Brimonidine decreases fluid production and pressure inside the eye in patients with ocular hypertension and glaucoma and has been approved since 2013 for treatment of facial erythema of rosacea. However, recent reports indicate that topical brimonidine can result in serious side effects.
Two case reports have recently brought brimonidine into the spotlight when topical application for hemostasis resulted in depression of the central nervous system. In the first case, a 70-year man with previously treated squamous cell carcinoma on his head and neck, was subjected to application of brimonidine (0.33%) for hemostasis. This resulted in rapid decline in mental status, entering a comatose condition, but successfully returned to normal within 18 hours. In the second case, a 90-year old man suffering from painful actinic facial (left sideburn) keratosis was treated with topical brimonidine, at similar doses as the first case. The patient went into an altered mental state, but recovered within 24 hours (4).
Application of topical brominidine at similar sites in both patients, right temple and left sideburn, allowed brominidine to cross the blood brain barrier leading to a deterioration in mental condition characterised by respiratory failure and somnolence.
Previously, toxicity related to brimonidine for ulcerated hemangioma in a 2-month-old girl who developed CNS depression and apnea, which normalized within 7 hours was reported (5). Similar reports in infants (6) have resulted in cautionary advice against the use of brimonidine as a hemostatic agent, particularly for cases of endoscopic nasal and sinus surgery as well as in ophthalmology.
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- Burke J, Kharlamb A, Shan T, Runde E, Padillo E, Manlapaz C, et al. Adrenergic and imidazoline receptor-mediated responses to UK-14,304-18 (brimonidine) in rabbits and monkeys. A species difference. Ann N Y Acad Sci. 1995;763:78-95.
- Enyedi LB, Freedman SF. Safety and efficacy of brimonidine in children with glaucoma. J AAPOS. 2001;5(5):281-4.
- Shagalov DR, Taylor D, Schleichert R, Weiss J, Weiss E. Association of Central Nervous System Depression With Topical Brimonidine When Used for Hemostasis: A Serious Adverse Event. JAMA Dermatol. 2017;153(6):575-7.
- Gill K, Bayart C, Desai R, Golden A, Raimer P, Tamburro J. Brimonidine Toxicity Secondary to Topical Use for an Ulcerated Hemangioma. Pediatr Dermatol. 2016;33(4):e232-4.
- Kiryazov K, Stefova M, Iotova V. Can ophthalmic drops cause central nervous system depression and cardiogenic shock in infants? Pediatr Emerg Care. 2013;29(11):1207-9.
Written by Joseph M. Antony, PhD