FLUORESCITE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLUORESCITE (FLUORESCITE).
Fluorescein is a fluorescent dye that, after intravenous injection, distributes to the retinal and choroidal vasculature. It absorbs blue light at 490 nm and emits yellow-green fluorescence at 530 nm, allowing visualization of blood flow and leakage through the blood-retinal barrier.
| Metabolism | Fluorescein is metabolized in the liver and kidneys to fluorescein monoglucuronide; a small amount is excreted unchanged in urine. |
| Excretion | Eliminated primarily via renal excretion as unchanged drug (90% within 72 hours); minor biliary/fecal elimination (<5%). |
| Half-life | Terminal elimination half-life approximately 4–5 hours in adults with normal renal function; prolonged in renal impairment. |
| Protein binding | Approximately 70–85% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | 0.75–1.0 L/kg, indicating distribution into extracellular fluid. |
| Bioavailability | Intravenous: 100%; not administered orally (negligible oral bioavailability due to first-pass metabolism and poor absorption). |
| Onset of Action | Intravenous: 1–2 minutes; Intra-arterial: immediately upon injection. |
| Duration of Action | Intravenous: 15–20 minutes for visible retinal fluorescence; intra-arterial: 5–10 seconds for choroidal filling. |
5 mL (500 mg) intravenously, followed by a second dose after 30 minutes if needed. For children, 0.1 mL/kg (10 mg/kg) intravenously.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dosage adjustment required for renal impairment. |
| Liver impairment | No specific dosage adjustment required for hepatic impairment. |
| Pediatric use | 0.1 mL/kg (10 mg/kg) intravenously, maximum 5 mL. |
| Geriatric use | No specific adjustment required; use with caution in patients with renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FLUORESCITE (FLUORESCITE).
| Breastfeeding | Fluorescein is excreted into human breast milk after intravenous administration, with a milk-to-plasma ratio of approximately 0.6. Peak milk concentration occurs around 1-2 hours after injection. Limited data suggest minimal risk; however, caution is advised. Nursing should be withheld for 24–48 hours after administration to reduce potential infant exposure. |
| Teratogenic Risk | Fluorescein sodium does not appear to be teratogenic in animal studies; however, there are no adequate and well-controlled studies in pregnant women. Transplacental passage occurs, but risks to the fetus from intravenous fluorescein are considered low. No specific malformations or embryotoxic effects have been consistently reported. Use only if clearly needed. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to fluorescein or any component of the formulation."]
| Precautions | ["Severe allergic reactions including anaphylaxis, hypotension, and bronchospasm; may be life-threatening.","Extravasation causes intense pain and may lead to tissue necrosis; avoid intra-arterial administration.","Caution in patients with a history of allergy, asthma, or previous reaction to fluorescein."] |
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| Fetal Monitoring | No specific maternal or fetal monitoring is required beyond standard precautions during fluorescein angiography. Assess for maternal allergic reactions (urticaria, anaphylaxis) and extravasation at injection site. Fetal heart rate monitoring is not routinely indicated but may be considered in high-risk pregnancies. |
| Fertility Effects | No known adverse effects on fertility in animal studies. Human data are lacking, but fluorescein is not expected to impact reproductive function at diagnostic doses. |