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Prednicarbate

Class: Anti-inflammatory Agents
ATC Class: D07AC18
VA Class: DE200
Chemical Name: (11β)-17-[(ethoxycarbonyl)oxy]-11-hydroxy-21-(1-oxopropoxy)-pregna-1,4-diene-3,20-dione
Molecular Formula: C27H36O8
CAS Number: 73771-04-7
Brands: Dermatop

Introduction

A synthetic corticosteroid.1 2 3 11

Uses for Prednicarbate

Corticosteroid-responsive Dermatoses

Relief of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.1 2 3 4 11

Generally most effective in acute or chronic dermatoses (e.g., seborrheic or atopic dermatitis, localized neurodermatitis, anogenital pruritus, psoriasis, late phase of allergic contact dermatitis, inflammatory phase of xerosis).b

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Topical therapy generally preferred over systemic therapy; fewer associated adverse systemic effects.b

Topical therapy generally only controls manifestations of dermatoses; eliminate cause if possible.b

Topical efficacy may be increased by using a higher concentration or occlusive dressing therapy. (See Administration with Occlusive Dressing under Dosage and Administration.)b

Response may vary from one topical corticosteroid preparation to another.b

Anti-inflammatory activity may vary considerably depending on the vehicle, drug concentration, site of application, disease, and individual patient.b

Prednicarbate 0.1% ointment and 0.1% cream are considered to have medium-range potency.1 c

Prednicarbate Dosage and Administration

General

  • Consider location of the lesion and the condition being treated when choosing a dosage form.b

  • Creams are suitable for most dermatoses, but ointments may also provide some occlusion and are usually used for the treatment of dry, scaly lesions.b

  • Formulation affects percutaneous penetration and subsequent activity; extemporaneous preparation or dilution of commercially available products with another vehicle may decrease effectiveness.b

  • Patients applying a topical corticosteroid to a large surface area and/or to areas under occlusion should be evaluated periodically for evidence of hypothalamic-pituitary-adrenal (HPA)-axis suppression by appropriate endocrine testing (e.g., ACTH stimulation, plasma cortisol, urinary free cortisol).b (See Hypothalamic-Pituitary-Adrenal Axis Suppression and also Systemic Effects, under Cautions.)

Administration

Topical Administration

For dermatologic use only; avoid contact with eyes.1 c

Apply creams and ointments topically to the skin or scalp.1 c

The area of skin to be treated may be thoroughly cleansed before topical application to reduce the risk of infection; however, some clinicians believe that, unless an occlusive dressing is used, cleansing of the treated area is unnecessary and may be irritating.b

Apply cream or ointment sparingly in a thin film and rub gently into the affected area.1 c

After a favorable response is achieved, frequency of application or concentration (strength) may be decreased to the minimum necessary to maintain control and to avoid relapse; discontinue if possible.b

Administration with Occlusive Dressing

Occlusive dressings may be used for severe or resistant dermatoses.1 3 11 (See Occlusive Dressings under Cautions.)

Soak or wash the affected area to remove scales; apply a thin film of cream or ointment; rub gently into the lesion; and apply another thin film.b Cover affected area with a thin, pliable plastic film and seal it to adjacent normal skin with adhesive tape or hold in place with a gauze or elastic bandage.b

If affected area is moist, incompletely seal the edges of the plastic film or puncture the film to allow excess moisture to escape.b For added moisture in dry lesions, apply cream or ointment and cover with a dampened cloth before the plastic film is applied or briefly soak the affected area in water before application of the drug and plastic film.b

Thin polyethylene gloves may be used on the hands and fingers, plastic garment bags may be used on the trunk or buttocks, a tight shower cap may be used for the scalp, or whole-body suits may be used instead of plastic film to provide occlusion.b

Frequency of occlusive dressing changes depends on the condition being treated; cleansing of the skin and reapplication of the corticosteroid are essential at each dressing change.b

Occlusive dressing is usually left in place for 12–24 hours and therapy is repeated as needed.b Although occlusive dressing may be left in place for 3–4 days at a time in resistant conditions, most clinicians recommend intermittent use of occlusive dressings for 12 hours daily to reduce the risk of adverse effects (particularly infection) and systemic absorption and for greater convenience.b

The drug and an occlusive dressing may be used at night, and the drug or a bland emollient may be used without an occlusive dressing during the day.b

In patients with extensive lesions, sequential occlusion of only one portion of the body at a time may be preferable to whole-body occlusion.b (See Occlusive Dressings under Cautions.)

Dosage

Pediatric Patients

Administer the least amount of topical preparations that provide effective therapy.b (See Pediatric Use under Cautions.)

Corticosteroid-responsive Dermatoses
Topical

Children ≥1 year of age: Apply cream sparingly twice daily.1

Children ≥10 years of age: Apply ointment sparingly twice daily.11

Discontinue when control is achieved; if improvement does not occur within 2 weeks, consider reassessment of the diagnosis.1

Adults

Corticosteroid-responsive Dermatoses
Topical

Apply cream or ointment sparingly twice daily.1 3 4 11

Discontinue when control is achieved; if improvement does not occur within 2 weeks, consider reassessment of the diagnosis.1

Prescribing Limits

Pediatric Patients

Corticosteroid-responsive Dermatoses
Topical (Cream)

Children ≥ 1 year of age: Maximum 3 weeks.1

Special Populations

No special population dosage recommendations at this time.1 c

Cautions for Prednicarbate

Contraindications

  • Known hypersensitivity to prednicarbate or any ingredient in the formulation.1 c

Warnings/Precautions

Sensitivity Reactions

Allergic contact dermatitis may manifest as failure to heal rather than irritation as occurs with other topical preparations that do not contain corticosteroids; confirm with diagnostic patch testing.1 b c

General Precautions

Hypothalamic-Pituitary-Adrenal Axis Suppression

Topically applied corticosteroids can be absorbed in sufficient amounts to reversibly suppress the HPA axis.1 b c

Perform periodic HPA-axis evaluation by appropriate testing (e.g., ACTH stimulation, morning plasma cortisol, urinary free cortisol), especially in patients applying a topical corticosteroid to a large surface area or to areas under occlusion.1 b c

If HPA-axis suppression occurs, withdraw the drug, reduce the frequency of application, and/or substitute a less potent corticosteroid.1 b c

HPA-axis function recovery generally is prompt and complete following drug discontinuance.1 b c

Rarely, glucocorticosteroid insufficiency may require systemic corticosteroid therapy.1 b c

Systemic Effects

Systemic absorption following topical administration may result in manifestations of Cushing's syndrome, hyperglycemia, and glucosuria in some patients.1 b c

Adverse systemic effects may occur when corticosteroids are used on large areas of the body, for prolonged periods of time, with an occlusive dressing, and/or concurrently with other corticosteroid-containing preparations.b

Infants and children may be more susceptible to adverse systemic effects.1 b c (See Pediatric Use under Cautions.)

Local Effects

Possible adverse local reactions (e.g., burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, miliaria); may occur more frequently with the use of occlusive dressings, especially with prolonged therapy.1 b c

Prolonged use of topical corticosteroids may cause atrophy of the epidermis and subcutaneous tissue;b these effects are most likely to occur (even with short-term use) in intertriginous (e.g., axilla, groin), flexor, and facial areas.b

If irritation occurs, discontinue drug and institute appropriate therapy.1 b c

Skin Infection

If concurrent skin infection is present or develops, initiate appropriate anti-infective therapy.1 b c If infection does not respond promptly, discontinue topical corticosteroid therapy until the infection has been controlled.1 b c

When topical corticosteroids and topical anti-infectives are used concomitantly, consider that the corticosteroid may mask clinical signs of bacterial, fungal, or viral infections; prevent recognition of ineffectiveness of the anti-infective; or suppress hypersensitivity reactions to ingredients in the formulation.b In addition, consider the cautions, precautions, and contraindications associated with the anti-infective.b (See Occlusive Dressings under Cautions.)

Some manufacturers state that topical corticosteroids are contraindicated in patients with tuberculosis of the skin, dermatologic fungal infections, and cutaneous or systemic viral infection (including vaccinia and varicella and herpes simplex of the eye or adjacent skin).b However, most clinicians believe topical corticosteroids can be used with caution if the infection is treated.b

Occlusive Dressings

Adverse systemic corticosteroid effects may occur with use of occlusive dressings on large areas of the body and for prolonged periods of time; monitor accordingly.b (See Hypothalamic-Pituitary-Adrenal Axis Suppression and also Systemic Effects, under Cautions.)

Adverse local reactions may occur more frequently with the use of occlusive dressings, especially with prolonged therapy.1 b c (See Local Effects under Cautions.)

Do not use occlusive dressings on weeping or exudative lesions.b

Do not use occlusive dressings in patients with primary skin infection.b

Remove occlusive dressings covering large areas if body temperature increases; thermal homeostasis may be impaired.b

Use plastic occlusive material with care to avoid the risk of suffocation.b

Specific Populations

Pregnancy

Category C.1 c

Lactation

Not known whether topical prednicarbate is distributed into milk.1 c Caution advised if topical prednicarbate is used.1 c

Pediatric Use

Safety and efficacy of prednicarbate cream not established in children <1 year of age.1 In children ≥1 year of age, safety and efficacy of cream for >3 weeks not established.1

Safety and efficacy of prednicarbate ointment not established in children <10 years of age.c

Do not use cream to treat diaper dermatitis.1 Tight-fitting diapers or plastic pants may constitute occlusive dressings.1 b

Children are more susceptible to topical corticosteroid-induced HPA-axis suppression and Cushing's syndrome than mature individuals because of a greater skin surface area-to-body weight ratio,1 b c especially when topical corticosteroids are applied to >20% of body surface area.1 The risk of adrenal suppression appears to increase with decreasing age.b (See Systemic Effects under Cautions.)

Manifestations of adrenal suppression in children include linear growth retardation, delayed weight gain, low plasma cortisol concentrations, and lack of response to corticotropin (ACTH) stimulation.1 b c

Children also are at greater risk of glucocorticoid insufficiency during and/or after withdrawal of treatment.1 c

Intracranial hypertension has occurred in children; manifestations include bulging fontanelles, headaches, and bilateral papilledema.1 b c

Topical corticosteroid therapy in children should be limited to the minimum amount necessary for therapeutic efficacy; chronic topical corticosteroid therapy may interfere with growth and development.b

Common Adverse Effects

Burning, itching, drying, scaling, cracking, pain, irritant dermatitis,c mild atrophy, telangiectasia,1 folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, skin atrophy, striae, miliaria.c

Interactions for Prednicarbate

Specific Drugs and Laboratory Tests

Drug or Test

Interaction

Nitroblue-tetrazolium test for bacterial infection

Concurrent use of corticosteroids reportedly may result in false-negative resultsb

Prednicarbate Pharmacokinetics

Absorption

Bioavailability

Topically applied prednicarbate can be absorbed through normal intact skin.1 b c

Percutaneous penetration of corticosteroids following topical application to the skin varies among individuals and may be increased by occlusive dressings, high corticosteroid concentrations, and certain vehicles.b

Only minimal amounts of topical corticosteroid reach the dermis and subsequently the systemic circulation after application to most normal skin areas; more absorption occurs from the scrotum, axilla, eyelid, face, and scalp than from the forearm, knee, elbow, palm, and sole.b

Absorption is markedly increased by loss of the skin’s keratin layer and by inflammation and/or diseases of the epidermal barrier (e.g., psoriasis, eczema).1 b c

Distribution

Extent

Not known whether topical prednicarbate is distributed into milk.1 b c

Elimination

Metabolism

Once absorbed through the skin, topically applied corticosteroids are metabolized primarily in the liver.b

Elimination Route

Topical corticosteroids and metabolites are excreted by the kidneys and, to a lesser extent, in bile.b

Stability

Storage

Topical

Cream

5–25°C.1

Ointment

15–30°C.c

Actions

  • Medium-range corticosteroid activity.1 c

  • Precise mechanism of action for topical anti-inflammatory activity is unknown; therapeutic benefit in the management of corticosteroid-responsive dermatoses mediated primarily through anti-inflammatory, antipruritic, and vasoconstrictive actions.1 b c

  • Anti-inflammatory effects may occur through induction of phospholipase A2 inhibitory proteins (lipocortins); decreased arachidonic acid release from membrane phospholipids.1 c Decreased arachidonic acid precursors may downregulate biosynthesis of potent inflammatory mediators (e.g., prostaglandins, leukotrienes).1 c

  • Decreases inflammation by stabilizing leukocyte lysosomal membranes, preventing release of destructive acid hydrolases from leukocytes; inhibiting macrophage accumulation in inflamed areas; reducing leukocyte adhesion to capillary endothelium; reducing capillary wall permeability and edema formation; decreasing complement components; antagonizing histamine activity and release of kinin from substrates; reducing fibroblast proliferation, collagen deposition, and subsequent scar tissue formation; and possibly by other mechanisms as yet unknown.b

Advice to Patients

  • Importance of using only as directed, only for the disorder for which it was prescribed, and for no longer than prescribed; avoid contact with the eyes and only apply externally as directed.1 c (See Topical Administration under Dosage and Administration.)

  • Importance of not using cream on the face, underarms, or groin areas.1

  • Importance of informing patients that treated areas of the skin should not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by a clinician.1 c

  • Importance of reporting any local adverse reactions, especially those occurring under occlusive bandage, to a clinician.b 1 c

  • Importance of informing parents of children that cream should not be used for diaper dermatitis or applied in the diaper area as diapers or plastic pants may constitute occlusive dressing.1

  • Advise patient to discontinue medication when control is achieved; if no improvement is seen in 2 weeks, contact clinician.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs; other corticosteroid-containing preparations should not be used without first consulting with clinician.1 c

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 c

  • Importance of advising patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Prednicarbate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Topical

Cream

0.1%

Dermatop Emollient

Dermik

Ointment

0.1%

Dermatop

Dermik

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions January 1, 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Dermik Laboratories. Dermatop (prednicarbate) emollient cream 0.1% prescribing information. Berwyn, PA; 2003 May.

2. Schäfer-Korting M, Korting HC, Kerscher MJ et al. Prednicarbate activity and benefit/risk ratio in relation to other topical glucocorticoids. Clin Pharmacol Ther. 1993; 54:448-56. [IDIS 321791] [PubMed 8222488]

3. Hoechst-Roussel Dermatology. Dermatop (prednicarbate) emollient cream 0.1% product monograph. Somerville, NJ; 1993 Jul.

4. Hanifin J, Abrams BB, Cherill RJ. Management of atopic dermatitis with prednicarbate emollient cream 0.1%, a nonhalogenated prednisolone derivative. J Geriatr Dermatol. 1994; 2:119-27.

5. Cornell RC, Cherill RJ, Abrams BB. Safety of prednicarbate emollient cream 0.1% and ointment 0.1%, nonhalogenated, midpotency topical steroid formulations. J Geriatr Dermatol. 1994; 2:57-65.

6. Korting HC, Vieluf D, Kerscher M. 0.25% Prednicarbate cream and the corresponding vehicle induce less skin atrophy than 0.1% betamethasone-17-valerate cream and 0.05% clobetasol-17-propionate cream. Eur J Clin Pharmacol. 1992; 42:159-61. [IDIS 293468] [PubMed 1618247]

7. Korting HC, Kerscher MJ, Schäfer-Korting M. Topical glucorticoids with improved benefit/risk ratio: do they exist? J Am Acad Dermatol. 1992; 27:87-92.

8. Hoechst-Roussel Dermatology, Somerville, NJ: Personal communication.

9. Hein R, Korting HC, Mehring T. Differential effect of medium potent nonhalogenated double-ester-type and conventional glucocorticoids on proliferation and chemotaxis of fibroblasts in vitro. Skin Pharmacol. 1994; 7:300-6. [PubMed 8054213]

10. Levy J, Gassmuller J, Schroder G et al. Comparison of the effects of calcipotriol, prednicarbate and clobetasol 17-propionate on normal skin assessed by ultrasound measurement of skin thickness. Skin Pharmacol. 1994; 7:231-6. [PubMed 8024805]

11. Dermik Laboratories. Dermatop (prednicarbate) ointment 0.1% prescribing information. Berwyn, PA; 2003 Apr.

a. AHFS drug information 2007. McEvoy GK, ed. Prednicarbate emollient. Bethesda, MD: American Society of Health-Systems Pharmacists; 2007:3535.

b. AHFS drug information 2007 McEvoy GK, ed. Topical corticosteroids general statement. Bethesda, MD: American Society of Health-System Pharmacists; 2007:3423–5.

c. Dermik Laboratories. Dermatop (prednicarbate) ointment 0.1% prescribing information. Bridgewater, NJ; 2006 July.

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