BRIMONIDINE TARTRATE solution

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 1.5 mg in 1 mL

Administration route:

OPHTHALMIC

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Brimonidine Tartrate Ophthalmic Solution, 0.15% is indicated for the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Brimonidine Tartrate Ophthalmic Solution, 0.15% 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, 0.15% is supplied sterile in opaque white LDPE plastic bottles and natural tips with purple polypropylene caps as follows: 10 mL in 10 mL bottle NDC 54868-6094-0 Storage: Store at 15°-25° C (59° - 77°F). Rx Only Distributed by: Falcon Pharmaceuticals, Ltd. Fort Worth, Texas 76134 Manufactured by: Alcon Laboratories, Inc. Fort Worth, Texas 76134 Printed in USA *POLYQUAD is a registered trademark of Alcon Research, Ltd. **ALPHAGAN P is a registered trademark of Allergan, Inc. 349040-1008

Authorization status:

New Drug Application

Summary of Product characteristics

BRIMONIDINE TARTRATE - BRIMONIDINE TARTRATE SOLUTION
PHYSICIANS TOTAL CARE, INC.
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DESCRIPTION
Brimonidine Tartrate Ophthalmic Solution, 0.15% (1.5 mg brimonidine
tartrate per mL equivalent to
1.0 mg brimonidine free base per mL) is a relatively selective
alpha-2-adrenergic agonist for
ophthalmic use. The chemical name of brimonidine tartrate is
5-bromo-6-(2-imidazolidinylideneamino)
quinoxaline L-tartrate. It is an off-white to pale yellow powder. It
has a molecular weight of 442.24 as
the tartrate salt, and is both soluble in water (1.5 mg/mL) and in the
product vehicle (3.0 mg/mL) at
pH 7.2. The structural formula is:
In solution, Brimonidine Tartrate Ophthalmic Solution, 0.15% has a
clear, greenish-yellow color. It has
an osmolality of 250 - 350 mOsmol/kg and a pH of 6.6-7.4.
Each mL of Brimonidine Tartrate Ophthalmic Solution, 0.15% contains:
ACTIVE INGREDIENT: brimonidine
tartrate 0.15% (1.5 mg/mL) INACTIVES: povidone; boric acid; sodium
borate; calcium chloride;
magnesium chloride; potassium chloride; mannitol; sodium chloride;
POLYQUAD* 0.001%
(0.01 mg/mL); purified water; with hydrochloric acid and/or sodium
hydroxide to adjust pH.
CLINICAL PHARMACOLOGY
Mechanism of Action:
Brimonidine Tartrate Ophthalmic Solution, 0.15% is an alpha-2
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:
In a pharmacokinetic study, 14 healthy subjects (4 males and 10
females) received a single topical
ocular administration of Brimonidine Tartrate Ophthalmic Solution,
0.15%, one drop per eye. The peak
plasma concentrations (C
) and AUC
were 73 ± 19 pg/mL and 375 ± 89 pg•hr/mL, respectively.
T
was 1.7 ± 0.7 hours after dosing. The systemic half-life was
approximately 2.1 hours.
Brimonidine is metabolized primarily by the liver. _In vitro
_metabolism data from