, Volume 55, Issue 1, pp 145-163
Date: 15 Nov 2012

Topical Mometasone

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Summary

Synopsis

Mometasone, a synthetic 16α-methyl analogue of beclomethasone, is classified as a ‘potent’ glucocorticoid for dermatological use. It is available as 0.1% cream, ointment and lotion formulations for the treatment of patients with inflammatory glucocorticoid-responsive dermatoses.

In patients with atopic dermatitis, the effects of mometasone 0.1% applied once daily over 2 to 3 weeks were similar to those of other glucocorticoids of similar potency, such as betamethasone dipropionate 0.05% twice daily and methylprednisolone aceponate 0.1% once daily. Mometasone 0.1% was significantly superior to twice-daily application of less potent glucocorticoids such as clobetasone 0.05%, hydrocortisone 1.0%, hydrocortisone butyrate and hydrocortisone valerate 0.2%. In patients with seborrhoeic dermatitis, mometasone 0.1% was more effective than ketoconazole 2.0% and hydrocortisone 1.0% in trials lasting 4 or 6 weeks. In the management of scalp psoriasis and psoriasis vulgaris, mometasone 0.1% applied once daily for 2 to 8 weeks was generally more effective than other glucocorticoids of similar or weaker potency such as betamethasone valerate 0.1%, fluocinolone acetonide 0.025%, fluticasone propionate 0.005%, triamcinolone acetonide 0.1% and hydrocortisone 1.0% and as effective as diflucortolone valerate 0.1%. Alternate day application of mometasone 0.1% for 2 weeks was as effective as once-daily application in maintaining symptom control in a small number of patients with psoriasis vulgaris.

Although mometasone demonstrates greater anti-inflammatory activity and a longer duration of action than betamethasone, it has low potential to cause adverse systemic effects such as suppression of the hypothalamic-pituitary-adrenal (HPA) axis. Moreover, its atrophogenic potential is low and no greater than that of other glucocorticoids in its class, such as betamethasone valerate. Transient, mild to moderate, local adverse effects such as burning, stinging, folliculitis, dryness, acneiform eruptions and signs of skin atrophy have been reported with mometasone. Mometasone has shown a low risk of primary sensitisation and cross-reactions in preliminary patch test studies.

Mometasone is a well tolerated topical glucocorticoid effective in the management of patients with atopic dermatitis, seborrhoeic dermatitis, scalp psoriasis and psoriasis vulgaris. In addition to its low potential for causing primary sensitisation and cross-reactions with other topical glucocorticoids, mometasone offers the convenience of once-daily administration.

Pharmacological Properties

Mometasone has high lipophilicity and displays greater in vitro affinity for glucocorticoid receptors in rat epidermis than betamethasone dipropionate. In suppressing erythema induced by ultraviolet (UV)-B light, mometasone showed greater activity and a longer duration of action than betamethasone dipropionate and betamethasone valerate. However, it showed little potential to suppress the hypothalamic-pituitary-adrenal axis in patients and healthy volunteers.

An in vitro study on human fibroblasts and keratinocytes reported the anti-proliferative effects of mometasone to be negligible or small compared with those of betamethasone valerate. No clinical or histological signs of skin atrophy were observed in 6 volunteers after 12 months of once-daily application of mometasone 0.1% cream. Some clinical trials have found the atrophogenic potential of mometasone to be low and similar to that of hydrocortisone, prednicarbate, betamethasone valerate and methylprednisolone aceponate. However, in one trial, mometasone 0.1% ointment was associated with a significantly greater incidence and severity of skin atrophy and telangiectasia than methylprednisolone aceponate 0.1% ointment.

Little topically applied mometasone reaches the systemic circulation. In human volunteers, only 0.7% of mometasone 0.1% ointment was systemically absorbed after a contact time of 8 hours without occlusive dressing. After application of 10g 0.1% ointment under occlusion, the plasma concentration of mometasone peaked at about 130 ng/L in 12 hours and then declined rapidly.

Therapeutic Use

Atopic dermatitis. In short term studies (≤6 weeks) once-daily mometasone 0.1% cream or ointment was significantly more effective in reducing total sign and symptom severity scores than twice-daily clobetasone 0.05% ointment, clobetasone 0.05% cream, hydrocortisone butyrate cream, hydrocortisone valerate 0.2% cream and hydrocortisone 1.0% cream and as effective as once-daily methylprednisolone aceponate 0.1% cream or twice-daily betamethasone dipropionate 0.05% ointment in the treatment of moderate to severe atopic dermatitis.

Seborrhoeic dermatitis. Once-daily application of mometasone 0.1% solution was more effective and showed a faster onset of action than ketoconazole 2.0% shampoo applied twice weekly over 4 weeks in the treatment of patients with moderate to severe seborrhoeic dermatitis. Significantly greater improvement was observed after 6 weeks with mometasone 0.1% cream applied once daily than with hydrocortisone 1.0% cream applied twice daily. Psoriasis. Mometasone 0.1% lotion or ointment applied once daily was significantly more effective than twice-daily betamethasone valerate 0.1% lotion or ointment over 2 to 8 weeks in 3 trials in patients with scalp psoriasis or psoriasis vulgaris. The once-daily application of mometasone 0.1% cream, lotion or ointment formulations produced significantly greater reductions in total psoriatic symptom scores than once-daily hydrocortisone 1% ointment, twice-daily fluticasone propionate 0.005% ointment, triamcinolone acetonide 0.1% lotion or ointment or 3-times-daily fluocinolone acetonide 0.025% cream or ointment. In patients with psoriasis vulgaris, mometasone applied once daily was as effective as twice-daily diflucortolone valerate 0.1% ointment and triamcinolone acetonide 0.1% cream. Results of a preliminary short term study suggest that application of mometasone 0.1% ointment on alternate days may be as effective as once-daily application in maintenance therapy in patients with psoriasis vulgaris.

Tolerability

Topical mometasone 0.1% cream was associated with local cutaneous adverse effects in 1.6 and 7.0% of 319 adult and 74 paediatric patients, respectively. The most commonly encountered adverse effects included stinging, burning, pruritus, folliculitis, dryness, acneiform/erythematous eruptions, tenderness and signs of skin atrophy. These adverse effects were transient and of mild or mild to moderate intensity.

Preliminary patch test studies have reported that the risk of primary sensitisation or cross-reaction with mometasone is low, even in patients known to be hypersensitive to glucocorticoids.

Dosage and Administration

Mometasone 0.1% cream, ointment or lotion is indicated for the symptomatic relief of inflammation and pruritus in patients with glucocorticoid-responsive dermatoses. It should be applied without occlusion to the affected areas once daily. Like other topical glucocorticoids, mometasone should not be used in patients with primary cutaneous viral, bacterial or fungal infections, rosacea, acne, perioral dermatitis, or perianal or genital pruritus. It may be used with caution in children aged ≥2 years.

Various sections of the manuscript reviewed by: A. Goossens, Department of Dermatology, Katholieke Universiteit, Leuven, Belgium; B. Homey, Department of Dermatology, Heinrich Heine University, Dusseldorf, Germany; V. Koivukangas, Department of Dermatology, University of Oulu, Oulu, Finland; A.T. Lane, Department of Dermatology, Stanford University School of Medicine, Stanford, California, USA; H.I. Maibach, Department of Dermatology, University of California San Francisco, School of Medicine, San Francisco, California, USA; M. Wilkinson, Department of Dermatology, The General Infirmary at Leeds, Leeds, England; J.M. Wishart, Department of Dermatology, Auckland Hospital, Auckland, New Zealand.