Dosing and uses of Simbrinza (brinzolamide/brimonidine)
Adult dosage forms and strengths
brinzolamide/brimonidine
ophthalmic suspension
- 1%/0.2%
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
Pediatric dosage forms and strengths
brinzolamide/brimonidine
ophthalmic suspension
- 1%/0.2%
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
Simbrinza (brinzolamide/brimonidine) adverse (side) 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
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
Pregnancy and 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.
Pharmacology of Simbrinza (brinzolamide/brimonidine)
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)
