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cytarabine (Cytosar-U)
Chemotherapy Agents
Administration: iv, injection

How it is administered

Cytarabine is administered as an injection. It can be given intravenously (IV), subcutaneously (under the skin), or intrathecally (into the spinal fluid, using preservative-free formulations only). The specific route and schedule depend on the treatment plan and type of leukemia being treated. Cytarabine is not effective if taken by mouth.

Common presentations include single-dose or multi-dose vials for IV or subcutaneous use, and preservative-free vials for intrathecal administration.

How it works

Cytarabine is a type of chemotherapy medication known as an antimetabolite. It works by interfering with the DNA synthesis of rapidly dividing cells, such as cancer cells. Cytarabine is especially effective during the S-phase of the cell cycle, which is when DNA is being copied in preparation for cell division.

Once inside the body, cytarabine is converted into an active form that blocks the action of an enzyme called DNA polymerase. This prevents the cancer cells from making new DNA, stopping their growth and eventually leading to cell death. Cytarabine can also be incorporated into the DNA and RNA of cells, causing further disruption to their function. Because it targets cells that are dividing quickly, it is particularly useful in treating certain types of blood cancers.

Common side effects

  • Bone marrow suppression (anemia, low white blood cells, low platelets)
  • Fever
  • Nausea and vomiting
  • Diarrhea
  • Mouth sores (mucositis)
  • Rash
  • Liver dysfunction
  • Bleeding
  • Infections (due to low white blood cells)
  • Loss of appetite
  • Hair loss (alopecia)
  • Cytarabine syndrome (fever, muscle pain, bone pain, rash, conjunctivitis, malaise)
  • Less common: neurological effects (confusion, drowsiness), lung problems, allergic reactions, and rarely, severe skin reactions

Who Should take it

Cytarabine is indicated for use in combination with other approved anti-cancer drugs for remission induction in acute non-lymphocytic leukemia (also known as acute myeloid leukemia, or AML) in adults and children. It is also used in the treatment of acute lymphocytic leukemia (ALL) and the blast phase of chronic myeloid leukemia (CML).

Additionally, preservative-free cytarabine can be given intrathecally for the prevention and treatment of meningeal (central nervous system) leukemia. While cytarabine is not specifically approved for T-Cell Prolymphocytic Leukemia, it may be used as part of broader leukemia treatment regimens depending on the clinical situation.

Who should not take it

Cytarabine should not be used in patients who are hypersensitive (allergic) to the drug. It should be used with extreme caution in patients with pre-existing bone marrow suppression, as it can further decrease blood cell counts and increase the risk of infection or bleeding.

Patients with poor liver or kidney function may need dose adjustments or closer monitoring, as they may be at higher risk for side effects. Cytarabine can cause harm to a developing fetus, so it should not be used during pregnancy unless absolutely necessary. Women of childbearing age should avoid becoming pregnant while taking cytarabine. It is also not known if cytarabine passes into breast milk, so breastfeeding is not recommended during treatment.

Commonly used with

Cytarabine is commonly used in combination with other chemotherapy agents, such as daunorubicin, as part of multi-drug regimens for leukemia. For example, the '7+3' regimen for AML combines cytarabine with daunorubicin. It may also be used with other drugs like cyclophosphamide, vincristine, prednisone, and methotrexate, depending on the type of leukemia and treatment protocol.

In the setting of central nervous system involvement, cytarabine may be given with methotrexate and hydrocortisone intrathecally.

Commonly tested with

Cytarabine is often tested in clinical trials in combination with other chemotherapy drugs for various types of leukemia, including daunorubicin, asparaginase, etoposide, and others. It is also studied in protocols that include supportive medications to manage side effects, such as corticosteroids for cytarabine syndrome or antiemetics for nausea.

Drug interactions may occur with digoxin, gentamicin, and fluorocytosine, so these combinations may be monitored or studied for safety.

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