hexaminolevulinate (Rx)

1-10%

Dysuria

Hematuria

Headache

Pain

Urinary retention

Spasm

Contraindications

Hypersensitivity

Porphyria

Gross hematuria

Cautions

Anaphylaxis, including anaphylactoid shock reported; ensure trained personnel and therapies for anaphylaxis are available before and during administration

Failed detection

• May fail to detect some bladder tumors, including malignant lesions; NOT a replacement for random biopsies or other evaluation procedures
• Do not perform cystoscopy with blue light alone as malignant lesions can be missed unless the bladder is initially examined under white light

False positive fluorescence

• False fluorescence may occur during blue light cystoscopy and be unable to detect either dysplasia or carcinoma
• Fluorescent areas in bladder mucosa may result from inflammation, cystoscopic trauma, scar tissue, or bladder mucosal biopsy from previous cystoscopic examination
• Use only catheters made of vinyl (uncoated or coated with hydrogel), latex (amber or red), or silicone for bladder instillation; do not use catheters coated or embedded with silver or antibiotics
• The presence of urine and/or blood within the bladder may interfere detection of tissue fluorescence; ensure bladder is emptied prior to cystoscopy fluid instillation

Pregnancy

There are no available data on use in pregnant women to inform a drug associated risk of adverse developmental outcomes

Systemic absorption following administration is expected to be minimal

Lactation

There are no data on the presence of hexaminolevulinate in human or animal milk, the effects on a breastfed infant, or the effects on milk production

Systemic absorption following administration is expected to be minimal

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.

Mechanism of Action

Hexaminolevulinate is an ester of aminolevulinic acid, a heme precursor; used as photoactive intermediate protoporphyrin IX (PpIX) and other photoactive porphyrins (PAPs); PpIX and PAPs referentially accumulate in neoplastic cells and are detected at light wavelengths of 360-450 to distinguish between cancerous and normal tissue

Pharmacokinetics

Half-Life: Biphasic; 39 minutes initial half-life, 76 hr terminal half-life

Absorption: 7% following 1 hr instillation

Metabolism: Rapidly by human blood

Bioavailability: 7% (intravesical)

Bladder Instillation

See prescribing information for full instructions and diagrams

Reconstitute powder with 50 mL diluent (supplied); resulting concentration is 2 mg/mL

Use solution immediately after reconstitution; otherwise store in refrigerator at 2-8 degrees C (36-46 degrees F) for up to 2 hr

After bladder instillation, retain for at least 1 hr (not to exceed 3 hr) before evacuating and performing cystoscopic exam (under white and then blue lights with Karl Storz D-Light C Photodynamic Diagnostic system)

Avoid contact with skin; f skin does come in contact with hexaminolevulinate solution, wash immediately with soap and water and dry off

After voiding the bladder of hexaminolevulinate solution, routinely wash the patient’s perineal skin region with soap and water and dry