Anti allergic drugs used in ENT

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Anti-Allergic Drugs Used in ENT

Allergic conditions in ENT practice - primarily allergic rhinitis, allergic otitis, urticaria, and angioedema - are managed with a stepwise pharmacological approach. Below is a systematic classification.

1. Antihistamines (H1 Receptor Antagonists)

The backbone of anti-allergic therapy. They block H1 receptors, reducing itching, sneezing, and rhinorrhea. Classified into two generations:

First-Generation (Sedating)

DrugNotes
DiphenhydramineHighly sedating; significant anticholinergic effects
ChlorpheniramineMost commonly used; moderate sedation
PromethazineStrong antiemetic + antihistamine; useful in vertigo/vestibular allergy
HydroxyzineUseful in urticaria and pruritus
Cyclizine / MeclizineUsed in vestibular disorders and motion sickness in ENT
  • Cross the blood-brain barrier readily
  • Significant anticholinergic side effects (dry mouth, urinary retention, constipation)
  • Tachyphylaxis can develop
  • Avoid in patients performing skilled tasks (pilots, drivers)

Second-Generation (Non-Sedating)

DrugNotes
LoratadineLipophobic; minimal CNS effects; OTC
FexofenadineLeast sedating; no QTc prolongation; safe in cardiac patients
CetirizineSlightly sedating at higher doses; fast onset
DesloratadineActive metabolite of loratadine; potent
LevocetirizineR-enantiomer of cetirizine; highly potent
  • Lipophobic - do not cross the BBB readily
  • Little to no anticholinergic activity
  • Safe in asthma patients
  • Metabolized by CYP3A4 - be aware of CYP3A4 inhibitors (e.g., erythromycin, ketoconazole)
  • Little tachyphylaxis; strongly recommended for allergic rhinitis

Topical (Intranasal) Antihistamines

DrugNotes
AzelastineMost commonly used; rapid onset; as effective or superior to oral antihistamines for nasal congestion
OlopatadineAvailable for nasal and ocular use
  • Work directly at target organ (nose, eyes)
  • At least as effective as intranasal corticosteroids for sneezing, itching, rhinorrhea, and ocular symptoms
  • Best used in combination with intranasal corticosteroids (not as monotherapy)
Key Point (Cummings Otolaryngology): "The most effective combination for the treatment of allergic rhinitis is an intranasal steroid with an intranasal antihistamine."

2. Intranasal Corticosteroids (First-Line Therapy)

The most effective class for allergic rhinitis - superior to antihistamines and leukotriene receptor antagonists for controlling nasal inflammation.
DrugNotes
Fluticasone propionateLow systemic bioavailability; onset within 12 hours; aqueous spray
Fluticasone furoateMore potent; once daily; very low bioavailability
Mometasone furoateVery low systemic absorption; approved from age 2
BudesonideOnly intranasal steroid with Pregnancy Category B; aqueous, scent-free
Triamcinolone acetonideAvailable OTC in the US; aqueous spray
Beclomethasone dipropionateOlder agent; higher systemic bioavailability; may cause growth suppression in children
CiclesonideProdrug activated locally; minimal systemic effects
FlunisolideSignificant systemic bioavailability; poorly tolerated due to propylene glycol base
Key points:
  • First-line therapy for allergic rhinitis (except mildest cases)
  • Start 2 weeks before pollen season
  • Daily dosing more efficacious than as-needed dosing
  • Side effects: epistaxis, nasal dryness, local irritation; rare septal perforation
  • Aim spray away from the nasal septum
  • Newer agents generally free of HPA axis suppression
  • May have a negative effect on short-term growth in children - use the lowest effective dose

3. Leukotriene Receptor Antagonists (LTRAs)

Block leukotriene receptors on target cells, reducing nasal congestion, rhinorrhea, and sneezing.
DrugNotes
MontelukastOnly agent approved for allergic rhinitis; also for asthma and exercise-induced bronchospasm; approved from 6 months of age
ZafirlukastUsed in asthma; less evidence in rhinitis
  • Efficacy parallels antihistamines but inferior to intranasal corticosteroids
  • Particularly useful in patients with concurrent asthma (unified airway disease)
  • Not recommended as monotherapy or first-line for allergic rhinitis
  • Can be second-line or when intranasal corticosteroids are contraindicated

4. Mast Cell Stabilizers

DrugMechanismNotes
Cromolyn sodium (Sodium cromoglicate)Stabilizes mast cell membranes; inhibits degranulation and histamine releaseLipophobic; no systemic absorption; must be given 3-4x/day; best used prophylactically before allergen exposure; inferior to intranasal corticosteroids
KetotifenMast cell stabilizer + H1 antagonistUsed as eye drops for allergic conjunctivitis
  • Will not treat symptoms once mast cells have already degranulated
  • Compliance is difficult due to frequent dosing
  • Consider in patients who cannot tolerate intranasal corticosteroids
  • Free of systemic adverse effects (no systemic absorption)

5. Decongestants

Reduce nasal congestion by alpha-adrenergic vasoconstriction; have minimal effect on rhinorrhea, itching, or sneezing.

Oral Decongestants

DrugNotes
PseudoephedrineAlpha-2 agonist; effective; controlled availability (precursor to methamphetamine)
PhenylephrineNot superior to placebo in clinical trials; not recommended
  • Side effects: hypertension, insomnia, tachycardia, arrhythmia, anorexia
  • Often combined with antihistamines (e.g., loratadine + pseudoephedrine)

Topical Decongestants

DrugNotes
OxymetazolineImidazoline; very effective; rebound congestion (rhinitis medicamentosa) if used >3-5 days
XylometazolineSimilar to oxymetazoline
NaphazolineOlder agent; significant rebound
TetrahydrozolinePrimarily used as eye drops
  • Do not use for more than 3-5 days - risk of rebound congestion (rhinitis medicamentosa)

6. Intranasal Anticholinergics

DrugNotes
Ipratropium bromideDecreases watery nasal secretions from seromucous glands; used for rhinorrhea in allergic and non-allergic rhinitis; needs 6x/day dosing due to short half-life
  • Useful as adjuvant therapy in patients with persistent rhinorrhea despite intranasal corticosteroid use
  • Combination with intranasal corticosteroids more effective than either alone

7. Systemic Corticosteroids

  • Used for short courses in severe allergic inflammation only
  • Prednisone, methylprednisolone, dexamethasone
  • Oral preferred over parenteral for allergic rhinitis
  • Not recommended for routine use - largely replaced by intranasal steroids
  • Effects noticed within 12-24 hours

8. Biologics

DrugMechanismNotes
OmalizumabHumanized anti-IgE monoclonal antibodyNot FDA-approved for allergic rhinitis; approved for chronic urticaria and asthma; superior to immunotherapy alone when combined; costs ~$18,000/year
DupilumabIL-4/IL-13 receptor antagonistApproved for chronic rhinosinusitis with nasal polyps (CRSwNP)
Mepolizumab / BenralizumabAnti-IL-5 / anti-IL-5REosinophilic disease; nasal polyps

9. Immunotherapy (Disease-Modifying)

The only treatment that alters the natural course of allergic disease.
  • Subcutaneous Immunotherapy (SCIT) - conventional allergy shots
  • Sublingual Immunotherapy (SLIT) - sublingual drops or tablets
"Immunotherapy is the most effective treatment of allergic rhinitis." - Cummings Otolaryngology Head and Neck Surgery

Summary: Hierarchical Treatment Approach

Mild Intermittent AR:
  → Oral/intranasal antihistamine ± decongestant

Moderate-Severe or Persistent AR:
  → Intranasal corticosteroid (FIRST-LINE)
  → Add intranasal antihistamine (most effective combination)
  → Add montelukast if concurrent asthma

Persistent rhinorrhea:
  → Add intranasal ipratropium bromide

Prophylaxis before allergen season:
  → Start INCS 2 weeks early; consider cromolyn sodium

Disease modification:
  → Allergen immunotherapy (SCIT or SLIT)

Severe/refractory/CRSwNP:
  → Biologics (omalizumab, dupilumab)

Sources:
  • Cummings Otolaryngology Head and Neck Surgery, Chapter 35
  • KJ Lee's Essential Otolaryngology, Chapter on Treatment of Allergy
  • Scott-Brown's Otorhinolaryngology Head & Neck Surgery, Vol 1
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