| FIELD OF APPLICATION | DETAILS |
|---|---|
| Generic Name |
Mometasone furoate
|
| Active Ingredient |
Mometasone furoate / Mometasone furoate monohydrate
|
| US Brand Names |
Asmanex, Nasonex, Elocon, Dulera
|
| Drug Category |
Dermatology
|
| Drug Class |
Prophylactic / preventive therapy, Palliative treatment, Immunosuppressive therapy, Targeted therapy
|
| Dosage Forms |
Aerosol, Aerosol, metered, Aerosol, powder, Capsule, Capsule, coated, Capsule; powder, Cream, Cream; kit, Emulsion, Gel, Implant, Inhalant, Kit, Lotion, Ointment, Powder, Powder, metered, Solution, Solution; spray, Spray, Spray, metered, Spray, suspension, Spray; suspension, Suspension
|
| Route of Administration |
Buccal, Cutaneous, Intrasinal, Intrasinal; Nasal, Intrasinal; Respiratory (inhalation), Nasal, Nasal; Respiratory (inhalation), Nasal; Topical, Oral, Respiratory (inhalation), Topical
|
| FDA Approval Status |
FDA Approved (April 1987)
Approved |
Mometasone Furoate Overview
Mometasone furoate is a synthetic, potent (Group III) glucocorticoid corticosteroid. Chemically, it belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins, and derivatives, which are steroids based on a hydroxylated prostane skeleton. It features a 17-furoate ester moiety and halogenated substitutions that confer high lipophilicity and intense glucocorticoid receptor selectivity.
In clinical medicine, Mometasone furoate is utilized across dermatology, allergy, pulmonology, and otolaryngology. Inhaled formulations (such as dry powder inhalers) are indicated for the prophylaxis and maintenance treatment of asthma in patients 4 years of age and older. Nasal spray formulations are available over-the-counter (OTC) and by prescription for upper respiratory allergic symptoms (rhinorrhea, sneezing) in patients 2 years and older, as well as for the treatment of chronic rhinosinusitis with nasal polyps in adults and seasonal allergic rhinitis prophylaxis. Topically applied as a cream, lotion, or ointment, Mometasone furoate is indicated for the relief of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses, such as dermatitis, eczema, and plaque psoriasis.
What Is Mometasone Furoate and How Does It Work?
Mometasone furoate is a small molecule glucocorticoid prodrug that exhibits exceptionally strong binding affinity for the human glucocorticoid receptor. Remarkably, its glucocorticoid receptor binding affinity is 22 times stronger than that of dexamethasone and significantly higher than many other traditional corticosteroids.
Its core cellular and physiological mechanisms include:
- Glucocorticoid Receptor Activation: Mometasone furoate diffuses across target cell membranes into the cytosol, binding tightly to glucocorticoid receptors. Binding induces a conformational change, detachment from chaperone proteins, and nuclear translocation. Receptors dimerize and bind to glucocorticoid response elements (GRE) on DNA, upregulating anti-inflammatory gene transcription while suppressing pro-inflammatory cytokines (such as interleukins 4 and 5).
- Transcription Factor Inhibition: It directly blocks key inflammatory transcription factors, including nuclear factor kappa B (NF-kB) and activator-protein-1 (AP-1).
- Inhibition of Inflammatory Cells & Mediators: In asthma and allergic rhinitis, it inhibits mast cells, eosinophils, basophils, and lymphocytes, while halting the synthesis and release of histamine, leukotrienes, and eicosanoids.
Is Mometasone Furoate FDA Approved?
Yes, Mometasone furoate received its initial US FDA approval in April 1987. It is approved across various brand-name and generic prescription formulations, as well as OTC nasal spray preparations.
What Is Mometasone Furoate Used For?
- Prophylaxis and maintenance treatment of asthma in adults and pediatric patients 4 years of age and older (inhaled).
- Symptomatic treatment of upper respiratory allergic symptoms (sneezing, rhinorrhea, nasal congestion) in patients 2 years and older (OTC nasal spray).
- Treatment of chronic rhinosinusitis phenotype with nasal polyps in adults 18 years of age and older (prescription nasal spray).
- Prophylaxis and treatment of seasonal allergic rhinitis in patients 12 years and older (prescription nasal spray or combination with olopatadine).
Before Taking Mometasone Furoate: Contraindications & Precautions
Do not use if you have a documented hypersensitivity to Mometasone furoate or any formulation ingredients. Inhaled formulations are contraindicated as primary therapy for acute bronchospasm or status asthmaticus. Avoid applying topical or nasal preparations over untreated viral, fungal, or bacterial skin or mucosal infections, or onto open wounds. Use during pregnancy and lactation only if potential maternal benefits strictly justify fetal or infant risks.
Who Should Not Take Mometasone Furoate?
- Individuals with a documented hypersensitivity to Mometasone furoate or any formulation ingredients.
- Primary treatment of status asthmaticus or acute bronchospasm requiring emergency bronchodilators.
- Patients with untreated, localized ocular, nasal, or cutaneous viral, fungal, or bacterial infections.
- Application of topical formulations to open wounds or severely eroded skin barriers.
Mometasone Furoate, Pregnancy & Fertility
Systemic bioavailability following topical or nasal administration is extremely low (<1%). Inhaled formulations result in minor systemic exposure. Animal reproduction studies with corticosteroids demonstrate embryo-fetal toxicity and teratogenicity at high systemic doses. Mometasone furoate should be used during pregnancy only if the potential maternal benefit justifies the potential risk to the fetus. It is unknown whether Mometasone furoate is excreted in human breast milk; caution should be exercised when administered to nursing mothers.
Tell Your Doctor Before Taking Mometasone Furoate
Inform your physician if you have a history of tuberculosis, ocular herpes simplex, untreated systemic infections, recent nasal ulcers, nasal surgery, or ocular disorders such as cataracts or glaucoma. Disclose if you are taking strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir).
Mometasone Furoate Dosage & Administration
For asthma maintenance (inhalation), dosing ranges from 110 mcg to 440 mcg inhaled once or twice daily. For allergic rhinitis or nasal polyps (nasal spray), standard adult dosing is 2 sprays per nostril once daily (200 mcg total); pediatric dosing (ages 2–11) is 1 spray per nostril once daily (100 mcg total). For corticosteroid-responsive dermatoses, apply a thin film of 0.1% cream, ointment, or lotion to clean, dry skin once daily. Always rinse the mouth and spit after inhalation to prevent oral thrush, and direct nasal sprays away from the nasal septum.
Standard Mometasone Furoate Dosing
- Asthma Prophylaxis (Inhaler): Dosing varies by age and prior asthma therapy, typically ranging from 110 mcg to 440 mcg inhaled once or twice daily.
- Allergic Rhinitis / Nasal Polyps (Nasal Spray): Standard adult dosing is 2 sprays (50 mcg per spray) in each nostril once daily (total daily dose of 200 mcg). For pediatric patients (2 to 11 years), 1 spray in each nostril once daily (100 mcg total).
- Dermatoses (Topical Cream / Ointment / Lotion 0.1%): Apply a thin film to affected skin areas once daily.
How Mometasone Furoate Is Administered
- Nasal Spray: Shake well before use. Prime the pump prior to initial use or after inactivity. Direct the spray away from the nasal septum.
- Oral Inhaler: Inhale deeply through the mouth. Rinse mouth thoroughly with water and spit out without swallowing after each inhalation to reduce oral candidiasis risk.
- Topical Formulations: Smooth gently onto clean, dry affected skin once daily. Do not cover with occlusive dressings unless directed by a physician.
Mometasone Furoate Clinical Efficacy & Research
Clinical trials demonstrate that Mometasone furoate provides high anti-inflammatory potency with minimal systemic adverse effects. In asthma trials, daily inhalation significantly improved forced expiratory volume in 1 second (FEV1), reduced nocturnal awakenings, and decreased rescue beta-agonist reliance. In allergic rhinitis studies, nasal administration produced rapid onset of relief within 11 hours. In dermatological evaluations, once-daily topical 0.1% application was as effective as twice-daily administration of other potent Group III corticosteroids in resolving plaque psoriasis and eczema.
Mometasone Furoate Side Effects & Safety Profile
Mometasone furoate does not carry an FDA Black Box Warning.
Common reactions include epistaxis, nasal burning, and headaches with nasal sprays; oropharyngeal candidiasis (thrush), dysphonia (hoarseness), and cough with inhalers; and localized burning, pruritus, or skin atrophy with topical application. Serious adverse risks include HPA axis suppression, Cushingoid features, nasal septum perforation, ocular complications (cataracts, glaucoma), and increased risk of secondary infections. Holds no FDA Black Box Warning.
Common Mometasone Furoate Side Effects
- Nasal Route: Epistaxis (nosebleeds), nasal burning/irritation, headache, pharyngitis, and viral upper respiratory tract infection.
- Inhalation Route: Oropharyngeal candidiasis (thrush), dysphonia (hoarseness), headache, and cough.
- Topical Route: Localized burning, pruritus, skin atrophy, tingling, and folliculitis.
Serious Mometasone Furoate Adverse Events
- Oropharyngeal or systemic fungal infections (candidiasis).
- Hypothalamic-pituitary-adrenal (HPA) axis suppression or Cushingoid features with prolonged high-dose use.
- Nasal septum perforation or localized candida infection of the nasal mucosa.
- Ocular complications, including cataracts, glaucoma, or increased intraocular pressure.
- Impaired wound healing and increased susceptibility to secondary infections.
Managing Mometasone Furoate Side Effects
Rinse the mouth with water after each inhaler dose to prevent oral thrush. If epistaxis occurs with nasal spray use, withhold therapy temporarily or adjust administration technique away from the septum. Discontinue topical application if severe skin irritation or allergic contact sensitization develops.
Mometasone Furoate Drug Interactions & What to Avoid
Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, cobicistat) increases systemic corticosteroid exposure, significantly elevating the risk of HPA axis suppression and systemic side effects. Avoid using oral inhalers for emergency rescue during sudden asthma attacks. Systemic food and alcohol interactions are minimal across topical, nasal, and inhaled formulations.
Mometasone Furoate Drug-Drug Interactions
- Strong CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Ritonavir, Cobicistat): Mometasone furoate is metabolized by CYP3A4. Co-administration with strong CYP3A4 inhibitors increases systemic corticosteroid exposure, elevating the risk of HPA axis suppression and systemic steroid adverse effects.
Mometasone Furoate, Food & Alcohol
Systemic food and alcohol interactions are minimal for inhaled, nasal, and topical formulations.
Mometasone Furoate: Missed Dose, Overdose & Storage
If a dose is missed, take, inhale, or apply it as soon as remembered on that day unless near the next scheduled dose; do not double up. Acute overdose via nasal, inhaled, or topical routes is unlikely to produce systemic toxicity due to low systemic bioavailability, but chronic overuse leads to systemic hypercorticism and HPA axis suppression. Store all formulations at room temperature (20°C–25°C) protected from direct heat, light, and moisture.
Missed Dose of Mometasone Furoate
Take, inhale, or apply the missed dose as soon as remembered on that day. If it is almost time for the next scheduled dose, skip the missed dose and resume your regular daily schedule. Do not double up doses.
Mometasone Furoate Overdose & Emergency
Acute overdose via nasal, inhaled, or topical routes is unlikely to produce life-threatening toxicity due to low systemic bioavailability. Chronic overuse of high doses can lead to systemic steroid toxicity, HPA axis suppression, hypercorticism, and immunosuppression.
How to Store Mometasone Furoate
Store nasal sprays, inhalers, and topical creams/ointments at controlled room temperature between 20°C and 25°C (68°F to 77°F). Protect from light, excessive moisture, and direct heat. Do not puncture or incinerate inhaler canisters. Keep out of reach of children.
Mometasone Furoate Patient Management & Monitoring
Assess baseline pulmonary function (FEV1/FVC), asthma severity, or nasal mucosal integrity prior to initiating therapy. Periodically monitor growth velocity in pediatric patients receiving chronic treatment. Inspect the nasal mucosa for septum erosion or fungal infection, and regularly check for signs of skin atrophy, striae, or cataracts during long-term therapy.
Tests Before Starting Mometasone Furoate
- Baseline clinical evaluation of asthma severity, pulmonary function (FEV1/FVC), or nasal mucosal integrity.
- Baseline ocular examination (intraocular pressure and lens inspection) in patients with a history of glaucoma or cataracts.
Monitoring During Mometasone Furoate Treatment
Periodically assess asthma symptom control and growth velocity in pediatric patients receiving chronic therapy. Inspect nasal mucosa for septum erosion or fungal infection. Monitor for cutaneous atrophy or striae when using topical formulations.
Mometasone Furoate Do’s and Don’ts
- Do rinse mouth and spit water out after using oral inhalers.
- Do point nasal spray tips away from the center of the nose (nasal septum).
- Do apply topical creams thinly once daily to affected skin.
- Do not use oral inhalers as a rescue medicine for sudden asthma attacks.
- Do not stop taking prescribed asthma inhalers abruptly without consulting your doctor.
Frequently Asked Questions
What exact type of chemical is Mometasone furoate?
Mometasone furoate is a synthetic, halogenated glucocorticoid corticosteroid featuring a 17-furoate ester group.
Is Mometasone furoate a fast-acting rescue inhaler?
No, inhaled Mometasone furoate is a long-term maintenance controller medication used for asthma prophylaxis; it will not relieve sudden asthma attacks.
Why is rinsing the mouth necessary after using an Asmanex inhaler?
Rinsing the mouth with water and spitting it out removes residual drug particles from the mouth, preventing oral thrush (candidiasis) and voice hoarseness.
Is Mometasone furoate nasal spray available over the counter?
Yes, OTC formulations of Mometasone furoate nasal spray (such as Nasonex 24HR) are available for upper respiratory allergic symptoms.
How strong is Mometasone furoate compared to other steroids?
Mometasone furoate has a glucocorticoid receptor binding affinity 22 times stronger than dexamethasone, making it a very potent anti-inflammatory agent.
Can Mometasone furoate cream be used on the face?
Topical Mometasone furoate is a potent Group III steroid. It should generally be avoided on the face, groin, or axillae unless specifically directed by a dermatologist due to high skin thinning risks.
Does Mometasone furoate cause weight gain?
Nasal, inhaled, and topical forms have low systemic absorption, making systemic side effects like weight gain or moon face very rare when used at recommended doses.
References
- DrugBank Database – Mometasone Furoate Clinical and Pharmacological Profile (DB14512)
- Official FDA Prescribing Information – Nasonex / Asmanex / Elocon
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