Source: Health Products Regulatory Authority (ZA) Revision Year: 2021 Publisher: Pfizer Laboratories (Pty) Ltd, 85 Bute Lane, Sandton 2196, South Africa Tel: +27(0)11 320 6000 / 0860 734 937 (Toll-free South Africa)
Category and class: A26 Cytostatic agents
Cytarabine, a pyrimidine nucleoside analogue, is an antineoplastic medicine which inhibits the synthesis of deoxyribonucleic acid. In vitro, it also has antiviral and immunosuppressant properties. Detailed studies on the mechanism of cytotoxicity in vitro suggest that the primary action of cytarabine is inhibition of deoxycytidine synthesis, although inhibition of cytidylic kinases and incorporation of the compound into nucleic acids may also play a role in its cytostatic and cytocidal actions.
Cytarabine is deaminated to arabinofuranosyl uracil in the liver and kidneys. After intravenous administration to humans, only 5,8% of the administered dose is excreted unaltered in the urine within 12–24 hours; 90% of the dose is excreted as the deaminated medicine. Cytarabine appears to be metabolised rapidly, primarily by the liver and perhaps by the kidney. After a single high intravenous dose, blood levels fall to unmeasurable levels within 15 minutes in most patients. Some patients have no demonstrable circulating cytarabine as early as 5 minutes after injection.
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