Nasal steroids

I. Introduction

Nasal corticosteroids (commonly referred to as nasal steroids) are a pharmacological class of topical anti-inflammatory agents primarily used to manage inflammatory conditions of the nasal mucosa, particularly allergic rhinitis and nasal polyposis. These medications are applied intranasally and work by reducing mucosal inflammation, vascular permeability, and histamine release, providing relief from nasal congestion, sneezing, rhinorrhea, and itching.

Nasal steroids are considered first-line therapy for moderate-to-severe allergic rhinitis and have a well-established safety profile when used at recommended doses. Their utility also extends to non-allergic rhinitis, chronic rhinosinusitis, nasal polyps, and adjunctive therapy in asthma and sinus infections.

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II. Mechanism of Action

Nasal corticosteroids exert their action by mimicking endogenous glucocorticoids, binding to intracellular glucocorticoid receptors in the nasal epithelial cells. Upon activation, they influence gene transcription and protein synthesis to:

1. Suppress inflammatory cytokines (e.g., IL-1, IL-6, TNF-α)

2. Inhibit recruitment and activation of inflammatory cells such as eosinophils, mast cells, macrophages, and T-lymphocytes

3. Reduce vascular permeability and mucosal edema

4. Downregulate expression of adhesion molecules, decreasing immune cell migration

5. Inhibit histamine release, reducing allergic responses

Their local application minimizes systemic exposure, contributing to a favorable safety profile compared to oral steroids.

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III. Approved Nasal Steroid Agents (Generic and Brand Names)

The following are the most widely used nasal corticosteroids, categorized by generation and potency:

Generic Name	Brand Name(s)	Generation
Beclometasone dipropionate	Beconase AQ, QNASL	First
Budesonide	Rhinocort	First
Flunisolide	Nasalide, Nasarel	First
Triamcinolone acetonide	Nasacort AQ	First
Fluticasone propionate	Flonase, ClariSpray	Second
Fluticasone furoate	Veramyst, Flonase Sensimist	Second
Mometasone furoate	Nasonex	Second
Ciclesonide	Omnaris, Zetonna	Second
Dexamethasone	Off-label in compounded sprays	Potent systemic
Hydrocortisone	Rarely used intranasally	Mild potency

Second-generation steroids generally exhibit greater glucocorticoid receptor affinity, higher lipophilicity, and lower systemic bioavailability, contributing to superior efficacy and safety.

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IV. Indications and Clinical Use Cases

1. Allergic Rhinitis (Seasonal and Perennial)

   • First-line therapy for moderate to severe symptoms

   • Monotherapy or in combination with oral antihistamines

2. Non-Allergic Rhinitis

   • Vasomotor rhinitis

   • Gustatory rhinitis

3. Nasal Polyps

   • Reduce size of polyps

   • Prevent recurrence post-surgery

4. Chronic Rhinosinusitis (CRS)

   • Especially effective in CRS with nasal polyps (CRSwNP)

   • Adjunct to saline irrigation and antibiotics

5. Adjunctive Therapy in Asthma

   • Treats upper airway inflammation contributing to asthma severity

6. Prevention of Recurrence Post-Polypectomy or Sinus Surgery

7. Off-label/Compounded Uses

   • Eosinophilic granulomatosis with polyangiitis (EGPA)

   • Local therapy in autoimmune sinonasal disorders

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V. Pharmacokinetics and Local Delivery Characteristics

Parameter	Description
Onset of Action	6–12 hours for symptom relief; full effect in 1–2 weeks
Systemic Absorption	Low (<1% to 49%), depending on formulation (lowest in ciclesonide, mometasone, fluticasone)
Metabolism	Hepatic (CYP3A4) for systemically absorbed fraction
Excretion	Renal and fecal elimination of inactive metabolites
Bioavailability	Lower in newer agents (fluticasone, ciclesonide) → minimal systemic effects

VI. Dosing Recommendations (Adults)

Drug	Typical Adult Dose	Frequency
Beclometasone	1–2 sprays/nostril (42 mcg/spray)	BID
Budesonide	1–2 sprays/nostril (32 mcg/spray)	Once or BID
Fluticasone propionate	1–2 sprays/nostril (50 mcg/spray)	Once daily
Mometasone furoate	2 sprays/nostril (50 mcg/spray)	Once daily
Ciclesonide	2 sprays/nostril (50 mcg/spray)	Once daily
Triamcinolone	1–2 sprays/nostril (55 mcg/spray)	Once daily

Dosage for children is lower and age-dependent. Always refer to product-specific monographs.

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VII. Adverse Effects and Safety Considerations

Local (most common):

• Nasal dryness

• Burning or stinging sensation

• Epistaxis (nosebleeds)

• Nasal irritation or crusting

• Unpleasant taste or smell

• Nasal septal perforation (rare, with chronic misuse or improper technique)

• Thrush (candida) in the nasal passage (very rare)

Systemic (rare with proper use):

• HPA axis suppression (especially with high doses of first-gen agents)

• Growth suppression in children (minimal with second-gen)

• Ocular complications (intraocular pressure increase, cataracts)

• Immunosuppression (only theoretical with long-term high-dose)

Pregnancy & Lactation:

• Most intranasal steroids are Pregnancy Category B or C

• Budesonide is often the preferred agent in pregnancy due to safety data

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VIII. Technique of Administration

Improper administration greatly reduces efficacy and increases risk of side effects.

Key steps:

1. Blow the nose gently before use

2. Shake the bottle well

3. Point the nozzle away from the nasal septum

4. Spray towards the lateral wall of the nostril

5. Inhale gently while spraying

6. Avoid forceful sniffing afterward

7. Rinse mouth or wipe nasal tip after use

Spacer devices and saline irrigation may enhance delivery and minimize local irritation.

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IX. Contraindications

• Hypersensitivity to any component of the product

• Recent nasal surgery or trauma (until healing is complete)

• Active nasal infection (e.g. herpes simplex or tuberculosis)

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X. Drug Interactions

Generally minimal, due to low systemic absorption. However:

Interacting Drug	Effect
Strong CYP3A4 inhibitors	May increase systemic corticosteroid exposure (e.g. ritonavir, ketoconazole)
Other intranasal drugs	May irritate or reduce absorption

Combination use with antihistamines, anticholinergics, or decongestants is common in multidrug regimens for rhinitis.

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XI. Advantages of Nasal Steroids Over Other Modalities

Therapy	Benefits of Nasal Steroids
Oral Antihistamines	More effective in controlling nasal congestion and inflammation
Intranasal Antihistamines	Longer duration of action; lower rebound effects
Decongestants	No risk of rebound congestion (rhinitis medicamentosa)
Systemic Corticosteroids	Lower systemic side effects, safer for long-term use

XII. Recent Advances and Emerging Concepts

1. Dual Therapy Sprays: Combination of antihistamine + steroid (e.g., fluticasone + azelastine = Dymista)

2. Dry Powder Formulations: Better mucosal adherence and delivery (e.g., QNASL)

3. Biologic Therapy in CRSwNP:

   • Dupilumab (IL-4/13 blocker) used when nasal steroids fail

   • Nasal steroids often continued as baseline treatment

4. Personalized Nasal Therapy:

   • Individualized based on eosinophilic vs non-eosinophilic rhinitis

   • Gene expression studies for steroid responsiveness

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XIII. Summary of Key Nasal Steroid Comparisons

Drug	Potency	Systemic Bioavailability	Onset	Special Notes
Beclometasone	Moderate	~44%	6–12 hrs	First-gen; higher systemic risk
Budesonide	Moderate	~34%	6 hrs	Preferred in pregnancy
Fluticasone	High	<2%	12 hrs	Popular; low systemic effects
Mometasone	High	<1%	12 hrs	Well tolerated; long acting
Ciclesonide	High	<1%	12 hrs	Prodrug; low systemic exposure