Cherry D A, Gourlay G K
Pain Management Unit, Flinders Medical Centre, Bedford Park, Australia.
Agents Actions. 1994 Oct;42(3-4):173-4. doi: 10.1007/BF01983487.
Of the currently available mu agonist drugs, the following are relatively contraindicated: 1. Methadone--unpredictable duration of action [5]. 2. Pethidine--unwanted central effects, metabolised to an active metabolite and too short acting. 3. Codeine--too weak and with constipating side-effects. 4. Fentanyl--too short acting. 5. Oxycodone--too short acting although suppositories may overcome some theoretical disadvantages. 6. Dextropropoxyphene--weak agonist which is possibly metabolised to a cardiotoxic metabolite [6]. Morphine remains the drug of choice for chronic pain when administered in a sustained release preparation. MS Contin, a slow release oral formulation of morphine, is available and has a predictable duration of action lasting from 8-12 h, while improved formulations are about to be released in the near future in some countries. Prescribers need to take into account the relatively poor oral bioavailability of morphine when calculating the daily morphine dose.
在目前可用的μ阿片受体激动剂药物中，以下药物相对禁忌使用：1. 美沙酮——作用持续时间不可预测[5]。2. 哌替啶——有不良的中枢作用，可代谢为活性代谢物且作用时间过短。3. 可待因——作用太弱且有便秘副作用。4. 芬太尼——作用时间过短。5. 羟考酮——作用时间过短，尽管栓剂可能克服一些理论上的缺点。6. 右丙氧芬——弱激动剂，可能代谢为心脏毒性代谢物[6]。当以缓释制剂给药时，吗啡仍然是慢性疼痛的首选药物。美施康定是一种吗啡缓释口服制剂，已可获得，其作用持续时间可预测，为8至12小时，而在一些国家，改进型制剂在不久的将来即将推出。开处方者在计算每日吗啡剂量时需要考虑到吗啡相对较差的口服生物利用度。
