AK-Fluor

In the U.S.

• AK-Fluor
• Angioscein
• Fluorescite

Available Dosage Forms:

• Solution

Therapeutic Class: Disclosing Agent

Fluorescein injection is used to help certain parts of the eye (eg, retina, iris) become more visible during eye medical procedures.

This medicine is to be given only by or under the direct supervision of your doctor.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur:

• Bluish color
• cold, clammy skin
• confusion
• cough
• difficulty breathing
• difficulty swallowing
• dizziness
• fast heartbeat
• hives, itching, or skin rash
• lightheadedness
• noisy breathing
• pain, redness, swelling, or peeling of the skin
• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
• severe pain in the arm
• sweating
• tightness in the chest
• unconsciousness
• unusual tiredness or weakness

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Abdominal or stomach pain
• diarrhea
• nausea
• vomiting
• yellow skin and urine

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

AK-FLUOR® 10% (100 mg/mL) and 25% (250 mg/mL) is indicated in diagnostic fluorescein angiography or angioscopy of the retina and iris vasculature.

Hypersensitivity

AK-FLUOR® is contraindicated in patients with known hypersensitivity to fluorescein sodium or any other ingredients in this product. Rare cases of death due to anaphylaxis have been reported [see Warnings and Precautions (5.1) and Adverse Reactions (6.2)].

Mechanism of Action

Fluorescein sodium responds to electromagnetic radiation and light between the wavelengths of 465 to 490 nm and fluoresces, i.e., emits light at wavelengths of 520 to 530 nm. Thus, the hydrocarbon is excited by blue light and emits light that appears yellowish green. Following intravenous injection of fluorescein sodium in an aqueous solution, the unbound fraction of the fluorescein can be excited with a blue light flash from a fundus camera as it circulates through the ocular vasculature, and the yellowish green fluorescence of the dye is captured by the camera. In the fundus, the fluorescence of the dye demarcates the retinal and/or choroidal vasculature under observation, distinguishing it from adjacent areas/structures.

Pharmacokinetics

Distribution.

Within 7 to 14 seconds after IV administration into the antecubital vein, fluorescein usually appears in the central retinal artery of the eye. Within a few minutes of IV administration of fluorescein sodium, 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 into interstitial space (0.5 L/kg).

Metabolism.

Fluorescein is metabolized to fluorescein monoglucuronide. After IV administration of fluorescein sodium (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.

Excretion.

Fluorescein and its metabolite are mainly eliminated via renal excretion. After IV 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 was essentially complete by 48 to 72 hours after administration of 500 mg fluorescein.

Carcinogenesis, Mutagenesis, Impairment of Fertility

There have been no long-term studies done using fluorescein in animals to evaluate carcinogenic potential.

After administration of fluorescein sodium, skin will attain a temporary yellowish discoloration. Urine attains a bright yellow color. Discoloration of the skin usually fades in 6 to 12 hours and usually fades in urine in 24 to 36 hours. [see Warnings and Precautions (6.1)].

Rx only

Manufactured by:
Akorn Inc.
Lake Forest, IL 60045

FL00N
Rev. 07/08

Summary of Use during Lactation

After intravenous use in a nursing mother, milk levels and the dose received by the infant are much higher. It is unlikely that these higher levels are problematic for most infants, but exposure to intense light, such as phototherapy, should probably be avoided for a few days after the maternal dose.

Because absorption from the eye is limited, fluorescein would not be expected to cause any adverse effects in breastfed infants. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.

Drug Levels

Maternal Levels. A woman received 5 mL of 10% fluorescein (500 mg) injection shortly after delivering a set of twins. Milk samples were obtained periodically by manual expression for 76 hours after the dose. The highest concentration of 372 mcg/L was obtained in the first sample 6 hours after the dose. By 76 hours after the dose, the milk fluorescein concentration was 170 mcg/L. The half-life of fluorescein in milk was 62 hours.[1]

A mother nursing a 3-month-old infant had 2% fluorecein drops applied into each eye. Blood and milk samples were taken 3 times at 30-minute intervals after the dose. Milk levels at these times were 20, 22 and 15 mcg/L, respectively.[2]

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

References

1. Maguire AM, Bennett J. Fluorescein elimination in human breast milk. Arch Ophthalmol. 1988;106:718-9. Letter. PMID: 336998

2. Mattern J, Mayer PR. Excretion of fluorescein into breast milk. Am J Ophthalmol. 1990;109:598-9. Letter. PMID: 2333925