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Pronunciation |
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(PEN
toe stat
in) |
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U.S. Brand
Names |
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Nipent™ |
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Generic
Available |
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No |
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Synonyms |
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DCF; Deoxycoformycin; 2'-deoxycoformycin |
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Pharmacological Index |
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Antineoplastic Agent, Antibiotic |
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Use |
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Treatment of adult patients with alpha-interferon-refractory hairy cell
leukemia; non-Hodgkin's lymphoma, cutaneous T-cell lymphoma |
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Pregnancy Risk
Factor |
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D |
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Contraindications |
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Limited or severely compromised bone marrow reserves (white blood cell count
<3000 cells/mm3) |
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Warnings/Precautions |
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The FDA currently recommends that procedures for proper handling and disposal
of antineoplastic agents be considered. Pregnant women or women of childbearing
age should be apprised of the potential risk to the fetus; use extreme caution
in the presence of renal insufficiency; use with caution in patients with signs
or symptoms of impaired hepatic function. |
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Adverse
Reactions |
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>10%:
Central nervous system: Headache, neurologic disorder, fever, fatigue,
chills, pain
Dermatologic: Rash
Gastrointestinal: Vomiting, nausea, anorexia, diarrhea
Hematologic: Leukopenia, anemia, thrombocytopenia
Hepatic: Hepatic disorder, abnormal LFTs
Neuromuscular & skeletal: Myalgia
Respiratory: Coughing
Miscellaneous: Allergic reaction
1% to 10%:
Cardiovascular: Chest pain, arrhythmia, peripheral edema
Central nervous system: Anxiety, confusion, depression, dizziness, insomnia,
lethargy, coma, seizures, malaise
Dermatologic: Dry skin, eczema, pruritus
Gastrointestinal: Constipation, flatulence, stomatitis, weight loss
Genitourinary: Dysuria
Hematologic: Myelosuppression
Hepatic: Liver dysfunction
Local: Thrombophlebitis
Neuromuscular & skeletal: Arthralgia, paresthesia, back pain, weakness
Ocular: Abnormal vision, eye pain, keratoconjunctivitis
Otic: Ear pain
Renal: Renal failure, hematuria
Respiratory: Bronchitis, dyspnea, lung edema, pneumonia
Miscellaneous: Death, opportunistic infections, diaphoresis
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Overdosage/Toxicology |
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Symptoms of overdose include severe renal, hepatic, pulmonary, and CNS
toxicity
Supportive therapy |
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Drug
Interactions |
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Increased toxicity: Vidarabine, fludarabine, allopurinol |
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Stability |
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Vials 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; 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 |
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Mechanism of
Action |
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An antimetabolite inhibiting adenosine deaminase (ADA), prevents ADA from
controlling intracellular adenosine levels through the irreversible deamination
of adenosine and deoxyadenosine. ADA is found to exhibit the highest activity in
lymphoid tissue. Patients receiving pentostatin accumulate deoxyadenosine (dAdo)
and deoxyadenosine 5'-triphosphate (dATP); accumulation of dATP results in cell
death, probably through inhibiting DNA or RNA synthesis. Following a single
dose, pentostatin has the ability to inhibit ADA for periods exceeding 1
week. |
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Pharmacodynamics/Kinetics |
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Distribution: I.V.: Vd: 36.1 L (20.1 L/m2); distributes
rapidly to body tissues and may obtain plasma concentrations ranging from 12-36
ng following doses of 250 mcg/kg for 4-5 days
Half-life, terminal: 5-15 hours
Elimination: ~50% to 96% is recovered in urine within 24 hours
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Usual Dosage |
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Refractory hairy cell leukemia: Adults (refer to individual protocols): 4
mg/m2 every other week; I.V. bolus over greater than or equal to 3-5
minutes in D5W or NS at concentrations greater than or equal to 2
mg/mL
Clcr <60 mL/minute: Use extreme caution
Clcr 50-60 mL/minute: 2 mg/m2/dose
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Mental Health: Effects
on Mental Status |
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Sedation is common; may cause anxiety, confusion, insomnia,
depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Leukopenia is common; avoid clozapine and carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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This drug can only be administered by infusion on a specific schedule.
Frequent blood tests and monitoring will be necessary. Maintain adequate
hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You
may experience nausea and vomiting, diarrhea, or loss of appetite (frequent
small meals or frequent mouth care may help or request medication from
prescriber); dizziness, weakness, or lethargy (use caution when driving);
susceptibility to infections (avoid crowds and exposure to infection). Use
frequent oral care with soft toothbrush or cotton swabs to reduce incidence of
mouth sores. May cause headache (request medication). Report signs of infection
(eg, fever, chills, sore throat, mouth sores, burning urination, perianal
itching, or vaginal discharge); unusual bruising or bleeding (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. Both male and
female should use appropriate barrier contraceptive measures. Do not
breast-feed. |
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Dosage Forms |
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Powder for injection: 10 mg/vial |
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References |
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Brogden 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):S103-7.
Dillman RO, "A New Chemotherapeutic Agent: Deoxycoformycin (Pentostatin),"
Semin Hematol, 1994, 31(1):16-27.
Jeffrey LP, Chairman, National Study Commission on Cytotoxic Exposure.
Position Statement.
"The Handling of Cytotoxic Agents by Women Who Are Pregnant, Attempting to Conceive, or Breast-Feeding,"
January 12, 1987.
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.
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