Fluorescite

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Fluorescite

Classes

Ophthalmological Diagnostic Agents

Administration
Injectable Administration Intravenous Administration

Administer by intravenous injection. An intradermal skin test may be performed prior to intravenous administration.
Inspect product for particulate matter and discoloration before administration.
Do not mix or dilute with other solutions or drugs. Flush intravenous cannulas with 0.9% Sodium Chloride Injection before and after other medications are injected to avoid physical incompatibility reactions (personal communication, Akorn Inc., November 10, 2006).
Ophthalmologist monitoring of patient during procedure and for 30 minutes after completion is strongly recommended.
Leave venous assess open for 5 minutes following injection for emergency measures if needed.
Emergency resuscitation resources must be available during procedure.
 
Skin test:
If a potential allergy to fluorescein is suspected, an intradermal skin test may be performed prior to intravenous administration.
Inject 5 mg intradermally, and evaluate 30 to 60 minutes after administration.
Of note, a negative skin test is not proof that a patient is not allergic to fluorescein.
 
IV push:
Follow administration guidelines to avoid extravasation.
Connect fluorescein syringe to transparent tubing with a 23 gauge butterfly needle.
Insert needle and draw the patient's blood to the hub of the syringe; visualize small air bubble in the tubing.
Slowly inject the blood back into the vein while watching the skin; if a skin bulge is seen over the needle tip, stop the injection before fluorescein is injected.
When certain extravasation has not occurred, turn off room lights, and inject dose rapidly (1 mL/second) into antecubital vein.
Luminescence usually becomes visible in the retina and choroidal vessels in 7 to 14 seconds.

Ophthalmic Administration

Ophthalmic strip:
Remove contact lenses prior to procedure; flush the eye(s) with sterile, 0.9% Sodium Chloride Irrigation, and wait at least 1 hour before replacing lenses.
Anesthetize eye(s).
Apply in 1 of 2 manners; either, retract upper lid and touch tip of the strip to the bulbar conjunctiva on the temporal side until an adequate amount of stain is available OR moisten strip with Sterile Water for Irrigation and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly until appropriate staining is achieved and blink several times after strip removal.

Adverse Reactions
Severe

cardiac arrest / Early / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
laryngeal edema / Rapid / Incidence not known
bronchospasm / Rapid / Incidence not known
seizures / Delayed / Incidence not known

Moderate

neuritis / Delayed / Incidence not known
phlebitis / Rapid / Incidence not known
hypotension / Rapid / Incidence not known

Mild

vomiting / Early / 4.0-20.0
nausea / Early / 4.0-20.0
skin discoloration / Delayed / 10.0
contact lens discoloration / Delayed / 10.0
urine discoloration / Early / 10.0
injection site reaction / Rapid / 1.0
dizziness / Early / 1.0
fever / Early / Incidence not known
sneezing / Early / Incidence not known
dysgeusia / Early / Incidence not known
metallic taste / Early / Incidence not known
photosensitivity / Delayed / Incidence not known
musculoskeletal pain / Early / Incidence not known
headache / Early / Incidence not known
syncope / Early / Incidence not known
urticaria / Rapid / Incidence not known
flushing / Rapid / Incidence not known
rash / Early / Incidence not known
chills / Rapid / Incidence not known
malaise / Early / Incidence not known
back pain / Delayed / Incidence not known

Common Brand Names

AK-Fluor, Fluorescite, Ful-Glo

Dea Class

Rx

Description

Fluorescent dye; diagnostic aid; used topically to visualize the anterior surface of the eye and systemically in fluorescein angiography to examine the retinal and choroidal circulation; significant anaphylactoid reactions possible with IV use.

Dosage And Indications
For radiographic examination (i.e., diagnostic angiography or angioscopy) of the retina and iris vasculature. Intravenous and Intradermal dosage Adults

500 mg IV. A lower dose of 200 mg IV may be appropriate in cases where highly sensitive imaging system is used. If a potential fluorescein allergy is suspected, an intradermal test dose may be performed before intravenous administration. Inject 5 mg intradermally, and evaluate 30 to 60 minutes later. A negative skin test is not proof that the patient will not experience a hypersensitivity reaction.

Children

7.7 mg/kg (Max: 500 mg) IV. If a potential fluorescein allergy is suspected, an intradermal test dose may be performed before intravenous administration. Inject 5 mg intradermally, and evaluate 30 to 60 minutes later. A negative skin test is not proof that the patient will not experience a hypersensitivity reaction.

For staining the anterior segment of the eye for eye trauma diagnosis. Topical dosage (ophthalmic strips) Adults

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

Children†

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

For staining the anterior segment of the eye for contact lens fitting. Ophthalmic dosage (ophthalmic strips) Adults

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

Children†

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

For staining the anterior segment of the eye for post-ophthalmic surgery wound closure assessment following anterior chamber reformation. Topical dosage (ophthalmic strips) Adults

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

Children†

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

For staining the anterior segment of the eye for lacrimal drainage diagnosis. Topical dosage (ophthalmic strips) Adults

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

Children†

Use 1 strip per eye; either touch tip of strip to the bulbar conjunctiva of the anesthetized eye until an adequate amount of stain is available or moisten strip with sterile water and place at the fonix in the lower cul-de-sac close to the punctum, then have patient close eyes tightly and blink several times after strip removal.

Dosing Considerations
Hepatic Impairment

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that dosage adjustments are not needed.

Renal Impairment

Fluorescein is metabolized and eliminated renally. Systemic dosage may be modified depending on clinical response and degree of renal impairment, but no standardized recommendations are available.
Continuous hemodialysis
In dialyzed patients, 250 mg (100 mg/mL) IV injection is recommended.

Drug Interactions

Angiotensin-converting enzyme inhibitors: (Moderate) Patients on angiotensin-converting enzyme inhibitors are at an increased risk of adverse reactions when administered fluorescein injection. If fluorescein injection is deemed necessary in a patient on ACE inhibitor therapy, monitor as appropriate during and after the procedure.
Benzalkonium Chloride: (Moderate) The use of fluorescein with benzalkonium chloride aqueous solutions may be incompatible.
Benzalkonium Chloride; Benzocaine: (Moderate) The use of fluorescein with benzalkonium chloride aqueous solutions may be incompatible.
Beta-blockers: (Moderate) Patients on beta-blockers are at an increased risk of adverse reaction when administered fluorescein injection. It is thought that beta-blockers may worsen anaphylaxis severity by exacerbating bronchospasm or by increasing the release of anaphylaxis mediators; alternately, beta-blocker therapy may make the patient more pharmacodynamically resistance to epinephrine rescue treatment.

How Supplied

AK-Fluor/Fluorescein/Fluorescein Sodium/Fluorescite Intravenous Inj Sol: 10%, 25%
Fluorescein/Fluorescein Sodium/Ful-Glo Ophthalmic Strip: 0.6mg, 1mg

Maximum Dosage
Adults

Maximum dosage limits are not available.

Elderly

Maximum dosage limits are not available.

Adolescents

Maximum dosage limits are not available.

Children

Maximum dosage limits are not available.

Mechanism Of Action

Fluorescein is a fluorescent dye that is used as a diagnostic aid. The unbound fraction of the drug responds to electromagnetic radiation and light between the wavelengths of 465—490 nm and emits light at wavelengths of 520—530 nm. Thus, the fluorescein hydrocarbon is excited by blue light and emits yellowish-green light. Fluorescein is used both systemically to highlight the vascular circulation of the eye and topically to visualize the anterior surface of the eye. After intravenous injection, fluorescein circulates through the vasculature. A blue flash from a fundus camera onto the retina elicits the hallmark yellowish-green fluorescence of the dye. The fluorescence demarcates the retinal and/or choroidal vasculature under observation, distinguishing it from adjacent areas and structures. Images captured by the fundus camera are used to diagnosis abnormalities in and to monitor disease progression of the ocular vascular system. Following topical application of fluorescein on the eye, a cobalt blue lamp or slit lamp device is used to visualize the anterior ocular surface for defects and for contact lens fittings.

Pharmacokinetics

Fluorescein is administered intravenously in the antecubital vein and topically to the ocular surface. The drug undergoes rapid metabolism to fluorescein monoglucuronide with a hepatic clearance estimated at 1.5 mL/min/kg. Elimination of fluorescein and its metabolites occurs mainly through renal excretion with a renal clearance rate estimated at 1.75 mL/min/kg. The urine remains slightly fluorescent for 24—36 hours post dose.

Intravenous Route

Following IV administration, fluorescein is approximately 80% protein bound within human plasma and has a very rapid distribution within the vascular system; fluorescein may be seen in the central artery of the eye within 7—14 seconds of dosing. Soon after, fluorescein distributes into interstitial space with a total estimated volume of distribution of 0.5 L/kg. In a pharmacokinetic study of 7 healthy adults, approximately 80% of a 14 mg/kg dose was metabolized within 1 hour of IV administration. The manufacturer reports that systemic clearance was essentially complete by 48—72 hours after IV administration of 500 mg fluorescein.

Pregnancy And Lactation
Pregnancy

Use fluorescein during pregnancy only if clearly needed. There are insufficient data with the use of fluorescein in pregnant women to inform a drug-associated risk. It is not know whether fluorescein can cause fetal harm when administered to a pregnant woman. An accidental exposure has been documented in a case report. A 45-year-old woman was exposed via fluorescein angiography at pregnancy week 9. No adverse side effects to the mother or child were observed. Adequate animal reproduction studies have not been conducted with fluorescein.

Use fluorescin with caution in a breast-feeding woman. Fluorescein has been shown to be transferred into human milk for up to 4 days after IV administration.