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Genetic variants in cytochrome P450 (CYP) (<jats:italic>CYP2D6<\/jats:italic>), dopamine receptor (<jats:italic>DRD2<\/jats:italic>, <jats:italic>DRD3<\/jats:italic>) and serotonin receptor (<jats:italic>HTR2A<\/jats:italic>, <jats:italic>HTR2C<\/jats:italic>) genes were previously associated with antipsychotic\u2010induced hyperprolactinaemia. Our aim was to evaluate whether aripiprazole affects prolactin secretion and its relationship with pharmacogenetics. Thirty\u2010one healthy volunteers receiving a 10\u2010mg single oral dose of aripiprazole were genotyped for 12 polymorphisms in <jats:italic>CYP2D6<\/jats:italic>, <jats:italic>DRD2<\/jats:italic>, <jats:italic>DRD3<\/jats:italic>, <jats:italic>HTR2A<\/jats:italic> and <jats:italic>HTR2C<\/jats:italic> genes by qPCR. Aripiprazole and dehydro\u2010aripiprazole plasma concentrations were measured by HPLC\u2010MS\/MS. Prolactin concentrations of the 31 volunteers taking aripiprazole and 12 volunteers receiving ibuprofen were determined by ELISA. Prolactin concentrations after ibuprofen intake were considered as control, since it is known to cause no effect. Prolactin concentrations were slightly higher in the aripiprazole group compared to the ibuprofen group. All prolactin pharmacokinetic parameters were higher in females than in males. CYP2D6 poor and intermediate metabolizers had notably higher prolactin C<jats:sub>max<\/jats:sub> and AUC<jats:sub>0\u201012<\/jats:sub> than normal and ultrarapid metabolizers. The <jats:italic>DRD3<\/jats:italic> rs6280 polymorphism affected prolactin levels: volunteers carrying Ser\/Ser genotype had significantly lower prolactin levels than volunteers carrying the Gly allele. Furthermore, <jats:italic>HTR2C<\/jats:italic> rs3813929 C\/C homozygotes had significantly lower prolactin levels than T allele carriers. Nevertheless, aripiprazole did increase prolactin levels compared to ibuprofen.<\/jats:p>","DOI":"10.1111\/bcpt.13323","type":"journal-article","created":{"date-parts":[[2019,9,14]],"date-time":"2019-09-14T13:08:28Z","timestamp":1568466508000},"page":"236-246","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["Effects of aripiprazole on circadian prolactin secretion related to pharmacogenetics in healthy volunteers"],"prefix":"10.1111","volume":"126","author":[{"given":"Dora","family":"Koller","sequence":"first","affiliation":[{"name":"Clinical Pharmacology Department University Hospital of the Princess, Te\u00f3filo Hernando Institute, School of Medicine, Health Research Institute of the Princess (IP), Autonomus University of Madrid Madrid Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Carmen","family":"Belmonte","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology Department University Hospital of the Princess, Te\u00f3filo Hernando Institute, School of Medicine, Health Research Institute of the Princess (IP), Autonomus University of Madrid Madrid Spain"},{"name":"UICEC University Hospital of the Princess, Platform SCREN (Spanish Clinical Research Network) Health Research Institute of the Princess (IP) Madrid Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Miriam","family":"Saiz\u2010Rodr\u00edguez","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology Department University Hospital of the Princess, Te\u00f3filo Hernando Institute, School of Medicine, Health Research Institute of the Princess (IP), Autonomus University of Madrid Madrid Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Pablo","family":"Zubiaur","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology Department University Hospital of the Princess, Te\u00f3filo Hernando Institute, School of Medicine, Health Research Institute of the Princess (IP), Autonomus University of Madrid Madrid Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Manuel","family":"Rom\u00e1n","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology Department University Hospital of the Princess, Te\u00f3filo Hernando Institute, School of Medicine, Health Research Institute of the Princess (IP), Autonomus University of Madrid Madrid Spain"},{"name":"UICEC University Hospital of the Princess, Platform SCREN (Spanish Clinical Research Network) Health Research Institute of the Princess (IP) Madrid Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dolores","family":"Ochoa","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology Department University Hospital of the Princess, Te\u00f3filo Hernando Institute, School of Medicine, Health Research Institute of the Princess (IP), Autonomus University of Madrid Madrid Spain"},{"name":"UICEC University Hospital of the Princess, Platform SCREN (Spanish Clinical Research Network) Health Research Institute of the Princess (IP) Madrid Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Francisco","family":"Abad\u2010Santos","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology Department University Hospital of the Princess, Te\u00f3filo Hernando Institute, School of Medicine, Health Research Institute of the Princess (IP), Autonomus University of Madrid Madrid Spain"},{"name":"UICEC University Hospital of the Princess, Platform SCREN (Spanish Clinical Research Network) Health Research Institute of the Princess (IP) Madrid Spain"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2019,10]]},"reference":[{"issue":"9","key":"e_1_2_7_2_1","first-page":"638","article-title":"Schizophrenia: overview and treatment options","volume":"39","author":"Patel KR","year":"2014","journal-title":"P T Peer\u2010Rev J Formul 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