Dose-dependent effect of the CYP2D6 genotype on the steady-state fluvoxamine concentration.


:Several studies have reported that the cytochrome P450 (CYP) 2D6 plays an important role in the fluvoxamine metabolism. However, some other studies have reported that the CYP2D6 genotype has no major impact on the fluvoxamine concentration. This study investigated the dose-dependent effect of CYP2D6-variant alleles on the steady-state fluvoxamine concentration. There were 23 patients whose plasma concentrations of fluvoxamine were measured at 4 doses (50, 100, 150, and 200 mg/d). The differences in the plasma fluvoxamine concentration were analyzed between 2 genotype groups divided by the number of CYP2D6-variant alleles (with 0 and 1 or 2 variant alleles). The results demonstrated the nonlinear kinetics of fluvoxamine metabolism, and the degree of nonlinear kinetics decreased as the dose was increased. Significant differences in fluvoxamine concentration were observed between the subjects with 0 variant alleles and the subjects with 1 or 2 variant alleles (P = 0.044) when they were treated by 50 mg of fluvoxamine. There were no significant differences in the plasma concentration of fluvoxamine at 100, 150, and 200 mg/d. The present study suggests that the effect of the CYP2D6 genotype on fluvoxamine metabolism is greater at lower doses of fluvoxamine.


Ther Drug Monit


Watanabe J,Suzuki Y,Fukui N,Sugai T,Ono S,Inoue Y,Someya T




Has Abstract


2008-12-01 00:00:00












  • Assessment of drug concentrations in tears in therapeutic drug monitoring: I. Determination of valproic acid in tears by gas chromatography/mass spectrometry with EC/NCI mode.

    abstract::A rapid and sensitive method for the quantitation of valproic acid in tears has been developed using gas chromatography/electron capture negative chemical ionization/mass spectrometry. Valproic acid was converted directly into its pentafluorobenzyl ester derivative without the need to perform any extraction from the b...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Nakajima M,Yamato S,Shimada K,Sato S,Kitagawa S,Honda A,Miyamoto J,Shoda J,Ohya M,Miyazaki H

    更新日期:2000-12-01 00:00:00

  • Teicoplanin measurement in patients with renal failure: comparison of fluorescence polarization immunoassay, microbiological assay, and high-performance liquid chromatographic assay.

    abstract::Characterization of antibiotic pharmacokinetics in patients with renal insufficiency may be complicated by interfering substances within the assay. We compared three different assays for teicoplanin in serum and dialysate of 10 hemodialysis and six continuous ambulatory peritoneal dialysis (CAPD) patients. The microbi...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Awni WM,St Peter WL,Guay DR,Kenny MT,Matzke GR

    更新日期:1991-11-01 00:00:00

  • The use of TDM data to assess the validity of defined daily doses of antiepileptics: a comparison between a Czech and Swedish University Hospital.

    abstract::Prescribed daily doses (PDDs) of antiepileptic drugs (AED) (N03A ATC group) were recorded for drugs used in monotherapy or in combination therapy in the University Hospitals in Ostrava, Czech Republic and Huddinge, Sweden. Plasma concentrations were used as an indicator of the quality of treatment. PDDs were compared ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,多中心研究


    authors: Koristkova B,Sjöqvist F,Grundmann M,Bergman U

    更新日期:2006-10-01 00:00:00

  • Lacosamide therapeutic monitoring in patients with epilepsy: effect of concomitant antiepileptic drugs.

    abstract:BACKGROUND:Lacosamide (LCM) is one of the newer antiepileptic drugs (AEDs) licensed as add-on treatment for partial epilepsy. Data on LCM pharmacokinetics and interactions are limited and partly contradictory. The purpose of this study was to assess the effect of concomitant AED therapy on steady state plasma concentra...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,随机对照试验


    authors: Contin M,Albani F,Riva R,Candela C,Mohamed S,Baruzzi A

    更新日期:2013-12-01 00:00:00

  • Differences in Theophylline Clearance Between Patients With Chronic Hepatitis and Those With Liver Cirrhosis.

    abstract:BACKGROUND:Theophylline, a xanthine derivative drug, is used for the treatment of respiratory diseases, such as asthma, and is primarily eliminated by hepatic metabolism. There is marked interindividual variability in theophylline clearance. Therefore, the aim of this study was to evaluate the influence of chronic hepa...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Kurata Y,Muraki S,Kashihara Y,Hirota T,Araki H,Ieiri I

    更新日期:2020-12-01 00:00:00

  • Clonazepam disposition in pediatric patients.

    abstract::Plasma clonazepam (CZP) and its metabolite [7-aminoclonazepam (7ACZP) and 7-acetamidoclonazepam (7AACZP)] concentrations were measured during a single dosing interval in 10 pediatric epilepsy patients (2-18 years, 11-102 kg) who had been receiving CZP therapeutically from 2 weeks to 4 years. These concentrations were ...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章


    authors: Walson PD,Edge JH

    更新日期:1996-02-01 00:00:00

  • Identification of uridine diphosphate glucuronosyltransferases involved in the metabolism and clearance of mycophenolic acid.

    abstract::Mycophenolic acid, the active metabolite of the immunosuppressant and antiproliferative agent, mycophenolate mofetil, is primarily metabolized by glucuronidation to the inactive 7-O-glucuronide. Although the uridine diphosphate (UDP) 7-O-glucuronide is the principal excretion product of this drug, carboxyl-linked gluc...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,评审


    authors: Mackenzie PI

    更新日期:2000-02-01 00:00:00

  • Pharmacokinetics of diltiazem and its metabolites after repeated single dosing in healthy volunteers.

    abstract::In a crossover study balanced for sex, treatments, and treatment order, we have investigated the pharmacokinetics of diltiazem after single oral doses in 10 healthy middle-aged volunteers. The diltiazem doses employed were 60 mg and 120 mg and contained 1.85 MBq [14C] diltiazem. The absorption was rapid and did not di...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Höglund P,Nilsson LG

    更新日期:1989-09-01 00:00:00

  • Δ9-Tetrahydrocannabinol and Cannabidiol Time Courses in the Sera of "Light Cannabis" Smokers: Discriminating Light Cannabis Use from Illegal and Medical Cannabis Use.

    abstract:BACKGROUND:Δ9-tetrahydrocannabinol (THC) and cannabidiol (CBD) time courses in serum and physiological and behavioral effects associated with smoking 1 or 4 "light cannabis" cigarettes were studied. Biomarkers to differentiate light cannabis versus illegal and medical cannabis use were also investigated. METHODS:Sera ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Pichini S,Mannocchi G,Berretta P,Zaami S,Pirani F,Pacifici R,Busardò FP

    更新日期:2020-02-01 00:00:00

  • Aluminum toxicity in patients with chronic renal failure.

    abstract::During the past two decades, in association with the commencement of chronic dialysis therapy and prolongation of the uremic state, aluminum toxicity has represented a major cause of morbidity and mortality in uremic patients. The uremic patient has been found to be at higher risk of aluminum loading and toxicity from...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,评审


    authors: Alfrey AC

    更新日期:1993-12-01 00:00:00

  • Serum concentrations and side effects in psychiatric patients during risperidone therapy.

    abstract::Steady state serum concentrations of risperidone and 9-hydroxyrisperidone (9-OH-risperidone), the active moiety, were measured in 42 patients. The concentration-to-dose ratios (C/D) varied by a factor of 20, from 1.8 to 36.8 (nmol/l)/(mg/24 hours), and 90% of the active moiety was constituted of 9-OH-risperidone. No c...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章


    authors: Olesen OV,Licht RW,Thomsen E,Bruun T,Viftrup JE,Linnet K

    更新日期:1998-08-01 00:00:00

  • Diffusion characteristics of placental preparations affect the digoxin passage across the isolated placental lobule.

    abstract::Our aim was to evaluate the isolated placental lobule to study maternofetal transplacental digoxin transfer and accumulation in placental tissue in vitro. Digoxin passage across the isolated lobule of 10 human placentas was calculated from repeated fetal and maternal perfusate samples, and placental tissue digoxin con...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Schmolling J,Jung S,Reinsberg J,Schlebusch H

    更新日期:1997-02-01 00:00:00

  • Determination of pentamidine in whole blood, plasma, and urine by high-performance liquid chromatography.

    abstract::The analysis of pentamidine in whole blood, plasma, and urine by liquid chromatography is described. Extraction was made with a mixture of acetonitrile and chloroform followed by back-extraction into phosphate buffer. A reversed-phase chromatographic system with fluorescence detection was used. The precision of the me...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Ericsson O,Rais M

    更新日期:1990-07-01 00:00:00

  • Drugs in sports: analytical trends.

    abstract::A minority of athletes continues to use prohibited drugs in sports to enhance performance. Athletes discovered using these drugs can be subject to severe penalties, often resulting in media and public scrutiny, especially at major events such as the Olympic Games. The International Olympic Committee (IOC) has set out ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,评审


    authors: Kazlauskas R,Trout G

    更新日期:2000-02-01 00:00:00

  • A high-performance liquid chromatography-mass spectrometry method using a novel atmospheric pressure chemical ionization approach for the rapid simultaneous measurement of tacrolimus and cyclosporin in whole blood.

    abstract::Concentration monitoring and dose individualization is required to optimize either tacrolimus or cyclosporin therapy. In this study, the validation of a simple, rapid high-performance liquid chromatography-tandem mass spectrometry method for the simultaneous measurement of tacrolimus and cyclosporin in whole blood is ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Salm P,Taylor PJ,Rooney F

    更新日期:2008-06-01 00:00:00

  • Establishing Serum Reference Ranges for Antihypertensive Drugs.

    abstract:BACKGROUND:Therapeutic drug monitoring (TDM) involves the measurement of serum drug concentrations to optimize pharmacotherapy. Traditionally, blood pressure measurements alone, and not TDM, have been used to evaluate the antihypertensive drug response. However, approximately 50% of hypertensive patients treated with l...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Rognstad S,Søraas CL,Bergland OU,Høieggen A,Strømmen M,Helland A,Opdal MS

    更新日期:2021-02-01 00:00:00

  • Generic Olanzapine Substitution in Patients With Schizophrenia: Assessment of Serum Concentrations and Therapeutic Response After Switching.

    abstract:BACKGROUND:Several reports of loss of efficacy or adverse effects have been described after generic substitution of antipsychotics. To date, studies comparing serum drug levels in patients switched to generic antipsychotics in a standard clinical setting are lacking. The aim of this study was to investigate if switchin...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Italiano D,Bruno A,Santoro V,Lanza G,Muscatello MR,Zoccali R,Spina E

    更新日期:2015-12-01 00:00:00

  • Radioimmunoassay of zidovudine: extended use and potential application.

    abstract::When first approved, the dosing regimens for zidovudine were 1,200-1,500 mg/day; however, because toxicity developed, the daily dose had to be reduced to 500-600 mg/day. At these lower doses, plasma concentrations for a considerable segment of the dosing interval are often below the assay sensitivity for the high-perf...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: DeRemer M,D'Ambrosio R,Bartos L,Cousins S,Morse GD

    更新日期:1997-04-01 00:00:00

  • Use of a monoclonal antibody for the therapeutic monitoring of cyclosporine in plasma and whole blood.

    abstract::The evaluation of a radioimmunoassay (RIA) for the monitoring of cyclosporine (CSA) that utilizes a monoclonal antibody specific for the parent compound is described. The assay exhibited good analytical recovery (greater than 95%), precision (coefficient of variation less than 10%), and linearity in plasma and whole b...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Copeland KR,Yatscoff RW

    更新日期:1988-01-01 00:00:00

  • Serum drug concentrations in clinical perspective.

    abstract::Determination of serum concentrations of certain drugs is becoming increasingly important for optimal patient care. These drugs include many antibiotics, several antiarrhythmics, cardiac glycosides, lithium, phenytoin, some other anticonvulsants, salicylates, and theophylline. Serum level determinations can also be us...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,评审


    authors: Koch-Weser J

    更新日期:1981-01-01 00:00:00

  • Low oral bioavailability and pharmacokinetics of senkyunolide a, a major bioactive component in Rhizoma Chuanxiong, in the rat.

    abstract::The pharmacokinetics of senkyunolide A, one of the major bioactive ingredients in the traditional Chinese medicinal herb Rhizoma Chuanxiong, which is commonly used for the treatment of cardiovascular diseases, was studied in rats. After intravenous (IV) administration, senkyunolide A was extensively distributed (Vd/F:...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Yan R,Lin G,Ko NL,Tam YK

    更新日期:2007-02-01 00:00:00

  • The aminoglycoside panel: a new approach to monitoring aminoglycoside therapy.

    abstract::The aminoglycoside antibiotics gentamicin and tobramycin have been monitored traditionally by measuring peak and trough drug levels in serum. We found interpretation of these data to be hazardous, due to variations in the drug administration-specimen collection process and routine medical events and practices. We desc...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Gorsky JE,Latts JR

    更新日期:1983-06-01 00:00:00

  • Current Practice for Therapeutic Drug Monitoring of Biopharmaceuticals in Rheumatoid Arthritis.

    abstract::The treatment of rheumatoid arthritis (RA) has largely improved in the biopharmaceutical era. These compounds, primarily tumor necrosis factor (TNF) inhibitors, are effective, but some patients may show poor response, sometimes because of the presence of antidrug antibodies (ADAs). In some instances, clinicians may in...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章,评审


    authors: Medina F,Plasencia C,Goupille P,Ternant D,Balsa A,Mulleman D

    更新日期:2017-08-01 00:00:00

  • Ipecac toxicity in "Munchausen syndrome by proxy".

    abstract::The authors report a case that offers insight into the diagnostic challenges of "Munchausen Syndrome by Proxy." Initial presentation with history of fever and later with intractable vomiting led to invasive and expensive diagnostic evaluation before confirming the diagnosis. Certain toxic effects of emetine were clini...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Bader AA,Kerzner B

    更新日期:1999-04-01 00:00:00

  • Acute tolerance to pressor effects of cocaine in humans.

    abstract::We have suggested previously that acute tolerance to the chronotropic effect of cocaine develops and that tolerance is incomplete, such that the heart-rate decline in the presence of stable plasma cocaine concentrations approaches a plateau that exceeds the baseline heart rate. One possible mechanism for heart-rate de...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Ambre JJ

    更新日期:1993-12-01 00:00:00

  • The pH dependency of the binding of drugs to plasma proteins in man.

    abstract::An analysis of pH-induced changes of drug binding may contribute to the understanding of the mechanisms involved and the clinical relevance. A literature search was performed, and acceptance criteria set up, to select reported data for quantitative evaluation. The relationship between percentage of unbound drug, fu, a...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Hinderling PH,Hartmann D

    更新日期:2005-02-01 00:00:00

  • Therapeutic drug monitoring of theophylline in frail elderly patients: oral compared with nasogastric tube administration.

    abstract:SUMMARY:Treating debilitated elderly patients through nasogastric tube (NGT) can change the pharmacokinetic characteristics of drugs, mainly those that are slow released (SR). The purpose of this study was to compare pharmacokinetic parameters between patients who receive SR theophylline orally and those who receive it...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Berkovitch M,Dafni O,Leiboviz A,Mayan H,Habut B,Segal R

    更新日期:2002-10-01 00:00:00

  • Mycophenolic acid interaction with cyclosporine and tacrolimus in vitro and in vivo: evaluation of additive effects on rat blood lymphocyte function.

    abstract::The effect of mycophenolic acid (MPA) in combination with either cyclosporine (CsA) or tacrolimus (TRL) on whole-blood lymphocyte function was assessed in vitro as well as in vivo. For the in vitro studies, rat whole blood was incubated with different concentrations of MPA together with CsA or TRL. In vivo, rats (n = ...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Barten MJ,Shipkova M,Bartsch P,Dhein S,Streit F,Tarnok A,Armstrong VW,Mohr FW,Oellerich M,Gummert JF

    更新日期:2005-04-01 00:00:00

  • Vancomycin monitoring: one or two serum levels?

    abstract::Based on the principle that vancomycin therapy requires sustained therapeutic concentrations while avoiding high peaks, some authors reported that optimal vancomycin levels could be ensured by measuring trough levels alone (Cmin). The aim of this work was to assess the performance of a one-compartment Bayesian forecas...

    journal_title:Therapeutic drug monitoring

    pub_type: 杂志文章


    authors: Andrés I,López R,Pou L,Piñol F,Pascual C

    更新日期:1997-12-01 00:00:00

  • Doping-control analysis of the 5alpha-reductase inhibitor finasteride: determination of its influence on urinary steroid profiles and detection of its major urinary metabolite.

    abstract::5alpha-Reductase inhibitors such as finasteride are prohibited in sports according to the World Anti-Doping Agency. This class of drugs is used therapeutically to treat benign prostatic hyperplasia, as well as male baldness, by decreasing 5alpha-reductase activity. Accordingly, metabolic pathways of endogenous as well...

    journal_title:Therapeutic drug monitoring

    pub_type: 临床试验,杂志文章


    authors: Thevis M,Geyer H,Mareck U,Flenker U,Schänzer W

    更新日期:2007-04-01 00:00:00