Upneeq®
Oxymetazoline 0.1% · ophthalmic solution
Aesthetics/Presbyopia
Approved uses
Acquired blepharoptosis
1 drop into one or both ptotic eyes once daily
Lid elevation is measurable at 5 minutes, peaks near 2 hours, and persists through 8 hours.
OFF-LABELNot in the FDA label for this product
Ptosis of ocular myasthenia gravis
1 drop in the ptotic eye once daily, the labeled frequency
Case report
Single case report, one 68-year-old patient: one drop raised MRD1 by 2.0 mm and gained 15 points on a superior 36-point field screening within 2 hours, with the effect lasting at least 7 hours. The untreated contralateral lid fell, which the authors suggest may be specific to myasthenia. N of 1, no controlled data.
Cosmetic eyelid elevation and conjunctival redness in patients without severe ptosis
1 drop in each eye once daily, the labeled frequency
RCT · n=114 · single dose
Randomized double-masked single-center trial, N=114 (57 treated, 57 control), mean ages 36 and 31: two hours after one drop, MRD1 changed 0.9 mm versus -0.3 mm with placebo (p<0.001) and redness scores fell 2.6 versus 0.5 (p=0.002), with better patient-perceived appearance (p=0.002). Adverse events were all mild and did not differ between groups; the trial measured a single instillation, not chronic use.
Contraindications
None.
Available FormsOphthalmic solution, carton of 30 single patient-use containers, 0.3 mL each, oxymetazoline HCl 0.1% (1 mg/mL, equivalent to 0.09% oxymetazoline base)
Mechanism of ActionAlpha adrenoceptor agonist acting on a subset of adrenoreceptors in Müller's muscle of the eyelid. Marginal reflex distance 1 reaches its maximum increase about 2 hours after dosing and the increase continues through 8 hours.
Warnings & Precautions
- Ptosis from neurologic disease: Rule out stroke, cerebral aneurysm, Horner syndrome, myasthenia gravis, external ophthalmoplegia, orbital infection, and orbital masses, particularly with decreased levator function or other neurologic signs.
- Cardiovascular effects: Alpha-adrenergic agonists may impact blood pressure; caution in severe or unstable cardiovascular disease, orthostatic hypotension, and uncontrolled hypertension or hypotension.
- Vascular insufficiency: Caution in cerebral or coronary insufficiency and in Sjögren's syndrome; watch for signs of potentiation.
- Angle closure glaucoma: Risk may increase in untreated narrow-angle glaucoma; pain, redness, blurred vision, and photophobia warrant immediate evaluation.
- Container contamination: Tip contact with the eye or any surface risks injury and contamination of this unpreserved solution.
- Antihypertensives and cardiac glycosides: Caution with beta-blockers, antihypertensives, cardiac glycosides, and alpha-adrenergic antagonists used for cardiovascular disease or benign prostatic hypertrophy.
- MAO inhibitors: Caution, since they affect the metabolism and uptake of circulating amines.
- Pediatric ingestion: Accidental oral ingestion of imidazolines by children has caused hospitalization, including bradycardia, hypotension, sedation, and coma.
Common Side Effects
- Ocular (1-5%): Punctate keratitis, conjunctival hyperemia, dry eye, blurred vision, instillation site pain, eye irritation.
- Systemic (1-5%): Headache.
Pregnancy & LactationPregnancy: No human data. No adverse developmental effects in rats or rabbits at up to 7 and 278 times the maximum recommended human ophthalmic dose respectively; maternal toxicity with delayed skeletal ossification occurred at the highest rabbit dose.
Lactation: No human data on milk levels or milk production; oxymetazoline was detected in the milk of lactating rats.
Pediatric UseSafety and effectiveness not established under 13 years of age.