ABSTRACT Dersimelagon is a novel investigational orally administered selective agonist of the melanocortin‐1 receptor. The drug–drug interaction (DDI) potential of dersimelagon was investigated in both nonclinical (in vitro) and clinical studies. The in vitro inhibition of CYP/UGT isoforms and efflux/uptake transporters by dersimelagon was assessed ...
Akihito Ogasawara +4 more
wiley +1 more source
ABSTRACT The two most extensively studied cannabinoids, cannabidiol (CBD) and delta‐9‐tetrahydrocannabinol (THC), are used for myriad conditions. THC is predominantly eliminated via the cytochromes P450 (CYPs), whereas CBD is eliminated through both CYPs and UDP‐glucuronosyltransferases (UGTs).
Lixuan Qian +4 more
wiley +1 more source
Evaluation of an in-capillary approach for performing quantitative cytochrome P450 activity studies [PDF]
An automated in-capillary assay requiring very small quantities of reagents was developed for performing in vitro cytochrome P450 (CYP450) drug metabolism studies. The approach is based on the following: (i) hydrodynamic introduction of nanoliter volumes
Curcio, R. +3 more
core
A service improvement project to review prescribing information provided by general practitioners for new referrals to a UK National Health Service hospital pain clinic: potential implications of CYP2D6 enzyme inhibition. [PDF]
INTRODUCTION: Chronic pain is often managed using co-prescription of analgesics and adjuvants, with concomitant medication prescribed for comorbidities.
Fitzgerald, P +3 more
core +1 more source
Five new Schiff bases from 4‐aminoantipyrine were synthesized, characterized, and evaluated for their antimicrobial and DNA cleavage activities, and drug similarity properties and cytotoxicity prediction using in silico analysis. All Schiff bases had good antibacterial and antifungal activities. All compounds showed self‐activating DNA cleavage ability
Aşkın Erbaş +7 more
wiley +1 more source
Pharmacological aspects of neonatal antidepressant withdrawal [PDF]
Depression is common in reproductive age women, and continued pharmacologic treatment of depression during pregnancy may be necessary to prevent relapse, which could be harmful for both the fetus and the mother. Although data on drug safety are imperfect
Brouwers, Jacobus R. B. J. +5 more
core +2 more sources
Itraconazole-induced Torsade de Pointes in a patient receiving methadone substitution therapy [PDF]
Issues. Methadone, a pharmacological agent used to treat heroin dependence is relatively safe, but may cause cardiac arrhythmias in the concurrent presence of other risk factors. Approach and Key Findings.
Narayanan, S. +2 more
core
Effect of the inhibition of CYP3A4 or CYP2D6 on the pharmacokinetics and pharmacodynamics of oxycodone [PDF]
Purpose: The main metabolic pathways of oxycodone, a potent opioid analgetic, are N-demethylation (CYP3A4) to inactive noroxycodone and O-demethylation (CYP2D6) to active oxymorphone.
Drewe, Jürgen +5 more
core
Current evidence for a modulation of low back pain by human genetic variants [PDF]
The manifestation of chronic back pain depends on structural, psychosocial, occupational and genetic influences. Heritability estimates for back pain range from 30% to 45%. Genetic influences are caused by genes affecting intervertebral disc degeneration
Aberle +200 more
core +1 more source
An Extensively Humanized Mouse Model to Predict Pathways of Drug Disposition and Drug/Drug Interactions, and to Facilitate Design of Clinical Trials [PDF]
Species differences in drug metabolism and disposition can confound the extrapolation of in vivo pharmacokinetic data to man, and also profoundly compromise drug efficacy studies due to differences in pharmacokinetics, in metabolites produced (which are ...
A. Rode +21 more
core +3 more sources

