Clobenate

Clobenate

clobetasol

Manufacturer:

Micro Labs

Distributor:

UNILAB, Inc

Marketer:

Westmont
Full Prescribing Info
Contents
Clobetasol propionate.
Action
Pharmacologic Classification: Steroidal anti-inflammatory/Antipruritic.
Pharmacology: Pharmacodynamics: Mechanism of Action: Clobetasol proprionate is a highly potent topical corticosteroid. Like other topical corticosteroids, clobetasol propionate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
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 dressing. Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin and occlusive dressings may increase percutaneous absorption.
Mean peak plasma clobetasol propionate concentrations of 0.63 ng/ml occurred in one study eight hours after the second application (13 hours after an initial application) of 30 g clobetasol propionate 0.05% ointment to normal individuals with healthy skin. Following the application of a second dose of 30 g clobetasol propionate cream 0.05%, mean peak plasma concentrations were slightly higher than the ointment and occurred 10 hours after application.
In a separate study, mean peak plasma concentrations of approximately 2.3 ng/ml and 4.6 ng/ml occurred respectively in patients with psoriasis and eczema three hours after a single application of 25 g clobetasol propionate 0.05% ointment.
Once absorbed through the skin, topical corticosteroids enter 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, including clobetasol and its metabolites, are also excreted in the bile.
Indications/Uses
Relief and short-term treatment of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses including: Psoriasis (e.g., moderate to severe plaque-type psoriasis); Eczematous dermatitis; Recalcitrant dermatoses; Lichen planus; Discoid lupus erythematosus; Other skin conditions which do not respond satisfactorily to less potent steroids.
Dosage/Direction for Use
For short-term use by adults only. Creams are especially used for moist or weeping surfaces.
General recommendations: This product should not be used on the face, groin, or axillae.
Do not use with occlusive dressings (including bandage or any cover or wrap).
As with other corticosteroids, therapy should be discontinued when control is achieved. If no improvement is seen within 2 weeks, reassessment of the diagnosis may be necessary.
Reduce the frequency of application or change the treatment to a less potent preparation as soon as clinically feasible.
Allow adequate time for absorption after each application before applying an emollient.
Wash hands after each application, unless the hands are being treated.
Total dose should not exceed 50 grams per week.
Recommended dose: Apply a thin layer of clobetasol cream and gently rub in using only enough to cover the entire affected area/s.
Frequency of application is 1 to 2 times a day (preferably in the morning and evening), according to the severity of the condition, until improvement occurs. In more responsive conditions, this may be within a few days.
Or, as prescribed by a physician.
Patients who frequently relapse (recalcitrant dermatoses): Once an acute episode has been treated effectively with a continuous course of topical corticosteroid, intermittent dosing (1 to 2 times a week, without occlusion) may be considered. This has been shown to be helpful in reducing the frequency of relapse.
Application should be continued to all previously affected sites or to known sites of potential relapse. This regimen should be combined with routine daily use of emollients. The condition and the benefits and risks of continued treatment must be re-evaluated on a regular basis.
Overdosage
Acute overdosage is very unlikely to occur. However, in the case of chronic overdosage or misuse, the features of hypercorticism may appear.
In the event of overdose, clobetasol should be withdrawn gradually by reducing the frequency of application or by substituting a less potent corticosteroid. Further management should be as clinically indicated or as recommended by health professionals.
Contraindications
Hypersensitivity to clobetasol proprionate or other ingredients in the product.
Children below 12 years old.
Treatment of the following conditions: Untreated cutaneous infections; Rosacea; Acne vulgaris; Pruritus without inflammation; Perioral dermatitis; Perianal and genital pruritus; Primary cutaneous viral infections (e.g., herpes simplex, chickenpox).
Special Precautions
FOR EXTERNAL USE ONLY. Avoid contact with the eyes.
Because of the potency of clobetasol proprionate and its potential for causing adverse systemic effects during topical therapy, the usual dosage should NOT be exceeded and occlusive dressings (including bandages) should NOT be applied to areas of clobetasol proprionate application (see Dosage & Administration).
Endocrine System Effects: Clobetasol proprionate is a highly potent topical corticosteroid that has been shown to suppress the HPA axis at doses as low as 2 g/day.
Systemic absorption of topical corticosteroids may cause manifestations of hypercortisolism (Cushing's syndrome) and reversible HPA axis suppression, leading to glucocorticosteroid insufficiency. If either of the previously mentioned are observed, withdraw the drug gradually by reducing the frequency of application, or by substituting a less potent corticosteroid. Abrupt withdrawal of treatment may result in glucocorticosteroid insufficiency.
Because of the potential systemic absorption, patients should be periodically evaluated for HPA axis suppression. Factors that predispose a patient using topical corticosteroid to HPA axis suppression include potency and formulation of topical steroid, application over large surface areas, duration of exposure, use under occlusion, increased hydration of the stratum corneum, use on thin skin areas (e.g., face), use on broken skin or other conditions with an altered skin barrier, and use in patients with liver failure. If HPA axis suppression occurs, the drug should either be gradually withdrawn, the frequency of application reduced, or replaced with a less potent steroid. Manifestations of adrenal insufficiency may require supplemental systemic corticosteroids. Recovery of HPA axis function is generally prompt and complete upon discontinuation of topical corticosteroids.
Cushing's syndrome, hyperglycemia, and unmasking of latent diabetes can also result from systemic absorption of topical corticosteroids. Pediatric patients may be more susceptible to systemic toxicity from topical corticosteroids.
Local Effects: Local adverse reactions may more likely occur with occlusive use, prolonged use or use of higher potency corticosteroids. Reactions include atrophy, striae, telangiectasias, burning, itching, irritation, dryness, folliculitis, acneiform eruption, hypopigmentation, hypertrichosis, perioral dermatitis, allergic contact dermatitis, secondary infection, and miliaria. Some local adverse reactions may be irreversible. Clobetasol proprionate is not recommended in patients with acne vulgaris, rosacea or perioral dermatitis (see Contraindications).
Hypersensitivity: Clobetasol should be used with caution in patients with a history of local hypersensitivity to other corticosteroids or any excipients of the product. Allergic contact dermatitis with corticosteroids is usually diagnosed by observing a failure to heal rather than noting a clinical exacerbation. Clinical diagnosis of allergic contact dermatitis can be confirmed with patch testing. Although hypersensitivity reactions are rare with topical steroids, clobetasol proprionate should be discontinued and appropriate therapy instituted.
Concomitant Skin Infections: In cases of bacterial infections of the skin, appropriate antifungal or antibacterial agents should be used as primary therapy. If it is considered necessary, the topical corticosteroid may be used as an adjunct to control inflammation, erythema and itching. Is a favorable response does not occur promptly, use of clobetasol proprionate should be discontinued until the infection has been adequately controlled.
Use in Psoriasis: Topical steroids may be hazardous in psoriasis due to rebound relapses, development of tolerance, risk of generalized pustular psoriasis and development of local or systemic toxicity due to impairment of the skin's barrier function. Careful patient supervision is important in these patients.
Renal and Hepatic Impairment: In case of systemic absorption (when application is over a large surface area for a prolonged period) metabolism and elimination may be delayed therefore increasing the risk of systemic toxicity. Therefore, the minimum quantity should be used for the shortest duration to achieve the desired clinical benefit.
Use in Children: Children (<12 years old): Care should be taken when using clobetasol proprionate to ensure the amount applied is the minimum that provides therapeutic benefit. Use of clobetasol proprionate is not recommended for children below 12 years old (see Contraindications).
Because of a higher ratio of skin surface area to body mass, pediatric patients are at a greater risk than adults of HPA axis suppression and Cushing's syndrome when they are treated with topical corticosteroids. They are therefore also at greater risk of glucocorticosteroid insufficiency during or after withdrawal of treatment. Adverse effects including striae have been reported with inappropriate use of topical corticosteroids in infants and children.
HPA axis suppression, Cushing's syndrome, linear growth retardation, delayed weight gain, and intracranial hypertension have been reported in children receiving topical corticosteroids. Manifestations of adrenal suppression in children include low plasma cortisol levels and absence of response to adrenocorticotropic hormone stimulation. Manifestations of intracranial hypertension include bulging fontanelles, headaches, and bilateral papilledema.
Use in Elderly: Elderly (≥65 years old): Clinical studies have not identified differences in responses between the elderly and younger patients. The greater frequency of decreased hepatic or renal function in the elderly may delay elimination if systemic absorption occurs. Therefore, the minimum quantity should be used for the shortest duration to achieve the desired clinical benefit.
Use In Pregnancy & Lactation
Pregnancy: Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Clobetasol proprionate should only be used in pregnancy if the potential benefit justifies the potential risk to the fetus. The minimum quantity should be used for the minimum duration.
Corticosteroids have been shown to be teratogenic in laboratory animals when administered systemically at relatively low doses. Some have also been shown to be teratogenic after dermal application to laboratory animals. Clobetasol proprionate has greater teratogenic potential than other less potent steroids.
Lactation: 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 clobetasol proprionate is administered to a breastfeeding woman.
If used during lactation, clobetasol should not be applied to the breasts to avoid accidental ingestion by the infant.
Adverse Reactions
The most common (5%) adverse effect with clobetasol proprionate is burning or stinging of the skin. As with other topical corticosteroids, prolonged use (i.e., >14 days) of large amounts (i.e., ≥2 g/day) of clobetasol or treatment of extensive areas can result in sufficient systemic absorption to produce the features of hypercorticism.
Less common adverse effects (<2% of patients) include: Immune System: Generalized rash, hypersensitivity.
Endocrine: HPA axis suppression, including Cushingoid features (e.g., moon face, central obesity), delayed weight gain/growth retardation in children, osteoporosis, glaucoma, hyperglycemia/glucosuria, cataract, hypertension, increased weight or obesity, decreased endogenous cortisol levels, alopecia, trichorrhexis.
Skin and Subcutaneous Tissue: Allergic contact dermatitis or dermatitis, cracking and fissuring of the skin, erythema, exacerbation of underlying symptoms, folliculitis, hypertrichosis, irritation, pigmentation changes, pruritus, pustular psoriasis, rash, skin atrophy, skin dryness, skin thinning, skin wrinkling, striae, telangiectasia, urticaria.
Others: Application site irritation/pain, dilatation of superficial blood vessels, numbness of the fingers, opportunistic infection, tenderness in the elbow.
Drug Interactions
Corticosteroids: Do not use other corticosteroid-containing products with clobetasol proprionate unless directed by a physician. Concomitant use may increase the total systemic corticosteroid exposure.
Drugs inhibiting cytochrome P3A4 (CYP3A4): These drugs (e.g., ritonavir and itraconazole) have been shown to inhibit the metabolism of corticosteroids leading to increased systemic exposure. Clinical relevance of this interaction depends on the dose and route of administration of the corticosteroids and the potency of the CYP3A4 inhibitor.
Tell the doctor if the patient is taking other medicines, including vitamins, supplements, and herbal medicines.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
D07AD01 - clobetasol ; Belongs to the class of very potent (group IV) corticosteroids. Used in the treatment of dermatological diseases.
Presentation/Packing
Topical cream (tube) 500 mcg/g (0.05% w/w) x 5 g, 15 g.
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