section name header

Pronunciation

sye-TARE-a-been

Classifications

Therapeutic Classification: antineoplastics

Pharmacologic Classification: antimetabolites

Indications

High Alert


Action

  • Inhibits DNA synthesis by inhibiting DNA polymerase (cell-cycle S-phase–specific).
Therapeutic effects:
  • Death of rapidly replicating cells, particularly malignant ones.

Pharmacokinetics

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.

Time/Action Profile

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

ROUTEONSETPEAKDURATION
SUBQ, IV (1st phase)24 hr7–9 days12 days
SUBQ, IV (2nd phase)15–24 days15–24 days25–34 days
ITrapid5 hr14–28 days



Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

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

Interactions

Drug-drug:

Route/Dosage

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

IV Administration:

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Cytosar-U

Code

NDC Code