Nasal preparations

I. Introduction

Nasal preparations are a broad category of medicinal products administered via the intranasal route to exert local or systemic effects. These preparations target the nasal mucosa, the olfactory region, or enable drug delivery into the systemic circulation via the highly vascularized nasal epithelium. They are pivotal in managing a variety of conditions including allergic rhinitis, nasal congestion, sinusitis, nasal polyps, epistaxis, migraine, hormone replacement, vaccination, and more.

Due to their non-invasive administration, rapid onset, and minimal systemic side effects (in many cases), nasal preparations have become essential components of both prescription and over-the-counter (OTC) therapeutic regimens.

---

II. Advantages of the Intranasal Route

• Avoids first-pass hepatic metabolism

• Rapid onset of action

• Non-invasive and painless

• Suitable for local and systemic drug delivery

• Useful for patients with swallowing difficulties

• Access to the central nervous system via olfactory route (in development)

---

III. Classification of Nasal Preparations

Nasal preparations may be classified based on:

1. Therapeutic Class / Pharmacological Action

2. Formulation Type

1. By Therapeutic Class

• Nasal Decongestants

• Nasal Corticosteroids

• Antihistamines (Intranasal)

• Anticholinergics

• Antibiotics and Antiseptics

• Antiviral Nasal Sprays

• Analgesics and Antimigraine Agents

• Hormonal Nasal Sprays (e.g., desmopressin, calcitonin)

• Vaccines (e.g., Live Attenuated Influenza Vaccine - LAIV)

• Antidiuretic Hormone Analogues

• Saline Solutions / Irrigation

• Hemostatics (for epistaxis)

• Antiseptics / Disinfectants

• Neurological and CNS Delivery Agents (e.g., midazolam)

2. By Formulation

• Nasal sprays (metered or pump)

• Nasal drops

• Nasal gels

• Nasal ointments

• Nasal powders

• Nasal irrigation solutions

• Pressurized aerosols

---

IV. Common Examples of Nasal Preparations

Drug/Class	Example Product Names	Main Indication
Oxymetazoline (decongestant)	Afrin, Dristan	Nasal congestion, sinusitis
Fluticasone propionate (steroid)	Flonase, Avamys	Allergic rhinitis, nasal polyps
Azelastine (antihistamine)	Astepro, Rhinolast	Allergic rhinitis
Ipratropium bromide	Atrovent Nasal	Rhinorrhea, non-allergic rhinitis
Desmopressin acetate	DDAVP Nasal	Diabetes insipidus, nocturnal enuresis, hemophilia A
Sumatriptan	Imitrex Nasal	Acute migraine
Calcitonin	Miacalcin Nasal	Osteoporosis
Zanamivir	Relenza	Influenza A & B (limited nasal delivery)
Naloxone	Narcan Nasal	Opioid overdose reversal
Midazolam	Nayzilam	Acute seizure episodes
Live Attenuated Flu Vaccine	FluMist	Influenza prophylaxis
Mupirocin (off-label)	Bactroban	MRSA nasal colonization
Saline irrigation	NeilMed, Sterimar	Nasal hygiene, rhinitis, post-op nasal care
Silver sulfadiazine (compounded)	RayaSore Kit (topical nasal burn care)	Burn management (limited nasal use)

V. Key Pharmacological Subtypes

1. Nasal Decongestants

• Mechanism: Alpha-adrenergic agonists → vasoconstriction of nasal mucosal vessels

• Examples: Oxymetazoline, Xylometazoline, Phenylephrine, Naphazoline

• Uses: Relief of nasal congestion from rhinitis or sinusitis

• Warning: Rhinitis medicamentosa (rebound congestion with prolonged use > 3–5 days)

2. Intranasal Corticosteroids

• Mechanism: Anti-inflammatory via suppression of immune cell activity and cytokine production

• Examples: Mometasone, Fluticasone, Budesonide, Triamcinolone, Beclometasone

• Uses: Seasonal/perennial allergic rhinitis, nasal polyps, chronic rhinosinusitis

• Advantage: High local efficacy, low systemic absorption

3. Intranasal Antihistamines

• Mechanism: H1 receptor antagonists

• Examples: Azelastine, Olopatadine

• Uses: Seasonal allergic rhinitis, vasomotor rhinitis

• Note: More rapid onset than oral antihistamines

4. Anticholinergics

• Mechanism: Inhibits parasympathetic-mediated nasal secretions

• Example: Ipratropium nasal spray

• Uses: Rhinorrhea (especially non-allergic)

5. Hormonal/Nasal Peptides

• Examples:

  • Desmopressin: ADH analogue for diabetes insipidus, hemophilia

  • Calcitonin: For osteoporosis and Paget’s disease

• Systemic effect via nasal mucosa absorption

6. Analgesics / Antimigraine Nasal Sprays

• Example: Sumatriptan

• Advantage: Non-oral delivery during migraine with vomiting

7. Seizure Rescue Therapy

• Example: Midazolam (Nayzilam)

• Indication: Intermittent acute seizure clusters

• Fast CNS access

8. Opioid Overdose Rescue

• Naloxone nasal spray (Narcan): Fast-acting reversal agent, now available OTC

9. Nasal Vaccines

• Example: FluMist (Live Attenuated Influenza Vaccine)

• Target: Induces mucosal and systemic immunity

• Limitations: Not suitable for immunocompromised or <2 years old

10. Nasal Irrigation

• Examples: Isotonic or hypertonic saline sprays, Neti pots

• Uses: Mucociliary clearance, sinus surgery recovery, rhinitis

• Additives: Bicarbonate, xylitol, corticosteroids (custom)

---

VI. Clinical Considerations

Consideration	Relevance
Technique	Correct angle, spray method, and nostril clearance enhances efficacy
Safety in Children	Dose adjustments; avoid decongestants in <6 years
Pregnancy/Lactation	Budesonide preferred; avoid vasoconstrictors unless necessary
Long-Term Use	Caution with steroids and vasoconstrictors
Compounding Potential	For unique needs (e.g., nasal antifungals, triple therapy)
Infectious Risk	Clean delivery devices to avoid contamination

VII. Adverse Effects

Type	Common Manifestations
Local irritation	Burning, dryness, stinging, sneezing, epistaxis
Rebound congestion	Seen with overuse of nasal decongestants
Infections	Rare fungal overgrowth or bacterial colonization
Systemic absorption	Minimal in newer corticosteroids; risk in hormonal agents
Septal perforation	Rare; improper application of steroids

VIII. Contraindications and Cautions

• Severe nasal septum deviation or nasal obstruction: May limit delivery

• Recent nasal surgery: Use under physician guidance only

• Hypersensitivity to product ingredients

• Hypertension, arrhythmia, or glaucoma: Avoid vasoconstrictors unless monitored

---

IX. Drug Interactions

Interacting Agent	Effect / Interaction
MAO inhibitors	Hypertensive crisis risk with vasoconstrictors
CYP3A4 inhibitors	May increase systemic steroid effects (fluticasone, etc.)
Other intranasal agents	May alter local absorption or cause additive irritation
Sedatives	If combined with CNS-active nasal agents like midazolam

X. Emerging Trends and Future Directions

1. Biologic Nasal Therapies: mAb nasal delivery for immune modulation

2. Nose-to-Brain Delivery Systems: Direct CNS access for neurologic drugs

3. Nanoparticle Formulations: Enhanced mucosal retention and permeation

4. Dry Powder Nasal Vaccines: Improved stability and cold-chain independence

5. Smart Nasal Devices: Metered-dose delivery with electronic monitoring

---

XI. Storage and Stability

• Store in a cool, dry place

• Avoid freezing or overheating

• Observe expiration dates especially with biologicals and vaccines

• Multi-use bottles must be discarded after the recommended period (usually 30–60 days after opening)

---

XII. Role in COVID-19 and Infectious Disease Research

• Nasal sprays studied for prevention (e.g., nitric oxide sprays, intranasal interferons)

• Ongoing development of mucosal vaccines (e.g., intranasal COVID-19 vaccine candidates)

• Nasal antiviral prophylaxis remains an area of active exploration