Dosing and uses of Valrubicin (Valstar)
Adult dosage forms and strengths
intravesical solution
- 40mg/mL
Bladder Carcinoma
Indicated for intravesicular treatment of BCG-Refractory bladder carcinoma in situ
800 mg intravesical once weekly for 6 weeks; retain in bladder for 2 hours before voiding
Monitor q3month for recurrence/progression of CIs
Administration
Reconstitution: withdraw contents of 4 vials, each containing 200 mg in 5 mL (allowed to warm to room temp without heating), & dilute with 55 mL Ns
Instill slowly via gravity flow through a urinary catheter (following sterile insertion)
Withdraw the catheter & allow patient to retain solution for 2 hours
After 2 hours, patient should void
Use caution when preparing, handling, and disposaL
Pediatric dosage forms and strengths
Not recommended
Valrubicin (Valstar) adverse (side) effects
>10%
Urinary frequency (61%)
Urinary urgency (57%)
Dysuria (56%)
Bladder spasm (31%)
Hematuria (29%)
Bladder pain (28%)
Urinary incontinence (22%)
Cystitis (15%)
UTI (15%)
1-10%
Abd pain (5%)
Nausea (5%)
Headache (4%)
Malaise (4%)
Urinary retention (4%)
Back pain (3%)
Dizziness (3%)
Rash (3%)
Diarrhea (3%)
Anemia (2%)
Chest pain (2%)
Vomiting (2%)
Vasodilation (2%)
Pneumonia (1%)
Asthenia (undefined)
Warnings
Contraindications
Hypersensitivity to valrubicin, anthracyclines or other ingredients
Perforated bladder mucosa
Active UTI
Small bladder capacity; unable to tolerate a 75 mL instillation
Cautions
Complete response in only 20%
Delaying cystectomy can lead to development of metastatic bladder cancer, which is lethaL
Not for administration to patients with a perforated bladder or to those in whom the integrity of the bladder mucosa has been compromised
Evaluate status of bladder before intravesical instillation of therapy
Use with caution in patients with severe irritable bladder symptoms
Advise females of reproductive potential of potential risk to fetus and to use effective contraception
Delay valrubicin therapy for 2 weeks after transurethral resection or fulguration
Urine may be red-tinged for 24 hr post-instillation
Was unavailable since 2002 due to manufacturing problems; reintroduced 2009
Pregnancy and lactation
Pregnancy category: C
Lactation: not known if excreted in breast milk, do not nurse
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Valrubicin (Valstar)
Mechanism of action
Semisynthetic analog of doxorubicin; inhibits DNA topoisomerase II, which in turn inhibits DNA synthesis; causes extensive chromosomal damage and arrests cells at the G2 phase of the cell cycle; readilly penetrate cells but does not appear to intercalate DNA
Pharmacokinetics
Absorption: Negligible systemic absorption
Metabolites: N-trifluoroacetyladriamycin, N-trifluoroacetyladriamycinoL
Excretion: Urine
