Expiration date: 01/2025
Product form, composition and packaging
The solution for injection is transparent, colorless. 1 ml of 1 FL. citarabine 20 mg 100 mg. Excipients: sodium chloride, sodium lactate, lactic acid, water d / I. the solution for injection is transparent, colorless. 1 ml of 1 FL. citarabine 50 mg 500 mg. Excipients: sodium lactate, lactic acid, water d / I. The solution for injection is transparent, colorless. 1 ml of 1 FL. cytarabine 50 mg 1 g excipients: sodium lactate, lactic acid, water d/I. Clinico-pharmacological group: Antineoplastic drug.
Pharmacological action
Anticancer drug. It belongs to the group of pyrimidine exchange antimetabolites and is an S-phase-specific drug. Inhibits the synthesis of DNA. In the result of phosphorylation turns in arabinosyl citizensabout (Ara-TSTF), which is a competitive inhibits DNA polymerase. In addition, there is evidence that DNA synthesis is inhibited also by embedding cytarabine into DNA and RNA. Possible development of resistance to citarabine is associated with inhibition of membrane transport, deficiency of phosphorylating enzymes, increased activity of inactivating enzymes, reduced affinity of DNA polymerase or increased pool of deoxy-CTF. Cytotoxic effect is achieved by creating constant high intracellular concentrations of Ara-CTF.
Pharmacokinetics Absorption and distribution In continuous I/V infusion cytarabine at conventional dose (100-200 mg/m2 of body surface) is achieved in the concentration 0.04-0.6 µmol/l p/to the introduction of Cmax in plasma is reached within 20-60 min, then there is a biphasic decline in concentration. Cytarabine penetrates the GEB. After continuous infusion in the cerebrospinal fluid, a concentration of 10-40% of the plasma concentration is achieved. The plasma protein binding is 15%. Metabolism After I/V administration of the cytarabine under the action of titidindezaminaza rapidly and almost completely biotransformiroetsa in the liver and other tissues to inactive uracil-metabolite (Ara-U). A minor part of cytarabine undergoes phosphorylation under the action of kinases at the intracellular level, resulting in the formation of the active metabolite Ara-TSTF. The excretion of T1 / 2 in the initial (?-phase) phase is 10 minutes, in the final (?-phase) - about 1-3 hours. Due to minimal activity in the Central nervous system desaminase the elimination of cytarabine from the cerebrospinal fluid is slow, with T1/2 2-11 hours is unchanged, the news is 4-10% of the administered dose. In the first 24 hours 71-96% of the administered drug is found in the urine in the form of Ara-U.
Indications
acute non-lymphoblastic and / or lymphoblastic leukemia (for the induction of remission, as well as maintenance therapy), * prevention and treatment of neuroleukosis (intrathecal administration in the form of monotherapy and in combination with other anticancer drugs), treatment of non-Hodgkin's lymphomas, * treatment of blast crises in chronic myeloid leukemia. High-dose citarabin therapy: * refractory to therapy non-Hodgkin's lymphomas, * refractory to therapy acute lymphoblastic and/or non-lymphoblastic leukemia, as well as options with an unfavorable prognosis, * relapses of acute leukemia, * secondary leukemia after previous chemotherapy and/or radiation therapy, * manifest leukemia after transformation of preleukosis, * acute non-lymphoblastic leukemia in patients younger than 60 years (for consolidation remission), * blast crises in chronic myeloid leukemia.
