NASONEX

NASONEX - Names and Identifiers

Name	MometasoneFuroate
Synonyms	NASONEX SCH-32088 MometasoneFuroate Mometasone furoate MOMETASONE FUROATE MOMETASONE 17-FUROATE (11-beta,16-alpha)-xy-16-methyl pregna-1,4-diene-3,20-dione,9,21-dichloro-17-((2-furanylcarbonyl)oxy)-11-hydro (11BETA,16ALPHA)-9,21-DICHLORO-17-[(2-FURANYLCARBONYL)OXY]-11-HYDROXY-16-METHYLPREGNA-1,4-DIENE-3,20-DIONE (8xi,11beta,14xi,16alpha)-9,21-dichloro-11-hydroxy-16-methyl-3,20-dioxopregna-1,4-dien-17-yl furan-2-carboxylate 9-chloro-17-(2-chloroacetyl)-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one furoate 9-Chloro-17-(2-chloroacetyl)-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one furoate
CAS	83919-23-7
EINECS	617-501-0
InChI	InChI=1/C27H30Cl2O6/c1-15-11-19-18-7-6-16-12-17(30)8-9-24(16,2)26(18,29)21(31)13-25(19,3)27(15,22(32)14-28)35-23(33)20-5-4-10-34-20/h4-5,8-10,12,15,18-19,21,31H,6-7,11,13-14H2,1-3H3/t15-,18?,19?,21+,24+,25+,26+,27+/m1/s1
InChIKey	WOFMFGQZHJDGCX-ZULDAHANSA-N

NASONEX - Physico-chemical Properties

Molecular Formula	C27H30Cl2O6
Molar Mass	521.43
Density	1.37±0.1 g/cm3(Predicted)
Melting Point	218-220°C
Boling Point	655.5±55.0 °C(Predicted)
Specific Rotation(α)	D26 +58.3° (dioxane)
Flash Point	350.233°C
Solubility	DMSO: ≥20mg/mL
Vapor Presure	0mmHg at 25°C
Appearance	White powder
Color	white to off-white
pKa	13.02±0.70(Predicted)
Storage Condition	2-8°C
Refractive Index	1.604
MDL	MFCD00866003
Physical and Chemical Properties	Crystallized from aqueous methanol, melting point 218-220 °c. [Α] D20 58.3 ° (dioxane). UV absorption maximum (methanol):247nm (λ 26300).
Use	Mometasone furoate is a corticosteroid drug that can be used for the treatment of asthma, rhinitis, and certain skin conditions. It has a glucocorticoid receptor binding affinity 22 times stronger than dexamethasone and higher than many other corticosteroids as well. Mometasone furoate is formulated as a dry powder inhaler, nasal spray, and ointment for its different indications

NASONEX - Risk and Safety

WGK Germany	3
HS Code	29372290

NASONEX - Indication

Inhaled mometasone furoate is indicated for prophylaxis of asthma in patients ≥4 years. Applied topically as an ointment, mometasone furoate is indicated for symptomatic treatment of dermatitis and pruritis in patients ≥2 years.

Mometasone furoate nasal spray is available both over-the-counter (OTC) and by prescription. The OTC nasal spray formulation of mometasone furoate is indicated for the treatment of upper respiratory allergic symptoms (e.g. rhinorrhea, sneezing) in patients ≥2 years of age. The prescription formulation is indicated for the treatment of chronic rhinosinusitis with nasal polyps in patients ≥18 year old and for the and prophylaxis of seasonal allergic rhinitis in patients ≥12 years old. It is also approved in combination with olopatadine for the symptomatic treatment of seasonal allergic rhinitis in patients ≥12 years.

Last Update：2024-01-02 23:10:35

NASONEX - Mechanism of action

In asthma, mometasone is believed to inhibit mast cells, eosinophils, basophils, and lymphocytes3. There is also evidence of inhibition of histamine, leukotrienes, and cytokines3.

Corticosteroids diffuse across cell membranes into the cytosol of cells where they bind to glucocorticoid receptors to produce their activity. Mometasone furoate has a particularly high receptor affinity compare to other corticosteroids, 22 times higher than that of dexamethasone. Mometasone furoate binding to a glucocorticoid receptor causes conformational changes in the receptor, separation from chaperones, and the receptor moves to the nucleus. Once at the nucleus, receptors dimerize and bind to a DNA sequence known as the glucocorticoid response element which either increases expression of anti-inflammatory molecules or inhibits expression of pro-inflammatory molecules (such as interleukins 4 and 5). Mometasone furoate also reduces inflammation by blocking transcription factors such as activator-protein-1 and nuclear factor kappa B (NF-kappaB)

Last Update：2023-08-16 23:22:23

NASONEX - Toxicity

Overdose with a mometasone furoate inhaler may occur with chronic overuse. Symptoms of chronic overuse may present as hypercorticism and adrenal suppression, and patients may not require any more treatment than monitoring

In animal studies of pregnancy, some fetal toxic effects were seen at or above the maximum recommended human dose, though rodents are more sensitive to these effects than humans. The benefits and risks of use should be considered in pregnant patients

It is unknown if mometasone furoate is excreted in breast milk but other corticosteroids are and therefore caution should be exercised when administering to nursing mothers

Safety and effectiveness in pediatric populations has been established through clinical trials, though there may be a reduction in expected growth of about 1cm per year depending on the dose and duration of treatmentLabel. Pediatric patients should be titrated to the lowest effective dose for mometasone furoate inhalers

A trial of geriatric patients showed no difference in safety or efficacy compared to younger patients, however patients of an even greater age may still be more sensitive to mometasone furoate

The use of a mometasone furoate inhaler in moderate or severe hepatic impairment rarely leads to detectable plasma concentrations though caution may be prudent with increasing degrees of severity

The effects of mometasone furoate in renal impairment, and across gender and race have not been studied

Last Update：2023-08-16 23:22:23