Rasburicase

Pronunciation: ras-BURE-i-kase
Class: Antimetabolite

Trade Names

Elitek
- Injection, lyophilized powder for solution 1.5 mg
- Injection, lyophilized powder for solution 7.5 mg

Fasturtec (Canada)

Pharmacology

Catalyzes enzymatic oxidation of poorly soluble uric acid into an inactive and soluble metabolite (allantoin).

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Pharmacokinetics

Distribution

Vd is 110 to 127 mL/kg in children and 75.8 to 138 mL/kg in adults.

Elimination

Half-life ranges from 15.7 to 22.5 h.

Special Populations

Renal Function Impairment

CrCl did not impact the pharmacokinetics of rasburicase.

Hepatic Function Impairment

Baseline liver enzymes did not impact the pharmacokinetics of rasburicase.

Race

The geometric mean values of body weight–normalized Cl were approximately 40% lower in Japanese than in white patients.

Indications and Usage

Initial management of plasma uric acid levels in children and adults with leukemia, lymphoma, and solid tumor malignancies who are receiving anticancer therapy expected to result in tumor lysis and subsequent elevation of plasma uric acid.

Unlabeled Uses

Gout.

Contraindications

Individuals with G-6-PD deficiency; known history of anaphylaxis or hypersensitivity; hemolytic or methemoglobinemia reactions to rasburicase or any of its excipients.

Dosage and Administration

Adults and Children

IV 0.2 mg/kg, infused over 30 min, as a single dose for 5 days.

General Advice

  • For IV infusion only. Do not administer as a bolus injection.
  • Follow manufacturer's instructions for reconstituting the powder for injection and subsequent further dilution. Reconstitute with the diluent provided.
  • Do not administer if particulate matter, cloudiness, or discoloration is noted.
  • Infuse over 30 min through a separate line or flush line with at least 15 mL of normal saline prior to and after infusion.
  • Do not use filters during reconstitution or infusion of rasburicase.

Storage/Stability

Store vials at 36° to 46°F. Do not freeze. Protect from light. Store reconstituted or diluted solution at 36° to 46°F for up to 24 h. Discard unused product solution after 24 h.

Drug Interactions

None well documented.

Laboratory Test Interactions

At room temperature, rasburicase causes enzymatic degradation of uric acid in blood/plasma/serum samples, potentially resulting in spuriously low plasma uric acid assay readings. To avoid ex vitro uric acid degradation, uric acid must be analyzed in plasma. Blood must be collected into prechilled tubes containing heparin. Samples must be immediately immersed in an ice water bath. Plasma samples must be prepared by centrifugation in a precooled centrifuge (4°C). Finally, the plasma must be maintained in an ice water bath and analyzed for uric acid within 4 h of collection.

Adverse Reactions

Cardiovascular

Ischemic coronary artery disorders, supraventricular arrhythmias (2% or more).

CNS

Headache (26%); anxiety (24%).

Dermatologic

Rash (13%).

GI

Nausea (58%); vomiting (50%); abdominal pain (22%); constipation, diarrhea (20%); mucositis (15%); abdominal and GI infections (2% or more).

Hematologic

Hemolysis; methemoglobinemia

Hypersensitivity

Severe allergic reactions including anaphylaxis (eg, bronchospasm, chest paint and tightness, dyspnea, hypoxia, hypotension, shock, and urticaria.

Metabolic

Peripheral edema (50%); hypophosphatemia (17%); hyperbilirubinemia (16%); fluid overload (12%); hyperphosphatemia (10%).

Respiratory

Pulmonary hemorrhage, respiratory failure (2% or more).

Miscellaneous

Fever (46%); pharyngolaryngeal pain (14%); sepsis (12%); antibody formation, increased ALT (11%).

Precautions

Warnings

Anaphylaxis

May cause severe hypersensitivity reactions, including anaphylaxis. Immediately and permanently discontinue rasburicase in a patient who develops clinical evidence of a serious hypersensitivity reaction.

Hemolysis

Do not administer to patients with G-6-PD deficiency. Immediately and permanently discontinue rasburicase in patients developing hemolysis. Screen patients at higher risk for G-6-PD deficiency before starting therapy.

Methemoglobinemia

May occur. Immediately and permanently discontinue rasburicase in a patient who develops methemoglobinemia.

Interference with uric acid measurements

Rasburicase enzymatically degrades uric acid in blood samples left at room temperature. Collect blood samples in prechilled tubes containing heparin and immediately immerse and maintain sample in an ice water bath. Assay plasma samples within 4 h of collection.


Monitor

Monitor all patients for allergic reactions (eg, bronchospasm, chest pain and tightness, dyspnea, hypoxia, hypotension, shock, urticaria), hemolysis, and methemoglobinemia.


Pregnancy

Category C .

Lactation

Undetermined.

Overdosage

Symptoms

None well documented.

Patient Information

  • Advise patient, family, or caregiver that medication will be prepared and administered by a health care provider in a medical facility.
  • Advise patient or caregiver to report the following to health care provider: allergic reactions, bronchospasm, chest pain or tightness, dyspnea, hypotension, hypoxia, intolerable injection-site reactions, shock, urticaria, or any unusual symptoms.

Copyright © 2009 Wolters Kluwer Health.

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