Mometasone nasal spray

Generic Name: Mometasone furoate
Pharmacologic Class: Corticosteroid (nasal)
Therapeutic Class: Intranasal anti-inflammatory agent
ATC Code: R01AD09
Legal Classification: Prescription-only medication in many countries

Common Brand Names: Nasonex, MomeWell, Elocon Nasal, Mometamax (veterinary), Sinuva (implant), Mometasone Teva

Available Formulations:
– Nasal spray suspension: 50 mcg/actuation
– Dose per bottle: Commonly 60, 120 actuations

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Mechanism of Action

Mometasone furoate is a high-potency synthetic corticosteroid that exerts anti-inflammatory, antipruritic, and vasoconstrictive effects locally within the nasal mucosa:

• Inhibits the release of pro-inflammatory mediators including leukotrienes, prostaglandins, and cytokines by suppressing phospholipase A2 activity and reducing mRNA expression of inflammatory genes

• Reduces infiltration and activity of eosinophils, basophils, neutrophils, mast cells, and lymphocytes

• Minimizes edema, mucus secretion, nasal congestion, sneezing, itching, and rhinorrhea

Unlike oral steroids, mometasone acts locally with minimal systemic absorption, thereby limiting systemic adverse effects.

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Therapeutic Indications

Adults and Children ≥2 years:

1. Allergic rhinitis (seasonal and perennial):

   • First-line agent for moderate-to-severe allergic rhinitis

2. Nasal polyps (≥18 years):

   • Reduces size, improves nasal airflow, and delays surgery

3. Non-allergic rhinitis (off-label):

   • Effective in vasomotor rhinitis and irritant-induced rhinitis

4. Sinusitis (adjunctive to antibiotics):

   • Acute and chronic rhinosinusitis

5. Nasal congestion associated with the common cold (short-term, off-label):

6. Prophylaxis of seasonal allergic rhinitis:

   • Starting 2–4 weeks prior to pollen exposure

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Dosage and Administration

Adults and Adolescents ≥12 years:

• Allergic rhinitis / nasal polyps: 2 sprays per nostril once daily (total 200 mcg/day)

• Maintenance (once controlled): 1 spray per nostril once daily (100 mcg/day)

• Maximum dose: 4 sprays/day (200 mcg)

Children 2–11 years:

• 1 spray per nostril once daily (100 mcg/day)

In nasal polyps (≥18 years):

• Start with 2 sprays per nostril twice daily (400 mcg/day)

• May reduce to once daily if symptoms improve

Onset of Action:

• Noticeable effect within 12 hours, but full benefit may require several days to weeks of regular use

Administration Technique:

• Shake the bottle before each use

• Blow the nose gently before spraying

• Insert applicator and aim slightly outward away from nasal septum

• Avoid sniffing deeply

• Wipe the applicator tip and replace the cap after each use

• Prime the spray if unused for more than 7 days or when new

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Pharmacokinetics

• Bioavailability: <1% (minimal systemic absorption)

• Metabolism: Extensive first-pass hepatic metabolism via CYP3A4

• Plasma half-life: 5.8 hours

• Excretion: Mainly fecal (via biliary route)

• Protein binding: >98%

• Systemic exposure: Lower than many other intranasal steroids (e.g., fluticasone)

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Contraindications

• Hypersensitivity to mometasone or any formulation component

• Untreated local nasal infections (bacterial, viral, or fungal)

• Recent nasal surgery or trauma (delayed wound healing risk)

• Children <2 years (due to safety and efficacy concerns)

• Active or latent tuberculosis involving the respiratory tract

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Warnings and Precautions

1. Local nasal effects:

   • Epistaxis (nosebleeds)

   • Nasal septal perforation (rare)

   • Candida albicans nasal/oral infection (especially with prolonged use)

   • Periodic nasal examination is advised during long-term therapy

2. Systemic corticosteroid effects (rare):

   • HPA axis suppression (high-dose, prolonged use)

   • Growth retardation in children (monitor growth regularly)

   • Ocular effects: glaucoma, increased intraocular pressure, cataracts (long-term use)

3. Immunosuppression:

   • Patients should avoid exposure to chickenpox or measles

   • Discontinue use if systemic corticosteroid-like symptoms develop

4. Delayed wound healing:

   • Avoid use in patients with nasal ulcers, recent surgery, or trauma until healed

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Adverse Effects

Common (>1%):

• Epistaxis (nosebleeds)

• Nasal irritation or burning

• Pharyngitis

• Headache

• Cough

• Upper respiratory tract infections

Uncommon (0.1–1%):

• Nasal septum perforation

• Altered sense of smell or taste

• Dry nose or throat

• Hoarseness

Rare (<0.1%):

• Hypersensitivity reactions (angioedema, rash)

• Candida infections (nasal/oropharyngeal)

• Anaphylaxis (extremely rare)

• Glaucoma or cataracts (long-term, high-dose exposure)

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Drug Interactions

Interacting Agent	Potential Effect	Recommendation
CYP3A4 inhibitors (e.g., ketoconazole, ritonavir)	↑ systemic corticosteroid levels	Caution; monitor for systemic effects
Other corticosteroids	Additive systemic burden	Avoid duplication unless justified
Immunosuppressants	Additive immune suppression	Monitor for infections

Mometasone has low systemic absorption; however, caution is advised in concurrent use with potent CYP3A4 inhibitors (may increase risk of systemic corticosteroid effects).

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Pregnancy and Lactation

Pregnancy:

• Category C (FDA)

• Animal studies show adverse effects, but limited human data

• Generally considered safe when used at the lowest effective dose for the shortest duration

Lactation:

• Unknown if mometasone is excreted in breast milk

• Use cautiously in nursing mothers

• No documented adverse effects in breastfed infants from nasal formulations

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Use in Special Populations

• Children:

  • Approved for use in children ≥2 years for allergic rhinitis

  • Monitor for growth retardation with long-term use

• Elderly:

  • No specific precautions; similar tolerability as younger adults

• Renal or hepatic impairment:

  • No dosage adjustment needed

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Monitoring Parameters

• Symptom improvement (nasal congestion, sneezing, rhinorrhea)

• Epistaxis or mucosal irritation

• Regular nasal mucosa examination (for ulceration or candidiasis)

• Monitor growth in pediatric patients receiving long-term therapy

• In high-risk patients: consider intraocular pressure monitoring

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Comparative Notes with Other Nasal Steroids

Parameter	Mometasone	Fluticasone	Budesonide
Systemic bioavailability	<1%	<2%	~30%
Dosing frequency	Once daily	Once daily	Once or twice daily
Potency	High	High	Moderate
Onset of action	Within 12–24 hrs	Similar	Similar
FDA Pregnancy Category	C	C	B

Mometasone is considered among the most potent and least systemically absorbed intranasal corticosteroids, making it suitable for long-term use in allergic rhinitis with favorable safety.

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Patient Counseling Points

• Shake bottle well before each use

• Use daily at the same time for best effect

• It may take several days for full relief – continue use even if symptoms improve slowly

• Rinse the nozzle regularly to prevent blockage

• Avoid blowing your nose immediately after spraying

• Contact your doctor if you experience frequent nosebleeds, persistent irritation, or vision changes

• Do not share nasal spray with others to prevent infection spread

• Use the lowest effective dose and do not exceed prescribed frequency

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Storage Instructions

• Store at 15°C to 30°C (59°F to 86°F)

• Protect from freezing and direct sunlight

• Keep the bottle upright and cap tightly closed

• Discard after labeled number of sprays (usually after 120 actuations), even if liquid remains