Olonase

Approved Indications:

• Seasonal Allergic Rhinitis (SAR):
  Indicated in patients aged ≥12 years for the relief of symptoms associated with seasonal allergic rhinitis, including nasal congestion, rhinorrhea, sneezing, and nasal itching.
• Perennial Allergic Rhinitis (Off-label/Accepted Use):
  May be used off-label in some clinical settings where both antihistaminic and anti-inflammatory action is required year-round.
• Patients Refractory to Monotherapy:
  Approved for use in patients not adequately controlled by either an intranasal corticosteroid or antihistamine alone.

Formulation:
Nasal spray (each actuation contains:

• Mometasone Furoate 50 mcg
• Olopatadine Hydrochloride 665 mcg)

Age 12 years and older:

• Dose: 2 sprays per nostril once daily
• Total daily dose: Mometasone 200 mcg + Olopatadine 2.66 mg
• Duration: Use for the duration of the allergy season or as prescribed
• Onset of action: Some patients may experience relief within 15 minutes, especially for antihistaminic effects

Children (<12 years):

• Not approved for use; safety and efficacy have not been established

Elderly:

• No dose adjustment necessary

Renal/Hepatic Impairment:

• No specific dosage adjustment needed; however, use with caution in patients with severe hepatic impairment due to corticosteroid metabolism

Administration Instructions:

• Shake bottle well before each use
• Prime before first use or if not used for more than 2 weeks
• Blow nose gently before administration
• Avoid spraying into eyes or mouth
• Rinse mouth or gargle after use (optional, to reduce systemic absorption)

Mometasone Furoate is a potent synthetic glucocorticoid that binds intracellular glucocorticoid receptors in nasal epithelial cells. It inhibits inflammatory cytokines, prostaglandins, and leukotrienes, thereby reducing nasal mucosal inflammation, edema, and congestion.

Olopatadine Hydrochloride is a selective histamine H1-receptor antagonist with additional mast cell stabilizing properties. It blocks histamine-mediated allergic symptoms such as sneezing, rhinorrhea, and nasal itching, while preventing mast cell degranulation and release of inflammatory mediators.

Combined, this dual-action nasal spray offers broad-spectrum relief from both the early-phase (histamine-driven) and late-phase (inflammatory) responses of allergic rhinitis.

Mometasone Furoate:

• Absorption: Minimal systemic absorption; bioavailability <1%
• Peak plasma time: ~1 hour
• Metabolism: Hepatic metabolism via CYP3A4 to inactive metabolites
• Elimination: Primarily in feces (biliary); minimal renal clearance
• Half-life: 5.8 hours

Olopatadine Hydrochloride:

• Absorption: Systemic absorption is low after nasal administration
• Peak plasma time: 1–2 hours
• Bioavailability: ~57% (nasal route)
• Metabolism: Limited hepatic metabolism
• Elimination: Primarily renal (65–75% excreted unchanged in urine)
• Half-life: Approximately 8–12 hours

• Pregnancy:
• No formal FDA pregnancy category (post-PLLR rule), but prior classifications suggest Category C
• Animal studies indicate potential risks at high doses
• Should be used during pregnancy only if the potential benefit outweighs the risk
• Lactation:
• Unknown whether mometasone or olopatadine is excreted in human breast milk after intranasal use
• Given low systemic exposure, the risk to infants is likely minimal, but use with caution
• Recommendation:
• Use only when clearly needed during pregnancy or lactation
• Consider alternate therapies with better-established safety if needed for long-term use

• Primary Class: Combination Antiallergic Nasal Agent
• Subclasses:
• Mometasone Furoate: Inhaled corticosteroid (nasal anti-inflammatory)
• Olopatadine Hydrochloride: Second-generation antihistamine with mast cell stabilizer properties

• Known hypersensitivity to mometasone, olopatadine, or any component of the formulation
• Recent nasal surgery, trauma, or ulcers (due to delayed wound healing risk from corticosteroids)
• Ocular use is contraindicated; not intended for ophthalmic administration
• Untreated local infections (e.g., tuberculosis, herpes simplex in the nasal mucosa)

• Nasal Mucosal Changes: Monitor for nasal septal perforation or ulceration, especially with long-term use
• Systemic Corticosteroid Effects: At high doses or prolonged use, may cause adrenal suppression, delayed wound healing, and immunosuppression
• Glaucoma and Cataracts: Monitor for increased intraocular pressure with prolonged corticosteroid use
• Growth Suppression: Rare but possible in adolescents with long-term corticosteroid exposure
• Epistaxis and Local Irritation: Common with corticosteroid nasal sprays; monitor if persistent
• Mast Cell Disorders: Use with caution in individuals with systemic mastocytosis or similar allergic conditions

Common Adverse Effects:

• Local (Nasal):
• Epistaxis
• Nasal dryness or irritation
• Headache
• Bitter taste
• Sneezing
• Systemic (Rare):
• Fatigue, dizziness
• Cough or throat irritation

Less Common / Serious Effects:

• Nasal septal perforation
• Adrenal suppression (rare, long-term high-dose use)
• Anaphylaxis or severe hypersensitivity (rare)
• Increased intraocular pressure or glaucoma

Timing:

• Most local adverse events occur early and are dose-dependent.
• Systemic effects are rare due to low systemic bioavailability.

• CYP3A4 Inhibitors (e.g., ketoconazole, ritonavir):
  May increase systemic exposure to mometasone → risk of corticosteroid-related side effects
• Alcohol or CNS Depressants:
  Olopatadine may have additive sedative effects in very sensitive individuals, though risk is minimal due to nasal administration
• Other Antihistamines:
  Systemic antihistamines used concurrently may increase the risk of anticholinergic side effects (dry mouth, drowsiness)
• Live Vaccines:
  Use corticosteroids with caution in immunocompromised patients due to reduced vaccine efficacy

Enzyme Systems Involved:

• Mometasone: Metabolized by CYP3A4
• Olopatadine: Limited hepatic metabolism; minimal CYP involvement

• 2023 ARIA Guidelines (Allergic Rhinitis and its Impact on Asthma):
  Combination intranasal corticosteroids + antihistamines (e.g., mometasone + olopatadine) shown to be more effective than monotherapy in reducing overall nasal symptom burden.
• FDA Labeling Updates (2022):
  Reinforced instructions regarding non-ocular use and priming before first use.
• Clinical Preference:
  Increasingly preferred for patients with moderate-to-severe seasonal allergic rhinitis, especially when nasal congestion is prominent.

• Temperature: Store at 20°C to 25°C (68°F to 77°F)
• Excursion Range: Permitted between 15°C and 30°C (59°F to 86°F)
• Humidity Protection: Keep container tightly closed to protect from moisture
• Light Protection: Store in original container, away from direct sunlight
• Handling Instructions:
• Shake well before use
• Prime the device before initial use and after 14 days of non-use
• Do not freeze
• Keep out of reach of children
• Discard after labeled number of sprays (typically after 120 actuations or as specified)