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 differ between treatments. The disposition could be described using a two-compartment model with terminal half-lives of 5.68 +/- 2.62 h (mean +/- SD) after 60 mg and 5.5 +/- 2.22 h after 120 mg. The half-life of the metabolite N-demethyldiltiazem (MA) was similar to or slightly longer than that of diltiazem, whereas the half-life of deacetyldiltiazem (M1) was longer: 9.80 +/- 5.27 h and 10.43 +/- 5.38 h (n = 5). The area under the curve (AUC) of diltiazem increased significantly more than twofold after doubling of the dose, indicating an increased bioavailability, probably because of decreased presystemic elimination. The ratio between the AUCs for metabolites and diltiazem were 0.48 +/- 0.12 and 0.45 +/- 0.06 for MA and 0.16 +/- 0.10 and 0.15 +/- 0.10 for M1 after 60 mg and 120 mg diltiazem. The cumulative excretions of radioactivity within 120 h were 86 +/- 9% and 87 +/- 6%. The tracer was mainly excreted in urine (69 +/- 7% and 72 +/- 6%) and the remaining amounts were excreted in feces.
journal_name
Ther Drug Monitjournal_title
Therapeutic drug monitoringauthors
Höglund P,Nilsson LGsubject
Has Abstractpub_date
1989-09-01 00:00:00pages
551-7issue
5eissn
0163-4356issn
1536-3694journal_volume
11pub_type
杂志文章abstract:BACKGROUND:The efficacy of drugs for the treatment of substance-related disorders is moderate at best. Therapeutic drug monitoring (TDM) could be an instrument to improve outcomes. Because TDM for most of those drugs is not established, the authors reviewed the literature and built a rating scale to detect the potentia...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/FTD.0b013e31822fbf7c
更新日期:2011-10-01 00:00:00
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
doi:10.1097/00007691-200002000-00022
更新日期:2000-02-01 00:00:00
abstract:BACKGROUND:A fast and easy-to-use liquid chromatography-tandem mass spectrometry method for the determination and quantification of 6 triazoles [fluconazole (FLZ), isavuconazole (ISZ), itraconazole (ITZ), hydroxy-itraconazole (OH-ITZ), posaconazole (PSZ), and voriconazole (VRZ)] in human plasma and serum was developed ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000438
更新日期:2017-10-01 00:00:00
abstract::A 7.5-year-old girl who was treated with phenobarbital (PHB) for epilepsy was admitted with decreased levels of consciousness. She had been known to have high PHB levels of unknown cause, without symptoms. Her PHB levels were very high, as expected, but primidone levels were also detected although she and her parents ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/FTD.0b013e3182843206
更新日期:2013-04-01 00:00:00
abstract:BACKGROUND:Treatment with monoclonal antibodies (mAbs) against programmed cell death protein 1 receptor is subject to high variation in treatment outcome among cancer patients. For these agents, no exposure-response (ER) relationships have been investigated in routine health care settings. However, ER relationships hav...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000534
更新日期:2018-10-01 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:BACKGROUND:The once-daily formulation of tacrolimus has been reported to exhibit the same efficacy and safety profile as compared with the immediate-release form administered twice daily. However, as a result of differences in their pharmacokinetic (PK) profile, the PK models or Bayesian estimators (MAP-BE) previously ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e3181cc70db
更新日期:2010-04-01 00:00:00
abstract::Phenytoin binding to serum proteins and factors influencing protein binding were investigated in 38 critically ill trauma patients. In 24% of these patients, the free fraction of phenytoin was < or = 10%, whereas in 76%, the free phenytoin fraction was increased > 10%--up to 24%. Nonantiepileptic comedication, sex, or...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199404000-00005
更新日期:1994-04-01 00:00:00
abstract::Monitoring plasma concentrations of therapeutic drugs presents special problems when these drugs are metabolized to compounds that have pharmacologic activity. This presentation reviews several methods for evaluating the pharmacologic activity of drug metabolites and describes the impact of active drug metabolites on ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/00007691-198001000-00004
更新日期:1980-01-01 00:00:00
abstract:BACKGROUND:Non-vitamin K antagonist oral anticoagulants (NOACs) are approved for several indications for prophylaxis of thromboembolism at fixed oral doses. The analysis of NOAC activity/concentration may be required in special patient populations. Heptest coagulation assay determines both factor Xa and thrombin inhibi...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000157
更新日期:2015-06-01 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::A rapid and reliable micro procedure for the high pressure liquid chromatographic analysis of cimetidine. N"-cyano-N-methyl-N'-[2-[[(5-methyl-1H-imidazol-4-yl)methyl]thio]ethyl]guanidine, in serum or plasma is described. The percentage analytical recovery of cimetidine and internal standard (beta-hydroxypropyl-theophy...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-197901030-00010
更新日期:1979-01-01 00:00:00
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
doi:
更新日期:1983-06-01 00:00:00
abstract::After observing the phenomenon clinically, seven post-hemodialysis patients were studied for a rebound effect of gentamicin levels. Serum gentamicin levels were obtained immediately after dialysis and 1 hr postdialysis. An average 25.7% rebound occurred in the serum levels. A slow redistribution of gentamicin out of t...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198204000-00015
更新日期:1982-01-01 00:00:00
abstract:BACKGROUND:No information on the pharmacokinetic characteristics of amlodipine (AML) metabolites is available. This study aimed to develop a method based on isocratic liquid chromatography coupled to tandem mass spectrometry for the simultaneous determination of AML and its 2 major metabolites, dehydroamlodipine (DH-AM...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000449
更新日期:2017-12-01 00:00:00
abstract::The immunosuppressants cyclosporine, tacrolimus, sirolimus, everolimus, and probably also mycophenolic acid require therapeutic drug monitoring (TDM)-guided dosing to ensure that blood concentrations are kept within the target range in transplant patients. Reliable, accurate, and precise test methods are therefore ess...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000205
更新日期:2015-12-01 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::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...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31818d73b3
更新日期:2008-12-01 00:00:00
abstract:OBJECTIVE:This naturalistic therapeutic drug monitoring (TDM) study aimed to evaluate the relationship between dosage, serum concentration, and clinical outcome in children and adolescents treated with the serotonin reuptake inhibitor sertraline for different indications. METHODS:Steady-state trough serum concentratio...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31827a1aad
更新日期:2013-02-01 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:In this study, the authors studied the effect of thioridazine (TDZ) on the pharmacokinetic profile of quetiapine (QTP) in Taiwanese patients with schizophrenia. METHODS:Sixteen subjects with schizophrenia were recruited for this study. The authors pretreated 8 patients with TDZ 50 mg daily continuously give...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,多中心研究
doi:10.1097/FTD.0b013e31825479cc
更新日期:2012-06-01 00:00:00
abstract::The remarkably strong formation of the mycophenolic acid molecular ion from mycophenolic acid glucuronide during electrospray atmospheric pressure ionization in patients' serum samples is described. It is concluded that because of this effect appropriate chromatographic separation prior to tandem-mass spectrometric an...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200112000-00021
更新日期:2001-12-01 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:BACKGROUND:To increase target attainment rates, switching the mode of administration from intermittent (InI) to continuous infusion (CoI) has been proposed. In this study, target attainment rates and interpatient variation in exposure were compared between vancomycin InI- and CoI-treated critically ill patients. METHO...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000295
更新日期:2016-06-01 00:00:00
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::An isocratic, high-performance liquid chromatography method has been developed for simultaneous determination of the oral antidiabetic tolbutamide and two of its metabolites, 4-hydroxytolbutamide and carboxytolbutamide, in human plasma and urine. The method was based on simple one-step liquid-liquid extraction with te...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199912000-00015
更新日期:1999-12-01 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::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::A 64-year-old man on chronic hemodialysis for end-stage renal disease developed peritoneal carcinomatosis, and palliative chemotherapy with fluorouracil was started. The drug was administered (325 mg/m as IV bolus, at 2 PM) on 2 separate occasions, ie, 1 hour after dialysis and 2 days later, 49 hours after dialysis. T...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/01.ftd.0000183384.89275.f4
更新日期:2005-12-01 00:00:00
abstract::A population pharmacokinetic model was developed after administration of orogastric and/or intravenous indomethacin for the treatment of patent ductus arteriosus in preterm infants. Plasma indomethacin concentrations (n=227) were obtained from 90 preterm infants of median gestational age 27 weeks, mean postnatal age o...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章
doi:10.1097/FTD.0b013e31815b3e13
更新日期:2007-12-01 00:00:00