Cytarabin
Cytarabin Uses, Dosage, Side Effects, Food Interaction and all others data.
Cytarabin inhibits deoxyribonucleic acid (DNA) synthesis specifically at the S-phase of the cell cycle. It also has an antiviral and immunosuppressant activity.
Cytarabin is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute myelogenous leukemia and meningeal leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Cytarabin is metabolized intracellularly into its active triphosphate form (cytosine arabinoside triphosphate). This metabolite then damages DNA by multiple mechanisms, including the inhibition of alpha-DNA polymerase, inhibition of DNA repair through an effect on beta-DNA polymerase, and incorporation into DNA. The latter mechanism is probably the most important. Cytotoxicity is highly specific for the S phase of the cell cycle.
| Trade Name | Cytarabin |
| Availability | Prescription only |
| Generic | Cytarabine |
| Cytarabine Other Names | Citarabina, Cytarabine, Cytarabinum, Cytosine arabinoside |
| Related Drugs | Venclexta, prednisone, methotrexate, dexamethasone, triamcinolone, Decadron, rituximab, hydroxyurea, Rituxan, cyclophosphamide |
| Weight | 100mg/vial, 500mg/vial |
| Type | Injection |
| Formula | C9H13N3O5 |
| Weight | Average: 243.2166 Monoisotopic: 243.085520541 |
| Protein binding | 13% |
| Groups | Approved, Investigational |
| Therapeutic Class | Cytotoxic Chemotherapy |
| Manufacturer | Ferring Pharmaceuticals Pvt Ltd, Pfizer Ltd, Atco Laboratories Limited |
| Available Country | India, Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cytarabin is used for Leukaemic meningitis, Induction and maintenance of remission in acute leukaemias
Cytarabin is also used to associated treatment for these conditions: Acute Lymphocytic Leukemia (ALL), Acute Myeloid Leukemia (AML), Acute Promyelocytic Leukemia (APL), Leptomeningeal Metastases, Meningeal leukemia, Non-Hodgkin's Lymphoma (NHL), Blast phase Chronic myelocytic leukemia
How Cytarabin works
Cytarabin acts through direct DNA damage and incorporation into DNA. Cytarabin 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.
Dosage
Cytarabin dosage
Intrathecal (Adult)-
- Leukaemic meningitis:5-75 mg/m2 or 30-100 mg once every 2-7 days to once daily for 4 or 5 days.
- For lymphomatous meningitis: 50 mg every 2 wk for 5 doses, then every 4 wk for 5 doses.
Parenteral (Adult)-Induction and maintenance of remission in acute leukaemias:
- As monotherapy: 200 mg/m2 daily by continuous IV infusion for 5 days, at intervals of approx 2 wk.
- In combination therapy: 100 mg/m2 bid by rapid IV inj or 100 mg/m2 daily by continuous IV infusion both for 7 days. Maintenance: 1-1.5 mg/kg once or twice wkly via IV or SC.
Intravenous: Reconstitute with bacteriostatic water for inj (standard-dose), further dilute in 250-1,000 ml NaCl 0.9% or dextrose 5% in water for infusion.
Intrathecal: Reconstitute with preservative free NaCl 0.9%, further dilute with Elliot’s B soln, NaCl 0.9% or lactated Ringer’s inj to preferred final vol (up to 12 ml).
Side Effects
Nausea, vomiting, fever, rash, diarrhoea, anorexia, oral and anal inflammation or ulceration, hepatic dysfunction, headache, weakness, confusion, thrombocytopenia, fatigue.
Toxicity
Cytarabin syndrome may develop - it is characterized by fever, myalgia, bone pain, occasionally chest pain, maculopapular rash, conjunctivitis, and malaise.
Precaution
Patient with previous drug-induced bone marrow suppression. Renal or hepatic impairment. Pregnancy and lactation.
Interaction
May reduce efficacy of 5-fluorocytosine, digoxin, gentamicin. May increase risk of neurotoxicity with other cytotoxic agents (intrathecal).
Food Interaction
No interactions found.Cytarabin Drug Interaction
Unknown: lorazepam, lorazepam, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, ubiquinone, ubiquinone, copper gluconate, copper gluconate, glycerin, glycerin, acetaminophen, acetaminophen, bioflavonoids, bioflavonoids, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, ondansetron, ondansetron
Cytarabin Disease Interaction
Major: infections, myelosuppressionModerate: hepatic dysfunction, renal dysfunction
Elimination Route
Less than 20% of the orally administered dose is absorbed from the gastrointestinal tract.
Half Life
10 minutes
Elimination Route
The primary route of elimination of cytarabine is metabolism to the inactive compound ara-U, followed by urinary excretion of ara-U.
Pregnancy & Breastfeeding use
Pregnancy Category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Contraindication
Patient with active meningeal infection.
Acute Overdose
Symptoms: Irreversible CNS toxicity and death. Severe arachnoiditis including encephalopathy.
Management: Therapy cessation followed by treatment of ensuing bone marrow depression including whole blood or platelet transfusion and antibiotics. Maintain vital functions.
Storage Condition
IV/SC: Store between 15-25°C. Intrathecal: Store between 2-8°C. Avoid freezing.
Innovators Monograph
You find simplified version here Cytarabin
Cytarabin contains Cytarabine see full prescribing information from innovator Cytarabin Monograph, Cytarabin MSDS, Cytarabin FDA label
