These preparations are all intended for topical administration.
LIDEX 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)]-, (6(alpha),11(beta), 16(alpha))-. It has the following chemical structure:
LIDEX Cream contains fluocinonide 0.5 mg/g in FAPG® 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.
LIDEX 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.
LIDEX 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.
LIDEX 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.
LIDEX-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)]-,(6(alpha),11(beta), 16(alpha))-. It has the following chemical structure:
SYNALAR Cream contains fluocinolone acetonide 0.25 mg/g in a water-washable aqueous base of butylated hydroxytoluene, cetyl alcohol, citric acid, edetate disodium, methylparaben and propylparaben (preservatives), mineral oil, polyoxyl 20 cetostearyl ether, propylene glycol, simethicone, stearyl alcohol, water (purified) and white wax.
SYNALAR Ointment contains fluocinolone acetonide 0.25 mg/g in a white petroleum USP vehicle.
SYNALAR Topical Solution contains fluocinolone acetonide 0.1 mg/mL in a water-washable base of citric acid and propylene glycol.
SYNEMOL Cream contains fluocinolone acetonide 0.25 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).
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.
: 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.
These products are indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Topical corticosteroids are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.
General: Systemic absorption of topical corticosteroids has produced reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of Cushing' 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.
Children may absorb proportionally larger amounts of topical corticosteroids and thus be more susceptible to systemic toxicity. (See PRECAUTIONS --Pediatric Use. ) These preparations are 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:
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 hypothalamic-pituitary-adrenal (HPA) axis suppression and Cushing' syndrome than mature patients because of a larger skin surface area to body weight ratio. HPA axis suppression, Cushing' 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.
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.
Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects. (See PRECAUTIONS .)
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.
LIDEX® (fluocinonide) Topical Solution 0.05% --Plastic squeeze bottles: 20cc (NDC 99207-517-44), 60cc (NDC 99207-517-46). Store at room temperature. Avoid excessive heat, above 40°C (104°F).
Manufactured by: West Pharmaceutical Services Lakewood, Inc.
Lakewood, NJ 08701
LIDEX® (fluocinonide) Cream 0.05% --15 g Tube (NDC 99207-511-13), 30 g Tube (NDC 99207-511-14), 60 g Tube (NDC 99207-511-17), 120 g Tube (NDC 99207-511-22). Store at room temperature. Avoid excessive heat, above 40°C (104°F).
LIDEX® (fluocinonide) Gel 0.05% --15 g Tube
(NDC 99207-507-13), 30 g Tube (NDC 99207-507-14), 60 g Tube (NDC 99207-507-17). Store at controlled room temperature:
LIDEX® (fluocinonide) Ointment 0.05% --15 g Tube
(NDC 99207-514-13), 30 g Tube (NDC 99207-514-14), 60 g Tube (NDC 99207-514-17), 120 g Tube (NDC 99207-514-22). Store at room temperature. Avoid temperature over 30°C (86°F).
LIDEX-E® (fluocinonide) Cream 0.05% --15 g Tube
(NDC 99207-513-13), 30 g Tube (NDC 99207-513-14), 60 g Tube (NDC 99207-513-17). Store at room temperature. Avoid excessive heat, above 40°C (104°F).
SYNALAR® (fluocinolone acetonide) Cream 0.025% --15 g Tube (NDC 99207-501-13), 60 g Tube (NDC 99207-501-17). Store at room temperature; avoid freezing and excessive heat, above 40°C (104°F).
SYNALAR® (fluocinolone acetonide) Topical Solution 0.01% --20cc (NDC 99207-506-44), 60cc
(NDC 99207-506-46). Store at room temperature. Avoid freezing.
SYNALAR® (fluocinolone acetonide) Ointment 0.025% --15 g Tube (NDC 99207-504-13), 60 g Tube
(NDC 99207-504-17). Store at room temperature, avoid freezing and excessive heat, above 40°C (104°F).
SYNEMOL® (fluocinolone acetonide) Cream 0.025% --60 g Tube (NDC 99207-509-17). Store at room temperature. Avoid excessive heat, above 40°C (104°F).
MEDICIS, The Dermatology Company®
Scottsdale, AZ 85258
by: Patheon, Inc.
CANADA L5N 7K9
U.S. Patent No. 4,017,615 for LIDEX Ointment.