The pharmacokinetics of zileuton in healthy young and elderly volunteers.


:The effects of age and gender on the single and multiple dose pharmacokinetics of zileuton have been examined in a phase I nonblinded study. A total of 27 healthy volunteers were evaluable, 9 in the young group (age range 20 to 40 years; 5 males and 4 females) and 18 in the elderly group (range 65 to 81 years; 9 males and 9 females). A single oral dose of zileuton 600mg was given to all volunteers on day 1 of the study and at 6-hour intervals from days 3 to 7. Analysis of variance showed slight but significant decreases in the mean apparent clearance of total and free drug in the healthy elderly population after a single zileuton dose, but no significant age-related differences after multiple 6-hourly doses. Similarly, zileuton peak and trough plasma concentrations, and values for half-life, volume of distribution and protein binding were not significantly affected by age after either a single dose or multiple administration. Moreover, gender effects on the pharmacokinetics were also absent after correction for bodyweight differences. From the results of the present study, it is concluded that there is no pharmacokinetic basis for alteration of zileuton dosage schedules in elderly patients.


Clin Pharmacokinet


Braeckman RA,Granneman GR,Locke CS,Machinist JM,Cavannaugh JH,Awni WM




Has Abstract


1995-01-01 00:00:00








29 Suppl 2


  • Pharmacokinetic, pharmacodynamic and pharmacogenetic profile of the oral antiplatelet agent ticagrelor.

    abstract::Acute coronary syndromes (ACS) remain life-threatening disorders associated with high morbidity and mortality, despite advances in treatment over the last decade. Adenosine diphosphate-induced platelet activation via P2Y(12) receptors plays a pivotal role in the pathophysiology of ACS. The current standard of treatmen...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Teng R

    更新日期:2012-05-01 00:00:00

  • Drug-Drug Interaction Studies of Elagolix with Oral and Transdermal Low-Dose Hormonal Add-Back Therapy.

    abstract:BACKGROUND AND OBJECTIVE:Elagolix is an oral, non-peptide, gonadotropin-releasing hormone receptor antagonist. It is approved for the treatment of moderate-to-severe pain associated with endometriosis and is being investigated for the treatment of heavy menstrual bleeding associated with uterine fibroids. Use of low-do...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Nader A,Mostafa NM,Ali F,Shebley M

    更新日期:2021-01-01 00:00:00

  • Clinical pharmacokinetics of nabumetone. The dawn of selective cyclo-oxygenase-2 inhibition?

    abstract::Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) of the 2,6-disubstituted naphthyl-alkanone class. Nabumetone is metabolised to an active metabolite 6-methoxy-2-napthylacetic acid (6-MNA) which is a relatively selective cyclo-oxygenase-2 inhibitor that has anti-inflammatory and analgesic properties. Nabumet...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Davies NM

    更新日期:1997-12-01 00:00:00

  • Pharmacokinetic Studies in Neonates: The Utility of an Opportunistic Sampling Design.

    abstract:BACKGROUND AND OBJECTIVE:The use of an opportunistic (also called scavenged) sampling strategy in a prospective pharmacokinetic study combined with population pharmacokinetic modelling has been proposed as an alternative strategy to conventional methods for accomplishing pharmacokinetic studies in neonates. However, th...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Leroux S,Turner MA,Guellec CB,Hill H,van den Anker JN,Kearns GL,Jacqz-Aigrain E,Zhao W,TINN (Treat Infections in NeoNates) and GRiP (Global Research in Paediatrics) Consortiums.

    更新日期:2015-12-01 00:00:00

  • Models for placental transfer studies of drugs.

    abstract::Pregnancy is a specific dynamic state, and the potential usefulness of caring for a disorder in the fetus or the mother is now well established. Previously, pregnant women have been excluded from clinical trials, therefore only a few studies concerning evaluation of the pregestational metabolism or transplacental tran...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Bourget P,Roulot C,Fernandez H

    更新日期:1995-02-01 00:00:00

  • Inter-individual differences in baseline coagulation activities and their implications for international normalized ratio control during warfarin initiation therapy.

    abstract:BACKGROUND AND OBJECTIVE:Genetic polymorphisms of cytochrome P450 (CYP) 2C9 (CYP2C9) and vitamin K epoxide reductase complex subunit 1 (VKORC1) and patient demographic characteristics are responsible for inter-individual differences in warfarin maintenance dosage requirements. At present, however, the factors associate...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,随机对照试验


    authors: Ichimura Y,Takahashi H,Lee MT,Shiomi M,Mihara K,Morita T,Chen YT,Echizen H

    更新日期:2012-12-01 00:00:00

  • Dose-Dependent Bioavailability and CYP3A Inhibition Contribute to Non-Linear Pharmacokinetics of Voriconazole.

    abstract::Voriconazole is both a substrate and a potent inhibitor of cytochrome P450 (CYP) 3A. It has a high bioavailability and non-linear pharmacokinetics. We investigated the pharmacokinetics and metabolism of 50 mg and 400 mg doses of intravenous and oral voriconazole in 14 healthy volunteers. Concurrently, we determined sy...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章


    authors: Hohmann N,Kocheise F,Carls A,Burhenne J,Weiss J,Haefeli WE,Mikus G

    更新日期:2016-12-01 00:00:00

  • Salivary antipyrine half-life during injectable progestagen contraception.

    abstract::Antipyrine pharmacokinetics were studied in 6 healthy women before and 2, 8 and 12 weeks after administering the injectable progestagen (progestin), norethisterone (norethindrone) enanthate 200mg intramuscularly. Additionally, antipyrine kinetics in 5 women who had previously used the injectable contraceptive for 8 to...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Joshi JV,Gupta KC,Hazari KT,Gokral J,Pohujani S,Satoskar R

    更新日期:1986-03-01 00:00:00

  • Protein binding as a primary determinant of the clinical pharmacokinetic properties of non-steroidal anti-inflammatory drugs.

    abstract::The ability of a wide variety of anionic, cationic, and neutral drugs to bind in a reversible manner to plasma proteins has long been recognised. Non-steroidal anti-inflammatory drugs (NSAIDs) are distinguished as a class by the high degree to which they bind to plasma protein. Plasma protein binding properties are pr...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Lin JH,Cocchetto DM,Duggan DE

    更新日期:1987-06-01 00:00:00

  • Population pharmacokinetics and dosing recommendations for cisplatin during intraperitoneal peroperative administration: development of a limited sampling strategy for toxicity risk assessment.

    abstract:BACKGROUND:Ovarian cancer is the leading cause of gynaecological cancer-related death in Western countries. Intraperitoneal (IP) peroperative chemotherapy is an interesting therapeutic option. However, very few data are available regarding pharmacokinetics and especially population pharmacokinetics. PATIENTS AND METHO...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Royer B,Jullien V,Guardiola E,Heyd B,Chauffert B,Kantelip JP,Pivot X

    更新日期:2009-01-01 00:00:00

  • Pharmacokinetics of cyclosporin microemulsion in patients with inflammatory bowel disease.

    abstract:OBJECTIVE:To obtain a pharmacokinetic profile of cyclosporin microemulsion formulation in patients with inflammatory bowel disease. PATIENTS AND PARTICIPANTS:58 consecutive patients (19 women and 39 men), aged 16 to 64 years (mean age 38 years), with a diagnosis of ulcerative colitis (29 patients) or Crohn's disease (...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Latteri M,Angeloni G,Silveri NG,Manna R,Gasbarrini G,Navarra P

    更新日期:2001-01-01 00:00:00

  • A Mechanism-Based Population Pharmacokinetic Analysis Assessing the Feasibility of Efavirenz Dose Reduction to 400 mg in Pregnant Women.

    abstract:BACKGROUND:Reducing the dose of efavirenz can improve safety, reduce costs, and increase access for patients with HIV infection. According to the World Health Organization, a similar dosing strategy for all patient populations is desirable for universal roll-out; however, it remains unknown whether the 400 mg daily dos...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Schalkwijk S,Ter Heine R,Colbers AC,Huitema ADR,Denti P,Dooley KE,Capparelli E,Best BM,Cressey TR,Greupink R,Russel FGM,Mirochnick M,Burger DM

    更新日期:2018-11-01 00:00:00

  • Lopinavir/ritonavir pharmacokinetics in HIV and hepatitis C virus co-infected patients without liver function impairment: influence of liver fibrosis.

    abstract:BACKGROUND AND OBJECTIVE:To assess the influence of hepatitis C virus (HCV) co-infection and the extent of liver fibrosis on lopinavir/ritonavir pharmacokinetics in HIV-infected patients without liver function impairment. METHODS:Cross-sectional, comparative study enrolling HIV-infected adults receiving lopinavir/rito...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Moltó J,Valle M,Blanco A,Negredo E,DelaVarga M,Miranda C,Miranda J,Domingo P,Vilaró J,Tural C,Costa J,Barbanoj MJ,Clotet B

    更新日期:2007-01-01 00:00:00

  • The fentanyl HCl patient-controlled transdermal system (PCTS): an alternative to intravenous patient-controlled analgesia in the postoperative setting.

    abstract::Inadequate pain control in the postoperative period not only contributes to patient discomfort, but also causes physiological changes that may result in increased risk of myocardial ischaemia, deep vein thrombosis and pulmonary embolism. These events complicate postoperative recovery and may lead to longer hospital st...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Sinatra R

    更新日期:2005-01-01 00:00:00

  • The clinical pharmacokinetics of escitalopram.

    abstract::Escitalopram is the (S)-enantiomer of the racemic selective serotonin reuptake inhibitor antidepressant citalopram. Clinical studies have shown that escitalopram is effective and well tolerated in the treatment of depression and anxiety disorders. Following oral administration, escitalopram is rapidly absorbed and rea...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Rao N

    更新日期:2007-01-01 00:00:00

  • Cellular Uptake of Glucocerebrosidase in Gaucher Patients Receiving Enzyme Replacement Treatment.

    abstract:BACKGROUND:Enzyme replacement therapy (ERT) is currently the standard treatment for patients with Gaucher disease type I (GD1), but the pharmacokinetics have hardly been studied. This study aimed to quantify in vivo enzyme activity in peripheral leukocytes from patients receiving long-term treatment with imiglucerase o...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Gras-Colomer E,Martínez-Gómez MA,Moya-Gil A,Fernandez-Zarzoso M,Merino-Sanjuan M,Climente-Martí M

    更新日期:2016-09-01 00:00:00

  • Population pharmacokinetic modeling of veliparib (ABT-888) in patients with non-hematologic malignancies.

    abstract:BACKGROUND AND OBJECTIVE:Veliparib (ABT-888) is a potent oral inhibitor of Poly(ADP-ribose) polymerase enzyme that is currently in development for the treatment of non-hematologic and hematologic malignancies. This analysis characterizes the population pharmacokinetics of veliparib, including developing a structural ph...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,多中心研究,随机对照试验


    authors: Salem AH,Giranda VL,Mostafa NM

    更新日期:2014-05-01 00:00:00

  • Sex-related differences in drug disposition in man.

    abstract::Sex-related differences in the disposition of some analgesics, anxiolytics and hypnotics have recently been reported. With certain benzodiazepines, sex has been shown to be a more important determinant of variability in drug disposition than age, while with other benzodiazepines an age-related decline in clearance was...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Wilson K

    更新日期:1984-05-01 00:00:00

  • Pharmacokinetics of grepafloxacin after oral administration of single and repeat doses in healthy young males.

    abstract::The pharmacokinetics of grepafloxacin in healthy male subjects following single oral administration of doses ranging from 200 to 1200 mg, and following repeated oral administration of 400 and 800 mg doses are reported. Plasma levels of grepafloxacin reached a peak within 2 hours (on average) following drug administrat...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章


    authors: Efthymiopoulos C,Bramer SL,Maroli A

    更新日期:1997-01-01 00:00:00

  • The relative bioavailability of temafloxacin administered through a nasogastric tube with and without enteral feeding.

    abstract::The relative bioavailability of a single oral dose of temafloxacin given with and without enteral feeding was determined in 18 healthy male volunteers in a randomised crossover study. Subjects were administered 600mg of temafloxacin orally as an intact tablet, or a crushed tablet suspended in water administered throug...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Lubowski TJ,Nightingale CH,Sweeney K,Quintiliani R

    更新日期:1992-01-01 00:00:00

  • Clinical Pharmacokinetics and Pharmacodynamics of Drugs in the Central Nervous System.

    abstract::Despite contributing significantly to the burden of global disease, the translation of new treatment strategies for diseases of the central nervous system (CNS) from animals to humans remains challenging, with a high attrition rate in the development of CNS drugs. The failure of clinical trials for CNS therapies can b...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Srinivas N,Maffuid K,Kashuba ADM

    更新日期:2018-09-01 00:00:00

  • Nonparametric expectation maximisation (NPEM) population pharmacokinetic analysis of caffeine disposition from sparse data in adult caucasians: systemic caffeine clearance as a biomarker for cytochrome P450 1A2 activity.

    abstract:OBJECTIVE:To explore the ability of the nonparametric expectation maximisation (NPEM) method of population pharmacokinetic modelling to deal with sparse data in estimating systemic caffeine clearance for monitoring and evaluation of cytochrome P450 (CYP) 1A2 activity. DESIGN AND PARTICIPANTS:Nonblind, single-dose clin...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章


    authors: Terziivanov D,Bozhinova K,Dimitrova V,Atanasova I

    更新日期:2003-01-01 00:00:00

  • Steady-state pharmacokinetics of controlled release oral morphine sulphate in healthy subjects.

    abstract::The pharmacokinetics of oral morphine sulphate as controlled release tablets ('MS-Contin') and solution were compared at steady-state. Plasma morphine concentrations were determined over 24 hours following the last dose of each drug when given in a randomised, crossover fashion to healthy subjects. Radioimmunoassay wa...

    journal_title:Clinical pharmacokinetics

    pub_type: 临床试验,杂志文章,随机对照试验


    authors: Savarese JJ,Goldenheim PD,Thomas GB,Kaiko RF

    更新日期:1986-11-01 00:00:00

  • The influence of renal function on plasma concentration, urinary excretion and antihypertensive effect of guanfacine.

    abstract::18 hypertensive patients with a glomerular filtration rate (GFR) between 3.8 and 113ml/min received guanfacine as single intravenous and multiple oral dose treatment. Mean plasma concentrations of guanfacine on the fifth day or oral treatment ranged from 6.5 to 8.6ng/ml in patients with normal renal function (GFR > 90...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Kirch W,Köhler H,Braun W,von Gizycki C

    更新日期:1980-09-01 00:00:00

  • Individualising gentamicin dosage regimens. A comparative review of selected models, data fitting methods and monitoring strategies.

    abstract::The various components required for individualising clinical drug dosage regimens are reviewed, including a study of 3 types of fitting procedures, 2 types of gentamicin pharmacokinetic model and the utility of D-optimal times for obtaining serum gentamicin concentrations. The combination of the current Bayesian fitti...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Jelliffe RW,Iglesias T,Hurst AK,Foo KA,Rodriguez J

    更新日期:1991-12-01 00:00:00

  • Clinical pharmacokinetics of dothiepin. Single-dose kinetics in patients and prediction of steady-state concentrations.

    abstract::The pharmacokinetics of dothiepin were evaluated in 9 depressed patients following a single oral dose of 75 mg. Blood and plasma concentrations of dothiepin and 2 major metabolites, northiaden and dothiepin S-oxide, were measured by gas chromatography/mass fragmentography. The mean (+/-SD) peak plasma concentrations o...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Maguire KP,Norman TR,McIntyre I,Burrows GD

    更新日期:1983-03-01 00:00:00

  • Clinical pharmacokinetics of fluconazole.

    abstract::Fluconazole was recently developed for the treatment of superficial and systemic fungal infections. Triazole groups and insertion of 2 fluoride atoms increase the polarity and hydrosolubility of the drug, allowing it to be used in a parenteral form. Bioassay methods using Candida pseudotropicalis as a test organism we...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Debruyne D,Ryckelynck JP

    更新日期:1993-01-01 00:00:00

  • First-pass elimination. Basic concepts and clinical consequences.

    abstract::First-pass elimination takes place when a drug is metabolised between its site of administration and the site of sampling for measurement of drug concentration. Clinically, first-pass metabolism is important when the fraction of the dose administered that escapes metabolism is small and variable. The liver is usually ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Pond SM,Tozer TN

    更新日期:1984-01-01 00:00:00

  • Clarithromycin clinical pharmacokinetics.

    abstract::Clarithromycin is a semisynthetic macrolide antibiotic, structurally related to erythromycin. It has a more favourable pharmacokinetic profile than erythromycin, thus allowing twice-daily administration and possibly increasing compliance among outpatients. Clarithromycin is well absorbed from the gastrointestinal trac...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章,评审


    authors: Fraschini F,Scaglione F,Demartini G

    更新日期:1993-09-01 00:00:00

  • Pharmacokinetics of orally administered duloxetine in children and adolescents with major depressive disorder.

    abstract:BACKGROUND:Duloxetine, a selective serotonin (5-hydroxytryptamine) and norepinephrine reuptake inhibitor, has been approved since 2004 for the treatment of adults with major depressive disorder (MDD). It is currently not approved for use in pediatric patients (aged <18 years) with MDD. The clinical development program ...

    journal_title:Clinical pharmacokinetics

    pub_type: 杂志文章


    authors: Lobo ED,Quinlan T,Prakash A

    更新日期:2014-08-01 00:00:00