Mathisen Lene Cecilie, Skjelbred Per, Skoglund Lasse A, Øye Ivar
Department of Pharmacology, Oslo University School of Medicine, Oslo Norway Department of Maxillofacial Surgery, Ullevål Hospital, Oslo Norway Section of Dental Pharmacology and Pharmacotherapeutics, University of Oslo, Oslo Norway.
Pain. 1995 May;61(2):215-220. doi: 10.1016/0304-3959(94)00170-J.
We examined the analgesic effect of racemic ketamine and its 2 enantiomers in 16 female patients (age: 20-29 years) suffering acute pain after oral surgery and in 7 female patients (age: 42-79 years) suffering chronic neuropathic orofacial pain. All 3 forms of ketamine consistently relieved postoperative pain, (S)-ketamine being 4 times more potent than (R)-ketamine. The analgesic effect was maximal 5 min after i.m. injection and lasted for about 30 min. The 7 patients with neuropathic pain received ketamine at one or several occasions. Four patients (age: 54-79 years) who had suffered pain for more than 5 years did not experience an analgesic effect, whereas 3 patients (age: 42-53 years) who had suffered pain for less than 3 years reported pain relief lasting from 24 h to 3 days. The individual type of response did not depend on the form of ketamine used. The mental side effects were qualitatively similar for the 3 forms of ketamine. Relative to the analgesic effect (S)-ketamine caused more disturbing side effects than did (R)-ketamine. The mean serum concentration of each form of ketamine at the time of maximal effect was close to the approximate Kd value for PCP site occupancy by that particular form. This is in concert with the hypothesis that the effect of ketamine on acute nociceptive pain is due to N-methyl-D-aspartate (NMDA) receptor inhibition and adds to the evidence that NMDA receptors are important for the perception of acute, nociceptive pain in humans.(ABSTRACT TRUNCATED AT 250 WORDS)
我们研究了消旋氯胺酮及其两种对映体对16名（年龄20 - 29岁）口腔手术后遭受急性疼痛的女性患者以及7名（年龄42 - 79岁）患有慢性神经性口面部疼痛的女性患者的镇痛效果。氯胺酮的所有三种形式均能持续缓解术后疼痛，其中(S)-氯胺酮的效力是(R)-氯胺酮的4倍。肌肉注射后5分钟镇痛效果达到最大，并持续约30分钟。7名神经性疼痛患者曾一次或多次接受氯胺酮治疗。4名疼痛超过5年的患者（年龄54 - 79岁）未体验到镇痛效果，而3名疼痛少于3年的患者（年龄42 - 53岁）报告疼痛缓解持续24小时至3天。个体反应类型不取决于所用氯胺酮的形式。氯胺酮的三种形式在精神方面的副作用在性质上相似。相对于镇痛效果，(S)-氯胺酮比(R)-氯胺酮引起的不良副作用更多。每种形式的氯胺酮在最大效应时的平均血清浓度接近该特定形式占据苯环己哌啶（PCP）位点的近似解离常数（Kd）值。这与氯胺酮对急性伤害性疼痛的作用是由于N - 甲基 - D - 天冬氨酸（NMDA）受体抑制的假设一致，并进一步证明NMDA受体对人类急性伤害性疼痛的感知很重要。（摘要截选至250字）
