Other dermatologicals

Brimonidine Tartrate

Approved 31 Jan 2022EyeSolution/drops

The FDA lists this product in 22 strengths and forms.

Indications

Brimonidine tartrate ophthalmic solution, 0.15% is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. Brimonidine tartrate ophthalmic solution is an alpha adrenergic agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. ( 1 )

Contraindications

Neonates and infants (pediatric patients younger than 2 years old). ( 4.1 ) Hypersensitivity Reactions. ( 4.2 )

4.1Neonates and Infants (Pediatric Patients Younger than 2 Years Old)

Brimonidine tartrate ophthalmic solution is contraindicated in neonates and infants (pediatric patients younger than 2 years old) [see Use in Specific Populations ( 8.4 )] .

4.2Hypersensitivity Reactions

Brimonidine tartrate ophthalmic solution is contraindicated in patients who have exhibited a hypersensitivity reaction to any component of this medication in the past.

Warnings and precautions

Potentiation of vascular insufficiency. ( 5.1 )

5.1Potentiation of Vascular Insufficiency

Brimonidine tartrate ophthalmic solution may potentiate syndromes associated with vascular insufficiency. Brimonidine tartrate ophthalmic solution should be used with caution in patients with depression, cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, or thromboangiitis obliterans.

5.2Severe Cardiovascular Disease

Although brimonidine tartrate ophthalmic solution had minimal effect on the blood pressure of patients in clinical studies, caution should be exercised in treating patients with severe cardiovascular disease.

Indications

Contraindications

Neonates and infants (pediatric patients younger than 2 years old). ( 4.1 ) Hypersensitivity Reactions. ( 4.2 )

4.1Neonates and Infants (Pediatric Patients Younger than 2 Years Old)

Brimonidine tartrate ophthalmic solution is contraindicated in neonates and infants (pediatric patients younger than 2 years old) [see Use in Specific Populations ( 8.4 )] .

4.2Hypersensitivity Reactions

Brimonidine tartrate ophthalmic solution is contraindicated in patients who have exhibited a hypersensitivity reaction to any component of this medication in the past.

Warnings and precautions

Potentiation of vascular insufficiency. ( 5.1 )

5.1Potentiation of Vascular Insufficiency

5.2Severe Cardiovascular Disease

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

There are no adequate and well-controlled studies with brimonidine tartrate ophthalmic solution in pregnant women. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. In animal studies, brimonidine crossed the placenta and entered into the fetal circulation to a limited extent (see Data). Because animal reproduction studies are not always predictive of human response, brimonidine tartrate ophthalmic solution should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.

Data Human Data Limited available data from postmarketing safety reports and published literature with topical use of brimonidine ophthalmic solution in pregnant women are insufficient to inform a drug-associated risk of pregnancy-related adverse outcomes including miscarriage, stillbirth, congenital anomaly, and events experienced by offspring while breastfeeding. Animal Data Embryofetal studies were conducted in pregnant rabbits administered brimonidine tartrate by daily oral gavage on gestation days 6 to 18, to target the period of organogenesis.

Brimonidine caused miscarriage at 5 mg/kg/day (approximately 70-or 50-times the recommended human ophthalmic dose [RHOD] based on AUC, respectively for brimonidine tartrate 0.15%). The no observed adverse effect level (NOAEL) for developmental toxicity in rabbits was 1 mg/kg/day (approximately 9-and 6-fold the RHOD based on AUC, respectively for brimonidine tartrate 0.15%). No treatment-related malformations were observed in rabbits.

Signs of maternal sedation and fatigue were observed at all dose levels; the lowest observed adverse effect level (LOAEL) for maternal toxicity was 5 mg/kg/day, based on the dose response for these signs. Embryofetal studies were conducted in pregnant rats administered brimonidine tartrate by daily oral gavage on gestation days 6 to 15, to target the period of organogenesis. The NOAEL for developmental toxicity was 2.5 mg/kg/day (approximately 1,100-and 750-fold the RHOD based on AUC, respectively for brimonidine tartrate 0.15%).

No treatment-related malformations were observed in rats. The LOAEL for maternal toxicity was 2.5 mg/kg/day, based on signs of sedation and fatigue. The maternal NOAEL was 1 mg/kg/day (250-and 180-fold the RHOD based on AUC, respectively for brimonidine tartrate 0.15%). After pregnant rats received a single oral dose of 14 C-brimonidine tartrate, brimonidine and metabolites crossed the placenta and were detectable in fetal blood and organs.

Adverse reactions

The following serious adverse reactions are described elsewhere in the labeling: Potentiation of Vascular Insufficiency [see Warnings and Precautions ( 5.1 )] Severe Cardiovascular Disease [see Warnings and Precautions ( 5.2 )] Contamination of Topical Ophthalmic Products after Use [see Warnings and Precautions ( 5.3 )] Neonates and Infants (Pediatric Patients Younger than 2 Years Old) [see Contraindications ( 4.1 )] Most common adverse reactions occurring in approximately 5% to 20% of patients receiving brimonidine ophthalmic solution (0.1% to 0.2%) included allergic conjunctivitis, burning sensation, conjunctival folliculosis, conjunctival hyperemia, eye pruritus, hypertension, ocular allergic reaction, oral dryness, and visual disturbance.

( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Apotex Corp. at 1-800-706-5575 or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials 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 reactions occurring in approximately 10% to 20% of the subjects receiving brimonidine ophthalmic solution (0.1% to 0.2%) included: allergic conjunctivitis, conjunctival hyperemia, and eye pruritus.

Adverse reactions occurring in approximately 5% to 9% included: burning sensation, conjunctival folliculosis, hypertension, ocular allergic reaction, oral dryness, and visual disturbance. Adverse reactions occurring in approximately 1% to 4% of the subjects receiving brimonidine ophthalmic solution (0.1% to 0.2%) included: abnormal taste, allergic reaction, asthenia, blepharitis, blepharoconjunctivitis, blurred vision, bronchitis, cataract, conjunctival edema, conjunctival hemorrhage, conjunctivitis, cough, dizziness, 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 (primarily colds and respiratory infections), insomnia, keratitis, lid disorder, 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 reactions were reported in less than 1% of subjects: corneal erosion, hordeolum, nasal dryness, and taste perversion.

6.2Postmarketing Experience

The following reactions have been identified during postapproval use of brimonidine tartrate ophthalmic solutions. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Bradycardia, depression, hypersensitivity, iritis, keratoconjunctivitis sicca, miosis, nausea, skin reactions (including erythema, eyelid pruritus, rash, and vasodilation), syncope, and tachycardia.

Apnea, coma, hypotension, hypothermia, hypotonia, lethargy, pallor, respiratory depression, and somnolence have been reported in infants receiving brimonidine tartrate ophthalmic solutions.

Brimonidine Tartrate

Indications

Contraindications

4.1Neonates and Infants (Pediatric Patients Younger than 2 Years Old)

4.2Hypersensitivity Reactions

Warnings and precautions

5.1Potentiation of Vascular Insufficiency

5.2Severe Cardiovascular Disease

Two medicines in one question?

Brimonidine Tartrate

Indications

Contraindications

4.1Neonates and Infants (Pediatric Patients Younger than 2 Years Old)

4.2Hypersensitivity Reactions

Warnings and precautions

5.1Potentiation of Vascular Insufficiency

5.2Severe Cardiovascular Disease

Two medicines in one question?

5.3Contamination of Topical Ophthalmic Products After Use

Interactions

7.1Antihypertensives/Cardiac Glycosides

7.2CNS Depressants

7.3Tricyclic Antidepressants

7.4Monoamine Oxidase Inhibitors

Pregnancy and breastfeeding

8.1Pregnancy Risk Summary

Adverse reactions

6.1Clinical Trials Experience

6.2Postmarketing Experience

Composition

Strengths and forms

Official product information

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