Coluzzi F, Mattia C
Department of Anesthesia, Intensive Care Medicine and Pain Therapy, La Sapienza University, Rome, Italy.
Minerva Anestesiol. 2005 Jul-Aug;71(7-8):451-60.
Opioids are widely used as effective analgesic therapy for cancer pain. Despite years of controversy, their use has been also accepted in chronic non-cancer pain. Oxycodone alone and in combination has been used for over 80 years in the treatment of a variety of pain syndromes. As single agent, the controlled release (CR) oxycodone's market in the USA grew from 10% in 1996 to 53% in 2000 and it has become a leading opioid in the United States. Recent data showed that the fixed-combination oxycodone/acetaminophen (5 mg/325 mg) is the most often prescribed opioid across all the different chronic pain diagnoses. Compared with morphine, oxycodone has a higher oral bioavailability and is about twice as potent. Pharmacokinetic-pharmacodynamic data support oxycodone as a pharmacologically active opiod that does not require conversion to oxymoprhone for pharmacological activity. Seven studies addressed the safety and efficacy of oxycodone for the treatment of non-cancer pain (low back pain, osteoarthritis pain, and painful diabetic neuropathy). Both immediate release (IR) and CR oxycodone are equally effective and safe. Along these trials, mean daily dosage of oxycodone was approximately 40 mg, with a low incidence of intolerable typical opiate side effects. In cancer pain, oxycodone can be considered a valid alternative to oral morphine to be used for opioid rotation. No difference in analgesic efficacy between CR oxycodone and CR morphine was found. Controlled-release preparations, with a long duration of action, are attractive because they offer the advantage of longer dosing intervals and sustained analgesic effect.
阿片类药物被广泛用作癌症疼痛的有效镇痛疗法。尽管存在多年争议,但它们在慢性非癌性疼痛中的使用也已被接受。羟考酮单独使用或联合使用已在多种疼痛综合征的治疗中应用了80多年。作为单一药物,控释(CR)羟考酮在美国的市场份额从1996年的10%增长到2000年的53%,并已成为美国领先的阿片类药物。最近的数据显示,固定复方羟考酮/对乙酰氨基酚(5毫克/325毫克)是所有不同慢性疼痛诊断中最常处方的阿片类药物。与吗啡相比,羟考酮具有更高的口服生物利用度,效力约为吗啡的两倍。药代动力学-药效学数据支持羟考酮作为一种药理活性阿片类药物,其药理活性不需要转化为羟吗啡酮。七项研究探讨了羟考酮治疗非癌性疼痛(腰痛、骨关节炎疼痛和糖尿病性神经痛)的安全性和有效性。即释(IR)和CR羟考酮同样有效且安全。在这些试验中,羟考酮的平均日剂量约为40毫克,难以耐受的典型阿片类副作用发生率较低。在癌症疼痛中,羟考酮可被视为用于阿片类药物轮换的口服吗啡的有效替代药物。未发现CR羟考酮和CR吗啡在镇痛效果上有差异。作用持续时间长的控释制剂很有吸引力,因为它们具有给药间隔时间长和持续镇痛效果的优势。