Mometasone is a steroid medication used to treat certain skin conditions and some respiratory conditions. It is administered topically and as a nasal spray, depending on the indication. Mometasone furoate was patented in 1981 and was approved for medical use in 1987. It is on the World Health Organization’s List of Essential Medicines. In 2020, it was the 231st most commonly prescribed medication in the United States, with over 1 million prescriptions.
ATC code: D07AC13 – R01AD09
Drug class: Corticosteroid – Skin – Respiratory System
Pharmaceutical form: Cream and ointment – Nasal spray
Available dosages: 0.1% cream and ointment – 0.05% nasal spray
Brand: Momkin®
Indications: Psoriasis, eczema, vitiligo and lichen planus – allergic rhinitis and asthma
Pharmacodynamics
Like other topical corticosteroids, mometasone has anti-inflammatory, antipruritic, anti-redness, and vasoconstrictive effects.
Mechanism of action
Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. Inflammation is reduced by reducing the release of leukocyte acid hydrolases, preventing macrophage accumulation at inflamed sites, interfering with leukocyte adhesion to the capillary wall, reducing capillary membrane permeability, reducing complement proteins (the complement system), inhibiting the release of histamine and kinin, and interfering with scar tissue formation. The anti-inflammatory effects of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
In asthma, inhaled mometasone is believed to inhibit mast cells, eosinophils, basophils, and lymphocytes. There is also evidence that it inhibits histamine, leukotrienes, and cytokines.
Pharmacokinetics
Attract
The mean time to peak concentration is 1 to 2.5 hours. Bioavailability is reported as < encoded_tag_open ><, but studies of multiple doses of inhaled corticosteroids have shown a bioavailability of 11%. The 0.1% ointment may have a bioavailability of 0.7%.
Distribution
98% to 99% (laboratory concentration 5 to 500 ng/ml)
Metabolism
Hepatic
Cytochrome P450 3A4
Excretion
Half-life: The terminal half-life of an inhaled dose is approximately 5 hours, although 5.8 hours has been reported by other sources.
Excretion: 74% biliary and 8% renal
Uses
- Topically in the treatment of inflammatory skin disorders (such as dermatitis and psoriasis) and phimosis of the penis
- Inhaled for allergic rhinitis (such as hay fever) and asthma
Contraindications
- Allergy to mometasone
Warnings
- Safety/effectiveness in children for use beyond 3 weeks has not been established.
- Children may be more susceptible to systemic toxicity due to their larger skin surface area to body mass ratio.
- Do not use with occlusive dressings.
- Do not use for acne, rosacea, perioral dermatitis, or diaper dermatitis.
- If concomitant skin infections are present or develop, appropriate antifungal or antibacterial agents should be used in consultation with the physician. If the desired response does not occur promptly, treatment should be discontinued until the infection is adequately controlled.
- If irritation occurs, discontinue treatment and initiate appropriate therapy.
- Use of topical corticosteroids may increase the risk of posterior subcapsular cataracts and glaucoma. After eye contact; advise patients to report any visual symptoms and seek evaluation by an ophthalmologist.
- Systemic absorption of topical corticosteroids can cause reversible suppression of the hypothalamic-pituitary-adrenal (HPA) axis with the potential for glucocorticosteroid insufficiency. This may occur during treatment or after discontinuation of treatment.
- Manifestations of Cushing’s syndrome, hyperglycemia, and glucosuria can be induced in some patients by systemic absorption of topical corticosteroids during treatment.
- Factors that predispose a patient to HPA axis suppression with topical corticosteroids include: use of high-potency steroids, broad-spectrum therapy, long-term use, use of occlusive dressings, altered skin barrier, liver failure, and young age.
- Because of the potential for systemic absorption, the use of topical corticosteroids may require that patients be periodically evaluated for HPA axis suppression. This may be done using an adrenocorticotropic hormone (ACTH) stimulation test.
Side effects
- Burning
- Itching
- Acne rosacea
- Stimulation
- Dryness
- Folliculitis
- Hypertrichosis (excessive hair growth)
- Acne-like pimples
- Hypopigmentation
- Perioral dermatitis
- Allergic contact dermatitis
- Secondary infection
- Skin atrophy
- Striae (skin cracks)
- Miliaria (heat rash or heat rash)
- Blurred vision
- Cataract
- Glaucoma
- Increased intraocular pressure
- Central serous chorioretinopathy
Drug interactions
Contraindications
Mifepristone: Enhances each other’s effects. Contraindicated in patients undergoing long-term corticosteroid therapy due to increased risk of adrenal insufficiency.
Serious interference
Aldesleukin: Topical mometasone reduces the effects of aldesleukin by an unknown mechanism of interaction. Avoid or use an alternative drug.
Need a monitor
- Ceritinib: Reduces each other’s effects. Monitor closely for hyperglycemia and treat appropriately. Patients with a history of diabetes or glucose intolerance are at greater risk.
- Corticorlin: Topical mometasone reduces the effects of corticorlin (pharmacodynamic antagonism). Corticosteroid treatment may blunt the response to corticorlin.
- Hyaluronidase: Topical mometasone reduces the effects of hyaluronidase by an unknown mechanism. Patients receiving higher doses of corticosteroids may not experience optimal clinical response to standard doses of hyaluronidase. Higher doses of hyaluronidase may be required.
- Amastaxine: Mutually increase the toxicity of each other. Concomitant use of Amastaxine and topical mometasone may increase the risk of infection.
