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:

Physicians Total Care, Inc.

INN (International Name):

BRIMONIDINE TARTRATE

Composition:

BRIMONIDINE TARTRATE 2 mg in 1 mL

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Brimonidine tartrate ophthalmic solution 0.2% is indicated for lowering intraocular pressure in patients with open-angle glaucoma or ocular hypertension. The lOP lowering efficacy of brimonidine tartrate ophthalmic solution 0.2% 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 0.2% 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 sterile in a plastic bottle with a controlled drop tip in the following sizes: 5 mL bottles      NDC 54868-6287-0 10 mL bottles    NDC 54868-6287-1

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

BRIMONIDINE TARTRATE - BRIMONIDINE TARTRATE SOLUTION/ DROPS
PHYSICIANS TOTAL CARE, INC.
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BRIMONIDINE TARTRATE
OPHTHALMIC SOLUTION 0.2% (STERILE)
RX ONLY
DESCRIPTION:
Brimonidine Tartrate Ophthalmic Solution 0.2% is a relatively
selective alpha-2 adrenergic agonist for
ophthalmic use. In solution, brimonidine tartrate ophthalmic solution
0.2% has a clear, greenish-yellow
color. It has an osmolality of 280-330 mOsml/kg and a pH of 5.6-6.6
The structural formula is
C
H BrN • C H O
Mol. Wt. 442.24 (as the tartrate salt)
CHEMICAL NAME: 5-bromo-6-(2-imidazolidinylideneamino) quinoxaline
L-tartrate.
CAS Number 59803-98-4
EACH ML CONTAINS:
ACTIVE: Brimonidine tartrate: 0.2% (2 mg/mL).
INACTIVES: Citric Acid, Polyvinyl Alcohol, Sodium Chloride, Sodium
Citrate, Purified Water.
Hydrochloric Acid and/or Sodium Hydroxide may be added to adjust pH.
PRESERVATIVE ADDED: Benzalkonium Chloride (0.05 mg).
CLINICAL PHARMACOLOGY:
MECHANISM OF ACTION:
Brimonidine tartrate ophthalmic solution 0.2% 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:
11
10
5
4
6
6
Elevated IOP presents a major risk factor in glaucomatous field loss.
The higher the level of lOP, the
greater the likelihood of optic nerve damage and visual field loss.
Brimonidine tartrate has the action of
loweri