What Is Cytarabine?

This product is a pyrimidine anti-metabolite drug that mainly acts on the cell S proliferation stage. It inhibits cell DNA synthesis and interferes with cell proliferation.

English alias: Cytosine 1-beta-D-arabinofuranoside; 1-bD-Arabinofuranosylcytosine; cytarabine; cytosine arabinoside; 4-amino-1-beta-d-arabinofuranosyl-2 (1h) -pyrimidinone; arabinocytidine

Other names: Cytosine arabinoside; Hydrochloric acid

Cytarabine was first synthesized by Richard Walwick, Walden Roberts, and Charles Dekker of the University of California, Berkeley in 1959. The US Food and Drug Administration approved the entry of cytarabine into the market in June 1969; it was originally sold by Upjohn under the trade name Cytosar-U. The chemical structure of this drug is a nucleoside formed by the combination of cytosine and arabinose. Hence the name "cytarabine". Normally, cytosine combines with another sugar (deoxyribose) to form deoxycytidine, one of the components of DNA. However, some organisms of the phylum Porphyra can combine arabinose with cytosine to form another compound (not a component of DNA). People have found this compound in these organisms, namely cytarabine. Cytarabine and deoxycytidine are so similar that they can be incorporated into human DNA instead of the latter. However, the structural difference prevents the DNA from replicating, which kills the affected cells. When administered, cytarabine kills cancer cells with this mechanism of action. It was the first chemotherapeutic drug to work by altering the nucleoside itself--other earlier, similar drugs (such as 5-fluorouracil) changed bases. ^[1]

S36 / 37Wear suitable protective clothing and gloves.

Wear suitable protective clothing and gloves. ^[1]

R43 May cause sensitization by skin contact.

May cause sensitization by contact with skin.

R63Possible risk of harm to the unborn child.

There is a risk of harm to the fetus. ^[1]

This product is a pyrimidine anti-metabolite drug that mainly acts on the cell S proliferation stage. It inhibits cell DNA synthesis and interferes with cell proliferation. Cytarabine enters the human body and is converted to cytarabine triphosphate and cytarabine diphosphate by kinase phosphorylation, the former can strongly inhibit

Mainly used

1. Usual amount for adults (1) Induced remission:

1. Hematopoietic system: mainly bone marrow suppression, leukocytes and thrombocytopenia, severe cases can occur aplastic anemia or

1. This product can cause serum alanine aminotransferase ALT (SGPT), blood and urine

Tetrahydrouridine inhibits deoxygenase and prolongs cytarabine

When taken orally, less than 20% of cytarabine is absorbed by the digestive system, with poor results. After oral administration, due to the first pass effect, it is rapidly metabolized by the liver's cytosine deaminase to inactive uracil arabinocytidine. However, when injected subcutaneously or intramuscularly, thorium-labeled cytarabine produces a peak plasma radioactive concentration between 20 and 60 minutes after administration compared with intravenous injection. As for continuous intravenous injection, relatively constant plasma drug levels can be produced.

Intravenous cytarabine exhibits biphasic metabolism in the human body: the primary metabolic half-life is about 10 minutes. During this time, most of the cytarabine is converted into the non-pharmacological metabolite uracil in the liver. Cytarabine; secondary metabolism (metabolism of uracil arabinocytosine) has a longer half-life, about 1 to 3 hours. Metabolism also occurs in the kidneys, gastrointestinal mucosa, granulocytes and other tissues.

Cytarabine is excreted mainly by the kidney in any mode of administration-70% to 80% of the administered dose will appear in the urine within 24 hours; about 90% of it is a metabolite and 10% is the original drug. ^[2]

Cytarabine is a pyrimidine anti-metabolic drug that acts on S cell proliferation stage and is mainly used in acute myeloid leukemia, acute lymphocytic leukemia and lymphoma, and it is the core drug to induce chemotherapy in the treatment of these diseases.

Cytarabine has antiviral effects and is used to treat various herpes virus infections. However, cytarabine is mainly used for malignant hematological diseases due to its poor antiviral selectivity and its ability to cause bone marrow suppression and other serious adverse reactions. In addition, cytarabine has also been used in neurological studies to control the proliferation of glial cells. ^[2]