Apexicon E

Plain Topical Corticosteroids

For topical dermatologic use only. Not for ophthalmic, oral, or intravaginal use. Diflorasone is not generally recommended for use on the face, groin or in the axillae.
Restrict application to the active lesions and try to avoid normal surrounding skin.
The amount of cream or ointment needed to cover a certain area can be calculated. A 1 g application of cream covers 100 cm2 of skin. The entire skin surface of the average size adult will be covered by 30 g of topical steroid cream.
The manufacturer states that diflorasone may be used under an occlusive dressing for psoriasis or recalcitrant conditions. However, due to the potential for adverse systemic effects with very high potency corticosteroids, occlusive dressings should be used cautiously, if at all.
High potency corticosteroids such as diflorasone are not recommended for use in the diaper area of infants. If diflorasone is medically necessary, do not use tight fitting diapers or plastic pants on infants, as these garments may constitute occlusive dressings.
Wash hands before and after application. Use gloves if required by universal precautions. Apply sparingly in a thin film and rub gently into affected area.
Acute exudative inflammation, as occurs with poison ivy, may be best treated with the non-emollient cream formulation, which is drying. Dry, scaly dermatoses, as occur with eczema or psoriasis, may be best treated with emollient creams or ointments.

skin atrophy / Delayed / Incidence not known
increased intracranial pressure / Early / Incidence not known
papilledema / Delayed / Incidence not known
ocular hypertension / Delayed / Incidence not known
visual impairment / Early / Incidence not known

erythema / Early / 1.0-10.0
withdrawal / Early / Incidence not known
hypertension / Early / Incidence not known
Cushing's syndrome / Delayed / Incidence not known
pseudotumor cerebri / Delayed / Incidence not known
growth inhibition / Delayed / Incidence not known
hypothalamic-pituitary-adrenal (HPA) suppression / Delayed / Incidence not known
glycosuria / Early / Incidence not known
adrenocortical insufficiency / Delayed / Incidence not known
hyperglycemia / Delayed / Incidence not known
cataracts / Delayed / Incidence not known
impaired wound healing / Delayed / Incidence not known
skin ulcer / Delayed / Incidence not known
tolerance / Delayed / Incidence not known
contact dermatitis / Delayed / Incidence not known

maculopapular rash / Early / 1.0-10.0
pruritus / Rapid / 1.0-10.0
skin irritation / Early / 1.0-10.0
xerosis / Delayed / 1.0-10.0
striae / Delayed / Incidence not known
miliaria / Delayed / Incidence not known
hypertrichosis / Delayed / Incidence not known
purpura / Delayed / Incidence not known
infection / Delayed / Incidence not known
telangiectasia / Delayed / Incidence not known
folliculitis / Delayed / Incidence not known
acneiform rash / Delayed / Incidence not known
skin hypopigmentation / Delayed / Incidence not known
headache / Early / Incidence not known

Apexicon, Apexicon E, Florone, Florone-E, Maxiflor, Psorcon, Psorcon E

Rx

High potency, topical, fluorinated corticosteroid
Used to treat corticosteroid-responsive dermatoses and psoriasis
Long-term or extensive use can lead to systemic side effects

Apply a thin layer topically to the affected skin area(s) 1 to 4 times daily.

Apply a thin layer topically to the affected skin area(s) 1 to 4 times daily.

Apply a thin layer topically to the affected skin area(s) 1 to 3 times daily.

Apply a thin layer topically to the affected skin area(s) 1 to 4 times daily. The duration of the therapy depends on factors such as the topical corticosteroid potency, disease severity and anatomic location, and age. After improvement, may consider transitioning to lower-potency corticosteroid, using intermittent therapy, and combining treatment with noncorticosteroidal agents. Taper by reducing use to every other day, then twice weekly, then discontinue if adequate control is maintained. Guidelines recommend class 1 to 5 topical corticosteroids for up to 4 weeks for plaque psoriasis not involving intertriginous areas and class 1 to 7 topical corticosteroids for a minimum of up to 4 weeks for scalp psoriasis. Use of topical corticosteroids for more than 12 weeks may be considered under careful supervision.

Apply a thin layer topically to the affected skin area(s) 1 to 4 times daily. Guidelines recommend topical corticosteroids as monotherapy for short-term treatment of localized psoriasis.

Apply a thin layer topically to the affected skin area(s) 1 to 3 times daily. The duration of the therapy depends on factors such as the topical corticosteroid potency, disease severity and anatomic location, and age. After improvement, may consider transitioning to lower-potency corticosteroid, using intermittent therapy, and combining treatment with noncorticosteroidal agents. Taper by reducing use to every other day, then twice weekly, then discontinue if adequate control is maintained. Guidelines recommend class 1 to 5 topical corticosteroids for up to 4 weeks for plaque psoriasis not involving intertriginous areas and class 1 to 7 topical corticosteroids for a minimum of up to 4 weeks for scalp psoriasis. Use of topical corticosteroids for more than 12 weeks may be considered under careful supervision.

Apply a thin layer to the affected vulvar, labial, and perineal areas twice daily for 6 to 8 weeks. No significant adverse effects were noted during a 6-month to 3-year follow-up of 10 prepubertal girls.

Apply vigorously to the lesioned skin areas twice daily.

Apply vigorously to the lesioned areas twice daily. One study demonstrated complete remission in 63% of stage T1 patients and 25% of stage T2 patients with patch-stage mycosis fungoides. Total response rates (complete plus partial remission) exceed 80% for stage T2 and 90% for stage T1. The very high potency (Class I compounds) were most effective. The investigators suggest to apply the cream vigorously instead of thinly or sparingly. Thirteen percent of patients experienced reversible suppression of the HPA axis with no clinical side effects. One patient discontinued therapy due to skin atrophy.

†Indicates off-label use

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Metyrapone: (Major) Medications which affect pituitary or adrenocortical function, including all corticosteroid therapy, should be discontinued prior to and during testing with metyrapone. Patients taking inadvertent doses of corticosteroids on the test day may exhibit abnormally high basal plasma cortisol levels and a decreased response to the test. Although systemic absorption of topical corticosteroids is minimal, temporary discontinuation of these products should be considered if possible to reduce the potential for interference with the test results.

Apexicon/Apexicon E/Diflorasone/Diflorasone Diacetate/Florone/Florone-E/Maxiflor/Psorcon/Psorcon E Topical Cream: 0.05%
Apexicon/Diflorasone/Diflorasone Diacetate/Florone/Maxiflor/Psorcon/Psorcon E Topical Ointment: 0.05%

50 g/week topically.

50 g/week topically.

50 g/week topically.

10 g/week topically.

Topical corticosteroids exhibit anti-inflammatory, antipruritic, and vasoconstrictive properties. At the cellular level, corticosteroids induce peptides called lipocortins. Lipocortins antagonize phospholipase A2, an enzyme which causes the breakdown of leukocyte lysosomal membranes to release arachidonic acid. This action decreases the subsequent formation and release of endogenous inflammatory mediators including prostaglandins, kinins, histamine, liposomal enzymes and the complement system. Early anti-inflammatory effects of topical corticosteroids include the inhibition of macrophage and leukocyte movement and activity in the inflamed area by reversing vascular dilation and permeability. Later inflammatory processes such as capillary production, collagen deposition, keloid (scar) formation also are inhibited by corticosteroids. Clinically, these actions correspond to decreased edema, erythema, pruritus, plaque formation and scaling of the affected skin.

Diflorasone is administered topically to the skin as a cream or ointment. Anti-inflammatory effects are usually not seen for several hours after diflorasone application, since the mechanism of action requires alterations in synthesis of proteins. Because diflorasone is fluorinated and also contains a substituted 17-hydroxyl group, it is not metabolized in the skin. Once in the systemic circulation, diflorasone is metabolized in the liver, but systemic metabolism has not been fully quantified. Excretion of diflorasone and its metabolites occurs via the urine and bile.

The extent of percutaneous absorption of the topical corticosteroids is dependent on many factors, including the pharmaceutical vehicle and the integrity of the epidermis. In one study, 24 hours after a diflorasone application, 37.5% of the dose had penetrated the skin and 1.1% was systemically absorbed and excreted. Repeated application results in a cumulative depot effect in the skin, which may lead to a prolonged duration of action and increased systemic absorption. Absorption after topical application of diflorasone is increased in areas that have skin damage, inflammation, occlusion, or in areas where the stratum corneum is thin such as the eyelids, genitalia, axillae, and face. The use of occlusive dressings with the application of diflorasone enhances penetration into the skin, and may increase the chance of systemic absorption. Ointments have a hydrating effect, are lipophilic, and enhance the penetration of diflorasone into the skin.

There are no adequate and well-controlled studies of topical application of diflorasone during pregnancy. Topical corticosteroids, including diflorasone, should not be used in large amounts, on large areas, or for prolonged periods of time in pregnant women. Guidelines recommend mild to moderate potency agents over potent corticosteroids, which should be used in short durations. Fetal growth restriction and a significantly increased risk of low birthweight has been reported with use of potent or very potent topical corticosteroids during the third trimester, particularly when using more than 300 grams. 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.

It is not known whether topical administration of diflorasone could result in sufficient systemic absorption to produce detectable quantities in breast milk to cause issues during breast-feeding. However, most dermatologists stress that topical corticosteroids can be safely used during lactation. If applied topically, care should be used to ensure the infant will not come into direct contact with the area of application, such as the breast. Increased blood pressure has been reported in an infant whose mother applied a high potency topical corticosteroid ointment directly to the nipples. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested drug, healthcare providers are encouraged to report the adverse effect to the FDA.