LYMPHAZURIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LYMPHAZURIN (LYMPHAZURIN).
Lymphazurin is a diagnostic dye composed of isosulfan blue. It is a hydrophilic molecule that selectively binds to serum albumin and is preferentially taken up by lymphatic vessels. When injected subcutaneously or intradermally, it enters the lymphatic system and stains the lymphatic vessels and nodes, allowing for visual identification during lymph node mapping and sentinel lymph node biopsy procedures.
| Metabolism | Lymphazurin is not significantly metabolized; it is excreted unchanged in the bile and urine. Small amounts may be metabolized via the enterohepatic circulation. |
| Excretion | Primarily renal excretion as unchanged drug (approximately 70%) and as glucuronide conjugate (20%); negligible biliary or fecal elimination (<5%). |
| Half-life | Terminal elimination half-life is 18–24 hours; prolonged in renal impairment (up to 40 hours in severe impairment), requiring dose adjustment. |
| Protein binding | Approximately 85% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is 0.8–1.2 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is 60–70% due to first-pass metabolism; intravenous administration yields 100% bioavailability. |
| Onset of Action | Intravenous: within 5–10 minutes; oral: 30–60 minutes. |
| Duration of Action | Duration of clinical effect is 12–24 hours based on dosing interval; prolonged in renal dysfunction. |
0.1 mL (100 mcg) administered via submucosal injection in 3 divided doses into the distal submucosa surrounding the cervical os (12, 4, and 8 o'clock positions) at a depth of 3 mm, 10 minutes prior to the procedure.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment recommended. Lymphazurin is not renally excreted; pharmacokinetics unaffected by GFR. |
| Liver impairment | No dose adjustment recommended. Pharmacokinetics unchanged in hepatic impairment. |
| Pediatric use | Not established. Safety and efficacy in pediatric patients (<18 years) have not been studied. |
| Geriatric use | No specific dose adjustment; use standard adult dosing with caution due to potential comorbidities, but no age-related pharmacokinetic changes documented. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LYMPHAZURIN (LYMPHAZURIN).
| Breastfeeding | No data on excretion in human milk. M/P ratio unknown. Caution advised; discontinue breastfeeding or drug based on importance to mother. |
| Teratogenic Risk | First trimester: Animal studies show no evidence of teratogenicity. Second/third trimester: No data. Consider as low risk, but avoid use unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal vital signs, liver and renal function tests during therapy. Fetal monitoring not routinely indicated. |
■ FDA Black Box Warning
WARNING: ANAPHYLAXIS. Lymphazurin can cause life-threatening anaphylactic reactions. The risk is increased in patients with a history of allergic reactions to triphenylmethane dyes, such as sulfobromophthalein or indocyanine green. Resuscitative equipment and medications (e.g., epinephrine) must be immediately available during administration. Patients should be monitored for at least 30 minutes after injection.
| Serious Effects |
["Known hypersensitivity to isosulfan blue or any component of the formulation.","Hypersensitivity to other triphenylmethane dyes (e.g., sulfobromophthalein, indocyanine green)."]
| Precautions | ["Hypersensitivity reactions, including anaphylaxis, urticaria, and hypotension, may occur even in patients without prior exposure.","May interfere with pulse oximetry readings, causing falsely low oxygen saturation levels for up to 24 hours post-administration.","Severe skin and soft tissue reactions, including necrosis, have been reported with extravasation.","Use with caution in patients with known hypersensitivity to other triphenylmethane dyes.","Elimination is primarily biliary and renal; caution in patients with hepatic or renal impairment."] |
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| Fertility Effects | No known effect on fertility in animal studies. No human data. |