AHFS Class:

• Corticosteroids 84:06.08

Generic Name(s):

• Mometasone Furoate

Mometasone furoate is a synthetic corticosteroid.1,2,3,6,10

Mometasone furoate shares the actions of other topical corticosteroids and is used for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.1,2,3,7,10

For EENT uses of mometasone furoate, see 52:08.

Topical mometasone furoate cream and ointment are applied sparingly in thin films and are rubbed into the affected area, usually once daily.1,2 The cream and ointment also have been applied twice daily.2,3,7 A few drops of mometasone furoate lotion are applied to the affected area once daily, holding the nozzle of the bottle close to the area and squeezing gently.10 It is recommended that mometasone furoate preparations not be used with occlusive dressings, and that patients be warned that treated areas of the skin not be bandaged or otherwise covered or wrapped as to be occlusive unless directed by their physician.1,2,9,10

Mometasone furoate shares the toxic potentials of other topical corticosteroids,1,2,3,5,10 and the usual precautions for corticosteroid therapy should be observed.1,5,10 (See Cautions in the Topical Corticosteroids General Statement 84:06.08.)

Topical application of mometasone furoate cream or ointment in healthy individuals revealed little or no evidence of local irritation in most patients, and the potential for contact irritation from the preparations and their vehicles was minimal and comparable to that of other commonly used topical corticosteroid formulations.2 In addition, there was no evidence of contact sensitization,2 and the commercially available preparations appear to have minimal potential for inducing photoallergic or phototoxic reactions.2

Mometasone furoate does not appear to suppress the hypothalamic-pituitary-adrenal (HPA) axis substantially following topical application of usual doses.1,2,8,9,10 In patients with psoriasis or atopic dermatitis, 15 g of the 0.1% cream or ointment (15 mg of mometasone furoate) applied without occlusion to at least 30% of the body twice daily for 7 days caused a slight reduction in adrenal corticosteroid secretion, although plasma cortisol concentrations remained within the normal range and there was no evidence of HPA-axis suppression.1,2 Plasma cortisol concentrations were not altered following topical application of 7.5 g of the 0.1% ointment (7.5 mg of drug) applied without occlusion9 to at least 30% of the body twice daily for 21 days2 or following topical application of 15 mL of the 0.1% lotion to diseased skin in patients with scalp and body psoriasis twice daily for 7 days.10

Pending further accumulation of safety data,8,9 mometasone, like other topical corticosteroids, should not be used in the treatment of acne, rosacea, or perioral dermatitis.8 Mometasone furoate preparations are contraindicated in individuals with known hypersensitivity to the drug, other corticosteroids, or any ingredient in the respective formulation.1,2,10

Pediatric Precautions

If mometasone furoate is used for topical treatment of various corticosteroid-responsive dermatoses in children, the usual precautions associated with topical corticosteroid therapy in pediatric patients should be observed.1,5,10 (See Cautions: Pediatric Precautions, in the Topical Corticosteroids General Statement 84:06.08.)

Mutagenicity and Carcinogenicity

No evidence of mometasone-induced mutagenesis was seen in various in vitro test systems (e.g., Ames microbial mutagen test, mouse lymphoma assay, micronucleus test).1,2,10 Long-term studies to determine the carcinogenic potential of topical corticosteroids have not been performed to date.1,2,5,10

Pregnancy, Fertility, and Lactation

The teratogenic potential of topical mometasone furoate is not known;1 however, the drug has produced teratogenic effects characteristic of corticosteroids in animals following topical application.2 For additional information, see Cautions: Pregnancy, Fertility, and Lactation, in the Topical Corticosteroids General Statement 84:06.

Pharmacokinetics

Absorption

Percutaneous penetration of mometasone furoate varies among individuals and can be altered by using different vehicles;1,4,5,10 percutaneous penetration can be increased by the use of occlusive dressings and by inflammation and/or other disease of the epidermal barrier (e.g., psoriasis, eczema).1,5,10

Following topical application of mometasone furoate to normal skin, only small amounts of the drug appear to reach the dermis and subsequently the systemic circulation with the usual dosa about 0.7% of the drug reportedly reached systemic circulation during the 8-hour period after a single application of 880 mg of a 0.1% ointment in healthy individuals with normal skin.1,2,9 However, systemic absorption may be increased when the skin is inflamed or diseased.1,5 The extent of systemic absorption of the drug appears to be similar following topical application of the cream or ointment;1 the manufacturer states that a similar minimal degree of absorption would be expected with topical application of the lotion.10 Following topical application of 130 mg of mometasone furoate 0.1% cream or ointment in rabbits, approximately 5 or 6% of a topically applied dose, respectively, was absorbed systemically.1,2,9 In other studies, approximately 2.5 or 2% of a topically applied dose of the ointment was absorbed systemically in rats or dogs, respectively.1,2

Elimination

Following percutaneous penetration of mometasone furoate, drug that is systemically absorbed probably follows the metabolic pathways of systemically administered corticosteroids.1,2,5,10 (See Pharmacokinetics: Elimination, in the Corticosteroids General Statement 68:04.) However, systemic metabolism of mometasone has not been fully characterized or quantified;8,9 in animals, drug that is absorbed following topical application does not appear to accumulate in tissues.2 Systemically absorbed mometasone and its metabolites may be excreted in urine and, to some extent, in bile.1,2,10

Chemistry and Stability

Chemistry

Mometasone furoate is a synthetic corticosteroid.1,2,3,6,10 Mometasone is the 9α,21-dichloro-16α-methyl derivative of prednisolone2,6 and differs structurally from beclomethasone by the 16-methyl group being in the α rather than the β configuration and by the replacement of the hydroxyl group with a chlorine atom at position 21.3,6 Topical anti-inflammatory activity is enhanced by these structural modifications.6 Esterification of the hydroxyl group at position 17 of the mometasone molecule enhances topical anti-inflammatory activity of the furoate compared with mometasone.6 Mometasone furoate occurs as a white to off-white powder1,2,10 and has solubilities of less than 0.07 mg/mL in water and 8.3 mg/mL in alcohol at 25°C.9

Stability

Mometasone furoate cream, ointment, and lotion should be stored at 2-30°C.1,2,10 When stored at this temperature, the commercially available cream and ointment have an expiration date of 24 months following the date of manufacture.2

Additional Information

For further information on chemistry, pharmacology, absorption, uses, cautions, and methods of application of mometasone furoate, see the Topical Corticosteroids General Statement 84:06.08. The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

1. Schering Corporation. Elocon^® prescribing information. Kenilworth, NJ; 1987 April.

2. Schering Corporation. Elocon^® basic data book. Kenilworth, NJ; (undated).

3. Medansky RS, Brody NI, Kanof NB et al. Clinical investigations of mometasone furoate—a novel, nonfluorinated topical corticosteroid. Semin Derm . 1987; 6:94-100.

4. Cornell RC, Stoughton RB. The use of topical steroids in psoriasis. Dermatol Clin . 1984; 2:397-409.

5. Food and Drug Administration. Topical corticosteroids class labeling guideline. Available from: Professional Labeling Branch, Division of Drug Advertising and Labeling, Food and Drug Administration, Rockville, MD; (undated).

6. Shapiro EL, Gentles MJ, Tiberi RL et al. 17-Heteroaroyl esters of corticosteroids. 2: 11β-Hydroxy series. J Med Chem . 1987; 30:1581-8. [PubMed 3625707]

7. Anon. Mometasone—a new topical steroid. Med Lett Drugs Ther . 1987; 29:96-8. [PubMed 3670213]

8. Reviewers' comments (personal observations); 1987 Nov.

9. Winter-Sperry RL (Schering Corporation, Kenilworth, NJ): Personal communication; 1987 Nov 25.

10. Schering Corporation. Elocon^® lotion prescribing information. Kenilworth, NJ; 1989 Mar.