ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety

Therapeutic Drug Monitoring
Arzu GunesM G Scordo

Abstract

Risperidone is metabolized to its active metabolite, 9-hydroxyrisperidone, mainly by the cytochrome P450 enzymes CYP2D6 and 3A4. Its antipsychotic effect is assumed to be related to the active moiety, that is, the sum of risperidone and 9-hydroxyrisperidone. Both risperidone and 9-hydroxyrisperidone are substrates of P-glycoprotein (P-gp), a transport protein involved in drug absorption, distribution, and elimination. The aim of the present study was to evaluate the influence of polymorphisms in genes encoding CYP3A5 and P-gp (ABCB1) on the steady-state plasma levels of risperidone, 9-hydroxyrisperidone, and the active moiety, taking CYP2D6 genotype status into account. Forty-six white patients with schizophrenia treated with risperidone (1-10 mg/d) in monotherapy for 4-6 weeks were genotyped, and their plasma concentrations of risperidone and 9-hydroxyrisperidone were measured. Dose-corrected plasma concentrations (C/D) of risperidone, 9-hydroxyrisperidone, and active moiety showed up to 68-, 9-, and 10-fold interindividual variation, respectively. Six patients carried 1 CYP3A5*1 allele and therefore were likely to express the CYP3A5 enzyme. The CYP3A5 genotype did not influence risperidone, 9-hydroxyrisperidone, or active moi...Continue Reading

References

Aug 26, 1998·Therapeutic Drug Monitoring·O V OlesenK Linnet
Feb 27, 1999·Naunyn-Schmiedeberg's Archives of Pharmacology·J FangG B Baker
Mar 8, 2000·International Journal of Clinical Pharmacology and Therapeutics·M F Fromm
May 29, 2002·Life Sciences·David W BoultonJohn S Markowitz
Nov 12, 2002·Clinical Pharmacology and Therapeutics·Andreas JohneIvar Roots
Apr 17, 2003·European Journal of Clinical Pharmacology·Céline VerstuyftLaurent Becquemont
May 13, 2003·Pharmaceutical Research·Yoshinori MoritaKatsuhiko Okumura
Aug 2, 2003·Pharmacogenetics·Deanna L KroetzUNKNOWN Pharmacogenetics of Membrane Transporters Investigators
Jan 30, 2004·Clinical Pharmacology and Therapeutics·Catia MarzoliniRichard B Kim
Feb 3, 2005·The International Journal of Neuropsychopharmacology·Jun-Sheng WangC Lindsay DeVane
Mar 27, 2007·Journal of Clinical Pharmacy and Therapeutics·W MahatthanatrakulM Sunbhanich
Jan 30, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Marc VermeirAdriaan Cleton

❮ Previous
Next ❯

Citations

Apr 2, 2010·European Journal of Clinical Pharmacology·Yasmin NazirizadehChristoph Hiemke
Jun 22, 2010·European Journal of Clinical Pharmacology·Nikolina JovanovićAlma Mihaljević Peleš
Oct 12, 2010·European Journal of Clinical Pharmacology·Laura MagliuloMaria Gabriella Scordo
May 25, 2012·Journal of Pharmacokinetics and Pharmacodynamics·Hee-Doo YooYong-Bok Lee
Apr 23, 2013·Frontiers of Medicine·Qingqing XuShengying Qin
Jan 4, 2012·The Pharmacogenomics Journal·B AlmogueraUNKNOWN Spanish Consortium of Pharmacogenetics Research in Schizophrenia
Aug 17, 2011·Pharmacogenomics·Tim MoonsGeert Dom
Oct 25, 2013·International Review of Psychiatry·C Anthony AltarDavid Mrazek
Mar 5, 2016·Applied & Translational Genomics·Tyren M DodgenMichael S Pepper
Jun 5, 2014·Pharmacogenomics·Mark D Brennan
Jun 2, 2010·Pharmaceutics·David HolthoewerUlrich Schmitt
Jan 13, 2018·Basic & Clinical Pharmacology & Toxicology·Carmen BelmonteFrancisco Abad-Santos
May 4, 2018·Basic & Clinical Pharmacology & Toxicology·Miriam Saiz-RodríguezFrancisco Abad-Santos
Mar 28, 2019·Expert Review of Clinical Pharmacology·Ramón CacabelosJuan C Carril
Jul 10, 2020·British Journal of Clinical Pharmacology·Sanne Maartje KloosterboerBirgit C P Koch
May 5, 2017·Basic & Clinical Pharmacology & Toxicology·Nopphadol NuntamoolChonlaphat Sukasem
Dec 19, 2017·Human Psychopharmacology·Georgios PapazisisGeorgios Garyfallos
Dec 29, 2020·Frontiers in Genetics·Beatriz Carvalho HenriquesKatherine J Aitchison
Jul 3, 2021·Pharmaceutics·Francisco José Toja-CambaAnxo Fernández-Ferreiro

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.