Metanase

Approved Indications (by Route/Formulation):

A. Nasal Formulations (Spray):

• Seasonal Allergic Rhinitis (including hay fever) in adults and children ≥2 years
• Perennial Allergic Rhinitis in adults and children ≥2 years
• Nasal Polyps in adults ≥18 years (to reduce size and symptoms such as congestion)
• Prophylaxis of Seasonal Allergic Rhinitis in adults and adolescents ≥12 years (initiated 2–4 weeks before pollen season)

B. Inhalation Powder/Spray (Asthma):

• Maintenance Treatment of Asthma in patients ≥4 years (not for acute bronchospasm)
  Used as a controller medication to reduce inflammation and prevent exacerbations

C. Topical Formulations (Cream, Ointment, Lotion):

• Inflammatory and Pruritic Manifestations of Corticosteroid-Responsive Dermatoses (e.g., eczema, psoriasis, atopic dermatitis) in patients ≥2 years
• Seborrheic Dermatitis (Scalp lotion): In adults

D. Off-label/Investigational Uses:

• Eosinophilic Esophagitis (EoE): Off-label topical use as oral suspension (swallowed) in refractory EoE
• Lichen Planus and Oral Ulcerative Conditions: Off-label application in mucosal corticosteroid therapy

A. Intranasal Use (Allergic Rhinitis & Nasal Polyps):

• Adults & Adolescents ≥12 years:
• Allergic Rhinitis: 2 sprays (50 mcg/spray) per nostril once daily (total 200 mcg/day)
• Nasal Polyps: 2 sprays per nostril twice daily (total 400 mcg/day); may reduce to once daily if controlled
• Children 2–11 years: 1 spray per nostril once daily (total 100 mcg/day)

B. Oral Inhalation (Asthma Maintenance):

• Adults & Adolescents ≥12 years:
• Initial: 220 mcg once daily in the evening
• May increase to 220 mcg twice daily (maximum: 440 mcg/day) if inadequate response
• Children 4–11 years: 110 mcg once daily in the evening (via dry powder inhaler)

C. Topical (Skin Conditions):

• Apply a thin film of 0.1% cream, ointment, or lotion to affected areas once daily
• Do not apply to broken skin or use with occlusive dressings unless advised

Renal or Hepatic Impairment:

• No dose adjustment needed due to minimal systemic absorption with topical/nasal use
• Use inhaled formulations with caution in hepatic impairment

Elderly:

• No dose adjustment required; monitor for systemic corticosteroid effects

Mometasone furoate is a potent synthetic corticosteroid that binds to intracellular glucocorticoid receptors, modifying gene expression to inhibit the transcription of pro-inflammatory cytokines and mediators such as interleukins, prostaglandins, and leukotrienes. This results in anti-inflammatory, antipruritic, vasoconstrictive, and immunosuppressive effects at the local tissue level. In nasal and bronchial tissues, it reduces mucosal inflammation, vascular permeability, and eosinophil infiltration. In skin, it suppresses the inflammatory response and symptoms such as redness, itching, and swelling.

• Absorption:
• Nasal and inhaled forms have low systemic bioavailability (<1%); minimal absorption into circulation
• Topical absorption varies depending on formulation and skin integrity
• Distribution: High protein binding (~98%)
• Metabolism: Extensively metabolized in the liver by CYP3A4 into inactive metabolites
• Elimination:
• Primarily excreted in bile (feces); minor renal excretion
• Half-life: Approx. 5.8 hours (systemic circulation, inhaled form)
• Onset of Action:
• Nasal: Improvement seen within 11 hours of first dose
• Inhaled: Symptom control may take 1–2 weeks of regular use
• Topical: Symptom relief typically within a few days

• Pregnancy:
  Classified as FDA Category C (for formulations prior to label updates). Use only if clearly needed. Animal studies showed potential teratogenicity with high doses, but human data are limited.
• Lactation:
  Unknown if excreted in human milk after nasal/topical/inhaled use. Systemic exposure is low, but caution is advised. For topical use, avoid application to nipple area.
• Recommendation:
  Use only if benefits outweigh risks. Consider lowest effective dose and shortest duration, especially in pregnancy or lactation.

• Primary Class: Corticosteroid (Anti-inflammatory agent)
• Subclass by Route:
• Intranasal: Corticosteroid for allergic rhinitis
• Inhaled: Inhaled corticosteroid (ICS) for asthma
• Topical: Medium-to-high potency corticosteroid for dermatologic conditions

• Known hypersensitivity to mometasone furoate or any formulation excipients
• Untreated local infections (e.g., nasal or skin tuberculosis, herpes simplex)
• Nasal septum ulceration or recent nasal surgery (for intranasal use)
• Viral, fungal, or bacterial infections involving treatment site without appropriate antimicrobial coverage
• Not for use in acute asthma or status asthmaticus

• Systemic Corticosteroid Effects:
  Long-term use of high-dose inhaled or topical corticosteroids may cause adrenal suppression, growth retardation in children, osteoporosis, and Cushingoid features
• Growth Monitoring:
  Recommended in children receiving long-term inhaled or nasal corticosteroids
• Infection Risk:
  Corticosteroids may mask signs of local or systemic infection and delay healing
• Nasal Formulations:
  Monitor for nasal septum perforation, epistaxis, or Candida albicans infection
• Topical Use:
  Avoid prolonged use, especially on face, groin, or under occlusion. Risk of skin thinning, striae, and perioral dermatitis
• Ocular Effects:
  Prolonged use may increase intraocular pressure or cause cataracts

Common Side Effects (by route):

• Nasal:
• Headache
• Nosebleeds (epistaxis)
• Pharyngitis
• Nasal irritation or burning
• Inhaled:
• Oral candidiasis (thrush)
• Hoarseness or dysphonia
• Cough, upper respiratory infections
• Topical:
• Burning, itching, or dryness at application site
• Skin atrophy, telangiectasia (with prolonged use)

Serious Side Effects:

• Adrenal suppression
• Growth retardation in children (dose-related)
• Glaucoma, cataracts (with long-term use near eyes)
• Hypersensitivity or contact dermatitis

Timing:

• Most adverse effects occur early during use and may resolve with dose reduction or discontinuation

• CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir):
  May increase systemic exposure to mometasone, enhancing the risk of systemic corticosteroid effects
• Other Immunosuppressants:
  Additive immunosuppressive effects if used concurrently
• Live Vaccines:
  Caution with high-dose inhaled or systemic corticosteroids; may impair immune response
• No significant food or alcohol interactions reported with nasal/topical/inhaled forms

• Nasal Polyps:
  Recognized in recent ENT and allergy guidelines as first-line pharmacologic therapy for both initial and recurrent polyps
• Asthma Guidelines (GINA 2023):
  Mometasone inhalers included among preferred controller options for stepwise asthma management
• Topical Corticosteroid Stewardship:
  Emphasis on appropriate potency, duration, and patient education to avoid corticosteroid misuse and adverse skin effects
• Pediatric Use Cautions:
  Reinforced guidance on growth monitoring with long-term corticosteroid use in children

• Temperature: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C–30°C
• Humidity: Protect from excessive moisture
• Light: Store in original container; protect nasal and inhaler products from direct light
• Handling Instructions:
• Do not freeze inhaler or nasal spray
• Shake nasal spray well before use
• Discard nasal spray after labeled number of sprays even if some medication remains
• Topical products should be used within recommended time after opening