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他克莫司的舌下给药:当前趋势与现有证据

Sublingual administration of tacrolimus: current trends and available evidence.

作者信息

Doligalski Christina Teeter, Liu Esther C, Sammons Chelsea M, Silverman Andrew, Logan Angela Tong

机构信息

Department of Pharmacy, Tampa General Hospital, Tampa, Florida.

出版信息

Pharmacotherapy. 2014 Nov;34(11):1209-19. doi: 10.1002/phar.1492. Epub 2014 Sep 24.

DOI:10.1002/phar.1492
PMID:25251980
Abstract

Widespread anecdotal use of sublingual tacrolimus administration has arisen, although little literature exists to guide practice. Given the paucity of data, we conducted a survey to evaluate the practice of sublingual tacrolimus administration at transplant centers across the United States and evaluated the literature that is currently available. A 10-question online survey assessing the current state of sublingual tacrolimus use was distributed to pharmacists at transplant centers that each performed more than 100 solid organ transplantations in 2013. In addition, a literature review was performed by searching the PubMed database to identify available evidence for the sublingual administration of tacrolimus. The online survey was completed by 59 (65.6%) of the 90 targeted transplant centers, representing 51.3% of all solid organ transplantations performed in 2013. Sublingual administration of tacrolimus was used in all solid organ transplant populations, with ~67% of lung transplant centers using this route for tacrolimus. The most common dose conversion was 2 mg oral to 1 mg sublingual, with 92% of centers opening oral capsules and administering the contents sublingually. Home use of sublingual administration and use in the pediatric population was uncommon. Seven peer-reviewed reports and one abstract were identified in the literature review. Seven of the eight publications reported favorably on sublingual administration, although no consistent dose conversion or method of administration was elucidated. The majority of the transplant centers surveyed found sublingual tacrolimus a viable alternative when oral administration is unavailable. A large robust prospective evaluation of sublingual administration of tacrolimus is imperative to provide the most effective care to solid organ transplant recipients and to ensure optimal safety for both patients and providers who administer the drug.

摘要

尽管指导实践的文献很少,但他克莫司舌下给药已在广泛应用。鉴于数据匮乏,我们进行了一项调查,以评估美国各移植中心他克莫司舌下给药的情况,并对现有文献进行了评估。一项包含10个问题的在线调查,评估他克莫司舌下给药的现状,已分发给2013年各自进行了超过100例实体器官移植的移植中心的药剂师。此外,通过检索PubMed数据库进行文献综述,以确定他克莫司舌下给药的现有证据。90个目标移植中心中有59个(65.6%)完成了在线调查,占2013年所有实体器官移植的51.3%。他克莫司舌下给药应用于所有实体器官移植人群,约67%的肺移植中心使用此途径给予他克莫司。最常见的剂量转换是口服2mg相当于舌下1mg,92%的中心打开口服胶囊并舌下给药其内容物。在家中使用舌下给药以及在儿科人群中的使用并不常见。在文献综述中确定了7篇同行评审报告和1篇摘要。8篇出版物中有7篇对舌下给药给予了肯定评价,尽管未阐明一致的剂量转换或给药方法。大多数接受调查的移植中心发现,当无法口服给药时,他克莫司舌下给药是一种可行的替代方法。迫切需要对他克莫司舌下给药进行大规模、有力的前瞻性评估,以便为实体器官移植受者提供最有效的护理,并确保给药的患者和医护人员的最佳安全。

相似文献

1
Sublingual administration of tacrolimus: current trends and available evidence.他克莫司的舌下给药:当前趋势与现有证据
Pharmacotherapy. 2014 Nov;34(11):1209-19. doi: 10.1002/phar.1492. Epub 2014 Sep 24.
2
Adequate exposure to tacrolimus with sublingual administration in pediatric liver transplant patients.小儿肝移植患者经舌下给药充分暴露于他克莫司。
Int J Clin Pharmacol Ther. 2017 Apr;55(4):352-354. doi: 10.5414/CP202719.
3
Sublingual tacrolimus as an alternative to oral administration for solid organ transplant recipients.对于实体器官移植受者,舌下含服他克莫司可作为口服给药的替代方法。
Am J Health Syst Pharm. 2015 Feb 15;72(4):277-84. doi: 10.2146/ajhp140322.
4
Sublingual administration of tacrolimus in a renal transplant patient.肾移植患者中他克莫司的舌下给药
J Clin Pharm Ther. 2008 Feb;33(1):87-9. doi: 10.1111/j.1365-2710.2008.00884.x.
5
Tacrolimus prolonged release (Envarsus®): a review of its use in kidney and liver transplant recipients.他克莫司缓释胶囊(Envarsus®):在肾和肝移植受者中的应用评价。
Drugs. 2015 Feb;75(3):309-20. doi: 10.1007/s40265-015-0349-2.
6
Clinical pharmacokinetics of oral versus sublingual administration of tacrolimus in adult liver transplant recipients.成人肝移植受者口服与舌下含服他克莫司的临床药代动力学
Exp Clin Transplant. 2012 Dec;10(6):586-91. doi: 10.6002/ect.2012.0032. Epub 2012 Jul 5.
7
Sublingual tacrolimus: a pharmacokinetic evaluation pilot study.舌下他克莫司:一项药代动力学评价初步研究。
Pharmacotherapy. 2013 Jan;33(1):31-7. doi: 10.1002/phar.1149.
8
Use of sublingual tacrolimus in lung transplant recipients.肺移植受者中他克莫司舌下制剂的应用。
J Heart Lung Transplant. 2012 Feb;31(2):127-32. doi: 10.1016/j.healun.2011.10.015. Epub 2011 Dec 16.
9
Conversion From Once-Daily Prolonged-Release Tacrolimus to Once-Daily Extended-Release Tacrolimus in Stable Liver Transplant Recipients.稳定期肝移植受者从每日一次的缓释他克莫司转换为每日一次的延长释放他克莫司
Exp Clin Transplant. 2018 Jun;16(3):321-325. doi: 10.6002/ect.2016.0328. Epub 2017 Jul 11.
10
Determining the conversion ratios for oral versus sublingual administration of tacrolimus in solid organ transplant recipients.确定实体器官移植受者中他克莫司口服与舌下给药的转换比率。
Clin Transplant. 2019 Oct;33(10):e13727. doi: 10.1111/ctr.13727. Epub 2019 Oct 22.

引用本文的文献

1
Recipient Versus Donor CYP3A4/5 Genotypes in Adult Liver Transplant Recipients to Achieve Therapeutic Tacrolimus Concentrations Early Post-Transplant.成年肝移植受者中受者与供者CYP3A4/5基因型对移植后早期实现他克莫司治疗浓度的影响
Clin Transl Sci. 2025 Sep;18(9):e70329. doi: 10.1111/cts.70329.
2
Composite CYP3A (CYP3A4 and CYP3A5) phenotypes and influence on tacrolimus dose adjusted concentrations in adult heart transplant recipients.成年心脏移植受者复合 CYP3A(CYP3A4 和 CYP3A5)表型及其对他克莫司剂量调整浓度的影响。
Pharmacogenomics J. 2024 Feb 15;24(2):4. doi: 10.1038/s41397-024-00325-2.
3
Bioavailability of Orally Administered Drugs in Critically Ill Patients.
口服给药在危重症患者中的生物利用度。
J Pharm Pract. 2023 Aug;36(4):967-979. doi: 10.1177/08971900221100205. Epub 2022 May 6.
4
Immunosuppression in Lung Transplantation.肺移植中的免疫抑制。
Handb Exp Pharmacol. 2022;272:139-164. doi: 10.1007/164_2021_548.
5
Safety and Efficacy of Perioperative Sublingual Tacrolimus in Pancreas Transplant Compared With Oral Tacrolimus.围手术期舌下他克莫司与口服他克莫司在胰腺移植中安全性和疗效的比较。
Exp Clin Transplant. 2021 Jun;19(6):592-595. doi: 10.6002/ect.2020.0391. Epub 2021 May 6.
6
High Variability of Whole-Blood Tacrolimus Pharmacokinetics Early After Thoracic Organ Transplantation.胸器官移植术后早期全血他克莫司药代动力学的高度变异性
Eur J Drug Metab Pharmacokinet. 2020 Feb;45(1):123-134. doi: 10.1007/s13318-019-00591-7.
7
The Evolution of Lung Transplant Immunosuppression.肺移植免疫抑制的演变。
Drugs. 2018 Jul;78(10):965-982. doi: 10.1007/s40265-018-0930-6.
8
Individualizing immunosuppression in lung transplantation.肺移植中免疫抑制的个体化
Glob Cardiol Sci Pract. 2018 Mar 14;2018(1):5. doi: 10.21542/gcsp.2018.5.