Department of Clinical Pharmacy, University Medical Center Utrecht, Heidelberglaan 100, 3584 CX Utrecht, The Netherlands.
Department of Radiology and Nuclear Medicine, University Medical Center Utrecht, Heidelberglaan 100, 3584 CX Utrecht, The Netherlands.
Int J Mol Sci. 2022 Jan 13;23(2):818. doi: 10.3390/ijms23020818.
The prevalence of obesity has increased dramatically in the Western population. Obesity is known to influence not only the proportion of adipose tissue but also physiological processes that could alter drug pharmacokinetics. Yet, there are no specific dosing recommendations for radiopharmaceuticals in this patient population. This could potentially lead to underdosing and thus suboptimal treatment in obese patients, while it could also lead to drug toxicity due to high levels of radioactivity. In this review, relevant literature is summarized on radiopharmaceutical dosing and pharmacokinetic properties, and we aimed to translate these data into practical guidelines for dosing of radiopharmaceuticals in obese patients. For radium-223, dosing in obese patients is well established. Furthermore, for samarium-153-ethylenediaminetetramethylene (EDTMP), dose-escalation studies show that the maximum tolerated dose will probably not be reached in obese patients when dosing on MBq/kg. On the other hand, there is insufficient evidence to support dose recommendations in obese patients for rhenium-168-hydroxyethylidene diphosphonate (HEDP), sodium iodide-131, iodide 131-metaiodobenzylguanidine (MIBG), lutetium-177-dotatate, and lutetium-177-prostate-specific membrane antigen (PSMA). From a pharmacokinetic perspective, fixed dosing may be appropriate for these drugs. More research into obese patient populations is needed, especially in the light of increasing prevalence of obesity worldwide.
肥胖症在西方人群中的患病率显著增加。肥胖不仅已知会影响脂肪组织的比例，还会影响可能改变药物药代动力学的生理过程。然而，在这种患者人群中，没有针对放射性药物的具体剂量建议。这可能导致肥胖患者用药不足，从而治疗效果不佳，同时也可能由于放射性水平高而导致药物毒性。在这篇综述中，总结了有关放射性药物剂量和药代动力学特性的相关文献，我们旨在将这些数据转化为肥胖患者放射性药物剂量的实用指南。对于镭-223，肥胖患者的剂量已经确定。此外，对于钐-153-乙二胺四亚甲基膦酸（EDTMP），剂量递增研究表明，当按 MBq/kg 给药时，肥胖患者可能无法达到最大耐受剂量。另一方面，没有足够的证据支持肥胖患者使用放射性药物锝-168-羟乙基二膦酸盐（HEDP）、碘化钠-131、碘-131-间碘苄胍（MIBG）、镥-177- DOTATATE 和镥-177-前列腺特异性膜抗原（PSMA）的剂量建议。从药代动力学的角度来看，这些药物可能适合固定剂量。需要对肥胖患者人群进行更多的研究，特别是考虑到全球肥胖症患病率的不断增加。
