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术后疼痛中肌肉注射美普他酚与吗啡的比较

Intramuscular meptazinol and morphine in postoperative pain.

作者信息

Kaiko R F, Wallenstein S L, Rogers A G, Canel A, Jacobs B, Houde R W

出版信息

Clin Pharmacol Ther. 1985 May;37(5):589-96. doi: 10.1038/clpt.1985.92.

Abstract

Meptazinol is an agonist-antagonist opioid analgesic believed to be unique in its selectivity for mu1 (high affinity) receptors and its cholinergic activity. Our objectives were to determine the relative analgesic potency of intramuscular meptazinol and morphine and to compare mood and side effects in 102 patients with cancer who have postoperative pain. Meptazinol (50, 100, and 200 mg) and morphine (4, 8, and 16 mg) were given for moderate to severe pain in a double-blind, randomized but balanced, incomplete block design. Serial multiple assessments of pain, relief, mood, and side effects were made. The most precise estimates of relative analgesic potency indicate that meptazinol is equivalent to 10 mg morphine at 120 mg (95% confidence interval 80 to 170 mg) for peak effect and at 175 mg (95% confidence interval 125 to 270 mg) for total effect. Mean (+/- SE) times to peak effect and to remedication were 0.9 +/- 0.1 and 3.6 +/- 0.2 hours for meptazinol and 1.4 +/- 0.1 and 4.8 +/- 0.4 hours for morphine at equianalgesic peak effects. The percentages of subjects with one or more side effects were 18, 49, and 73 for graded meptazinol doses and 32, 49, and 65 for graded morphine doses. Mean numbers of side effects per subject were 0.3, 1.5, and 3.5 for meptazinol and 0.5, 0.7, and 1.7 for morphine. Profiles of side effects differed. Mood improvement and overall satisfaction were dose related and greater for morphine than for meptazinol. Side effects may limit the use of meptazinol in doses that relieve severe postoperative pain.

摘要

美普他酚是一种激动 - 拮抗型阿片类镇痛药,据信其对μ1(高亲和力)受体具有独特的选择性以及具有胆碱能活性。我们的目的是确定肌肉注射美普他酚和吗啡的相对镇痛效力,并比较102例术后疼痛的癌症患者的情绪和副作用。美普他酚(50、100和200毫克)和吗啡(4、8和16毫克)用于中度至重度疼痛,采用双盲、随机但平衡的不完全区组设计。对疼痛、缓解情况、情绪和副作用进行了系列多次评估。相对镇痛效力的最精确估计表明,美普他酚在120毫克(95%置信区间80至170毫克)时达到峰值效应,在175毫克(95%置信区间125至270毫克)时达到总效应,相当于10毫克吗啡。在等效镇痛峰值效应时,美普他酚达到峰值效应和再次用药的平均(±标准误)时间分别为0.9±0.1小时和3.6±0.2小时,吗啡分别为1.4±0.1小时和4.8±0.4小时。使用分级美普他酚剂量时,出现一种或多种副作用的受试者百分比分别为18%、49%和73%,使用分级吗啡剂量时分别为32%、49%和65%。每位受试者的平均副作用数量,美普他酚分别为0.3、1.5和3.5,吗啡分别为0.5、0.7和1.7。副作用的情况有所不同。情绪改善和总体满意度与剂量相关,吗啡比美普他酚更明显。副作用可能会限制美普他酚用于缓解严重术后疼痛的剂量。

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