HALOBETASOL PROPIONATE- halobetasol propionate ointment
Padagis Israel Pharmaceuticals Ltd
For Dermatologic Use Only. Not for Ophthalmic Use.
Halobetasol propionate ointment, 0.05% contains halobetasol propionate, a synthetic corticosteroid for topical dermatological use. The corticosteroids constitute a class of primarily synthetic steroids used topically as an anti-inflammatory and antipruritic agent.
Chemically halobetasol propionate is 21-chloro-6α, 9-difluoro-11β, 17-dihydroxy-16β-methylpregna-1, 4-diene-3-20-dione, 17-propionate, C25 H31 ClF2 O5 . It has the following structural formula:
Halobetasol propionate has the molecular weight of 485. It is a white crystalline powder insoluble in water.
Each gram of halobetasol propionate ointment, 0.05% contains 0.5 mg of halobetasol propionate in a base of aluminum stearate, beeswax, pentaerythritol cocoate, stearyl citrate, petrolatum, propylene glycol and sorbitan sesquioleate.
Like other topical corticosteroids, halobetasol propionate has anti-inflammatory, antipruritic and vasoconstrictive actions.
The mechanism of the anti-inflammatory activity of the topical corticosteroids, 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 .
The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle and the integrity of the epidermal barrier. Occlusive dressings with hydrocortisone for up to 24 hours have not been demonstrated to increase penetration; however, occlusion of hydrocortisone for 96 hours markedly enhances penetration. Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin may increase percutaneous absorption.
Human and animal studies indicate that less than 6% of the applied dose of halobetasol propionate enters the circulation within 96 hours following topical administration of the ointment.
Studies performed with halobetasol propionate ointment, 0.05% indicate that it is in the super-high range of potency as compared with other topical corticosteroids.
Halobetasol propionate ointment, 0.05% is a super-high potency corticosteroid indictated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Treatment beyond two consecutive weeks is not recommended, and the total dosage should not exceed 50 g/week because of the potential for the drug to suppress the hypothalamic-pituitary-adrenal (HPA) axis.
Halobetasol propionate ointment, 0.05% is contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.
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 applying a topical steroid to a large surface area or to areas 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 super potent 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.
Halobetasol propionate ointment, 0.05% produced HPA axis suppression when used in divided doses at 7 grams per day for one week in patients with psoriasis. These effects were reversible upon discontinuation of treatment.
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 upon discontinuation of topical corticosteroids. Infrequently, signs and symptoms of glucocorticosteroid insufficiency may occur requiring supplemental systemic corticosteroids. For information on systemic supplementation, see prescribing information for those products.
If irritation develops, halobetasol propionate ointment, 0.05% 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 testing.
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 halobetasol propionate ointment, 0.05% should be discontinued until the infection has been adequately controlled.
Halobetasol propionate ointment, 0.05% should not be used in the treatment of rosacea or perioral dermatitis, and it should not be used on the face, groin, or in the axillae.
Patients using topical corticosteroids should receive the following information and instructions:
- The medication is to be used as directed by the physician. It is for external use only. Avoid contact with the eyes.
- The medication should not be used for any disorder other than that for which it was prescribed.
- The treated skin 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 reactions.
- Parents of pediatric patients should be advised not to use tight-fitting diapers or plastic pants on a child being treated in the diaper area, as these garments may constitute occlusive dressing.
The following tests may be helpful in evaluating patients for HPA axis suppression: ACTH-stimulation test; A.M. plasma-cortisol test; Urinary free-cortisol test.
Long-term animal studies have not been performed to evaluate the carcinogenic potential of halobetasol propionate.
Positive mutagenicity effects were observed in two genotoxicity assays. Halobetasol propionate was positive in a Chinese hamster micronucleus test, and in a mouse lymphoma gene mutation assay in vitro.
Studies in the rat following oral administration at dose levels up to 50 µg/kg/day indicated no impairment of fertility or general reproductive performance.
In other genotoxicity testing, halobetasol propionate was not found to be genotoxic in the Ames/Salmonella assay, in the sister chromatid exchange test in somatic cells of the Chinese hamster, in chromosome aberration studies of germinal and somatic cells of rodents, and in a mammalian spot test to determine point mutations.
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