BRIMONIDINE TARTRATE solution/ drops

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

BRIMONIDINE TARTRATE (UNII: 4S9CL2DY2H) (BRIMONIDINE - UNII:E6GNX3HHTE)

Available from:

Regimed Medical

INN (International Name):

BRIMONIDINE TARTRATE

Composition:

BRIMONIDINE 2.0 mg in 1 mL

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Brimonidine Tartrate Ophthalmic Solution is indicated for lowering intraocular pressure in patients with open-angle glaucoma or ocular hypertension. The IOP lowering efficacy of Brimonidine Tartrate Ophthalmic Solution diminishes over time in some patients. This loss of effect appears with a variable time of onset in each patient and should be closely monitored. Brimonidine Tartrate Ophthalmic Solution is contraindicated in patients with hypersensitivity to brimonidine tartrate or any component of this medication. It is also contraindicated in patients receiving monoamine oxidase (MAO) inhibitor therapy.

Product summary:

Brimonidine Tartrate Ophthalmic Solution, 0.2% is supplied in white opaque plastic dropper bottles as followss:

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BRIMONIDINE TARTRATE- BRIMONIDINE TARTRATE SOLUTION/ DROPS
REGIMED MEDICAL
----------
BRIMONIDINE TARTRATE OPHTHALMIC SOLUTION, 0.2%
R
ONLY
DESCRIPTION
Brimonidine Tartrate Ophthalmic Solution, 0.2% is a relatively
selective alpha-2 adrenergic agonist for
ophthalmic use. The chemical name brimonidine tartrate is 5-bromo-6
(2-imidazolidinylideneamino)
quinoxaline L-tartrate. It is a white to slightly yellowish powder. In
solution, brimonidine tartrate has a
clear, grennish-yellow color. It has a molecular weight of 442.24 as
the tartrate salt and is water
soluble (34 mg/mL). The molecular formula is C
H
BrN •C
H
O
; the structural formula
is:
Brimonidine Tartrate Ophthalmic Solution, 0.2% is a sterile ophthalmic
solution.
Each mL of Brimonidine Tartrate Solution contains:
ACTIVE: Brimonidine Tartrate 2 mg (equivalent to 1.32 mg as
brimonidine free base).
PRESERVATIVE: Benzalkonium Chloride (0.05 mg)
INACTIVES: Citric Acid, Polyvinyl Alcohol, Sodium Citrate;
Hydrochloric Acid and/or Sodium
Hydroxide may be added to adjust pH (5.6 to 6.6), and Water for
Injection.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Brimonidine Tartrate Ophthalmic Solution is an alpha adrenergic
receptor agonist. It has a peak ocular
hypotensive effect occurring at two hours post-dosing.
Fluorophotometric studies in animals and
humans suggest that brimonidine tartrate has a dual mechanism of
action by reducing aqueous humor
production and increasing uveoscleral outflow.
PHARMACOKINETICS
After ocular administration of a 0.2% solution, plasma concentrations
peaked within 1 to 4 hours and
declined with a systemic half-life of approximately 3 hours. In
humans, systemic metabolism of
brimonidine is extensive. It is metabolized primarily by the liver.
Urinary excretion is the major route of
elimination of the drug and its metabolites. Approximately 87% of an
orally administered radioactive
dose was eliminated within 120 hours, with 74% found in the urine.
CLINICAL EVALUATIONS
Elevated IOP presents a major risk factor in glaucomatous field loss.
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