Kokki Hannu, Kumpulainen Elina, Lehtonen Marko, Laisalmi Merja, Heikkinen Marja, Savolainen Jouko, Rautio Jarkko
Department of Pharmacology and Toxicology, University of Kuopio, PO Box 1627, 70211 Kuopio, Finland.
Pediatrics. 2007 Oct;120(4):e1002-8. doi: 10.1542/peds.2007-0064.
Ibuprofen is the most commonly used nonsteroidal, antipyretic, antiinflammatory analgesic in children. Nonsteroidal, antipyretic, antiinflammatory analgesics act in both the peripheral tissues and the central nervous system. The central nervous system penetration of ibuprofen has been described in adults but not in children.
Our goals were to investigate the cerebrospinal fluid penetration of ibuprofen in children and evaluate the analgesic plasma concentration of ibuprofen after inguinal surgery in children.
A total 36 healthy children (25 boys) aged 3 months to 12 years received a single intravenous injection of ibuprofen (10 mg/kg). A paired cerebrospinal fluid and blood sample was obtained 10 minutes to 8 hours after the injection. In children having inguinal surgery, a second blood sample was obtained at the time that the child first had wound pain.
The ibuprofen level was determined in all cerebrospinal fluid and plasma samples. Cerebrospinal fluid concentrations ranged between 15 and 541 microg/L, and the highest concentrations were measured 30 to 38 minutes after dosing. In all cerebrospinal fluid samples collected after 30 minutes, ibuprofen concentration exceeded that of unbound plasma. The plasma analgesic concentrations after inguinal surgery ranged between 10 and 25 mg/L.
Ibuprofen penetrates the cerebrospinal fluid readily, with peak concentrations attained 30 to 40 minutes after intravenous injection of a 10 mg/kg dose. The plasma analgesic concentration after inguinal surgery with spinal anesthesia is 10 to 25 mg/L.
布洛芬是儿童最常用的非甾体类解热、抗炎镇痛药。非甾体类解热、抗炎镇痛药在外周组织和中枢神经系统均有作用。布洛芬在成人中的中枢神经系统渗透情况已有描述,但在儿童中尚无相关报道。
我们的目标是研究布洛芬在儿童中的脑脊液渗透情况,并评估儿童腹股沟手术后布洛芬的镇痛血浆浓度。
36名年龄在3个月至12岁的健康儿童(25名男孩)接受了单次静脉注射布洛芬(10mg/kg)。注射后10分钟至8小时采集配对的脑脊液和血液样本。对于接受腹股沟手术的儿童,在其首次出现伤口疼痛时采集第二份血液样本。
测定了所有脑脊液和血浆样本中的布洛芬水平。脑脊液浓度在15至541μg/L之间,给药后30至38分钟测得最高浓度。在30分钟后采集的所有脑脊液样本中,布洛芬浓度超过了未结合血浆中的浓度。腹股沟手术后的血浆镇痛浓度在10至25mg/L之间。
布洛芬能轻易穿透脑脊液,静脉注射10mg/kg剂量后30至40分钟达到峰值浓度。脊髓麻醉下腹股沟手术后的血浆镇痛浓度为10至25mg/L。