Adis, Auckland, New Zealand.
CNS Drugs. 2009 Oct;23(10):899-902. doi: 10.2165/11203740-000000000-00000.
Buprenorphine/naloxone (Suboxone) comprises the partial micro-opioid receptor agonist buprenorphine in combination with the opioid antagonist naloxone in a 4 : 1 ratio. When buprenorphine/naloxone is taken sublingually as prescribed, the naloxone exerts no clinically significant effect, leaving the opioid agonist effects of buprenorphine to predominate. However, when buprenorphine/naloxone is parenterally administered in patients physically dependent on full agonist opioids, the opioid antagonism of naloxone causes withdrawal effects, thus reducing the abuse potential of the drug combination. Buprenorphine/naloxone is an effective maintenance therapy for opioid dependence and has generally similar efficacy to methadone, although more data are needed. Less frequent dispensing of buprenorphine/naloxone (e.g. thrice weekly) does not appear to compromise efficacy and can improve patient satisfaction. Buprenorphine/naloxone is more effective than clonidine as a medically supervised withdrawal therapy. Moreover, buprenorphine/naloxone is a generally well tolerated medically supervised withdrawal and maintenance treatment. Thus, sublingual buprenorphine/naloxone is a valuable pharmacotherapy for the treatment of opioid dependence.
丁丙诺啡/纳洛酮（Suboxone）由部分μ-阿片受体激动剂丁丙诺啡与阿片受体拮抗剂纳洛酮以 4：1 的比例组成。当丁丙诺啡/纳洛酮被舌下含服处方使用时，纳洛酮不会产生临床上显著的效果，使丁丙诺啡的阿片激动作用占主导地位。然而，当丁丙诺啡/纳洛酮被给予依赖于完全激动剂阿片类药物的患者进行注射时，纳洛酮的阿片拮抗剂作用会引起戒断效应，从而降低药物组合的滥用潜力。丁丙诺啡/纳洛酮是一种有效的阿片类药物依赖维持治疗方法，其疗效与美沙酮大致相似，尽管还需要更多的数据。较少频率的丁丙诺啡/纳洛酮（例如每周三次）给药似乎不会影响疗效，并可以提高患者的满意度。丁丙诺啡/纳洛酮作为一种有医学监督的戒断治疗方法比可乐定更有效。此外，丁丙诺啡/纳洛酮作为一种有医学监督的戒断和维持治疗方法，通常具有良好的耐受性。因此，舌下含服丁丙诺啡/纳洛酮是治疗阿片类药物依赖的一种有价值的药物治疗方法。
