Hoffmann Ullrich, Kuno Saskia, Franke Gerd, Fusch Christoph, Haas Johannes P
Department of Pharmacology, Ernst-Moritz-Arndt University Greifswald, Friedrich-Loeffler-Str. 23d, D-17487 Greifswald, Germany.
Pediatr Crit Care Med. 2004 May;5(3):282-5. doi: 10.1097/01.pcc.0000123548.73664.18.
Brimonidine tartrate is a relatively selective alpha(2) adrenic agonist that lowers elevated intraocular pressure. A 2-yr-old boy presented with severe cardiorespiratory symptoms of systemic alpha(2) adrenergic intoxication after accidentally ingesting 2 mL of brimonidine ophthalmic solution (0.2%) orally. At 20 mins after ingestion, he became acutely pale and lethargic, with shallow infrequent respirations. The symptoms resolved completely within the next 10 hrs.
The pharmacokinetics of brimonidine in plasma and urine were analyzed using gas chromatography and mass spectrometry.
Maximum plasma concentrations were 40 ng/mL 5 hrs after ingestion. The plasma elimination half-life value was 2.7 hrs. Elimination via urine was calculated as having a terminal half-life value of 3.2 hrs.
This case illustrates the ability of brimonidine to gain rapid access to the central nervous system. This first passage is followed by a redistribution phase with rising plasma concentrations. Children who accidentally ingest brimonidine orally should be admitted to a pediatric intensive care unit.
酒石酸溴莫尼定是一种相对选择性的α₂肾上腺素能激动剂,可降低升高的眼压。一名2岁男孩意外口服2毫升0.2%的酒石酸溴莫尼定滴眼液后,出现严重的全身性α₂肾上腺素能中毒的心肺症状。摄入后20分钟,他变得急性面色苍白、嗜睡,呼吸浅而频率低。症状在接下来的10小时内完全缓解。
采用气相色谱和质谱法分析血浆和尿液中酒石酸溴莫尼定的药代动力学。
摄入后5小时血浆浓度最高达40纳克/毫升。血浆消除半衰期值为2.7小时。经尿液消除的终末半衰期值计算为3.2小时。
本病例说明了酒石酸溴莫尼定快速进入中枢神经系统的能力。首次通过后是血浆浓度上升的再分布阶段。意外口服酒石酸溴莫尼定的儿童应入住儿科重症监护病房。