Generic Name

Oxymetazoline Nasal

Mechanism

• Selective α₁‑ and α₂‑adrenergic receptor agonist
• Activates α₁ receptors → vasoconstriction of nasal mucosal arterioles → ↓ blood flow, ↓ mucosal edema, ↓ secretions.
• Activates α₂ receptors → inhibits norepinephrine release, amplifying vasoconstriction.
• Result: rapid, short‑acting decongestion of the nasal cavity.

Pharmacokinetics

• Absorption – Rapid local absorption; systemic bioavailability <5 % due to first‑pass metabolism.
• Distribution – Peaks in systemic circulation within 15–30 min; volume of distribution ≈ 30 L.
• Metabolism – Primarily via hepatic N‑dealkylation; minor renal excretion.
• Half‑life – Systemic t₁/₂ ≈ 8–12 h (shorter in nasal mucosa <1 h).
• Drug interactions – Minimal; caution with MAO inhibitors or agents causing systemic α‑agonism.

Indications

• Acute rhinitis (viral, allergic, or nonspecific).
• Decongestive relief for nasal congestion secondary to:
• al allergic rhinitis
• Upper airway infections (e.g., sinusitis)
• Non‑allergic rhinitis

Contraindications

• Contraindications
• Primary hypertension – may worsen due to systemic absorption.
• Recent or ongoing use of MAO inhibitors (oral or intranasal).
• Pregnancy – Category D (risk to fetus; use only if benefits outweigh risks).
• Warnings
• Rebound congestion (rhinitis medicamentosa) after prolonged use (>7 days).
• Systemic side effects (hypertension, tachycardia) if used >5 days.
• Use with caution in patients on β‑blockers or vasoactive medications.

Dosing

• Adults / Adolescents (≥12 y)
• 1 spray per nostril (0.1 mg per spray) – twice daily during ≤7 days.
• Pediatric (≤12 y) – Use only on pediatric‑approved products; typical dose 0.1 mg/spray once daily or as directed by pediatrician.
• Administration tips
• Tilt head back, spray at an angle to avoid posterior drip.
• Alternate nostrils to minimize local irritation.

Adverse Effects

• Rebound congestion often appears after 5–7 days; reduce or discontinue abruptly to avoid paradoxical swelling.

Monitoring

• Vital signs – BP, HR, especially during chronic use.
• Nasal mucosa – Inspect for epithelium damage or crusting.
• Duration of therapy – Keep ≤7 days; document use to avoid over‑use.
• Pediatric patients – Monitor for signs of irritability or distress.

Clinical Pearls

• “5‑Day Rule” – Stop after 5 days; earlier in patients with hypertension or β‑blocker therapy to reduce rebound risk.
• Dilution hack – For patients with congestion that limits spray action, a brief 30‑second nasal rinse with saline before administration can improve deposition.
• Packaging labeling – Look for “Do not exceed 1 spray per nostril, 2 times a day.”
• Safe re‑entry – If a patient needs continued decongestion beyond 7 days, consider transitioning to intranasal steroid sprays or saline irrigation.
• Ocular safety – Rarely, intranasal oxymetazoline can cause ocular vasoconstriction if spray drips into the eye; wear protective eyewear in workplace settings or shield eye area.

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• Reference: UpToDate, 2025; American Academy of Otolaryngology–Head & Neck Surgery Standards of Care.