Effect of unbound clearance on binding parameters of valproic acid to serum proteins.

abstract：:Procainamide administration often results in excessively high serum N-acetylprocainamide (NAPA) concentrations and subtherapeutic serum procainamide concentrations. Inhibition of N-acetylation of procainamide may prevent accumulation of excessive NAPA while maintaining therapeutic serum procainamide concentrations. Th...

journal_title：Journal of clinical pharmacology

authors： Tisdale JE,Rudis MI,Padhi ID,Svensson CK,Webb CR,Borzak S,Ware JA,Krepostman A,Zarowitz BJ

更新日期：1995-09-01 00:00:00

abstract：:Inflammatory conditions, such as rheumatoid arthritis, reduce response to calcium channel and beta-adrenergic antagonists but not the angiotensin II type 1 receptor (AT(1)R) antagonist valsartan. Inflammation also reduces clearance of some drugs or active metabolite, thereby reducing response. Active (n = 14) and cont...

journal_title：Journal of clinical pharmacology

authors： Daneshtalab N,Lewanczuk RZ,Russell AS,Jamali F

更新日期：2006-11-01 00:00:00

abstract：:Although population studies have demonstrated a relationship between casual office blood pressures and target organ events, the variability of these blood pressure measurements for individual patients has generated an interest in the role of ambulatory blood pressure monitoring for defining the presence of hypertensio...

journal_title：Journal of clinical pharmacology

authors： Prisant LM,Bottini PB,Carr AA

更新日期：1992-07-01 00:00:00

abstract：:Chemotherapy-induced nausea and vomiting (CINV) is a common treatment-related adverse event that negatively impacts the quality of life of cancer patients. During pediatric drug development, extrapolation of efficacy from adult to pediatric populations is a pathway that can minimize the exposure of children to unneces...

journal_title：Journal of clinical pharmacology

authors： Momper JD,Heinrichs MT,Krudys K,Griebel D,Kumar S,Kim I,Mehrotra N,Mulberg AE,Garimella N,Nelson R,Reaman G,Sinha V,Yao L,Zineh I,Burckart G,Sachs H,Mulugeta Y

更新日期：2020-06-01 00:00:00

abstract：:Sleep disturbances and decrements of daytime performance have been attributed to HMG-CoA reductase inhibitors. As a rule, lipophilic compounds more readily cross the blood-brain barrier and are more likely to affect central nervous system function. The authors compared the effects of lovastatin (40 mg), a lipophilic c...

journal_title：Journal of clinical pharmacology

authors： Kostis JB,Rosen RC,Wilson AC

更新日期：1994-10-01 00:00:00

abstract：:Six obese (mean weight 92 kg) and five normal (60 kg) subjects received 2 mg diazepam nightly for 30 nights. Determination of diazepam and desmethyldiazepam plasma concentrations during the dosing period and for a withdrawal period indicated that accumulation half-life for both diazepam (7.8 days in obese vs. 3.1 days...

journal_title：Journal of clinical pharmacology

authors： Abernethy DR,Greenblatt DJ,Divoll M,Shader RI

更新日期：1983-08-01 00:00:00

abstract：:The safety, tolerability, and pharmacokinetics of orally administered enzastaurin were evaluated in 2 placebo-controlled, dose escalation studies in healthy subjects. In the first human dose study, single doses (2-400 mg) were evaluated, with 22 subjects receiving enzastaurin. The mean half-lives of enzastaurin and it...

journal_title：Journal of clinical pharmacology

authors： Welch PA,Sinha VP,Cleverly AL,Darstein C,Flanagan SD,Musib LC

更新日期：2007-09-01 00:00:00

abstract：:Therapeutic drug monitoring (TDM) has become standard clinical practice for gentamicin, amikacin, and vancomycin to optimize efficacy and reduce toxicity. TDM after the first dose of antibiotic was adopted in our institution. This study aims to evaluate if target therapeutic drug concentrations could be achieved more ...

journal_title：Journal of clinical pharmacology

authors： Lim WXS,Chua WBB,Chua JM,Lee Q,Chan JW,Sultana R,Poh BH

更新日期：2020-01-01 00:00:00

abstract：:Glasdegib is approved for treating acute myeloid leukemia in elderly patients at 100 mg once daily in combination with low-dose cytarabine. Exposure-efficacy analysis showed that the survival benefit of glasdegib was not glasdegib exposure-dependent. The relationship between glasdegib exposure and adverse event (AE) c...

journal_title：Journal of clinical pharmacology

authors： Ruiz-Garcia A,Shaik N,Lin S,Jamieson C,Heuser M,Chan G

更新日期：2021-03-01 00:00:00

abstract：:Faldaprevir is a potent hepatitis C virus (HCV) NS3/4A protease inhibitor and an inhibitor of UDP-glucuronosyltransferase-1A1 (UGT1A1), which is involved in raltegravir clearance. Raltegravir, an HIV integrase inhibitor, may be used in combination with HCV treatment in HCV/HIV co-infected patients. In this open-label,...

journal_title：Journal of clinical pharmacology

authors： Joseph D,Rose P,Strelkowa N,Schultz A,Garcia J,Elgadi M,Huang F

更新日期：2015-04-01 00:00:00

abstract：:Beverage-drug interactions have remained an active area of research and have been the subject of extensive investigations in the past 2 decades. The known mechanisms of clinically relevant beverage-drug interactions include modulation of the activity of cytochrome P450 (CYP) 3A and organic anion-transporting polypepti...

journal_title：Journal of clinical pharmacology

authors： An G,Mukker JK,Derendorf H,Frye RF

更新日期：2015-12-01 00:00:00

abstract：:The chemoattractant receptor-homologous molecule expressed on T-helper 2 cells (CRTH2) is a G-protein-coupled receptor for prostaglandin D2 , a key mediator in inflammatory disorders. In this randomized, double-blind, placebo-controlled study we investigated the single- and multiple-dose tolerability, pharmacokinetics...

journal_title：Journal of clinical pharmacology

authors： Géhin M,Strasser DS,Zisowsky J,Farine H,Groenen PM,Dingemanse J,Sidharta PN

更新日期：2015-07-01 00:00:00

abstract：:The relative analgesic potency of oral and intramuscular oxymorphone was evaluated in a double-blind crossover comparison of graded single doses in patients with chronic pain due to cancer. When both duration and intensity of analgesia are considered (total effect), oral oxymorphone was 1/6 as potent as the intramuscu...

journal_title：Journal of clinical pharmacology

authors： Beaver WT,Wallenstein SL,Houde RW,Rogers A

更新日期：1977-04-01 00:00:00

abstract：:CBER's philosophy partners with the sponsor's philosophy in the development of electronic dossiers. Based on the experience gained from a number of dossiers, CBER has established a standard management paradigm and imaging platform by which the review of radiographs has been facilitated. ...

journal_title：Journal of clinical pharmacology

authors： Fauntleroy M

更新日期：2001-07-01 00:00:00

abstract：:Eleven subjects completed a clinical trial to determine the safety/tolerability of freeze-dried black raspberries (BRB) and to measure, in plasma and urine, specific anthocyanins-cyanidin-3-glucoside, cyanidin-3-sambubioside, cyanidin-3-rutinoside, and cyanidin-3-xylosylrutinoside, as well as ellagic acid. Subjects we...

journal_title：Journal of clinical pharmacology

authors： Stoner GD,Sardo C,Apseloff G,Mullet D,Wargo W,Pound V,Singh A,Sanders J,Aziz R,Casto B,Sun X

更新日期：2005-10-01 00:00:00

abstract：:Data from five randomized, placebo-controlled, multiple oral dose studies of empagliflozin in patients with type 2 diabetes mellitus (T2DM; N = 974; 1-100 mg q.d.; ≤12 weeks) were used to develop a population pharmacokinetic (PK) model for empagliflozin. The model consisted of two-compartmental disposition, lagged fir...

journal_title：Journal of clinical pharmacology

authors： Riggs MM,Staab A,Seman L,MacGregor TR,Bergsma TT,Gastonguay MR,Macha S

更新日期：2013-10-01 00:00:00

abstract：:The antihypertensive effect of a new beta-adrenergic receptor blocker, l-bunolol, was evaluated in 11 hospitalized hypertensive patients of whom four belonged to the high-renin, five to the normal-renin, and two to the low-renin subgroup. There was a significant decrease in blood pressure in most patients, often to no...

journal_title：Journal of clinical pharmacology

authors： Gavras H,Gavras I,Brunner HR,Laragh JH

更新日期：1977-05-01 00:00:00

abstract：:Bococizumab (RN316/PF-04950615), a humanized monoclonal antibody, binds to secreted proprotein convertase subtilisin/kexin type 9 (PCSK9) and prevents its downregulation of low-density lipoprotein receptor, leading to improved clearance and reduction of low-density lipoprotein cholesterol (LDL-C) in plasma. A mechanis...

journal_title：Journal of clinical pharmacology

authors： Udata C,Garzone PD,Gumbiner B,Joh T,Liang H,Liao KH,Williams JH,Meng X

更新日期：2017-07-01 00:00:00

abstract：:This study investigated the steady-state pharmacokinetic interaction between the HIV protease inhibitor, darunavir (TMC114), administered with low-dose ritonavir (darunavir/ritonavir), and clarithromycin in HIV-negative healthy volunteers. In a 3-way crossover study, 18 individuals received darunavir/ritonavir 400/100...

journal_title：Journal of clinical pharmacology

authors： Sekar VJ,Spinosa-Guzman S,De Paepe E,De Pauw M,Vangeneugden T,Lefebvre E,Hoetelmans RM

更新日期：2008-01-01 00:00:00

abstract：:This study evaluated the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of a novel depot formulation of abarelix, a new gonadotropin-releasing hormone (GnRH) antagonist. This was an open-label, sequential two-phase study in healthy male subjects ages 50 to 75. Subjects received a single intramuscular (IM) do...

journal_title：Journal of clinical pharmacology

authors： Wong SL,Lau DT,Baughman SA,Fotheringham N,Menchaca D,Garnick MB

更新日期：2004-05-01 00:00:00

abstract：:A series of clinical pharmacology studies was performed to screen for possible pharmacokinetic/dynamic contributions to drug interactions reported in rheumatoid arthritis patients receiving cyclosporine and nonsteroidal antiinflammatory drugs (NSAIDs). No clinically relevant pharmacokinetic changes in any of the drugs...

journal_title：Journal of clinical pharmacology

authors： Kovarik JM,Mueller EA,Gerbeau C,Tarral A,Francheteau P,Guerret M

更新日期：1997-04-01 00:00:00

abstract：:Maraviroc is a C-C chemokine receptor type-5 antagonist approved for the treatment of HIV-1. Previous studies show that cytochrome P450 3A5 (CYP3A5) plays a role in maraviroc metabolism. CYP3A5 is subject to a genetic polymorphism. The presence of 2 functional alleles (CYP3A5*1/*1) confers the extensive metabolism phe...

journal_title：Journal of clinical pharmacology

authors： Vourvahis M,McFadyen L,Nepal S,Valluri SR,Fang A,Fate GD,Wood LS,Marshall JC,Chan PLS,Nedderman A,Haynes J,Savage ME,Clark A,Smith KY,Heera J

更新日期：2019-01-01 00:00:00

abstract：:Trecovirsen, a 25-mer antisense phosphorothioate oligonucleotide targeted at the gag site of the HIV gene, was administered to HIV-positive volunteers as an i.v. infusion. Single doses ranged from 0.1 to 2.5 mg/kg in an ascending escalation in cohorts of 6 to 12 subjects. Plasma trecovirsen concentrations and pharmaco...

journal_title：Journal of clinical pharmacology

authors： Séréni D,Tubiana R,Lascoux C,Katlama C,Taulera O,Bourque A,Cohen A,Dvorchik B,Martin RR,Tournerie C,Gouyette A,Schechter PJ

更新日期：1999-01-01 00:00:00

abstract：:The electrocardiographic (ECG) effects of rivastigmine treatment were assessed in mild to moderately severe Alzheimer's disease (AD) by analysis of four 26-week, double-blind, multicenter, placebo-controlled, phase III clinical trials. Of an initial 2791 patients, 77% completed treatment. Seventy-one percent required ...

journal_title：Journal of clinical pharmacology

authors： Morganroth J,Graham S,Hartman R,Anand R

更新日期：2002-05-01 00:00:00

abstract：:This study investigated the potential pharmacokinetic interaction between the direct renin inhibitor aliskiren and modulators of P-glycoprotein and cytochrome P450 3A4 (CYP3A4). Aliskiren stimulated in vitro P-glycoprotein ATPase activity in recombinant baculovirus-infected Sf9 cells with high affinity (K(m) 2.1 micro...

journal_title：Journal of clinical pharmacology

authors： Vaidyanathan S,Camenisch G,Schuetz H,Reynolds C,Yeh CM,Bizot MN,Dieterich HA,Howard D,Dole WP

更新日期：2008-11-01 00:00:00

abstract：:The pharmacokinetics of exogenously administered DHEA have not been well characterized despite its increasing use in therapeutic and research investigations. The purpose of this study was to evaluate the pharmacokinetics of DHEA and its sulfated metabolite (DHEA-S) after single- and multiple-dose oral administration o...

journal_title：Journal of clinical pharmacology

authors： Frye RF,Kroboth PD,Kroboth FJ,Stone RA,Folan M,Salek FS,Pollock BG,Linares AM,Hakala C

更新日期：2000-06-01 00:00:00

abstract：:Several approaches are available to estimate the glomerular filtration rate (GFR) from the sinistrin clearance. To compare such approaches, GFR was estimated in six healthy volunteers, both after a bolus injection and a bolus dose followed by a 6-hour infusion. A recently developed high-performance liquid chromatograp...

journal_title：Journal of clinical pharmacology

authors： Buclin T,Pechère-Bertschi A,Séchaud R,Décosterd LA,Munafo A,Burnier M,Biollaz J

更新日期：1997-08-01 00:00:00

abstract：:The effect of pomegranate juice (PJ) or grapefruit juice (GFJ) on CYP3A activity was studied in vitro and in healthy human volunteers. In human liver microsomes, the mean 50% inhibitory concentrations (IC(50)) for PJ and GFJ versus CYP3A (triazolam alpha-hydroxylation) were 0.61% and 0.55%, (v/v) respectively, without...

journal_title：Journal of clinical pharmacology

authors： Farkas D,Oleson LE,Zhao Y,Harmatz JS,Zinny MA,Court MH,Greenblatt DJ

更新日期：2007-03-01 00:00:00

abstract：:Ofatumumab is a human monoclonal antibody that binds to a unique CD20 epitope on the surface of B lymphocytes, resulting in efficient lysis of CD20-expressing cells via complement-dependent cytotoxicity and antibody-dependent cell-mediated cytotoxicity. The potential effect of ofatumumab on cardiac repolarization and ...

journal_title：Journal of clinical pharmacology

authors： Jewell RC,Laubscher K,Lewis E,Fang L,Gafoor Z,Carey J,McKeown A,West S,Wright O,Sedoti D,Dixon I,Hottenstein CS,Chan G

更新日期：2015-01-01 00:00:00

abstract：:We report population pharmacokinetic, pharmacodynamic, and pharmacokinetic-safety analyses to support phase II/III dose/regimen selection of alisertib, a selective Aurora A kinase (AAK) inhibitor. Phase I studies in adult cancer patients evaluated dosing on Days 1-7 in 21-day cycles or Days 1-21 in 35-day cycles, with...

journal_title：Journal of clinical pharmacology

authors： Venkatakrishnan K,Zhou X,Ecsedy J,Mould DR,Liu H,Danaee H,Fingert H,Kleinfield R,Milton A

更新日期：2015-03-01 00:00:00