Department of Anesthesiology, Albany Medical College, Albany, NY 12208, USA.
Clin J Pain. 2011 Nov-Dec;27(9):824-38. doi: 10.1097/AJP.0b013e31821d8ac1.
The metabolism of opioids is critical to consider for multiple reasons. The most commonly prescribed opioid agents often have metabolites that are active and are the source of both analgesic activity and an increased incidence of adverse events. Many opioids are metabolized by cytochrome P450 enzymes. Polymorphisms in cytochrome P450 genes and inhibition or induction of cytochrome P450 enzymes by coadministered drugs may significantly impact the systemic concentration of opioids and their metabolites and the associated efficacy or adverse events.
This is a narrative review of the metabolism of various opioids that will highlight the impact of their active metabolites, and the potential impact of cytochrome P450 activity on analgesic activity.
An understanding of "opioid metabolic machinery," cytochrome P450 activity, and drug-drug interactions in the context of opioid selection may benefit clinicians and patients alike.
A greater appreciation of the metabolism of commonly prescribed opioid analgesics and the impact of their active metabolites on efficacy and safety may aid prescribers in tailoring care for optimal outcomes.
考虑到多种原因，阿片类药物的代谢至关重要。最常开的阿片类药物往往有代谢物，这些代谢物具有活性，是产生镇痛作用和增加不良反应发生率的根源。许多阿片类药物是由细胞色素 P450 酶代谢的。细胞色素 P450 基因的多态性以及同时使用的药物对细胞色素 P450 酶的抑制或诱导，可能会显著影响阿片类药物及其代谢物的全身浓度，以及相关的疗效或不良反应。
这是对各种阿片类药物代谢的叙述性综述，将重点介绍其活性代谢物的影响，以及细胞色素 P450 活性对镇痛活性的潜在影响。
了解“阿片类药物代谢机制”、细胞色素 P450 活性和药物-药物相互作用在阿片类药物选择方面的情况，可能使临床医生和患者都受益。
更深入地了解常用阿片类镇痛药的代谢以及其活性代谢物对疗效和安全性的影响，可能有助于临床医生为达到最佳效果而调整治疗方案。
