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 glucuronides have also been detected in vitro and in vivo. To identify human UDP glucuronosyltransferases that are active in the glucuronidation of mycophenolic acid, cDNAs encoding individual UDP glucuronosyltransferase forms have been expressed in cell culture, and the capacity of the expressed enzymes to use mycophenolic acid as a substrate has been assessed. Two UDP glucuronosyltransferase forms, UGT1A8 and UGT1A10, were active in the glucuronidation of mycophenolic acid. Both enzymes are predominantly expressed in the gastrointestinal tract and hence, may play a role in the metabolism of mycophenolic acid in the gastrointestinal tract and in the acquisition of resistance to the mito-inhibitory effects of this drug in cultured human colorectal carcinoma cell lines. The identities of the UDP glucuronosyltransferase forms that are mainly responsible for the glucuronidation of mycophenolic acid in the liver and kidney remain unknown; however, UGT1A9 may be important in this respect as the cDNA-expressed enzyme has some capacity to glucuronidate mycophenolic acid. Other UGT1A forms in the liver and kidney (UGT1A1, UGT1A3, UGT1A4, and UGT1A6) were inactive toward mycophenolic acid.
journal_name
Ther Drug Monitjournal_title
Therapeutic drug monitoringauthors
Mackenzie PIdoi
10.1097/00007691-200002000-00002subject
Has Abstractpub_date
2000-02-01 00:00:00pages
10-3issue
1eissn
0163-4356issn
1536-3694journal_volume
22pub_type
杂志文章,评审abstract:BACKGROUND:Raltegravir is the first human immunodeficiency virus-1 (HIV-1) integrase inhibitor used in treatment-experienced patients who have evidence of viral replication and HIV-1 strains resistance to multiple antiretroviral regimens. Etravirine is a novel NNRTI, active against HIV-1 strains harboring multiple NNRT...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e3181c05adf
更新日期:2009-12-01 00:00:00
abstract::The placental and milk transfer of chloroquine was studied in seven subjects and six subjects, respectively. Seven pregnant women at term were administered chloroquine phosphate (5 mg/kg) i.m. The maternal blood and arterial and venous umbilical cord blood were obtained during delivery. The maternal chloroquine blood ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198802000-00004
更新日期:1988-01-01 00:00:00
abstract::Fluorescence polarization immunoassay (FPIA) (TDx, Abbott Laboratories Diagnostics, Irvin, TX, U.S.A.) is commonly utilized for quantitative determination of gentamicin serum concentrations. Recently, automated homogeneous latex agglutination (LA) (Technicon Immuno-1, Miles Diagnostics Division, Tarrytown, NY, U.S.A.)...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199408000-00010
更新日期:1994-08-01 00:00:00
abstract::For the evaluation and interpretation of pharmacokinetic data reliable quantitative determinations are a requirement that can only be met by well-characterized and fully validated analytical methods. To cope with these requirements a method is being established that is based on an integrated and automated fiber-optic ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199608000-00017
更新日期:1996-08-01 00:00:00
abstract:BACKGROUND/OBJECTIVES:Drug of abuse consumption throughout pregnancy is a serious public health problem and an important economic cost to the health system. The aim of this work was to compare maternal interview and hair analysis to determine drug consumption throughout pregnancy and to study relations among maternal i...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e318288453f
更新日期:2013-06-01 00:00:00
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
doi:
更新日期:1989-09-01 00:00:00
abstract::In a phase I-II study, the authors evaluated the intracellular pharmacokinetics, toxicity, and efficiency of a high dose of mitoxantrone given as first induction in acute non-lymphocytic leukemia. Twenty-two patients with previously untreated de novo ANLL were included and received 30 or 40 mg/m2 mitoxantrone on day 1...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章
doi:10.1097/00007691-199812000-00010
更新日期:1998-12-01 00:00:00
abstract::Effects of carbamazepine coadministration on plasma concentrations of trazodone and its active metabolite, m-chlorophenylpiperazine (m-CPP) were studied in six depressed patients treated with trazodone. The daily dose of trazodone was 150 mg in three cases and 300 mg in three cases. Carbamazepine, 400 mg/day, was coad...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199604000-00010
更新日期:1996-04-01 00:00:00
abstract::The authors describe a reverse-phase high-performance liquid chromatography-electrospray-tandem mass spectrometry method for the measurement of nicotine in human plasma. Samples (500 microL) with added deuterium-labeled d3-nicotine as an internal standard (IS) were treated with a 2-step process of ether extraction (6 ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200410000-00015
更新日期:2004-10-01 00:00:00
abstract::To study the effect of pharmacologic agents on the biologic fate of adenosine, a reversed-phase high-performance liquid chromatography (HPLC) assay coupled with a solid-phase extraction (SPE) method was developed for simultaneous determination of plasma adenosine, hypoxanthine, xanthine, inosine, guanosine, and uric a...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200004000-00007
更新日期:2000-04-01 00:00:00
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
doi:
更新日期:1981-01-01 00:00:00
abstract:BACKGROUND:Paclitaxel (PTX; Taxol, Abraxane) is used in many regimens for breast cancer, non-small cell lung cancer (NSCLC), and ovarian cancer. Multiple studies have demonstrated that PTX exhibits a greater than 10-fold interpatient variability of clearance rates when patients are dosed according to body surface area ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e318296be01
更新日期:2013-12-01 00:00:00
abstract::The pharmacokinetic interaction between chloroquine (CQ) and imipramine was investigated in six healthy volunteers who received 300 mg of CQ, 50 mg of imipramine, and combined doses of both drugs in a randomized, crossover design. Blood and urine samples were collected at predetermined time intervals and were analyzed...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00007691-199302000-00008
更新日期:1993-02-01 00:00:00
abstract::Mixed-effect modeling has been suggested as a possible tool to detect and describe drug interactions in patient populations receiving drug combinations for the treatment of disease states. The mixed-effect modeling program, NONMEM, was used to measure the effects of the well-known digoxin-quinidine and digoxin-verapam...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章
doi:10.1097/00007691-199602000-00008
更新日期:1996-02-01 00:00:00
abstract::A radioimmunoassay (RIA) procedure for the determination of sulforidazine in human plasma was developed using an antiserum raised in rabbits immunized with N-(2-carboxyethyl)desmethylsulforidazine-porcine thyroglobulin conjugate. The RIA procedure can measure as low as 40 pg of sulforidazine in a 200-microliter human ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198802000-00016
更新日期:1988-01-01 00:00:00
abstract::The in vitro stability of cocaine (COC) was monitored in fresh whole blood and plasma stabilized with potassium fluoride (0.25%) for as long as 15 days. The samples were stored at 4 degreesC, 20 degreesC and 40 degreesC. Additionally, fresh plasma samples containing either benzoylecgonine (BZE), ecgonine methyl ester ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200104000-00014
更新日期:2001-04-01 00:00:00
abstract:INTRODUCTION:Enoxaparin is an anticoagulant used in the treatment of thromboembolic diseases. It is a hydrophilic molecule that is, predominantly, eliminated renally with few data to support dosing for subjects with renal impairment and/or obesity. A recently conducted randomized controlled clinical trial compared indi...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,随机对照试验
doi:10.1097/FTD.0b013e3181e64846
更新日期:2010-08-01 00:00:00
abstract::Phenytoin is an anticonvulsant that requires therapeutic drug monitoring. Recently, Bayer HealthCare, Diagnostics Division released a turbidimetric immunoassay of phenytoin on the ADVIA 1650 analyzer. We evaluated the analytic performance of this assay by comparing values obtained in 52 patients receiving Phenytoin us...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/01.ftd.0000164315.13825.dd
更新日期:2005-06-01 00:00:00
abstract:BACKGROUND:Dried blood spot (DBS) sampling is a blood collection tool that uses a finger prick to obtain a blood drop on a DBS card. It can be used for therapeutic drug monitoring, a method that uses blood drug concentrations to optimize individual treatment. DBS sampling is believed to be a simpler way of blood collec...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000659
更新日期:2019-12-01 00:00:00
abstract::The postulated therapeutic activity of nortriptyline metabolites has prompted investigation of dosage adjustments based on plasma levels of nortriptyline (NT) and its metabolites. The method assumes that metabolite concentrations vary independently of nortriptyline concentrations among patients. This study tests that ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198905000-00001
更新日期:1989-01-01 00:00:00
abstract:BACKGROUND:SB2, an infliximab (IFX) biosimilar to the reference infliximab (R.I.) product (Remicade), received approval in the European Union for all IFX indications. Many decision algorithms based on the measurement of IFX trough levels and antibodies to infliximab are being increasingly used to optimize IFX treatment...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000565
更新日期:2018-12-01 00:00:00
abstract::Levels of the anticonvulsant drugs phenobarbitone, phenytoin, carbamazepine, and primidone were measured in the plasma and saliva of 202 epileptic children (5 months-18 years old). Gas-liquid chromatography (GLC) and EMIT immunoassay were used to analyse the samples. Saliva to plasma ratios were as follows (means +/- ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198102000-00006
更新日期:1981-01-01 00:00:00
abstract::Palivizumab is a humanized, monoclonal antibody used to protect at-risk infants against respiratory syncytial virus (RSV) infection. The regular dosage scheme causes a low initial trough level and accumulation of the antibody after subsequent injections. Using a simple pharmacokinetic model, the authors devised an alt...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200206000-00020
更新日期:2002-06-01 00:00:00
abstract::A method for analyzing flecainide in plasma was developed and assessed. Based on the use of C18 extraction columns eight or fewer times, the rapid and simple extraction procedure provided consistent, high-efficiency flecainide extraction (>85%). Using reverse-phase, high-performance liquid chromatography with fluorome...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199808000-00014
更新日期:1998-08-01 00:00:00
abstract::This study was undertaken to model the relationship between clonazepam plasma concentrations and a central nervous system adverse effect (impairment of the psychomotor performance) following the oral administration of immediate-release tablets of clonazepam in healthy volunteers. Such a (P)pharmacokinetic/(P)pharmacod...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,随机对照试验
doi:10.1097/FTD.0b013e3181b1dd76
更新日期:2009-10-01 00:00:00
abstract:BACKGROUND:Serum trough concentrations as the sole means of monitoring safety and efficacy of vancomycin are insufficient. The daily area under the curve (AUC24) of serum concentration versus time to minimum inhibitory concentration (MIC) ratio of greater than 400 mg × h/L has emerged as a more robust dosing target. A ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000500
更新日期:2018-06-01 00:00:00
abstract::Studies examining associations between antidepressant response and plasma levels of bupropion and its metabolites have yielded contradictory findings. There have been no such studies in youth. This study explored such associations in 8 boys and 8 girls, age 11 to 17 years, all prescribed bupropion sustained release (S...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章
doi:10.1097/01.ftd.0000197093.92559.7a
更新日期:2006-04-01 00:00:00
abstract:BACKGROUND:Tacrolimus (TAC) has a narrow therapeutic index and high interindividual and intraindividual pharmacokinetic variability, necessitating therapeutic drug monitoring to individualize dosage. Recent evidence suggests that intragraft TAC concentrations may better predict transplant outcomes. This study aimed to ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31828e8162
更新日期:2013-10-01 00:00:00
abstract:BACKGROUND:Quality management and accreditation in the analytical laboratory setting are developing rapidly and becoming the standard worldwide. Quality management refers to all the activities used by organizations to ensure product or service consistency. Accreditation is a formal recognition by an authoritative regul...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31828526b4
更新日期:2013-06-01 00:00:00
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
doi:10.1097/00007691-200502000-00014
更新日期:2005-02-01 00:00:00