1
ELOCON®
brand of mometasone furoate ointment
Ointment 0.1%
For Dermatologic Use Only
Not for Ophthalmic Use
DESCRIPTION ELOCON® (mometasone furoate ointment) Ointment, 0.1%, contains
mometasone furoate, USP for dermatologic use. Mometasone furoate is a synthetic
corticosteroid with anti-inflammatory activity.
Chemically, mometasone furoate is 9a,21-dichloro-11b ,17-dihydroxy-16a-
methylpregna-1,4-diene-3,20-dione 17-(2-furoate), with the empirical formula C27H30CI2O6, a
molecular weight of 521.4 and the following structural formula:
[Structure]
Mometasone furoate is a white to off-white powder practically insoluble in water, slightly
soluble in octanol, and moderately soluble in ethyl alcohol.
Each gram contains: 1 mg mometasone furoate, USP in an ointment base of hexylene
glycol; phosphoric acid; propylene glycol stearate (55% monoester); white wax; white
petrolatum; and purified water.
CLINICAL PHARMACOLOGY Like other topical corticosteroids, mometasone furoate has
anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti-
inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are
thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called
lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of
inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common
precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by
phospholipase A2.
Pharmacokinetics: The extent of percutaneous absorption of topical corticosteroids is
determined by many factors including the vehicle and the integrity of the epidermal barrier.
Occlusive dressings with hydrocortisone for up to 24 hours have not been demonstrated to
increase penetration; however, occlusion of hydrocortisone for 96 hours markedly enhances
penetration. Studies in humans indicate that approximately 0.7% of the applied dose of
ELOCON Ointment, 0.1%, enters the circulation after 8 hours of contact on normal skin without
occlusion. Inflammation and/or other disease processes in the skin may increase percutaneous
absorption.
Studies performed with ELOCON Ointment indicate that it is in the medium range of
potency as compared with other topical corticosteroids.
In a study evaluating the effects of mometasone furoate ointment on the hypothalamic-
pituitary-adrenal (HPA) axis, 15 grams were applied twice daily for 7 days to six adult patients
with psoriasis or atopic dermatitis. The ointment was applied without occlusion to at least 30%
of the body surface. The results show that the drug caused a slight lowering of adrenal
corticosteroid secretion.
2
In a pediatric trial, 24 atopic dermatitis patients, of which 19 patients were age 2 to 12
years, were treated with ELOCON Cream, 0.1%, once daily. The majority of patients cleared
within 3 weeks.
Sixty-three pediatric patients ages 6 to 23 months, with atopic dermatitis, were enrolled
in an open-label, hypothalamic-pituitary-adrenal (HPA) axis safety study. ELOCON Ointment
was applied once daily for approximately 3 weeks over a mean body surface area of 39% (range
15% to 99%). In approximately 27% of patients who showed normal adrenal function by
Cortrosyn test before starting treatment, adrenal suppression was observed at the end of
treatment with ELOCON Ointment. The criteria for suppression were: basal cortisol level of £5
mcg/dL, 30-minute post-stimulation level of £18 mcg/dL, or an increase of <7 mcg/dL. Follow-
up testing 2 to 4 weeks after stopping treatment, available for 8 of the patients, demonstrated
suppressed HPA axis function in 3 patients, using these same criteria.
INDICATIONS AND USAGE ELOCON Ointment, 0.1%, is a medium potency corticosteroid
indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-
responsive dermatoses.
ELOCON (mometasone furoate ointment) Ointment, 0.1%, may be used in pediatric
patients 2 years of age or older, although the safety and efficacy of drug use for longer than 3
weeks have not been established (see PRECAUTIONS - Pediatric Use). Since safety and
efficacy of ELOCON Ointment have not been adequately established in pediatric patients below
2 years of age, its use in this age group is not recommended.
CONTRAINDICATIONS ELOCON Ointment is contraindicated in those patients with a
history of hypersensitivity to any of the components in the preparation.
PRECAUTIONS
General: Systemic absorption of topical corticosteroids can produce reversible hypothalamic-
pituitary-adrenal (HPA) axis suppression with the potential for glucocorticosteroid insufficiency
after withdrawal of treatment. Manifestations of Cushing’s syndrome, hyperglycemia, and
glucosuria can also be produced in some patients by systemic absorption of topical
corticosteroids while on treatment.
Patients applying a topical steroid to a large surface area or areas under occlusion should
be evaluated periodically for evidence of HPA axis suppression. This may be done by using the
ACTH stimulation, A.M. plasma cortisol, and urinary free cortisol tests.
In a study evaluating the effects of mometasone furoate ointment on the hypothalamic-
pituitary-adrenal (HPA) axis, 15 grams were applied twice daily for 7 days to six adult patients
with psoriasis or atopic dermatitis. The ointment was applied without occlusion to at least 30%
of the body surface. The results show that the drug caused a slight lowering of adrenal
corticosteroid secretion.
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 corticosteroid. Recovery of
HPA axis function is generally prompt upon discontinuation of topical corticosteroids.
Infrequently, signs and symptoms of glucocorticosteroid insufficiency may occur requiring
supplemental systemic corticosteroids. For information on systemic supplementation, see
Prescribing Information for those products.
Pediatric patients may be more susceptible to systemic toxicity from equivalent doses due
to their larger skin surface to body mass ratios (see PRECAUTIONS - Pediatric Use).
3
If irritation develops, ELOCON Ointment should be discontinued and appropriate
therapy instituted. Allergic contact dermatitis with corticosteroids is usually diagnosed by
observing failure to heal rather than noting a clinical exacerbation as with most topical products
not containing corticosteroids. Such an observation should be corroborated with appropriate
diagnostic patch testing.
If concomitant skin infections are present or develop, an appropriate antifungal or
antibacterial agent should be used. If a favorable response does not occur promptly, use of
ELOCON Ointment 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. This medication should not be used for any disorder other than that for which it was
prescribed.
3. The treated skin area should not be bandaged or otherwise covered or wrapped so as to be
occlusive unless directed by the physician.
4. Patients should report to their physician any signs of local adverse reactions.
5. Parents of pediatric patients should be advised not to use ELOCON Ointment in the
treatment of diaper dermatitis. ELOCON Ointment should not be applied in the diaper area
as diapers or plastic pants may constitute occlusive dressing (see DOSAGE AND
ADMINISTRATION).
6. This medication should not be used on the face, underarms, or groin areas unless directed by
the physician.
7. As with other corticosteroids, therapy should be discontinued when control is achieved. If no
improvement is seen within 2 weeks, contact the physician.
8. Other corticosteroid-containing products should not be used with ELOCON Ointment
without first consulting with the physician.
Laboratory Tests: The following tests may be helpful in evaluating patients for HPA axis
suppression:
ACTH stimulation test
A.M. plasma cortisol test
Urinary free cortisol test
Carcinogenesis, Mutagenesis, Impairment of Fertility: Long-term animal studies have not
been performed to evaluate the carcinogenic potential of ELOCON (mometasone furoate
ointment) Ointment. Long-term carcinogenicity studies of mometasone furoate were conducted
by the inhalation route in rats and mice. In a 2-year carcinogenicity study in Sprague-Dawley
rats, mometasone furoate demonstrated no statistically significant increase of tumors at
inhalation doses up to 67 mcg/kg (approximately 0.04 times the estimated maximum clinical
topical dose from ELOCON Ointment on a mcg/m2 basis). In a 19-month carcinogenicity study
in Swiss CD-1 mice, mometasone furoate demonstrated no statistically significant increase in the
incidence of tumors at inhalation doses up to 160 mcg/kg (approximately 0.05 times the
estimated maximum clinical topical dose from ELOCON Ointment on a mcg/m2 basis).
Mometasone furoate increased chromosomal aberrations in an in vitro Chinese hamster
ovary cell assay, but did not increase chromosomal aberrations in an in vitro Chinese hamster
4
lung cell assay. Mometasone furoate was not mutagenic in the Ames test or mouse lymphoma
assay, and was not clastogenic in an in vivo mouse micronucleus assay, a rat bone marrow
chromosomal aberration assay, or a mouse male germ-cell chromosomal aberration assay.
Mometasone furoate also did not induce unscheduled DNA synthesis in vivo in rat hepatocytes.
In reproductive studies in rats, impairment of fertility was not produced in male or female
rats by subcutaneous doses up to 15 mcg/kg (approximately 0.01 times the estimated maximum
clinical topical dose from ELOCON Ointment on a mcg/m2 basis).
Pregnancy:
Teratogenic Effects: Pregnancy Category C: Corticosteroids have been shown to be 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.
When administered to pregnant rats, rabbits, and mice, mometasone furoate increased
fetal malformations. The doses that produced malformations also decreased fetal growth, as
measured by lower fetal weights and/or delayed ossification. Mometasone furoate also caused
dystocia and related complications when administered to rats during the end of pregnancy.
In mice, mometasone furoate caused cleft palate at subcutaneous doses of 60 mcg/kg and
above. Fetal survival was reduced at 180 mcg/kg. No toxicity was observed at 20 mcg/kg.
(Doses of 20, 60 and 180 mcg/kg in the mouse are approximately 0.01, 0.02 and 0.05 times the
estimated maximum clinical topical dose from ELOCON Ointment on a mcg/m2 basis).
In rats, mometasone furoate produced umbilical hernias at topical doses of 600 mcg/kg
and above. A dose of 300 mcg/kg produced delays in ossification, but no malformations.
(Doses of 300 and 600 mcg/kg in the rat are approximately 0.2 and 0.4 times the estimated
maximum clinical topical dose from ELOCON Ointment on a mcg/m2 basis).
In rabbits, mometasone furoate caused multiple malformations (e.g., flexed front paws,
gallbladder agenesis, umbilical hernia, hydrocephaly) at topical doses of 150 mcg/kg and above
(approximately 0.2 times the estimated maximum clinical topical dose from ELOCON Ointment
on a mcg/m2 basis). In an oral study, mometasone furoate increased resorptions and caused cleft
palate and/or head malformations (hydrocephaly and domed head) at 700 mcg/kg. At 2800
mcg/kg most litters were aborted or resorbed. No toxicity was observed at 140 mcg/kg. (Doses
of 140, 700 and 2800 mcg/kg in the rabbit are approximately 0.2, 0.9 and 3.6 times the estimated
maximum clinical topical dose from ELOCON Ointment on a mcg/m2 basis).
When rats received subcutaneous doses of mometasone furoate throughout pregnancy or
during the later stages of pregnancy, 15 mcg/kg caused prolonged and difficult labor and reduced
the number of live births, birth weight and early pup survival. Similar effects were not observed
at 7.5 mcg/kg. (Doses of 7.5 and 15 mcg/kg in the rat are approximately 0.005 and 0.01 times
the estimated maximum clinical topical dose from ELOCON Ointment on a mcg/m2 basis).
There are no adequate and well-controlled studies of teratogenic effects from topically
applied corticosteroids in pregnant women. Therefore, topical corticosteroids should be used
during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing Mothers: Systemically administered corticosteroids appear in human milk and could
suppress growth, interfere with endogenous corticosteroid production, or cause other untoward
effects. It is not known whether topical administration of corticosteroids could result in
sufficient systemic absorption to produce detectable quantities in human milk. Because many
drugs are excreted in human milk, caution should be exercised when ELOCON Ointment is
administered to a nursing woman.
5
Pediatric Use: ELOCON Ointment may be used with caution in pediatric patients 2 years of age
or older, although the safety and efficacy of drug use for longer than 3 weeks have not been
established. Use of ELOCON Ointment is supported by results from adequate and well-
controlled studies in pediatric patients with corticosteroid-responsive dermatoses. Since safety
and efficacy of ELOCON Ointment have not been adequately established in pediatric patients
below 2 years of age, its use in this age group is not recommended.
ELOCON Ointment caused HPA axis suppression in approximately 27% of pediatric
patients ages 6 to 23 months, who showed normal adrenal function by Cortrosyn test before
starting treatment, and were treated for approximately 3 weeks over a mean body surface area of
39% (range 15% to 99%). The criteria for suppression were: basal cortisol level of £5 mcg/dL,
30-minute post-stimulation level of £18 mcg/dL, or an increase of <7 mcg/dL. Follow-up testing
2 to 4 weeks after stopping treatment, available for 8 of the patients, demonstrated suppressed
HPA axis function in 3 patients, using these same criteria. Long-term use of topical
corticosteroids has not been studied in this population. (see CLINICAL PHARMACOLOGY -
Pharmacokinetics).
Because of a higher ratio of skin surface area to body mass, pediatric patients are at a
greater risk than adults of HPA axis suppression and Cushing’s syndrome when they are treated
with topical corticosteroids. They are, therefore, also at greater risk of glucocorticosteroid
insufficiency during and/or after withdrawal of treatment. Pediatric patients may be more
susceptible than adults to skin atrophy, including striae, when they are treated with topical
corticosteroids. Pediatric patients applying topical corticosteroids to greater than 20% of body
surface are at higher risk of HPA axis suppression.
HPA axis suppression, Cushing’s syndrome, linear growth retardation, delayed weight
gain, and intracranial hypertension have been reported in children receiving topical
corticosteroids. Manifestations of adrenal suppression in children include low plasma cortisol
levels, and absence of response to ACTH stimulation. Manifestations of intracranial
hypertension include bulging fontanelles, headaches, and bilateral papilledema.
ELOCON (mometasone furoate ointment) Ointment, 0.1%, should not be used in the
treatment of diaper dermatitis.
Geriatrics Use: Clinical studies of ELOCON Ointment included 310 subjects who were 65
years of age and over and 57 subjects who were 75 years of age and over. No overall differences
in safety or effectiveness were observed between these subjects and younger subjects, and other
reported clinical experience has not identified differences in responses between the elderly and
younger patients. However, greater sensitivity of some older individuals cannot be ruled out.
ADVERSE REACTIONS In controlled clinical studies involving 812 patients, the incidence of
adverse reactions associated with the use of ELOCON Ointment was 4.8%. Reported reactions
included burning, pruritus, skin atrophy, tingling/stinging, and furunculosis. Reports of rosacea
associated with the use of ELOCON Ointment have been received. In controlled clinical studies
(n=74) involving pediatric patients 2 to 12 years of age, the incidence of adverse experiences
associated with the use of ELOCON Cream is approximately 7%. Reported reactions included
stinging, pruritus, and furunculosis.
The following adverse reactions were reported to be possibly or probably related to
treatment with ELOCON Ointment during a clinical study, in 5% of 63 pediatric patients 6
months to 2 years of age: decreased glucocorticoid levels, 1; an unspecified skin disorder, 1; and
a bacterial skin infection, 1. The following signs of skin atrophy were also observed among 63
6
patients treated with ELOCON Ointment in a clinical study: shininess 4, telangiectasia 1, loss of
elasticity 4, loss of normal skin markings 4, thinness 1. Striae and bruising were not observed in
this study.
The following additional local adverse reactions have been 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: irritation, dryness,
folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic
contact dermatitis, secondary infection, striae, and miliaria.
OVERDOSAGE Topically applied ELOCON Ointment can be absorbed in sufficient amounts
to produce systemic effects (see PRECAUTIONS).
DOSAGE AND ADMINISTRATION Apply a thin film of ELOCON Ointment to the affected
skin areas once daily. ELOCON Ointment may be used in pediatric patients 2 years of age or
older. Since safety and efficacy of ELOCON Ointment have not been adequately established in
pediatric patients below 2 years of age, its use in this age group is not recommended. (see
PRECAUTIONS - Pediatric Use).
As with other corticosteroids, therapy should be discontinued when control is achieved.
If no improvement is seen within 2 weeks, reassessment of diagnosis may be necessary. Safety
and efficacy of ELOCON Ointment in pediatric patients for more than 3 weeks have not been
established.
ELOCON Ointment should not be used with occlusive dressings unless directed by a
physician. ELOCON Ointment should not be applied in the diaper area if the child still requires
diapers or plastic pants as these garments may constitute occlusive dressing.
HOW SUPPLIED ELOCON Ointment, 0.1%, is supplied in 15-g (NDC 0085-0370-01) and
45-g (NDC 0085-0370-02) tubes; boxes of one.
Store ELOCON Ointment between 2°° C and 30°° C (36°° F and 86°° F).
ELOCON®
brand of mometasone furoate ointment
Ointment 0.1%
For Dermatologic Use Only
Not for Ophthalmic Use
SP Schering Corporation
Kenilworth, NJ 07033 USA
Rev. 7/17/02 XXXXXXXX
Copyright ã 1987, 1995, 2001, Schering Corporation. All rights reserved.
---------------------------------------------------------------------------------------------------------------------
This is a representation of an electronic record that was signed electronically and
this page is the manifestation of the electronic signature.
---------------------------------------------------------------------------------------------------------------------
/s/
---------------------
Jonathan Wilkin
7/17/02 06:17:53 PM