV or SC.
Reconstitution
IV: Reconstitute w/ bacteriostatic water for inj (standard-dose), further dilute in 250-1,000 mL NaCl 0.9% or dextrose 5% in water for infusion. Intrathecal: Reconstitute w/ preservative free NaCl 0.9%, further dilute w/ Elliot’s B soln, NaCl 0.9% or lactated Ringer’s inj to preferred final vol (up to 12 mL).
Monitor LFTs, CBC w/ differential and platelet count, BUN, serum uric acid, serum creatinine. Monitor for signs of an immediate reaction, chemical arachnoiditis, neurotoxicity.
Overdosage
Symptoms: Irreversible CNS toxicity and death. Severe arachnoiditis including encephalopathy. Management: Therapy cessation followed by treatment of ensuing bone marrow depression including whole blood or platelet transfusion and antibiotics. Maintain vital functions.
Drug Interactions
May reduce efficacy of 5-fluorocytosine, digoxin, gentamicin. May increase risk of neurotoxicity w/ other cytotoxic agents (intrathecal).
Action
Description: Mechanism of Action: Cytarabine inhibits deoxyribonucleic acid (DNA) synthesis specifically at the S-phase of the cell cycle. It also has an antiviral and immunosuppressant activity. Pharmacokinetics: Absorption: Time to peak plasma concentration: 20-60 min (IM/SC). Distribution: Crosses the placenta and blood-brain barrier w/ CSF levels of 40-50% of plasma level. Volume of distribution: 3±11.9 L/kg. Plasma protein binding: 13%. Metabolism: Converted by phosphorylation to an active form followed by deamination in the liver and kidneys to inactive uracil arabinoside (ARA-U). Excretion: Via urine (mostly as inactive metabolite; approx 10% as unchanged drug). Elimination half-life: Initial: Approx 10 min (IV); terminal: 1-3 hr (IV), 100-263 hr (intrathecal).
Chemical Structure
Cytarabine Source: National Center for Biotechnology Information. PubChem Database. Cytarabine, CID=6253, https://pubchem.ncbi.nlm.nih.gov/compound/Cytarabine (accessed on Jan. 22, 2020)
Storage
IV/SC: Store between 15-25°C. Intrathecal: Store between 2-8°C. Avoid freezing.
L01BC01 - cytarabine ; Belongs to the class of antimetabolites, pyrimidine analogues. Used in the treatment of cancer.
References
Anon. Cytarabine (Conventional). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/01/2016.Anon. Cytarabine (Liposomal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/01/2016.Buckingham R (ed). Cytarabine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/01/2016.Cytarabine for Injection, 1 g/vial [Bedford Labs]: Recall: Risk of Lack of Sterility. U.S. FDA. https://www.fda.gov/. Accessed 13/01/2016.Cytarabine Injection (Mylan Institutional LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/01/2016.Joint Formulary Committee. Cytarabine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/01/2016.McEvoy GK, Snow EK, Miller J et al (eds). Cytarabine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 13/01/2016.
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