Faculty of Pharmaceutical Sciences, The University of British Columbia, Vancouver, British Columbia, Canada.
Ann Pharmacother. 2013 Apr;47(4):543-60. doi: 10.1345/aph.1R604. Epub 2013 Apr 2.
To describe the evidence for serotonergic and adrenergic drug interactions with linezolid and discuss clinical management strategies.
A literature search of PubMed (1947-November 2012), MEDLINE (1946-November 2012), EMBASE (1974-November 2012), and International Pharmaceutical Abstracts (1970-November 2012) was conducted using the terms linezolid, drug interaction, serotonin syndrome, serotonin toxicity, sympathomimetic, serotonergic agents, and adrenergic agents. Citations of retrieved articles were also reviewed.
English-language articles describing coadministration of serotonergic or adrenergic agents with linezolid to humans were included. Studies published only in abstract form were excluded.
One prospective study, 6 retrospective studies, and 24 case reports were identified describing a serotonergic or adrenergic drug interaction. Incidence of serotonin syndrome in patients on linezolid and serotonergic agents ranged between 0.24% and 4%. Serotonergic agents determined to have probable (according to the Horn Drug Interaction Probability Scale) linezolid interactions in case reports included meperidine, citalopram, escitalopram, fluoxetine, paroxetine, sertraline, duloxetine, and venlafaxine. Serotonergic agent dose and duration of coadministration with linezolid did not appear to influence the occurrence of serotonin syndrome. Adrenergic medication coadministration was associated with a possible drug interaction as determined by the Horn Drug Interaction Probability Scale but did not appear to result in clinically significant drug interactions with linezolid.
Linezolid-associated serotonergic drug interactions occur more commonly than adrenergic interactions. Serotonergic interactions considered probable according to the Horn Drug Interaction Probability Scale do not appear to correlate with drug dosage; time of onset ranges from <1 to 20 days, and effect resolves in <1 to 5 days after discontinuation of offending agents. If coadministration of linezolid and a serotonergic agent cannot be avoided, clinicians should be aware of the symptoms and management of serotonergic toxicity; close monitoring is recommended and additional serotonergic agents should not be used. While adrenergic drug interactions with linezolid are less common in clinical practice, monitoring for signs of hypertension remains important.
描述与利奈唑胺相互作用的 5-羟色胺能和肾上腺素能药物的证据，并讨论临床管理策略。
在 PubMed（1947 年-2012 年 11 月）、MEDLINE（1946 年-2012 年 11 月）、EMBASE（1974 年-2012 年 11 月）和国际药学文摘（1970 年-2012 年 11 月）中使用了利奈唑胺、药物相互作用、血清素综合征、血清素毒性、拟交感神经药、5-羟色胺能制剂和肾上腺素能制剂等术语进行了文献检索，并对检索到的文章的参考文献进行了回顾。
纳入了描述人类同时使用 5-羟色胺能或肾上腺素能药物与利奈唑胺的协同作用的英文文章。仅以摘要形式发表的研究被排除在外。
确定了 1 项前瞻性研究、6 项回顾性研究和 24 份病例报告，描述了一种 5-羟色胺能或肾上腺素能药物相互作用。服用利奈唑胺和 5-羟色胺能药物的患者发生血清素综合征的发生率在 0.24%至 4%之间。根据霍恩药物相互作用可能性量表，被确定为与利奈唑胺有明确（probable）相互作用的 5-羟色胺能药物包括哌替啶、西酞普兰、依他普仑、氟西汀、帕罗西汀、舍曲林、度洛西汀和文拉法辛。5-羟色胺能药物的剂量和与利奈唑胺联合使用的时间似乎并没有影响血清素综合征的发生。根据霍恩药物相互作用可能性量表，肾上腺素能药物的联合使用与可能的药物相互作用有关，但似乎没有导致与利奈唑胺有临床意义的药物相互作用。
与利奈唑胺相关的 5-羟色胺能药物相互作用比肾上腺素能相互作用更常见。根据霍恩药物相互作用可能性量表，被认为是明确（probable）相互作用的 5-羟色胺能药物与药物剂量似乎没有相关性；发病时间从<1 天到 20 天不等，停药后<1 天到 5 天症状缓解。如果不能避免利奈唑胺和 5-羟色胺能药物同时使用，临床医生应了解血清素毒性的症状和管理；建议密切监测，不要同时使用其他 5-羟色胺能药物。虽然肾上腺素能药物与利奈唑胺的相互作用在临床实践中较少见，但监测高血压的迹象仍然很重要。
