Abstract:
:Despite its known teratogenic effects, thalidomide has been used to treat a variety of diseases ranging from alleviation of autoimmune disorders to prevention of metastasis of cancers. The exact method of action of thalidomide and its derivatives is still under investigation. Thalidomide undergoes very little metabolism by the cytochrome P 450 system in vitro, but at least two hydroxylated metabolites have been found in humans. The two metabolites are 5-hydroxythalidomide, formed by hydroxylation of the phthalimide ring, possibly via arene oxides, and 5'-hydroxythalidomide, formed by hydroxylation of the glutarimide ring, leading to diastereomeric products. These two metabolites, along with another minor metabolite of thalidomide, were tested in a rat aortic ring assay, a human saphenous vein model, and a tube formation assay to assess the metabolite's ability to inhibit angiogenesis. Of the metabolites tested, only 5'-OH-thalidomide showed biologic activity in the rat aortic ring assay, and none of the metabolites showed activity in the human model. The studies with thalidomide and thalidomide metabolites underline the difficulty and complexity of trying to isolate and evaluate a single biologically active agent. These studies, however, do suggest that at least one metabolite, 5'-OH-thalidomide, has moderate antiangiogenic activity at high concentrations. Unfortunately, because of the lack of observed activity of 5'-OH-thalidomide in the human saphenous vein assay, it remains unclear whether there is species specificity for the activity of this metabolite.
journal_name
Ther Drug Monitjournal_title
Therapeutic drug monitoringauthors
Price DK,Ando Y,Kruger EA,Weiss M,Figg WDdoi
10.1097/00007691-200202000-00017subject
Has Abstractpub_date
2002-02-01 00:00:00pages
104-10issue
1eissn
0163-4356issn
1536-3694journal_volume
24pub_type
杂志文章abstract::The effect of heparin sodium on the assay of gentamicin using the fluorescence polarization immunoassay system was investigated with varying heparin and gentamicin concentrations. Heparin had no significant effect on gentamicin concentrations as measured by this system. ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198409000-00011
更新日期:1984-01-01 00:00:00
abstract::Fentanyl, sufentanil, and morphine are commonly used in the conduct of anesthesia. Medical staff working with these drugs are at high risk of addiction. To detect and prevent diversion, a method was developed to quantify these drugs in discard syringes using the BioRad REMEDi HS Drug Profiling System. For fentanyl, th...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200210000-00014
更新日期:2002-10-01 00:00:00
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
doi:10.1097/FTD.0b013e318290eacc
更新日期:2013-12-01 00:00:00
abstract::A model for predicting unbound concentrations of mycophenolic acid (MPA) was developed in 84 subjects and then tested in an independent group of 19 hematopoietic cell transplant recipients. Total and unbound MPA concentrations and total mycophenolic glucuronide concentrations were measured between weeks 1 and 4 posttr...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章
doi:10.1097/FTD.0b013e318074d979
更新日期:2007-08-01 00:00:00
abstract::Results of phenobarbital analyses are presented for 14 patients with chronic renal failure, and compared using gas-liquid chromatography (GLC), enzyme immunoassay (EIA), and fluorescence polarization immunoassay (FPIA). Correlation of FPIA with GLC and EIA was poor. ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198409000-00019
更新日期:1984-01-01 00:00:00
abstract::Therapeutic drug monitoring in antituberculosis chemotherapy may play a strategic role in improving outcomes in selected patients. The most important use is in assisting clinicians to optimize therapy to achieve success and minimize toxicity. The other principal indication lies in the management of interaction of anti...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/00007691-199810000-00004
更新日期:1998-10-01 00:00:00
abstract::The pharmacokinetics of oxycodone have been determined after single-dose administration by the intravenous (4.6-7.3 mg), oral (tablets, 9.1 mg and syrup, 9.1 mg), and rectal (30 mg) routes, in 48 patients undergoing minor surgery. There were no significant differences in the mean elimination half-lives between the int...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00007691-199212000-00008
更新日期:1992-12-01 00:00:00
abstract::The clinical use of digoxin and phenytoin analyses (in 405 and 152 patients, respectively) furnished by our clinical pharmacological laboratory during a five-month period was evaluated prospectively from request forms. Of first-time analyses of digoxin, 12, 38, and 50% fell above, within, and below our recommended ran...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198103000-00006
更新日期:1981-01-01 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::Major advances in immunosuppression and reductions in the rates of acute rejection have led to increasing graft and patient survival rates during the past two decades. Chronic dysfunction of the renal allograft, however, remains a major clinical problem and probably represents the end result of the complex interplay b...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/00007691-200202000-00007
更新日期:2002-02-01 00:00:00
abstract::The authors describe a rapid, useful, specific, and very sensitive high-performance liquid chromatographic assay for the determination of fluvastatin (FV) level using atorvastatin as the internal standard (IS). After a simple deproteinization of 1.0 mL of plasma with acetonitrile, the drug and IS were extracted with t...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200302000-00013
更新日期:2003-02-01 00:00:00
abstract::A study was conducted to determine whether assay-specific quantitative differences exist in the determination of vancomycin serum concentrations obtained from patients with renal dysfunction. Vancomycin serum concentrations were obtained during the first week of therapy for each of three time intervals: 48-96 h, 96-14...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章
doi:10.1097/00007691-199612000-00004
更新日期:1996-12-01 00:00:00
abstract::A variety of medications are used in treating patients infected with the human immunodeficiency virus (HIV). These medications are used to control viremia and to prevent and treat opportunistic infections. An individual is often required to take numerous drugs at the same time and thus clinicians are confronted with p...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/00007691-200112000-00001
更新日期:2001-12-01 00:00:00
abstract:BACKGROUND:The pharmacokinetics of long-acting intramuscular paliperidone in a naturalistic setting is not well documented. The objective of this study was to investigate the relationship between dose and serum concentrations of paliperidone using data from a routine therapeutic drug monitoring service. METHODS:Serum ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000457
更新日期:2017-12-01 00:00:00
abstract::Monitoring of serum voriconazole concentrations has been proposed to optimize therapeutic effect and minimize toxicity. However, little is known about the clinical use of voriconazole therapeutic drug monitoring (TDM) by treating physicians. Four hundred seventy-eight episodes corresponding with 161 adult patients (me...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e3181ea3de6
更新日期:2010-10-01 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::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::Hydroxylation of midazolam (MDZ) is mediated almost exclusively by CYP3A isoforms. The authors describe a high-performance liquid chromatography assay involving MDZ, 1'-hydroxymidazolam, and 4-hydroxymidazolam in plasma. The compounds were eluted on an Ultrasphere ODS, 3-microm particle size, 7.5 cm x 4.6 mm reversed-...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199806000-00013
更新日期:1998-06-01 00:00:00
abstract::Metabolism of thiopurine drugs--azathioprine, 6-mercaptopurine, and 6-thioguanine--has provided a powerful pharmacogenetic model incorporating polymorphism of the enzyme thiopurine methyltransferase (TPMT) and the primary active metabolite, thioguanine nucleotide (TGN). However, a sense of uncertainty about the useful...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/01.ftd.0000169061.52715.3e
更新日期:2005-10-01 00:00:00
abstract::Sixty-two serum samples from 28 pediatric epileptic patients under treatment with phenytoin [diphenylhydantoin (DPH)] were obtained to study the correlation between total and free serum DPH concentrations. The effect of coadministered antiepileptic drugs on DPH protein binding was also studied. Binding of DPH to serum...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:
更新日期:1988-01-01 00:00:00
abstract:BACKGROUND:We report a feasibility study based on our large-scale experience with mycophenolate mofetil dose adjustment based on mycophenolic acid interdose area under the curve (AUC) in renal transplant patients. METHODS:Between 2005 and 2010, 13,930 requests for 7090 different patients (outside any clinical trial) w...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31821633a6
更新日期:2011-06-01 00:00:00
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
doi:10.1097/00007691-200002000-00002
更新日期:2000-02-01 00:00:00
abstract::The aim of this review is to provide information for interpreting outcome results from monitoring of antipsychotics in biological samples. A brief overview of the working mechanisms, pharmacological effects, drug interactions, and analytical methods of classical and atypical antipsychotics is given. Nineteen antipsych...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/FTD.0b013e3182708ec5.
更新日期:2012-12-01 00:00:00
abstract:BACKGROUND:Perampanel is a new antiepileptic drug (AED) that acts as a noncompetitive α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptor antagonist and is mainly metabolized by cytochrome P450 (CYP) 3A4. This study evaluated the influence of concomitant AEDs on the serum concentration profile of pera...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000416
更新日期:2017-08-01 00:00:00
abstract:BACKGROUND:Busulfan dose adjustment is routinely guided by plasma concentration monitoring using 4-9 blood samples per dose adjustment, but a pharmacometric Bayesian approach could reduce this sample burden. METHODS:The authors developed a nonparametric population model with Pmetrics. They used it to simulate optimal ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000276
更新日期:2016-06-01 00:00:00
abstract::There is increasing evidence that monitoring predose plasma levels of mycophenolic acid (MPA) is of benefit in renal transplant recipients treated with mycophenolate mofetil (MMF). Concomitant treatment with oral antibiotics leads to a 10% to 30% reduction in MPA area under the curve (AUC)0-12, probably by reducing en...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章
doi:10.1097/FTD.0b013e31803111d5
更新日期:2007-02-01 00:00:00
abstract:BACKGROUND:Human immunodeficiency virus (HIV)-infected individuals show large interindividual variation in response to antiretroviral therapy. Efavirenz (EFV) and nevirapine (NVP) are nonnucleoside reverse transcriptase inhibitors, which are prescribed in combination with other antiretroviral therapy in so-called highl...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31824868f3
更新日期:2012-04-01 00:00:00
abstract::Epilepsy is characterized by seizures recurring at interindividually differing time intervals. It may be difficult to assess drug response if time intervals between seizures are long. Thus, the existence of surrogate parameters that could be used to reliably identify drug efficacy and tolerability at an early stage an...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/FTD.0000000000000623
更新日期:2019-04-01 00:00:00
abstract::Racemic methadone is increasingly used to manage cancer pain. The authors studied 13 terminally ill patients with cancer pain, who underwent switching (rotation) from morphine to methadone. The relationship between initial morphine dose and final methadone dose, the pharmacokinetics of R- and S- methadone, and the deg...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/01.ftd.0000211827.03726.e4
更新日期:2006-06-01 00:00:00
abstract:BACKGROUND:Because of its superior sensitivity and specificity, multianalyte high-performance liquid chromatography coupled with tandem mass spectrometry has become the gold standard in clinical toxicology. Although several qualitative and quantitative liquid chromatography coupled with tandem mass spectrometry assays ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000429
更新日期:2017-10-01 00:00:00