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  • CLASSES

    Ophthalmological Corticosteroids
    Otic Corticosteroids
    Plain Topical Corticosteroids
    Topical Scalp Anti-inflammatories, with Corticosteroids

    DEA CLASS

    Rx

    DESCRIPTION

    Synthetic fluorinated corticosteroid of medium- to high-potency
    Used topically for inflammatory corticosteroid-responsive dermatoses and psoriasis in adult and pediatric patients; an otic oil-based solution is used for chronic eczematous external otitis
    Intravitreal implants are available that treat chronic non-infectious uveitis or diabetic macular edema

    COMMON BRAND NAMES

    Capex, Derma-Smoothe/FS, DermOtic Oil, Flac, Fluonid, Iluvien, Retisert, Synalar, YUTIQ

    HOW SUPPLIED

    Capex Topical Shampoo: 12mg
    Capex/Fluocinolone/Fluocinolone Acetonide/Fluonid/Synalar Topical Sol: 0.01%, 12mg
    Derma-Smoothe/FS/Fluocinolone/Fluocinolone Acetonide Topical Oil: 0.01%
    DermOtic Oil/Flac/Fluocinolone/Fluocinolone Acetonide Auricular (Otic) Oil: 0.01%
    Fluocinolone/Fluocinolone Acetonide/Iluvien Intravitreal Insert: 0.18mg, 0.19mg
    Fluocinolone/Fluocinolone Acetonide/Synalar Topical Cream: 0.01%, 0.025%
    Fluocinolone/Fluocinolone Acetonide/Synalar Topical Ointment: 0.025%
    Retisert Intravitreal Imp: 0.59mg

    DOSAGE & INDICATIONS

    For the treatment of mild to moderate inflammatory manifestations of corticosteroid-responsive dermatitis such as alopecia areata, atopic dermatitis, contact dermatitis, exfoliative dermatitis, Rhus dermatitis due to plants like poison ivy, or seborrheic dermatitis (facial and intertriginous areas), discoid lupus erythematosus (facial and intertriginous areas), eczema, granuloma annulare, intertrigo, cutaneous lichen planus, lichen simplex chronicus, polymorphous light eruption, pompholyx (dyshidrosis), nodular prurigo, anogenital or senilis pruritus, psoriasis (facial and intertriginous areas), or xerosis (inflammatory phase).
    For atopic dermatitis.
    Topical dosage (topical oil)
    Adults

    Apply topically as a thin film to the affected area 3 times per day.

    Adolescents, Children, and Infants 3 months and older

    Moisten skin and apply topically as a thin film to the affected areas twice daily. Do not treat longer than 4 weeks continuously. The FDA-approved use of Derma-Smoothe/FS oil in pediatric patients 3 months and older is limited to patients with moderate to severe atopic dermatitis. Do not apply to the face or diaper area. Avoid application to intertriginous areas.

    For psoriasis of the scalp.
    Topical dosage (topical oil)
    Adults

    Wet or dampen hair and scalp thoroughly prior to use. Apply a thin film of oil once daily, massage well and cover the scalp with the supplied shower cap. Leave on overnight or for a minimum of 4 hours before washing off. Wash hair with regular shampoo and rinse thoroughly. In a vehicle-controlled study, after 21 days of treatment 60% of patients receiving fluocinolone topical oil and 21% of patients receiving drug vehicle achieved a good to excellent clinical response.

    For seborrheic dermatitis of the scalp.
    Topical dosage (shampoo)
    Adults

    No more than one (1) ounce of shampoo should be applied to the scalp area once daily, worked into a lather and allowed to remain on the scalp for approximately 5 minutes. Rinse the hair and scalp completely twice. In vehicle-controlled studies, after 14 days of treatment, 84% of patients on fluocinolone and 29% of patients on drug vehicle had cleared or markedly improved.

    Topical dosage (cream, ointment, or topical solution)
    Adults

    Apply sparingly to the affected area 2 to 4 times per day, depending on the severity of the condition. In hairy sites, the hair should be parted to allow direct contact with the lesion. Occlusive dressings may be used for the management of recalcitrant conditions.

    Children and Adolescents

    Apply sparingly to the affected area 2 to 4 times per day, depending on the severity of the condition. In hairy sites, the hair should be parted to allow direct contact with the lesion. Occlusive dressings may be used for the management of recalcitrant conditions.

    For the treatment of chronic non-infectious uveitis affecting the posterior segment of the eye.
    Intravitreal implant dosage (Retisert)
    Adults

    Surgically insert 1 implant tablet (containing 0.59 mg fluocinolone acetonide) into the posterior segment of the affected eye. The implant releases fluocinolone acetonide at an initial rate of 0.6 mcg/day, decreasing over the first month to 0.3 to 0.4 mcg/day at steady state, and lasting approximately 30 months. If there is a recurrence of uveitis after the implant is depleted, the implant may be replaced.

    Intravitreal implant dosage (Yutiq)
    Adults

    Inject 1 implant (containing 0.18 mg fluocinolone acetonide) intravitreally. Monitor the patient for elevated intraocular pressure and endophthalmitis. The implant is designed to release fluocinolone acetonide at an initial rate of 0.25 mcg/day, and lasting 36 months.

    For the treatment of diabetic macular edema in patients who have been previously treated with a course of corticosteroids and did not have a clinically significant rise in intraocular pressure.
    Intravitreal implant dosage (Iluvien)
    Adults

    Inject 1 implant (containing 0.19 mg fluocinolone acetonide) intravitreally. Monitor the patient for elevated intraocular pressure and endophthalmitis. The implant is designed to release fluocinolone acetonide at an initial rate of 0.25 mcg/day, and lasting 36 months. According to the American Diabetes Association (ADA), intravitreous steroids are considered second-line alternative treatment options for central-involved diabetic macular edema (CIDME). These drugs are rarely used as first-line treatment options, because when compared against intravitreal injections of anti-vascular endothelial growth factor (anti-VEGF) agents, steroid therapies are associated with inferior visual acuity outcomes and increased rate of cataracts and glaucoma.

    For the treatment of chronic eczematous otitis externa.
    Otic topical dosage (Otic oil, e.g., DermOtic Oil 0.01%)
    Adults

    5 drops instilled into the affected ear(s) twice daily for 7 to 14 days; not to exceed 14 consecutive days of treatment.

    Children and Adolescents 2 years and older

    5 drops instilled into the affected ear(s) twice daily for 7 to 14 days; not to exceed 14 consecutive days of treatment.

    MAXIMUM DOSAGE

    NOTE: In general, corticosteroid dosage must be individualized and is highly variable depending on the nature and severity of the disease, dosage form selected, and patient age and response.

    Adults

    Topical: 4 applications/day cream, ointment, or topical solution; 3 applications/day topical oil; 1 ounce (30 mL)/day shampoo.
    Ophthalmic inserts: 1 Retisert implant approximately every 30 months; 1 Iluvien implant or Yutiq implant approximately every 36 months.

    Geriatric

    Topical: 4 applications/day cream, ointment, or topical solution; 3 applications/day topical oil; 1 ounce (30 mL)/day shampoo.
    Ophthalmic inserts: 1 Retisert implant approximately every 30 months; 1 Iluvien implant or Yutiq implant approximately every 36 months.

    Adolescents

    4 applications/day cream, ointment, or topical solution; 2 applications/day topical oil. Safety and efficacy have not been established for other dosage forms.

    Children

    2 years and older: 4 applications/day cream, ointment or topical solution; 2 applications/day topical oil. Safety and efficacy have not been established for other dosage forms.
    Less than 2 years: 2 applications/day topical oil. Safety and efficacy have not been established for other dosage forms.

    Infants

    3 months and older: 2 applications/day topical oil. Safety and efficacy have not been established for other dosage forms.
    Less than 3 months: Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no topical dosage adjustments are needed.

    Renal Impairment

    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    ADMINISTRATION

    Topical Administration
    Cream/Ointment/Lotion Formulations

    Cream, Ointment, or Topical Solution:
    For external use only.
    Apply sparingly in a thin film to the affected area and rub gently. Do not apply to areas of broken skin. Avoid contact with the eyes.
    When applying to hairy areas, part the hair and apply a small amount to the affected area or lesion; rub in gently.
    Until the medication has dried, protect from washing, clothing, or rubbing. Hair may be washed as usual but not immediately after application.
    Occlusive dressing may be used for the management of psoriasis or recalcitrant conditions; follow the orders of the prescriber.

    Other Topical Formulations

    Shampoo:
    For external use only.
    Prior to dispensing: Empty the contents of the enclosed capsule into the shampoo base prior to dispensing. Shake well. The extemporaneously prepared shampoo is stable for 2 months from the time of preparation.
    Shake shampoo well prior to each use.
    Apply to the scalp area and work into a lather. Let stand for 5 minutes, then rinse thoroughly.
    In case of eye contact, rinse liberally with water.
     
    Topical Body Oil:
    For external use only. Shake well before each use.
    Moisten the affected skin area; apply a thin film of oil to the affected area and rub in gently.
    Do not apply to the face, axillae, groin, or diaper area unless specifically directed by the prescriber. Avoid application to intertriginous areas.
    Do not use with occlusive dressing unless under the specific order of the prescriber.
     
    Scalp Topical Oil:
    For external use only. For use on the scalp only.
    Wet or dampen hair and scalp before using.
    Apply a thin film of oil, massage well, and cover the scalp with the supplied shower cap.
    Leave on overnight or for a minimum of 4 hours before washing off.
    Wash hair with regular shampoo and rinse thoroughly.

    Otic Administration

    Otic Oil:
    For external ear use only.
    The patient should tilt their head so the affected ear is facing up. Pull the earlobe backward and upward and use the supplied ear-dropper to apply the drops. The patient should keep their head tilted for approximately 1 minute and use a clean cotton ball to remove any excess medication dripping form the ear.
    Administration may be repeated, if necessary, for the opposite ear.
    Do not use occlusive dressings.
    Avoid contact with the eyes. In case of contact, rinse eyes liberally with water.

    Other Administration Route(s)

    Intravitreal Administration
    Intravitreal administration procedures should be carried out under aseptic conditions as directed for the specific product.
     
    Retisert implant tablet for surgical implantation:
    Fluocinolone intravitreal implants (Retisert) are surgically implanted into the posterior segment of the affected eye.
    Implants should only be handled by the suture tab, as damage to the implant can result in an increased rate of drug release.
    During implantation, care should be taken avoid sheer forces on the implant that could disengage the silicone cup reservoir (which contains a fluocinolone acetonide tablet) from the suture tab.
    Prolonged hydration may reduce the strength of the adhesive bond between the silicone cup reservoir and the suture tab, indicating a potential for the separation of these components. Monitor the integrity of the implant during ophthalmologic examinations.
    Do not resterilize fluocinolone intravitreal implant tablets by any method.
     
    Iluvien implant for intravitreal injection:
    Intravitreal administration should be carried out under aseptic conditions, which include use of sterile gloves, a sterile drape, a sterile caliper, and a sterile eyelid speculum (or equivalent). Adequate anesthesia and a broad-spectrum microbicide should be given prior to insertion.
    Optimal placement of the implant is inferior to the optic disc and posterior to the equator of the eye. Measure 4 millimeters inferotemporal from the limbus with the aid of calipers for point of entry into the sclera.
    The exterior of the tray should not be considered sterile. Do not use unit if there are signs of damage to the tray or lid. Do not touch the interior surface when peeling the lid from the tray. Visually check through the viewing window of the preloaded applicator to ensure that there is a drug implant inside.
    With sterile, gloved hands, remove the applicator from the tray touching only the sterile interior tray surface and applicator. The applicator tip must be kept above the horizontal plane prior to injection to ensure that the implant is properly positioned within the applicator.
    Just before inserting the needle into the eye, remove the protective cap and gently push the applicator button down and slide it to the first stop (at the curved black marks alongside the button track). At the first stop, release the button and it should move to the UP position. Do not use the unit if it does not move to the UP position.
    Inspect the tip of the needle to ensure it is not bent.
    Gently displace the conjunctiva so that after withdrawing the needle, the conjunctival and scleral needle entry sites will not align. Avoid contact between the needle and the lid margin or lashes. Insert the needle through the conjunctiva and sclera. To release the implant, while the button is in the UP position, advance the button by sliding it forward to the end of the button track and remove the needle. Do not remove the needle until the button reaches the end of the track.
    Remove the lid speculum and perform indirect ophthalmoscopy to verify placement of the implant, adequate central retinal artery perfusion and absence of any other complications.
    Immediately after the intravitreal injection, monitor the patient for elevation in intraocular pressure (IOP) and endophthalmitis. Appropriate monitoring may consist of a check for perfusion of the optic nerve head immediately after the injection, tonometry within 30 minutes following the injection, and biomicroscopy 2 to 7 days following the injection.
    Instruct patients to promptly report any symptoms suggestive of endophthalmitis.
     
    Yutiq implant for intravitreal injection:
    Intravitreal administration should be carried out under aseptic conditions, which include use of sterile gloves, a sterile drape, a sterile caliper, and a sterile eyelid speculum (or equivalent). Adequate anesthesia and a broad-spectrum microbicide should be given prior to insertion.
    Just prior to injection, administer topical and/or subconjunctival anesthesia at the injection site (inferotemporal quadrant recommended).
    Administer 2 to 3 drops of a broad-spectrum microbicide into the lower fornix. The lids may be scrubbed with cotton-tipped applicators soaked with a broad-spectrum microbicide. Place a sterile lid speculum. Have the patient look up and apply additional microbicide solution to the injection site. Allow 30 to 60 seconds for the topical antiseptic to dry prior to injection.
    Optimal placement is inferior to the optic disc and posterior to the equator of the eye. Measure 4 millimeters inferotemporal from the limbus with the aid of callipers for point of entry into the sclera.
    Using sterile procedure, open the sterile foil pouch.
    Remove the applicator from the sterile pouch by grasping the barrel of the applicator; do not grasp the plunger.
    Remove the black plunger stop from the plunger.
    Carefully remove the protective cap from the needle and inspect the needle tip to ensure it is not bent.
    Remove the trombone wire from the distal end of the needle. Prior to injection, keep the applicator tip above the horizontal plane to ensure that the implant does not fall out of the applicator.
    Gently displace the conjunctiva so that after withdrawing the needle, the conjunctival and scleral needle entry sites will not align. Care should be taken to avoid contact between the needle and the lid margin or lashes.
    Insert the needle through the conjunctiva and sclera up to the positive stop of the applicator.
    Depress the plunger at the back of the applicator fully to deliver the implant into the back of the eye.
    Remove the applicator from the eye and discard in biohazard sharps container.
    Remove the lid speculum and perform indirect ophthalmoscopy to verify adequate central retinal artery perfusion, absence of any other complications, and to verify the placement of the implant. Scleral depression may enhance visualisation of the implant. Immediate measurement of intraocular pressure (IOP) may be performed at the discretion of the ophthalmologist.
    Immediately after the intravitreal injection, monitor the patient for elevation in intraocular pressure (IOP) and endophthalmitis. Appropriate monitoring may consist of a check for perfusion of the optic nerve head immediately after the injection, tonometry within 30 minutes following the injection, and biomicroscopy 2 to 7 days following the injection. Instruct patients to promptly report any symptoms suggestive of endophthalmitis.

    STORAGE

    Generic:
    - Avoid excessive heat (above 104 degrees F)
    - Protect from freezing
    - Store between 59 to 77 degrees F
    Capex:
    - Product should be used within 2 months after opening
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    Derma-Smoothe/FS:
    - Store at 77 degrees F; excursions permitted to 59-86 degrees F
    DermOtic Oil :
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    Flac:
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
    Fluonid :
    - Avoid excessive heat (above 104 degrees F)
    - Protect from freezing
    - Store between 59 to 77 degrees F
    Iluvien:
    - Store at room temperature (between 59 to 86 degrees F)
    Retisert:
    - Protect from freezing
    - Store between 59 to 77 degrees F
    - Store in original container
    Synalar:
    - Avoid excessive heat (above 104 degrees F)
    - Protect from freezing
    - Store between 59 to 77 degrees F
    YUTIQ:
    - Store at room temperature (between 59 to 86 degrees F)

    CONTRAINDICATIONS / PRECAUTIONS

    Cushing's syndrome, hypothalamic-pituitary-adrenal (HPA) suppression, occlusive dressing, skin abrasion

    Systemic absorption of topical corticosteroids such as fluocinolone can produce reversible hypothalamic-pituitary-adrenal (HPA) suppression, manifestations of Cushing's syndrome, hyperglycemia, and glucosuria in some patients. To minimize risk of HPA axis suppression, patients should be treated for no more than 2 weeks at a time and only small areas should be treated. Conditions that increase systemic absorption include use over large surface areas, prolonged use, use in areas where the epidermal barrier is disrupted (i.e., skin abrasion), and the use of occlusive dressings. Fluocinolone and other fluorinated topical corticosteroids should be used cautiously on areas of the body that have a thin layer of skin. Absorption of topical steroids is markedly increased when these agents are applied to areas such as the axilla, eyelids, face, scalp, or scrotum. Patients applying fluocinolone to a large surface area or to areas under an occlusive dressing should be evaluated periodically for evidence of HPA axis suppression. If HPA axis suppression is noted, an attempt should be made to withdraw the drug, to reduce the frequency of application, or to substitute a less potent corticosteroid.

    Ocular exposure, ophthalmic administration

    Care should be taken to avoid ocular exposure to topical fluocinolone products; ophthalmic administration of topical fluocinolone creams, ointments, topical solutions and topical or otic oils should be avoided.

    Children, growth inhibition, increased intracranial pressure, infants, neonates

    Children, infants, and neonates may demonstrate a greater susceptibility to topical corticosteroid induced hypothalamic-pituitary-adrenal (HPA) axis suppression and Cushing's syndrome compared to adult patients because of larger skin surface area to body weight ratio. HPA axis suppression, Cushing's syndrome, and increased intracranial pressure have been reported in children receiving topical corticosteroids. Manifestations of adrenal suppression in children include growth inhibition (linear growth retardation and delayed weight gain), low plasma cortisol levels, and absence of response in ACTH stimulation. Manifestations of intracranial hypertension including bulging fontanelles, headaches, and bilateral papilledema. Administration of topical corticosteroids to children should be limited to the least amount compatible with an effective therapeutic regimen. Chronic use may interfere with growth and development. Use topical products with caution in young children; if children are being treated topically in the diaper area, tight-fitting diapers or plastic pants should be avoided as these garments may act as an occlusive dressing and increase systemic absorption of the drug. The safety and efficacy of fluocinolone otic drops have not been established in pediatric patients under 2 years of age. Safety and effectiveness of Retisert fluocinolone intravitreal implant tablets have not been established in pediatric patients below the age of 12 years ; the Iluvien and Yutiq intravitreal implants have not been studied in pediatric patients.
     

    Fungal infection, herpes infection, herpes simplex keratitis (dendritic keratitis), infection, measles, ocular infection, varicella, viral infection

    Topical corticosteroids should be used with caution in individuals with dermatological infections; the normal inflammatory response to local infections can be masked by corticosteroids such as fluocinolone. Application of topical corticosteroids to areas of infection, including tuberculosis of the skin, dermatologic fungal infection, and cutaneous or systemic viral infection (e.g., herpes infection, measles, varicella), should be initiated or continued only if the appropriate antiinfective treatment is instituted. If a favorable response does not occur promptly, the corticosteroid should be discontinued until the infection has been adequately controlled. Fluocinolone intravitreal implants (Retisert, Iluvien, and Yutiq) are contraindicated for use in ocular infection, including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, or varicella, as well as ophthalmic bacterial, mycobacterial, viral, and fungal infections. Corticosteroid implants are not recommended to be used in patients with a history of ocular herpes simplex because of the potential for reactivation of the viral infection. Corticosteroids reduce resistance to infections; do not perform simultaneous bilateral intravitreal implantation in order to limit the possibility of post-operative bilateral ophthalmic infection or other adverse effects.

    Acne rosacea, acne vulgaris, perioral dermatitis

    High-potency topical corticosteroids should not be used to treat acne vulgaris, acne rosacea, or perioral dermatitis. Fluocinolone may aggravate these conditions. Topical corticosteroids may delay the healing of non-infected wounds, such as venous stasis ulcers.

    Diabetes mellitus

    Topical corticosteroids, like fluocinolone, should be used with caution in patients with diabetes mellitus. Exacerbation of diabetes may occur with systemic absorption of the topical corticosteroid. Use of topical corticosteroids may further delay healing of skin ulcers in diabetic patients.

    Geriatric, skin atrophy

    Topical corticosteroids, like fluocinolone, should be used for brief periods, or under close medical supervision in patients with evidence of pre-existing skin atrophy. Geriatric patients may be more likely to have preexisting skin atrophy secondary to aging. Purpura and skin lacerations that may raise the skin and subcutaneous tissue from deep fascia may be more likely to occur with the use of topical corticosteroids in geriatric patients. Use of lower potency topical corticosteroids also may be necessary in some patients.

    Pregnancy

    There are no adequate and well-controlled studies of topical application or intravitreal insertion of fluocinolone during pregnancy. Use during pregnancy only when clearly needed. Topical corticosteroids, including fluocinolone, should not be used in large amounts, on large areas, or for prolonged periods of time in pregnant women. Guidelines recommend mild to moderate potency topical agents over potent corticosteroids, which should be used in short durations. Fetal growth restriction and a significantly increased risk of low birthweight has been reported with use of potent or very potent topical corticosteroids during the third trimester, particularly when using more than 300 grams. Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals.

    Breast-feeding

    It is not known whether topical or intravitreal administration of fluocinolone could result in sufficient systemic absorption to produce detectable quantities in breast milk.   However, most dermatologists stress that topical corticosteroids can be safely used during lactation and breast-feeding. If applied topically, care should be used to ensure the infant will not come into direct contact with the area of application, such as the breast. Increased blood pressure has been reported in an infant whose mother applied a high potency topical corticosteroid ointment directly to the nipples. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    Peanut hypersensitivity

    Fluocinolone body, scalp, and otic topical oils contain refined peanut oil, USP. Avoid using these products in patients with peanut hypersensitivity as hypersensitivity reactions have been reported. If wheal and flare type reactions, which may be limited to pruritus, or other manifestations of hypersensitivity develop, the products should be discontinued immediately. In one study, topical fluocinolone 0.01% in peanut oil was well tolerated even in patients with peanut allergic sensitivity. Another article concurred.

    Corticosteroid hypersensitivity

    Although true corticosteroid hypersensitivity is rare, patients who have demonstrated a prior hypersensitivity reaction to fluocinolone should not receive the drug. It is possible, though also rare, that such patients will display cross-hypersensitivity to other corticosteroids. It is advisable that patients who have a hypersensitivity reaction to any corticosteroid undergo skin testing, which, although not a conclusive predictor, may help to determine if hypersensitivity to another corticosteroid exists. Such patients should be carefully monitored during and following the administration of any corticosteroid.

    Glaucoma, implant insertion and removal complications, increased intraocular pressure

    Use of corticosteroids including the fluocinolone intravitreal implants may produce posterior subcapsular cataracts, increased intraocular pressure, and glaucoma. The Iluvien fluocinolone intravitreal implant is contraindicated for use in patients with glaucoma who have a cup to disc ratio greater than 0.8. Intravitreal implant insertion and removal complications have been reported, and may vary with the implant and the technique used for insertion. For example, patients with an absent or torn posterior capsule of the lens are at increased risk of migration of an intravitreal implant into the anterior chamber.

    ADVERSE REACTIONS

    Severe

    ocular hypertension / Delayed / 22.0-90.0
    visual impairment / Early / 10.0-40.0
    macular edema / Delayed / 10.0-40.0
    ocular hemorrhage / Delayed / 10.0-40.0
    retinal detachment / Delayed / 5.0-9.0
    retinal hemorrhage / Delayed / 5.0-9.0
    optic atrophy / Delayed / 2.0-2.0
    skin atrophy / Delayed / Incidence not known
    papilledema / Delayed / Incidence not known
    increased intracranial pressure / Early / Incidence not known
    wound dehiscence / Delayed / Incidence not known
    endophthalmitis / Delayed / Incidence not known

    Moderate

    cataracts / Delayed / 50.0-90.0
    blurred vision / Early / 10.0-40.0
    hypotonia / Delayed / 7.0-40.0
    conjunctival hyperemia / Early / 2.0-40.0
    erythema / Early / 1.0-10.0
    photophobia / Early / 2.0-9.0
    conjunctivitis / Delayed / 4.0-9.0
    photopsia / Delayed / 5.0-9.0
    ocular inflammation / Early / 1.0-9.0
    blepharitis / Early / 5.0-9.0
    hyphema / Delayed / 5.0-9.0
    corneal edema / Early / 4.0-9.0
    withdrawal / Early / Incidence not known
    growth inhibition / Delayed / Incidence not known
    hypothalamic-pituitary-adrenal (HPA) suppression / Delayed / Incidence not known
    Cushing's syndrome / Delayed / Incidence not known
    hypertension / Early / Incidence not known
    hyperglycemia / Delayed / Incidence not known
    glycosuria / Early / Incidence not known
    pseudotumor cerebri / Delayed / Incidence not known
    adrenocortical insufficiency / Delayed / Incidence not known
    ocular infection / Delayed / Incidence not known
    skin ulcer / Delayed / Incidence not known
    impaired wound healing / Delayed / Incidence not known
    tolerance / Delayed / Incidence not known
    contact dermatitis / Delayed / Incidence not known

    Mild

    ocular pain / Early / 8.0-90.0
    foreign body sensation / Rapid / 3.0-40.0
    ocular pruritus / Rapid / 3.0-40.0
    ocular irritation / Rapid / 1.0-40.0
    xerophthalmia / Early / 10.0-40.0
    blepharedema / Early / 10.0-40.0
    ptosis / Delayed / 10.0-40.0
    headache / Early / 9.0-33.0
    pharyngitis / Delayed / 5.0-20.0
    xerosis / Delayed / 1.0-10.0
    maculopapular rash / Early / 1.0-10.0
    pruritus / Rapid / 1.0-10.0
    skin irritation / Early / 1.0-10.0
    diplopia / Early / 5.0-9.0
    ocular discharge / Delayed / 2.0-9.0
    lacrimation / Early / 1.0-9.0
    arthralgia / Delayed / 2.0-5.0
    miliaria / Delayed / Incidence not known
    purpura / Delayed / Incidence not known
    folliculitis / Delayed / Incidence not known
    telangiectasia / Delayed / Incidence not known
    striae / Delayed / Incidence not known
    acneiform rash / Delayed / Incidence not known
    infection / Delayed / Incidence not known
    hypertrichosis / Delayed / Incidence not known
    skin hypopigmentation / Delayed / Incidence not known
    sinusitis / Delayed / Incidence not known

    DRUG INTERACTIONS

    Benzalkonium Chloride: (Moderate) The use of topical aluminum products (aluminum acetate, Burow's solution or aluminum chloride) with benzalkonium chloride aqueous solutions may be incompatible.
    Metyrapone: (Major) Medications which affect pituitary or adrenocortical function, including all corticosteroid therapy, should be discontinued prior to and during testing with metyrapone. Patients taking inadvertent doses of corticosteroids on the test day may exhibit abnormally high basal plasma cortisol levels and a decreased response to the test. Although systemic absorption of topical corticosteroids is minimal, temporary discontinuation of these products should be considered if possible to reduce the potential for interference with the test results.

    PREGNANCY AND LACTATION

    Pregnancy

    There are no adequate and well-controlled studies of topical application or intravitreal insertion of fluocinolone during pregnancy. Use during pregnancy only when clearly needed. Topical corticosteroids, including fluocinolone, should not be used in large amounts, on large areas, or for prolonged periods of time in pregnant women. Guidelines recommend mild to moderate potency topical agents over potent corticosteroids, which should be used in short durations. Fetal growth restriction and a significantly increased risk of low birthweight has been reported with use of potent or very potent topical corticosteroids during the third trimester, particularly when using more than 300 grams. Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals.

    It is not known whether topical or intravitreal administration of fluocinolone could result in sufficient systemic absorption to produce detectable quantities in breast milk.   However, most dermatologists stress that topical corticosteroids can be safely used during lactation and breast-feeding. If applied topically, care should be used to ensure the infant will not come into direct contact with the area of application, such as the breast. Increased blood pressure has been reported in an infant whose mother applied a high potency topical corticosteroid ointment directly to the nipples. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.

    MECHANISM OF ACTION

    Corticosteroids inhibit inflammatory responses to a variety of inciting agents including multiple inflammatory cytokines. They inhibit edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation. Corticosteroids are thought to act by inhibition of phospholipase A2 via induction of inhibitory proteins collectively called lipocortins. It is postulated that these proteins control biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting release of the common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Topical corticosteroids exhibit anti-inflammatory, antipruritic, and vasoconstrictive properties. These actions correspond to decreased edema, erythema, pruritus, plaque formation and scaling of the affected skin.

    PHARMACOKINETICS

    Fluocinolone is applied topically as a cream, ointment, solution, shampoo or topical oil and can be for ophthalmic use as an intravitreal implant. Anti-inflammatory effects are usually not seen for hours after fluocinolone application, since the mechanism of action requires alterations in synthesis of proteins. Because fluocinolone is fluorinated and also contains a substituted 17-hydroxyl group, it is not metabolized in the skin. Repeated application results in a cumulative depot effect in the skin, which may lead to a prolonged duration of action and increased systemic absorption. Fluocinolone is metabolized primarily in the liver and excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

    Topical Route

    The extent of percutaneous absorption of the topical corticosteroids is dependent on many factors, including the pharmaceutical vehicle and the integrity of the epidermis. Absorption after topical application of fluocinolone is increased in areas that have skin damage, inflammation, or occlusion, or in areas where the stratum corneum is thin such as the eyelids, genitalia, axillae, and face. The use of occlusive dressings with the application of fluocinolone enhances penetration into the skin, and may increase the chance of systemic absorption. Ointments have a hydrating effect, are lipophilic, and enhance the penetration of clobetasol into the skin. Fluocinolone solutions also have enhanced topical penetration versus cream preparations.

    Other Route(s)

    Ophthalmic Route
    There appears to be minimal systemic absorption following ophthalmic administration. Following intravitreal implantation of one 0.59 mg fluocinolone acetonide tablet (Retisert), fluocinolone acetonide is released at a rate of approximately 0.6 mcg/day, decreasing over the first month to a steady state of 0.3—0.4 mcg/day over approximately 30 months. In this time period, aqueous and vitreous humor concentrations are highly variable. In clinical trials, throughout an observational period of up to 34 months, aqueous and vitreous humor concentrations ranged from below the limit of detection (0.2 ng/mL) to 589 ng/mL. Following intravitreal implantation of a 0.2 mcg/day or 0.5 mcg/day fluocinolone acetonide insert, plasma concentrations of fluocinolone acetonide were below the lower limit of quantitation at all post-administration time points from day 7 through month 36 in a human pharmacokinetic study.