Introduction
Upneeq (oxymetazoline hydrochloride ophthalmic solution) 0.1% is a novel prescription eye drop approved by the FDA in 2020 for the treatment of acquired ptosis (drooping eyelids) in adults. It represents the first and only pharmacologic treatment specifically indicated for this condition, offering a non-invasive alternative to surgical intervention.
Mechanism of Action
Upneeq contains oxymetazoline hydrochloride, a selective alpha-adrenergic receptor agonist. When applied topically to the eye, it acts on Müller's muscle, a smooth muscle component of the upper eyelid. Stimulation of alpha-adrenergic receptors causes contraction of Müller's muscle, resulting in elevation of the upper eyelid by approximately 1-2 mm. The effect is temporary and reversible, typically lasting 6-8 hours after administration.
Indications
FDA-approved for the treatment of acquired ptosis in adults. Acquired ptosis includes:
- Involutional ptosis (age-related)
- Aponeurotic ptosis
- Not indicated for congenital ptosis or ptosis associated with neurological disorders
Dosage and Administration
Standard dosing: One drop applied to the affected eye(s) once daily Administration: Instill while looking downward, pulling down the lower eyelid to form a pouch Timing: Typically administered in the morning Special populations:- Renal impairment: No dosage adjustment necessary
- Hepatic impairment: Use with caution
- Geriatric patients: No dosage adjustment required
- Pediatrics: Safety and effectiveness not established
Pharmacokinetics
Absorption: Minimal systemic absorption following ocular administration Distribution: Primarily local ocular distribution Metabolism: Hepatic metabolism via oxidative mechanisms Elimination: Renal excretion of metabolites Half-life: Approximately 5-7 hours systemically (though local effects are shorter)Contraindications
- Hypersensitivity to oxymetazoline or any component of the formulation
- Patients with narrow-angle glaucoma
- Patients taking monoamine oxidase inhibitors (MAOIs)
- History of orthostatic hypotension
- Severe cardiovascular disease
Warnings and Precautions
- May cause increased blood pressure - use caution in hypertensive patients
- Potential for rebound redness or conjunctival hyperemia with prolonged use
- Risk of angle-closure glaucoma in susceptible individuals
- May cause pupillary dilation
- Use with caution in patients with cerebral or coronary insufficiency
- Potential for systemic adrenergic effects
Drug Interactions
Significant interactions:- MAO inhibitors: Increased pressor effects
- Tricyclic antidepressants: Potentiated pressor response
- Beta-blockers: Potential paradoxical hypertension
- Other sympathomimetic drugs: Additive effects
- Clinical significance: Monitor blood pressure when used concomitantly with these agents
Adverse Effects
Common (≥2%):- Conjunctival hyperemia (15%)
- Instillation site pain (7%)
- Dry eye (5%)
- Blurred vision (4%)
- Headache (3%)
- Acute angle-closure glaucoma
- Significant hypertension
- Cardiac arrhythmias
- Allergic reactions
Monitoring Parameters
- Eyelid position and symmetry at baseline and during treatment
- Intraocular pressure (particularly in glaucoma suspects)
- Blood pressure (especially in hypertensive patients)
- Visual acuity changes
- Signs of ocular irritation or allergic reaction
- Pupillary responses
Patient Education
- Administer only one drop per affected eye once daily
- Remove contact lenses before instillation and wait 10 minutes before reinserting
- Do not touch dropper tip to any surface to avoid contamination
- Effects typically begin within 5 minutes and peak at 2 hours
- Duration of effect is approximately 6-8 hours
- Report any eye pain, vision changes, or persistent redness
- Inform all healthcare providers about Upneeq use
- Store at room temperature (20-25°C)
References
1. FDA Prescribing Information: Upneeq (oxymetazoline hydrochloride ophthalmic solution) 0.1%. 2020. 2. Wirta D, et al. Oxyamphetamine hydrochloride for the treatment of acquired ptosis. American Journal of Ophthalmology. 2020;218:1-9. 3. Slonim CB, et al. Phase 3 clinical trial of oxymetazoline hydrochloride for the treatment of acquired blepharoptosis. Clinical Ophthalmology. 2020;14:3033-3043. 4. Goldberg RA, et al. Current trends in the management of ptosis. Ophthalmic Plastic and Reconstructive Surgery. 2021;37(1):1-7. 5. American Academy of Ophthalmology. Preferred Practice Pattern: Ptosis. 2022.