|Systematic (IUPAC) name|
|Trade names||Asmanex Twisthaler, Ecural mometAid, Elocon, Elocom, Elomet, Elosalic, Nasonex, Novasone|
|Bioavailability||Nasal spray is virtually undetectable in plasma; but systemic availability is comparable to fluticasone|
|Protein binding||98% to 99%|
|Biological half-life||5.8 hours|
|CAS Number||105102-22-5 83919-23-7|
|ATC code||D07AC13 (WHO) R01AD09 (WHO), R03BA07 (WHO)|
|Formula||C22H28Cl2O4 for Mometasone
C27H30O6Cl2 as Furoate
|Molar mass||427.361 g/mol (Mometasone)
521.4 g/mol (Furoate)
|(what is this?)|
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.
Mometasone is indicated for the alleviation of inflammatory and pruritic manifestations (with stinging and itching) of dermatosis which respond to treatment with glucocorticoids 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 hay fever (seasonal allergic rhinitis) and other allergies (perennial rhinitis), including nasal congestion, discharge, pruritus, and sneezing. It 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 patients over the age of 18. It can also produce nasal drip, a sensation of tickling in the throat, and loss of the sense of taste and smell.
The furoate of mometasone can be used with formoterol for the treatment of asthma, due to its anti-inflammatory properties.
- 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 (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.
Extensive metabolic hepatic metabolism 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 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.
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