Find cytarabine injection - 100 MG/5 ML SINGLE-DOSE VIAL medical information:
cytarabine injection - 100 MG/5 ML SINGLE-DOSE VIAL Clinical Pharmacology
Cell Culture Studies
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. Although the mechanism of action is not completely understood, it appears that cytarabine acts through the inhibition of DNA polymerase. A limited, but significant, incorporation of cytarabine into both DNA and RNA has also been reported. Extensive chromosomal damage, including chromatoid breaks, have been produced by cytarabine and malignant transformation of rodent cells in culture has been reported. Deoxycytidine prevents or delays (but does not reverse) the cytotoxic activity.
Cellular Resistance and Sensitivity
Cytarabine is metabolized by deoxycytidine kinase and other nucleotide kinases to the nucleotide triphosphate, an effective inhibitor of DNA polymerase; it is inactivated by a pyrimidine nucleoside deaminase, which converts it to the non-toxic uracil derivative. It appears that the balance of kinase and deaminase levels may be an important factor in determining sensitivity or resistance of the cell to cytarabine.
Human Pharmacology
Cytarabine is rapidly metabolized and is not effective orally; less than 20 percent of the orally administered dose is absorbed from the gastrointestinal tract.
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. After the distributive phase, more than 80 percent of plasma radioactivity can be accounted for by the inactive metabolite 1-β-D-arabinofuranosyluracil (ara-U). Within 24 hours about 80 percent of the administered radioactivity can be recovered in the urine, approximately 90 percent of which is excreted as ara-U.
Relatively constant plasma levels can be achieved by continuous intravenous infusion.
After subcutaneous or intramuscular administration of cytarabine labeled with tritium, peak-plasma levels of radioactivity are achieved about 20 to 60 minutes after injection and are considerably lower than those after intravenous administration.
Cerebrospinal fluid levels of cytarabine are low in comparison to plasma levels after single intravenous injection. However, in one patient in whom cerebrospinal fluid levels are examined after 2 hours of constant intravenous infusion, levels approached 40 percent of the steady state plasma level. With intrathecal administration, levels of cytarabine in the cerebrospinal fluid declined with a first order half-life of about 2 hours. Because cerebrospinal fluid levels of deaminase are low, little conversion to ara-U was observed.
Immunosuppressive Action
Cytarabine Injection is capable of obliterating immune responses in man during administration with little or no accompanying toxicity. Suppression of antibody responses to E-coli-VI antigen and tetanus toxoid have been demonstrated. This suppression was obtained during both primary and secondary antibody responses.
Cytarabine Injection also suppressed the development of cell-mediated immune responses such as delayed hypersensitivity skin reaction to dinitrochlorobenzene. However, it had no effect on already established delayed hypersensitivity reactions.
Following 5-day courses of intensive therapy with Cytarabine Injection the immune response was suppressed, as indicated by the following parameters: macrophage ingress into skin windows; circulating antibody response following primary antigenic stimulation; lymphocyte blastogenesis with phytohemagglutinin. A few days after termination of therapy there was a rapid return to normal.
cytarabine injection - 100 MG/5 ML SINGLE-DOSE VIAL Quick Finder
Only physicians experienced in cancer chemotherapy should use Cytarabine Injection.
For induction therapy patients should be treated in a facility with laboratory and supportive resources sufficient to...
Cytarabine Injection in combination with other approved anti-cancer drugs is indicated for remission induction in acute non-lymphocytic leukemia of adults and pediatric patients. It has also been found...
Cytarabine Injection is not active orally. The schedule and method of administration varies with the program of therapy to be used. Cytarabine Injection may be given by intravenous infusion or...
Cytarabine Injection is contraindicated in those patients who are hypersensitive to the drug.
(See boxed WARNING)
Cytarabine is a potent bone marrow suppressant. Therapy should be started cautiously in patients with pre-existing drug-induced bone marrow...
Expected Reactions
Because cytarabine is a bone marrow suppressant, anemia, leukopenia, thrombocytopenia, megaloblastosis and reduced reticulocytes...
There is no antidote for overdosage of Cytarabine Injection. Doses of 4.5 g/m2 by intravenous infusion over 1 hour every 12 hours for 12 doses have caused an unacceptable increase in...
Cytarabine Injection, an antineoplastic, is a sterile solution of cytarabine for intravenous, intrathecal or subcutaneous administration and is available in 20 mg/mL (100 mg/5 mL) single dose vial.
Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture. It exhibits cell phase specificity,...
Recommendations for the Safe Handling of Parenteral Antineoplastic Drugs, NIH Publications No. 83-2621. For sale by the Superintendent of Documents, U.S. Government Printing Office, Washington, D.C. 20402.
Cytarabine Injection is available as follows:
For Intravenous, Intrathecal and Subcutaneous Use Only