Napolin

Approved Indications:

• Allergic Conjunctivitis (Seasonal & Perennial):
• Relief from symptoms such as itching, redness, tearing, and swelling of the conjunctiva due to allergens like pollen, pet dander, dust mites, mold, etc.
• Ocular Irritation and Redness Relief:
• Temporary relief of redness and discomfort caused by wind, dust, smoke, or contact lens wear.

Clinically Accepted Off-Label Uses:

• Supportive Management in Viral Conjunctivitis:
• Used to relieve ocular itching and redness associated with viral conjunctivitis (as adjunctive therapy).
• Post-operative Minor Ocular Discomfort:
• Occasionally used under medical supervision to relieve inflammation and irritation following minor eye procedures.

Not indicated for bacterial or fungal eye infections.

Route of Administration: Ophthalmic (eye drops)

Adults and Children ≥6 years:

• Typical Dose:
• 1–2 drops in the affected eye(s) up to 4 times daily.
• Do not exceed 4 doses in 24 hours.
• Intended for short-term use only (not more than 72 consecutive hours).

Children <6 years:

• Use only under medical supervision due to risk of systemic adverse effects.

Elderly:

• Use with caution due to increased susceptibility to systemic effects (e.g., CNS depression, cardiovascular changes).

Renal and Hepatic Impairment:

• No dosage adjustment required for topical ophthalmic use.
• Caution advised in severe impairment due to possible systemic absorption.

Administration Instructions:

• Wash hands before use. Tilt head back and instill drops into the conjunctival sac.
• Avoid touching the dropper tip to the eye or any surface.
• Apply gentle pressure to the inner corner of the eye (nasolacrimal duct) for 1–2 minutes to reduce systemic absorption.
• Remove contact lenses before application and wait at least 15 minutes before reinsertion.

Naphazoline Hydrochloride is a sympathomimetic alpha-adrenergic agonist that acts on alpha-1 receptors in the conjunctival blood vessels. This causes vasoconstriction, reducing ocular redness and hyperemia.
Pheniramine Maleate is a first-generation H1 histamine receptor antagonist. It competitively blocks histamine at H1 receptors in the eye, reducing allergic symptoms like itching, burning, and watering. The combination rapidly relieves both vascular congestion and histamine-mediated allergic responses in the conjunctiva.

• Absorption:
• Naphazoline: Partially absorbed through the conjunctival mucosa.
• Pheniramine: Minimal systemic absorption after topical application.
• Onset of Action:
• Begins within 5–10 minutes of instillation.
• Duration of Action:
• Relief lasts for 4–6 hours.
• Distribution:
• Limited systemic distribution due to local topical use.
• Metabolism:
• Naphazoline undergoes hepatic metabolism.
• Pheniramine is also primarily metabolized in the liver if absorbed.
• Excretion:
• Excreted renally (mostly as metabolites, in negligible systemic quantities).

• Pregnancy:
• FDA Category C (Naphazoline)
• Insufficient human data available. Use only if clearly needed.
• Pheniramine may cross the placenta; caution advised during pregnancy.
• Lactation:
• Unknown whether these drugs are excreted in breast milk.
• Caution recommended if used during breastfeeding. Monitor infants for sedation or irritability.

• Primary Therapeutic Class:
• Ophthalmic Anti-Allergic + Ocular Decongestant
• Components:
• Naphazoline: Alpha-adrenergic vasoconstrictor
• Pheniramine: First-generation H1 antihistamine

• Hypersensitivity to naphazoline, pheniramine, or any ingredient in the formulation
• Narrow-angle (angle-closure) glaucoma
• Concurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping them
• Severe cardiovascular disease
• Children under 6 years without medical supervision

• Limit Duration of Use:
• Do not use for more than 72 hours continuously due to risk of rebound hyperemia and tachyphylaxis.
• Systemic Absorption Risk:
• Excessive or frequent use may lead to CNS depression (especially in children) or cardiovascular changes (e.g., bradycardia, hypertension).
• Use in Glaucoma Patients:
• May increase intraocular pressure; contraindicated in narrow-angle glaucoma.
• Drowsiness/CNS Effects:
• Pheniramine may cause sedation or dizziness if absorbed systemically.
• Use with Caution in Elderly:
• Higher risk of anticholinergic and cardiovascular adverse effects.

Common (Mild):

• Transient burning or stinging sensation
• Blurred vision immediately after application
• Ocular dryness or discomfort
• Mild eye redness (rebound hyperemia with prolonged use)

Less Common / Serious:

• Eye pain or persistent irritation
• CNS depression in children (lethargy, drowsiness, hypotonia)
• Cardiovascular effects (palpitations, elevated blood pressure)
• Allergic reactions (eyelid edema, rash, itching)

• Monoamine Oxidase Inhibitors (MAOIs):
• May cause hypertensive crisis due to potentiation of vasoconstrictor effects.
• Tricyclic Antidepressants:
• Additive anticholinergic and sympathomimetic effects.
• CNS Depressants (e.g., alcohol, sedatives, opioids):
• May enhance CNS depression when combined with pheniramine.
• Antihypertensives:
• Interaction potential due to vasoconstrictor effects of naphazoline.
• Enzyme Systems:
• No significant involvement of CYP450 enzymes at therapeutic ophthalmic doses.

• Label Enhancements:
• Warnings have been updated regarding safe use in children and risk of rebound congestion.
• Use Duration Recommendations:
• International guidelines (e.g., FDA, NICE) emphasize limiting use to ≤3 days to prevent tolerance and adverse effects.
• Ophthalmic Safety Recommendations:
• Eye care professionals now recommend careful use in patients with glaucoma, hypertension, or elderly patients.

• Recommended Temperature:
• Store between 15°C to 30°C (59°F to 86°F)
• Humidity and Light:
• Protect from excessive moisture and direct sunlight
• Freezing:
• Do not freeze
• Handling Instructions:
• Discard if solution becomes cloudy or changes color
• Do not touch the dropper tip to any surface
• After opening, use within 28 days (check product-specific label)