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Pronunciation(KLA dri been)
U.S. Brand NamesLeustatin®
Synonyms2-CdA; 2-Chlorodeoxyadenosine
Generic AvailableYes
Canadian Brand NamesLeustatin®
UseTreatment of hairy cell leukemia, chronic lymphocytic leukemia (CLL), chronic myelogenous leukemia (CML)
Use - Unlabeled/InvestigationalNon-Hodgkin's lymphomas, progressive multiple sclerosis
Pregnancy Risk FactorD
LactationEnters breast milk/contraindicated
ContraindicationsHypersensitivity to cladribine or any component of the formulation; pregnancy
Warnings/PrecautionsThe U.S. Food and Drug Administration (FDA) currently recommends that procedures for proper handling and disposal of antineoplastic agents be considered. Use with caution in patients with pre-existing hematologic or immunologic abnormalities.
Adverse Reactions>10%: Allergic: Fever (70%), chills (18%); skin reactions (erythema, itching) at the catheter site (18%) Central nervous system: Fatigue (17%), headache (13%) Dermatologic: Rash Hematologic: Myelosuppression, common, dose-limiting; leukopenia (70%); anemia (37%); thrombocytopenia (12%) Nadir: 5-10 days Recovery: 4-8 weeks 1% to 10%: Cardiovascular: Edema, tachycardia Central nervous system: Dizziness; pains; chills; malaise; severe infection, possibly related to thrombocytopenia Dermatologic: Pruritus, erythema Gastrointestinal: Nausea, mild to moderate, usually not seen at doses <0.3 mg/kg/day; constipation; abdominal pain Neuromuscular & skeletal: Myalgia, arthralgia, weakness Renal: Renal failure at high (>0.3 mg/kg/day) doses Miscellaneous: Diaphoresis, delayed herpes zoster infection, tumor lysis syndrome <1%, postmarketing and/or case reports: Paraparesis, quadriplegia (reported at high doses); increased risk of opportunistic infection
Ethanol/Nutrition/Herb InteractionsEthanol: Avoid ethanol (due to GI irritation).
StabilityStore intact vials under refrigeration 2°C to 8°C (36°F to 46°F). Dilutions in 500 mL NS are stable for 72 hours. Stable in PVC containers for 24 hours at room temperature of 15°C to 30°C (59°F to 86°F) and 7 days in Pharmacia Deltec® cassettes. Solutions for 7-day infusion should be prepared in bacteriostatic NS.
CompatibilityStable in NS; incompatible with D5WY-site administration: Compatible: Aminophylline, bumetanide, buprenorphine, butorphanol, calcium gluconate, carboplatin, chlorpromazine, cimetidine, cisplatin, cyclophosphamide, cytarabine, dexamethasone sodium phosphate, diphenhydramine, dobutamine, dopamine, doxorubicin, droperidol, enalaprilat, etoposide, famotidine, furosemide, granisetron, haloperidol, heparin, hydrocortisone sodium phosphate, hydrocortisone sodium succinate, hydromorphone, hydroxyzine, idarubicin, leucovorin, lorazepam, mannitol, meperidine, mesna, methylprednisolone sodium succinate, metoclopramide, mitoxantrone, morphine, nalbuphine, ondansetron, paclitaxel, potassium chloride, prochlorperazine edisylate, promethazine, ranitidine, sodium bicarbonate, teniposide, vincristine
Mechanism of ActionA purine nucleoside analogue; prodrug which is activated via phosphorylation by deoxycytidine kinase to a 5'-triphosphate derivative. This active form incorporates into DNA to result in the breakage of DNA strand and shutdown of DNA synthesis. This also results in a depletion of nicotinamide adenine dinucleotide and adenosine triphosphate (ATP). Cladribine is cell-cycle nonspecific.
Pharmacodynamics/KineticsAbsorption: Oral: 55%; SubQ: 100%; Rectal: 20% Distribution: Vd: 4.52 ± 2.82 L/kg Protein binding, plasma: 20% Metabolism: Hepatic; 5'-triphosphate moiety-active Half-life elimination: Biphasic: Alpha: 25 minutes; Beta: 6.7 hours; Terminal, mean: Normal renal function: 5.4 hours Excretion: Urine (21% to 44%) Clearance: Estimated systemic: 640 mL/hour/kg
DosageI.V.: Refer to individual protocols.Pediatrics: Acute leukemias: 6.2-7.5 mg/m2/day continuous infusion for days 1-5; maximum tolerated dose was 8.9 mg/m2/day. Adults: Hairy cell leukemia: Continuous infusion: 0.09-0.1 mg/kg/day days 1-7; may be repeated every 28-35 days or 3.4 mg/m2/day SubQ days 1-7 Chronic lymphocytic leukemia: Continuous infusion: 0.1 mg/kg/day days 1-7 or 0.028-0.14 mg/kg/day as a 2-hour infusion days 1-5 Chronic myelogenous leukemia: 15 mg/m2/day as a 1-hour infusion days 1-5; if no response increase dose to 20 mg/m2/day in the second course.
AdministrationI.V.: Administer as a 1- to 2-hour infusion or by continuous infusion
Monitoring ParametersMonitor periodic assessment of peripheral blood counts, particularly during the first 4-8 weeks post-treatment, is recommended to detect the development of anemia, neutropenia, and thrombocytopenia and for early detection of any potential sequelae (ie, infection or bleeding)
Patient EducationInform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. This drug can only be administered by infusion. It is important to maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake, and nutrition during therapy (small, frequent meals may help). You will be more susceptible to infection during therapy and for up to 1 year following therapy (avoid crowds and exposure to infection and do not have any vaccinations without consulting prescriber). May cause nausea or vomiting (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); muscle weakness or pain (consult prescriber for mild analgesics); or mouth sores (use frequent mouth care with soft toothbrush or cotton swabs and frequent mouth rinses). Report immediately rash, unusual excessive fatigue, and/or signs of infection. Report rapid heartbeat or palpitations; unusual bruising or bleeding; persistent GI disturbances; diarrhea or constipation; yellowing of eyes or skin; change in color of urine or stool; swelling, warmth, or pain in extremities; or difficult respirations. Pregnancy/breast-feeding precautions: Do not get pregnant while taking this medication. Consult prescriber for appropriate contraceptive measures. Do not breast-feed until prescriber advises it is safe.
Dental Health: Effects on Dental TreatmentNo significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic PrecautionsNo information available to require special precautions
Mental Health: Effects on Mental StatusMay cause drowsiness, dizziness, or insomnia
Mental Health: Effects on Psychiatric TreatmentMay cause bone marrow suppression; use caution with clozapine and carbamazepine
Oncology: Emetic PotentialVery low (<10%)
Oncology: VesicantNo
Dosage FormsInjection, solution [preservative free]: 1 mg/mL (10 mL)
ReferencesBaltz JK and Montello MJ, "Cladribine for the Treatment of Hematologic Malignancies,"Clin Pharm, 1993, 12(11):805-13. Beutler E, "Cladribine (2-Chlorodeoxyadenosine),"Lancet, 1992, 340(8825):952-6. Kearns CM, Biakley RL, Santane VM, et al, "Pharmacokinetics of Cladribine (2-Chlorodioxyadenosine) in Children with Acute Leukemia,"Cancer Research, 1994, 54:1235-39. Larson RA, et al, "Dose Escalation Trial of Cladribine Using 5 Daily I.V. Infusions in Patients with Advanced Hematologic Malignancies,"J Clin Oncol, 1996, 14(1):188-95. Liliemark J, "The Clinical Pharmacokinetics of Cladribine,"Clin Pharmacokinet, 1997, 32(2):120-31. Piro LD, "2-Chlorodeoxyadenosine Treatment of Lymphoid Malignancies,"Blood, 1992, 79(4):843-5. Robak T, "Cladribine in the Treatment of Chronic Lymphocytic Leukemia,"Leuk Lymphoma, 2001, 40(5-6):551-64. Saven A and Piro LD, "2-Chlorodeoxyadenosine: A Potent Antimetabolite With Major Activity in the Treatment of Indolent Lymphoproliferative Disorders,"Hematol Cell Ther, 1996, 38(Suppl 2):93-101. Stine KC, Saylors RL, Williams LL, et al, "2-Chlorodeoxyadenosine (2-CDA) for the Treatment of Refractory or Recurrent Langerhans Cell Histiocytosis (LCH) in Pediatric Patients,"Med Pediatr Oncol, 1997, 29:288-92. Tallman MS and Hakimian D, "Current Results and Prospective Trials of Cladribine in Chronic Lymphocytic Leukemia,"Semin Hematol, 1996, 33(Suppl 1):23-7. Tortorella C, Rovaris M, and Filippi M, "Cladribine. Ortho Biotech Inc,"Curr Opin Investig Drugs, 2001, 2(12):1751-6.
International Brand NamesBiodribin® (PL); Intocel® (AR); Leustat® (AR, GB); Leustatin® (AT, AU, BE, BG, BR, CA, CH, CR, CZ, DE, DK, DO, ES, FI, GT, HN, HR, IL, IT, LU, NL, NO, NZ, PA, SE, SV, TH); Leustatine® (FR); Litak® (CH, DE, IL, RO)
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