Related Experiment Video
Updated: Jul 14, 2026
08:38
Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
Once-daily tacrolimus extended-release formulation: 1-year post-conversion in stable pediatric liver transplant
T G Heffron1, M D Pescovitz, S Florman
1Emory University School of Medicine, Atlanta, GA, USA.
Summary
Pediatric liver transplant patients safely converted to once-daily tacrolimus extended-release (XL). Pharmacokinetics and safety were comparable to twice-daily tacrolimus (TAC), supporting XL as a convenient alternative.
Area of Science:
- Transplantation Immunology
- Pharmacology
- Pediatric Gastroenterology
Background:
- Tacrolimus (TAC) is a key immunosuppressant post-liver transplant.
- Current TAC formulations require twice-daily dosing.
- Optimizing dosing regimens is crucial for pediatric transplant management.
Purpose of the Study:
- To assess the pharmacokinetics, safety, and tolerability of a once-daily tacrolimus extended-release (XL) formulation.
- To evaluate the conversion from twice-daily TAC to once-daily XL in stable pediatric liver transplant recipients.
Main Methods:
- 18 stable pediatric liver transplant recipients were switched from twice-daily TAC to once-daily XL on a 1:1 dose basis.
- Pharmacokinetic profiles were analyzed on day 7 (TAC) and day 14 (XL).
- Safety and tolerability were monitored during the first year post-conversion.
Main Results:
- Steady-state exposure (AUC(0-24)) was equivalent between XL and TAC (mean XL/TAC ratio 100.9%).
- AUC(0-24) and C(min) showed strong correlations at steady state for both formulations.
- No acute rejection, graft loss, or death occurred in the first year post-conversion.
Conclusions:
- Once-daily tacrolimus extended-release (XL) is pharmacokinetically equivalent to twice-daily tacrolimus (TAC) in pediatric liver transplant recipients.
- Conversion to once-daily XL is safe and well-tolerated, with a profile consistent with TAC.
- This study supports the use of once-daily XL for convenient and effective immunosuppression in this population.
Related Concept Videos
01:26Pharmacokinetics in Pediatric Patients: Drug Excretion
In pediatric medicine, understanding the renal function and drug elimination nuances is crucial for administering safe and effective treatments. Newborns, in particular, display markedly slower renal functions than adults, profoundly affecting how drugs are cleared from their bodies. This slower drug clearance requires clinicians to extend the dosing intervals for many medications to prevent drug accumulation and toxicity while ensuring therapeutic efficacy.One key area where these adjustments...
01:24Pharmacokinetics in Pediatric Patients: Drug Metabolism
In pediatric care, understanding the nuances of hepatic drug metabolism is crucial, as it significantly differs from that of adults. This divergence is primarily due to the developmental stage of drug-metabolizing enzymes, which affects how medications are processed in the body. In neonates, for instance, the activity of Phase I enzymes—critical for the initial breakdown of drugs—is markedly reduced, functioning at just 20–40% of the levels seen in adults. This reduction poses a challenge in...
01:23Pharmacokinetics in Pediatric Patients: Overview and Drug Absorption
Understanding the physiological differences in the pediatric population is crucial for effective pharmacotherapy. Neonates, infants, and children exhibit significant variations in gastric pH, gastric emptying time, intestinal transit time, and biliary function. These variations profoundly affect oral drug absorption, necessitating a nuanced approach to pediatric dosing.Neonates present with a unique physiological profile, having a gastric pH greater than 4 and faster and more irregular gastric...
01:26Kidney Transplant II: Surgical Procedure
Preoperative ManagementThe primary goals of preoperative management in kidney transplantation are to optimize the patient’s metabolic state and prepare them for surgery through diet adjustments, necessary dialysis, and tailored medical treatment. This phase also involves comprehensive infection screening and patient education about the surgical procedure and postoperative care to improve outcomes and adherence.Medical ManagementA comprehensive evaluation is required for both the living donor...
01:17Pharmacokinetics in Pediatric Patients: Drug Distribution
Drug distribution in the pediatric population exhibits unique challenges and considerations due to the physiological differences between children, particularly neonates and infants, and adults. A crucial aspect of pediatric pharmacology is understanding how these differences impact the pharmacokinetics of various drugs, necessitating age-specific dosing strategies to ensure efficacy and safety.Neonates and infants have a higher total body water content, ~75%–90% of their body weight, compared...
01:01Dosage Regimen: Fixed Dose
Fixed-dose regimens are a common approach to administer drugs to achieve and maintain desired levels of the drug in the body. In this dosing strategy, a specific amount of medication is given at regular intervals, often multiple times a day, to ensure a consistent drug concentration in the bloodstream.
Fixed-dose regimens can be used for various routes of administration, including intravenous (IV) injections and oral medications. For IV administration, a predetermined amount of the drug is...
Fixed-dose regimens can be used for various routes of administration, including intravenous (IV) injections and oral medications. For IV administration, a predetermined amount of the drug is...