BRIMONIDINE TARTRATE- brimonidine tartrate solution
Bryant Ranch Prepack
1 INDICATIONS AND USAGE
Brimonidine Tartrate Ophthalmic Solution, 0.15% is indicated for the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
2 DOSAGE AND ADMINISTRATION
The recommended dose is one drop of Brimonidine Tartrate Ophthalmic Solution, 0.15% in the affected eye(s) three-times daily, approximately 8 hours apart.
Brimonidine Tartrate Ophthalmic Solution, 0.15% may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure. If more than one topical ophthalmic product is being used, the products should be administered at least 5 minutes apart.
3 DOSAGE FORMS AND STRENGTHS
Brimonidine tartrate ophthalmic solution, 1.5 mg/mL.
Brimonidine Tartrate Ophthalmic Solution, 0.15% is contraindicated in patients with hypersensitivity to any component of this product.
5 WARNINGS AND PRECAUTIONS
5.1 Potentiation of Vascular Insufficiency
Brimonidine Tartrate Ophthalmic Solution, 0.15% may potentiate syndromes associated with vascular insufficiency. Brimonidine Tartrate Ophthalmic Solution, 0.15% should be used with caution in patients with depression, cerebral or coronary insufficiency, Raynaud’s phenomenon, orthostatic hypotension, or thromboangiitis obliterans.
6 ADVERSE REACTIONS
6.1 Clinical Studies Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
Adverse events occurring in approximately 10-20% of the subjects included: allergic conjunctivitis, conjunctival hyperemia, and eye pruritis.
Adverse events occurring in approximately 5-9% of the subjects included: burning sensation, conjunctival folliculosis, hypertension, ocular allergic reaction, oral dryness, and visual disturbance.
Events occurring in approximately 1-4% of subjects included: allergic reaction, arthralgia, arthritis, asthenia, blepharitis, blepharoconjunctivitis, blurred vision, bronchitis, cataract, chest pain, conjunctival edema, conjunctival hemorrhage, conjunctivitis, cough, dizziness, diabetes mellitus, dyspepsia, dyspnea, epiphora, eye discharge, eye dryness, eye irritation, eye pain, eyelid edema, eyelid erythema, fatigue, flu syndrome, follicular conjunctivitis, foreign body sensation, gastrointestinal disorder, headache, hypercholesterolemia, hypotension, infection, insomnia, joint disorder, keratitis, lid disorder, osteoporosis, pharyngitis, photophobia, rash, rhinitis, sinus infection, sinusitis, somnolence, stinging, superficial punctate keratopathy, tearing, visual field defect, vitreous detachment, vitreous disorder, vitreous floaters, and worsened visual acuity.
The following events were reported in less than 1% of subjects: corneal erosion, nasal dryness, and taste perversion.
6.2 Postmarketing Experience
The following events have been identified during post-marketing use of brimonidine tartrate ophthalmic solutions in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. The events, which have been chosen for inclusion due to either their seriousness, frequency of reporting, possible causal connection to brimonidine tartrate ophthalmic solutions, or a combination of these factors, include: bradycardia, iritis, miosis, skin reactions (including erythema, eyelid pruritis, rash, and vasodilation), and tachycardia. Apnea, bradycardia, hypotension, hypothermia, hypotonia, and somnolence have been reported in infants receiving brimonidine tartrate ophthalmic solutions.
7 DRUG INTERACTIONS
7.1 Anti-hypertensives / Cardiac Glycosides
Alpha-2 agonists, as a class, may reduce blood pressure. Caution in using drugs such as beta-blockers (ophthalmic and systemic), anti-hypertensives and/or cardiac glycosides is advised.
7.2 CNS Depressants
Although specific drug interaction studies have not been conducted with Brimonidine Tartrate Ophthalmic Solution, 0.15%, the possibility of an additive or potentiating effect with CNS depressants (alcohol, barbiturates, opiates, sedatives, or anesthetics) should be considered.
7.3 Tricyclic Antidepressants
Tricyclic antidepressants have been reported to blunt the hypotensive effect of systemic clonidine. It is not known whether the concurrent use of these agents with Brimonidine Tartrate Ophthalmic Solution, 0.15% in humans can lead to resulting interference with its IOP-lowering effect. Caution, however, is advised in patients taking tricyclic antidepressants, which can affect the metabolism and uptake of circulating amines.
7.4 Monoamine Oxidase Inhibitors
Monoamine oxidase (MAO) inhibitors may theoretically interfere with the metabolism of brimonidine and potentially result in an increased systemic side-effect such as hypotension. Caution is advised in patients taking MAO inhibitors which can affect the metabolism and uptake of circulating amines
8 USE IN SPECIFIC POPULATIONS
Pregnancy Category: B
Reproductive studies performed in rats and rabbits with oral doses of 0.66 mg base/kg revealed no evidence of harm to the fetus due to Brimonidine Tartrate Ophthalmic Solution, 0.15%. Dosing at this level produced an exposure in rats and rabbits that is 80 and 40 times higher than the exposure seen in humans, respectively.
There are no adequate and well-controlled studies in pregnant women. In animal studies, brimonidine crossed the placenta and entered into the fetal circulation to a limited extent. Brimonidine Tartrate Ophthalmic Solution, 0.15% should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.
8.3 Nursing Mothers
It is not known whether this drug is excreted in human milk. In animal studies, brimonidine tartrate was excreted in breast milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
8.4 Pediatric Use
In a well-controlled clinical study conducted in pediatric glaucoma patients (ages 2 to 7 years), the most commonly observed adverse events with brimonidine tartrate ophthalmic solution 0.2% dosed three-times-daily were somnolence (50%-83% in patients ages 2 to 6 years) and decreased alertness. In pediatric patients 7 years of age or older (>20 kg), somnolence appears to occur less frequently (25%). Approximately 16% of patients on brimonidine tartrate ophthalmic solution discontinued from the study due to somnolence.
The safety and effectiveness of brimonidine tartrate ophthalmic solution have not been studied in pediatric patients below the age of 2 years. Brimonidine tartrate ophthalmic solution is not recommended for use in pediatric patients under the age of 2 years.
8.5 Geriatric Use
No overall differences in safety or effectiveness have been observed between elderly and other adult patients.
No information is available on overdosage in humans. Treatment of an oral overdose includes supportive and symptomatic therapy; a patent airway should be maintained.
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:
Formula: C11 H10 BrN5 • C4 H6 O6
CAS Number: 59803-98-4
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.
Contains: Active ingredient: brimonidine tartrate 1.5 mg/mL, Preservative: POLYQUAD* 0.01 mg/mL, Inactives: povidone, boric acid, sodium borate, calcium chloride, magnesium chloride, potassium chloride, mannitol, sodium chloride, purified water, with hydrochloric acid and/or sodium hydroxide to adjust pH.
All MedLibrary.org resources are included in as near-original form as possible, meaning that the information from the original provider has been rendered here with only typographical or stylistic modifications and not with any substantive alterations of content, meaning or intent.