Pharmacokinetic Differences Between Morning and Evening Administration of Cyclosporine and Tacrolimus Therapy

Iwahori, Tohru; Takeuchi, Hirohito; Matsuno, Naoto; Johjima, Y.; Konno, Osamu; Nakamura, Yuki; Hama, K.; Uchiyama, M; Ashizawa, Tetsuo; Okuyama, Kiyoshi; Nagao, Toshiyasu; Abudoshukur, M.; Hirano, Toshihiko; Oka, Kitaro

doi:10.1016/j.transproceed.2005.02.104

Cited by 27 publications

(22 citation statements)

References 6 publications

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“…A few studies have reported that tacrolimus pharmacokinetics showed circadian variation [1–3]. Min et al .…”

Section: Discussionmentioning

confidence: 99%

“…[2] and Iwahori et al . [3] have reported that the AUC 0–12 of tacrolimus was significantly greater, C max was higher and t max was shorter after the morning dose than after the evening dose in 12 stable liver and 11 kidney allograft recipients, respectively, in the early stage after transplantation. In the maintenance state, Hardinger et al .…”

Section: Discussionmentioning

confidence: 99%

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Lack of tacrolimus circadian pharmacokinetics and CYP3A5 pharmacogenetics in the early and maintenance stages in Japanese renal transplant recipients

Satoh

Kagaya

Saito

et al. 2008

Brit J Clinical Pharma

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WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Circadian variations of tacrolimus pharmacokinetics are controversial.• Also, the pharmacokinetics has time-dependent variability, such as a decrease in oral clearance and increase in the dose-adjusted AUC after transplantation.• Although the CYP3A5 polymorphism is associated with tacrolimus pharmacokinetics, differences in the influence of this gene on the pharmacokinetics between the early and maintenance stages have not yet been clarified. WHAT THIS STUDY ADDS• Tacrolimus pharmacokinetics did not show circadian variation in either the early or maintenance stage with our designated-time administration strategy. • Based on previous results and our own findings, the interval between food consumption and tacrolimus administration might influence the interindividual and interinstitutional variability of tacrolimus chronopharmacokinetics.• The CYP3A5 polymorphism may be associated with the time-dependent changes in tacrolimus oral clearance. AIMSWe investigated whether tacrolimus pharmacokinetics shows circadian variation and the influence of the CYP3A5 A6986G polymorphism on the pharmacokinetics in both the early and maintenance stages after renal transplantation. METHODSTacrolimus was administered twice daily at specified times (09.00 and 21.00 h) throughout the pre-and post-transplant period according to the trough-targeting strategy. Fifty recipients with stable graft function were studied on day 28 and beyond 1-year post transplantation. Whole blood samples were collected prior to and 1, 2, 3, 4, 6, 9 and 12 h after both the morning and evening doses during hospitalization. RESULTSTacrolimus pharmacokinetics did not show circadian variation in either the early or maintenance stage [AUC0-12 197.1 (95% confidence interval 182.9, 212.3) in daytime vs. 203.6 ng h ml -1 (189.8, 217.4) in the night-time at day 28, 102.0 (92.1, 111.9) vs. 107.7 (97.9, 117.5) at 1 year, respectively]. In CYP3A5 *1 allele carriers (CYP3A5 expressers), body weight-adjusted oral clearance was markedly decreased from the early stage to the maintenance stage [0.622 (0.534, 0.709) CONCLUSIONEquivalent daytime and night-time tacrolimus pharmacokinetics were achieved during both the early and maintenance stages with our specified-time administration strategy. The CYP3A5 polymorphism may be associated with the time-dependent changes in the oral clearance of tacrolimus, suggesting that genotyping of this polymorphism is useful for determining the appropriate dose of tacrolimus in both the early and maintenance stages after renal transplantation.

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“…A few studies have reported that tacrolimus pharmacokinetics showed circadian variation [1–3]. Min et al .…”

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Lack of tacrolimus circadian pharmacokinetics and CYP3A5 pharmacogenetics in the early and maintenance stages in Japanese renal transplant recipients

Satoh

Kagaya

Saito

et al. 2008

Brit J Clinical Pharma

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“…11) Oral administration of tacrolimus to kidney transplant patients 30 min after breakfast or supper yields T max values of 3.1 h and 7.5 h, respectively. 16) Thus, the T max seems to be delayed by supper intake. Furthermore, in liver transplant patients, the T max is prolonged in the evening (2.9 3.5 h) compared to the morning (1.6 h).…”

Section: Discussionmentioning

confidence: 95%

Pharmacokinetics of Orally Administered Tacrolimus in Lupus Nephritis Patients

et al. 2010

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The pharmacokinetics of orally administered tacrolimus were examined in six female lupus nephritis patients (mean age 43 years, range 24 55 years). Tacrolimus (3 mg) was administered after supper, and blood tacrolimus concentrations were measured just prior to dosing and 1, 2, 4, 6, 8, 12 and 24 h after administration. The maximum blood concentration (C max ) was observed 4 8 h (mean: 6.7 h) after administration. The mean C max and area under the tacrolimus concentrationti-me curve (AUC 0 24 h ) were 12.7 ng/ml and 163.1 ng･h/ml, respectively. Although there was a weak correlation between AUC 0 24 h values and tacrolimus concentrations 2, 4, and 6 h after administration, concentrations at 12 h and 24 h were highly correlated with AUC 0 24 h values, suggesting that the trough concentration (C 24 h ) and C 12 h are valid markers for therapeutic tacrolimus monitoring. Enzyme-linked immunoabsorbent assay (ELISA) and microparticle enzyme immunoassay (MEIA) measurements of blood tacrolimus concentrations were similar. We recommend that monitoring should be carried out by C 12 h in lupus nephritis outpatients.

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“…In the authors' data, the AUC 0-12 , AUC 0-4 , C 2 , and C max following evening administration were significant lower than those following morning administration both in patients treated with CYA and patients treated with TAC 46,47) (Figure 11). As TAC shows gradual blood concentration-time curve in comparison with CYA, TAC is hardly affected by delayed or reduced absorption in the evening, so that the differences between various PK parameters between morning and evening were smaller in TAC (Table 4).…”

Section: Pharmacokinetic Differences Between Morning and Eveningmentioning

confidence: 86%

Optimal Pharmacokinetics of Cyclosporine and Tacrolimus Based Relationship Among AUC, Trough and Peak Concentration

Takeuchi¹

2012

Readings in Advanced Pharmacokinetics - Theory, Methods and Applications

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Pharmacokinetic Differences Between Morning and Evening Administration of Cyclosporine and Tacrolimus Therapy

Cited by 27 publications

References 6 publications

Lack of tacrolimus circadian pharmacokinetics and CYP3A5 pharmacogenetics in the early and maintenance stages in Japanese renal transplant recipients

Lack of tacrolimus circadian pharmacokinetics and CYP3A5 pharmacogenetics in the early and maintenance stages in Japanese renal transplant recipients

Pharmacokinetics of Orally Administered Tacrolimus in Lupus Nephritis Patients

Optimal Pharmacokinetics of Cyclosporine and Tacrolimus Based Relationship Among AUC, Trough and Peak Concentration

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