Valrubicin

Pronunciation: (val-ROO-bi-sin)
Class: Anthracycline

Trade Names

Valstar
- Injection, solution, concentrate 40 mg/mL

Pharmacology

Inhibits the incorporation of nucleosides into nucleic acids, causing extensive chromosomal damage and arresting cell cycle in G2.

Pharmacokinetics

Absorption

After intravesical administration, penetrates into the bladder wall. Unless the bladder is perforated, only nanogram amounts of the drug are absorbed systemically.

Elimination

After retention, the drug is almost completely excreted by voiding the instillate.

Indications and Usage

Intravesical treatment of Bacillus Calmette-Guérin–refractory carcinoma in situ (CIS) of the urinary bladder in patients for whom immediate cystectomy would be associated with unacceptable morbidity or mortality.

Contraindications

UTI; patients with small bladder capacity (ie, unable to tolerate a 75 mL instillation); hypersensitivity to anthracyclines or polyoxyl castor oil.

Dosage and Administration

Adults

Intravesically 800 mg once a wk for 6 wk.

General Advice

• Delay administration at least 2 wk after transurethral resection and/or fulguration.
• Allow installation to warm slowly to room temperature, but do not heat.
• At temperatures below 39°F, polyoxyl castor oil may begin to form a waxy precipitate. If this occurs, warm the vial in the hand until the solution is clear.
• To avoid skin reactions, use of gloves during preparation and administration is recommended.
• To prevent leaching of a hepatotoxic plasticizer from polyvinyl chloride bags and IV tubing, prepare and store solution in glass, polypropylene, or polyolefin containers and tubing. It is recommended that non-DEHP–containing administration sets, such as those that are polyethylene-lined, be used.
• After draining the bladder, 75 mL of diluted valrubicin sterile solution should be instilled slowly via gravity over a period of several minutes. The solution should be retained for 2 h before voiding.
• Patients should maintain adequate hydration after treatment.
• Do not mix with other drugs.

Storage/Stability

Store in refrigerator at 36° to 46°F. Vials diluted in sodium chloride 0.9% injection are stable for 12 h at temperatures up to 77°F.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Vasodilation (2%).

CNS

Asthenia, headache, malaise (4%); dizziness (3%).

Dermatologic

Rash (3%).

GI

Nausea (5%); diarrhea (3%); vomiting (2%); flatulence (1%).

Genitourinary

Any local bladder symptom (88%); urinary frequency (61%); urinary urgency (57%); dysuria (56%); bladder spasm (31%); hematuria (29%); bladder pain (28%); urinary incontinence (22%); cystitis, UTI (15%); nocturia (7%); urinary retention (4%); urethral pain (3%); gross hematuria, pelvic pain (1%).

Hematologic-Lymphatic

Anemia (2%).

Local

Local procedural-related burning symptoms (5%).

Metabolic-Nutritional

Hyperglycemia, peripheral edema (1%).

Musculoskeletal

Back pain (3%); myalgia (1%).

Respiratory

Pneumonia (1%).

Miscellaneous

Abdominal pain (5%); chest pain (3%); fever (2%).

Precautions

Monitor In patients undergoing transurethral resection of the bladder, determine the status of the bladder before instillation of valrubicin. In case of bladder perforation, delay administration until bladder integrity has been restored.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

No specific precautions for use of valrubicin in elderly patients who are otherwise in good health.

Bladder carcinoma

Delaying cystectomy could lead to fatal metastatic bladder carcinoma.

Efficacy

Complete response only occurs in about 20% of patients with Bacillus Calmette-Guérin–refractory CIS.

Irritable bladder

Use with caution in patients with irritable bladder symptoms.

Special risk patients

Do not administer to patients with a perforated bladder or to those in whom the integrity of the bladder mucosa is compromised.

Overdosage

Symptoms

Irritable bladder symptoms.

Patient Information

• Instruct patients to report prolonged, irritable bladder symptoms or prolonged passage of red-colored urine immediately to health care provider.
• Instruct men to refrain from sexual activity while receiving valrubicin therapy.
• Advise patients to use an effective contraceptive method during treatment.

Copyright © 2009 Wolters Kluwer Health.