Department of Pediatric Nephrology, Faculty of Medicine and Health Sciences, Ghent University Hospital, C. Heymanslaan 10, 9000, Ghent, Belgium.
Health, Innovation and Research Institute, Faculty of Medicine and Health Sciences, Ghent University Hospital, C. Heymanslaan 10, 9000, Ghent, Belgium.
Paediatr Drugs. 2020 Aug;22(4):369-383. doi: 10.1007/s40272-020-00401-7.
Desmopressin is a synthetic analogue of the natural antidiuretic hormone arginine vasopressin. Over the years, it has been clinically used to manage nocturnal polyuria in children with enuresis. Various pharmaceutical formulations of desmopressin have been commercialized for this indication-nasal spray, nasal drops, oral tablet and oral lyophilizate. Despite the fact that desmopressin is a frequently prescribed drug in children, its use and posology is based on limited pediatric data. This review provides an overview of the current pediatric pharmacological data related to the different desmopressin formulations, including their pharmacokinetics, pharmacodynamics and adverse events. Regarding the pharmacokinetics, a profound food effect on the oral bioavailability was demonstrated as well as different plasma concentration-time profiles (double absorption peak) of the desmopressin lyophilizate between adults and children. Literature about maturational differences in distribution, metabolism and excretion of desmopressin is rather limited. Regarding the pharmacodynamics, formulation/dose/food effect and predictors of response were evaluated. The lyophilizate is the preferred formulation, but the claimed bioequivalence in adults (200 µg tablet and 120 µg lyophilizate), could not be readily extrapolated to children. Prescribing the standard flat-dose regimen to the entire pediatric population might be insufficient to attain response to desmopressin treatment, whereby dosing schemes based on age and weight were proposed. Moreover, response to desmopressin is variable, whereby complete-, partial- and non-responders are reported. Different reasons were enumerated that might explain the difference in response rate to desmopressin observed: different pathophysiological mechanisms, bladder capacity and other predictive factors (i.e. breast feeding, familial history, compliance, sex, etc.). Also, the relapse rate of desmopressin treatment was high, rendering it necessary to use a pragmatic approach for the treatment of enuresis, whereby careful consideration of the position of desmopressin within this treatment is required. Regarding the safety of the different desmopressin formulations, the use of desmopressin was generally considered safe, but additional measures should be taken to prevent severe hyponatremia. To conclude the review, to date, major knowledge gaps in pediatric pharmacological aspects of the different desmopressin formulations still remain. Additional information should be collected about the clinical relevance of the double absorption peak, the food effect, the bioequivalence/therapeutic equivalence, the pediatric adapted dosing regimens, the study endpoints and the difference between performing studies at daytime or at nighttime. To fill in these gaps, additional well designed pharmacokinetic and pharmacodynamic studies in children should be performed.
去氨加压素是一种合成的精氨酸血管加压素的天然抗利尿激素类似物。多年来,它已在临床上用于治疗遗尿症儿童的夜间多尿。为了这一适应证,已将不同的去氨加压素药物制剂商业化,包括鼻喷雾剂、滴鼻剂、口服片剂和口服冻干剂。尽管去氨加压素是儿童常用的处方药物,但它的使用和剂量是基于有限的儿科数据。这篇综述提供了一个关于不同去氨加压素制剂的儿科药理学数据的概述,包括它们的药代动力学、药效学和不良事件。关于药代动力学,已经证明了口服生物利用度受到食物的显著影响,以及成人和儿童之间去氨加压素冻干剂的不同血浆浓度-时间曲线(双峰吸收)。关于去氨加压素分布、代谢和排泄的成熟差异的文献相当有限。关于药效学,评估了制剂/剂量/食物效应和反应预测因子。冻干剂是首选的制剂,但在成人中声称的生物等效性(200µg 片剂和 120µg 冻干剂),不能轻易外推到儿童。对整个儿科人群使用标准的平坦剂量方案可能不足以达到去氨加压素治疗的反应,因此提出了基于年龄和体重的剂量方案。此外,去氨加压素的反应是可变的,报告了完全、部分和无反应者。列举了不同的原因,可能解释了观察到的去氨加压素反应率的差异:不同的病理生理机制、膀胱容量和其他预测因素(即母乳喂养、家族史、依从性、性别等)。此外,去氨加压素治疗的复发率很高,因此需要对遗尿症的治疗采取务实的方法,这就需要仔细考虑去氨加压素在这种治疗中的地位。关于不同去氨加压素制剂的安全性,去氨加压素的使用一般被认为是安全的,但需要采取额外的措施来预防严重的低钠血症。总之,到目前为止,不同去氨加压素制剂的儿科药理学方面仍存在重大知识空白。应该收集更多关于双峰吸收、食物效应、生物等效性/治疗等效性、儿科适应剂量方案、研究终点以及在白天或夜间进行研究之间的差异的临床相关性的信息。为了填补这些空白,应该在儿童中进行更多的、精心设计的药代动力学和药效学研究。