FLUOCINOLONE ACETONIDE
DESCRIPTION:
These preparations are all intended for topical administration.
FLUCORT preparations have as their active component the corticosteroid
fluocinonide, which is the 21-acetate ester of fluocinolone acetonide and has
the chemical name pregna-1,4-diene- 3,20-dione, 21-(acetyloxy)-6,9-difluoro- 11-
hydroxy- 16,17-((1-methylethylidene)bis(oxy))-, (6alpha,11beta, 16alpha)-.
FLUCORT cream contains fluocinonide 0.5 mg/g in FAPG(R) cream, a specially
formulated cream base consisting of citric acid, 1,2,6-hexanetriol, polyethylene
glycol 8000, propylene glycol and stearyl alcohol. This white cream vehicle is
greaseless, non-staining, anhydrous and completely water miscible. The base
provides emollient and hydrophilic properties. In this formulation the active
ingredient is totally in solution.
FLUCORT gel contains fluocinonide 0.5 mg/g in a specially formulated gel base
consisting of carbomer 940, edetate disodium, propyl gallate, propylene glycol,
sodium hydroxide and/or hydrochloric acid (to adjust the pH), and water
(purified). This clear, colorless thixotropic vehicle is greaseless, non-
staining and completely water miscible. In this formulation the active
ingredient is totally in solution.
FLUCORT ointment contains fluocinonide 0.5 mg/g in a specially formulated ointment
base consisting of glyceryl monostearate, white petrolatum, propylene carbonate,
propylene glycol, and white wax. It provides the occlusive and emollient effects
desirable in an ointment. In this formulation the active ingredient is totally
in solution.
FLUCORT topical solution contains fluocinonide 0.5 mg/mL in a solution of alcohol
(35%), citric acid, diisopropyl adipate, and propylene glycol. In this
formulation the active ingredient is totally in solution.
FLUCORT-E cream contains fluocinonide 0.5 mg/g in a water-washable aqueous
emollient base of cetyl alcohol, citric acid, mineral oil, polysorbate 60,
propylene glycol, sorbitan monostearate, stearyl alcohol, and water (purified).
SYNALAR preparations have as their active component the corticosteroid
fluocinolone acetonide, which has the chemical name pregna- 1,4-diene-3,20-
dione,6,9-difluoro- 11,21-dihydroxy- 16,17-((1-methylethylidene)bis(oxy))-,
(6alpha,11beta, 16alpha)-.
SYNALAR cream contains fluocinolone acetonide 0.25 mg/g in a water-washable
aqueous base of stearyl alcohol, propylene glycol, cetyl alcohol, polyoxyl 20
cetostearyl ether, mineral oil, white wax, simethicone, butylated
hydroxytoluene, edetate disodium, citric acid, and purified water, with
methylparaben and propylparaben as preservatives.
SYNALAR Ointment contains fluocinolone acetonide 0.25 mg/g in white petrolatum
U.S.P.
SYNALAR solution contains fluocinolone acetonide 0.1 mg/mL in a water-washable
base of citric acid and propylene glycol.
SYNEMOL Cream contains flucinolone acetonide 0.25mg/g in an emollient base of
cetyl alcohol, citric acid, mineral oil, polysorbate 60, propylene glycol,
corbitan monostearate, stearyl alcohol, and water (purified).
ACTIONS/CLINICAL PHARMACOLOGY:
Topical corticosteroids share anti-inflammatory, anti-pruritic and
vasoconstrictive actions.
The mechanism of anti-inflammatory activity of the topical corticosteroids is
unclear. Various laboratory methods, including vasoconstrictor assays, are used
to compare and predict potencies and/or clinical efficacies of the topical
corticosteroids. There is some evidence to suggest that a recognizable
correlation exists between vasoconstrictor potency and therapeutic efficacy in
man.
Pharmacokinetics: The extent of percutaneous absorption of topical
corticosteroids is determined by many factors including the vehicle, the
integrity of the epidermal barrier, and the use of occlusive dressings. A
significantly greater amount of fluocinonide is absorbed from the solution than
from the cream or gel formulations.
Topical corticosteroids can be absorbed from normal intact skin. Inflammation
and/or other disease processes in the skin increase percutaneous absorption.
Occlusive dressings substantially increase the percutaneous absorption of
topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic
adjunct for treatment of resistant dermatoses. (See DOSAGE AND ADMINISTRATION).
Once absorbed through the skin, topical corticosteroids are handled through
pharmacokinetic pathways similar to systemically administered corticosteroids.
Corticosteroids are bound to plasma proteins in varying degrees. Corticosteroids
are metabolized primarily in the liver and are then excreted by the kidneys.
Some of the topical corticosteroids and their metabolites are also excreted into
the bile.
INDICATIONS AND USAGE:
These products are indicated for the relief of the inflammatory and pruritic
manifestations of corticosteroid-responsive dermatoses.
CONTRAINDICATIONS:
Topical corticosteroids are contraindicated in those patients with a history of
hypersensitivity to any of the components of the preparation.
PRECAUTIONS:
GENERAL: Systemic absorption of topical corticosteroids has produced reversible
hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of
Cushing's syndrome, hyperglycemia, and glucosuria in some patients. Conditions
which augment systemic absorption include the application of the more potent
steroids, use over large surface areas, prolonged use and the addition of
occlusive dressings.
Therefore, patients receiving a large dose of a potent topical steroid applied
to a large surface area or under an occlusive dressing should be evaluated
periodically for evidence of HPA axis suppression by using the urinary free
cortisol and ACTH stimulation tests. 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 steroid.
Recovery of HPA axis function is generally prompt and complete upon
discontinuation of the drug. Infrequently, signs and symptoms of steroid
withdrawal may occur, requiring supplemental systemic corticosteroids.
Pediatric patients may absorb proportionally larger amounts of topical
corticosteroids and thus be more susceptible to systemic toxicity. (See
PRECAUTIONS--Pediatric Use).
Not for ophthalmic use. Severe irritation is possible if fluocinonide solution
contacts the eye. If that should occur, immediate flushing of the eye with a
large volume of water is recommended.
If irritation develops, topical corticosteroids should be discontinued and
appropriate therapy instituted.
As with any topical corticosteroid product, prolonged use may produce atrophy of
the skin and subcutaneous tissues. When used on intertriginous or flexor areas,
or on the face, this may occur even with short-term use.
In the presence of dermatological infections, the use of an appropriate
antifungal or antibacterial agent should be instituted. If a favorable response
does not occur promptly, the corticosteroid should be discontinued until the
infection has been adequately controlled.
INFORMATION FOR THE PATIENT: Patients using topical corticosteroids should
receive the following information and instructions:
1. This medication is to be used as directed by the physician. It is for
external use only. Avoid contact with the eyes. If there is contact with the
eyes and severe irritation occurs, immediately flush with a large volume of
water.
2. Patients should be advised not to use this medication for any disorder other
than for which it was prescribed.
3. The treated skin area should not be bandaged or otherwise covered or wrapped
as to be occlusive unless directed by the physician.
4. Patients should report any signs of local adverse reactions especially under
occlusive dressing.
5. Parents of pediatric patients should be advised not to use tight-fitting
diapers or plastic pants on a child being treated in the diaper area, as these
garments may constitute occlusive dressings.
LABORATORY TESTS: The following tests may be helpful in evaluating HPA axis
suppression: Urinary free cortisol test and ACTH stimulation test.
CARCINOGENESIS, MUTAGENESIS, AND IMPAIRMENT OF FERTILITY: Long-term animal
studies have not been performed to evaluate the carcinogenic potential or the
effect on fertility of topical corticosteroids.
Studies to determine mutagenicity with prednisolone and hydrocortisone have
revealed negative results.
PREGNANCY CATEGORY C: 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.
NURSING MOTHERS: 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 USE: PEDIATRIC PATIENTS MAY DEMONSTRATE GREATER SUSCEPTIBILITY TO
TOPICAL CORTICOSTEROID-INDUCED HPA AXIS SUPPRESSION AND CUSHING'S SYNDROME THAN
MATURE PATIENTS BECAUSE OF A LARGER SKIN SURFACE AREA TO BODY WEIGHT RATIO.
Parents of pediatric patients should be advised not to use tight-fitting diapers
or plastic pants on a child being treated in the diaper area as these garments
may constitute occlusive dressings.
Hypothalamic-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.
ADVERSE REACTIONS:
The following local adverse reactions are reported infrequently with topical
corticosteroids, but may occur more frequently with the use of occlusive
dressings. These reactions are listed in an approximate decreasing order of
occurrence: burning, itching, irritation, dryness, folliculitis, hypertrichosis,
acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact
dermatitis, maceration of the skin, secondary infection, skin atrophy, striae,
miliaria.
OVERDOSAGE:
Topically applied corticosteroids can be absorbed in sufficient amounts to
produce systemic effects (See PRECAUTIONS).
DOSAGE AND ADMINISTRATION:
Topical corticosteroids are 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 dressings may be used for the management of psoriasis or recalcitrant
conditions. Some plastic films may be flammable and due care should be exercised
in their use. Similarly, caution should be employed when such films are used on
children or left in their proximity, to avoid the possibility of accidental
suffocation.
If an infection develops, the use of occlusive dressings should be discontinued
and appropriate antimicrobial therapy instituted.
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