oxymetazoline ophthalmic (Rx)

Brand and Other Names:Upneeq
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Dosing & Uses

AdultPediatric

Dosing Form & Strengths

ophthalmic solution

  • 0.1% (as HCl salt [0.09% as base])

Blepharoptosis

Indicated for acquired blepharoptosis in adults

Instill 1 gtt to affected eye(s) qDay

Safety and efficacy not established

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Interactions

Interaction Checker

and oxymetazoline ophthalmic

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            1-10%

            Punctate keratitis (1-5%)

            Conjunctival hyperemia (1-5%)

            Dry eye (1-5%)

            Blurred vision (1-5%)

            Instillation site pain (1-5%)

            Eye irritation (1-5%)

            Headache (1-5%)

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            Warnings

            Contraindications

            None

            Cautions

            Alpha-adrenergic agonists may impact blood pressure; caution with severe or unstable cardiovascular disease, orthostatic hypotension, and uncontrolled hypertension or hypotension

            Caution with cerebral insufficiency, coronary insufficiency, or Sjögren syndrome

            May increase risk of angle-closure glaucoma in patients with untreated narrow-angle glaucoma

            Advise patients to seek medical care if signs and symptoms of cardiovascular disease, vascular insufficiency, or acute angle-closure glaucoma develop

            Ptosis may be associated with neurologic or orbital diseases such as stroke and/or cerebral aneurysm, Horner syndrome, myasthenia gravis, external ophthalmoplegia, orbital infection and orbital masses; give consideration to these conditions in the presence of ptosis with decreased levator muscle function and/or other neurologic signs

            Drug interaction overview

            • Alpha-adrenergic agonists, as a class, may impact blood pressure; caution if coadministered with beta-blockers, antihypertensives, and/or cardiac glycosides
            • Caution in patients taking MAO inhibitors, which can affect metabolism and uptake of circulating amines
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            Pregnancy & Lactation

            Pregnancy

            Data are not available regarding use during pregnancy to inform a drug-associated risk for major birth defects and miscarriage

            Animal studies

            • No adverse developmental effects observed after oral administration in pregnant rats and rabbits at systemic exposures up to 7 and 278 times the maximum recommended human ophthalmic dose

            Lactation

            Data are unavailable to assess effects on breastmilk quantity or production, or to establish the level of oxymetazoline present in human breastmilk

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Alpha-adrenergic agonist

            Targets a subset of adrenoreceptors in Mueller muscle of the eyelid for use to treat acquired blepharoptosis

            Absorption

            Ocular administration

            • Peak plasma time: 2 hr
            • Peak plasma concentration: 30.5 pg/mL
            • AUC: 468 pghr/mL

            Distribution

            Protein bound: 56.7-57.5%

            Metabolism

            Minimally metabolized; 95.9% of parent compound remained after 120-minute incubation with human liver microsomes

            Elimination

            Half-life: 8.3 hr

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            Administration

            Ophthalmic Administration

            Do not touch tip of applicator to eye or any surface, in order to avoid eye injury or contamination of ophthalmic solution

            Remove contact lenses before instilling drops; may reinsert 15 minutes after administration

            If >1 ophthalmic preparation administered, separate instillation by at least 15 minutes

            Discard single-use container immediately after dosing

            Storage

            Store foil-pouched single patient-use containers in the original child-resistant zipper bag

            Store at 20-25ºC (68-77ºF); protect from excessive heat

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.