OTOCROVIS

Fluocinolone acetonide, with the formula 6-alpha, 9-alpha-difluoro-16-alpha, 17 alpha-acetonide, is a corticosteroid that presents a high lipophilicity.

It has been used extensively in dermatological preparations and it has also been investigated thoroughly for its use in implantable corticosteroid devices.

This type of device containing fluocinolone acetonide was developed by Taro Pharmaceuticals and approved by FDA in May 2016.

Fluocinolone acetonide has been used extensively in different medical areas. -In dermatology, it is extensively used for the relief of inflammatory dermatosis, dermatitis, psoriasis, hypertrophic tissues, keloid tissues and atopic dermatitis. 17 -It has been used in shampoo products as a low to medium potency corticosteroid for the treatment of seborrheic dermatitis of the scalp. 12 -In ear drops, it is used as a low to medium potency corticosteroid for the treatment of chronic eczematous external otitis in adults and pediatric patients 2 years and older. 13 -As an intravitreal implant, it is indicated for the treatment of diabetic macular edema with patients that have been previously treated with a course of corticosteroids and no clinically significant rise in intraocular pressure. 14 -Fluocinolone acetonide was announced on October to be FDA approved for the treatment of chronic non-infectious uveitis affecting the posterior segment of the eye. 15 -Some reports have indicated the use of fluocinolone acetonide as a vasoprotective agent and for its use in the treatment of first-degree hemorrhoids.

Fluocinolone acetonide is a synthetic anti-inflammatory corticosteroid and thus, the effect of its interaction with the body produces vasoconstriction and suppression of membrane permeability, mitotic activity, immune response and release of inflammatory mediators.

For its ophthalmic indications, fluocinolone acetonide is administered as intravitreal micro-insert.

This preparation was observed in clinical trials to reduce the recurrence of uveitis flares by 2 fold when compared with the non treated patients even after six months after initial administration.

As well the intraocular pressure seemed to increase slightly with the presence of the fluocinolone implant but it is important to monitor intraocular pressure.

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When administered as an eye implant, fluocinolone acetonide presents a sustained delivery for even 12 months in which there can be observed a sustained release.

The concentration of fluocinolone acetonide are generally higher in the vitreous and retina with a little dispersion to the aqueous humor.

There are reports indicating that topical administration of fluocinolone acetonide produces a percutaneous absorption which is determined by the vehicle, integrity of the epidermal barrier and the use of occlusive dressing.

Independently of the route of administration, the systemic absorption of fluocinolone acetonide is below 0.1 ng/ml which indicates that the systemic distribution is very minimal and the effect of fluocinolone is mainly local.

This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.

Following absorption, fluocinolone acetonide metabolism is primarily hepatic.

It is important to mention that the systemically absorbed dose is very minimal.

Fluocinolone acetonide is mainly excreted by the kidneys.

It is important to mention that the systemically absorbed dose is very minimal.

The reported half-life of fluocinolone acetonide ranges between 1.3-1.7 hours.

This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal and the concentration in urine is lower than the minimum quantitation limit.

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Studies to determine the carcinogenic and its effect in fertility have not been performed.

It is important to consider that several corticosteroids have been shown to present genotoxic potential but fluocinolone acetonide was shown to not be genotoxic in the Ames test and mouse lymphoma TK assay.

Topical corticosteroids are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.

Solution is generally applied to the affected area as a thin film from two to four times daily depending on the severity of the condition.

In hairy sites, the hair should be parted to allow direct contact with the lesion.

Occlusive dressing may be used for the management of psoriasis or recalcitrant conditions.

If an infection develops, the use of occlusive dressings should be discontinued and appropriate antimicrobial therapy instituted.

USP, 0.01% is available in 20 mL (NDC 51672-1365-2) and 60 mL (NDC 51672-1365-4) bottles.

Store at 20° to 25°C (68° to 77°F) .

Avoid excessive heat.

Protect from freezing.

Store at 20° to 25°C (68° to 77°F) .

Avoid excessive heat.

Protect from freezing.

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.

There are no adequate and well-controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids.

Therefore, topical corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods of time.

It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk.

Systemically administered corticosteroids are secreted into breast milk in quantities not likely to have a deleterious effect on the infant.

Nevertheless, caution should be exercised when topical corticosteroids are administered to a nursing woman.

Pediatric patients may demonstrate greater susceptibility to topical corticosteroid-induced hypothalmic-pituitary-adrenal (HPA) axis suppression and Cushing's syndrome than mature patients because of a larger skin surface area to body weight ratio.

Hypothalmic-pituitary-adrenal (HPA) axis suppression, Cushing's syndrome, and intracranial hypertension have been reported in children receiving topical corticosteroids.

Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol levels, and absence of response to ACTH stimulation.

Manifestations of intracranial hypertension include 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 corticosteroid therapy may interfere with the growth and development of children.