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In Vitro Evaluation of CYP-Mediated Metabolism of Fezolinetant and Pharmacokinetic Interaction Between Fezolinetant and Fluvoxamine in Healthy Postmenopausal Smokers and Nonsmokers.
J Clin Pharmacol
November 2024
Amgen, Inc., Thousand Oaks, CA, USA.
Fezolinetant is an oral, nonhormonal, neurokinin 3 receptor antagonist treatment option for moderate to severe vasomotor symptoms associated with menopause. An in vitro study using human recombinant cytochrome P450 (CYP) enzymes and human liver microsomes showed that fezolinetant is metabolized to its major but inactive metabolite, ES259564, predominantly through CYP1A2, with minor contributions from CYP2C9 and CYP2C19. The clinical impact of CYP1A2 inhibition and induction on single-dose pharmacokinetics of fezolinetant was assessed in an open-label, single-sequence, phase 1 study in healthy postmenopausal women, where the impact of fluvoxamine, a strong CYP1A2 inhibitor, and smoking, a moderate CYP1A2 inducer, were evaluated.
View Article and Find Full Text PDF[The Impact of Antidepressants on COVID-19 and Post-Acute COVID-19 Syndrome: A Scoping-Review Update].
Fortschr Neurol Psychiatr
September 2024
LWL-Universitätsklinikum der Ruhr-Universität Bochum, Klinik für Psychiatrie, Psychotherapie und Präventivmedizin, Bochum, Germany.
Article Synopsis
- The study investigates the potential clinical benefits of antidepressants (AD), specifically fluvoxamine, against COVID-19 and Long COVID, given their preclinical antiviral and anti-inflammatory effects.
- A systematic review of literature identified 1016 articles, including a variety of studies that suggest fluvoxamine significantly reduces COVID-19 infections and severity, particularly when used early in treatment.
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Author Correction: A systematic review and meta-analysis, investigating dose and time of fluvoxamine treatment efficacy for COVID-19 clinical deterioration, death, and Long-COVID complications.
Sci Rep
July 2024
Natural Products for Neuroprotection and Anti‑Ageing (Neur‑Age Natura) Research Unit, Chulalongkorn University, Bangkok, 10330, Thailand.
Population pharmacokinetics of olanzapine in pediatric patients with psychiatric disorders.
Expert Opin Drug Metab Toxicol
August 2024
The National Clinical Research Center for Mental Disorders and Beijing Key Laboratory of Mental Disorders, Beijing Anding Hospital, Capital Medical University, Beijing, China.
Article Synopsis
- - The study aimed to create and validate a population pharmacokinetic model for oral olanzapine in pediatric Chinese patients to better tailor medication dosing for individuals aged 8-17 years.
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Serum Concentration-Dose Relationship and Modulation Factors in Children and Adolescents Treated with Fluvoxamine.
Pharmaceutics
June 2024
Department of Child and Adolescent Psychiatry, Psychosomatics and Psychotherapy, Centre for Mental Health, University Hospital of Wuerzburg, 97080 Wuerzburg, Germany.
Introduction: Fluvoxamine is used in children and adolescents ('youths') for treating obsessive compulsive disorder (OCD) but also off-label for depressive and anxiety disorders. This study aimed to investigate the relationship between fluvoxamine dose and serum concentrations, independent correlates of fluvoxamine concentrations, and a preliminary therapeutic reference range (TRR) for youths with OCD and treatment response.
Methods: Multicenter naturalistic data of a therapeutic drug monitoring service, as well as prospective data of the 'TDM Vigil study' (EudraCT 2013-004881-33), were analyzed.
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