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 - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (9)
- isocarboxazid
isocarboxazid, brimonidine. Mechanism: unknown. Contraindicated. Contraindicated in mfr prescribing info.
- linezolid
linezolid, brimonidine. Mechanism: unknown. Contraindicated. Contraindicated in mfr prescribing info.
- phenelzine
phenelzine, brimonidine. Mechanism: unknown. Contraindicated. Contraindicated in mfr prescribing info.
- procarbazine
procarbazine, brimonidine. Mechanism: unknown. Contraindicated.
- rasagiline
rasagiline, brimonidine. Mechanism: unknown. Contraindicated. Brimonidine should not be used in patients receiving MAO inhibitors.
- selegiline
selegiline, brimonidine. Mechanism: unknown. Contraindicated. Coadministration is contraindicated.
- selegiline transdermal
selegiline transdermal, brimonidine. Mechanism: unknown. Contraindicated. Contraindicated in mfr prescribing info.
- thalidomide
brimonidine and thalidomide both increase sedation. Contraindicated.
- tranylcypromine
tranylcypromine, brimonidine. Mechanism: unknown. Contraindicated. Contraindicated in mfr prescribing info.
Serious - Use Alternative (19)
- alfentanil
brimonidine and alfentanil both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- buprenorphine
brimonidine and buprenorphine both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- buprenorphine buccal
brimonidine and buprenorphine buccal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- buprenorphine subdermal implant
brimonidine and buprenorphine subdermal implant both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- buprenorphine transdermal
brimonidine and buprenorphine transdermal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- buprenorphine, long-acting injection
brimonidine and buprenorphine, long-acting injection both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- codeine
brimonidine and codeine both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- fentanyl
brimonidine and fentanyl both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- fentanyl intranasal
brimonidine and fentanyl intranasal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- fentanyl iontophoretic transdermal system
brimonidine and fentanyl iontophoretic transdermal system both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- fentanyl transdermal
brimonidine and fentanyl transdermal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- fentanyl transmucosal
brimonidine and fentanyl transmucosal both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- hydrocodone
brimonidine and hydrocodone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- hydromorphone
brimonidine and hydromorphone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- methadone
brimonidine and methadone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- morphine
brimonidine and morphine both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- oxycodone
brimonidine and oxycodone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- oxymorphone
brimonidine and oxymorphone both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
- remifentanil
brimonidine and remifentanil both increase sedation. Avoid or Use Alternate Drug. Limit use to patients for whom alternative treatment options are inadequate
Monitor Closely (173)
- acetaminophen/phenyltoloxamine
brimonidine and acetaminophen/phenyltoloxamine both increase sedation. Use Caution/Monitor.
- acrivastine
acrivastine and brimonidine both increase sedation. Use Caution/Monitor.
- alprazolam
brimonidine and alprazolam both increase sedation. Use Caution/Monitor.
- 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.
- amifostine
amifostine, brimonidine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration with blood pressure lowering agents may increase the risk and severity of hypotension associated with amifostine. When amifostine is used at chemotherapeutic doses, withhold blood pressure lowering medications for 24 hr prior to amifostine; if blood pressure lowering medication cannot be withheld, do not administer amifostine.
- amisulpride
amisulpride and brimonidine both increase sedation. Use Caution/Monitor.
- amitriptyline
brimonidine and amitriptyline both increase sedation. Use Caution/Monitor.
- amobarbital
brimonidine and amobarbital both increase sedation. Use Caution/Monitor.
- amoxapine
brimonidine and amoxapine both increase sedation. Use Caution/Monitor.
- aripiprazole
brimonidine and aripiprazole both increase sedation. Use Caution/Monitor.
- asenapine
asenapine and brimonidine both increase sedation. Use Caution/Monitor.
- asenapine transdermal
asenapine transdermal and brimonidine both increase sedation. Use Caution/Monitor.
- 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.
- avapritinib
avapritinib and brimonidine both increase sedation. Use Caution/Monitor.
brimonidine and avapritinib both increase sedation. Use Caution/Monitor. - baclofen
brimonidine and baclofen both increase sedation. Use Caution/Monitor.
- 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.
- benzhydrocodone/acetaminophen
benzhydrocodone/acetaminophen and brimonidine both increase sedation. Use Caution/Monitor.
- brexanolone
brimonidine and brexanolone both increase sedation. Use Caution/Monitor.
- brexpiprazole
brexpiprazole and brimonidine both increase sedation. Use Caution/Monitor.
brimonidine and brexpiprazole both increase sedation. Use Caution/Monitor. - brivaracetam
brimonidine and brivaracetam both increase sedation. Use Caution/Monitor.
brivaracetam and brimonidine both increase sedation. Use Caution/Monitor. - brompheniramine
brimonidine and brompheniramine both increase sedation. Use Caution/Monitor.
- buprenorphine subdermal implant
buprenorphine subdermal implant and brimonidine both increase sedation. Use Caution/Monitor.
- butabarbital
brimonidine and butabarbital both increase sedation. Use Caution/Monitor.
- butalbital
brimonidine and butalbital both increase sedation. Use Caution/Monitor.
- butorphanol
brimonidine and butorphanol both increase sedation. Use Caution/Monitor.
- candesartan
brimonidine increases effects of candesartan by pharmacodynamic synergism. Use Caution/Monitor.
- carbinoxamine
brimonidine and carbinoxamine both increase sedation. Use Caution/Monitor.
- cariprazine
brimonidine and cariprazine both increase sedation. Use Caution/Monitor.
- carisoprodol
brimonidine and carisoprodol both increase sedation. Use Caution/Monitor.
- cenobamate
brimonidine and cenobamate both increase sedation. Use Caution/Monitor.
- cetirizine
brimonidine and cetirizine both increase sedation. Use Caution/Monitor.
- chlordiazepoxide
brimonidine and chlordiazepoxide both increase sedation. Use Caution/Monitor.
- chlorpheniramine
brimonidine and chlorpheniramine both increase sedation. Use Caution/Monitor.
- chlorpromazine
brimonidine and chlorpromazine both increase sedation. Use Caution/Monitor.
- chlorzoxazone
brimonidine and chlorzoxazone both increase sedation. Use Caution/Monitor.
- 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.
- clemastine
brimonidine and clemastine both increase sedation. Use Caution/Monitor.
- clobazam
brimonidine and clobazam both increase sedation. Use Caution/Monitor.
- clomipramine
brimonidine and clomipramine both increase sedation. Use Caution/Monitor.
- clonazepam
brimonidine and clonazepam both increase sedation. Use Caution/Monitor.
- clonidine
brimonidine and clonidine both increase sedation. Use Caution/Monitor.
- clorazepate
brimonidine and clorazepate both increase sedation. Use Caution/Monitor.
- clozapine
brimonidine and clozapine both increase sedation. Use Caution/Monitor.
- cyclobenzaprine
brimonidine and cyclobenzaprine both increase sedation. Use Caution/Monitor.
- cyproheptadine
brimonidine and cyproheptadine both increase sedation. Use Caution/Monitor.
- dantrolene
brimonidine and dantrolene both increase sedation. Use Caution/Monitor.
- daridorexant
brimonidine and daridorexant both increase sedation. Use Caution/Monitor.
- desflurane
brimonidine and desflurane both increase sedation. Use Caution/Monitor.
- desipramine
brimonidine and desipramine both increase sedation. Use Caution/Monitor.
- deutetrabenazine
brimonidine and deutetrabenazine both increase sedation. Use Caution/Monitor.
- dexbrompheniramine
brimonidine and dexbrompheniramine both increase sedation. Use Caution/Monitor.
- dexchlorpheniramine
brimonidine and dexchlorpheniramine both increase sedation. Use Caution/Monitor.
- diazepam
brimonidine and diazepam both increase sedation. Use Caution/Monitor.
- difenoxin hcl
brimonidine and difenoxin hcl both increase sedation. Use Caution/Monitor.
- 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.
- digoxin
brimonidine increases effects of digoxin by pharmacodynamic synergism. Use Caution/Monitor.
- dimenhydrinate
brimonidine and dimenhydrinate both increase sedation. Use Caution/Monitor.
- diphenhydramine
brimonidine and diphenhydramine both increase sedation. Use Caution/Monitor.
- diphenoxylate hcl
brimonidine and diphenoxylate hcl both increase sedation. Use Caution/Monitor.
- doxepin
brimonidine and doxepin both increase sedation. Use Caution/Monitor.
- doxylamine
brimonidine and doxylamine both increase sedation. Use Caution/Monitor.
- droperidol
brimonidine and droperidol both increase sedation. Use Caution/Monitor.
- efavirenz
brimonidine and efavirenz both increase sedation. Use Caution/Monitor.
- entacapone
brimonidine and entacapone both increase sedation. Use Caution/Monitor.
- eprosartan
brimonidine increases effects of eprosartan by pharmacodynamic synergism. Use Caution/Monitor.
- esketamine intranasal
esketamine intranasal, brimonidine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely.
- estazolam
brimonidine and estazolam both increase sedation. Use Caution/Monitor.
- eszopiclone
brimonidine and eszopiclone both increase sedation. Use Caution/Monitor.
- ethanol
brimonidine and ethanol both increase sedation. Use Caution/Monitor.
- ethosuximide
brimonidine and ethosuximide both increase sedation. Use Caution/Monitor.
- ethotoin
brimonidine and ethotoin both increase sedation. Use Caution/Monitor.
- felbamate
brimonidine and felbamate both increase sedation. Use Caution/Monitor.
- fenfluramine
brimonidine and fenfluramine both increase sedation. Use Caution/Monitor.
- fexofenadine
brimonidine and fexofenadine both increase sedation. Use Caution/Monitor.
- flibanserin
brimonidine and flibanserin both increase sedation. Use Caution/Monitor.
- fluphenazine
brimonidine and fluphenazine both increase sedation. Use Caution/Monitor.
- flurazepam
brimonidine and flurazepam both increase sedation. Use Caution/Monitor.
- gabapentin
brimonidine and gabapentin both increase sedation. Use Caution/Monitor.
- ganaxolone
brimonidine and ganaxolone both increase sedation. Use Caution/Monitor.
- guanfacine
brimonidine and guanfacine both increase sedation. Use Caution/Monitor.
- haloperidol
brimonidine and haloperidol both increase sedation. Use Caution/Monitor.
- hydroxyzine
brimonidine and hydroxyzine both increase sedation. Use Caution/Monitor.
- iloperidone
brimonidine and iloperidone both increase sedation. Use Caution/Monitor.
- imipramine
brimonidine and imipramine both increase sedation. Use Caution/Monitor.
- irbesartan
brimonidine increases effects of irbesartan by pharmacodynamic synergism. Use Caution/Monitor.
- isoflurane
brimonidine and isoflurane both increase sedation. Use Caution/Monitor.
- ketamine
brimonidine and ketamine both increase sedation. Use Caution/Monitor.
- ketotifen, drug-eluting contact lens
brimonidine and ketotifen, drug-eluting contact lens both increase sedation. Use Caution/Monitor.
- lamotrigine
brimonidine and lamotrigine both increase sedation. Use Caution/Monitor.
- lasmiditan
lasmiditan, brimonidine. Either increases effects of the other by sedation. Use Caution/Monitor. Coadministration of lasmiditan and other CNS depressant drugs, including alcohol have not been evaluated in clinical studies. Lasmiditan may cause sedation, as well as other cognitive and/or neuropsychiatric adverse reactions.
- lemborexant
brimonidine and lemborexant both increase sedation. Use Caution/Monitor.
- levetiracetam
brimonidine and levetiracetam both increase sedation. Use Caution/Monitor.
- levocetirizine
brimonidine and levocetirizine both increase sedation. Use Caution/Monitor.
- levorphanol
brimonidine and levorphanol both increase sedation. Use Caution/Monitor.
- lisdexamfetamine
brinzolamide will increase the level or effect of lisdexamfetamine by passive renal tubular reabsorption - basic urine. Use Caution/Monitor.
- loratadine
brimonidine and loratadine both increase sedation. Use Caution/Monitor.
- lorazepam
brimonidine and lorazepam both increase sedation. Use Caution/Monitor.
- losartan
brimonidine increases effects of losartan by pharmacodynamic synergism. Use Caution/Monitor.
- loxapine
brimonidine and loxapine both increase sedation. Use Caution/Monitor.
- lumateperone
brimonidine and lumateperone both increase sedation. Use Caution/Monitor.
- lurasidone
lurasidone, brimonidine. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Potential for increased CNS depressant effects when used concurrently; monitor for increased sedation.
brimonidine and lurasidone both increase sedation. Use Caution/Monitor. - maprotiline
brimonidine and maprotiline both increase sedation. Use Caution/Monitor.
- meclizine
brimonidine and meclizine both increase sedation. Use Caution/Monitor.
- meperidine
brimonidine and meperidine both increase sedation. Use Caution/Monitor.
- meprobamate
brimonidine and meprobamate both increase sedation. 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.
- metaxalone
brimonidine and metaxalone both increase sedation. Use Caution/Monitor.
- methocarbamol
brimonidine and methocarbamol both increase sedation. Use Caution/Monitor.
- methohexital
brimonidine and methohexital both increase sedation. Use Caution/Monitor.
- methsuximide
brimonidine and methsuximide both increase sedation. Use Caution/Monitor.
- midazolam
brimonidine and midazolam both increase sedation. Use Caution/Monitor.
- mirtazapine
brimonidine and mirtazapine both increase sedation. Use Caution/Monitor.
- molindone
brimonidine and molindone both increase sedation. Use Caution/Monitor.
- nalbuphine
brimonidine and nalbuphine both increase sedation. Use Caution/Monitor.
- nitroglycerin rectal
nitroglycerin rectal, brimonidine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .
- nitrous oxide
brimonidine and nitrous oxide both increase sedation. Use Caution/Monitor.
- nortriptyline
brimonidine and nortriptyline both increase sedation. Use Caution/Monitor.
- olanzapine
brimonidine and olanzapine both increase sedation. Use Caution/Monitor.
- oliceridine
brimonidine and oliceridine both increase sedation. Use Caution/Monitor.
- olmesartan
brimonidine increases effects of olmesartan by pharmacodynamic synergism. Use Caution/Monitor.
- olopatadine intranasal
brimonidine and olopatadine intranasal both increase sedation. Use Caution/Monitor.
- opicapone
brimonidine and opicapone both increase sedation. Use Caution/Monitor.
- opium tincture
brimonidine and opium tincture both increase sedation. Use Caution/Monitor.
- orphenadrine
brimonidine and orphenadrine both increase sedation. Use Caution/Monitor.
- oxazepam
brimonidine and oxazepam both increase sedation. Use Caution/Monitor.
- paliperidone
brimonidine and paliperidone both increase sedation. Use Caution/Monitor.
- pentazocine
brimonidine and pentazocine both increase sedation. Use Caution/Monitor.
- pentobarbital
brimonidine and pentobarbital both increase sedation. Use Caution/Monitor.
- perampanel
brimonidine and perampanel both increase sedation. Use Caution/Monitor.
- perphenazine
brimonidine and perphenazine both increase sedation. Use Caution/Monitor.
- pheniramine
brimonidine and pheniramine both increase sedation. Use Caution/Monitor.
- phenobarbital
brimonidine and phenobarbital both increase sedation. Use Caution/Monitor.
- pimozide
brimonidine and pimozide both increase sedation. Use Caution/Monitor.
- pomalidomide
brimonidine and pomalidomide both increase sedation. Use Caution/Monitor.
- pregabalin
brimonidine and pregabalin both increase sedation. Use Caution/Monitor.
- primidone
brimonidine and primidone both increase sedation. Use Caution/Monitor.
- prochlorperazine
brimonidine and prochlorperazine both increase sedation. Use Caution/Monitor.
- promethazine
brimonidine and promethazine both increase sedation. Use Caution/Monitor.
- propofol
brimonidine and propofol both increase sedation. Use Caution/Monitor.
- protriptyline
brimonidine and protriptyline both increase sedation. Use Caution/Monitor.
- pyrilamine
brimonidine and pyrilamine both increase sedation. Use Caution/Monitor.
- quazepam
brimonidine and quazepam both increase sedation. Use Caution/Monitor.
- quetiapine
brimonidine and quetiapine both increase sedation. Use Caution/Monitor.
- ramelteon
brimonidine and ramelteon both increase sedation. Use Caution/Monitor.
- remimazolam
brimonidine and remimazolam both increase sedation. Use Caution/Monitor.
- reserpine
brimonidine and reserpine both increase sedation. Use Caution/Monitor.
- risperidone
brimonidine and risperidone both increase sedation. Use Caution/Monitor.
- sacubitril/valsartan
brimonidine increases effects of sacubitril/valsartan by pharmacodynamic synergism. Use Caution/Monitor.
- 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.
- scopolamine
brimonidine and scopolamine both increase sedation. Use Caution/Monitor.
- sevoflurane
brimonidine and sevoflurane both increase sedation. Use Caution/Monitor.
- sodium oxybate
brimonidine and sodium oxybate both increase sedation. Use Caution/Monitor.
- stiripentol
stiripentol, brimonidine. Either increases effects of the other by sedation. Use Caution/Monitor. Concomitant use stiripentol with other CNS depressants, including alcohol, may increase the risk of sedation and somnolence.
- sufentanil
brimonidine and sufentanil both increase sedation. Use Caution/Monitor.
- sufentanil SL
brimonidine and sufentanil SL both increase sedation. Use Caution/Monitor.
- 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.
- suvorexant
brimonidine and suvorexant both increase sedation. Use Caution/Monitor.
- tapentadol
brimonidine and tapentadol both increase sedation. Use Caution/Monitor.
- tasimelteon
brimonidine and tasimelteon both increase sedation. Use Caution/Monitor.
- telmisartan
brimonidine increases effects of telmisartan by pharmacodynamic synergism. Use Caution/Monitor.
- temazepam
brimonidine and temazepam both increase sedation. Use Caution/Monitor.
- tetrabenazine
brimonidine and tetrabenazine both increase sedation. Use Caution/Monitor.
- thioridazine
brimonidine and thioridazine both increase sedation. Use Caution/Monitor.
- thiothixene
brimonidine and thiothixene both increase sedation. Use Caution/Monitor.
- tiagabine
brimonidine and tiagabine both increase sedation. Use Caution/Monitor.
- tizanidine
brimonidine and tizanidine both increase sedation. Use Caution/Monitor.
- tolcapone
brimonidine and tolcapone both increase sedation. Use Caution/Monitor.
- topiramate
brimonidine and topiramate both increase sedation. Use Caution/Monitor.
topiramate, brinzolamide. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Increased risk of kidney stone formation. - tramadol
brimonidine and tramadol both increase sedation. Use Caution/Monitor.
- 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 (150)
- acebutolol
brimonidine increases effects of acebutolol by pharmacodynamic synergism. Minor/Significance Unknown.
- alfentanil
brimonidine increases effects of alfentanil by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- alfuzosin
brimonidine increases effects of alfuzosin by pharmacodynamic synergism. Minor/Significance Unknown.
- alprazolam
brimonidine increases effects of alprazolam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- amiloride
brimonidine increases effects of amiloride by pharmacodynamic synergism. Minor/Significance Unknown.
- amitriptyline
amitriptyline decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- amlodipine
brimonidine increases effects of amlodipine by pharmacodynamic synergism. Minor/Significance Unknown.
- amobarbital
brimonidine increases effects of amobarbital by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
brinzolamide, amobarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia. - amoxapine
amoxapine decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- butabarbital
brinzolamide, butabarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- aripiprazole
brimonidine increases effects of aripiprazole by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- asenapine
brimonidine increases effects of asenapine by pharmacodynamic synergism. Minor/Significance Unknown.
- atenolol
brimonidine increases effects of atenolol by pharmacodynamic synergism. Minor/Significance Unknown.
- azelastine
brimonidine increases effects of azelastine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- belladonna and opium
brimonidine increases effects of belladonna and opium by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- benazepril
brimonidine increases effects of benazepril by pharmacodynamic synergism. Minor/Significance Unknown. Additive hypotensive effects.
- bendroflumethiazide
brimonidine increases effects of bendroflumethiazide by pharmacodynamic synergism. Minor/Significance Unknown.
- benperidol
brimonidine increases effects of benperidol by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- betaxolol
brimonidine increases effects of betaxolol by pharmacodynamic synergism. Minor/Significance Unknown.
- bisoprolol
brimonidine increases effects of bisoprolol by pharmacodynamic synergism. Minor/Significance Unknown.
- bosentan
brimonidine increases effects of bosentan by pharmacodynamic synergism. Minor/Significance Unknown.
- brompheniramine
brimonidine increases effects of brompheniramine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- bumetanide
brimonidine increases effects of bumetanide by pharmacodynamic synergism. Minor/Significance Unknown.
- buprenorphine
brimonidine increases effects of buprenorphine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- buprenorphine buccal
brimonidine increases effects of buprenorphine buccal by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- butabarbital
brimonidine increases effects of butabarbital by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- butalbital
brimonidine increases effects of butalbital by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
brinzolamide, butalbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia. - butorphanol
brimonidine increases effects of butorphanol by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- ethotoin
brinzolamide, ethotoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- captopril
brimonidine increases effects of captopril by pharmacodynamic synergism. Minor/Significance Unknown. Both drugs lower blood pressure. Monitor blood pressure.
- carbinoxamine
brimonidine increases effects of carbinoxamine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- carvedilol
brimonidine increases effects of carvedilol by pharmacodynamic synergism. Minor/Significance Unknown.
- celiprolol
brimonidine increases effects of celiprolol by pharmacodynamic synergism. Minor/Significance Unknown.
- chloral hydrate
brimonidine increases effects of chloral hydrate by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- chlordiazepoxide
brimonidine increases effects of chlordiazepoxide by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- chlorothiazide
brimonidine increases effects of chlorothiazide by pharmacodynamic synergism. Minor/Significance Unknown.
- chlorpheniramine
brimonidine increases effects of chlorpheniramine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- chlorpromazine
brimonidine increases effects of chlorpromazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- chlorthalidone
brimonidine increases effects of chlorthalidone by pharmacodynamic synergism. Minor/Significance Unknown.
- cinnarizine
brimonidine increases effects of cinnarizine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- clemastine
brimonidine increases effects of clemastine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- clevidipine
brimonidine increases effects of clevidipine by pharmacodynamic synergism. Minor/Significance Unknown.
- clomipramine
clomipramine decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- clonazepam
brimonidine increases effects of clonazepam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- clonidine
brimonidine increases effects of clonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- clorazepate
brimonidine increases effects of clorazepate by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- clozapine
brimonidine increases effects of clozapine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- codeine
brimonidine increases effects of codeine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- cyclizine
brimonidine increases effects of cyclizine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- cyclopenthiazide
brimonidine increases effects of cyclopenthiazide by pharmacodynamic synergism. Minor/Significance Unknown.
- cyproheptadine
brimonidine increases effects of cyproheptadine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- desipramine
desipramine decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- dexchlorpheniramine
brimonidine increases effects of dexchlorpheniramine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- dexmedetomidine
brimonidine increases effects of dexmedetomidine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- dextromoramide
brimonidine increases effects of dextromoramide by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- diamorphine
brimonidine increases effects of diamorphine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- diazepam
brimonidine increases effects of diazepam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- difenoxin hcl
brimonidine increases effects of difenoxin hcl by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- diltiazem
brimonidine increases effects of diltiazem by pharmacodynamic synergism. Minor/Significance Unknown.
- dimenhydrinate
brimonidine increases effects of dimenhydrinate by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- diphenhydramine
brimonidine increases effects of diphenhydramine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- diphenoxylate hcl
brimonidine increases effects of diphenoxylate hcl by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- dipipanone
brimonidine increases effects of dipipanone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- doxazosin
brimonidine increases effects of doxazosin by pharmacodynamic synergism. Minor/Significance Unknown.
- doxepin
doxepin decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- doxylamine
brimonidine increases effects of doxylamine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- droperidol
brimonidine increases effects of droperidol by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- drospirenone
brimonidine increases effects of drospirenone by pharmacodynamic synergism. Minor/Significance Unknown.
- enalapril
brimonidine increases effects of enalapril by pharmacodynamic synergism. Minor/Significance Unknown.
- eplerenone
brimonidine increases effects of eplerenone by pharmacodynamic synergism. Minor/Significance Unknown.
- epoprostenol
brimonidine increases effects of epoprostenol by pharmacodynamic synergism. Minor/Significance Unknown.
- esmolol
brimonidine increases effects of esmolol by pharmacodynamic synergism. Minor/Significance Unknown.
- estazolam
brimonidine increases effects of estazolam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- ethacrynic acid
brimonidine increases effects of ethacrynic acid by pharmacodynamic synergism. Minor/Significance Unknown.
- ethanol
brimonidine increases effects of ethanol by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- etomidate
brimonidine increases effects of etomidate by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- felodipine
brimonidine increases effects of felodipine by pharmacodynamic synergism. Minor/Significance Unknown.
- fenoldopam
brimonidine increases effects of fenoldopam by pharmacodynamic synergism. Minor/Significance Unknown.
- fluphenazine
brimonidine increases effects of fluphenazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- flurazepam
brimonidine increases effects of flurazepam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- fosinopril
brimonidine increases effects of fosinopril by pharmacodynamic synergism. Minor/Significance Unknown.
- fosphenytoin
brinzolamide, fosphenytoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- furosemide
brimonidine increases effects of furosemide by pharmacodynamic synergism. Minor/Significance Unknown.
- guanfacine
brimonidine increases effects of guanfacine by pharmacodynamic synergism. Minor/Significance Unknown.
- haloperidol
brimonidine increases effects of haloperidol by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- hydralazine
brimonidine increases effects of hydralazine by pharmacodynamic synergism. Minor/Significance Unknown.
- hydrochlorothiazide
brimonidine increases effects of hydrochlorothiazide by pharmacodynamic synergism. Minor/Significance Unknown.
- hydromorphone
brimonidine increases effects of hydromorphone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- hydroxyzine
brimonidine increases effects of hydroxyzine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- iloperidone
brimonidine increases effects of iloperidone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- iloprost
brimonidine increases effects of iloprost by pharmacodynamic synergism. Minor/Significance Unknown.
- imidapril
brimonidine increases effects of imidapril by pharmacodynamic synergism. Minor/Significance Unknown.
- imipramine
imipramine decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- indapamide
brimonidine increases effects of indapamide by pharmacodynamic synergism. Minor/Significance Unknown.
- isradipine
brimonidine increases effects of isradipine by pharmacodynamic synergism. Minor/Significance Unknown.
- ketanserin
brimonidine increases effects of ketanserin by pharmacodynamic synergism. Minor/Significance Unknown.
- labetalol
brimonidine increases effects of labetalol by pharmacodynamic synergism. Minor/Significance Unknown.
- levorphanol
brimonidine increases effects of levorphanol by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- lisinopril
brimonidine increases effects of lisinopril by pharmacodynamic synergism. Minor/Significance Unknown.
- lofepramine
lofepramine decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- loprazolam
brimonidine increases effects of loprazolam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- lorazepam
brimonidine increases effects of lorazepam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- lormetazepam
brimonidine increases effects of lormetazepam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- loxapine
brimonidine increases effects of loxapine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- loxapine inhaled
brimonidine increases effects of loxapine inhaled by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- maprotiline
maprotiline decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- mecamylamine
brimonidine increases effects of mecamylamine by pharmacodynamic synergism. Minor/Significance Unknown.
- meperidine
brimonidine increases effects of meperidine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- meprobamate
brimonidine increases effects of meprobamate by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- methadone
brimonidine increases effects of methadone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- methyclothiazide
brimonidine increases effects of methyclothiazide by pharmacodynamic synergism. Minor/Significance Unknown.
- metolazone
brimonidine increases effects of metolazone by pharmacodynamic synergism. Minor/Significance Unknown.
- metoprolol
brimonidine increases effects of metoprolol by pharmacodynamic synergism. Minor/Significance Unknown.
- metyrosine
brimonidine increases effects of metyrosine by pharmacodynamic synergism. Minor/Significance Unknown.
- midazolam
brimonidine increases effects of midazolam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- minoxidil
brimonidine increases effects of minoxidil by pharmacodynamic synergism. Minor/Significance Unknown.
- moexipril
brimonidine increases effects of moexipril by pharmacodynamic synergism. Minor/Significance Unknown.
- morphine
brimonidine increases effects of morphine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- moxisylyte
brimonidine increases effects of moxisylyte by pharmacodynamic synergism. Minor/Significance Unknown.
- moxonidine
brimonidine increases effects of moxonidine by pharmacodynamic synergism. Minor/Significance Unknown.
- nadolol
brimonidine increases effects of nadolol by pharmacodynamic synergism. Minor/Significance Unknown.
- nalbuphine
brimonidine increases effects of nalbuphine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- nebivolol
brimonidine increases effects of nebivolol by pharmacodynamic synergism. Minor/Significance Unknown.
- nicardipine
brimonidine increases effects of nicardipine by pharmacodynamic synergism. Minor/Significance Unknown.
- nifedipine
brimonidine increases effects of nifedipine by pharmacodynamic synergism. Minor/Significance Unknown.
- nisoldipine
brimonidine increases effects of nisoldipine by pharmacodynamic synergism. Minor/Significance Unknown.
- nortriptyline
nortriptyline decreases effects of brimonidine by pharmacodynamic antagonism. Minor/Significance Unknown.
- olanzapine
brimonidine increases effects of olanzapine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- opium tincture
brimonidine increases effects of opium tincture by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- oxazepam
brimonidine increases effects of oxazepam by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- oxycodone
brimonidine increases effects of oxycodone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- oxymorphone
brimonidine increases effects of oxymorphone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- paliperidone
brimonidine increases effects of paliperidone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- papaveretum
brimonidine increases effects of papaveretum by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- penbutolol
brimonidine increases effects of penbutolol by pharmacodynamic synergism. Minor/Significance Unknown.
- pentazocine
brimonidine increases effects of pentazocine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- pentobarbital
brinzolamide, pentobarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
brimonidine increases effects of pentobarbital by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression. - perindopril
brimonidine increases effects of perindopril by pharmacodynamic synergism. Minor/Significance Unknown.
- phenobarbital
brinzolamide, phenobarbital. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- perphenazine
brimonidine increases effects of perphenazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- phenobarbital
brimonidine increases effects of phenobarbital by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- phenoxybenzamine
brimonidine increases effects of phenoxybenzamine by pharmacodynamic synergism. Minor/Significance Unknown.
- phentolamine
brimonidine increases effects of phentolamine by pharmacodynamic synergism. Minor/Significance Unknown.
- phenytoin
brinzolamide, phenytoin. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
- pimozide
brimonidine increases effects of pimozide by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- pindolol
brimonidine increases effects of pindolol by pharmacodynamic synergism. Minor/Significance Unknown.
- prazosin
brimonidine increases effects of prazosin by pharmacodynamic synergism. Minor/Significance Unknown.
- primidone
brinzolamide, primidone. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Increased risk of anticonvulsant induced osteomalacia.
brimonidine increases effects of primidone by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression. - prochlorperazine
brimonidine increases effects of prochlorperazine by pharmacodynamic synergism. Minor/Significance Unknown. Increased CNS depression.
- secobarbital
brinzolamide, secobarbital. 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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Formulary
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