Cytarabine
- Atc Codes:L01BC01
- CAS Codes:147-94-4#69-74-9
- PHARMGKB ID:147-94-4#69-74-9
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Alexan, Cytarabine, DepoCyte; Belgium: Cytarabine, Cytosar, DepoCyte; Bulgaria: Alexan, Cytarabine, DepoCyte; Cyprus: Cytarabine, DepoCyte; Czech Republic: Alexan, Cytosar, DepoCyte; Denmark: Arabine, Cytarabine, DepoCyte; Estonia: Cytosar, DepoCyte; Finland: Cytarabine, DepoCyte; France: Aracytine, Cytarabine, DepoCyte; Germany: Alexan, Ara-Cell, Cytarabin, DepoCyte; Greece: Aracytin, Citabion, DepoCyte; Hungary: Alexan, Cytosar, DepoCyte; Ireland: Cytarabine, DepoCyte; Italy: Aracytin, Cytarabine, DepoCyte; Latvia: Cytosar, DepoCyte; Lithuania: Cytosar, DepoCyte; Luxembourg: Cytarabinum, DepoCyte; Netherlands: Alexan, Cytarabine, DepoCyte; Poland: Alexan, Cytosar, DepoCyte; Portugal: Alexan, Ara-Cell, Citaloxan, Citarabina, Cytosar, DepoCyte; Romania: Alexan, Cytosar, DepoCyte; Slovakia: Alexan, Cytosar, DepoCyte; Slovenia: Cytosar, DepoCyte; Spain: Citarabina, DepoCyte; Sweden: Arabine, Cytarabine, DepoCyte; UK: Cytarabine, DepoCyte.
North America
Canada: Cytarabine, Cytosar, Depocyt; USA: Cytarabine, Cytosar-U, Depocyt.
Latin America
Argentina: Ara-C, Citagenin, Citarabina; Brazil: Aracytin, Citarax, Darbin; Mexico: Cytosar-U, Laracit, Medsara, Novumtrax.
Asia
Japan: Cylocide.
Drug combinations
Cytarabine and Daunorubicin Hydrochloride
Cytarabine, Daunorubicin Hydrochloride and Etoposide
Chemistry
Cytarabine: C~9~H~13~N~3~O~5~. Mw: 243.22. (1) 2(1H)-Pyrimidinone, 4-amino-1-β-D-arabinofuranosyl-; (2) 1-β-D-Arabinofuranosylcytosine. CAS-147-94-4 (1969).
Cytarabine Hydrochloride: C~9~H~13~N~3~O5 HCl. Mw: 279.68. 1-β-D-Arabinofuranosylcytosine monohydrochloride. CAS-69-74-9 (1964).
Pharmacologic Category
Antineoplastic Agents; Antimetabolite; Pyrimidine Analog. (ATC-Code: L01BC01).
Mechanism of action
Inhibits DNA synthesis. Cytosine enters into cells by a carrier process, and must then be converted to its active compound, aracytidine triphosphate. Cytosine is a pyrimidine analog and is incorporated into DNA. The primary action is inhibition of DNA polymerase resulting in decreased DNA synthesis and repair. Cytarabine is specific for the S phase of the cell cycle (blocks progression from the G~1~ to the S phase). Also has immunosuppressive effects.
Therapeutic use
Acute myeloid leukemia, acute lymphocytic leukemia, chronic myelocytic leukemia, and lymphomas. Prophylaxis and treatment of meningeal leukemia. Used in combination regimens for the treatment of leukemias, meningeal leukemia, Hodgkin’s lymphoma, and non-Hodgkin lymphoma.
Pregnancy and lactiation implications
Teratogenic in animal studies. Limb, ear defects, pancytopenia, WBC depression, electrolyte abnormalities, prematurity, low birth weight, decreased hematocrit or platelets described in neonates. Risk to the fetus is decreased if therapy is avoided during the 1^st^ trimester. Excretion in breast milk unknown.
Unlabeled use
Contraindications
Hypersensitivity to cytarabine or any component of the formulation. Hypersensitivity to cytarabine or any ingredient in the formulation. If active meningeal infection, liposomal cytarabine contraindicated.
Warnings and precautions
Hazardous agent. A cytarabine syndrome (fever, myalgia, bone pain, chest pain, maculopapular rash, conjunctivitis, and malaise) may occur. Potent myelosuppressive agent (caution if prior bone marrow suppression). Episodes of acute pancreatitis reported in patients receiving continuous infusion and in patients previously treated with L-asparaginase. With high dose therapy, tumor lysis syndrome and subsequent hyperuricemia may occur. Use with caution in hepatic and renal impairment (higher risk for CNS toxicities). Case reports of fatal cardiomyopathy when high-dose cytarabine was used in combination with cyclophosphamide. Some products may contain benzyl alcohol; do not use products containing benzyl alcohol or products reconstituted with bacteriostatic diluent intrathecally or for high-dose cytarabine regimens. High-dose regimens associated with GI, CNS, pulmonary, and ocular toxicities, and cardiomyopathy. Neurotoxicity associated with high-dose treatment may present as acute cerebellar toxicity or may be severe with seizure and/or coma.