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Apexicon

Generic Name: diflorasone diacetate
Dosage Form: ointment

Apexicon Ointment
(diflorasone diacetate ointment, USP, 0.05%)

Rx only

FOR EXTERNAL USE ONLY

NOT FOR OPHTHALMIC USE

DESCRIPTION

Apexicon® Ointment (diflorasone diacetate ointment USP 0.05%) contains 0.5 mg diflorasone diacetate in an ointment base.

Chemically, diflorasone diacetate is 6α,9-difluoro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17,21- diacetate with the molecular formula C26H32F2O7 and a molecular weight of 494.54. The structural formula is represented below:

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Each gram of Apexicon® Ointment (diflorasone diacetate ointment USP 0.05%), for topical administration, contains 0.5 mg diflorasone diacetate in an ointment base consisting of propylene glycol, glyceryl monostearate and white petrolatum.

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.

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. They 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.

CONTRAINDICATIONS

Topical steroids 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 or under an occlusive dressing should be evaluated periodically for evidence of HPA axis suppression by using the urinary free cortisol and ACTH stimulations 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 Patients: 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 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, 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: Teratogenic effectsPregnancy 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.

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: 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 pediatric patients receiving topical corticosteroids. Manifestations of adrenal suppression in pediatric patients 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 pediatric patients 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 have been reported 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:

  1. Burning
  2. Itching
  3. Irritation
  4. Dryness
  5. Folliculitis
  6. Hypertrichosis
  7. Acneiform eruptions
  8. Hypopigmentation
  9. Perioral dermatitis
  10. Allergic contact dermatitis
  11. Maceration of the skin
  12. Secondary infections
  13. Skin atrophy
  14. Striae
  15. Miliaria

OVERDOSAGE

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

DOSAGE AND ADMINISTRATION

Apexicon® Ointment (diflorasone diacetate ointment USP 0.05%) should be applied to the affected area as a thin film from one to three times daily depending on the severity or resistant nature 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 initiated.

HOW SUPPLIED

Apexicon® Ointment (diflorasone diacetate ointment USP 0.05%) is available in the following size tubes:

 
NDC 0462-0394-30        30 gram tube
 
NDC 0462-0394-60        60 gram tube

Store at controlled room temperature 15° to 30°C (59° to 86°F). Keep tightly closed.

January 2008

PharmaDerm®
A division of Nycomed US Inc.
Melville, NY 11747
www.pharmaderm.com

I8394D
R1/08

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 30 G LABEL

NDC 0462-0394-30

PharmaDerm ®

Apexicon ® Ointment
(diflorasone diacetate ointment USP 0.05%)

FOR EXTERNAL USE ONLY
NOT FOR OPHTHALMIC USE

Rx only
30 g

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 30 G CARTON

NDC 0462-0394-30

PharmaDerm ®

Apexicon ® Ointment
(diflorasone diacetate ointment USP 0.05%)

FOR EXTERNAL USE ONLY
NOT FOR OPHTHALMIC USE

Rx only
30 g

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 60 G LABEL

NDC 0462-0394-60

PharmaDerm ®

Apexicon ® Ointment
(diflorasone diacetate ointment USP 0.05%)

FOR EXTERNAL USE ONLY
NOT FOR OPHTHALMIC USE

Rx only
60 g

PACKAGE LABEL – PRINCIPAL DISPLAY PANEL – 60 G CARTON

NDC 0462-0394-60

PharmaDerm ®

Apexicon ® Ointment
(diflorasone diacetate ointment USP 0.05%)

FOR EXTERNAL USE ONLY
NOT FOR OPHTHALMIC USE

Rx only
60 g

Apexicon 
diflorasone diacetate ointment ointment
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0462-0394
Route of Administration TOPICAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
diflorasone diacetate (diflorasone diacetate) diflorasone diacetate 0.5 mg  in 1 g
Inactive Ingredients
Ingredient Name Strength
Petrolatum  
Glyceryl Monostearate  
Propylene Glycol  
Packaging
# Item Code Package Description
1 NDC:0462-0394-30 1 TUBE (1 TUBE) in 1 CARTON
1 30 g in 1 TUBE
2 NDC:0462-0394-60 1 TUBE (1 TUBE) in 1 CARTON
2 60 g in 1 TUBE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA075374 09/30/2009
Labeler -  Pharmaderm, A division of Nycomed US Inc. (043838424)
Registrant - Nycomed US Inc. (043838424)
Establishment
Name Address ID/FEI Operations
Nycomed US Inc. 043838424 ANALYSIS
Establishment
Name Address ID/FEI Operations
Nycomed US Inc. 174491316 MANUFACTURE
Revised: 09/2009
 
Pharmaderm, A division of Nycomed US Inc.
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