Mometasone furoate

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Mometasone furoate
Mometasone furoate.png
Mometasone furoate ball-and-stick.png
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 namesElocon Elocom, Elomet, Elosalic Novasone Nasonex Asmanex Twisthaler Essex pharma markets the medication under the brand name Ecural mometAid.
AHFS/Drugs.commonograph
Pregnancy cat.C (US)
Legal statusRx Only (US)
Routestopical, inhalation
Pharmacokinetic data
BioavailabilityNasal spray is virtually undetectable in plasma; but systemic availability is comparable to fluticasone.[1]
Protein binding98% to 99%
Metabolismhepatic
Half-life5.8 hours
Identifiers
CAS number105102-22-5 YesY 83919-23-7
ATC codeD07AC13 R01AD09, R03BA07
PubChemCID 441336
DrugBankDB00764
ChemSpider390091 YesY
ChEBICHEBI:47564 YesY
ChEMBLCHEMBL1161 YesY
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
FormulaC22H28Cl2O4 for Mometasone
C27H30O6Cl2 as Furoate
Mol. mass427.361 g/mol (Mometasone)
521.4 g/mol (Furoate)
 N (what is this?)  (verify)
 
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Mometasone furoate
Mometasone furoate.png
Mometasone furoate ball-and-stick.png
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 namesElocon Elocom, Elomet, Elosalic Novasone Nasonex Asmanex Twisthaler Essex pharma markets the medication under the brand name Ecural mometAid.
AHFS/Drugs.commonograph
Pregnancy cat.C (US)
Legal statusRx Only (US)
Routestopical, inhalation
Pharmacokinetic data
BioavailabilityNasal spray is virtually undetectable in plasma; but systemic availability is comparable to fluticasone.[1]
Protein binding98% to 99%
Metabolismhepatic
Half-life5.8 hours
Identifiers
CAS number105102-22-5 YesY 83919-23-7
ATC codeD07AC13 R01AD09, R03BA07
PubChemCID 441336
DrugBankDB00764
ChemSpider390091 YesY
ChEBICHEBI:47564 YesY
ChEMBLCHEMBL1161 YesY
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
FormulaC22H28Cl2O4 for Mometasone
C27H30O6Cl2 as Furoate
Mol. mass427.361 g/mol (Mometasone)
521.4 g/mol (Furoate)
 N (what is this?)  (verify)

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, administration, and pharmacodynamics[edit]

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]

It reduces inflammation by causing several effects:[6][7][8]

The exact anti-inflammatory mechanism of action is unknown.

Availability[edit]

Merck markets the medication under the following brand names; Elocon (Elocom, Elomet, Elosalic) and Novasone as a cream or ointment for skin conditions, Nasonex as a nasal spray for upper respiratory conditions such as nasal sinus inflammation, Asmanex Twisthaler as a dry powder inhaler (DPI) for lower respiratory conditions. Essex pharma markets the medication under the brand name Ecural and Progreś Laboratories markets it under mometAid. It is also marketed by Perrigo as an ointment for the scalp.In India it is marketed by Intas under the trade name 'Eziwin'.

It is also available as a veterinary drug in an otic (ears) form for treatment of otitis externa under the brand name Mometamax.[9]

References[edit]

  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ Khope S (March 2010). "Topical mometasone furoate for phimosis". Indian pediatr 47 (3): 282. PMID 20371899. 
  5. ^ 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.
  6. ^ Product Information: NASONEX(R) nasal spray, mometasone furoate monohydrate nasal spray. Schering Corporation, Kenilworth, NJ, 2010.
  7. ^ Publishers, Jones and Bartlett (2009-07-15). Nurse's Drug Handbook 2010. p. 677. ISBN 978-0-7637-7900-9 
  8. ^ Mani S. Kavuru (2007). "ch. 9 Anti-inflammatory agents". Diagnosis and Management of Asthma. ISBN 978-1-932610-38-3 
  9. ^ "Mometamax". Intervet USA. Retrieved 19 June 2010. 

External links[edit]