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 by decreasing the liberation of
hydrolase acids of
leukocytes, the prevention of the accumulation of
macrophages in the sites of inflammation, the interference with the 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 is also reduced. It is believed that the action of corticosteroid anti-inflammatory agents is 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 the skin reduces the inflammation associated with chronic or acute dermatosis. Although mometasone furoate does not have significant systemic immunomodulatory effects, it can be considered a local immunosuppressive drug because clinical studies have shown reductions (vs. baseline ) in neutrophils (a white blood cell) in the nasal mucosa. It could be also considered an antihistamine along with its glucocorticoid effects because it significantly reduces histamine and eosinophil cationic protein levels.
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 6β-hydroxymometasone. In human hepatic microsomes, the formation of these metabolites is regulated by
CYP3A4. The C17α
furoate ester of mometasone, is the marketed medication. In addition to its glucocorticoid activity, mometasone also has very potent
progestogenic activity and acts as a
partial agonist of the
mineralocorticoid receptor. ==Society and culture==