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| Trade names | Nasonex, Asmanex, Elocon, others[1] |
| Other names | LAS-41002,9α,21-Dichloro-11β,17α-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione 17α-(2-furoate) |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Topical,inhalation (nasal spray) |
| Drug class | Corticosteroid;Glucocorticoid |
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| Pharmacokinetic data | |
| Bioavailability | Nasal spray is virtually undetectable in plasma; but systemic availability is comparable tofluticasone[9] |
| Protein binding | 98% to 99% |
| Metabolism | Liver |
| Eliminationhalf-life | 5.8 hours |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.125.600 |
| Chemical and physical data | |
| Formula | C22H28Cl2O4 for mometasone C27H30O6Cl2 as furoate |
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Mometasone, also known asmometasone furoate, is asteroid (specifically, aglucocorticoid) medication used to treat certainskin conditions,hay fever, andasthma.[10][11][12] Specifically it is used to prevent rather than treat asthma attacks.[10] It can be applied to the skin, inhaled, or used in the nose.[10][11][12] Mometasonefuroate, not mometasone, is used in medical products.[13]
Common side effects when used for asthma include headache, sore throat, andthrush.[10] It is therefore recommended to rinse the mouth after use.[10] Long-term use may increase the risk forglaucoma andcataracts.[10] Common side effects when used in the nose includeupper respiratory tract infections andnose bleeds.[12] Common side effects when applied on the skin includeacne,skin atrophy, and itchiness.[11] It works by decreasinginflammation.[10]
Mometasone furoate was patented in 1981 and came into medical use in 1987.[14] It is on theWorld Health Organization's List of Essential Medicines[15] and is available as ageneric medication.[16][17] In 2023, it was the 272nd most commonly prescribed medication in the United States, with more than 800,000 prescriptions.[18][19]
Mometasone furoate is used in the treatment of inflammatory skin disorders (such aseczema[20] andpsoriasis) (topical form),allergic rhinitis (such ashay fever) (topical form),asthma (inhalation form)[21][22] for patients unresponsive to less potentcorticosteroids, and penilephimosis.[23] In terms of steroid strength, it is more potent thanhydrocortisone, and less potent thandexamethasone.[24]
Some low-quality evidence suggests the use of mometasone for symptomatic improvement in children withadenoid hypertrophy.[25]
Mometasone is used to alleviate inflammation and itchiness in skin conditions that respond to treatment with glucocorticoids such as psoriasis and atopic dermatitis.[26][27]
Nasal Mometasone is used in people over two years of age to diminish the symptoms of hay fever (seasonal allergic rhinitis) and other allergies (perennial rhinitis), including nasal congestion, discharge, pruritus, sneezing, and treatnasal polyps.[6]
It is not useful for thecommon cold.[28]
Mometasone furoate can be used withformoterol for the treatment of asthma, due to its anti-inflammatory properties.[25][22]
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People should not use inhaled mometasone or mometasonenasal spray if they have:
Those who are using mometasone nasal or inhaled for a long period of time (e.g. more than three months) should get regular eye exams to check forglaucoma andcataracts and should take precautions to avoid infections such as taking a vitamin D supplement, staying away from those with an infection (chickenpox, measles, colds or flu, COVID-19), washing foods, hand washing and calling a family doctor at the first sign of a severe infection.
People should not use mometasone topical (skin cream) if:
The risks of Mometasone furoate to the baby during pregnancy cannot be ruled out.
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The nasal spray form of mometasone may cause the followingside effects:
Serious side effects include:Thrush (fungal infection in the nose or throat), slow wound healing, eye problems such as glaucoma or cataracts, weakened immune system (immunodeficiency) which causes increased susceptibility to infections andadrenal insufficiency.
The inhaled form of mometasone for asthma may cause the following side effects:
Serious side effects may include allergic reactions (anaphylaxis), increased risk ofosteoporosis, glaucoma and cataracts, thrush in the mouth or throat, growth retardation in children,bronchospasms, adrenal insufficiency and weakened immune system which causes increased susceptibility to infections.
The topical (skin cream) version may cause:
The only serious side effect that is known with mometasone topical isadrenal insufficiency.
Mometasone furoate reduces inflammation by causing several effects:[6][29][30]
In addition to theglucocorticoid properties of mometasone furoate, it is a very potentagonist of theprogesterone receptor as well as apartial agonist of themineralocorticoid receptor.[31]
Mometasone, like other corticosteroids, possesses anti-inflammatory, antipruritic, and vasoconstrictive properties. For allergies, corticosteroids reduce the allergic reactions in various types of cells (mastocytes and eosinophils) 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 enzymecytochrome P450 2C8 which participates in the activity of monooxygenase.[32]
The inflammation is reduced by decreasing the liberation ofhydrolase acids ofleukocytes, the prevention of the accumulation ofmacrophages in the sites of inflammation, the interference with the adhesion of leukocytes tocapillary walls, the reduction of the permeability of the capillary membranes and consequentlyedema, the reduction of complementary components, inhibition of histamine andkinin liberation, and interference with scar tissue formation.[33] 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 ofphospholipase A2, collectively called lipocortins. The lipocortins, in turn, control the biosynthesis of potent mediators of inflammation as theprostaglandins andleukotrienes, inhibiting the liberation of the molecular precursors ofarachidonic acid. Intranasal mometasone alleviates symptoms such asrhinorrhea 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 (vs. baseline ) in neutrophils (a white blood cell) in the nasal mucosa.[citation needed] It could be also considered an antihistamine along with its glucocorticoid effects because it significantly reduces histamine and eosinophil cationic protein levels.[citation needed]
Extensive metabolic hepatic metabolism of mometasone furoate to multiple metabolites occurs. No principal metabolites are detectable in plasma. Afterin vitro incubation, one of the minor metabolites formed is furoate 6β-hydroxymometasone. In human hepatic microsomes, the formation of these metabolites is regulated byCYP3A4.[6]
Mometasone by itself is asynthetic,steroidalglucocorticoid orcorticosteroid that was never marketed.[34][35][36] The C17αfuroateester of mometasone, is the marketed medication.[34][35][36] Mometasone furoate acts as aprodrug of mometasone.[37] In addition to its glucocorticoid activity, mometasone also has very potentprogestogenic activity and acts as apartial agonist of themineralocorticoid receptor.[31]
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.[1]
The following combination medications are available as of 2022:[38]
| Combination | Commercial Name | Notes |
|---|---|---|
| azelastine | Nasaflex | |
| clotrimazole andgentamicin | Mometamax, Mometavet | Veterinary use |
| clotrimazole andmupirocin | Derma Q | |
| florfenicol andterbinafine | Claro | Veterinary use |
| formoterol | Dulera, Hexaler Bronquial Duo, Zenhale | |
| fusidic acid | Bactirest-M, Dermotil Fusid, Momate-F | |
| gentamicin andposaconazole | Mometamax Ultra | Veterinary use |
| hydroquinone andtretinoin | Acnezac-MH | |
| miconazole | Elica M, Elica-M, and Sensicort-F | |
| mupirocin | Sensicort-B | |
| orbifloxacin andposaconazole | 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 |
Mometasone nasal spray should not be used to treat symptoms (e.g., sneezing, stuffy, runny, itchy nose) caused by the common cold. Mometasone nasal spray is in a class of medications called corticosteroids. It works by blocking the release of certain natural substances that cause allergy symptoms.
