• IV: Treatment of leukemias and non-Hodgkin’s lymphomas (in combination with other agents).
• IT: Prophylaxis and treatment of meningeal leukemia.

Contraindicated in:

• Hypersensitivity
• Active meningeal infection (IT only);OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• Active infection
• ↓bone marrow reserve
• Renal impairment
• Hepatic impairment
• Women of reproductive potential.

CV: edema.

Derm: alopecia, rash.

EENT: corneal toxicity (high dose), hemorrhagic conjunctivitis (high dose), visual disturbances (including blindness).

GI: nausea, vomiting, GI ulceration (high dose), HEPATOTOXICITY, stomatitis.

GU: sterility, urinary incontinence.

Hemat: (less with IT use): anemia, leukopenia, thrombocytopenia.

Metab: hyperuricemia.

Neuro: IT: abnormal gait, CHEMICAL ARACHNOIDITIS, CNS dysfunction (high dose), confusion, drowsiness, headache.

Resp: PULMONARY EDEMA (HIGH DOSE).
Misc: cytarabine syndrome, fever.

Drug-Drug:

• ↑bone marrow depression with other antineoplastics or radiation therapy.
• ↑risk of cardiomyopathy when used in high-dose regimens with cyclophosphamide.
• May ↓ antibody response to live-virus vaccines and ↑ risk of adverse reactions.
• May ↓ absorption of digoxin tablets.
• May ↓ the efficacy of gentamicin when used to treat Klebsiella pneumoniae infections.
• Recent treatment with asparaginase may ↑ risk of pancreatitis.
• ↑risk of neurotoxicity with concurrently administered IT antineoplastics (IT only).

(Generic available)

• Solution for injection: 20 mg/mL; 100 mg/mL;
• In combination with: daunorubicin (Vyxeos). See Appendix [not included in this PDA edition].

• IV (Adults): Induction dose: 200 mg/m²/day for 5 days every 2 wk as a single agent or 2–6 mg/kg/day (100–200 mg/m²/day) as a single daily dose or in 2–3 divided doses for 5–10 days or until remission occurs as part of combination chemotherapy. Maintenance: 70–200 mg/m²/day for 2–5 days monthly. Refractory leukemias/lymphomas: 3 g/m² every 12 hr for up to 12 doses.
• SC (Adults): Maintenance: 1–1.5 mg/kg every 1–4 wk.
• IT (Adults): Usual dose = 30 mg/m² every 4 days; range = 5–75 mg/m² once daily for 4 days or every 4 days until CNS findings normalize, followed by one additional treatment.

Cytosar-U

• Inhibits DNA synthesis by inhibiting DNA polymerase (cell-cycle S-phase–specific).

• Death of rapidly replicating cells, particularly malignant ones.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: antimetabolites

Absorption: Absorption occurs from SUBQ sites, but blood levels are lower than with IV administration; IT administration results in negligible systemic exposure.

Distribution: Widely distributed; IV- and SUBQ-administered cytarabine crosses the blood-brain barrier but not in sufficient quantities.

Metabolism/Excretion: Metabolized mostly by the liver; <10% excreted unchanged by the kidneys. Metabolism to inactive drug in the CSF is negligible because the enzyme that metabolizes it is present in very low concentrations in the CSF.

Half-life: IV, SUBQ: 1–3 hr; IT: 100–236 hr.

(IV, SUBQ — effects on WBCs; IT — levels in CSF)

• : Caution patient to avoid crowds and persons with known infections. Report symptoms of infection (fever, chills, cough, hoarseness, sore throat, lower back or side pain, painful or difficult urination) immediately.
• Instruct patient to report unusual bleeding. Advise patient of thrombocytopenia precautions (use soft toothbrush and electric razor, avoid falls, do not drink alcoholic beverages or take medication containing aspirin or NSAIDs; may precipitate gastric bleeding).
• Instruct patient to inspect oral mucosa for redness and ulceration. If mouth sores occur, advise patient to use sponge brush and rinse mouth with water after eating and drinking. Stomatitis may require treatment with opioid analgesics.
• Instruct patient not to receive any vaccinations without advice of health care professional.
• Advise patient that this medication may have teratogenic effects. Contraception should be used during therapy and for at least 4 mo after therapy is concluded.
• Emphasize the need for periodic lab tests to monitor for side effects.
• IT: Inform patient about the expected side effects (headache, nausea, vomiting, fever) and about early signs of neurotoxicity. Instruct patient to notify health care professional if these signs occur.

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