Cytarabine

Trade Names:
Cytosar-U
- Sterile powder for reconstitution 100 mg, 500 mg, 1 g, 2 g vials

Pharmacology

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Cytarabine exhibits cell-phase specificity, primarily killing cells undergoing DNA synthesis (S-phase) and under certain conditions, blocking the progression of cells from the G ₁ -phase to the S-phase.

Pharmacokinetics

Distribution

Distribution t _½ is about 10 min.

Metabolism

Metabolized by deoxycytidine kinase and other nucleotide kinases to nucleotide triphosphate (active). Inactivated by a pyrimidine nucleotide deaminase to nontoxic uracil derivative.

Elimination

Elimination t _½ is about 1 to 3 h. About 80% is excreted in the urine within 24 h (90% of which is excreted as ara-U).

Indications and Usage

Acute lymphocytic leukemia, acute and chronic myelocytic leukemia, meningeal leukemia, erythroleukemia, non-Hodgkin lymphoma.

Unlabeled Uses

Hodgkin disease, bone marrow transplantation.

Contraindications

Standard considerations.

Dosage and Administration

Continuous IV infusion or rapid injection 100 to 200 mg/m ² /day or 3 mg/kg/day as a continuous IV infusion over 24 h or in divided doses by rapid injection for 5 to 10 days with the courses repeated about every 2 wk.

Continuous IV infusion or rapid injection 100 to 200 mg/m ² /day as a continuous IV infusion over 24 h or in divided doses by rapid injection for 5 to 10 days with the courses repeated about every 2 wk.

Subcutaneous 1 mg/kg/dose 1 or 2 times/wk.

Subcutaneous or IM 1 to 1.5 mg/kg/dose every 1 to 4 wk.

70 to 200 mg/m ² /day IV for 2 to 5 days repeated every mo.

Continuous infusion 100 mg/m ² /day on days 1 through 7, or 100 mg/m ² every 12 h for 7 days.

Cytarabine 10 mg/m ² /dose subcutaneously twice daily for 7 to 14 days in combination with other chemotherapeutic drugs.

Continuous infusion 100 mg/m ² /day on days 1 through 7, or 100 mg/m ² every 12 h for 7 days.

IV 2,000 to 3,000 mg/m ² every 12 h for 2 to 6 days. Suspend or modify the dose of cytarabine if ANC is less than 1,000/mm ³ or the platelet count is less than 50,000/mm ³ .

IV 1,000 to 3,000 mg/m ² every 12 h for 2 to 6 days. Suspend or modify the dose of cytarabine if ANC is less than 1,000/mm ³ or the platelet count is less than 50,000/mm ³ .

May require dosage reduction; specific guidelines not established.

Follow dosage adjustment guidelines recommended for adults.

Intrathecally to 75 mg/m ² at intervals ranging from once a day for 4 days to once every 4 days (range, 2 to 7 days).

Intrathecally to 75 mg/m ² at intervals ranging from once a day for 4 days to once every 4 days (range, 2 to 7 days). Many clinicians recommend dosing intrathecal cytarabine by the child's age.

Prophylactic use of corticosteroid eye drops decreases the risk of conjunctivitis or keratitis. Begin prophylactic therapy prior to chemotherapy and continue for 48 h after the last dose of cytarabine.

General Advice

• Administer by subcutaneous/IM injection, by IV injection or infusion, or intrathecally.
• Rotate injection sites for subcutaneous/IM administration.

• High dose
• Dilute with preservative-free sodium chloride 0.9%.
• Give IV infusion over 1 to 3 h.

• Intrathecal
• Dilute with an isotonic buffered diluent without preservative such as Lactated Ringer's injection or sodium chloride 0.9%.

• IV infusion
• Reconstitute with bacteriostatic water for injection (with 0.9% benzyl alcohol). May be further diluted with greater than 50 mL of sodium chloride 0.9% for IV infusion.
• Give by bolus injection over 1 to 3 min through a running IV line; infuse IV over 15 min in greater than 50 mL of sodium chloride 0.9%; continuous IV infusion over 5 days. Cytarabine doses are often infused over 30 min.

• Subcutaneous/IM
• Smaller volumes of diluent can be used to prepare a 100 mg/mL solution for subcutaneous/IM injection.

Storage/Stability

• Store at room temperature.
• When reconstituted with bacteriostatic water for injection (with benzyl alcohol), cytarabine is stable for 2 days at room temperature. Use preservative-free cytarabine solutions within 24 h of reconstitution. Discard if solution appears hazy.
• Diluted cytarabine solutions (concentration 0.5 mg/mL) are stable for 8 days at room temperature when diluted with sterile water, sodium chloride 0.9%, or dextrose 5%.

Drug Interactions

Prior therapy with L-asparaginase may increase the risk of acute pancreatitis.

Oral absorption of digoxin may be decreased.

Gentamicin effectiveness against Klebsiella pneumoniae strains may be decreased.

Cytarabine may decrease the oral absorption of quinolone antibiotics.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache, dizziness; seizures, cerebral or cerebellar dysfunction presenting as personality changes, somnolence, coma, ataxia, dysarthria, and nystagmus (high dose); sensory neuropathy (high dose); necrotizing leukoencephalopathy with intrathecal cytarabine and cranial radiation.

Dermatologic

Rash; cellulitis; thrombophlebitis; palmar-plantar erythrodysesthesia; severe rash with desquamation (high dose).

GI

Nausea; vomiting; anorexia; mucositis; diarrhea; transient elevation of LFTs; neutropenic colitis; severe GI ulceration (high dose).

Hematologic

Bone marrow suppression.

Respiratory

Pulmonary edema, diffuse interstitial pneumonitis (high dose).

Miscellaneous

Cytarabine syndrome; arthralgias; myalgias; chest pain; fever; general feeling of discomfort or weakness; reddened eyes; skin rash.

Special Senses

Hemorrhagic conjunctivitis, corneal toxicity, photophobia (high dose).

Precautions

Pregnancy

Category D .

Lactation

Undetermined.

Children

Conventional cytarabine is indicated for use in children.

Hypersensitivity

Cases of anaphylaxis have occurred resulting in acute cardiopulmonary arrest which required resuscitation. This occurred immediately after IV administration.

Renal Function

Patients with renal function impairment may have a higher likelihood of CNS toxicity after high-dose cytarabine. Use the drug with caution and possibly at reduced doses in patients with poor kidney function.

Hepatic Function

Patients with hepatic function impairment may have a higher likelihood of CNS toxicity after high-dose cytarabine. Use the drug with caution and possibly at reduced doses in patients with poor liver function.

Benzyl alcohol

Benzyl alcohol is contained in the diluent for some conventional cytarabine products. Benzyl alcohol has been reported to be associated with a fatal “gasping syndrome” in premature infants. Do not use conventional cytarabine injection with benzyl alcohol intrathecally.

Extravasation risk

May cause local irritation or phlebitis. Refer to your institution specific protocol.

Infection

Viral, bacterial, fungal, parasitic, or saprophytic infections in any location in the body may be associated with the use of cytarabine alone or in combination with other immunosuppressive agents.

Hyperuricemia

Hyperuricemia may occur because of rapid cell lysis; monitor serum uric acid. Minimize effects of hyperuricemia with hydration, urinary alkalinization, and allopurinol.

Intrathecal use

If used intrathecally, do not use a diluent with benzyl alcohol.

Neuropathies

Peripheral motor and sensory neuropathies have occurred.

Neurotoxicity

Enhanced neurotoxicity has been associated with concurrent use of intrathecal cytarabine and other cytotoxic agents administered intrathecally.

Patient Information

• Inform patients about the expected adverse reactions of headache, nausea, vomiting, and fever, and about the early signs and symptoms of neurotoxicity. Instruct patients to seek medical attention if signs or symptoms of neurotoxicity develop, or if oral dexamethasone is not well tolerated.

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