Upneeq
Upneeq
Generic Name
Upneeq
Mechanism
- α₂‑adrenergic receptor activation on the iris dilator muscle triggers a cascade that increases phosphorylase activity, leading to relaxation of the circular iris sphincter and contraction of the dilator.
- The drug also exerts modest α₁‑adrenergic activity, contributing to vasoconstriction of ocular blood vessels and mild intraocular pressure (IOP) reduction.
- Result: pharmacologic mydriasis lasting several hours, suitable for surgical preparation and cosmetic permanent dilation.
Pharmacokinetics
| Parameter | Key Findings |
| Absorption | Corneal penetration is efficient; aqueous humor concentration reaches ~0.2 µg/mL within 30 min. |
| Distribution | Primarily local; minimal systemic absorption after topical instillation. |
| Metabolism | Local catabolism by aqueous humor enzymes into inactive metabolites. |
| Elimination | Excreted via tear film and conjunctival drainage; negligible systemic exposure. |
| Half‑life | Local ocular half‑life ~2–3 h; effect persists up to 6–8 h. |
Indications
- Permanent cosmetic pupil dilation: Patients seeking a self‑sustained dilated pupil for aesthetic reasons (e.g., for photographic portraits).
- Ophthalmic surgical pupil dilation:
- Anterior segment surgeries (e.g., cataract extraction, corneal grafts).
- Prevention of postoperative mydriasis and iris hypodysfunction.
- Reduction of IOP in selected cases.
Contraindications
- Contraindications
- Angle‑closure glaucoma: risk of precipitating acute closure by excessive dilation.
- Irregular pupil or orbital trauma: may exacerbate discomfort or damage.
- Known hypersensitivity to apraclonidine or excipients (e.g., benzethonium chloride).
- Warnings
- First‑time users may experience transient hyperemia and anisocoria; counsel on expected ocular irritation.
- Systemic effects are rare but include mild tachycardia or blood pressure changes if absorbed.
- Use with caution in patients with systemic adrenergic disorders (e.g., pheochromocytoma).
Dosing
- Typical dose: 6–7.5 µL (≈1 drop) of 1 % apraclonidine solution per eye.
- Timing
- Surgical use: Instill 45 min before the procedure.
- Cosmetic use: Single dose; effect may last up to 8 h, with gradual fading over 1–3 months.
- Technique
- Rinse eye with saline afterward if spillage occurs.
- Avoid contact with eyelids or eyelashes to prevent irritation.
Adverse Effects
| Category | Adverse Effect |
| Common |
• Burning, stinging, tearing (≤35%) • Mild blurred vision (≈10%) • Light syncope due to transient blood‑pressure drop (≈2%) |
| Serious |
• Acute angle‑closure crisis (rare – <0.01%) • Optic nerve compression in narrow-angle patients (≤0.001%) • Severe ocular irritation leading to corneal abrasion ( <0.01%) |
Monitoring
- Baseline and postoperative IOP: keep within safe limits (≤21 mmHg).
- Pupil size/circularity: monitor for anisocoria or over‑dilation.
- Visual acuity and oculomotor function: reassess at 24 h and weekly for cosmetic patients.
- Patient symptom diary: report persistent burning, foreign‑body sensation, or vision changes promptly.
Clinical Pearls
- Patient selection matters: Exclude those with narrow angles, recent ocular surgeries, or ocular surface disease to reduce risk of angle‑closure or corneal toxicity.
- Avoid over‑dilation: Use the minimal effective dose (1 drop) and monitor ocular pressure; consider a second dose if the pupil does not achieve adequate dilation after 30 min.
- Cosmetic longevity: Patients with malignant melanoma of the iris or developed cataract may experience rapid fading; counsel accordingly.
- Adherence to wearing sunglasses: After cosmetic use, recommend UV protection for the first 24 h to reduce photophobia from the dilated pupil.
- Rare systemic absorption: In patients on beta‑blockers or antihypertensives, be vigilant for oral or cardiovascular side effects; use a low‑dose ophthalmic formulation.
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• Upneeq is a valuable addition to the ophthalmic armamentarium, offering precise control over pupil size with minimal systemic exposure when administered correctly.