HYDROCORTISONE 21-ACETATE
DESCRIPTION:
WYCORT CREAM: Contains Hydrocortisone Acetate 1% or 2.5% and Pramoxine
HCl 1% in a hydrophillic cream base containing stearic acid, cetyl alcohol,
aquaphor, isopropylpalmitate, polyoxyl-40 stearate, propylene glycol, potassium
sorbate, sorbic acid, triethanolamine lauryl sulfate and water.
structural formula, the chemical name, molecular formula and molecular weight
for active ingredients are presented below.
Hydrocortisone acetate
(Pregn-4-ene-3,20-dione,21 - (acetyloxy)-11, 17-dihydroxy-,(11 beta)-.)
C23H32O6; mol wt: 404.50
ACTIONS/CLINICAL PHARMACOLOGY:
Topical corticosteroids share anti-inflammatory, anti-pruritic and
vasoconstrictive actions.
The mechanism of anti-inflammatory activity of the topical corticosteroids is
unclear. Various laboratory methods, including vasoconstrictor assays, are used
to compare and predict potencies and/or clinical efficacies of the topical
corticosteroids. There is some evidence to suggest that a recognizable
correlation exists between vasoconstrictor potency and therapeutic efficacy in
man.
Pramoxine hydrochloride is a topical anesthetic agent which provides temporary
relief from itching and pain. It acts by stabilizing the neuronal membrane of
nerve endings with which it comes into contact.
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 dressings.
Topical corticosteroids can be absorbed from normal intact skin. Inflammation
and/or other disease processes in the skin increase percutaneous absorption.
Occlusive dressings substantially increase the percutaneous absorption of
topical corticosteroids. Thus, occlusive dressings may be a valuable therapeutic
adjunct for treatment of resistant dermatoses (See DOSAGE AND ADMINISTRATION).
Once absorbed through the skin, topical corticosteroids are handled through
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 and their metabolites are also excreted into
the bile.
INDICATIONS AND USAGE:
Topical corticosteroids are indicated for the relief of the inflammatory and
pruritic manifestations of corticosteroid-responsive dermatoses of the anal
region.
CONTRAINDICATIONS:
Topical corticosteroids are contraindicated in those patients with a history of
hypersensitivity to any of the components of the preparation.
PRECAUTIONS:
GENERAL: Systemic absorption of topical corticosteroids has produced reversible
hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of
Cushing's syndrome, hyperglycemia, and glucosuria in some patients.
Conditions which augment systemic absorption include the application of the more
potent steroids, use over large surface areas, prolonged use, and the addition
of occlusive dressings.
Therefore, patients receiving a large dose of a potent topical steroid applied
to a large surface area and under an occlusive dressing should be evaluated
periodically for evidence of HPA axis suppression by using the urinary free
cortisol and ACTH stimulation tests. 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 steroid.
Recovery of HPA axis function is generally prompt and complete upon
discontinuation of the drug. Infrequently, signs and symptoms of steroid
withdrawal may occur, requiring supplemental systemic corticosteroids.
Children may absorb proportionally larger amounts of topical corticosteroids and
thus be more susceptible to systemic toxicity. (See PRECAUTIONS--Pediatric Use).
If irritation develops, topical corticosteroids should be discontinued and
appropriate therapy instituted.
In the presence of dermatological infections, the use of an appropriate
antifungal or antibacterial agent should be instituted. If a favorable response
does not occur promptly, the corticosteroid should be discontinued until the
infection has been adequately controlled.
INFORMATION FOR THE PATIENT: Patients using topical corticosteroids should
receive the following information and instructions:
1. This medication is to be used as directed by the physician. It is for
external use only. Avoid contact with the eyes.
2. Patients should be advised not to use this medication for any disorder other
than for which it was prescribed.
3. The treated skin area should not be bandaged or otherwise covered or wrapped
as to be occlusive unless directed by the physician.
4. Patients should report any signs of local adverse reactions especially under
occlusive dressing.
5. Parents of pediatric patients should be advised not to use tightfitting
diapers or plastic pants on a child being treated in the diaper area, as these
garments may constitute occlusive dressings.
LABORATORY TESTS: The following tests may be helpful in evaluating the HPA axis
suppression:
Urinary free cortisol test
ACTH stimulation test
CARCINOGENESIS, MUTAGENESIS, AND IMPAIRMENT OF FERTILITY: Long-term animal
studies have not been performed to evaluate the carcinogenic potential or the
effect on fertility of topical corticosteroids.
Studies to determine mutagenicity with prednisolone and hydrocortisone have
revealed negative results.
PREGNANCY CATEGORY C: Corticosteroids are generally teratogenic in laboratory
animals when administered systemically at relatively low dosage levels. The more
potent corticosteroids have been shown to be teratogenic after dermal
application in laboratory animals. There are no adequate and well-controlled
studies in pregnant women on teratogenic effects from topically applied
corticosteroids. Therefore, topical corticosteroids should be used during
pregnancy only if the potential benefit justifies the potential risk to the
fetus. Drugs of this class should not be used extensively on pregnant patients,
in large amounts, or for prolonged periods of time.
NURSING MOTHERS: It is not known whether topical administration of
corticosteroids could result in sufficient systemic absorption to produce
detectable amounts in breast milk. Systemically administered corticosteroids are
secreted into breast milk in quantities NOT likely to have a deleterious effect
on the infant. Nevertheless, caution should be exercised when topical
corticosteroids are administered to a nursing woman.
PEDIATRIC USE: PEDIATRIC PATIENTS MAY DEMONSTRATE GREATER SUSCEPTIBILITY TO
TOPICAL CORTICOSTEROID-INDUCED HPA AXIS SUPPRESSION AND CUSHING'S SYNDROME THAN
MATURE PATIENTS BECAUSE OF A LARGER SKIN SURFACE AREA TO BODY WEIGHT RATIO.
Hypothalamic-pituitary-adrenal (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 fontanelles, headaches, and bilateral papilledema.
Administration of topical corticosteroids to children should be limited to the
least amount compatible with an effective therapeutic regimen. Chronic
corticosteroid therapy may interfere with the growth and development of
children.
ADVERSE REACTIONS:
The following local adverse reactions are reported infrequently with topical
corticosteroids, but may occur more frequently with the use of occlusive
dressings. These reactions are listed in an approximate decreasing order of
occurrence:
Burning Hypopigmentation
Itching Perioral dermatitis
Irritation Allergic contact dermatitis
Dryness Maceration of the skin
Folliculitis Secondary infection
Hypertrichosis Skin Atrophy
Acneiform eruptions Striae
Miliaria
OVERDOSAGE:
Topically applied corticosteroids can be absorbed in sufficient amounts to
produce systemic effects (See PRECAUTIONS).
DOSAGE AND ADMINISTRATION:
Topical corticosteroids are generally applied to the affected area as a thin
film three or four times daily depending on the severity of the condition.
Occlusive dressings may be used for the management of psoriasis or recalcitrant
conditions. If an infection develops, the use of occlusive dressings should be
discontinued and appropriate antimicrobial therapy instituted.
For cleansing of anogenital area, spread Analpram HC(R) Lotion 2.5% on cotton or
tissue and wipe affected area.
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