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Indications and Dosage
Ophthalmic
Ocular hypertension, Open-angle glaucoma Adult: Available preparation:
Brinzolamide 1% (10 mg/mL) and timolol 0.5% (5 mg/mL) suspension Instill 1 drop into the conjunctival sac of the affected eye(s) bid. |
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Renal Impairment
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Contraindications
Hypersensitivity to brinzolamide, timolol, or sulfonamides. Reactive airway disease (e.g. current or history of bronchial asthma, severe COPD), sinus bradycardia, sick sinus syndrome, sino-atrial block, 2nd or 3rd degree atrioventricular block, overt cardiac failure, cardiogenic shock, severe allergic rhinitis, hyperchloraemic acidosis. Severe renal impairment (CrCl <30 mL/min).
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Special Precautions
Patient with CV diseases (e.g. coronary heart disease, Prinzmetal angina, cardiac failure, 1st degree heart block), hypotension, diabetes mellitus, myasthenia gravis, peripheral vascular disease (PVD), Raynaud’s disease, history of psychiatric illness, mild to moderate COPD, thyrotoxicosis, corneal diseases, history of atopy or severe anaphylactic reaction to allergens. Not intended for use in narrow-angle glaucoma. Severe hepatic and mild to moderate renal impairment. Pregnancy and lactation.
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Adverse Reactions
Significant: Bacterial keratitis, impairment of mental alertness and/or physical coordination.
Cardiac disorders: Decreased heart rate. Eye disorders: Blurred vision, eye irritation, eye pain, foreign body sensation of eye, punctate keratitis. Gastrointestinal disorders: Dysgeusia. |
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Patient Counseling Information
This drug may cause transient blurring of vision or other visual disturbances, if affected, do not drive or operate machinery. Remove contact lenses prior to administration and reinsert after 15 minutes.
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Monitoring Parameters
Perform ophthalmic exam and monitor intraocular pressure periodically.
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Drug Interactions
Brinzolamide: May enhance adverse effect of other carbonic anhydrase inhibitors. Serum concentration may be increased by CYP3A4 inhibitors (e.g. ketoconazole, ritonavir).
Timolol: Additive hypotensive and/or marked bradycardic effects with calcium channel blockers or β-adrenergic blocking agents, antiarrhythmics (e.g. amiodarone), digitalis glycosides, parasympathomimetics, guanethidine. Increased beta-blockade (e.g. decreased heart rate) with quinidine, cimetidine. May increase the hypoglycaemic effect of antidiabetic agents. May decrease response to epinephrine. |
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Action
Description: Brinzolamide inhibits carbonic anhydrase in the ciliary process of the eye thereby decreasing the secretion of aqueous humour leading to reduction of intraocular pressure.
Timolol is a nonselective β-adrenergic receptor blocker. It reduces intraocular pressure by decreasing aqueous humour formation and possibly increasing sympathetic outflow. Pharmacokinetics: Absorption: Absorbed through the cornea into systemic circulation. Timolol: Time to peak plasma concentration: Approx 1-2 hours. Distribution: Brinzolamide: Plasma protein binding: Approx 60%. Timolol: Crosses placenta and enters breast milk. Metabolism: Brinzolamide: Metabolised to N-desethyl brinzolamide. Timolol: Extensively metabolised in the liver by CYP2D6. Excretion: Brinzolamide: Via urine (approx 60%, approx 20% as metabolite). Timolol: Via urine (approx 20% as unchanged drug, remainder as metabolites). Elimination half-life: 4 hours. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Brinzolamide, CID=68844, https://pubchem.ncbi.nlm.nih.gov/compound/Brinzolamide (accessed on Jan. 21, 2020)  Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 33624, Timolol. https://pubchem.ncbi.nlm.nih.gov/compound/33624. Accessed July 26, 2022. |
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Storage
Store between 2-30°C. Do not freeze.
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MIMS Class
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References
Anon. Brinzolamide (EENT). AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 06/04/2018. Anon. Brinzolamide and Timolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/04/2018. Buckingham R (ed). Brinzolamide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/04/2018. Buckingham R (ed). Timolol Maleate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/04/2018. Joint Formulary Committee. Brinzolamide with Timolol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/04/2018. Novartis New Zealand Limited. Azarga Eye Drops Suspension data sheet 31 August 2017. Medsafe. http://www.medsafe.govt.nz/. Accessed 06/04/2018.
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