Synalar (Fluocinolone)
Fluocinolone
Brand Name(s): Derma-Smoothe/FS®, Fluonid®, FS® Shampoo, Synalar®, Synemol®, Retisert™ | Capex™
Classification:
Dermatological Agents
» Topical Antiinflammatory Agents
» Corticosteroids
Hormones and Hormone Modifiers
» Adrenal Agents
» Corticosteroids
Ophthalmic Agents
» Ophthalmic Antiinflammatory Agents
» Corticosteroids
Description: Fluocinolone is a topical, synthetic fluorinated corticosteroid. Compared with other topical corticosteroids, fluocinolone is considered a low-to-medium potency agent. Low-potency topical corticosteroids have modest antiinflammatory properties and are usually effective in treating thin, acute, inflammatory skin conditions. Since the stratum corneum is thin on the face and intertriginous areas, low-potency topical corticosteroids are preferred. Low potency topical corticosteroids are also considered the safest for chronic use and are preferred in the elderly or pediatrics patients. Fluocinolone is available as a cream, ointment, topical solution, shampoo, topical oil. The topical oil is also available as an otic solution for the treatment of chronic eczematous external otitis. An intravitreal implant (Retisert™) for the treatment of chronic non-infectious uveitis was approved by the FDA in April 2005. Potency varies according to the vehicle used. This drug was approved by the FDA in 1961.
Mechanism of Action: Topical corticosteroids exhibit anti-inflammatory, antipruritic, and vasoconstrictive properties. At the cellular level, corticosteroids induce peptides called lipocortins. Lipocortins antagonize phospholipase A2, an enzyme which causes the breakdown of leukocyte lysosomal membranes to release arachidonic acid. This action decreases the subsequent formation and release of endogenous inflammatory mediators including prostaglandins, kinins, histamine, liposomal enzymes and the complement system. Early anti-inflammatory effects of topical corticosteroids include the inhibition of macrophage and leukocyte movement and activity in the inflamed area by reversing vascular dilation and permeability. Later inflammatory processes such as capillary production, collagen deposition, keloid (scar) formation also are inhibited by corticosteroids. With topical application to affected skin, these actions correspond to decreased edema, erythema, pruritus, plaque formation, and scaling. With topical ophthalmic application, these actions correspond to decreased edema, capillary dilatation, migration of leukocytes, fibrin and collagen deposition, and scar formation associated with inflammation; it may also reduce capillary and fibroblast proliferation. Ocular application of corticosteroids also results in potentiation of epinephrine vasoconstriction, decreased macrophage movement, and stabilization of lysosomal membranes. Corticosteroids are able to increase intraocular pressures, the degree of which is related to the relative potency of the agent employed, as well as the concentration of the agent and the release from the pharmaceutical vehicle. Decreases in vascularization and scarring make these agents useful in limiting tissue damage in chemical and thermal exposures.
Derma Smoothe FS Topical Oil (Oil 0.01 %) 
Pharmacokinetics: Fluocinolone is applied topically as a cream, ointment, solution, shampoo or topical oil and can be for ophthalmic use as an intravitreal implant. 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. 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.
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.
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[ Revised 11/21/2005 11:39:00 AM ]
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