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Clinical Pharmacokinetics

ISSN 0312-5963, 1179-1926

13 papers in the library · 396 citations · publishing 2005-2025

Papers

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Modeling Whole-Body Dynamic PET Microdosing Data to Predict the Whole-Body Pharmacokinetics of Glyburide in Humans.

Clinical Pharmacokinetics November 1, 2025 Léa Comin, Solène Marie, Moreno Ursino et al.

Whole-body dynamic (WB4D) positron emission tomography (PET) imaging data using radiolabeled analogs of drugs are mostly analyzed using descriptive approaches, with no relationship to traditional pharmacokinetic studies based on blood sampling. Here, we build a pharmacokinetic (PK) model from WB4D PET data obtained using a microdose of radiolabeled glyburide ([11C]glyburide) in humans, aiming...

Pharmacokinetics, Pharmacodynamics, and Urinary Recovery of Oral Mescaline Hydrochloride in Healthy Participants.

Clinical Pharmacokinetics July 14, 2025 Lorenz Mueller, Aaron Klaiber, Laura Ley et al. 4 citations

Mescaline is a classic serotonergic psychedelic with a long history of human use. The present study analyzed the pharmacokinetics, pharmacokinetic-pharmacodynamic relationship, and urinary recovery of oral mescaline hydrochloride. Data from 105 single-dose administrations (100-800 mg) in 49 participants from two phase I trials were analyzed with compartmental pharmacokinetics and...

Correction: Clinical Pharmacokinetics of Psilocin After Psilocybin Administration: A Systematic Review and Post‑Hoc Analysis

Clinical Pharmacokinetics February 21, 2025 Marije E. Otto, Katelijne V. van der Heijden, Jan W. Schoones et al. correction

Correction to: Clinical Pharmacokinetics (2025) 64:53–66 https://doi.org/10.1007/s40262-024-01454-4 In the original version of this article, the given and family names of J. G. Coen van Hasselt were incorrectly structured as Coen J.G. van Hasselt. The correct name should read as given name: J. G. Coen and family name: van Hasselt.

Clinical Pharmacokinetics of N,N-Dimethyltryptamine (DMT): A Systematic Review and Post-hoc Analysis.

Clinical Pharmacokinetics February 1, 2025 Katelijne V. van der Heijden, Marije E. Otto, Jan W. Schoones et al. 7 citations

N,N-Dimethyltryptamine (DMT) is currently being studied for its therapeutic potential in various psychiatric disorders. An understanding of its pharmacokinetics (PK) is essential to determine appropriate dose ranges in future clinical studies. We conducted a systematic literature review on the PK of DMT. Clinical studies that administered known amounts of DMT and reported PK data and/or...

DOI: 10.1007/s40262-024-01450-8 (opens in new tab) Full text (opens in new tab) DMT Psychedelics Pharmacology Mental health treatment

Clinical Pharmacokinetics of Psilocin After Psilocybin Administration: A Systematic Review and Post-Hoc Analysis

Clinical Pharmacokinetics 2025 Marije E. Otto, Katelijne V. van der Heijden, Jan W. Schoones et al. 20 citations

Overall, we found the pharmacokinetic parameters of psilocin to be consistent between studies. This review may guide the further clinical development of psilocybin-based therapies.

Microdosing as a Potential Tool to Enhance Clinical Development of Novel Antibiotics: A Tissue and Plasma PK Feasibility Study with Ciprofloxacin

Clinical Pharmacokinetics January 7, 2022 Z. Oesterreicher, Sabine Eberl, B. Wulkersdorfer et al.

Background and Objective In microdose studies, drug pharmacokinetics is measured in humans after administration of subtherapeutic doses. While previous microdose studies focused primarily on plasma pharmacokinetics, we set out to evaluate the feasibility of microdosing for a pharmacokinetic assessment in subcutaneous tissue and epithelial lining fluid. Methods Healthy subjects received a single...

Pharmacokinetics of Escalating Doses of Oral Psilocybin in Healthy Adults

Clinical Pharmacokinetics March 28, 2017 Randall Brown, Christopher R. Nicholas, Nicholas V. Cozzi et al. 189 citations

IntroductionPsilocybin is a psychedelic tryptamine that has shown promise in recent clinical trials for the treatment of depression and substance use disorders. This open-label study of the pharmacokinetics of psilocybin was performed to describe the pharmacokinetics and safety profile of psilocybin in sequential, escalating oral doses of 0.3, 0.45, and 0.6 mg/kg in 12 healthy...

DOI: 10.1007/s40262-017-0540-6 (opens in new tab) Psilocybin Pharmacokinetics Pharmacology Urine +2

Pharmacokinetics and Pharmacodynamics of Lysergic Acid Diethylamide in Healthy Subjects

Clinical Pharmacokinetics February 14, 2017 Patrick C. Dolder, Yasmin Schmid, Andrea E. Steuer et al. 134 citations

BACKGROUND AND OBJECTIVE: Lysergic acid diethylamide (LSD) is used recreationally and in clinical research. The aim of the present study was to characterize the pharmacokinetics and exposure-response relationship of oral LSD. METHODS: We analyzed pharmacokinetic data from two published placebo-controlled, double-blind, cross-over studies using oral administration of LSD 100 and 200 µg in 24 and...

Successful Use of [14C]Paracetamol Microdosing to Elucidate Developmental Changes in Drug Metabolism

Clinical Pharmacokinetics February 2, 2017 M. Mooij, Esther van Duijn, C. Knibbe et al.

BackgroundWe previously showed the practical and ethical feasibility of using [14C]-microdosing for pharmacokinetic studies in children. We now aimed to show that this approach can be used to elucidate developmental changes in drug metabolism, more specifically, glucuronidation and sulfation, using [14C]paracetamol (AAP).MethodsInfants admitted to the intensive care unit received a single oral...

To Apply Microdosing or Not? Recommendations to Single Out Compounds with Non-Linear Pharmacokinetics.

Clinical Pharmacokinetics January 2016 Sieto Bosgra, Maria L H Vlaming, Wouter Vaes

Microdosing studies allow clinical investigation of pharmacokinetics earlier in drug development, before all high-dose safety concerns have been sorted out. Furthermore, microdosing allows inclusion of target groups that are inadmissible in high-dose phase I trials. A potential concern when considering a microdosing study is that a particular drug candidate may display non-linear...

Predicting Drug Candidate Victims of Drug-Drug Interactions, using Microdosing

Clinical Pharmacokinetics February 16, 2012 Marie Croft, Brendan J. Keely, Ian D. Morris et al. 42 citations

ObjectiveThe aim of this crossover human male volunteer study was to investigate the utility of microdosing in the investigation of drug-drug interactions.MethodsA mixture of midazolam, tolbutamide, caffeine and fexofenadine were administered as a microdose (25 μg each) before and after administration of a combined pharmacological dose of ketoconazole (400 mg) and fluvoxamine (100 mg) to...

DOI: 10.2165/11597070-000000000-00000 (opens in new tab) Microdose Pharmacology Pharmacokinetics Tolbutamide +7

Contribution of cytochrome P450 2D6 to 3,4-methylenedioxymethamphetamine disposition in humans: use of paroxetine as a metabolic inhibitor probe.

Clinical Pharmacokinetics 2005 Mireia Segura, Magí Farré, Simona Pichini et al.

3,4-Methylenedioxymethamphetamine (MDMA) is a synthetic amphetamine derivative typically used for recreational purposes. The participation of cytochrome P450 (CYP) 2D6 in the oxidative metabolism of MDMA may suggest an increased risk of acute toxicity in CYP2D6 poor metabolisers. This study was aimed at assessing the contribution of CYP2D6 to MDMA disposition in vivo using paroxetine as a...