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Brimonidine
Published in Anton C. de Groot, 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
Published in Neil T. Choplin, Carlo E. Traverso, Atlas of Glaucoma, 2014
Jennifer E. Williamson, Janet B. Serle
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.
The prophylactic effect of betaxolol 0.5% versus brimonidine 0.2% on IOP elevation after Nd:YAG laser posterior capsulotomy
Published in Clinical and Experimental Optometry, 2022
Navid Elmi Sadr, Elnaz Saber, Fatemeh Paknazar
Studies have shown that IOP begins to increase just after laser application and reaches a peak after 3–4 hours.3–6,12,15,20 However, this acute rise of IOP is transient but can be vision-threatening in some patients. Brimonidine 0.2% and apraclonidine 0.5% have become the drugs of choice for prophylaxis of IOP elevation after laser application.8,9 Brimonidine tartrate is a selective α2-adrenergic agonist which lowers IOP by decreasing aqueous production and increasing uveoscleral outflow.23 Ocular allergic reactions, central nervous system depression, dry mouth, and granulomatous anterior uveitis are the reported side effects of brimonidine.12,13,24 So, as there are limitations to the use of brimonidine in all patients, numerous studies have been performed to compare the effectiveness of other anti-glaucoma medications with brimonidine 0.2% and with each other to prevent acute IOP rise following Nd:YAG laser posterior capsulotomy. Brimonidine purite 0.15%, bimatoprost 0.03%, levobunolol 0.5%, timolol 0.5%, pilocarpin, dorzolamide 2% and oral acetazolamide have been studied.12–20
Brimonidine tartrate ophthalmic solution 0.025% for redness relief: an overview of safety and efficacy
Published in Expert Review of Clinical Pharmacology, 2022
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.
Fixed-combination topical anti-hypertensive ophthalmic agents
Published in Expert Opinion on Pharmacotherapy, 2020
Lindsay Machen, Reza Razeghinejad, Jonathan S. Myers
Brimonidine is preserved with BAK and manufactured in a 0.1%, 0.15%, and 0.2% formulation with an approximate pH of 6.5 [26]. The 0.15% formulation tends to be better tolerated however all formulations can result in adverse ocular surface side effects and discontinuation [45,46]. Brimonidine is lipophilic and can cross the blood-brain-barrier with potential systemic side effects; brimonidine is contraindicated in children less than 2 years of age due to the risk of bradycardia, hypotension, and respiratory depression [44]. Despite the absolute contraindication in children, brimonidine is the only category B medication in pregnancy, defined as animal studies showing no demonstrable risk to a fetus without adequate and well-controlled studies in pregnant women [41]. While brimonidine is safe during pregnancy, brimonidine can be excreted in breast milk, and given the potentially devastating consequences of infantile exposure, avoidance of brimonidine in breastfeeding mothers has been recommended [47]. Due to the alpha-2 stimulation, brimonidine can cause a mild pupillary miosis.