Locoid Lipocream®(hydrocortisone butyrate 0.1%)Cream

locoid lipocream (Hydrocortisone Butyratecream 
[Ferndale Laboratories]

For Dermatological Use Only

DESCRIPTION

Locoid Lipocream® Cream contains the topical corticosteroid hydrocortisone butyrate, a hydrocortisone ester.

It has the chemical name: (11ß)-11,21-dihydroxy-17-[(1-oxobutyl)oxy]-pregn-4-ene-3,20-dione;

the molecular formula: C25H36O6;

the molecular weight: 432.54;

and the CAS registry number: 13609-67-1.

The structural formula is:

Image from Drug Label Content

Each gram of Locoid Lipocream® Cream contains 1 mg of hydrocortisone butyrate in a hydrophilic base consisting of cetostearyl alcohol, ceteth-20, mineral oil, white petrolatum, citric acid, sodium citrate, propylparaben and butylparaben (preservatives) and purified water.

CLINICAL PHARMACOLOGY

Topical corticosteroids share anti-inflammatory, anti-pruritic and vasoconstrictive actions.

The mechanism of anti-inflammatory activity of topical corticosteroids is unclear. Various laboratory methods, including vasoconstrictor assays, are used to compare and predict potencies and/or clinical efficacies of topical corticosteroids. There is some evidence to suggest that a recognizable correlation exists between vasoconstrictor potency and therapeutic efficacy in man.

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 or widespread application may increase the possibility of hypothalamic-pituitary-adrenal (HPA) axis suppression.

The vasoconstrictor assay showed that Locoid Lipocream® Cream had a more pronounced skin blanching effect than Locoid® Cream, suggesting greater percutaneous absorption from the former. At the present time, no adequate HPA axis suppresion studies have been conducted for Locoid Lipocream® Cream.

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

Locoid Lipocream® (hydrocortisone butyrate 0.1%) Cream is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

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 HPA axis suppression, manifestations of Cushing’s syndrome, hyperglycemia, and glucosuria in some patients. Conditions which increase the risk of systemic toxicity include the application of more potent steroids, use over large surface areas, prolonged use, and the addition of occlusive dressings. 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.
  4. Patients should report any signs of local adverse reactions.
  5. 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 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 in Salmonella ryphimurium strains TA98, TA100, and TA92 with prednisolone and hydrocortisone have revealed negative results.

Pregnancy

Teratogenic Effects

Pregnancy Category C:

Corticosteroids are generally 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.

In teratogenicity studies, topical administration of 1% or 10% hydrocortisone butyrate in an ointment to pregnant Wistar rats (gestational days 6-15) or New Zealand white rabbits (gestational days 6-18) resulted in no teratogenic findings. However, a dose-dependant increase in fetal resorptions was reported in rabbits, and fetal resorptions were observed in rats treated with 10% hydrocortisone butyrate.

The doses given to rats are approximately 8 to 80 times the human topical dose based on a body surface area comparison (assuming 100% absorption).

For rabbits, the doses given were approximately 0.2 and 2 times the human topical dose. Increased resorptions were also noted in Wistar rats given subcutaneous administrations of hydrocortisone butyrate (9mg/kg/day; 3 times the human topical dose) on gestational days 9 through 15. In CS mice given subcutaneous administrations of 1mg/kg/day (0.2 times the human topical dose), an increased number of cervical ribs and one fetus with clubbed legs was reported.

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.

Locoid Lipocream® (hydrocortisone butyrate 0.1%) Cream should not be used extensively on pregnant patients, in large amounts, or for longer than two weeks.

Nursing Mothers

It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities 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

Safety and effectiveness in pediatric patients have not been established.

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.

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.

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, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae and miliaria.

OVERDOSAGE

Topically applied corticosteroids can be absorbed in sufficient amounts to produce systemic effects. (See PRECAUTIONS.)

DOSAGE AND ADMINISTRATION

Locoid Lipocream® (hydrocortisone butyrate 0.1%) Cream should be applied to the affected areas as a thin film two or three times daily (depending on the severity of the condition) and for no longer than two weeks. If an infection develops, appropriate antimicrobial therapy should be instituted.

HOW SUPPLIED

Locoid Lipocream® (hydrocortisone butyrate 0.1%) Cream is supplied in tubes containing:

15 g NDC 0496-0821-15

45 g NDC 0496-0821-45

60 g NDC 0496-0821-25

STORAGE

Store at controlled temperature between 59º - 77ºF (15º - 25ºC).

Image from Drug Label Content

Protected Under U.S. Patent


LOCOID LIPOCREAM (Hydrocortisone Butyrate)
PRODUCT INFO
Product Code 0496-0821 Dosage Form CREAM
Route Of Administration TOPICAL DEA Schedule
INGREDIENTS
Name (Active Moiety) Type Strength
Hydrocortisone Butyrate (Hydrocortisone) Active 1 MILLIGRAM  In 1 GRAM
cetostearyl alcohol Inactive  
ceteth-20 Inactive  
mineral oil Inactive  
white petrolatum Inactive  
citric acid Inactive  
sodium citrate Inactive  
propylparaben Inactive  
butylparaben Inactive  
water Inactive  
IMPRINT INFORMATION
Characteristic Appearance Characteristic Appearance
Color Score
Shape Symbol
Imprint Code Coating
Size
PACKAGING
# NDC Package Description Multilevel Packaging
1 0496-0821-15 15 GRAM In 1 TUBE None
2 0496-0821-45 45 GRAM In 1 TUBE None
3 0496-0821-25 60 GRAM In 1 TUBE None

Revised: 09/2006Ferndale Laboratories