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Oxymetazoline (ophthalmic): Drug information

Oxymetazoline (ophthalmic): Drug information
(For additional information see "Oxymetazoline (ophthalmic): Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Upneeq
Pharmacologic Category
  • Imidazoline Derivative;
  • Vasoconstrictor
Dosing: Adult
Blepharoptosis

Blepharoptosis: Ophthalmic: Instill 1 drop in affected eye(s) once daily.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic, as hydrochloride [preservative free]:

Upneeq: 0.1% (30 ea, 45 ea)

Generic Equivalent Available: US

No

Administration: Adult

Ophthalmic: For ophthalmic use only. Remove contact lenses before use; after instilling drops, wait at least 15 minutes before inserting. Instill into lower eyelid immediately after opening container; discard any unused portion. Do not touch tip of container to eye or any surface. Allow 15 minutes between application of other ophthalmic agents.

Use: Labeled Indications

Blepharoptosis: Treatment of acquired blepharoptosis in adults.

Medication Safety Issues
Sound-alike/look-alike issues:

Oxymetazoline may be confused with oxymetholone.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10:

Local: Application site pain (1% to 5%)

Nervous system: Headache (1% to 5%)

Ophthalmic: Blurred vision (1% to 5%), conjunctival hyperemia (1% to 5%), dry eye syndrome (1% to 5%), eye irritation (1% to 5%), punctate keratitis (1% to 5%)

Frequency not defined: Nervous system: Transient burning or stinging in the eyes

Contraindications

There are no contraindications listed in the manufacturer's labeling.

Documentation of allergenic cross-reactivity for ophthalmic sympathomimetics is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Warnings/Precautions

Concerns related to adverse effects:

• Ptosis: Ptosis associated with neurologic (eg, cerebral aneurysm, Horner syndrome, myasthenia gravis, stroke) or orbital disease (eg, external ophthalmoplegia, orbital infection, orbital masses) may occur. Evaluate patients who develop ptosis, especially in presence of decreased levator muscle function and/or other neurologic signs.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with severe or unstable cardiovascular disease including orthostatic hypotension, uncontrolled hypertension, or uncontrolled hypotension; advise patients to contact health care provider if condition worsens.

• Glaucoma: Use with caution in patients with untreated narrow-angle glaucoma; advise patients to contact health care provider if signs and symptoms occur.

• Vascular disease: Use with caution in patients with cerebral insufficiency, coronary insufficiency, or Sjögren syndrome; advise patients to contact health care provider if signs and symptoms of vascular insufficiency occur.

Other warnings/precautions:

• Appropriate use: For topical ophthalmic use only. To avoid contamination, do not touch tip of container to any surface.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies (studies conducted with oral oxymetazoline).

If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988).

Breastfeeding Considerations

It is not known if oxymetazoline is present in breast milk following ophthalmic administration.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Mechanism of Action

Stimulates alpha-adrenergic receptors in the Müller's muscle of the eyelid.

Pharmacokinetics

Protein binding: ~57%.

Metabolism: Hepatic: Minimally to mono-oxygenated and dehydrogenated products of oxymetazoline.

Half-life elimination: Terminal: 8.3 hours (range: 5.6 to 13.9 hours).

Time to peak: Median: 2 hours (range: 0.5 to 12 hours).

Pricing: US

Solution (Upneeq Ophthalmic)

0.1% (per each): $8.33

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Afrin (AE);
  • Alerfrin (ES);
  • Alosol (AR);
  • Clarivis (PE);
  • Clarix (VE);
  • Iliadin (CL);
  • Oftinal (ES);
  • Oxilin (IT);
  • Oxylin (CN, IN, NL, ZA)


For country code abbreviations (show table)
  1. Samples JR, Meyer SM. Use of ophthalmic medications in pregnant and nursing women. Am J Ophthalmol. 1988;106(5):616-623. doi:10.1016/0002-9394(88)90597-1 [PubMed 2903673]
  2. Upneeq (oxymetazoline) [prescribing information]. Bridgewater, NJ: RVL Pharmaceuticals Inc; October 2021.
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