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Trade Names:
Fludara
- Powder for injection 50 mg

Mechanism of Action

Pharmacology

Fludarabine is a fluorinated nucleotide analog of the antiviral agent vidarabine. Fludarabine's metabolite appears to act by inhibiting DNA polymerase alpha, ribonucleotide reductase, and DNA primase, thus inhibiting DNA synthesis.

Pharmacokinetics

Absorption

Fludarabine is rapidly converted to the active metabolite, 2‐fluoro‐ara‐A, within minutes after IV infusion.

Distribution

In vitro, plasma protein binding of fludarabine ranged between 19% and 29%.

Metabolism

The t _½ of 2‐fluoro‐ara‐A is approximately 20 h.

Elimination

Renal Cl represents approximately 40% of the total body Cl.

Indications and Usage

Refractory or progressive chronic B-cell lymphocytic leukemia.

Unlabeled Uses

Leukemias, non-Hodgkin lymphoma.

Contraindications

Standard considerations.

Dosage and Administration

IV 25/m ² /day over approximately 30 min daily for 5 consecutive days. Each 5‐day course should commence every 28 days.

IV Reduce dose 20% in moderate renal function impairment (CrCl 30 to 70 mL/min/1.73 m ² ). Do not administer in patients with severely impaired renal function (CrCl less than 30 mL/min/1.73 m ² ).

Drug Interactions

Concomitant therapy may cause severe or fatal pulmonary toxicity.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Deep venous thrombosis, phlebitis (at least 1%); aneurysm; angina; arrhythmia; cerebrovascular accident; CHF; MI; supraventricular tachycardia; transient ischemic attack.

CNS

Weakness (65%); fatigue (38%); paresthesia (12%); malaise (8%); agitation; coma; confusion; headache; weakness.

Dermatologic

Rash (15%); diaphoresis (13%); pruritus (at least 1%); alopecia; seborrhea.

EENT

Visual disturbances (15%); hearing loss, sleep disorder (at least 1%); cerebellar syndrome; depression; impaired mentation.

GI

Nausea/vomiting (36%); anorexia (34%); diarrhea (15%); GI bleeding (13%); constipation (at least 1%); dysphagia; esophagitis; mucositis; stomatitis.

Genitourinary

Dysuria, hematuria; urinary infection (at least 1%); abnormal renal function test; hemorrhagic cystitis; proteinuria; renal failure; urinary hesitancy.

Hematologic-Lymphatic

Anemia (60%); neutropenia (59%); thrombocytopenia (55%); autoimmune hemolytic anemia; pancytopenia (postmarketing).

Hepatic

Abnormal LFTs (at least 1%); cholelithiasis; liver failure.

Hypersensitivity

Anaphylaxis.

Metabolic-Nutritional

Hyperglycemia (at least 1%); tumor lysis syndrome (including hyperuricemia, hyperphosphatemia, hypocalcemia, metabolic acidosis, hyperkalemia, hematuria, urate crystalluria, renal failure).

Musculoskeletal

Myalgia (16%); arthralgia; osteoporosis.

Respiratory

Cough (44%); dyspnea, pneumonia (22%); hemoptysis, upper respiratory tract infections (at least 1%); allergic pneumonitis; bronchitis; epistaxis; hypoxia; pharyngitis; pulmonary hypersensitivity; sinusitis; respiratory distress, pulmonary hemorrhage, pulmonary fibrosis, respiratory failure (postmarketing).

Miscellaneous

Fever (69%); infection (44%); pain (22%); chills, edema (19%); dehydration; hemorrhage.

Precautions

Pregnancy

Category D .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Administer cautiously.

Dose-dependent toxicity

There are clear dose-dependent toxic effects seen with fludarabine.

Transfusion

Transfusion-associated graft/host disease may occur after transfusion of non-irradiated blood.

Tumor lysis syndrome

Tumor lysis syndrome has occurred.

Overdosage

Symptoms

Irreversible CNS toxicity characterized by delayed blindness, coma, and death; severe thrombocytopenia and neutropenia.

Patient Information

• Review the treatment regimen including dosing schedule, duration of treatment, and monitoring that will be required.
• Advise patient, family, or caregiver that medication will be prepared and administered by health care providers in a health care setting.
• Advise patient, family, or caregiver that medication may be used in combination with other agents to achieve maximum benefit possible.
• Advise patient, family, or caregiver to immediately report any of the following to health care provider: rash; hives; difficulty breathing; fever, chills, or other signs of infection; bleeding or unusual bruising; sores in mouth; dark urine; yellowing of skin or eyes; pain, redness, or swelling at injection site.
• Advise patient, family, or caregiver to report any of the following to health care provider: persistent nausea, vomiting, diarrhea, or appetite loss; persistent or worsening general body weakness.
• Caution women of childbearing potential to avoid becoming pregnant during therapy.