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- Title
Lisdexamfetamine and amphetamine pharmacokinetics in oral fluid, plasma, and urine after controlled oral administration of lisdexamfetamine.
- Authors
Comiran, Eloisa; Carlos, Graciela; Barreto, Fabiano; Pechanksy, Flavio; Fröehlich, Pedro E.; Limberger, Renata P.
- Abstract
Lisdexamfetamine (LDX) is a long‐acting prodrug stimulant indicated for the treatment of attention‐deficit/hyperactivity disorder (ADHD) and binge‐eating disorder (BED) symptoms. In vivo hydrolysis of the LDX amide bond releases the therapeutically active d‐amphetamine (d‐AMPH). This study aims to describe the pharmacokinetics of LDX and its major metabolite d‐AMPH in human oral fluid, urine and plasma after a single 70 mg oral dose of LDX dimesylate. Six volunteers participated in the study. Oral fluid and blood samples were collected for up to 72 h and urine for up to 120 h post‐drug administration for the pharmacokinetic evaluation of intact LDX and d‐AMPH. Samples were analyzed by LC‐MS/MS. Regarding noncompartmental analysis, d‐AMPH reached the maximum concentration at 3.8 and 4 h post‐administration in plasma and oral fluid, respectively, with a mean peak concentration value almost six‐fold higher in oral fluid. LDX reached maximum concentration at 1.2 and 1.8 h post‐administration in plasma and oral fluid, respectively, with a mean peak concentration value almost three‐fold higher in plasma. Intact LDX and d‐AMPH were detected in the three matrices. The best fit of compartmental analysis was found in the one‐compartment model for both analytes in plasma and oral fluid. There was a correlation between oral fluid and plasma d‐AMPH concentrations and between parent to metabolite concentration ratios over time in plasma as well as in oral fluid.
- Subjects
SALIVA; PHARMACOKINETICS; URINE; BULIMIA; AMPHETAMINES
- Publication
Biopharmaceutics & Drug Disposition, 2021, Vol 42, Issue 1, p3
- ISSN
0142-2782
- Publication type
Article
- DOI
10.1002/bdd.2254