Mometasone
Mometasone and its derivate mometasone furoate are steroids, medications used to treat certain skin conditions, hay fever, and asthma. Specifically, they are used to prevent, rather than treat, asthma attacks. They can be applied to the skin, inhaled, or used in the nose. Currently only mometasone furoate is used in medical products.
Common side effects when used for asthma include headache, sore throat, and thrush. It is therefore recommended to rinse the mouth after use. Long-term use may increase the risk for glaucoma and cataracts. Common side effects when used in the nose include upper [respiratory tract infection]s and nose bleeds. Common side effects when applied on the skin include acne, skin atrophy, and itchiness. It works by decreasing inflammation.
Mometasone furoate was patented in 1981 and came into medical use in 1987. It is on the World Health Organization's List of Essential Medicines and is available as a generic medication. In 2023, it was the 272nd most commonly prescribed medication in the United States, with more than 800,000 prescriptions.
Medical uses
Mometasone furoate is used in the treatment of inflammatory skin disorders such as eczema and psoriasis, allergic rhinitis such as hay fever, asthma for patients unresponsive to less potent corticosteroids, and penile phimosis. Some low-quality evidence suggests the use of mometasone for symptomatic improvement in children with adenoid hypertrophy. In terms of steroid strength, it is more potent than hydrocortisone, and less potent than dexamethasone.Mometasone is used to alleviate inflammation and itchiness in skin conditions that respond to treatment with glucocorticoids such as psoriasis and atopic dermatitis. Nasal mometasone is used in people over two years of age to diminish the symptoms of hay fever and other allergies, including nasal congestion, discharge, pruritus, sneezing, and treat nasal polyps. Mometasone furoate can be used with formoterol for the treatment of asthma, due to its anti-inflammatory properties.
It is not useful for the common cold.
Contraindications
People should not use inhaled mometasone or mometasone nasal spray if they have glaucoma, cataracts, hypersensitivity, or are allergic to any ingredient in mometasone.Those who are using mometasone nasal or inhaled for a long period of time should get regular eye exams to check for glaucoma and cataracts and should take precautions to avoid infections such as taking a vitamin D supplement, staying away from those with an infection, washing foods, hand washing and calling a family doctor at the first sign of a severe infection.
People should not use mometasone topical if hypersensitive or allergic to any ingredient in the skin cream.
Risks of mometasone furoate to the baby during pregnancy cannot be ruled out.
Side effects
The nasal spray form of mometasone may cause the following side effects:- headache
- Viral upper respiratory infections
- sore throat
- nose bleeds
- cough
- muscle and joint pain
The inhaled form of mometasone for asthma may cause the following side effects:
- headache
- stuffy or runny nose
- dry throat
- swelling of nose, throat and sinuses
- flu-like symptoms
- painful menstrual periods
The topical version may cause:
- burning and itching at the application site
- acne
- changes in skin color
- dryness at the application site
- skin sores
Pharmacology
Pharmacodynamics
Mometasone furoate reduces inflammation by causing several effects:- Reversing the activation of inflammatory proteins
- Activating the secretion of anti-inflammatory proteins
- Stabilizing cell membranes
- Decreasing the influx of inflammatory cells
Mechanism of action
Mometasone, like other corticosteroids, possesses anti-inflammatory, antipruritic, and vasoconstrictive properties. For allergies, corticosteroids reduce the allergic reactions in various types of cells that are responsible for allergic reactions. Mometasone and other corticosteroids circulate in the blood easily, crossing cellular membranes and binding with cytoplasmic receptors, resulting in the transcription and synthesis of proteins. It also inhibits the actions of the enzyme cytochrome P450 2C8 which participates in the activity of monooxygenase.The inflammation is reduced by decreasing the liberation of hydrolase acids of leukocytes, the prevention of the accumulation of macrophages in the sites of inflammation, the interference with the adhesion of leukocytes to capillary walls, the reduction of the permeability of the capillary membranes and consequently edema, the reduction of complementary components, inhibition of histamine and kinin liberation, and interference with scar tissue formation. The proliferation of fibroblasts and collagen deposits is also reduced. It is believed that the action of corticosteroid anti-inflammatory agents is bound to inhibitive proteins of phospholipase A2, collectively called lipocortins. The lipocortins, in turn, control the biosynthesis of potent mediators of inflammation as the prostaglandins and leukotrienes, inhibiting the liberation of the molecular precursors of arachidonic acid. Intranasal mometasone alleviates symptoms such as rhinorrhea aquosa, nasal congestion, nasal drip, sneezing, and pharyngeal itching. Topical administration applied to the skin reduces the inflammation associated with chronic or acute dermatosis.
Although mometasone furoate does not have significant systemic immunomodulatory effects, it can be considered a local immunosuppressive drug because clinical studies have shown reductions in neutrophils in the nasal mucosa. It could be also considered an antihistamine along with its glucocorticoid effects because it significantly reduces histamine and eosinophil cationic protein levels.
Pharmacokinetics
Metabolism
Extensive metabolic hepatic metabolism of mometasone furoate to multiple metabolites occurs. No principal metabolites are detectable in plasma. After in vitro incubation, one of the minor metabolites formed is furoate 6β-hydroxymometasone. In human hepatic microsomes, the formation of these metabolites is regulated by CYP3A4.Mometasone
Mometasone by itself is a synthetic, steroidal glucocorticoid or corticosteroid that was never marketed. The C17α furoate ester of mometasone, is the marketed medication. Mometasone furoate acts as a prodrug of mometasone. In addition to its glucocorticoid activity, mometasone also has very potent progestogenic activity and acts as a partial agonist of the mineralocorticoid receptor.Society and culture
Availability
As of 2016, mometasone furoate is available worldwide in formulations for nasal, oral inhalation, and topical administration, for human and veterinary use, either as a single active agent or in combination with other medications, under many brand names.Combinations
The following combination medications are available as of 2022:| Combination | Commercial Name | Notes |
| azelastine | Nasaflex | |
| clotrimazole and gentamicin | Mometamax, Mometavet | Veterinary use |
| clotrimazole and mupirocin | Derma Q | |
| florfenicol and terbinafine | Claro | Veterinary use |
| formoterol | Dulera, Hexaler Bronquial Duo, Zenhale | |
| fusidic acid | Bactirest-M, Dermotil Fusid, Momate-F | |
| gentamicin and posaconazole | Mometamax Ultra | Veterinary use |
| hydroquinone and tretinoin | Acnezac-MH | |
| miconazole | Elica M, Elica-M, and Sensicort-F | |
| mupirocin | Sensicort-B | |
| orbifloxacin and posaconazole | Posatex, Posatex voor honden, Posatex für Hunde | Veterinary use |
| salicylic acid | Cortimax-S, Elicasal, Elocom Plus, Elosalic, Mezo-S, Momate-S, Momesalic, Momtas-S, Monsalic, Sensicort-S | |
| terbinafine | Cutizone-T, Mezo-T, MomelomTerbi-Humanity | |
| tiotropium | Tiomom | - |