Mometasone furoate

615.49800

521.43

04201GDN4R

746171

DTXSID4023333

C29268

QS02CA91|R03AK|R03AL

2937229000

113.02000

6.32690

Distributed as 0.1% ointment with a petrolatum base.

1.37 g/cm3

218-220 °C

655.5ºC at 760 mmHg

350.2ºC

1.604

Insoluble

Keep container tightly sealed. Store in cool, dry conditions in well sealed containers.

NONH for all modes of transport

1

WW8223000

Stable if stored as directed.

|Danger|H360 (94.26%): May damage fertility or the unborn child [Danger Reproductive toxicity]|P201, P202, P260, P264, P270, P273, P281, P307+P311, P308+P313, P314, P321, P391, P405, and P501|Aggregated GHS information provided by 122 companies from 11 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

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 treatment. 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.

98% to 99% (in vitro concentration of 5 to 500ng/mL).

There are 3 formulations of mometasone furoate with various indications. The inhaler is indicated for prophylaxis of asthma in patients ≥4 years. The nasal spray is indicated for treating nasal symptoms of allergic rhinitis in patients ≥2 years, treating symptoms of nasal congestion from seasonal allergic rhinitis in patients ≥2 years, treating nasal polyps in patients ≥18 years, and prophylaxis of seasonal allergic rhinitis in patients ≥12 years. The ointment is indicated for symptomatic treatment of dermatitis and pruritis in patients ≥2 years.|FDA Label|For the treatment of acute canine otitis externa or acute exacerbations of recurrent otitis caused by mixed infections of susceptible strains of bacteria sensitive to florfenicol (Staphylococcus pseudintermedius) and fungi sensitive to terbinafine (Malassezia pachydermatis).|Treatment of acute otitis externa and acute exacerbations of recurrent otitis externa, associated with bacteria susceptible to orbifloxacin and fungi susceptible to posaconazole, in particular Malassezia pachydermatis.|Seasonal and perennial allergic rhinitis|Persistent asthma|Bemrist Breezhaler is indicated as a maintenance   treatment of asthma in adults and adolescents 12 years of age and older not adequately controlled with inhaled corticosteroids and inhaled short acting beta2-agonists.|Atectura Breezhaler is indicated as a maintenance treatment of asthma in adults and adolescents 12 years of age and older not adequately controlled with inhaled corticosteroids and inhaled short acting beta2-agonists.|Maintenance treatment of asthma in adults whose disease is not adequately controlled.|Treatment of asthma

Mometasone is a synthetic corticosteroid with an affinity for glucocorticoid receptors 22 times higher than that of [dexamethasone]. Mometasone furoate also has a lower affinity to mineralocorticoid receptors than natural corticosteroids, making it more selective in its action. Mometasone furoate diffuses across cell membranes to activate pathways responsible for reducing inflammation.

Agents that are used to treat allergic reactions. Most of these drugs act by preventing the release of inflammatory mediators or inhibiting the actions of released mediators on their target cells. (From AMA Drug Evaluations Annual, 1994, p475) (See all compounds classified as Anti-Allergic Agents.)|Substances that reduce or suppress INFLAMMATION. (See all compounds classified as Anti-Inflammatory Agents.)|Drugs used to treat or prevent skin disorders or for the routine care of skin. (See all compounds classified as Dermatologic Agents.)

The mean time to peak concentration is 1.0 to 2.5 hours. Bioavailability has been reported as <1% but studies of repeat doses of inhaled corticosteroids suggest a bioavailability of 11%. The 0.1% ointment may have a bioavailability of 0.7%.|For an inhaled dose, approximately 74% is excreted in the feces and 8% is excreted in the urine.|Steady state volume of distribution of 152L.|The clearance rate of mometasone furoate is not readily available, though it may be close to 90L/h.

Metabolism of mometasone furoate is largely performed hepatically by cytochrome P450 3A4 producing a number of metabolites. Some of these metabolites include free mometasone and 6-beta-hydroxy-mometasone furoate.

The terminal half life of an inhaled dose is approximately 5 hours though it has been reported as 5.8 hours by other sources.

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

Asmanex

Veterinary drugs -> Neptra -> EMA Drug Category|Otologicals, Corticosteroids and antiinfectives in combination -> Veterinary pharmacotherapeutic group|Veterinary drugs -> Posatex -> EMA Drug Category|Otologicals -> Veterinary pharmacotherapeutic group|Human Drugs -> EU pediatric investigation plans|Human drugs -> Bemrist Breezhaler -> EMA Drug Category|Drugs for obstructive airway diseases -> Human pharmacotherapeutic group|Human drugs -> Atectura Breezhaler -> EMA Drug Category|Human drugs -> Zimbus Breezhaler -> EMA Drug Category|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients