What is the mechanism of action of cytarabine?
Mechanism of Action Cytarabine is a pyrimidine analog and is also known as arabinosylcytosine (ARA-C). It is converted into the triphosphate form within the cell and competes with cytidine to incorporate itself in the DNA. The sugar moiety of cytarabine hinders the rotation of the molecule within the DNA.
What does cytarabine do to the body?
Cytarabine is a type of chemotherapy drug. It kills cancer cells by stopping them from making and repairing DNA that they need to grow and multiply.
What class of drug is cytarabine?
Drug type: Cytarabine is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug. This medication is classified as an “antimetabolite.” (For more detail, see “How cytarabine works” section below).
What phase is affected by cytarabine?
Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture. It exhibits cell phase specificity, primarily killing cells undergoing DNA synthesis (S-phase) and under certain conditions blocking the progression of cells from the G1 phase to the S-phase.
Which cell cycle is most affected by cytarabine?
Its mode of action is due to its rapid conversion into cytosine arabinoside triphosphate, which damages DNA when the cell cycle holds in the S phase (synthesis of DNA). Rapidly dividing cells, which require DNA replication for mitosis, are therefore most affected.
How does cytarabine prevent replication?
It does this by inhibiting the production of the cells’ genetic material, DNA and RNA. Both DNA and RNA are needed for growth and multiplication of cells. Cytarabine causes a deficiency of DNA and RNA in the cancer cells, and this causes the cells to grow in an unbalanced way, resulting in the death of the cells.
What is the half life of cytarabine?
Human Pharmacology Following rapid intravenous injection of cytarabine labeled with tritium, the disappearance from plasma is biphasic. There is an initial distributive phase with a half-life of about 10 minutes, followed by a second elimination phase with a half-life of about 1 to 3 hours.
How does cytarabine prevent DNA replication of cytosine?
Cytarabine is an S-phase specific antimetabolite cytotoxic agent, which when converted intracellularly to cytosine arabinoside triphosphate competes with the physiologic substrate deoxycitidine triphosphate, thus resulting in both inhibition of DNA polymerase and DNA synthesis.
Does cytarabine cause anemia?
Expected Reactions. Because cytarabine is a bone marrow suppressant, anemia, leukopenia, thrombocytopenia, megaloblastosis and reduced reticulocytes can be expected as a result of administration with cytarabine. The severity of these reactions are dose and schedule dependent.
Is cytarabine a neurotoxic?
Abstract. Neurotoxicity from high-dose cytarabine, a pyrimidine metabolite used in treatment for acute myeloid leukemia, is a known but dose-limiting toxicity which has incidences in up to 14% in patients receiving high doses of the drug.
Does cytarabine cause neuropathy?
Intravenous (IV) therapy may cause a peripheral neuropathy that varies greatly in its severity. The high IV cytarabine doses now commonly used can cause seizures, cerebral dysfunction, or an acute cerebellar syndrome with an incidence up to 14%.
How is cytarabine metabolized?
Cytarabine is rapidly and extensively metabolized mainly in the liver but also in kidneys, GI mucosa, granulocytes, and to a lesser extent in other tissues by the enzyme cytidine deaminase, producing the inactive metabolite 1-ß-d-arabinofuranosyluracil (ara-U, uracil arabinoside).
What is cytarabine cytotoxicity?
Cytotoxicity is highly specific for the S phase of the cell cycle. Cytarabine acts through direct DNA damage and incorporation into DNA. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture.
Does cytarabine kill S phase cells?
Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture. It exhibits cell phase specificity, primarily killing cells undergoing DNA synthesis (S-phase) and under certain conditions blocking the progression of cells from the G1 phase to the S-phase.
What is cytarabine used to treat?
Cytarabine is a Nucleoside Metabolic Inhibitor. The mechanism of action of cytarabine is as a Nucleic Acid Synthesis Inhibitor. L01XY01