Prescrire Int. 2007 Dec;16(92):232-5.
(1) Two drugs with similar efficacy are available in France for heroin replacement therapy: methadone and buprenorphine. (2) Buprenorphine is sold in the form of sublingual tablets, but some patients dissolve and inject them. Methadone is the main alternative for these patients. Other intravenous opiate derivatives can also be tried, although they have not been approved for this indication. (3) In order to help prevent patients from injecting themselves with buprenorphine, a sublingual combination of buprenorphine + naloxone is to be marketed in France. (4) From a pharmacological point of view, this combination makes sense. Naloxone, an opiate antagonist, is very poorly absorbed with sublingual administration, but if it is injected intravenously, it will antagonise the effects of buprenorphine. However, clinical studies are needed to determine whether or not this prevents injection. (5) A double-blind trial in 326 patients compared replacement therapy with buprenorphine 16 mg + naloxone 4 mg/day versus buprenorphine 16 mg + placebo. The addition of naloxone did not reduce the efficacy of sublingual buprenorphine, but the frequency with which patients injected the drugs was not studied in this trial. (6) This combination of buprenorphine + naloxone has not been directly compared with methadone. (7) In addition to the classical adverse effects of opiates, buprenorphine can cause hepatic adverse effects. (8) Little evidence is available on the effects of intravenous injection of buprenorphine + naloxone. According to an epidemiological survey conducted in Finland, where the combination is also marketed, about 8% of patients regularly inject it intravenously. (9) Patients who are likely to inject buprenorphine should be switched to methadone.
（1）在法国，有两种疗效相似的药物可用于海洛因替代疗法：美沙酮和丁丙诺啡。（2）丁丙诺啡以舌下片形式出售，但一些患者会将其溶解后注射。美沙酮是这些患者的主要替代药物。其他静脉注射阿片类衍生物也可尝试，尽管它们尚未被批准用于此适应症。（3）为帮助预防患者注射丁丙诺啡，丁丙诺啡+纳洛酮舌下组合制剂将在法国上市。（4）从药理学角度来看，这种组合是合理的。纳洛酮是一种阿片拮抗剂，舌下给药时吸收很差，但如果静脉注射，它将拮抗丁丙诺啡的作用。然而，需要进行临床研究以确定这是否能防止注射。（5）一项针对326名患者的双盲试验比较了丁丙诺啡16毫克+纳洛酮4毫克/天与丁丙诺啡16毫克+安慰剂的替代疗法。添加纳洛酮并未降低舌下丁丙诺啡的疗效，但该试验未研究患者注射药物的频率。（6）丁丙诺啡+纳洛酮这种组合尚未与美沙酮进行直接比较。（7）除了阿片类药物的经典不良反应外，丁丙诺啡还可引起肝脏不良反应。（8）关于静脉注射丁丙诺啡+纳洛酮的效果，几乎没有证据。根据在芬兰进行的一项流行病学调查，该组合在芬兰也有销售，约8%的患者经常静脉注射它。（9）可能注射丁丙诺啡的患者应改用美沙酮。
