Dosing & Uses
Dosing Forms & Strengths
brinzolamide/brimonidine
ophthalmic suspension
- 1%/0.2%
Open-Angle-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
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%
Open-Angle-Glaucoma
Indicated for reduction of elevated intraocular pressure in patients with primary open-angle glaucoma
<2 years: Contraindicated
≥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: Contraindicated
≥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
Interactions
Interaction Checker
No Results
Contraindicated
Serious
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious (0)
Monitor Closely (14)
- amantadine
brinzolamide will decrease the level or effect of amantadine by Other (see comment). Modify Therapy/Monitor Closely. Excretion rate of amantadine increases rapidly when urine is acidic, administration of urine acidifying drugs may increase elimination of amantadine from the body. Monitor for efficacy of amantadine.
- aspirin
brinzolamide, aspirin. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- aspirin rectal
brinzolamide, aspirin rectal. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- aspirin/citric acid/sodium bicarbonate
brinzolamide, aspirin/citric acid/sodium bicarbonate. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- balsalazide
brinzolamide, balsalazide. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- choline magnesium trisalicylate
brinzolamide, choline magnesium trisalicylate. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- diflunisal
brinzolamide, diflunisal. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- lisdexamfetamine
brinzolamide will increase the level or effect of lisdexamfetamine by passive renal tubular reabsorption - basic urine. Use Caution/Monitor.
- mesalamine
brinzolamide, mesalamine. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- salicylates (non-asa)
brinzolamide, salicylates (non-asa). Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- salsalate
brinzolamide, salsalate. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- sulfasalazine
brinzolamide, sulfasalazine. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
- topiramate
topiramate, brinzolamide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of kidney stone formation.
- willow bark
brinzolamide, willow bark. Either increases levels of the other by Other (see comment). Use Caution/Monitor. Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. CAIs also shift salicylates from plasma to the CNS, leading to potential neurotoxicity.
Minor (9)
- amobarbital
brinzolamide, amobarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- butabarbital
brinzolamide, butabarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- butalbital
brinzolamide, butalbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- ethotoin
brinzolamide, ethotoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- fosphenytoin
brinzolamide, fosphenytoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- pentobarbital
brinzolamide, pentobarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- phenobarbital
brinzolamide, phenobarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- phenytoin
brinzolamide, phenytoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- primidone
brinzolamide, primidone. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
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
Postmarketing Reports
Serious skin and subcutaneous tissue reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN)
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; exercise caution
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
Hypersensitivity reactions
- Formulation contains brinzolamide, a sulfonamide; although administered topically absorbed systemically
- The same types of adverse reactions attributable to sulfonamides may occur with topical administration
- Fatalities have occurred due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias
- Sensitization may recur when sulfonamide is re-administered irrespective of route of administration; if signs of serious reactions or hypersensitivity occur, discontinue use immediately
Pregnancy & Lactation
Pregnancy
There are no adequate and well-controlled studies in pregnant women; therapy should be administered during pregnancy only if potential benefit justifies the potential risk to the fetus
Animal data
- Developmental toxicity studies with brinzolamide in rabbits at oral doses of 1, 3, and 6 mg/kg/day (20, 60, and 120 times recommended human ophthalmic dose) produced maternal toxicity at 6 mg/kg/day and significant increase in the number of fetal variations, such as accessory skull bones, which was only slightly higher than historic value at 1 and 6 mg/kg
- In rats, statistically, decreased body weights of fetuses from dams receiving oral doses of 18 mg/kg/day (180 times the recommended human ophthalmic dose) during gestation were proportional to reduced maternal weight gain, with no statistically significant effects on organ or tissue development. Increases in unossified sternebrae reduced ossification of the skull, and unossified hyoid that occurred at 6 and 18 mg/kg were not statistically significant
- No treatment-related malformations were seen; following oral administration of 14C-brinzolamide 14Cbrinzolamide to pregnant rats, radioactivity was found to cross the placenta and was present in fetal tissues and blood
Lactation
There is no information regarding presence of dapagliflozin in human milk, effects on breastfed infants, or effects on milk production; dapagliflozin is present in milk of lactating rats
Due to species-specific differences in lactation physiology, the clinical relevance of these data are not clear; since human kidney maturation occurs in utero and during first 2 years of life when lactational exposure may occur, there may be risk to developing human kidney
Because of potential for serious adverse reactions in breastfed infants, advise women that use of this medication is not recommended while breastfeeding
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
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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