What Is Mometasone Furoate Cream?

Mometasone white to off-white crystalline powder, molecular formula is C27H30Cl2O6, molecular weight is 521.242900, density is 1.35g / cm3, melting point is 220ºC (decomposes), boiling point is 586.6ºC at 760mmHg, flash point is 308.5ºC, refractive index is 1.603 The vapor pressure is 4.47E-18mmHg at 25 ° C.

Chinese name: Momisson
Foreign name: mometasone

CAS number: 105102-22-5
Molecular formula: C27H30Cl2O6

Introduction to mometasone compounds

Momisson Basic Information

Chinese name

Chinese alias: Mometasone furoate impurity G; Mometasone; Mometasone; 9,21-bischloro-11beta, 17alpha-bishydroxy-16alpha-methylpregnant-1,4-diene-3 20-dione;

English name: mometasone

English alias: Pregna-1,4-diene-3,20-dione, 9,21-dichloro-11,17-dihydroxy-16-methyl-, (11b, 16a)-(9CI); Mometasone; 9a, 21- dichloro-11b, 17-dihydroxy-16a-methylpregna-1,4-diene-3,20-dione; MOMETOSONE FUROATE;

CAS number: 105102-22-5

Molecular formula: C ₂₇ H ₃₀ Cl ₂ O ₆

Molecular weight: 521.442900

Structural formula:

Exact mass: 520.14200

PSA: 93.81000

LogP: 4.86920 ^[1]

Physical properties of mometasone

Appearance and properties: white to off-white crystalline powder

Density: 1.35g / cm ³

Melting point: 220ºC (decomposes)

Boiling point: 586.6ºC at 760mmHg

Flash point: 308.5ºC

Refractive index: 1.603

Vapor pressure: 4.47E-18mmHg at 25 ° C ^[1]

Mometasone pharmacological effects:

1. Anti-inflammatory activity: Glucocorticoids can reduce the production, release, and activity of inflammatory mediators (such as kallikrein, histamine, liposome enzymes, prostaglandins, leukotrienes), thereby improving the initial clinical symptoms of the inflammatory process. It can inhibit leukocyte attachment and cell migration, and can also reverse vascular dilatation and increase in vascular permeability in local areas, thereby reducing the aggregation of cells in inflammatory sites and reducing the exudation of serum.

2. Immunosuppression: Glucocorticoids can reduce the body's response to immune complexes and delayed hypersensitivity reactions. This is because it can inhibit the toxic effect of the antigen-antibody complex of skin allergic vasculitis precipitated on the blood vessel wall, and inhibit the effects of lymphokines, target cells and macrophages that produce contact dermatitis. In addition, glucocorticoids can also inhibit the production of T lymphocytes and macrophages sensitized by target cells.

3. Anti-proliferative effect: can reduce the formation of proliferative tissues characteristic of psoriasis. Mometasone is a strong local corticosteroid. With the effect of hydrocortisone, stronger than fluocinolone and triamcinolone. Can be absorbed from normal non-damaged skin. ^[2]

Mometasone Pharmacokinetics

For local application, the onset time of allergic or idiopathic dermatitis is 3 to 21 days, and psoriasis is 3 days. Bioavailability is 0.7%. At the same time, the use of closed dressings or for inflamed skin can increase percutaneous absorption. The absorption varies greatly between individuals and anatomical parts. Forearm 1%, scalp 4%, forehead 7%, scrotum 36%, penetrability The best areas are in the groin, armpits and face. After transdermal absorption, it is mainly excreted by the kidneys, and a small amount is secreted into the bile. Nasal spray, the onset of allergic rhinitis is 2 days. Nasal spray administration is almost undetectable in plasma. After administration, drugs that are swallowed and absorbed are extensively metabolized into several metabolites in the liver. Most are cleared from the bile, and a small amount is cleared from the urine as metabolites. The elimination half-life of the parent drug is 5.8h. ^[2]

Mometasone indication

Mometasone creams and ointments are suitable for skin diseases that are effective for topical treatment of glucocorticoids, such as contact dermatitis, atopic dermatitis, eczema, neurodermatitis, and itchy and non-infectious inflammatory skin diseases such as psoriasis; Nasal aerosols are used to treat seasonal or perennial allergic rhinitis. It is used to relieve inflammation and pruritus of skin diseases that can be treated with corticosteroids. ^[2]

Mometasone dosage

1. (1) Topical application: Apply evenly to the affected area once a day for 3 weeks or until symptoms disappear; (2) Nasal administration: use a nasal aerosol.

2. Children: (1) Nasal administration: For the treatment of seasonal and perennial allergic rhinitis: For patients 12 years of age and older, the usual dose is once a day, each time sprayed twice on each nostril (50 g each) ); The recommended dose for children aged 3 to 11 years is once a day, one spray per nostril; for children younger than 3 years, the effectiveness and safety of Mometasone nasal spray is not clear; (2) Topical: For children 6 to 12 years of age with atopic dermatitis, treatment with 0.1% mometasone furoate for 6 weeks is effective in reducing symptoms without causing adrenal suppression or skin atrophy. ^[2]

Mometasone adverse reactions

Occasionally irritating reactions such as burning, itching, tingling. Long-term topical application can cause skin atrophy, telangiectasia, acne-like dermatitis, perioral dermatitis, and increased susceptibility to infection. High-dose applications can produce symptoms such as hyperglycemia, hypertension, and Cushing's syndrome, which should be reduced. ^[2]

Mometasone contraindications

Those who are allergic to mometasone or other glucocorticoids are contraindicated. ^[2]

Momisson notes

1. (1) tuberculosis; (2) untreated fungal, bacterial or systemic viral infections. (3) Herpes simplex on the eye; (4) Avoid use before nasal surgery, nasal trauma, or ulcers are cured; (5) pregnant women; (6) lactating women; (7) children.

2. Not for use on the eyes.

3. Avoid bandaging or large area use.

4. For patients with moderate to severe seasonal allergic rhinitis, it is recommended to use mometasone nasal aerosol for preventive treatment 2 to 4 weeks before the beginning of the pollen season. Shake the container thoroughly before each application.

5. For local infections involving the nasal mucosa, mometasone should not be used without treatment. If accompanied by a skin infection, anti-infective drugs must be used simultaneously. If clinical symptoms do not improve in time, mometasone should be stopped until the infection is under control.

6. If irritation or allergic reactions occur during use, medication should be stopped and treated appropriately.

7. Because glucocorticoids have the effect of inhibiting wounds, for patients who have recently undergone nasal surgery or suffered trauma, nasal medication should not be used until the wound has healed.

8. Patients who use mometasone nasal aerosol for several months or longer should regularly check the nasal mucosa. If local fungal infection occurs in the nasopharynx, the drug should be discontinued or appropriate treatment should be given. Persistent nasopharyngeal irritation may be an indication of discontinuation.

9. When patients using systemic glucocorticoids switch to mometasone, some patients may have symptoms of withdrawal of glucocorticoids such as joint and / or muscle pain, fatigue, and fatigue, although the nasal symptoms have eased. Depression, patients should be encouraged to continue using mometasone. In addition, the conversion of systemic glucocorticoids to topical nasal cavity can also expose pre-existing allergic diseases such as allergic conjunctivitis and eczema (because these conditions are suppressed during systemic administration).

10. In patients receiving glucocorticoid therapy, immune function may be suppressed, so you should be alert to the danger of certain infections (such as chicken pox, measles).

11. Excessive, long-term local use of glucocorticoids may inhibit the hypothalamic-pituitary-adrenal axis, resulting in secondary adrenal insufficiency. Symptomatic treatment or gradual reduction to stop medication can be used.

12. The effects of drugs on children: If long-term or long-term use of mometasone in a package will increase the systemic absorption of the drug, it will also increase the risk of inhibiting adrenal function, which must be paid attention to. Especially for infants and children, due to the relatively large body surface area, the use of mometasone is more sensitive to hypothalamic-pituitary-adrenal axis inhibition and Cushing's syndrome than adults, and it can affect the growth and development of children. Mometasone should take care to minimize the amount of medication.

13. The impact of drugs on pregnancy: Mometasone's safety to pregnant women is not clear, and pregnant women should be cautious.

14. Effects of drugs on breastfeeding: It is unknown whether topical glucocorticoids can be excreted from breast milk. For breastfeeding women using mometasone still need to consider stopping breastfeeding or stopping medication. ^[2]

Mometasone Drug Interactions

Hydrocortisone ^[2]

Momisson Expert Reviews

It has a certain effect on local inflammation of the skin. Mometasone furoate is a synthetic medium-acting topical glucocorticoid containing chlorine. The basic nucleus of its steroid is halogenated at position 9 and the side chain at position 17 is Furfuric acid replacement, replaced by chlorine atom, has a better effect than hydrocortisone acetate hydrocortisone, which is equivalent to triamcinolone, but has a small inhibitory effect on the PHA axis. The intensity of mometasone increased without adverse reactions. ^[2]