Brinzolamide (Azopt) eye drops for open-angle glaucoma

Brinzolamide is a medication used to lower high pressure in the eye in people with open-angle glaucoma or ocular hypertension. It belongs to a class of drugs called carbonic anhydrase inhibitors. By decreasing the production of fluid in the eye, it helps reduce pressure. Brinzolamide is often prescribed as eye drops and is usually used in combination with other medications for better efficacy in managing glaucoma.

Brinzolamide decreases the formation of aqueous humor by inhibiting the enzyme carbonic anhydrase resulting in a reduction in the intraocular pressure. It is used for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Brinzolamide Dose in Adults

Brinzolamide in the treatment of Elevated intraocular pressure:  

  • You typically use it as eye drops.
  • Just put one drop in the eye that needs it, three times a day.
  • This helps lower the pressure inside the eye, which is important for conditions like glaucoma.

Brinzolamide Dose in Childrens

Safety and efficacy of brinzolamide in children has not been established. 

Pregnancy Risk Factor C

  • When it comes to pregnancy, Brinzolamide is categorized as a Pregnancy Risk Factor C.
  • This means that there have been adverse events observed in animal studies related to reproduction.
  • It indicates a potential risk to the fetus, although there may not be enough human studies to confirm this risk.

Brinzolamide use during breastfeeding:

  • The manufacturer suggests that if you're breastfeeding and considering using Brinzolamide, you should weigh the importance of the medication for your treatment against the potential risks to your breastfeeding infant.

Brinzolamide Dose in Renal Disease:

  • For individuals with a creatinine clearance (CrCl) of 30 mL/minute or higher, no dosage adjustments are typically needed according to the manufacturer's instructions.
  • For those with a CrCl below 30 mL/minute, using Brinzolamide is not recommended. This is because it hasn't been studied extensively in this population, and both Brinzolamide and its metabolite are mainly eliminated through the kidneys.

Brinzolamide Dose in Liver Disease:

  • According to the manufacturer's recommendations, no dose adjustments are typically specified for patients with liver disease.

Common Side Effects of Brinzolamide Include:

  • Cardiovascular:
    • Hyperemia
  • Central Nervous System:
    • Foreign Body Sensation of Eye
    • Headache
  • Dermatologic:
    • Dermatitis
  • Gastrointestinal:
    • Dysgeusia
  • Ophthalmic:
    • Blurred Vision
    • Blepharitis
    • Eye Discharge
    • Eye Discomfort
    • Eye Pain
    • Eye Pruritus
    • Keratitis
    • Xerophthalmia
  • Respiratory:
    • Rhinitis

Contraindication to Brinzolamide include:

  • If someone is allergic to brinzolamide or any part of the medication, they shouldn't use it.
  • In Canada, there are extra reasons not to use it: if you're allergic to sulfonamide, if your kidney function is severely impaired (with a creatinine clearance less than 30 mL per minute), or if you have hyperchloremic acidosis.
  • These are additional reasons why you shouldn't use brinzolamide, as listed in Canadian guidelines.

Warnings and Precautions

Ophthalmic effects

  • Using brinzolamide eye drops might make your vision temporarily blurry.
  • This can affect your ability to do things that need you to be mentally sharp, like driving or using machinery.
  • It's important to be cautious and aware of this potential side effect, especially right after using the eye drops.

Sulfonamide"sulfa"Allergy:

  • The FDA-approved labeling for medications containing sulfonamide typically includes a warning against use in patients with a known allergy to sulfonamides.
  • While there was once concern about cross-reactivity between different types of sulfonamide medications, recent research suggests that this may not be as common as previously thought.
  • Specifically, the risk of severe allergic reactions, such as anaphylaxis, due to antibody production, is unlikely with nonantibiotic sulfonamides.
  • However, there is still some uncertainty regarding T-cell-mediated reactions, such as maculopapular rash, and some clinicians may choose to avoid exposure to sulfonamides in patients who have experienced severe reactions like Stevens-Johnson syndrome or toxic epidermal necrolysis.

Acute angle-closure glaucoma:

  • The use of Brinzolamide has not been studied in cases of acute angle-closure glaucoma.
  • This means there isn't enough information available to determine its safety and effectiveness for this specific type of glaucoma.

Corneal edema

  • Brinzolamide should be used cautiously in patients with low corneal endothelial cell counts because they may have a higher risk of developing corneal edema, which is swelling of the cornea.

Renal impairment

  • Brinzolamide use is not recommended in patients with severe renal impairment because it hasn't been studied extensively in this group.
  • Severe renal impairment refers to significant kidney problems.
  • Since Brinzolamide is eliminated from the body primarily through the kidneys, using it in individuals with severe kidney issues could potentially lead to complications.

Brinzolamide: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Indirect-Acting Alpha-/Beta Agonists

Inhibitors of carbonic anhydrase may increase the serum concentrations of Alpha-/Beta Agonists (Indirect Acting).

Amantadine

Carbonic Anhydrase Inhibitors could increase serum Amantadine concentrations.

Strong CYP3A4 inhibitors

May increase serum Brinzolamide concentrations

Risk Factor X (Avoid Combination)

Carbonic Anhydrase inhibitors

This may increase the toxic/adverse effects of other Carbonic Anhydrase Inhibitors. It has been reported that acid-base disorders can be caused by concurrent use of oral and ophthalmic carbonic anhydrase inhibiters. Management: If possible, avoid concurrent use of different carbonic acidase inhibitors. Patients should be closely monitored for kidney stones and metabolic acidosis.

Monitoring parameters:

  • Regular Eye Exams: It's important to have regular eye check-ups while using Brinzolamide.
  • Monitoring Intraocular Pressure: Your eye pressure will be checked to ensure Brinzolamide is working effectively.
  • Alertness During Exams: Be attentive during eye exams as Brinzolamide may temporarily blur vision.

How to administer Brinzolamide?

Using Brinzolamide Eye Drops

  • Shake Before Use: Give the bottle a good shake before applying the eye drops.
  • Remove Contact Lenses: Take out your contact lenses before using Brinzolamide. Wait for at least 15 minutes before putting them back in.
  • Timing with Other Eye Medications: If you're using more than one eye medication, space them out by at least 10 minutes.
  • Avoid Contact: Make sure the tip of the bottle doesn't touch your eye or anything else around it.

Mechanism of action of Brinzolamide:

  • Brinzolamide works by slowing down a substance called carbonic anhydrase in your eye.
  • This helps decrease the production of fluid called aqueous humor.
  • With less fluid being made, the pressure inside your eye goes down.
  • So, using Brinzolamide helps lower the pressure inside your eye.

Absorption:

  • When you apply Brinzolamide as eye drops, some of it gets absorbed into your bloodstream.

Distribution:

  • It mostly goes into your red blood cells, where it attaches to carbonic anhydrase, the target it works on.

Protein Binding:

  • About 60% of Brinzolamide attaches to proteins in your blood.

Metabolism:

  • It changes into another form called N-desethyl brinzolamide in your body.

Excretion:

  • Your body gets rid of Brinzolamide mainly through your urine, both in its original form and as the changed version.

International Brands of Brinzolamide:

  • Azopt
  • Azoptic
  • Benozol
  • Brinz
  • Brinzo-Vision
  • Brinzopt
  • BrinzoQuin
  • Ocubrin

Brinzolamide Brands in Pakistan:

Brinzolamide [Drops 10 mg]

Brizopt Drops

Bosch Pharmaceuticals (Pvt) Ltd.

 

Brinzolamide [Eye Drops 1 %w/v]

Azopt

Novartis Pharma (Pak) Ltd