brinzolamide / timolol maleate

Action and Spectrum

Action and Spectrum 

Glaucoma and ocular hypertension are treated together. Whereas beta adrenergic receptor blockers like timolol maleate reduce aqueous humour production, carbonic anhydrase inhibitors such as brinzolamide decrease the production of aqueous humour. This will increase the uveoscleral outflow also. Both drugs administered together have greater efficacy towards reducing IOP, which is necessary for preserving vision and optic nerve integrity. 

Drug Interaction

Adverse Reaction

Frequency defined 

Eye irritation (4%) 

Foreign body sensation (1%) 

Blurred vision (6%) 

Eye pain (3%) 

Dysgeusia (2%) 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with the combination of brinzolamide and timolol maleate. 

Contraindication / Caution

Contraindication/Cautions 

Acute heart failure 

Pregnancy 

Lactation 

Cardiogenic shock 

Thyroid 

Pregnancy / Lactation

Pregnancy consideration:   

Pregnancy category: not assigned 

Lactation: excreted into human milk: unknown 

 Pregnancy categories:  

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology 

Combining both brinzolamide with timolol maleate can reduce “intraocular pressure (IOP)” in the myopia or ocular hypertension patients. This occurs through blocking carbonic anhydrase activity by brinzolamide, which reduces aqueous humor production. In addition, it enhances uveoscleral outflow to further decrease aqueous humor generation using beta-adrenergic receptor antagonist known as timolol maleate. The latter is more effective in lowering IOP than when used alone; thus, preserving vision and ensuring optic nerve’s safety. 

Pharmacodynamics 

The exact activity is not known 

Pharmacokinetics 

Absorption 

It is absorbed systemically when applied in the topical form 

Distribution 

It is distributed through different tissues and organs 

Metabolism 

It is hydrolysed into inactive metabolites which undergoes first pass metabolism in the liver 

Elimination/Excretion 

The route of excretion is renal 

Adminstartion

Administration 

It is applied topically into the eye 

Patient Information Leaflet

Patient information leaflet  

Generic Name: brinzolamide / timolol maleate  

Pronounced: (BRIN-zoh-luh-mide / TYE-moh-lol MAL-ee-ate)  

Why do we use brinzolamide / timolol maleate?  

To avoid optic nerve damage and preserve vision, it is used to control elevated pressure inside the eye and open-angle corneal glaucoma or ocular hypertension. It helps when monotherapy isn’t enough on its own.