Zocare

Ophthalmic Use:

• Allergic Conjunctivitis: Relief of ocular symptoms such as redness, itching, and watering associated with seasonal or perennial allergic conjunctivitis.
• Nonspecific Irritative Conjunctivitis: For temporary relief of minor eye irritation caused by wind, dust, pollen, smoke, or light exposure.
• Viral Conjunctivitis (supportive use): Though not antiviral, used to relieve symptomatic eye redness and discomfort in some viral conjunctivitis cases (off-label and supportive only).

Adults and Elderly:

• Usual Dose: 1–2 drops in the affected eye(s) up to 4 times daily.
• Route: Ophthalmic (topical, eye drops only).
• Duration: Short-term use only (ideally not exceeding 3–5 days due to risk of rebound hyperemia).

Pediatric Use:

• Children ≥6 years: 1 drop in affected eye(s) 2–3 times daily under medical supervision.
• Children <6 years: Use not routinely recommended; consult physician.

Special Populations:

• Renal/Hepatic Impairment: No dose adjustment required; systemic absorption is minimal.
• Contact Lens Wearers: Remove lenses before administration. Wait at least 15 minutes before reinsertion.

Antazoline is a first-generation antihistamine that acts as an H1 receptor antagonist. It stabilizes conjunctival mast cells and prevents histamine-mediated responses such as vasodilation, increased vascular permeability, and sensory nerve activation, thereby reducing redness, itching, and tearing.
Tetryzoline is a selective alpha-adrenergic agonist with vasoconstrictive action. It reduces conjunctival congestion and hyperemia by constricting arterioles in the eye, thereby relieving redness. The combination offers rapid symptomatic relief from both allergic and irritative stimuli.

• Absorption: Minimal systemic absorption when applied topically to the eye.
• Distribution: Largely confined to ocular tissues; negligible systemic distribution.
• Metabolism: Antazoline undergoes hepatic metabolism if systemically absorbed; Tetryzoline is minimally metabolized.
• Elimination: Excreted via renal route if absorbed; mostly excreted unchanged.
• Onset of Action: Within minutes of administration.
• Duration of Effect: 4–6 hours for both agents.

• Pregnancy: Data in pregnant women are limited. Antazoline and Tetryzoline should be used during pregnancy only if clearly needed. No well-controlled human studies available.
• Lactation: It is unknown whether Antazoline or Tetryzoline is excreted in human breast milk. Systemic exposure is low, but caution is advised, especially with repeated or long-term use.
• Recommendation: Use only under healthcare provider supervision during pregnancy and lactation.

• Primary Class: Ophthalmic Antiallergic and Vasoconstrictor Combination.
• Subclasses:
• Antazoline – First-generation H1-antihistamine
• Tetryzoline – Ocular decongestant (Alpha-adrenergic agonist)

• Known hypersensitivity to Antazoline, Tetryzoline, or any excipients in the formulation.
• Narrow-angle glaucoma.
• Severe cardiovascular disease (caution due to alpha-adrenergic effects).
• Patients taking monoamine oxidase inhibitors (MAOIs).
• Children under 6 years (relative contraindication due to lack of safety data).

• Rebound Hyperemia: Prolonged use (>5 days) may result in rebound redness and chronic vasodilation.
• Intraocular Pressure: Use with caution in patients with glaucoma.
• Systemic Absorption Risk: Excessive dosing may result in systemic sympathomimetic effects (especially in children).
• Elderly Patients: Increased susceptibility to side effects such as eye dryness or irritation.
• Monitoring: Regular ophthalmologic evaluation if used beyond a few days.

Common (Ocular):

• Transient burning or stinging sensation
• Eye dryness
• Blurred vision
• Mydriasis (pupil dilation)

Less Common:

• Eye redness (rebound)
• Increased lacrimation (watery eyes)
• Headache

Rare but Serious:

• Tachycardia, hypertension (with systemic absorption)
• CNS effects: Drowsiness, irritability (especially in children)
• Allergic reactions: Eyelid swelling, dermatitis

• MAO Inhibitors: May potentiate the vasoconstrictive effects of Tetryzoline, leading to hypertensive crisis.
• CNS Depressants: Antazoline may enhance sedative effects if absorbed systemically.
• Adrenergic Agonists: Risk of additive cardiovascular effects.
• Contact Lens Absorption: Benzalkonium chloride (preservative) may be absorbed by soft lenses—remove lenses before use.

• No major changes in formulation or regulatory guidelines in recent years.
• Continuing caution advised regarding over-the-counter use beyond 72 hours without physician supervision.
• EMA and FDA continue to recommend short-term symptomatic use only due to risk of rebound hyperemia and sensitization.

• Temperature: Store below 25°C. Do not freeze.
• Humidity/Light: Protect from excessive heat, light, and moisture.
• Handling: Keep bottle tightly closed. Avoid contamination of dropper tip.
• Shelf-life After Opening: Discard 28 days after opening unless otherwise specified by the manufacturer.