Advertisement

International Journal of Clinical Pharmacy

, Volume 39, Issue 6, pp 1298–1303 | Cite as

Trough level from twice daily to once daily tacrolimus in early conversion kidney transplant recipients: a prospective study

  • Sayamon Sukkha
  • Busba Chindavijak
  • Preecha Montakantikul
  • Atiporn Ingsathit
  • Wichit Nosoongnoen
  • Vasant Sumethkul
Research Article
  • 273 Downloads

Abstract

Background Early conversion from twice-daily tacrolimus (TAC-BID) to once-daily tacrolimus (TAC-OD) provides a greater benefit of reducing under-exposure of TAC-OD during the first period after transplantation. Information regarding the conversion dose among Asian kidney transplant recipients is still limited. Objective This study aimed to compare the trough levels (Cmin) of TAC-BID (Prograf®) and TAC-OD (Advagraf®). The values were obtained from early conversion intervention by 1:1 milligram per-milligram. Setting A university-based hospital. Method This study employed a single-center, open-label, prospective and single-armed design. Fifteen de novo standard risk kidney transplant recipients were enrolled. Fourteen days after transplantation, the Cmin of TAC-BID (pre-conversion Cmin) was determined. Subsequently, TAC-BID was converted to TAC-OD with a similar dose. The Cmin of TAC-OD was first measured at a steady state (immediate post-conversion Cmin) and compared. All enrolled patients received therapeutic monitoring at the first and second months. Main outcome measure Pre-conversion Cmin of TAC-BID and immediate post-conversion Cmin of TAC-OD. Results The immediate post-conversion Cmin was found to be 23% lowered than the pre-conversion Cmin. However, the Cmin of TAC-OD was found to be similar to the pre-conversion Cmin compared during the follow-up period. Renal function was found to be stable in all patients over 2 months. Conclusion Early conversion therapy was associated with a significantly lower immediate post-conversion Cmin but comparable Cmin throughout the follow-up period. The “one to one conversion ratio” from TAC-BID to TAC-OD could be performed among Asian de novo kidney transplant recipients at an early period after transplantation.

Keywords

Early conversion Formulation Kidney transplant Tacrolimus Trough level 

Notes

Acknowledgements

The authors would like to thank Supatat Chumnumwat, PharmD, BCPS, for his assistance in drafting the manuscript. Special thanks go to Stephen Pinder and Thomas McManamon for English editing. We also wish to thank Pitchaya Dilokpattanamongkol, BCPS, BCCP, for her helpful suggestion.

Funding

This research received no specific grant from any funding agency in the public, commercial or not-for-profit sectors.

Conflicts of interest

The authors have no conflicts of interest to declare.

References

  1. 1.
    Wu MJ, Cheng CY, Chen CH, Wu WP, Cheng CH, Yu DM, et al. Lower variability of tacrolimus trough concentration after conversion from prograf to advagraf in stable kidney transplant recipients. Transplantation. 2011;92(6):648–52.CrossRefPubMedGoogle Scholar
  2. 2.
    Stifft F, Stolk LM, Undre N, van Hooff JP, Christiaans MH. Lower variability in 24-hour exposure during once-daily compared to twice-daily tacrolimus formulation in kidney transplantation. Transplantation. 2014;97(7):775–80.PubMedGoogle Scholar
  3. 3.
    Wlodarczyk Z, Squifflet JP, Ostrowski M, Rigotti P, Stefoni S, Citterio F, et al. Pharmacokinetics for once-versus twice-daily tacrolimus formulations in de novo kidney transplantation: a randomized, open-label trial. Am J Transplant. 2009;9(11):2505–13.CrossRefPubMedGoogle Scholar
  4. 4.
    Wlodarczyk Z, Ostrowski M, Mourad M, Kramer BK, Abramowicz D, Oppenheimer F, et al. Tacrolimus pharmacokinetics of once- versus twice-daily formulations in de novo kidney transplantation: a substudy of a randomized phase III trial. Ther Drug Monit. 2012;34(2):143–7.CrossRefPubMedGoogle Scholar
  5. 5.
    Borobia AM, Romero I, Jimenez C, Gil F, Ramirez E, De Gracia R, et al. Trough tacrolimus concentrations in the first week after kidney transplantation are related to acute rejection. Ther Drug Monit. 2009;31(4):436–42.CrossRefPubMedGoogle Scholar
  6. 6.
    Caillard S, Moulin B, Buron F, Mariat C, Audard V, Grimbert P, et al. Advagraf ®, a once-daily prolonged release tacrolimus formulation, in kidney transplantation: literature review and guidelines from a panel of experts. Transpl Int. 2016;29(8):860–9.CrossRefPubMedGoogle Scholar
  7. 7.
    Liu JP, Chow SC. Sample size determination for the two one-sided tests procedure in bioequivalence. J Pharmacokinet Biopharm. 1992;20(1):101–4.CrossRefPubMedGoogle Scholar
  8. 8.
    Tsuchiya T, Ishida H, Tanabe T, Shimizu T, Honda K, Omoto K, et al. Comparison of pharmacokinetics and pathology for low-dose tacrolimus once-daily and twice-daily in living kidney transplantation: prospective trial in once-daily versus twice-daily tacrolimus. Transplantation. 2013;96(2):198–204.CrossRefPubMedGoogle Scholar
  9. 9.
    European Medicines Agency (EMA). Guideline on the investigation of bioequivalence. 2010. http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/01/WC500070039.pdf. Accessed 1 Sep 2017.
  10. 10.
    Alloway R, Steinberg S, Khalil K, Gourishankar S, Miller J, Norman D, et al. Conversion of stable kidney transplant recipients from a twice daily Prograf-based regimen to a once daily modified release tacrolimus-based regimen. Transplant Proc. 2005;37(2):867–70.CrossRefPubMedGoogle Scholar
  11. 11.
    Glowacki F, Lionet A, Hammelin JP, Labalette M, Provot F, Hazzan M, et al. Influence of cytochrome P450 3A5 (CYP3A5) genetic polymorphism on the pharmacokinetics of the prolonged-release, once-daily formulation of tacrolimus in stable renal transplant recipients. Clin Pharmacokinet. 2011;50(7):451–9.CrossRefPubMedGoogle Scholar
  12. 12.
    Midtvedt K, Jenssen T, Hartmann A, Vethe NT, Bergan S, Havnes K, et al. No change in insulin sensitivity in renal transplant recipients converted from standard to once-daily prolonged release tacrolimus. Nephrol Dial Transplant. 2011;26(11):3767–72.CrossRefPubMedGoogle Scholar
  13. 13.
    Abbott Laboratories, Diagnostics Division, Abbott Park, IL, Architect System, Tacrolimus, Ref 1 L77.Google Scholar
  14. 14.
    Diez Ojea B, Alonso Alvarez M, Aguado Fernandez S, Banos Gallardo M, Garcia Melendreras S, Gomez Huertas E. Three-month experience with tacrolimus once-daily regimen in stable renal allografts. Transplant Proc. 2009;41(6):2323–5.CrossRefPubMedGoogle Scholar
  15. 15.
    de Jonge H, Kuypers DR, Verbeke K, Vanrenterghem Y. Reduced C0 concentrations and increased dose requirements in renal allograft recipients converted to the novel once-daily tacrolimus formulation. Transplantation. 2010;90(5):523–9.CrossRefPubMedGoogle Scholar
  16. 16.
    Hatakeyama S, Fujita T, Yoneyama T, Yoneyama T, Koie T, Hashimoto Y, et al. A switch from conventional twice-daily tacrolimus to once-daily extended-release tacrolimus in stable kidney transplant recipients. Transplant Proc. 2012;44(1):121–3.CrossRefPubMedGoogle Scholar
  17. 17.
    Jannot M, Masson I, Alamartine E, Mariat C. Early conversion from twice-daily tacrolimus to once-daily extended formulation in renal transplant patients before hospital discharge. Ann Transplant. 2014;19:320–4.CrossRefPubMedGoogle Scholar
  18. 18.
    Barraclough KA, Isbel NM, Johnson DW, Campbell SB, Staatz CE. Once-versus twice-daily tacrolimus: are the formulations truly equivalent? Drugs. 2011;71(12):1561–77.CrossRefPubMedGoogle Scholar
  19. 19.
    MacPhee IA, Holt DW. A pharmacogenetic strategy for immunosuppression based on the CYP3A5 genotype. Transplantation. 2008;85(2):163–5.CrossRefPubMedGoogle Scholar
  20. 20.
    Yaowakulpatana K, Vadcharavivad S, Ingsathit A, Areepium N, Kantachuvesiri S, Phakdeekitcharoen B, et al. Impact of CYP3A5 polymorphism on trough concentrations and outcomes of tacrolimus minimization during the early period after kidney transplantation. Eur J Clin Pharmacol. 2016;72(3):277–83.CrossRefPubMedGoogle Scholar
  21. 21.
    Gaber AO, Alloway RR, Bodziak K, Kaplan B, Bunnapradist S. Conversion from twice-daily tacrolimus capsules to once-daily extended-release tacrolimus (LCPT): a phase 2 trial of stable renal transplant recipients. Transplantation. 2013;96(2):191–7.CrossRefPubMedPubMedCentralGoogle Scholar
  22. 22.
    Singh N, Von Visger J, Zachariah M. Extended release once a day tacrolimus. Curr Opin Organ Transplant. 2015;20(6):657–62.CrossRefPubMedGoogle Scholar
  23. 23.
    European Medicines Agency (EMA). Envarsus (tacrolimus extended release tablets): EU summary of product characteristics. 2014. http://www.ema.europa.eu/. Accessed 1 Sep 2017.
  24. 24.
    Medicines Evaluation Board in the Netherlands. Public assessment report: tacrolimus sandoz 0.5 mg, 1 mg and 5 mg, capsules, hard Sandoz B.V. 2010. http://db.cbg-meb.nl/Pars/h102100.pdf. Accessed 1 Sep 2017.
  25. 25.
    Alloway RR, Sadaka B, Trofe-Clark J, Wiland A, Bloom RD. A randomized pharmacokinetic study of generic tacrolimus versus reference tacrolimus in kidney transplant recipients. Am J Transplant. 2012;12(10):2825–31.CrossRefPubMedPubMedCentralGoogle Scholar

Copyright information

© Springer International Publishing AG 2017

Authors and Affiliations

  • Sayamon Sukkha
    • 1
  • Busba Chindavijak
    • 1
  • Preecha Montakantikul
    • 1
  • Atiporn Ingsathit
    • 2
  • Wichit Nosoongnoen
    • 1
  • Vasant Sumethkul
    • 2
  1. 1.Division of Clinical Pharmacy, Department of Pharmacy, Faculty of PharmacyMahidol UniversityBangkokThailand
  2. 2.Department of Medicine, Faculty of Medicine, Ramathibodi HospitalMahidol UniversityBangkokThailand

Personalised recommendations