CLADRIBINE
(cla'dri-been)
Leustatin
Classifications: antineoplastic; antimetabolite, purine antagonist
Prototype: 6-mercaptopurine
Pregnancy Category: D

Availability

1 mg/mL injection

Actions

Cladribine is a synthetic antineoplastic agent with selective toxicity toward certain normal and malignant lymphocytes and monocytes. It accumulates intracellularly, preventing repair of single-stranded DNA breaks and ultimately interfering with cellular metabolism and DNA synthesis.

Therapeutic Effects

Cladribine is cytotoxic to both actively dividing and quiescent lymphocytes and monocytes, inhibiting both DNA synthesis and repair.

Uses

Treatment of hairy cell leukemia.

Unlabeled Uses

Advanced cutaneous T-cell lymphomas, chronic lymphocytic leukemia, non-Hodgkin's lymphomas, acute myeloid leukemia, autoimmune hemolytic anemia, mycosis fungoides.

Contraindications

Hypersensitivity to cladribine; pregnancy (category D).

Cautious Use

Hepatic or renal impairment. Safety and efficacy in children not established.

Route & Dosage

Hairy Cell Leukemia
Adult: IV 0.09 mg/kg/d by 7 d continuous infusion

Chronic Lymphocytic Leukemia
Adult: IV 0.1 mg/kg/d by 7 d continuous infusion or 0.028–0.14 mg/kg/d as 2 h infusion for 5 consecutive d

Administration

Intravenous

PREPARE: IV Infusion (single daily dose): IV infusion (7-day dose): The calculated dose of cladribine is injected into an infusion reservoir using a 0.22 micron filter. An amount of bacteriostatic NS is added through a 0.22 micron filter to bring the total to 100 mL. (Note: reservoir usually prepared by the pharmacist.)  

ADMINISTER: IV Infusion (single daily dose): Distribute evenly over ordered time (i.e., 2 h or 24 h).  IV infusion (7-day dose): Give through a central line and control by a pump device (e.g., Deltec pump) to deliver 100 mL evenly over 7 d.  

INCOMPATIBILITIES Solution/additive: Do not mix with any other diluents or drugs.

Adverse Effects (1%)

CNS: Headache, dizziness. GI: Nausea, diarrhea. Hematologic: Myelosuppression (neutropenia), anemia, thrombocytopenia. Metabolic: Fever. CNS: Headache, dizziness. Urogenital: Elevated serum creatinine.

Interactions

Drug: Additive risk of bleeding with anticoagulants, nsaids, platelet inhibitors, salicylates.

Pharmacokinetics

Onset: Therapeutic effect 10 d to 4 mo. Duration: 7–25+ mo. Distribution: Crosses placenta; distributed into breast milk. Metabolism: In malignant leukocytes, cladribine is phosphorylated to form its monophosphate and triphosphate forms, presumably its active forms, which are subsequently incorporated into cellular DNA. Half-Life: Initial 35 min, terminal 6.7 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug