Mometasone furoate is the furoate ester form of mometasone (a topical synthetic glucocorticoid receptor agonist).
Mometasone furoate is the furoate
ester form of mometasone (a topical synthetic glucocorticoid receptor agonist).[1]
With anti-pruritic, anti-inflammatory, and vasoconstrictive properties, it
is utilized to manage asthma, rhinitis, and certain skin conditions. It is
formulated as a nasal spray, dry powder inhaler, and ointment for its distinct
indications. [1,2]
Pharmacological Class: Corticosteroids
Mometasone furoate has a stronger glucocorticoid receptor
binding affinity that is 22 times greater than dexamethasone and much greater
when compared with numerous other corticosteroids. It diffuses across cell
membranes and activates pathways which are responsible for reducing inflammation.
Upon administration, this corticosteroid binds to
cytoplasmic glucocorticoid receptors and consequently activates glucocorticoid
receptor-mediated gene expression. This stimulates phospholipase A2 inhibitory
proteins, which in turn controls the release of the inflammatory precursor
arachidonic acid from the phospholipid membrane via phospholipase A2.
It also alleviates inflammation by inhibiting release of
transcription factors like nuclear factor kappa B (NF-kappaB) and
activator-protein-1 and. In asthma, mometasone is thought to suppress
lymphocytes, basophils, mast cells, and eosinophils. Evidence also indicates
inhibition of cytokines, histamine, and leukotrienes. [1,2]
Absorption
The mean time to peak concentration is about 1.0 to 2.5 hours. The bio-availability has been noted to be as <1%. Repeated dose of inhaled corticosteroids shows a bio-availability of 11% in some studies. Therefore, the 0.1% ointment may have a bio-availability of 0.7%.
Volume of distribution
The steady-state volume of distribution is 152 L.
Protein binding
The protein binding is about 98-99% (in vitro concentration
of 5 to 500ng/mL).
Metabolism
Mometasone furoate is metabolised hepatically by cytochrome
P450 3A4 generating numerous metabolites such as 6-beta-hydroxy-mometasone
furoate and free mometasone.
Route of elimination
About 74% is eliminated in the faeces for an inhaled dose,
and 8% is eliminated in the urine.
Half-life
The terminal half-life of an inhaled dose is about five
hours though it has been reported as 5.8 hours by other sources.
Clearance
The clearance rate of mometasone furoate is not readily
available. However, it may be close to 90 L/h. [2]
It is contraindicated:
Concomitant use of mometasone and strong cytochrome P450 3A4
inhibitors (such as ritonavir, telithromycin, atazanavir, nelfinavir,
clarithromycin, indinavir, saquinavir, itraconazole, and nefazodone) should be
avoided, as it may suppress the metabolism and systemic exposure leading to
increased systemic corticosteroid adverse effects.[6]
(a) For cream:
Mometasone furoate may cause the below adverse effects:
(b) For nasal spray:
The most commonly occurring adverse reactions (≥5%) include:
(c) For Inhalation Aerosol:
The most commonly adverse reactions determined in ≥ 3% of patients included:
(a) For Cream
(b) For Nasal spray
(c) Inhalation Aerosol
(a) Mometasone furoate for management of dermatitis and
other skin diseases
Compared to the control cream, 0.1% mometasone furoate cream
was found to prevent the occurrence of moderate-to-severe acute radiation
dermatitis in 124 breast cancer people receiving postmastectomy radiation in a double-blinded
randomized trial.[8] A review by Fabrizio Spada et al. reported
higher efficacy of mometasone furoate with a low risk of both local and
systemic side effects for combating eczema, psoriasis, and seborrhoeic
dermatitis.[9]
The local application of mometasone furoate was reported to
prevent acute radiation dermatitis in people with head and neck squamous cell
carcinomas in a randomized, self-controlled, prospective analysis. [10]
(b) Mometasone furoate for management of rhinitis
A systematic review by Desiderio Passali et al. demonstrated
that mometasone furoate nasal spray effectively combat inflammatory diseases of
the nose, seasonal and perennial allergic rhinitis, paranasal sinuses, and
rhinosinusitis. [11] In a randomized, prospective, double-blinded,
placebo-controlled trial of 64 patients, Mometasone furoate -impregnated
biodegradable nasal dressings improve the endoscopic appearance in the healing
process of chronic rhinosinusitis with nasal polyps after endoscopic sinus
surgery. [12]
(c) Mometasone furoate for management of asthma
In a 12-week, placebo-controlled, double-blind, double-dummy
trial, all the three doses of mometasone furoate (50, 100, and 200 mcg two
times a day) were well-tolerated and found to substantially improve forced
expiratory volume in one second (FEV1) after 12 weeks of therapy in children
aged 5-11 years suffering from persistent asthma.[13]
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