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Mometasone furoate is a glucocorticosteroid used topically to reduce inflammation of the skin or in the airways. It is a prodrug of the free form mometasone (INN).

Uses

Mometasone furoate is used in the treatment of inflammatory skin disorders (such as eczema and psoriasis), allergic rhinitis (such as hay fever), asthma^[2]^[3] for patients unresponsive to less potent corticosteroids, and penile phimosis.^[4] In terms of steroid strength, it is more potent than hydrocortisone, and less potent than dexamethasone.^[5]

There is some low quality evidence suggesting the use of mometasone for symptomatic improvement in children with adenoid hypertrophy.^[6]

Mometasone is indicated for the alleviation of inflammatory and pruritic manifestations (with stinging and itching) of dermatosis which respond to treatment with glucocorticoides such as psoriasis and atopic dermatitis (affection dermic chronic, characterized by the apparition of squamous eruptions, accompanied by itching).

Nasal mometasone is employed in adults (including the elderly) and children over 2 years, diminishing the symptoms such as hayfever (seasonal allergic rhinitis) and other allergies (perennial rhinitis), including nasal congestion, discharge, pruritus and sneezing.^[7] Mometasone can be used two to four weeks before pollen season, reducing the severity of symptoms. It is also indicated for the treatment of nasal polyps and symptoms associated with including congestion and hyposmia in adult patients over the age of 18. It can also produce nasal drip, sensation of tickling in the throat and loss of the sense of taste and smell.

Asthma

The furoate of mometasone can be employed together with formoterol for the treatment of asthma, due to its anti-inflammatory properties.^[8]

Pharmacodynamics

It reduces inflammation by causing several effects:^[9]^[10]^[11]

reversing the activation of inflammatory proteins
activating the secretion of anti-inflammatory proteins
stabilising 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.^[12]

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 eosinofiles) 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. Mometasone also inhibits the actions of the enzyme cytochrome P450 2C8 which participates in the activity of Monooxygenase.^[13]

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.^[14] 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 prostaglandin's and leukotriens, inhibiting the liberation of the molecular precursors of arachidonic acid. Intranasal mometasone alleviates symptoms such as rhinorrea acuosa, nasal congestion, nasal drip, sneezing, and pharyngeal itching. Topical administration applied to skin reduces the inflammation associated with chronic or acute dermatosis.

Metabolism

There are extensive metabolic hepatic metabolism to multiple metabolites. There do not exist principal metabolites detectable in plasma. After in-vitro incubation, one of the minor metabolites formed is furoate 6ß-hydroxi-mometasone. In human hepatic microsomes, the formation of these metabolites is regulated by cytochromo P450 3A4.

Availability

Mometasone is marketed under the brand names Elocom (and its derivatives) and Hhsone as a cream or ointment for skin conditions, Nasonex as a nasal spray for upper respiratory conditions and Asmanex Twisthaler as a dry powder inhaler (DPI) for lower respiratory conditions.

It is also available as a veterinary drug in the form of ear drops for treatment of otitis externa under the brand name Mometamax.^[15]

References

^ Zia R Tayab, Tom C Fardon, Daniel K C Lee, Kay Haggart, Lesley C McFarlane, Brian J Lipworth, and Günther Hochhaus (November 2007). "Pharmacokinetic/pharmacodynamic evaluation of urinary cortisol suppression after inhalation of fluticasone propionate and mometasone furoate". Br J Clin Pharmacol 64 (5): 698–705. doi:10.1111/j.1365-2125.2007.02919.x. PMC 2203259. PMID 17509041.
^ Tan RA, Corren J (December 2008). "Mometasone furoate in the management of asthma: a review". Ther Clin Risk Manag 4 (6): 1201–8. PMC 2643101. PMID 19337427.
^ Bousquet J (May 2009). "Mometasone furoate: an effective anti-inflammatory with a well-defined safety and tolerability profile in the treatment of asthma". Int. J. Clin. Pract. 63 (5): 806–19. doi:10.1111/j.1742-1241.2009.02003.x. PMID 19392928.
^ Khope S (March 2010). "Topical mometasone furoate for phimosis". Indian pediatr 47 (3): 282. PMID 20371899.
^ Williams D. What does potency actually mean for inhaled corticosteroids?. The Journal Of Asthma: Official Journal Of The Association For The Care Of Asthma [serial online]. July 2005;42(6):409-417. Available from: MEDLINE with Full Text, Ipswich, MA. Accessed October 25, 2011.
^ Chohan, A; Lal, A; Chohan, K; Chakravarti, A; Gomber, S (13 July 2015). "Systematic review and meta-analysis of randomized controlled trials on the role of mometasone in adenoid hypertrophy in children.". International journal of pediatric otorhinolaryngology. PMID 26235732.
^ Stjärne, P.; Mösges R; Jorissen M; Passàli D; Bellussi L; Staudinger H; Danzig M. (Feb 2006). A randomized controlled trial of mometasone furoate nasal spray for the treatment of nasal polyposis 132 (2). Arch Otolaryngol Head Neck Surg. pp. 179–185. |accessdate= requires |url= (help)
^ Bousquet, J. (May 2009). Mometasone furoate: an effective anti-inflammatory with a well-defined safety and tolerability profile in the treatment of asthma. 63 (5). Int J Clin Pract. pp. 806–819. |accessdate= requires |url= (help)
^ Product Information: NASONEX(R) nasal spray, mometasone furoate monohydrate nasal spray. Schering Corporation, Kenilworth, NJ, 2010.
^ Publishers, Jones and Bartlett (2009-07-15). Nurse's Drug Handbook 2010. p. 677. ISBN 978-0-7637-7900-9.
^ Mani S. Kavuru (2007). "ch. 9 Anti-inflammatory agents". Diagnosis and Management of Asthma. ISBN 978-1-932610-38-3.
^ Austin RJ, Maschera B, Walker A, Fairbairn L, Meldrum E, Farrow SN et al. (2002). "Mometasone furoate is a less specific glucocorticoid than fluticasone propionate". Eur. Respir. J. 20 (6): 1386–92. PMID 12503693.
^ Walsky, R. L.; Gaman EA; Obach RS. (Jan 2005). "Pharmacokientics, Pharmacodynamics, and Drug Metabolism". Examination of 209 drugs for inhibition of cytochrome P450 2C8. 45 (1) (Pfizer Global Research and Development ed.). USA.: J Clin Pharmacol. pp. 68–78. Retrieved 2012-11-17.
^ Blaiss, MS. (Nov 2011). Safety update regarding intranasal corticosteroids for the treatment of allergic rhinitis. 32 (6). Allergy Asthma Proc. pp. 413–418. |accessdate= requires |url= (help)
^ "Mometamax". Intervet USA. Retrieved 19 June 2010.

External links

Mometasone Furoate Oral Inhalation (MedlinePlus)
Mometasone Furoate Nasal Inhalation (MedlinePlus)
Nasonex Home page
Asmanex Home page
Elica Home page
U.S. National Library of Medicine: Drug Information Portal - Mometasone furoate

UpToDate Contents

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1. 慢性的な手の湿疹 chronic hand eczema
2. 味覚および嗅覚障害の評価および治療 evaluation and treatment of taste and smell disorders
3. 慢性鼻副鼻腔炎のマネージメント management of chronic rhinosinusitis
4. 小児における不眠の問題をもたらす医学的障害 medical disorders resulting in problem sleeplessness in children
5. 吸入ステロイドの主な副作用 major side effects of inhaled glucocorticoids

English Journal

Mometasone furoate hydrogel for scalp use: in vitro and in vivo evaluation.

Salgado A1, Raposo S, Marto J, Silva AN, Simões S, Ribeiro HM.Author information 1Laboratório de Tecnologia Farmacêutica, Faculdade de Farmácia, iMed.UL - Research Institute for Medicines and Pharmaceutical Sciences, Universidade de Lisboa , Lisboa , Portugal.AbstractDermatological inflammatory diseases often affect the scalp and the eyebrows. Common dosage forms available on the market for those situations are lotions; however, the presence of hair limits their use. Gels, for their consistency and adhesiveness, are a suitable alternative to the lotions in these situations. The aim of this study was to develop a new stable gel containing mometasone furoate (MF), with anti-inflammatory activity and a controlled delivery, to improve topical treatment of scalp dermatitis. Pharmaceutical development, physical and chemical characterization, stability, in vitro release and permeation studies and in vivo anti-inflammatory activity were performed. The gel presented an acidic pH and an apparent viscosity of 35 Pa.s. The microbiological analysis showed that the results were within the established specification limits. The release and the permeation profiles suggest that the drug is mainly retained in the upper skin layers. MF gel was tested in an animal model of cutaneous inflammation and presented similar anti-inflammatory activity compared to a commercially available MF dosage form. The gel was chemically, physically and microbiologically stable. The results suggest that the developed hydrogel formulation containing MF can be of actual value for improving the clinical effectiveness in the treatment of scalp dermatitis.
Pharmaceutical development and technology.Pharm Dev Technol.2014 Aug;19(5):618-22. doi: 10.3109/10837450.2013.819012. Epub 2013 Jul 22.
Dermatological inflammatory diseases often affect the scalp and the eyebrows. Common dosage forms available on the market for those situations are lotions; however, the presence of hair limits their use. Gels, for their consistency and adhesiveness, are a suitable alternative to the lotions in these
PMID 23869426

Steroid-eluting sinus implant for in-office treatment of recurrent nasal polyposis: a prospective, multicenter study.

Lavigne F1, Miller SK, Gould AR, Lanier BJ, Romett JL.Author information 1Department of Otolaryngology, Centre hospitalier de l'Université de Montréal (CHUM), Hôpital Notre-Dame, Montréal, Québec, Canada.AbstractBACKGROUND: Treatment options for chronic rhinosinusitis with recurrent polyposis (CRSwNP) after endoscopic sinus surgery (ESS) are limited, and include frequent use of systemic steroids and revision surgery. A bioabsorbable, steroid-eluting implant was studied for its ability to dilate sinuses obstructed by polyps and provide localized, controlled steroid delivery to reestablish sinus patency. This study assessed the initial feasibility, safety, and efficacy of steroid-eluting implants placed in the office setting in patients who were candidates for revision ESS.
International forum of allergy & rhinology.Int Forum Allergy Rhinol.2014 Mar 5. doi: 10.1002/alr.21309. [Epub ahead of print]
BACKGROUND: Treatment options for chronic rhinosinusitis with recurrent polyposis (CRSwNP) after endoscopic sinus surgery (ESS) are limited, and include frequent use of systemic steroids and revision surgery. A bioabsorbable, steroid-eluting implant was studied for its ability to dilate sinuses obst
PMID 24599580

Fluticasone furoate is more effective than mometasone furoate in restoring tobacco smoke inhibited SOCS-3 expression in airway epithelial cells.

Nasreen N1, Gonzalves L2, Peruvemba S1, Mohammed KA3.Author information 1Division of Pulmonary Critical Care & Sleep Medicine, College of Medicine, University of Florida, United States; NF/SGVHS, Malcom Randal VA Medical Center, Gainesville, FL, United States.2Division of Pulmonary Critical Care & Sleep Medicine, College of Medicine, University of Florida, United States.3Division of Pulmonary Critical Care & Sleep Medicine, College of Medicine, University of Florida, United States; NF/SGVHS, Malcom Randal VA Medical Center, Gainesville, FL, United States. Electronic address: mkamal@medicine.ufl.edu.AbstractFluticasone furoate (FF) and mometasone furoate (MF) are potent glucocorticoids recommended for the treatment of allergic rhinitis and other inflammatory diseases. However, whether these drugs render any anti-inflammatory effects in Chronic Obstructive Pulmonary Disease (COPD) is unclear. Emerging data on suppressors of cytokine signaling-3 (SOCS-3) activation in the lungs during inflammation suggests that SOCS3 can be potential targets for regulating pulmonary inflammatory responses in COPD. In this study, we compared the effect of FF with MF on SOCS-3 expression in tobacco smoke (TS) exposed BAEpCs in vitro and in a mouse model of COPD in vivo. BAEpCs were exposed to TS or room air and later were treated with either FF (1nmol-100nmol) or MF (10-500nmol) inhibitors in the presence and absence of Jak1 and Stat-3 inhibitors. C57BL/6 mice were exposed to TS for 6 months, and treated with either FF, MF for 2 and 4 weeks. FF induced 7 fold increases in SOCS-3 expression in BAEpCs whereas MF induced a three fold increase when compared to control. Jak1 and Stat-3 inhibitors significantly inhibited the FF and MF induced SOCS-3 expression in BAEpCs. In addition, FF and MF restored TS inhibited SOCS-3 expression in the airway epithelium of COPD mice. FF and MF treatments significantly reduced leukocyte infiltration in airways and inhibited lung inflammation. Our study elucidates a novel mechanism for the anti-inflammatory action of FF in COPD. The superior efficacy of FF may be in part due to the increased expression of SOCS-3 in BAEpCs.
International immunopharmacology.Int Immunopharmacol.2014 Mar;19(1):153-60. doi: 10.1016/j.intimp.2013.12.029. Epub 2014 Jan 13.
Fluticasone furoate (FF) and mometasone furoate (MF) are potent glucocorticoids recommended for the treatment of allergic rhinitis and other inflammatory diseases. However, whether these drugs render any anti-inflammatory effects in Chronic Obstructive Pulmonary Disease (COPD) is unclear. Emerging d
PMID 24434372

Japanese Journal

薬物小児通年性アレルギー性鼻炎に対するモメタゾンフランカルボン酸エステル水和物点鼻液の多施設共同,二重盲検,無作為化,プラセボ対照試験

岡本美孝,鈴木五男
耳鼻咽喉科臨床 106(11), 1045-1057, 2013-11
NAID 40019845805

P/O-053 Mometasone furoate (MF)による末梢気道炎症抑制効果の検討(成人喘息(治療・管理)1,一般演題,第25回日本アレルギー学会春季臨床大会)

知花和行,塩原太一,武政聡浩,佐藤陽子,新井良,藤松孝旨,渡部峰明,林ゆめ子,石井芳樹,福田健
アレルギー 62(3・4), 400, 2013-04-10
NAID 110009627868

P/O-052 Mometasone Furoate (MF)とSalmeterol/Fluticasone Propionate配合剤(SFC)の気管支拡張効果の比較検討(成人喘息(治療・管理)1,一般演題,第25回日本アレルギー学会春季臨床大会)

杉山公美弥,戸田正夫,武田綾野,舘脇正充,平田博国,原澤寛,福田健
アレルギー 62(3・4), 399, 2013-04-10
NAID 110009627867

「モメタゾン」

Mometasone furoate
Systematic (IUPAC) name
	(11β,16α)-9,21-dichloro-11-hydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl 2-furoate
Clinical data
Trade names	Elocon Elocom, Elomet, Elosalic Novasone Nasonex Asmanex Twisthaler Essex pharma markets the medication under the brand name Ecural mometAid.
AHFS/Drugs.com	monograph
Pregnancy; category	US: C (Risk not ruled out);
Legal status	Rx Only (US);
Routes of; administration	topical, inhalation
Pharmacokinetic data
Bioavailability	Nasal spray is virtually undetectable in plasma; but systemic availability is comparable to fluticasone.
Protein binding	98% to 99%
Metabolism	hepatic
Biological half-life	5.8 hours
Identifiers
CAS Registry Number	105102-22-5 83919-23-7
ATC code	D07AC13 R01AD09, R03BA07
PubChem	CID: 441336
DrugBank	DB00764
ChemSpider	390091
ChEBI	CHEBI:47564
ChEMBL	CHEMBL1161
Synonyms	(9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl furan-2-carboxylate
Chemical data
Formula	C22H28Cl2O4 for Mometasone; C27H30O6Cl2 as Furoate
Molecular mass	427.361 g/mol (Mometasone); 521.4 g/mol (Furoate)
	SMILES O=C(O[C@]2(C(=O)CCl)[C@H](C)C[C@H]3[C@@H]4CCC\1=C\C(=O)\C=C/[C@]/1(C)[C@@]4(Cl)[C@@H](O)C[C@]23C)c5occc5 ;
	InChI InChI=1S/C27H30Cl2O6/c1-15-11-19-18-7-6-16-12-17(30)8-9-24(16,2)26(18,29)21(31)13-25(19,3)27(15,22(32)14-28)35-23(33)20-5-4-10-34-20/h4-5,8-10,12,15,18-19,21,31H,6-7,11,13-14H2,1-3H3/t15-,18+,19+,21+,24+,25+,26+,27+/m1/s1 ; Key:WOFMFGQZHJDGCX-ZULDAHANSA-N ;
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