BRIMOCHEK EYE DROPS 0.2%

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

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

BRIMOCHEK EYE DROPS 0.2% was registered with Health Science Authority of Singapore by DCH AURIGA SINGAPORE. It is marketed with the registration number of SIN15099P with effective from 2016-10-14.

This product contains 2mg/ml of Brimonidine in the form of OPHTHALMIC SOLUTION.

The medicine was manufactured by Indoco Remedies LTD (Plant II) in INDIA

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: S01EA05

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