Synalar

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

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.

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 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.

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.

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
wound dehiscence / Delayed / Incidence not known
endophthalmitis / Delayed / Incidence not known

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
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

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
pruritus / Rapid / 1.0-10.0
skin irritation / Early / 1.0-10.0
xerosis / Delayed / 1.0-10.0
maculopapular rash / 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
folliculitis / Delayed / Incidence not known
purpura / Delayed / Incidence not known
infection / Delayed / Incidence not known
miliaria / Delayed / Incidence not known
acneiform rash / Delayed / Incidence not known
telangiectasia / Delayed / Incidence not known
hypertrichosis / Delayed / Incidence not known
striae / Delayed / Incidence not known
skin hypopigmentation / Delayed / Incidence not known
sinusitis / Delayed / Incidence not known

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

Rx

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

Apply a thin layer topically to the affected skin area(s) 2 times daily until symptoms resolve. Proactive, intermittent application of topical corticosteroids 1 to 2 times weekly to areas that commonly flare is recommended to help prevent relapses.

Apply a thin layer topically to the affected skin area(s) 2 times daily until symptoms resolve. Proactive, intermittent application of topical corticosteroids 1 to 2 times weekly to areas that commonly flare is recommended to help prevent relapses.

Apply a thin layer topically to the affected skin area(s) 2 times daily until symptoms resolve. If no improvement within 2 weeks, reassess diagnosis. Proactive, intermittent application of topical corticosteroids 1 to 2 times weekly to areas that commonly flare is recommended to help prevent relapses.

Apply a thin layer topically to the affected skin area(s) 2 times daily until symptoms resolve for up to 4 weeks. If no improvement within 2 weeks, reassess diagnosis. Proactive, intermittent application of topical corticosteroids 1 to 2 times weekly to areas that commonly flare is recommended to help prevent relapses.

Apply up to 1 ounce topically to the scalp area once daily; work into a lather and allow to remain on the scalp for approximately 5 minutes, then rinse the hair and scalp thoroughly with water.

Apply a thin layer topically to the affected skin area(s) 2 to 4 times daily.

Apply a thin layer topically to the affected skin area(s) 2 to 4 times daily.

Apply a thin layer topically to the affected skin area(s) 3 to 4 times daily.

Apply a thin layer topically to the affected skin area(s) 3 to 4 times daily.

Apply a thin layer topically to the affected skin area(s) 2 to 4 times daily. The duration of the therapy depends on factors such as the topical corticosteroid potency, disease severity and anatomic location, and age. After improvement, may consider transitioning to lower-potency corticosteroid, using intermittent therapy, and combining treatment with noncorticosteroidal agents. Taper by reducing use to every other day, then twice weekly, then discontinue if adequate control is maintained. Guidelines recommend class 1 to 5 topical corticosteroids for up to 4 weeks for plaque psoriasis not involving intertriginous areas and class 1 to 7 topical corticosteroids for a minimum of up to 4 weeks for scalp psoriasis. Use of topical corticosteroids for more than 12 weeks may be considered under careful supervision.

Apply a thin layer topically to the affected skin area(s) 2 to 4 times daily. Guidelines recommend topical corticosteroids as monotherapy for short-term treatment of localized psoriasis.

Apply a thin layer topically to the affected skin area(s) 3 to 4 times daily. The duration of the therapy depends on factors such as the topical corticosteroid potency, disease severity and anatomic location, and age. After improvement, may consider transitioning to lower-potency corticosteroid, using intermittent therapy, and combining treatment with noncorticosteroidal agents. Taper by reducing use to every other day, then twice weekly, then discontinue if adequate control is maintained. Guidelines recommend class 1 to 5 topical corticosteroids for up to 4 weeks for plaque psoriasis not involving intertriginous areas and class 1 to 7 topical corticosteroids for a minimum of up to 4 weeks for scalp psoriasis. Use of topical corticosteroids for more than 12 weeks may be considered under careful supervision.

Apply a thin layer topically to the affected skin area(s) 3 to 4 times daily. Guidelines recommend topical corticosteroids as monotherapy for short-term treatment of localized psoriasis.

Apply topically to the psoriatic scalp area(s) once daily. The duration of the therapy depends on factors such as the topical corticosteroid potency, disease severity and anatomic location, and age. After improvement, may consider transitioning to lower-potency corticosteroid, using intermittent therapy, and combining treatment with noncorticosteroidal agents. Taper by reducing use to every other day, then twice weekly, then discontinue if adequate control is maintained. Guidelines recommend class 1 to 7 topical corticosteroids for a minimum of up to 4 weeks for scalp psoriasis. Use of topical corticosteroids for more than 12 weeks may be considered under careful supervision.

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.

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.

0.19 mg implant by intravitreal injection in the affected eye(s). The implant is designed to release fluocinolone acetonide at an initial rate of 0.25 mcg/day, and lasting 36 months. Steroid therapies are associated with inferior visual acuity outcomes and increased rate of cataracts and glaucoma when compared against intravitreal injections of anti-vascular endothelial growth factor (anti-VEGF) agents.

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

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

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

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

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.
Voriconazole: (Moderate) Monitor for potential adrenal dysfunction with concomitant use of voriconazole and fluocinolone. In patients taking corticosteroids, voriconazole-associated CYP3A4 inhibition of their metabolism may lead to corticosteroid excess and adrenal suppression. Corticosteroid exposure is likely to be increased. Voriconazole is a strong CYP3A4 inhibitor, and fluocinolone is a CYP3A4 substrate.

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/Synalar Topical Cream: 0.01%, 0.025%
Fluocinolone/Fluocinolone Acetonide/Synalar Topical Ointment: 0.025%
Iluvien/YUTIQ Intravitreal Insert: 0.18mg, 0.19mg
Retisert Intravitreal Imp: 0.59mg

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.

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.

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.

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

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.

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.

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.

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.

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.

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.

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.