brinzolamide/brimonidine (Rx)

Brand and Other Names:Simbrinza
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

brinzolamide/brimonidine

ophthalmic suspension

  • 1%/0.2%
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Glaucoma

Indicated for reduction of elevated intraocular pressure in patients with primary open-angle glaucoma

Instill 1 gtt in affected eye(s) TID

Ocular Hypertension

Indicated for reduction of elevated intraocular pressure in patients with ocular hypertension

Instill 1 gtt in affected eye(s) TID

Administration

Shake well before use

If more than 1 ophthalmic drop is administered, the drugs should be administered at least 5 minutes apart

Dosage Forms & Strengths

brinzolamide/brimonidine

ophthalmic suspension

  • 1%/0.2%
more...

Glaucoma

Indicated for reduction of elevated intraocular pressure in patients with primary open-angle glaucoma

<2 years: Safety and efficacy not established

≥2 years: Instill 1 gtt in affected eye(s) TID

Ocular Hypertension

Indicated for reduction of elevated intraocular pressure in patients with ocular hypertension

<2 years: Safety and efficacy not established

≥2 years: Instill 1 gtt in affected eye(s) TID

Administration

Shake well before use

If more than 1 ophthalmic drop is administered, the drugs should be administered at least 5 minutes apart

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Interactions

Interaction Checker

and brinzolamide/brimonidine

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10% (brimonidine)

            Somnolence in children (50-83%)

            Xerostomia (10-30%)

            Ocular hyperemia (10-30%)

            Burning and stinging (10-30%)

            Headache (10-30%)

            Blurring (10-30%)

            Foreign body sensation (10-30%)

            Fatigue/drowsiness (10-30%)

            Conjunctival follicles (10-30%)

            Ocular allergic reactions (10-30%)

            Ocular pruritus (10-30%)

            1-10% (brinzolamide)

            Blurred vision (5-10%)

            Dysgeusia (5-10%)

            Blepharitis (1-5%)

            Dermatitis (1-5%)

            Dry eye (1-5%)

            Foreign body sensation (1-5%)

            Headache (1-5%)

            Hyperemia (1-5%)

            Ocular discharge (1-5%)

            Ocular discomfort (1-5%)

            Ocular keratitis (1-5%)

            Ocular pain (1-5%)

            Ocular pruritus (1-5%)

            Rhinitis (1-5%)

            1-10% (brimonidine)

            Corneal staining/erosion (3-9%)

            Photophobia (3-9%)

            Eyelid erythema (3-9%)

            Ocular ache/pain (3-9%)

            Ocular dryness (3-9%)

            Tearing (3-9%)

            Upper respiratory symptoms (3-9%)

            Eyelid edema (3-9%)

            Conjunctival edema (3-9%)

            Dizziness (3-9%)

            Blepharitis (3-9%)

            Ocular (3-9%)

            Irritation (3-9%)

            Gastrointestinal symptoms (3-9%)

            Asthenia (3-9%)

            Conjunctival blanching (3-9%)

            Abnormal vision (3-9%) Muscular pain (3-9%)

            Lid crusting (<3%)

            Conjunctival hemorrhage (<3%)

            Abnormal taste (<3%)

            Insomnia (<3%)

            Conjunctival discharge (<3%)

            Depression (<3%)

            Hypertension (<3%)

            Anxiety (<3%)

            Palpitations/arrhythmias (<3%)

            Nasal dryness (<3%)

            Syncope (<3%)

            <1% (brinzolamide)

            Allergic reactions

            Alopecia

            Chest pain

            Conjunctivitis

            Diarrhea

            Diplopia

            Dizziness

            Dry mouth

            Dyspnea

            Dyspepsia

            Eye fatigue

            Hypertonia

            Keratoconjunctivitis

            Keratopathy

            Kidney pain

            Lid margin crusting or sticky sensation

            Nausea

            Pharyngitis

            Tearing

            Urticaria

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            Warnings

            Contraindications

            Hypersensitivity

            Neonates and infants (younger than 2 yr)

            Cautions

            Contains brinzolamide, a sulfonamide; caution with history of sulfonamide allergy

            Carbonic anhydrase activity observed in both the cytoplasm and around the plasma membranes of the corneal endothelium, and therefore there is an increased potential for developing corneal edema in patients with low endothelial cell counts

            Brinzolamide and its metabolite are excreted predominantly by the kidney and is not recommended in patients with severe renal impairment

            Not studied in patients with acute angle-closure glaucoma

            Contains benzalkonium chloride (preservative); remove contact lenses during instillation to avoid absorption by soft lenses (may reinsert 15 minutes after instillation)

            Brimonidine elicits <5% mean decrease in blood pressure 2 hr after instillation; caution with severe cardiovascular disease

            Not studied with severe hepatic impairment

            Brimonidine may potentiate syndromes associated with vascular insufficiency (eg, depression, cerebral or coronary insufficiency, Raynaud’s phenomenon, orthostatic hypotension, thromboangiitis obliterans)

            Bacterial keratitis reported from inadvertent contamination of multiple-dose containers of topical ophthalmics

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Unknown whether distributed in human breast milk; do not breast feed

            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

            Brinzolamide: Carbonic anhydrase inhibitor; inhibition of carbonic anhydrase in ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport

            Brimonidine: Alpha2 adrenergic receptor agonist; decreases aqueous humor secretion and increases uveoscleral outflow

            Absorption

            Peak plasma time: 1-4 hr (brimonidine)

            Peak plasma concentration: <10 ng/mL (brinzolamide)

            Distribution

            Protein bound: ~60% (brinzolamide)

            Due to its affinity for carbonic anhydrase (CA) II, brinzolamide distributes extensively into RBCs

            Metabolism

            Metabolized by liver (brimonidine)

            Metabolites: N-desethyl brinzolamide

            Elimination

            Half-life: 111 days (brinzolamide); 3 hr (brimonidine)

            Excretion: Predominantly in urine (brinzolamide); 87% urine (brimonidine)

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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.
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            • Compare formulary status to other drugs in the same class.
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            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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