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Oxymetazoline (Ophthalmic)

Medically reviewed by Drugs.com. Last updated on Apr 22, 2020.

Pronunciation

(oks i met AZ oh leen)

Index Terms

  • Oxymetazoline HCl
  • Oxymetazoline Hydrochloride
  • Upneeq

Dosage Forms

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

Solution, Ophthalmic, as hydrochloride [preservative free]:

Upneeq: 0.1% (30 ea)

Brand Names: U.S.

  • Upneeq

Pharmacologic Category

  • Imidazoline Derivative
  • Vasoconstrictor

Pharmacology

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

Metabolism

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

Time to Peak

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

Half-Life Elimination

Terminal: 8.3 hours (range: 5.6 to 13.9 hours).

Protein Binding

~57%.

Use: Labeled Indications

Blepharoptosis: Treatment of acquired blepharoptosis in adults.

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.

Dosing: Adult

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

Dosing: Geriatric

Refer to adult dosing.

Administration

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.

Storage

Store single-use patient containers in original child-resistant foil pouches at 20°C to 25°C (68°F to 77°F). Protect from heat. After opening patient-use container, discard any unused portion.

Drug Interactions

There are no known significant interactions.

Adverse Reactions

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

Warnings/Precautions

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.

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).

Patient Education

What is this drug used for?

• It is used to treat a drooping eyelid.

Frequently reported side effects of this drug:

• Dry eyes

• Eye pain, redness, or other irritation

• Headache

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Change in eyesight

• High or low blood pressure like very bad headache or dizziness, passing out, or change in eyesight

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.