Capex 0.010 %

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. Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.

Once absorbed through the skin, topical corticosteroids are handled through the same metabolic and elimination pathways as after systemic administration.

Additional Information: Local Treatment—Topical Application: Topical efficacy depends on the inherent glucocorticoid activity (or potency) of the steroid, the concentration in the preparation, permeability coefficient, the vehicle and excipients and local metabolic processes. Except for serious conditions, low-potency glucocorticoids are preferred by many authorities because adverse effects on the skin appear to be less severe than with high potency agents, even if the latter are used at appropriately lower concentrations. Only hydrocortisone and its acetate are available for nonprescription topical use.

Drugs with a high lipid-water distribution coefficient penetrate well from absorbable or non-oleaginous vehicles and tend to remain longer in the skin than water-soluble agents, exerting a more extended local action but lesser systemic side effects, especially if the drug is metabolized rapidly systemically. However, it is desirable that the agents be metabolized in the skin so that less is delivered to the systemic circulation.

Steroids that have the 17-OH group substituted and/or which are fluorinated are metabolized poorly locally and hence may have a significant potential for systemic effects; for this reason, special caution is urged when such compounds are used in children.

Occlusive dressings may be used, especially for low-potency, poorly penetrant steroids. The stratum corneum under the dressing becomes macerated and more permeable. However, such dressings increase absorption into the bloodstream and hence favor systemic effects.

Anti-inflammatory Properties: Cortisol and the synthetic analogs of cortisol have the capacity to prevent or suppress the development of the local heat, redness, swelling, and tenderness by which inflammation is recognized. At the microscopic level, they inhibit not only the early phenomena of the inflammatory process (edema, fibrin deposition, capillary dilation, migration of leukocytes into the inflamed area, and phagocytic activity) but also the later manifestations (capillary proliferation, fibroblast proliferation, deposition of collagen, and, still later, cicatrization).

Although understanding of these effects is unsatisfactory, many observations have been made that have therapeutic relevance and that must be taken into account in explanatory formulations. Perhaps the most important of these for the physician is that corticosteroids inhibit the inflammatory response whether the inciting agent is radiant, mechanical, chemical, infectious, or immunological. In clinical terms, the administration of corticosteroids for their anti-inflammatory effects is palliative therapy; the underlying cause of the disease remains; the inflammatory manifestations are merely suppressed.

It is this suppression of inflammation and its consequences that has made the corticosteroids such valuable therapeutic agents-indeed, at times lifesaving. It is also this property that gives them a nearly unique potential for therapeutic disaster. The signs and symptoms of inflammation are expressions of the disease process that are often used by the physician in diagnosis and in evaluating the effectiveness of treatment. These may be missing in patients treated with corticosteroids.

Anti-inflammatory effects depend upon the direct local action of the steroids. Topical or systemic glucocorticoids often markedly improve certain skin diseases, such as pruritus, psoriasis, dermatitis herpetiformis and eczema; pemphigus; erythema multiforme, exfoliative dermatitis and mycosis fungoides usually require systemic treatment, which may be life-saving.

Like other topical corticosteroids, fluocinolone acetonide has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids in general is unclear. Various laboratory methods, including skin blanching assays, are used to compare and predict potencies and/or clinical efficacies of the topical corticosteroids. There is evidence of recognizable correlation between vasoconstrictor potency and therapeutic efficacy in man. Generally, fluocinolone acetonide is considered to be in the low range of corticosteroid potency.

No studies have been done on fluocinolone shampoo to show any drug interaction. Generally, there are known drug interactions caused by glucocorticoids, not necessarily from topical application.

Glucocorticoids decrease the hypoglycemic activity of insulin and oral hypoglycemics, so that a change in dose of the antidiabetic drugs may be necessitated. The usual doses of mineralocorticoids and large doses of some glucocorticoids cause hypokalemia and may exaggerate the hypokalemic effects of thiazides and high-cleaning diuretics.

In combination with amphotericin-B, they also may cause hypokalemia. Glucocorticoids appear to enhance the ulcerogenic effects of NSAIDs. They decrease the plasma levels of salicylates, and salicylism may occur on discontinuing steroids. Glucocorticoids may increase or decrease the effects of prothrombopenic anticoagulants. Estrogens, phenobarbital, phenytoin and rifampin increase the metabolic clearance of adrenal steroids and hence necessitate dose adjustments.

The following tests may be helpful in evaluating patients for HPA axis suppression: ACTH stimulation test, A.M. plasma cortisol test, and urinary free cortisol test.

Long-term animal studies have not been performed to evaluate the carcinogenic potential or the effect on fertility of fluocinolone shampoo.

Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk. Because many drugs are excreted in human milk, caution should be exercised when fluocinolone shampoo is administered to a nursing woman.

Safety and effectiveness in children and infants have not been established. Because of a higher ratio of skin surface area to body mass, children are at a greater risk than adults of HPA-axis-suppression when they are treated with topical corticosteroids. They are therefore also at greater risk of glucocorticosteroid insufficiency after withdrawal of treatment, and of Cushing's syndrome while on treatment. Adverse effects including striae have been reported with inappropriate use of topical corticosteroids in infants and children.

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 fontanelle, headaches, and bilateral papilledema.

Systemic absorption of topical corticosteroids can produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression with the potential for glucocorticosteroid insufficiency after withdrawal of treatment. Manifestations of Cushing's syndrome, hyperglycemia, and glucosuria can also be produced in some patients by systemic absorption of topical corticosteroids while on treatment.

Patients receiving a large dose of a higher potency topical steroid applied to a large surface area or under occlusion should be evaluated periodically for evidence of HPA axis suppression. This may be done by using the ACTH stimulation, A.M. plasma cortisol, and urinary free cortisol tests.

Patients receiving superpotent corticosteroids should not be treated for more than 2 weeks at a time, and only small areas should be treated at any one time due to the increased risk of HPA suppression.

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 corticosteroid. Recovery of HPA axis function is generally prompt and complete upon discontinuation of topical corticosteroids. Infrequently, signs and symptoms of glucocorticosteroid insufficiency may occur requiring supplemental systemic corticosteroids.

Children may be more susceptible to systemic toxicity from equivalent doses due to their larger skin surface to body mass ratios.

If irritation develops, fluocinolone shampoo should be discontinued and appropriate therapy instituted. Allergic contact dermatitis with corticosteroids is usually diagnosed by observing failure to heal rather than noting a clinical exacerbation as with most topical products not containing corticosteroids. Such an observation should be corroborated with appropriate diagnostic patch test.

If concomitant skin infections are present or develop, an appropriate antifungal or antibacterial agent should be used. If a favorable response does not occur promptly, use of fluocinolone shampoo should be discontinued until the infection has been adequately controlled.

Teratogenic Effects: Pregnancy Category C: Corticosteroids have been shown to be teratogenic in laboratory animals when administered systemically at relatively low dosage levels. Some corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. No studies have been done on fluocinolone shampoo to show teratologic effects on animals.

Patients using topical corticosteroids should receive the following information and instructions: This medication is to be used as directed by the physician. It is for external use only. Avoid contact with the eyes. In case of contact, wash eyes liberally with water.

This medication should not be used for any disorder other than that for which it was prescribed.

The treated area should not be bandaged or otherwise covered or wrapped so as to be occlusive unless directed by the physician.

Patients should report to their physician any signs of local adverse reaction.

Fluocinolone shampoo mixture is to be discarded after 3 months.