Chemical formula: C₂₀H₁₂O₅ Molecular mass: 332.306 g/mol PubChem compound: 16850
Fluorescein is a fluorochrome used in medicine as a diagnostic stain. Fluorescein is used to make the blood vessels of the ocular fundus visible (angiography of the retina and choroid).
Within 7 to 14 seconds after intravenous administration into antecubital vein, fluorescein usually appears in the central artery of the eye. Within a few minutes of intravenous administration of fluorescein, a yellowish discoloration of the skin occurs, which begins to fade 6 to 12 hours after dosing. Various estimates of volume of distribution indicate that fluorescein distributes well into interstitial space (0.5 L/kg).
Fluorescein undergoes rapid metabolism to fluorescein monoglucuronide. After intravenous administration of fluorescein (14 mg/kg) to 7 healthy subjects, approximately 80% of fluorescein in plasma was converted to glucuronide conjugate after a period of 1 hour post dose, indicating relatively rapid conjugation.
Fluorescein and its metabolites are mainly eliminated via renal excretion. After intravenous administration, the urine remains slightly fluorescent for 24 to 36 hours. A renal clearance of 1.75 ml/min/kg and a hepatic clearance (due to conjugation) of 1.50 ml/min/kg have been estimated. The systemic clearance of fluorescein is essentially complete by 48 to 72 hours after administration of 500 mg fluorescein. Although a longer excretion rate in patients with renal impairment is possible, limited experience in renally impaired subjects (glomerular filtration rate below 20 ml/min) suggests that, in general, no dose adjustment is required.
Non-clinical data for sodium fluorescein reveal no special hazard for humans based on studies of single dose toxicity.
Fluorescein did not show teratogenic effects in rats and rabbits. Fluorescein crosses the placental barrier. After the intravenous application of 500 mg/kg intense fluorescence was detectable both in the fetus and the amniotic fluid.
Studies on mutagenicity did not show any mutagenic effects of fluorescein.
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