Abstract:
:To investigate the pharmacokinetics of naloxone in healthy volunteers, we undertook an open-label crossover study in which six male volunteers received naloxone on five occasions: intravenous (0.8 mg), intramuscular (0.8 mg), intranasal (0.8 mg), intravenous (2 mg), and intranasal (2 mg). Samples were collected for 4 hours after administration for 128 samples in total. A population pharmacokinetic analysis was undertaken using NONMEM. The data were best described by a three-compartment model with first-order absorption for intramuscular and intranasal administration, between-subject variability on clearance and central volume, lean body weight on clearance, and weight on central volume. Relative bioavailability of intramuscular and intranasal naloxone was 36% and 4%, respectively. The final parameter estimates were clearance, 91 L/hr; central volume, 2.87 L; first peripheral compartment volume, 1.49 L, second peripheral compartment volume, 33.6 L; first intercompartmental clearance, 5.66 L/hr; second intercompartmental clearance, 29.8 L/hr; Ka (intramuscular), 0.65; and Ka (intranasal), 1.52. Median time to peak concentration for intramuscular naloxone was 12 minutes and for intranasal, 6 to 9 minutes. A combination of intravenous and intramuscular naloxone provided immediate high and then detectable concentrations for 4 hours. Intranasal naloxone had poor bioavailability compared with intramuscular. Combined intravenous and intramuscular administration may be a useful alternative to naloxone infusions.
journal_name
Ther Drug Monitjournal_title
Therapeutic drug monitoringauthors
Dowling J,Isbister GK,Kirkpatrick CM,Naidoo D,Graudins Adoi
10.1097/FTD.0b013e3181816214subject
Has Abstractpub_date
2008-08-01 00:00:00pages
490-6issue
4eissn
0163-4356issn
1536-3694journal_volume
30pub_type
临床试验,杂志文章abstract::With the introduction of a cyclosporin monitoring strategy based on the use of a sample collected 2 hours after dosing (C2) rather than the predose sample (C0), there was concern that the differences in blood cyclosporin results from the various assay systems would result in assay-specific target ranges for C2 monitor...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章,多中心研究
doi:10.1097/00007691-200304000-00005
更新日期:2003-04-01 00:00:00
abstract:BACKGROUND:Stiripentol (STP) was approved as an orphan drug in 2007 in Europe as adjunctive therapy with valproic acid (VPA) and clobazam (CLB) for Dravet syndrome. Dravet syndrome is a highly pharmacoresistant form of epilepsy, which starts in early childhood. Data about STP pharmacokinetics and interactions are still...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31825dc4a6
更新日期:2012-08-01 00:00:00
abstract::The immunosuppressant mycophenolic acid (MPA) used for solid organ transplantation is predominantly metabolized to a pharmacologically inactive phenolic glucuronide (MPAG) and, to a lesser extent, to the pharmacologically active acyl glucuronide (AcMPAG). The recently introduced CEDIA Mycophenolic Acid Assay from Micr...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e3181cc342a
更新日期:2010-02-01 00:00:00
abstract::The analysis of quinine in whole blood, plasma, urine, and samples dried on filter paper is described. Extraction was made with toluene followed by back-extraction into phosphate buffer. A reversed-phase liquid chromatography system with fluorescence detection was used. The within-day coefficient of variation of the m...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199308000-00012
更新日期:1993-08-01 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: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:BACKGROUND:The objective of this study was to investigate the serum concentrations of olanzapine in relation to age, sex, and other factors in Chinese patients aged between 10 and 90 years. METHODS:Data for 884 olanzapine patients, deposited between 2016 and 2017, were retrieved from the therapeutic drug monitoring da...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000738
更新日期:2020-08-01 00:00:00
abstract::The greater and more consistent absorption of cyclosporine from the microemulsion formulation (Neoral; Novartis Pharmaceuticals Ltd., Frimley, UK) when compared with that from the original form (Sandimmune; Novartis Pharmaceuticals Ltd., Frimley, UK) results in greater systemic exposure. Lung transplant recipients cou...
journal_title:Therapeutic drug monitoring
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1097/00007691-199902000-00004
更新日期:1999-02-01 00:00:00
abstract::The preferred dose of netilmicin was determined in each of 39 patients with severe gram-negative sepsis treated at two centres. The dose was based upon the attainment of recommended serum concentrations. Patient age varied from 18 to 87 years (mean 58), estimated creatinine clearance from 20 to 150 ml/min (mean 71), a...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:
更新日期:1986-01-01 00:00:00
abstract:BACKGROUND:Body weight may affect pharmacokinetic parameters in various ways and may therefore have a significant impact on the serum concentration of a drug at a given dose. Although patients with major depressive disorder frequently show an elevated body mass index, studies investigating the relation between body wei...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e318237b0fa
更新日期:2011-12-01 00:00:00
abstract::The high incidence of psychiatric illness in the postpartum period and the increasing percentage of women who breastfeed has focused attention on the treatment of breastfeeding women with psychotropic medications and, additionally, the exposure of nursing infants to these medications. Consequently, there has been an i...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200402000-00011
更新日期:2004-02-01 00:00:00
abstract::Monoclonal antibodies (mAbs) may be used as biopharmaceuticals to treat various diseases, ranging from oncology to inflammatory and cardiovascular affections. Trustworthy analytical methods are necessary to study their pharmacokinetics, both during their development and in post-marketing studies. Because biopharmaceut...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章,评审
doi:10.1097/FTD.0000000000000419
更新日期:2017-08-01 00:00:00
abstract::Lopinavir is one of the most-widely used protease inhibitors in the treatment of HIV-1 infected patients. Concentration-effect relationships have been described for both antiviral activity and toxicity. Less is known about patient characteristics that may determine interpatient variability in lopinavir plasma concentr...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/01.ftd.0000245681.12092.d6
更新日期:2006-10-01 00:00:00
abstract::The authors have developed a simple isocratic high-pressure liquid chromatographic (HPLC) assay for the simultaneous determination of lamotrigine and other frequently coadministered antiepileptic drugs in serum samples. Lamotrigine extraction was performed on a reversed-phase Oasis HBL preparation column. The eluates ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-200010000-00019
更新日期:2000-10-01 00:00:00
abstract:BACKGROUND:Busulfan (Bu) and cyclophosphamide (Cy) are frequently included in conditioning regimens before hematopoietic stem cell transplantation (HSCT). Both drugs are detoxified by glutathione transferases (GST), and GST gene variants may explain some of the interindividual variability in pharmacokinetics and drug t...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000180
更新日期:2015-08-01 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::The performance of the ROCHE FP NAPA reagent, a newly reformulated monoclonal antibody-based fluorescence polarization immunoassay (FPIA) for N-acetylprocainamide, was compared with two commercially available polyclonal antibody-based immunoassays, the Abbott TDx and Syva EMIT. Although excellent correlation was obser...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199406000-00013
更新日期:1994-06-01 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:Desmopressin (D-amino D-arginine vasopressin: dDAVP) is used for the treatment of patients with hemophilia A and Von Willebrand disease. Studies on the rationale of dosing are scarce and mainly focus on the underlying causes of the vast differences in desmopressin response among individuals. The aim of this ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000791
更新日期:2020-12-01 00:00:00
abstract::Six groups of six male Wistar rats were administered methadone in their drinking water over the concentration range 0-0.25 mg/ml. Hair and trunk blood samples were collected after a 6-week period of drug administration. Immunoreactive methadone was measured by radioimmunoassay and methadone and its major metabolite, 2...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199612000-00014
更新日期:1996-12-01 00:00:00
abstract::The interlaboratory variability in the assay of theophylline and various anticonvulsant drugs was evaluated in a 16-month prospective study by using two independent experimental approaches: (a) a conventional method based on the distribution of quality control (QC) lyophilized human sera spiked with the test drugs (ph...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:
更新日期:1991-03-01 00:00:00
abstract::This case report highlights a very rare adverse drug reaction of oral roxithromycin causing toxic epidermal necrolysis (TEN). A 54-year-old male patient diagnosed with upper respiratory tract infection was prescribed oral roxithromycin 150 mg twice daily for 7 days. On the 10th day, the patient was admitted to the eme...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e318260b087
更新日期:2012-08-01 00:00:00
abstract:BACKGROUND:The indication for the antiepileptic drug lacosamide (LCM) was recently extended to include children from the age of 4 years. Real-life data on the use and serum concentrations of LCM in children and adolescents are limited. The purpose of this study was to investigate the use of LCM in this patient group in...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000599
更新日期:2019-06-01 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::The study was designed to determine the steady-state pharmacokinetic profile of diazepam and desmethyldiazepam following a 15-mg controlled-release capsule dosed once daily at either 7 a.m. or 11 p.m. compared with the respective profiles of the conventional 5-mg tablet dosed three times a day at 7 a.m., 12 p.m., and ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-198312000-00008
更新日期:1983-01-01 00:00:00
abstract::Urinary excretion of lipocalin-type prostaglandin D synthase (L-PGDS) has been suggested to be a useful biomarker of early diabetic nephropathy. We studied whether L-PGDS is also a marker of gentamicin (GM)-induced renal damage in the "creatinine-blind" range. A prospective study was conducted in 6 patients who were g...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0b013e31819566f1
更新日期:2009-02-01 00:00:00
abstract::We describe the case of a pediatric patient on azathioprine therapy with previously undiagnosed homozygote thiopurine S-methyltransferase (TPMT) deficiency, resulting in myelotoxic thiopurine metabolite levels. The patient was successfully treated with a very low azathioprine dose of 50 mg once a week (4% of standard ...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/FTD.0000000000000366
更新日期:2017-02-01 00:00:00
abstract::Digoxin and gentamicin are widely used in pediatric medicine, and therapeutic monitoring is mandatory because of their narrow margin of safety and wide interpatient and intrapatient pharmacokinetic variabilities. Saliva sampling may be of potential interest, especially in children, in whom blood sampling is often diff...
journal_title:Therapeutic drug monitoring
pub_type: 杂志文章
doi:10.1097/00007691-199806000-00003
更新日期:1998-06-01 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::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
doi:10.1097/FTD.0b013e31803bb85d
更新日期:2007-04-01 00:00:00