SIMBRINZA EYE DROPS, SUSPENSION 10mg/ML + 2mg/ML

Brinzolamide
Brimonidine

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

Brinzolamide | Brinzolamide |

Description

Brinzolamide is a highly specific, non-competitive, reversible carbonic anhydrase inhibitor. Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye. It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II). Inhibition of carbonic anhydrase in the 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. The result is a reduction in intraocular pressure. Brinzolamide is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Indication

For the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

Mechanism of Action

Brinzolamide is a highly specific inhibitor of CA-II, which is the main CA isoenzyme involved in the secretion of aqueous humor. Inhibition of CA in the ciliary process of the eye slows the formation of bicarbonate, and reduces sodium and fluid transport. This results in a reduction in the rate of aqueous humor secretion and the intraocular pressure. Brinzolamide is absorbed systemically following topical ocular administration. Since it has a high affinity for CA-II, brinzolamide binds extensively to red blood cells, where CA-II is primarily found. As sufficient CA-II activity remains, adverse effects resulting from the systemic inhibition of CA by brinzolamide are not observed. The metabolite N-desethyl brinzolamide is also formed. This metabolite binds to CA and accumulates in red blood cells as well. In the presence of brinzolamide, the metabolite binds mainly to carbonic anhydrase I (CA-I).

Pharmacodynamics

Used in the treatment of glaucoma, brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. Brinzolamide can decrease intraocular pressure by approximately 16-19% in patients with elevated intraocular pressure.

Pharmacokinetics

Absorption:

Absorbed into systemic circulation following topical ocular application

Distribution:

Not Available

Metabolism:

Ophthalmic

Elimination:

Not Available

Half-life

111 days

Clearance

Not Available

Toxicity

Not Available

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline | Brimonidina | Brimonidine | Brimonidinum | Bromoxidine | Brimonidine |

Description

Brimonidine is a drug used to treat glaucoma. It acts via decreasing aqueous humor synthesis. A topical gel formulation, marketed under the name Mirvaso, was FDA approved on August 2013 for the treatment of rosacea.

Indication

The ophthalmic solution is indicated for patients with open-angle glaucoma or ocular hypertension to lower intraocular pressure. The topical gel is indicated for the treatment of persistent (nontransient) facial erythema of rosacea in adults 18 years or older.

Mechanism of Action

Brimonidine is an alpha adrenergic receptor agonist (primarily alpha-2). It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that Brimonidine has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow. The topical gel reduces erythema through direct vasocontriction.

Pharmacodynamics

Brimonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveoscleral outflow.

Pharmacokinetics

Absorption:

Minimal systemic absorption occurs after ocular insertion. When the topical gel was applied to adult patients with facial erythema associated with rosacea, the plasma maximum concentration (Cmax) and area under the concentration-time curve (AUC) were 46 ± 62 pg/mL and 417 ± 264 pg.hr/mL, respectively. These values were reached on Day 15 of treatment.

Distribution:

Not Available

Metabolism:

Metabolized primarily by the liver.

Elimination:

Urinary excretion is the major route of elimination of the drug and its metabolites.

Half-life

2 hours [ophthalmic solution]

Clearance

Not Available

Toxicity

Oral LD50 is 50 mg/kg in mice and 100 mg/kg in rats. Common adverse reactions of the topical gel formulation include erythema, flushing, skin burning sensation, and contact dermatitis.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

SIMBRINZA EYE DROPS, SUSPENSION 10mg/ML + 2mg/ML was registered with Health Science Authority of Singapore by NOVARTIS (SINGAPORE) PTE LTD. It is marketed with the registration number of SIN15085P with effective from 2016-09-06.

This product contains 10mg/mL of Brinzolamide, and 2mg/mL of Brimonidine in the form of OPHTHALMIC SUSPENSION.

The medicine was manufactured by Alcon-Couvreur N.V. in BELGIUM

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: S01EC54

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