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Pronunciation(PEN toe stat in)
U.S. Brand NamesNipent®
SynonymsCL-825; Co-Vidarabine; dCF; Deoxycoformycin; 2'-Deoxycoformycin; NSC-218321
Generic AvailableNo
Canadian Brand NamesNipent®
UseTreatment of hairy cell leukemia; non-Hodgkin's lymphoma, cutaneous T-cell lymphoma
Pregnancy Risk FactorD
Pregnancy ImplicationsPentostatin has been found to be teratogenic in animals. There are no adequate and well-controlled studies in humans. Women of childbearing potential should be advised to avoid becoming pregnant. If used during pregnancy, the patient should be apprised of the potential risk to the fetus.
LactationExcretion in breast milk unknown/contraindicated
ContraindicationsHypersensitivity to pentostatin or any component; pregnancy
Warnings/PrecautionsUse cautiously in patients with bone marrow suppression, renal or hepatic dysfunction.
Adverse Reactions>10%: Central nervous system: Fever, chills, headache Dermatologic: Skin rash (25% to 30%), alopecia (10%) Gastrointestinal: Mild to moderate nausea, vomiting (60%), stomatitis, diarrhea (13%), anorexia Genitourinary: Acute renal failure (35%) Hematologic: Thrombocytopenia (50%), dose-limiting in 25% of patients; anemia (40% to 45%), neutropenia, mild to moderate, not dose-limiting (11%) Nadir: 7 days Recovery: 10-14 days Hepatic: Transaminases increased, mild-moderate, usually transient (30%); hepatitis (19%), usually reversible Respiratory: Pulmonary edema (15%), may be exacerbated by fludarabine Miscellaneous: Infection (57%; 35% severe, life-threatening) 1% to 10%: Cardiovascular: Chest pain, arrhythmia, peripheral edema Central nervous system: Opportunistic infection (8%); anxiety, confusion, depression, dizziness, insomnia, nervousness, somnolence, myalgia, malaise Dermatologic: Dry skin, eczema, pruritus Gastrointestinal: Constipation, flatulence, weight loss Neuromuscular & skeletal: Paresthesia, weakness Ocular: Moderate to severe keratoconjunctivitis, abnormal vision, eye pain Otic: Ear pain Respiratory: Dyspnea, pneumonia, bronchitis, pharyngitis, rhinitis, epistaxis, sinusitis (3% to 7%) <1%: Dysuria, hematuria, hypersensitivity reactions, BUN increased, thrombophlebitis; lethargy, seizure, coma (uncommon at doses <4 mg/m2)
Overdosage/ToxicologySymptoms of overdose include severe renal, hepatic, pulmonary, and CNS toxicity. Treatment is supportive.
Drug InteractionsIncreased toxicity: Vidarabine, allopurinol; combined use with fludarabine may lead to severe, even fatal, pulmonary toxicity
StabilityVials are stable under refrigeration at 2°C to 8°C; reconstituted vials, or further dilutions, may be stored at room temperature exposed to ambient light. Reconstitute with SWFI to a concentration of 2 mg/mL. The injection may be further diluted with 25-50 mL NS or D5W for infusion. Diluted solutions are stable for 24 hours in D5W or 48 hours in NS or lactated Ringer's at room temperature. Infusion with 5% dextrose injection USP or 0.9% sodium chloride injection USP does not interact with PVC-containing administration sets or containers.
CompatibilityStable in LR, NS; variable stability (consult detailed reference) in D5WY-site administration: Compatible: Fludarabine, melphalan, ondansetron, paclitaxel, sargramostim
Mechanism of ActionPentostatin is a purine antimetabolite that inhibits adenosine deaminase, preventing the deamination of adenosine to inosine. Accumulation of deoxyadenosine (dAdo) and deoxyadenosine 5'-triphosphate (dATP) results in a reduction of purine metabolism and DNA synthesis and cell death.
Pharmacodynamics/KineticsDistribution: I.V.: Vd: 36.1 L (20.1 L/m2); rapidly to body tissues Half-life elimination: Distribution half-life: 30-85 minutes; Terminal: 5-15 hours Excretion: Urine (~50% to 96%) within 24 hours (30% to 90% as unchanged drug)
DosageRefractory hairy cell leukemia: Adults (refer to individual protocols):4 mg/m2 every other week or 4 mg/m2 weekly for 3 weeks, then every 2 weeks or 5 mg/m2 daily for 3 days every 3 weeks Dosing interval in renal impairment: Clcr<60 mL/minute: Use extreme caution Clcr 50-60 mL/minute: 2 mg/m2/dose
AdministrationAdminister I.V. as a 15- to 30-minute infusion; continuous infusion regimens have been reported, but are not commonly usedI.V. bolus over
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 given by infusion on a specific schedule. Report immediately any redness, swelling, burning, or pain at infusion site; or signs of hypersensitivity (eg, respiratory difficulty or swallowing, chest tightness, rash, hives, swelling of lips or mouth). Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. You may be more susceptible to infection (avoid crowds and exposure to infection and do not have any vaccinations without consulting prescriber). May cause nausea and vomiting, or loss of appetite (small, frequent meals or frequent mouth care may help - or request medication from prescriber); headache (consult prescriber for approved analgesic); dizziness, confusion or lethargy (use caution when driving); or mouth sores (use frequent oral care with soft toothbrush or cotton swabs). Report signs of infection (eg, fever, chills, sore throat, mouth sores, burning urination, perianal itching, or vaginal discharge); unusual bruising or bleeding (eg, tarry stools, blood in urine, stool, or vomitus); vision changes or hearing; muscle tremors, weakness, or pain; CNS changes (eg, hallucinations, confusion, insomnia, seizures); or respiratory difficulty. Pregnancy/breast-feeding precautions: Do not get pregnant while taking this medication. Consult prescriber for appropriate contraceptive measures. Do not breast-feed.
Dental Health: Effects on Dental TreatmentKey adverse event(s) related to dental treatment: Stomatitis.
Dental Health: Vasoconstrictor/Local Anesthetic PrecautionsNo information available to require special precautions
Mental Health: Effects on Mental StatusSedation is common; may cause anxiety, confusion, insomnia, depression
Mental Health: Effects on Psychiatric TreatmentLeukopenia is common; avoid clozapine and carbamazepine
Oncology: Emetic PotentialModerate (30% to 60%)
Oncology: VesicantNo
Dosage FormsInjection, powder for reconstitution: 10 mg
ReferencesBrogden RN and Sorkin EM, "Pentostatin. A Review of Its Pharmacodynamic and Pharmacokinetic Properties, and Therapeutic Potential in Lymphoproliferative Disorders,"Drugs, 1993, 46(4):652-77. Catovsky D, "Clinical Experience With 2'-Deoxycoformycin,"Hematol Cell Ther, 1996, 38(Suppl 2):103-7. Dillman RO, "A New Chemotherapeutic Agent: Deoxycoformycin (Pentostatin),"Semin Hematol, 1994, 31(1):16-27. Kane BJ, Kuhn JG, and Roush MK, "Pentostatin: An Adenosine Deaminase Inhibitor For the Treatment of Hairy Cell Leukemia,"Ann Pharmacother, 1992, 26(7-8):939-47. Spiers AS, "The Role of Pentostatin (2'-Deoxycoformycin, dCF) in the Management of Lymphoproliferative Malignancies,"Blood Rev, 1987, 1(2):106-10.
International Brand NamesNipent® (CA, DE, ES, FR, GB, IT, NL)
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3-5 minutes in D5W or NS at concentrations 