• Miscellaneous ocular agents

Upneeq Generic Name & Formulations

General Description

Oxymetazoline HCL 0.1%; oph soln; preservative-free.

Pharmacological Class


How Supplied

Single patient-use containers—15, 30


Store at 20°C to 25°C (68°F to 77°F). 

Protect from excessive heat.

Store single patient-use containers in the child-resistant foil pouches. 

Discard opened containers immediately after use.

Generic Availability


Upneeq Indications


Acquired blepharoptosis.

Upneeq Dosage and Administration


Instill one drop into one or both ptotic eye(s) once daily.


<13yrs: not established.

Upneeq Contraindications

Not Applicable

Upneeq Boxed Warnings

Not Applicable

Upneeq Warnings/Precautions


Ptosis with decreased levator muscle function and/or other neurologic signs. Severe or unstable/uncontrolled cardiovascular disease. Orthostatic hypotension. Uncontrolled hypertension or hypotension. Cerebral or coronary insufficiency. Sjögren's syndrome. Increased risk of angle closure glaucoma. Contact lenses (remove; may reinsert 15mins after administration). Pregnancy. Nursing mothers.

Pregnancy Considerations

There are no available data on Upneeq use in pregnant women.

Nursing Mother Considerations

No clinical data available to assess the effects of oxymetazoline on breastmilk production, or to establish the level of oxymetazoline present in human breastmilk. Consider the benefits to the mother vs the potential risks to the breastfed child.

Pediatric Considerations

Safety and effectiveness of Upneeq have not been established in pediatric patients under 13 years of age. 

Geriatric Considerations

No overall differences in safety or effectiveness observed between patients 65 years and older and younger patients.

Upneeq Pharmacokinetics


Following ocular administration, time to reach peak oxymetazoline concentration (Tmax) values ranged from 0.5 to 12 hours with a median Tmax of 2 hours.




Half-life: 8.3 hours (range: 5.6–13.9 hours).

Upneeq Interactions


Caution with concomitant beta-blockers, antihypertensives, cardiac glycosides, alpha-1 receptor antagonists. Concomitant MAOIs may affect the metabolism and uptake of circulating amines; caution. Allow ≥15mins between dosing of other ophthalmic drugs.

Upneeq Adverse Reactions

Adverse Reactions

Punctate keratitis, conjunctival hyperemia, dry eye, vision blurred, instillation site pain, eye irritation, headache.

Upneeq Clinical Trials

Clinical Trials

Approval was based on data from 2 double-masked, vehicle-controlled, parallel-group phase 3 trials (Trial 1 and Trial 2) that evaluated the efficacy and safety of Upneeq in 304 patients with acquired blepharoptosis. Patients were randomly assigned 2:1 to receive Upneeq once daily or vehicle for 42 days. 

The primary endpoint was the mean change from baseline in the number of points seen on the Leicester Peripheral Field Test in the study eye at hour 6 on day 1 and hour 2 on day 14. A secondary end point included the change from baseline in marginal reflex distance 1 (MRD1).

In both studies, improvement in superior visual field was observed with Upneeq at the 2-hour time point and maintained at the 6-hour time point. Results from Trial 1 (N=140) showed that Upneeq met the primary endpoint demonstrating a statistically significant improvement at hour 6 on day 1 (mean difference 3.7; 95% CI, 1.8-5.6; P <.01) and at hour 2 on day 14 (mean difference 4.2; 95% CI, 2.0-6.0; P <.01) vs vehicle. 

Additionally, statistically significant improvements in the Upneeq treatment arm were noted in Trial 2 (N=164) at hour 6 on day 1 (mean difference 4.2; 95% CI, 2.4-6.1; P <.01) and at hour 2 on day 14 (mean difference 5.3; 95% CI, 3.7-7.1; P <.01) vs vehicle. Both studies demonstrated greater MRD1 increases at both time points vs vehicle.

Upneeq Note

Not Applicable

Upneeq Patient Counseling

Patient Counseling

Contact lenses: Remove prior to administration; reinsert 15 minutes after administration.

Allow 15 minutes between applications of other ophthalmic drugs.

Upon opening, use the single patient-use container immediately; any remaining contents should be discarded after administration.

Do not touch the tip of the container to the eye or to any surface.

Consideration should be given to neurologic or orbital diseases (egg, stroke and/or cerebral aneurysm, Horner syndrome, myasthenia gravis, external ophthalmoplegia, orbital infection and orbital masses) in the presence of ptosis with decreased levator muscle function and/or other neurologic signs.

Patients with cardiovascular disease, orthostatic hypotension, and/or uncontrolled hypertension or hypotension: Alpha-adrenergic agonists may impact blood pressure.