Pentazocine and codeine: effects on human performance and mood and interactions with diazepam.

Medical biology Pub Date : 1986-01-01
U Saarialho-Kere, M J Mattila, T Seppälä
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Abstract

Effects of two opioid analgesics on performance and their interactions with diazepam were studied double-blind and cross over in ten healthy students. At two-week intervals the subjects received first a single oral dose of placebo, codeine (100 mg) or pentazocine (75 mg). Then, 1 h 30 min later they were all given diazepam (0.25 mg/kg) orally. Lastly, naloxone (0.4 mg) was injected intravenously at 4 h. In addition to this, the subjects on pentazocine received a second 75 mg dose at 3 h. Codeine and pentazocine alone failed to affect performance in objective tests (body sway, digit symbol substitution, flicker fusion, Maddox wing, nystagmus) recorded at 1 h 30 min. Visual analogue scales showed subjective drug effects: pentazocine made the volunteers talkative, contented, interested and energetic, whilst codeine rendered them mentally slow. 75 mg of pentazocine and 100 mg of codeine produced comparable plasma opiate activity (determined in morphine equivalents) according to radioreceptor bioassay with [3H]-dihydromorphine as a ligand. Impaired performance was clear at the tests done 1.5 and 2.5 h after diazepam. No major interactions were found between opiates and diazepam in objective tests with the exception that nystagmus was stronger after the combined treatment than after diazepam alone. Codeine reduced the absorption of diazepam. Subjectively codeine and pentazocine counteracted the effects of diazepam. The subjects overestimated their performance after opiate + diazepam when compared to diazepam alone.(ABSTRACT TRUNCATED AT 250 WORDS)

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戊唑嗪和可待因:对人类表现和情绪的影响以及与地西泮的相互作用。
对10名健康学生进行双盲和交叉实验,研究了两种阿片类镇痛药对学业成绩的影响及其与地西泮的相互作用。每隔两周,受试者首先接受单剂量口服安慰剂,可待因(100毫克)或戊唑嗪(75毫克)。1 h 30 min后给予地西泮(0.25 mg/kg)口服。最后,在4小时静脉注射纳洛酮(0.4 mg)。除此之外,在3小时服用戊唑嗪的受试者接受第二次75 mg剂量。单独使用可待因和戊唑嗪在1小时30分钟记录的客观测试(身体摇摆、数字符号替换、闪烁融合、马多克斯翼、眼球震颤)中没有影响表现。视觉模拟评分显示主观药物效应:Pentazocine使志愿者健谈,满足,感兴趣和精力充沛,而可待因使他们智力迟钝。根据以[3H]-二氢吗啡为配体的放射受体生物测定,75毫克戊唑嗪和100毫克可待因产生相当的血浆阿片活性(以吗啡当量测定)。在地西泮后1.5和2.5小时的测试中,表现明显受损。在客观试验中没有发现阿片类药物和地西泮之间的主要相互作用,除了联合治疗后的眼球震颤比单独使用地西泮后的眼球震颤更强。可待因减少地西泮的吸收。主观上可待因和戊唑嗪抵消了地西泮的作用。与单独使用地西泮相比,受试者高估了阿片类药物+地西泮后的表现。(摘要删节250字)
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