Hexaminolevulinate

Medically reviewed by Drugs.com. Last updated on Nov 8, 2023.

Pronunciation

(hex a mee noe LEV ue lin ate)

Index Terms

HAL
Hexaminolevulinate HCl
Hexaminolevulinate Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravesical, as hydrochloride:

Cysview: 100 mg (1 ea)

Brand Names: U.S.

Cysview

Pharmacologic Category

Contrast Agent

Pharmacology

Upon intravesical administration, hexaminolevulinate, an ester of aminolevulinic acid and a porphyrin precursor, enters urinary epithelial cells and is used in the formation of photoactive intermediate protoporphyrin IX (PpIX) and other photoactive porphyrins (PAPs). PpIX and PAPs are thought to preferentially accumulate in neoplastic cells. Following photoexcitation with the Karl Storz D-Light Photodynamic Diagnostic (PDD) system (white and blue light), PpIX and PAPs fluoresce and can be used to detect malignant lesions on cystoscopy; fluorescence from tumor tissue appears bright red and demarcated.

Half-Life Elimination

Biphasic; Initial: 39 minutes; Terminal: ~76 hours

Use: Labeled Indications

Detection of bladder cancer: Imaging agent for cystoscopic detection of bladder cancer (including carcinoma in situ), in patients with known or suspected lesion(s) based on prior cystoscopy, or in patients undergoing surveillance cystoscopy for bladder cancer. Hexaminolevulinate is used with the Karl Storz D-Light C Photodynamic Diagnostic (PDD) system to perform Blue Light Cystoscopy (BLC) as an adjunct to the white light cystoscopy.

Limitations of use: Not a replacement for random bladder biopsies or other procedures used to detect bladder cancer.

Contraindications

Known hypersensitivity to hexaminolevulinate, any derivative of aminolevulinic acid, or any component of the formulation; porphyria; gross hematuria

Dosing: Adult

Detection of bladder cancer: Intravesical instillation: 100 mg (50 mL) instilled into empty bladder via urinary catheter.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Reconstitution

Wear gloves for preparation (skin exposure may increase the risk for sensitization). Withdraw 50 mL of diluent (provided) into a 50 mL syringe with a luer lock tip. See manufacturer’s instructions if using vial adapter. Inject ~10 mL of diluent from the syringe into the hexaminolevulinate powder vial, and keeping the syringe attached, gently shake the vial to dissolve the powder (usually dissolves immediately). Withdraw all of the reconstituted solution back into the syringe (final concentration of 2 mg/mL); cap syringe securely and mix gently.

Administration

Intravesical instillation: Slowly instill solution (50 mL) via intravesical catheter into emptied bladder; catheter may be a straight or intermittent urethral catheter with a proximal funnel opening to accommodate a luer lock adapter. Use only catheters which are vinyl (uncoated or coated in hydrogel), latex (amber or red), and silicone for instillation; do not use catheters coated or embedded with silver or antibiotics. Indwelling catheters (eg, Foley catheters) may only be used if inserted shortly before and removed following instillation of hexaminolevulinate. Following instillation, remove catheter and instruct the patient to retain the solution for at least 1 hour (maximum: 3 hours); patient may stand, sit, and move around while retaining instillation; solution should be evacuated immediately prior to the initiation of the cystoscopic procedure. After voiding of the bladder, the perineal skin region should be washed with soap and water and dried (avoid skin contact with hexaminolevulinate solution). Begin cystoscopic exam within 30 minutes of evacuation (but not less than 1 and no more than 3 hours after instillation into bladder); if the patient retained the solution for <1 hour, allow 1 hour to pass from the instillation to the initiation of cystoscopic examination. Refer to manufacturer's instructions for details on cystoscopic examination procedure.

Storage

Store intact kit at 20°C to 25°C (68°F to 77°F); excursions are permitted to 15°C to 30°C (59°F to 86°F). The reconstituted solution should be used shortly after reconstitution, however, may be stored refrigerated at 2°C to 8°C (36°F to 46°F) in the labeled syringe for up to 2 hours in a syringe. Discard if not used within 2 hours.

Drug Interactions

BCG (Intravesical): May diminish the diagnostic effect of Hexaminolevulinate. Avoid combination

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Central nervous system: Headache, procedural pain

Genitourinary: Bladder spasm (2%), bladder pain, dysuria, hematuria

<1%, postmarketing, and/or case reports: Abnormal urinalysis, anaphylaxis (including anaphylactoid shock), cystitis, hypersensitivity reaction

Warnings/Precautions

Concerns related to adverse events:

• Hypersensitivity: Hypersensitivity reactions, including anaphylaxis and anaphylactoid shock, have been reported following administration. Immediate treatment for anaphylaxis and/or hypersensitivity reactions and trained personnel should be available during use.

Other warnings/precautions:

• Appropriate use: Bladder must be emptied of urine prior to instillation of fluids for cystoscopy. Biopsy/resect bladder mucosal lesions only following completion of both white and blue light rigid cystoscopy. Do not use in patients with gross hematuria.

• Failed detection: May fail to detect some bladder tumors (including malignant tumors). Cystoscopic examination with hexaminolevulinate is not a replacement for random biopsies or other procedures usually performed in the cystoscopic evaluation for cancer. Both light settings of the PDD system (white before blue) must be used for the most accurate detection of malignancies.

• False fluorescence: Fluorescent areas detected during blue light cystoscopy may not indicate a bladder mucosal lesion. False positive fluorescent areas may result from inflammation, cystoscopic trauma, scar tissue, or bladder mucosal biopsy from prior cystoscopic examinations, as well as recent BCG immunotherapy or intravesical chemotherapy. The presence of urine and/or blood in the bladder may interfere with detection.

Monitoring Parameters

Monitor for signs/symptoms of hypersensitivity

Pregnancy Considerations

Adequate animal reproduction studies have not been conducted. Systemic absorption is expected to be minimal.

Patient Education

What is this drug used for?

• It is used with a light test to check for bladder cancer.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Blood in the urine

• Severe bladder irritation

• Unable to pass urine

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine’s uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.