Presystemic extraction: mechanisms and consequences.

abstract：:Propafenone and its 5-hydroxy metabolite exhibit different electrophysiological properties. Objectives of the CAQ-PAF study were (1) to develop a strategy favoring propafenone instead of 5-hydroxypropafenone in plasma following oral administration of propafenone and (2) to evaluate the potential of low-dose quinidine ...

journal_title：Journal of clinical pharmacology

authors： O'Hara GE,Philippon F,Gilbert M,Champagne J,Michaud V,Charbonneau L,Pruneau G,Hamelin BA,Geelen P,Turgeon J

更新日期：2012-02-01 00:00:00

abstract：:This study was designed to determine the pharmacokinetics and dose proportionality of clentiazem (CLZ) after single doses (SD) of 20, 40, and 80 mg and multiple dose administration (SS) of 40, 80, and 160 mg/day for 5 days. The study was an open-label, randomized four-period complete crossover design. Twenty-four heal...

journal_title：Journal of clinical pharmacology

authors： Bhargava VO,Shah AK,Weir SJ,Nordbrock EE,Giesing DH

更新日期：1993-05-01 00:00:00

abstract：:The new antidepressant nomifensin (Hoechst 36984), a drug which showed less cardiotoxicity than tricyclics, was compared in a single-blind comparative trial with viloxazine. Forty elderly depressed patients were treated during four weeks. Nomifensin, N=21, 75 mg/day; viloxazine, N=19, 150 mg/day). Antidepressant effec...

journal_title：Journal of clinical pharmacology

authors： Moizeszowicz J,Subirá S

更新日期：1977-01-01 00:00:00

abstract：:The approved antiretroviral drugs, emtricitabine and tenofovir disoproxil fumarate, were considered good candidates for a fixed-dose combination product that could be administered as a single pill once daily (qd), thereby simplifying existing treatment regimens and promoting patient adherence. As both drugs are extens...

journal_title：Journal of clinical pharmacology

authors： Blum MR,Chittick GE,Begley JA,Zong J

更新日期：2007-06-01 00:00:00

abstract：:The incidence of migraine is higher among women than men and peaks during the reproductive years, when contraceptive medication use is common. Atogepant, a potent, selective antagonist of the calcitonin gene-related peptide receptor-in development for migraine prevention-is thus likely to be used by women taking oral ...

journal_title：Journal of clinical pharmacology

authors： Ankrom W,Xu J,Vallee MH,Dockendorf MF,Armas D,Boinpally R,Min KC

更新日期：2020-09-01 00:00:00

abstract：:The effect of epoprostenol on the pharmacokinetics of furosemide was investigated in 23 patients with end-stage congestive heart failure (CHF) receiving conventional therapy alone or conventional therapy plus epoprostenol. Estimates of the apparent oral clearance, volume of distribution, and absorption rate constant f...

journal_title：Journal of clinical pharmacology

authors： Carlton LD,Patterson JH,Mattson CN,Schmith VD

更新日期：1996-03-01 00:00:00

abstract：:Comparative pharmacokinetics of vitamin K epoxide reductase antagonists tecarfarin and warfarin were assessed before and after coadministration for 21 days of the CYP450 inhibitor fluconazole in a randomized, open-label, single-center drug interaction study. Twenty healthy adult participants were randomized 1:1 to rec...

journal_title：Journal of clinical pharmacology

authors： Bavisotto LM,Ellis DJ,Milner PG,Combs DL,Irwin I,Canafax DM

更新日期：2011-04-01 00:00:00

abstract：:Fifteen healthy women participated in a study to determine the effect of multiple doses of troglitazone on the pharmacokinetics of Ortho-Novum 1/35 (35 micrograms ethinyl estradiol [EE] and 1 mg norethindrone [NE]). Participants received three cycles (21 days each of active drug followed by 7 days without medication) ...

journal_title：Journal of clinical pharmacology

authors： Loi CM,Stern R,Koup JR,Vassos AB,Knowlton P,Sedman AJ

更新日期：1999-04-01 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：:The efficacy of intravenously administered metoprolol, a cardioselective beta-adrenergic blocking agent, was evaluated in the treatment of supraventricular tachyarrhythmias in 16 patients. The arrhythmias that were treated were atrial fibrillation (11 patients), atrial flutter (2 patients), supraventricular tachycardi...

journal_title：Journal of clinical pharmacology

authors： Amsterdam EA,Kulcyski J,Ridgeway MG

更新日期：1991-08-01 00:00:00

abstract：:A single evening dose of a clonidine-chlorthalidone combination (Combipres) was compared with the usual twice-daily schedule in 11 patients with essential hypertension. No significant difference was found between the blood pressures recorded on the two regimens or between morning and afternoon pressures on the once-da...

journal_title：Journal of clinical pharmacology

authors： Grossman SH,Gunnells JC

更新日期：1980-04-01 00:00:00

abstract：:Ixekizumab (LY2439821), a humanized immunoglobulin G subclass 4 (IgG4) monoclonal antibody that selectively binds and neutralizes interleukin (IL) 17A has demonstrated efficacy in the treatment of psoriasis. A population pharmacokinetics-pharmacodynamics model was developed using NONMEM 7.2 to describe the temporal re...

journal_title：Journal of clinical pharmacology

authors： Tham LS,Tang CC,Choi SL,Satterwhite JH,Cameron GS,Banerjee S

更新日期：2014-10-01 00:00:00

abstract：:A number of herbal preparations have been shown to interact with prescription medications secondary to modulation of cytochrome P450 (CYP) and/or P-glycoprotein (P-gp). The purpose of this study was to determine the influence of Panax ginseng on CYP3A and P-gp function using the probe substrates midazolam and fexofena...

journal_title：Journal of clinical pharmacology

authors： Malati CY,Robertson SM,Hunt JD,Chairez C,Alfaro RM,Kovacs JA,Penzak SR

更新日期：2012-06-01 00:00:00

abstract：:Nine healthy subjects received 400 mg sodium valproate orally in the fasting state. Binding parameters of valproic acid to serum proteins were determined by Scatchard analysis for individual series of valproic acid data. Total and unbound (intrinsic) clearances (CLt and CLu) were calculated by dividing the dose by the...

journal_title：Journal of clinical pharmacology

authors： Kodama Y,Tsutsumi K,Teraoka I,Fujii I,Takeyama M

更新日期：1993-02-01 00:00:00

abstract：:The authors examined the pharmacokinetics of the CD19 receptor-directed tyrosine kinase inhibitor B43-Genistein in 17 patients (4 children, 13 adults) with B-lineage lymphoid malignancies, including 12 patients with acute lymphoblastic leukemia (ALL) and 5 patients with non-Hodgkin's lymphoma (NHL). The immunoconjugat...

journal_title：Journal of clinical pharmacology

authors： Chen CL,Levine A,Rao A,O'Neill K,Messinger Y,Myers DE,Goldman F,Hurvitz C,Casper JT,Uckun FM

更新日期：1999-12-01 00:00:00

abstract：:To determine the elimination of high-molecular-weight hydroxyethyl starch (HES, Mw 450,000) in normal subjects, ten volunteers were given 500 ml 6% HES solution by intravenous infusion, and serial blood and urine samples were collected for nonglucose total carbohydrate determination. On the average, 46 and 64 per cent...

journal_title：Journal of clinical pharmacology

authors： Yacobi A,Stoll RG,Sum CY,Lai CM,Gupta SD,Hulse JD

更新日期：1982-04-01 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：:The most recent International Conference on Harmonisation E14 Q&A document states that a separate positive control would not be necessary provided sufficiently high exposures are achieved in the early-phase studies. Realistically, a phase 1 study is unlikely to include a pharmacological positive control, and in cases ...

journal_title：Journal of clinical pharmacology

authors： Ferber G,Fernandes S,Täubel J

更新日期：2018-01-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit cyclooxygenase-1 (COX-1), thereby inhibiting platelet function via blockade of thromboxane A2 (TxA2) formation, and COX-2, the enzyme that mediates inflammatory responses. Meloxicam is a relatively COX-2-selective anti-arthritis drug that shows significant TxA2 inh...

journal_title：Journal of clinical pharmacology

authors： Rinder HM,Tracey JB,Souhrada M,Wang C,Gagnier RP,Wood CC

更新日期：2002-08-01 00:00:00

abstract：:Mavrilimumab is a fully human monoclonal antibody that binds to granulocyte-macrophage colony stimulating factor receptor α (GM-CSFRα) with high affinity and specificity and has potential application in various inflammatory diseases. The objective of this investigation was to develop a mechanistic population model to ...

journal_title：Journal of clinical pharmacology

authors： Wang B,Lau YY,Liang M,Vainshtein I,Zusmanovich M,Lu H,Magrini F,Sleeman M,Roskos L

更新日期：2012-08-01 00:00:00

abstract：:This was a preliminary feasibility study to assess the pharmacokinetics and acute safety of a single dose of orally inhaled testosterone via the AERx system, a novel handheld aerosol delivery system in postmenopausal women. Twelve postmenopausal women stabilized on oral estrogen therapy were treated with a single dose...

journal_title：Journal of clinical pharmacology

authors： Davison S,Thipphawong J,Blanchard J,Liu K,Morishige R,Gonda I,Okikawa J,Adams J,Evans A,Otulana B,Davis S

更新日期：2005-02-01 00:00:00

abstract：:The cytochromes P450 (CYPs) constitute a superfamily of hemoprotein enzymes that are responsible for the biotransformation of numerous xenobiotics, including therapeutic agents. Studies of the biochemical and enzymatic properties of these enzymes and their molecular genetics and regulation of gene expression and activ...

journal_title：Journal of clinical pharmacology

authors： Venkatakrishnan K,Von Moltke LL,Greenblatt DJ

更新日期：2001-11-01 00:00:00

abstract：:A population pharmacokinetic (PPK) model of pomalidomide was developed and the influence of demographic and disease-related covariates on PPK parameters was assessed based on data from 6 clinical trials of pomalidomide (dose range, 0.5-10 mg) in healthy participants (n = 96) and patients with multiple myeloma (MM; n =...

journal_title：Journal of clinical pharmacology

authors： Li Y,Xu Y,Liu L,Wang X,Palmisano M,Zhou S

更新日期：2015-05-01 00:00:00

abstract：:MC4-NN2-0453 is a novel, long-acting, selective, melanocortin-4-receptor agonist developed for treatment of obesity. This first-human-dose, randomized, double-blind, placebo-controlled trial investigated the safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple doses of MC4-NN2-0453 in ov...

journal_title：Journal of clinical pharmacology

authors： Royalty JE,Konradsen G,Eskerod O,Wulff BS,Hansen BS

更新日期：2014-04-01 00:00:00

abstract：:The hydrochlorothiazide component of Maxzide (Lederle Laboratories, Pearl River, NY) has been shown to be more bioavailable than the hydrochlorothiazide component of Dyazide (Smith, Kline and French Laboratories, Philadelphia, PA). The authors compared the antihypertensive effectiveness of a half-tablet of Maxzide (25...

journal_title：Journal of clinical pharmacology

authors： Casner PR,Dillon KR

更新日期：1990-08-01 00:00:00

abstract：:The absolute bioavailability of oral melatonin tablets was studied in 12 normal healthy volunteers. Subjects were administered, in a randomized crossover fashion, melatonin 2 mg intravenously and 2 and 4 mg orally. Blood was sampled over approximately eight (estimated) half-lives. Both the 2 and the 4 mg oral dosages ...

journal_title：Journal of clinical pharmacology

authors： DeMuro RL,Nafziger AN,Blask DE,Menhinick AM,Bertino JS Jr

更新日期：2000-07-01 00:00:00

abstract：:The effect of food on the oral bioavailability of sustained-release morphine sulfate tablets (ORAMORPH SR; Roxane Laboratories, Inc., Columbus, OH; OSR) was examined in an open-label, randomized, two-period crossover study. Healthy male volunteers received a 30-mg OSR tablet orally every 12 hours for seven doses durin...

journal_title：Journal of clinical pharmacology

authors： Bass J,Shepard KV,Lee JW,Hulse J

更新日期：1992-11-01 00:00:00

abstract：:CGS 13080, a selective thromboxane synthetase inhibitor, was given intravenously (0.6 mg/kg over 6 hours) to eight hypertensive (diastolic 95-115 mm Hg) euvolemic caucasian females on their customary salt intake (24 hour urine Na: 142.9 +/- 14.8 meq). No change occurred in blood pressure or glomerular filtration rate ...

journal_title：Journal of clinical pharmacology

authors： Weir MR,Klassen DK,Hoover N,Douglas FL

更新日期：1989-12-01 00:00:00

abstract：:This study examined warfarin usage for elderly Medicare beneficiaries with atrial fibrillation (AF) who suffered traumatic brain injury (TBI), hip fracture, or torso injuries. Using the 5% Chronic Condition Data Warehouse administrative claims data, this study included fee-for-service Medicare beneficiaries who had a ...

journal_title：Journal of clinical pharmacology

authors： Liu X,Baumgarten M,Smith G,Gambert S,Gottlieb S,Rattinger G,Albrecht J,Langenberg P,Zuckerman I

更新日期：2015-01-01 00:00:00

abstract：:Approximately equianalgesic oral doses of codeine, an oxycodone compound resembling Percodan, and pentazocine were compared for adverse effects in a double-blind, randomized study of four doses of each drug given over two days to 247 postsurgical patients with pain. Placebo and parenteral morphine were also treated as...

journal_title：Journal of clinical pharmacology

authors： Kantor TG,Hopper M,Laska E

更新日期：1981-01-01 00:00:00