LOCASALEN®
Novartis
Flumethasone Pivalate – Salicylic Acid
Topical Corticosteroid – Squamolytic
Action And Clinical Pharmacology: Locasalen exhibits pronounced anti-inflammatory, anti-allergic antiproliferative and antipruritic effects. Flumethasone pivalate, a topical corticoid of proven efficacy, is in solution in the ointment base rather than as suspended microcrystals and attains a higher degree of penetration into the skin where it remains active in the epidermis for a long period of time.
The salicylic acid component facilitates transepidermal penetration and also contributes therapeutic properties which are beneficial in respect of the indications of Locasalen. In a lipophilic base of this type salicylic acid 3% is squamolytic and mildly keratolytic, softening the horny layer of normal and hyperkeratotic skin and enhancing penetration. It also displays a significant antiseptic effect against bacteria and fungi. Even though no pH can be determined in this type of vehicle an acidogenic effect is exerted on contact with aqueous media (surface of the skin), to reinforce or restore the physiological acidity of the epidermal hydrolipidic mantle. The epidermoplastic effect promotes normalization of pathological cornification processes.
Lipophilic in character, the fatty ointment base spreads easily and readily penetrates (facilitating release of flumethasone pivalate), leaving a thin oily film on the skin, rendering it hydrophobic. The ointment can passively absorb a certain volume of water at and below body temperature while the outer layer of ointment remains hydrophobic. Evaporation does not take place and by virtue of this occlusive effect Locasalen will block insensible perspiration, slight sensible perspiration and the loss of heat to the atmosphere, thereby exerting a lubricating and emollient action, and also rehydration of the skin. The ointment adheres well to dry skin but for cosmetic reasons, can be rubbed into the skin with remaining traces removable by dabbing the area with a dry tissue. Locasalen is easily removed with soap and water or a skin cleansing agent. The ointment does not stain clothes or bed linen.
Indications And Clinical Uses: The treatment of subacute to hyperchronic, inflammatory and/or dysplastic skin diseases, as well as hyperkeratotic conditions in particular. Its indications thus include: chronic constitutional eczema or neurodermatitis; and chronic exogenous eczema irrespective of origin (e.g. skin disorders due to attrition), occupational eczema, chronic eczema of microbial or mycotic origin, tylotic eczema, hyperkeratosis as encountered in ichthyosis or chronic dyshidrosis, pustulosis of the palms and soles, lichen planus and chronic cutaneous lupus erythematosus and psoriasis.
Contra-Indications: Tuberculosis of the skin, syphilitic skin infections, viral and acute fungal infections of the skin, rosacea, perioral dermatitis, acne vulgaris. Systemic fungal infections. This preparation is not for ophthalmic use. Locasalen is contraindicated in individuals with a history of hypersensitivity to its components, to corticosteroids in general or to other salicylates.
Corticosteroids are also contraindicated in untreated bacterial infection.
Manufacturers’ Warnings In Clinical States: Locasalen is not indicated in acute weeping or subacute exudative stages.
In children and patients with marked renal insufficiency, repeated applications to extensive areas of skin should be avoided because transcutaneous absorption of the salicylic acid component might possibly give rise to systemic effects.
Likewise corticosteroids are known to be absorbed percutaneously. Since a moderate decrease in adrenocortical function has been reported, the risk of systemic side effects should be borne in mind. In patients requiring applications of Locasalen to extensive areas and/or under occlusive dressings, adrenal function should be carefully monitored.
All contact of the drug with the eyes, mouth and mucous membranes should be avoided.
Pregnancy: Animal experiments relevant to the safety assessment of corticosteroids, although not specifically conducted with Locasalen, have shown either teratogenic potential or other adverse effects on the embryo and/or fetus. However, no reports on adverse effects with Locasalen in human pregnancy have been received to date.
When using Locasalen in pregnancy, the risk-benefit relationship must be carefully considered and the therapy should be clearly indicated. However, the use of Locasalen in large amounts, on large areas of skin (especially under occlusive dressings), or for prolonged periods of time should be avoided during pregnancy.
Lactation: It is not known whether the active substances of Locasalen and/or their metabolite(s) pass into the breast milk when the preparation is applied topically. For safety reasons, nursing mothers should not use the product.
Precautions: If sensitivity or idiosyncratic reactions occur Locasalen should be discontinued and appropriate measures taken.
Patients should be advised to inform subsequent physicians of the prior use of corticosteroids.
In the presence of an infection, the use of an appropriate antifungal or antibacterial agent should be instituted. If a favorable response does not occur promptly, Locasalen should be discontinued until the infection has been adequately controlled. During the use of topical corticosteroids secondary infections may occur.
Application under occlusive dressings should be of limited duration and confined to small areas of diseased skin. Occlusive dressing should not be applied if there is an elevation of temperature.
In infants and small children, whose skin is more sensitive, Locasalen should be used with caution.
Prolonged use of topical corticosteroid products may produce atrophy of the skin and of subcutaneous tissues, particularly on flexor surfaces and on the face. Therefore, long-term treatment, especially of the facial skin, should always be avoided. The use of Locasalen should be discontinued if the above reactions are noted.
In exceptional cases where Locasalen is applied in large amounts, to large areas of skin, or under occlusive dressings, this should only be done if the patient is kept under close medical supervision.
The product should be used with caution in patients with stasis dermatitis and other skin diseases associated with impaired circulation.
Locasalen should not be allowed to come into contact with the conjunctiva.
Adverse Reactions: The local tolerability of Locasalen proved to be very good. Cases in which local irritation made it advisable to discontinue the medication accounted for less than 2% of the total number of patients treated. Adverse reactions consist mainly of local reddening of the skin, desquamation, pruritus and smarting.
In isolated cases, mild skin atrophy due to flumethasone pivalate has also been observed.
Locasalen contains no preservatives, odor correcting agents, emulsifiers, stabilizers or antibiotic supplement which have been recognized as potential sensitizers. Hypersensitivity to salicylic acid can occur; however, the incidence in the population as a whole is approximately 0.2%.
Treatment should be discontinued if severe irritation or sensitization develops.
Systemic side effects attributable to the transcutaneous absorption of salicylic acid have not been reported. Absorption of salicylic acid does occur; however, investigations have shown that irrespective of the amount of Locasalen employed, and even applied under occlusive dressings, plasma concentrations of salicylic acid did not exceed ordinary therapeutic levels as a result of transcutaneous absorption. The risk of systemic side effects however should be borne in mind, particularly when using the preparation in pediatrics. Investigations have shown that under extreme conditions – where 40 to 60 g of ointment were applied daily to 89 to 90% of the body surface under occlusive dressings – plasma cortisol and urinary steroids have been observed to decrease below normal levels. This decrease proved transitory and was not accompanied by any clinical symptoms. Isolated cases of Cushing’s syndrome have been reported.
When occlusive dressings are used, pustules, miliaria, folliculitis and pyoderma may occur. The following local adverse skin reactions have been reported with the use of topical steroids: dryness, itching, burning, local irritation, acneiform eruptions, skin atrophy, atrophy of s.c. tissues, hypertrichosis, folliculitis, change in pigmentation, secondary infection and contact allergy. Adrenal suppression has also been reported following topical corticosteroid therapy. Posterior subcapsular cataracts have been reported following systemic use of corticosteroids.
Topical corticosteroids may also give rise to striae rubrae distensae, telangiectasia, purpura or steroid acne, particularly if applied for prolonged periods of time, to large areas, under occlusive dressings, or to areas of increased skin permeability, such as the face of axillae.
Symptoms And Treatment Of Overdose: Symptoms and Treatment: Poisoning due to accidental ingestion is not anticipated. No specific antidote exists hence treatment of overdosage is symptomatic.
Dosage: As a rule Locasalen should be applied once or twice daily when dressings are not used and once daily when employed under occlusive dressing. It is not usually necessary to cover the treated area. The thickness of the layer should vary depending on the nature and severity of the skin disorder, since in this way it is possible to regulate moisture retention. In cases in which transitory exudation must be anticipated, Locasalen should be applied in a very thin layer, thereby allowing larger quantities of moisture to be released through the film of ointment. Locasalen can also exert an occlusive effect but only if applied in a thick layer. It penetrates well into the skin and, when rubbed in thoroughly, leaves on the skin a transparent oily film, that can be removed with soap and water or a skin cleanser. Excess film can be removed relatively well with paper tissues, leaving scarcely any perceptible sheen.
Availability And Storage: Each g of ointment, colorless, soft to moderately firm in consistency with a smooth, homogeneous surface appearance contains: flumethasone pivalate 0.02% and salicylic acid 3%. Nonmedicinal ingredients: lanolin, propylene glycol and white petrolatum. Tartrazine-free. Tubes of 15 and 50 g.
LOCASALEN® Novartis Flumethasone Pivalate – Salicylic Acid Topical Corticosteroid – Squamolytic
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