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Mometasone, also known as mometasone y 3 s, is a
steroid A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes that alter membrane fluidity; and ...
medication used to treat certain skin conditions, hay fever, and asthma. Specifically it is used to prevent rather than treat asthma attacks. It can be applied to the skin, inhaled, or used in the nose. Mometasone furoate, not mometasone, is used in medical products. Common side effects when used for asthma includes asthma and
thrush ''The Man from U.N.C.L.E.'' is an American spy fiction television series produced by Metro-Goldwyn-Mayer Television and first broadcast on NBC. The series follows secret agents, played by Robert Vaughn and David McCallum, who work for a secret ...
. It is therefore recommended to rinse the mouth after use. Long term use may increase the risk for
glaucoma Glaucoma is a group of eye diseases that result in damage to the optic nerve (or retina) and cause vision loss. The most common type is open-angle (wide angle, chronic simple) glaucoma, in which the drainage angle for fluid within the eye re ...
and cataracts. Common side effects when used in the nose includes upper respiratory tract infections and nose bleeds. Common side effects when applied on the skin include acne,
skin atrophy Atrophoderma refers to conditions involving skin atrophy. Types include: * Follicular atrophoderma * Linear atrophoderma of Moulin * Atrophoderma of Pasini and Pierini Morphea is a form of scleroderma that involves isolated patches of hard ...
, and itchiness. It works by decreasing
inflammation Inflammation (from la, wikt:en:inflammatio#Latin, inflammatio) is part of the complex biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or Irritation, irritants, and is a protective response involving im ...
. Mometasone furoate was patented in 1981 and came into medical use in 1987. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication. In 2020, it was the 231st most commonly prescribed medication in the United States, with more than 1million prescriptions.


Medical uses

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 Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones. Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are in ...
, and penile phimosis. In terms of steroid strength, it is more potent than hydrocortisone, and less potent than dexamethasone. Some low-quality evidence suggests the use of mometasone for symptomatic improvement in children with adenoid hypertrophy. Mometasone is used to alleviate inflammation and itchiness in skin conditions that respond to treatment with glucocorticoids such as psoriasis and atopic dermatitis.
Nasal Nasal is an adjective referring to the nose, part of human or animal anatomy. It may also be shorthand for the following uses in combination: * With reference to the human nose: ** Nasal administration, a method of pharmaceutical drug delivery ** ...
mometasone is used in adults (including the elderly) and children over two years of age, to diminish the symptoms of hay fever (seasonal allergic rhinitis) and other allergies (perennial rhinitis), including nasal congestion, discharge, pruritus, and sneezing and to treat nasal polyps. It is not useful for the common cold.


Asthma

Mometasone furoate can be used with formoterol for the treatment of asthma, due to its anti-inflammatory properties.


Contraindications

People should not use inhaled mometasone or mometasone nasal spray if: * glaucoma or cataracts * hypersensitivity or allergic to any ingredient in mometasone Those who are using mometasone nasal or inhaled for a long period of time (e.g. more than three months) should get regular eye exams to check for
glaucoma Glaucoma is a group of eye diseases that result in damage to the optic nerve (or retina) and cause vision loss. The most common type is open-angle (wide angle, chronic simple) glaucoma, in which the drainage angle for fluid within the eye re ...
and cataracts and should take precautions to avoid infections such as taking a vitamin D supplement, staying away from those with an infection (chickenpox, measles, colds or flu, COVID-19), washing foods, hand washing and calling a family doctor at the first sign of a severe infection. People should not use mometasone topical (skin cream) if: * hypersensitive or allergic to any ingredient in the skin cream Mometasone furoate is in class C in terms of safety while use during
pregnancy Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ...
. Therefore, its risks to the baby cannot be ruled out. Therefore, the use in pregnancy is not recommended.


Side effects

The nasal spray form of mometasone may cause the following
side effect In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...
s: * headache *
Viral Viral means "relating to viruses" (small infectious agents). Viral may also refer to: Viral behavior, or virality Memetic behavior likened that of a virus, for example: * Viral marketing, the use of existing social networks to spread a marke ...
upper respiratory infections * sore throat * nose bleeds * cough * muscle and joint pain Serious side effects include:
Thrush ''The Man from U.N.C.L.E.'' is an American spy fiction television series produced by Metro-Goldwyn-Mayer Television and first broadcast on NBC. The series follows secret agents, played by Robert Vaughn and David McCallum, who work for a secret ...
(fungal infection in the nose or throat), slow wound healing, eye problems such as glaucoma or cataracts, weakened immune system (
immunodeficiency Immunodeficiency, also known as immunocompromisation, is a state in which the immune system's ability to fight infectious diseases and cancer is compromised or entirely absent. Most cases are acquired ("secondary") due to extrinsic factors that a ...
) which causes an increased susceptibility to infections and adrenal insufficiency. The inhaled form of mometasone for asthma may cause the following side effects * headache * stuffy or runny nose * dry throat * swelling of nose, throat and sinuses *
flu like symptoms Influenza-like illness (ILI), also known as flu-like syndrome or flu-like symptoms, is a medical diagnosis of possible influenza or other illness causing a set of common symptoms. These include fever, shivering, chills, malaise, dry cough, lo ...
* painful menstrual periods Serious side effects may include: allergic reactions (
anaphylaxis Anaphylaxis is a serious, potentially fatal allergic reaction and medical emergency that is rapid in onset and requires immediate medical attention regardless of use of emergency medication on site. It typically causes more than one of the follo ...
), increased risk of osteoporosis, glaucoma and cataracts, thrush in the mouth or throat, growth retardation in children, bronchospasms, adrenal insufficiency and weakened immune system which causes an increased susceptibility to infections. The topical (skin cream) version may cause: * burning and itching at the application site * acne * changes in skin color * dryness at application site * skin sores The only serious side effect that is known with mometasone topical is adrenal insufficiency.


Pharmacology


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 Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every verte ...
properties of mometasone furoate, it is a very potent agonist of the
progesterone receptor The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found inside cells. It is activated by the steroid hormone progesterone. In humans, PR is encoded by a single ''PGR'' gene res ...
as well as a
partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonist ...
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 in decreasing the liberation of
hydrolase Hydrolase is a class of enzyme that commonly perform as biochemical catalysts that use water to break a chemical bond, which typically results in dividing a larger molecule into smaller molecules. Some common examples of hydrolase enzymes are es ...
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 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
prostaglandin The prostaglandins (PG) are a group of physiologically active lipid compounds called eicosanoids having diverse hormone-like effects in animals. Prostaglandins have been found in almost every tissue in humans and other animals. They are der ...
s 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. 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.


Mometasone

Mometasone by itself is a
synthetic Synthetic things are composed of multiple parts, often with the implication that they are artificial. In particular, 'synthetic' may refer to: Science * Synthetic chemical or compound, produced by the process of chemical synthesis * Synthetic o ...
,
steroid A steroid is a biologically active organic compound with four rings arranged in a specific molecular configuration. Steroids have two principal biological functions: as important components of cell membranes that alter membrane fluidity; and ...
al
glucocorticoid Glucocorticoids (or, less commonly, glucocorticosteroids) are a class of corticosteroids, which are a class of steroid hormones. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every verte ...
or
corticosteroid Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones. Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are in ...
that was never marketed. The C17α furoate
ester In chemistry, an ester is a compound derived from an oxoacid (organic or inorganic) in which at least one hydroxyl group () is replaced by an alkoxy group (), as in the substitution reaction of a carboxylic acid and an alcohol. Glycerides ...
of mometasone, is the marketed medication. Mometasone furoate acts as a prodrug of mometasone. In addition to its glucocorticoid activity, mometasone also has very potent progestogenic activity and acts as a
partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonist ...
of the mineralocorticoid receptor.


Society and culture


Brand names

As of 2016 mometasone furoate was available worldwide in formulations for nasal, oral inhalation, and topical administration, for human and for veterinary use, and in combinations with other drugs, under many brand names. It was available as the single active agent in the following brands: Alcom, Altosone, Asmanex, Atozon, Aureox, Belloseta, Bioelementa, Biometasona, Bloctimo, Borgasone, Breso, Broner, Codermo, Cortynase, Cutimom, Cutizone, Cutticom, Dance, Demoson, Dergentil, Derimod, Dermacortine, Dermaten, Dermome, Dermosona, Dermotasone, Dermovel, Desdek, Ecelecort, Ecural, Edelan, Elica, Elisone, Elisox, Elitasone, Elna, Elocan, Elocom, Elocon, Elocortin, Elofute, Elomet, Elomox, Eloskin, Eloson, Elosone, Elovent, Elox, Etacid, Eversone, Eztom, F-Din, Fenisona, Flazcort, Flogocort, Fremomet, Frondava, Fu Mei Song, Fulmeta, Furo, Furoato de Mometasona, Furoderm, Gistan-H, Honmet, Iflacort, Intercon, Ivoxel, Kalmente, Konex, Ladexol, Lisoder, Logren, Loksin, Lomeane, M-Furo, Makiren, Mefurosan, Melocort, Mena, Mesone, Metacortil, Metactiv, Metaflam, Metagra, Metasafe, Metason, Metasone, Metaspray, Metatop, Metaz, Metmin, Metsone, Midermin, Mifusin, Minyear, Mofacort, Mofulex, Mofur, Mofuroate, Molison, Momate, Momax, Momecon, Momecort, Momecutan, Momederm, MomeGalen, Momegen, Momekort, Momelab, Momentum, Momeplus, Momerid, Momeson, Momesone, Momester, Momet, Mometa, Mometagen, Mometason, Mometasona, Mometasona Furoato, Mometasone Furoate, Mometasone Furoate Hydrate, Mometasonfuroaat, Mometasonfuroat, Mometasoni Furoas, Mometasonum, Mometasyn, Mometasyn, Mometax, Mometazon, Mometazona, Mometazona Fuorat, Mometazonfuroat, Mometix-AQ, Momevate, Momexa, Mommex, Mommox, Momtas, Monaliz, Monez, Monovel, Monovo, Mosone, Motaderm, Motaneal, Movesan, Mtaz, Mundoson, Murozo, Myrey, Narinex, Nasamet, Nasehaler, Nasocure, Nasomet, Nasometin, Nasonex, Nassomet, Nazofix, Nazoster, Netonox, Nexomist, Novasone, Ovison, Ovixan, Oximax, Pharmecort, Pluster, Pronasal, Propel, Prospiril, Pydercon, Rinelon, Rinitek, Rino-Val, Rinobudex, Rinonex, Rinosal, Rinosona, Rinoval, Risonel, Rinocort, Sensicort, Septopic, Silkaren, Soneta, Suavicort, Suqi, Synaller, Tabunex, Topcort, Topison, Uniclar, Uniderm, Vizomet, Yperod, Zalconex, and Zynovate.


Combinations

The following combination drugs are available as of 2022: * Mometasone and azelastine as Nasaflex * Mometasone and clotrimazole and gentamicin for veterinary use as Mometamax and Mometavet * Mometasone and clotrimazole and mupirocin as Derma Q * Mometasone and florfenicol and
terbinafine Terbinafine, sold under the brand name Lamisil among others, is an antifungal medication used to treat pityriasis versicolor, fungal nail infections, and ringworm including jock itch and athlete's foot. It is either taken by mouth or appli ...
for veterinary use as Claro * Mometasone and formoterol as Dulera, Hexaler Bronquial Duo, and Zenhale * Mometasone and fusidic acid as Bactirest-M, Dermotil Fusid, and Momate-F * Mometasone and gentamicin and posaconazole for veterinary use as Mometamax Ultra * Mometasone and hydroquinone and tretinoin as Acnezac-MH * Mometasone and miconazole as Elica M, Elica-M, and Sensicort-F * Mometasone and mupirocin as Sensicort-B * Mometasone and
orbifloxacin Orbifloxacin (brand name Orbax) is a fluoroquinolone antibiotic which is approved for use in dogs, marketed by Schering-Plough Animal Health. See also * Quinolone Quinolone may refer to: * 2-Quinolone * 4-Quinolone * Quinolone antibiotic ...
and posaconazole for veterinary use as Posatex, Posatex voor honden, and Posatex für Hunde * Mometasone and salicylic acid as Cortimax-S, Elicasal, Elocom Plus, Elosalic, Mezo-S, Momate-S, Momesalic, Momtas-S, Monsalic, and Sensicort-S * Mometasone and
terbinafine Terbinafine, sold under the brand name Lamisil among others, is an antifungal medication used to treat pityriasis versicolor, fungal nail infections, and ringworm including jock itch and athlete's foot. It is either taken by mouth or appli ...
as Cutizone-T, Mezo-T, and MomelomTerbi-Humanity * Mometasone and tiotropium as Tiomom


References


External links

* {{Portal bar , Medicine Antiasthmatic drugs Corticosteroid esters 2-Furyl compounds Glucocorticoids Mineralocorticoids Organochlorides Pregnanes Progestogens Schering-Plough brands Merck & Co. brands Wikipedia medicine articles ready to translate Combination drugs