Mometasone furoate is a glucocorticoid or corticosteroid used topically to reduce inflammation of the skin or in the airways. It is a prodrug of the free form mometasone (INN).
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Medical uses
Mometasone furoate is used in the treatment of inflammatory skin disorders (such as eczema and psoriasis) (topical form), allergic rhinitis (such as hay fever) (topical form), asthma (inhalation form) for patients unresponsive to less potent corticosteroids, and penile phimosis. In terms of steroid strength, it is more potent than hydrocortisone, and less potent than dexamethasone.
Some low-quality evidence suggests the use of mometasone for symptomatic improvement in children with adenoid hypertrophy.
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 adults (including the elderly) and children over 2 years to diminish the symptoms such as hay fever (seasonal allergic rhinitis) and other allergies (perennial rhinitis), including nasal congestion, discharge, pruritus, and sneezing and to treat nasal polyps.
Asthma
Mometasone furoate can be used with formoterol for the treatment of asthma, due to its anti-inflammatory properties.
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
In addition to the glucocorticoid properties of mometasone furoate, it is a very potent agonist of the progesterone receptor as well as a partial agonist of the mineralocorticoid receptor.
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 (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 enzyme cytochrome P450 2C8 which participates in the activity of monooxygenase.
The inflammation is reduced in decreasing the liberation of hydrolace acids of leukocytes, the prevention of the accumulation macrophages in the sites of inflammation, the interference with 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 are also reduced. It is believed that the action of corticosteroid anti-inflammatory agents are 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 skin reduces the inflammation associated with chronic or acute dermatosis.
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 6?-hydroxymometasone. In human hepatic microsomes, the formation of these metabolites is regulated by CYP3A4.
Society and culture
Brand names
As of 2016 mometasone furoate was available worldwide in formulations for nasal, oral inhalation, and topical administration, for human and for veterinary use, and in combinations with other drugs, under many brand names.
The following combination drugs were available as of 2016:
- Mometasone and azelastine as Nasaflex
- Mometasone and clotrimazole and gentamicin for veterinary use as Mometamax
- Mometasone and florfenicol and terbinafine for veterinary use as Claro
- Mometasone and formoterol as Dulera and Zenhale
- Mometasone and fusidic acid as Momate-F
- Mometasone and miconazole as Elica M and Sensicort-F
- Mometasone and mupirocin as Sensicort-B
- Mometasone and orbifloxacin and posaconazole for veterinary use as Posatex
- Mometasone and salicylic acid as Belosalic, Cortimax-S, Elicasal, Elocom Plus, Elosalic, Momate, Momesalic, Momtas, Monsalic, and Sensicort-S
- Mometasone and tazarotene as Tazasone Forte
- Mometasone and terbinafine as Cutizone-T
It was available as of 2016 as the single active agent in the following brands: Alcom, Altosone, Asmanex, Atozon, Aureox, Belloseta, Bioelementa, Biometasona, Bloctimo, Borgasone, Breso, Broner, Codermo, Cortynase, Cutimom, Cutizone, Cutticom, Dance, Demoson, Dergentil, Derimod, Dermacortine, Dermaten, Dermome, Dermosona, Dermotasone, Dermovel, Desdek, Ecelecort, Ecural, Edelan, Elica, Elisone, Elisox, Elitasone, Elna, Elocan, Elocom, Elocon, Elocortin, Elofute, Elomet, Elomox, Eloskin, Eloson, Elosone, Elovent, Elox, Etacid, Eversone, Eztom, F-Din, Fenisona, Flazcort, Flogocort, Fremomet, Frondava, Fu Mei Song, Fulmeta, Furo, Furoato de Mometasona, Furoderm, Gistan-H, Honmet, Iflacort, Intercon, Ivoxel, Kalmente, Konex, Ladexol, Lisoder, Logren, Loksin, Lomeane, M-Furo, Makiren, Mefurosan, Melocort, Mena, Mesone, Metacortil, Metactiv, Metaflam, Metagra, Metasafe, Metason, Metasone, Metaspray, Metatop, Metaz, Metmin, Metsone, Midermin, Mifusin, Minyear, Mofacort, Mofulex, Mofur, Mofuroate, Molison, Momate, Momax, Momecon, Momecort, Momecutan, Momederm, MomeGalen, Momegen, Momekort, Momelab, Momentum, Momeplus, Momerid, Momeson, Momesone, Momester, Momet, Mometa, Mometagen, Mometason, Mometasona, Mometasona Furoato, Mometasone Furoate, Mometasone Furoate Hydrate, Mometasonfuroaat, Mometasonfuroat, Mometasoni furoas, Mometasonum, Mometasyn, Mometasyn, Mometax, Mometazon, Mometazona, Mometazona Fuorat, Mometazonfuroat, Mometix-AQ, Momevate, Momexa, Mommex, Mommox, Momtas, Monaliz, Monez, Monovel, Monovo, Mosone, Motaderm, Motaneal, Movesan, Mtaz, Mundoson, Murozo, Myrey, Narinex, Nasamet, Nasehaler, Nasocure, Nasomet, Nasometin, Nasonex, Nassomet, Nazofix, Nazoster, Netonox, Nexomist, Novasone, Ovison, Ovixan, Oximax, Pharmecort, Pluster, Pronasal, Propel, Prospiril, Pydercon, Rinelon, Rinitek, Rino-Val, Rinobudex, Rinonex, Rinosal, Rinosona, Rinoval, Risonel, Sensicort, Septopic, Silkaren, Soneta, Suavicort, Suqi, Synaller, Tabunex, Topcort, Topison, Uniclar, Uniderm, Vizomet, Yperod, Zalconex, and Zynovate.
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