Brimonidine
Anton C. de Groot in Monographs in Contact Allergy, 2021
Brimonidine is a quinoxaline derivative and a selective α2-adrenergic receptor agonist. Upon ocular administration, brimonidine acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor; it also enhances its outflow. Brimonidine ophthalmic solution is indicated for patients with open- angle glaucoma or ocular hypertension to lower intraocular pressure. A topical gel is indicated for the treatment of persistent facial erythema of rosacea in adults, where it reduces erythema through direct vasoconstriction. In pharmaceutical products, brimonidine is employed as brimonidine tartrate (CAS number 70359-46-5, EC number not available, molecular formula C15H16BrN5O6) (1).
Medical Therapy for Glaucoma
Neil T. Choplin, Carlo E. Traverso in Atlas of Glaucoma, 2014
Both apraclonidine and brimonidine have been approved by the USFDA for three times daily administration. These agents are commonly prescribed twice daily due to the poor compliance with t.i.d. dosing. IOP should be evaluated in the afternoon to determine whether t.i.d. dosing would be beneficial in an individual patient. Side effects include dry mouth, fatigue, drowsiness, systemic hypotension, and ocular allergy, which occur in about 12% of patients receiving brimonidine and up to 35% of patients receiving apraclonidine (Figure 14.10). An allergic response to apraclonidine does not preclude the use of brimonidine. Between 10% and 20% of patients with a documented ocular allergic response to apraclonidine developed an allergy to brimonidine. Brimonidine was formulated in concentrations of 0.15% and 0.1% to reduce the rate of allergy.
Acne, rosacea, and similar disorders
Rashmi Sarkar, Anupam Das, Sumit Sethi in Concise Dermatology, 2021
Erythemato-telangiectatic rosacea: Topical alpha receptor agonists like brimonidine (0.5%) have shown the strongest efficacy in controlling facial erythema in rosacea. Another alpha receptor agonist, oxymetazoline, has also shown good results. Topical tacrolimus has been shown to cause improvement in a small number of cases. In patients not responding to topical treatment, low‐dose β‐blocking medications, e.g. propranolol should be considered. Laser therapy (using pulse dye laser, intense pulsed light) can also be used to eliminate the malar telangiectatic vessels. In recalcitrant lesions, botulinum toxins have been found to be helpful to reduce facial flushing.
Low‐dose brimonidine for relief of ocular redness: integrated analysis of four clinical trials
Published in Clinical and Experimental Optometry, 2019
Stacey L Ackerman, Gail L Torkildsen, Eugene Mclaurin, Jason L Vittitow
Brimonidine is a highly selective α2‐receptor agonist with relatively low binding affinity for α1 receptors (ratio of α2: α1 binding affinity of ~1,000:1).1998 Because α2 receptors are expressed predominantly in veins, it is possible that α2‐receptor agonists for ocular use may have a lower potential for tachyphylaxis and rebound redness.2007 Brimonidine is approved by the US Food and Drug Administration in an ophthalmic solution (0.15 and 0.2-per cent) for lowering intraocular pressure in patients with open‐angle glaucoma or ocular hypertension,1998 and in a topical gel (0.33-per cent) for the treatment of non‐transient facial erythema of rosacea in adults.2013 Additionally, brimonidine instilled in the eyes at low doses (0.025–0.2 per cent) has been shown to control bleeding during ocular surgery,2002 prevent bleeding from intravitreal injections,2011 and induce conjunctival blanching before surgery,2009 demonstrating the ocular vasoconstrictive effects of brimonidine. In December 2017, low‐dose brimonidine tartrate (0.025 per cent; Lumify eye drops, Bausch & Lomb Incorporated, Rochester, New York, USA) received approval in the USA to relieve redness of the eye due to minor irritations.2017
Evaluation of Efficacy and Safety of Brimonidine Tartrate Ophthalmic Solution, 0.025% for Treatment of Ocular Redness
Published in Current Eye Research, 2018
Gail L. Torkildsen, Christine M. Sanfilippo, Heleen H. DeCory, Paul J. Gomes
As expected based on results for mean ocular redness, the percentage of subjects with total clearance of ocular redness at Day 0 (Visit 1) was significantly higher in the brimonidine treatment group compared to the vehicle treatment group at all post-instillation assessment times (P ≤ 0.040; Figure 2). The proportion of subjects with total clearance peaked at the 15 minute time point with 78.9% of the subjects in the brimonidine group showing total clearance, and at 4 hours post-instillation, 22% of subjects still maintained total clearance. Brimonidine remained effective at reducing ocular redness throughout the study with 34.5% and 33.3% of brimonidine-treated subjects showing total clearance of redness at 5 minutes post-instillation on Days 14 and 28 (Visits 2 and 3), respectively, compared to none of the vehicle-treated subjects (P ≤ 0.0161). Similarly, in the PP population, a greater percentage of subjects in the brimonidine treatment group had total clearance of ocular redness compared to the vehicle treatment group at all time points throughout the study (P ≤ 0.014), with the exception of the 240 minute time point on Day 0 (P = 0.1374).
Brimonidine tartrate ophthalmic solution 0.025% for redness relief: an overview of safety and efficacy
Published in Expert Review of Clinical Pharmacology, 2022
Jihei Sara Lee, Chan Yun Kim
A number of studies have since then demonstrated a possible alternative: brimonidine tartrate, an α2-adrenergic receptor agonist, originally approved in 1996 as an ophthalmic solution at a concentration of 0.2% for lowering intraocular pressure (IOP) in patients with glaucoma or ocular hypertension. Topical application of the drug effectively reduced hyperemia and subconjunctival hemorrhage following various types of ocular surgery [14–17]. In 2013, the drug was approved for treatment of persistent facial erythema in a form of a topical gel in a concentration of 0.33% [18,19]. In 2017, it was approved for the purpose of relieving conjunctival hyperemia by the US Food and Drug Administration in a lower concentration, 0.025%. Numerous clinical trials have so far established efficacy and safety of brimonidine. In this review, we examine the mechanism, efficacy, and safety of low-dose brimonidine tartrate in relieving ocular redness.
Related Knowledge Centers
- Glaucoma
- Hypotension
- Ocular Hypertension
- Rosacea
- Allergy
- Pregnancy
- Alpha-2 Adrenergic Receptor
- Medication
- Eye Drop
- Aqueous Humour