Trade Names:Leustatin- Solution for injection 1 mg/mL
The selective toxicity of cladribine toward certain normal and malignant lymphocyte and monocyte populations is based on the relative activities of deoxycytidine kinase, deoxynucleotidase, and adenosine deaminase. In cells with a high ratio of deoxycytidine kinase to deoxynucleotidase, cladribine passively crosses the cell membrane. Cladribine is cytotoxic to actively dividing and quiescent lymphocytes and monocytes, inhibiting DNA synthesis and repair.
Vd is about 4.5 L/kg. About 20% protein bound.
The t ½ is about 5.4 h. Cl is about 978 mL/h/kg.
Hairy cell leukemia.
Chronic lymphocytic leukemia, non-Hodgkin lymphoma, acute myeloid leukemia.
Continuous IV infusion 0.09 mg/kg/day for 7 days, single course. It can be prepared each day as a 24-h infusion or as a single dose to infuse over 7 days in an ambulatory infusion pump. For patients weighing more than 85 kg, preparation of a single dose for administration over 7 days is not advised because solutions may be inadequately preserved because of increased dilution of benzyl alcohol.
Store vials in refrigerator and protect from light. May be frozen. If frozen, allow to thaw at room temperature. Do not heat, microwave, or refreeze. After dilution, cladribine solution may be stored in the refrigerator for up to 8 h prior to administration.
None well documented.
None well documented.
Fatigue; headache; dizziness; insomnia.
Rash; injection-site reactions.
Bone marrow suppression; decreased CD4 count.
WarningsBone marrow suppression
Severe bone marrow suppression, including neutropenia, anemia, and thrombocytopenia, has been observed in patients treated with cladribine, especially at high doses.Nephrotoxicity
Associated with high dose and concurrent nephrotoxic drugs.Neurotoxicity
Severe cases more common with continuous high-dose infusions. Serious neurological toxicity (including irreversible paraparesis and quadraparesis) has been reported with doses 4 to 9 times the recommended dose for hairy cell leukemia. Severe neurological toxicity has been rarely reported with standard dosing regimens.
Monitor CBC at baseline and for 4 to 8 wk after therapy.Hyperuricemia
May occur because of rapid cell lysis; monitor serum uric acid. Minimize effects of hyperuricemia with hydration, urinary alkalinization, and allopurinol.Neurologic exam
Perform baseline neurologic exam and monitor for 4 to 12 wk after therapy.Renal function
Assess renal function at baseline and throughout therapy.
Category D .
Safety and efficacy not established.
Local irritation or phlebitis may occur. Refer to the institution's specific protocol.
Fever 37.8°C (100°F or higher) was associated with the use of cladribine in about 66% of patients in the first month of therapy.
Irreversible neurologic toxicity (paraparesis/quadriparesis); acute nephrotoxicity; severe bone marrow suppression resulting in neutropenia, anemia, and thrombocytopenia.
Copyright © 2009 Wolters Kluwer Health.