Ariflu

• Seasonal Allergic Rhinitis (SAR):
  Treatment of nasal symptoms including nasal congestion, sneezing, rhinorrhea, and nasal itching associated with seasonal allergies.
• Perennial Allergic Rhinitis (PAR):
  Management of year-round nasal allergy symptoms caused by allergens such as dust mites, pet dander, and mold.
• Vasomotor Rhinitis:
  Relief of symptoms such as nasal congestion and rhinorrhea related to nonallergic rhinitis.
• Other Clinically Accepted Uses:
  Sometimes used off-label for adjunctive treatment of chronic rhinosinusitis with nasal polyps when inflammation and allergy overlap.

Formulation:
Intranasal spray containing fixed doses of azelastine hydrochloride and fluticasone propionate.

Adult Dosing:

• Typical Dose: 1 spray per nostril twice daily (morning and evening).
• Maximum dose should not exceed 2 sprays per nostril per day.

Pediatric Dosing:

• Ages 12 and above: Same as adults (1 spray per nostril twice daily).
• Safety and efficacy not established in children under 12 years.

Administration Instructions:

• Shake the bottle gently before use.
• Clear nasal passages prior to administration.
• Insert applicator tip into each nostril, spray while gently inhaling through the nose.
• Avoid blowing the nose immediately after administration.
• Use regularly for optimal symptom control; may begin prior to allergen exposure.

Special Populations:

• No dose adjustment typically necessary for elderly, renal or hepatic impairment.

This combination provides dual action:

• Azelastine Hydrochloride: A selective histamine H1 receptor antagonist that blocks histamine-mediated allergic symptoms such as sneezing, itching, and rhinorrhea. It also has mast cell stabilizing and anti-inflammatory effects, reducing mediator release and eosinophil recruitment.
• Fluticasone Propionate: A potent corticosteroid that exerts anti-inflammatory effects by binding to glucocorticoid receptors, inhibiting multiple inflammatory cytokines and cells involved in the allergic response. This leads to reduced nasal mucosal edema, congestion, and inflammation.

Together, they provide rapid and sustained relief of nasal allergy symptoms by combining antihistamine effects with corticosteroid-mediated inflammation suppression.

• Absorption:
  Azelastine: ~40% absorbed systemically after nasal administration.
  Fluticasone propionate: Minimal systemic bioavailability (<2%) due to extensive first-pass metabolism.
• Distribution:
  Both drugs bind extensively to plasma proteins (Azelastine ~88–90%).
• Metabolism:
  Fluticasone is primarily metabolized in the liver via CYP3A4. Azelastine undergoes hepatic metabolism mainly by demethylation and conjugation.
• Elimination:
  Both drugs and their metabolites are primarily excreted in feces; minor renal elimination.
• Half-life:
  Azelastine: ~22 hours
  Fluticasone: ~7.8 hours

• Pregnancy:
  Classified as Category C (FDA). Animal studies have shown some adverse effects at high doses; no adequate well-controlled studies in humans. Use only if benefits outweigh risks.
• Lactation:
  Unknown if either drug is excreted in human milk. Use caution and consider the benefits of breastfeeding vs. therapy.

• Primary Therapeutic Class: Combination Intranasal Antihistamine + Corticosteroid
• Subclasses:
• Azelastine: Second-generation H1 receptor antagonist
• Fluticasone: Intranasal corticosteroid

• Hypersensitivity to azelastine, fluticasone, or any excipients.
• Nasal ulcers, untreated nasal infections, or recent nasal surgery or trauma.
• Concurrent use of systemic antifungals or strong CYP3A4 inhibitors (due to fluticasone metabolism).

• Use with caution in patients with active or latent infections (fungal, bacterial, viral).
• Risk of nasal mucosal irritation or bleeding; monitor for persistent epistaxis.
• May cause somnolence; avoid hazardous tasks if affected.
• Potential adrenal suppression with prolonged use of corticosteroids.
• Monitor for glaucoma or cataracts with long-term corticosteroid use.
• Avoid concurrent use with other intranasal corticosteroids.

Common:

• Bitter taste
• Nasal irritation or burning sensation
• Headache
• Epistaxis (nosebleed)
• Dryness of nasal mucosa

Serious but Rare:

• Hypersensitivity reactions (rash, angioedema)
• Bronchospasm or wheezing (especially in asthmatics)
• Nasal septal perforation (rare)
• Adrenal suppression with long-term use

• CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) may increase fluticasone systemic exposure → risk of adrenal suppression.
• Additive CNS depressant effects with alcohol or sedatives due to azelastine.
• Avoid concomitant use with other nasal corticosteroids to prevent toxicity.

• Combination intranasal sprays like azelastine + fluticasone are increasingly recommended as first-line therapy for moderate to severe allergic rhinitis for rapid and comprehensive symptom control.
• Guidelines from allergy societies endorse use for both seasonal and perennial allergic rhinitis.
• Recent formulations have improved patient adherence through reduced dosing frequency and side effects.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from light and moisture.
• Keep container tightly closed.
• Do not freeze.
• Discard after the expiration date.