A novel CRTH2 antagonist: Single- and multiple-dose tolerability, pharmacokinetics, and pharmacodynamics of ACT-453859 in healthy subjects.

abstract：:The objective of this study was to establish effects of inhaled loxapine on the QTc interval in this randomized, placebo-controlled, double-blind crossover study. Forty-eight healthy volunteers received a single inhaled placebo or 10 mg loxapine. Plasma concentrations of loxapine increased with a median Tmax of 1 minu...

journal_title：Journal of clinical pharmacology

authors： Spyker DA,Voloshko P,Heyman ER,Cassella JV

更新日期：2014-06-01 00:00:00

abstract：:Sirolimus (RAPA) and cyclosporine (CsA) are immunosuppressive compounds that are being used concomitantly in renal transplant patients. Both drugs are dosed orally, have common intestinal and hepatic metabolism and intestinal transport mechanisms, and thus offer potential for pharmacokinetic drug interactions. A singl...

journal_title：Journal of clinical pharmacology

authors： Zimmerman JJ,Harper D,Getsy J,Jusko WJ

更新日期：2003-10-01 00:00:00

abstract：:The bioavailability and pharmacokinetics of dilevalol following oral and intravenous administration were investigated in 12 healthy male volunteers. Dilevalol HCl was administered as a 200-mg oral tablet and a 50-mg intravenous infusion using a randomized cross-over design. Blood and urine samples were collected over ...

journal_title：Journal of clinical pharmacology

authors： Kramer WG,Nagabhushan N,Affrime MB,Perentesis GP,Symchowicz S,Patrick JE

更新日期：1988-07-01 00:00:00

abstract：:The population pharmacokinetic (PK) profile of oral clonidine was characterized in newborns with neonatal abstinence syndrome, and significant covariates affecting its PK parameters were identified. Plasma clonidine concentration data were obtained from a clinical trial in which 36 newborns, aged 1 to 25 days (postnat...

journal_title：Journal of clinical pharmacology

authors： Xie HG,Cao YJ,Gauda EB,Agthe AG,Hendrix CW,Lee H

更新日期：2011-04-01 00:00:00

abstract：:Transporters play an important role in drug absorption, disposition, and drug action. The evaluation of drug transporters requires a comprehensive understanding of transporter biology and pharmacology. Physiologically based pharmacokinetic (PBPK) models may offer an integrative platform to quantitatively evaluate the ...

journal_title：Journal of clinical pharmacology

authors： Pan Y,Hsu V,Grimstein M,Zhang L,Arya V,Sinha V,Grillo JA,Zhao P

更新日期：2016-07-01 00:00:00

abstract：:Twelve patients chronically maintained on warfarin were administered 80 mg atorvastatin for 2 weeks. Mean prothrombin times decreased slightly, but only for the first few days of the two-week treatment period. Thus atorvastatin had no consistent effect on the anticoagulant activity of warfarin and adjustment in warfar...

journal_title：Journal of clinical pharmacology

authors： Stern R,Abel R,Gibson GL,Besserer J

更新日期：1997-11-01 00:00:00

abstract：:Antinociception by nonsteroidal antiinflammatory drugs, notably diclofenac and S(+)-ibuprofen, has traditionally been attributed to peripheral tissue cyclooxygenase inhibition. This study investigates the potential role of the nitric oxide system for the central antinociceptive effects of diclofenac, S(+)-, and R(-)-i...

journal_title：Journal of clinical pharmacology

authors： Björkman R,Hallman KM,Hedner J,Hedner T,Henning M

更新日期：1996-12-01 00:00:00

abstract：:The effects of graded doses of anisotropine methylbromide on nocturanl gastric secretion were investigated in a double-blind crossover study in man. Single doses considerably higher than those usually employed for daytime use in adjunctive therapy of peptic ulcer disease significantly reduced acid secretion without si...

journal_title：Journal of clinical pharmacology

authors： Freston JW,Forbes JA

更新日期：1977-01-01 00:00:00

abstract：:The impact of a microgravity simulation using a head-down tilt (-6 degrees) on lidocaine pharmacokinetics used as a probe to evaluate hepatic blood flow is discussed. Eight healthy male subjects were selected for a 7-day study, including a 4-day head-down tilt from day 2 to day 5. Subjects were given 1 mg/kg of lidoca...

journal_title：Journal of clinical pharmacology

authors： Saivin S,Pavy-Le Traon A,Cornac A,Güell A,Houin G

更新日期：1995-07-01 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：:Coronary heart disease, hypertension, and dyslipidemia are highly prevalent and commonly coexist in people who are middle-aged and older. Previous data suggested that lowering cholesterol concentrations in individuals at high risk of cardiovascular disease improved clinical outcomes. Xuezhikang, a partial extract of r...

journal_title：Journal of clinical pharmacology

authors： Li JJ,Lu ZL,Kou WR,Chen Z,Wu YF,Yu XH,Zhao YC,Chinese Coronary Secondary Prevention Study Group.

更新日期：2009-08-01 00:00:00

abstract：:Controlled-onset extended-release verapamil (COER-V) is designed so drug concentrations rise sharply in the early morning to coincide with the peak incidence of cardiovascular events. The primary objective of this study was to compare the diurnal pattern of forearm vascular resistance (FVR) between hypertensives and n...

journal_title：Journal of clinical pharmacology

authors： Nguyen BN,Parker RB,Noujedehi M,Sullivan JM,Johnson JA

更新日期：2000-12-01 00:00:00

abstract：:In a double-blind sequential trial, the influence of transdermal electrical nerve stimulation (TENS) was studied in patients who were treated with total infusions of metoclopramide 3.5 mg/kg to counter the emetic action of cisplatin 60-90 mg/m2. Transdermal electrical nerve stimulation further reduced the emetic episo...

journal_title：Journal of clinical pharmacology

authors： Saller R,Hellenbrecht D,Bühring M,Hess H

更新日期：1986-02-01 00:00:00

abstract：:Avibactam is a non-β-lactam β-lactamase inhibitor intended for use as a fixed-dose combination with ceftazidime for the treatment of certain serious Gram-negative infections. As avibactam is primarily excreted unchanged in the urine, renal impairment may affect its pharmacokinetics. This phase 1 study investigated the...

journal_title：Journal of clinical pharmacology

authors： Merdjan H,Tarral A,Das S,Li J

更新日期：2017-02-01 00:00:00

abstract：:An open-label study evaluated the effect of steady-state venlafaxine on the single-dose pharmacokinetic profile of risperidone, a CYP2D6 substrate; its active metabolite, 9-hydroxyrisperidone; and the total active moiety (risperidone plus 9-hydroxyrisperidone). Thirty healthy subjects received a 1 mg oral dose of risp...

journal_title：Journal of clinical pharmacology

authors： Amchin J,Zarycranski W,Taylor KP,Albano D,Klockowski PM

更新日期：1999-03-01 00:00:00

abstract：:The effect of lovastatin given before percutaneous coronary angioplasty (PTCA) on early restenosis was investigated in men with mild to moderate hypercholesterolemia. Thirty-four hypercholesterolemic patients (serum LDL cholesterol 130-200 mg/dL) undergoing their first PTCA completed a 6-month prospective, double-blin...

journal_title：Journal of clinical pharmacology

authors： Beigel Y,Zafrir N,Teplitzky Y,Neuman Y,Gavish D,Wurzel M,Fainaru M

更新日期：1995-06-01 00:00:00

abstract：:Supine office blood pressures (SOBP) and 24-hour automated ambulatory blood pressure monitorings (AABPM) showed blood pressure reductions from a stable baseline to active treatment with 120-, 240-, and 480-mg doses of a new verapamil QD capsule (solid-spheroidal-oral once-daily drug-absorption system: (SODAS) in patie...

journal_title：Journal of clinical pharmacology

authors： Carr AA,Bottini PB,Prisant LM,Fisher LD,Devane JG,O'Brien DE,Rhoades RB

更新日期：1991-02-01 00:00:00

abstract：:Gestational diabetes mellitus (GDM) has affected a great number of pregnant women worldwide. Artemisia extracts have been found to exhibit a potent antidiabetic effect in the treatment of type 2 diabetes mellitus. We aimed to examine the effects of Artemisia extract on insulin resistance and lipid profiles in pregnant...

journal_title：Journal of clinical pharmacology

authors： Sun X,Sun H,Zhang J,Ji X

更新日期：2016-12-01 00:00:00

abstract：:Four protease inhibitor antiviral agents (ritonavir, indinavir, nelfinavir, saquinavir) were evaluated as in vitro inhibitors of the activity of six human cytochromes using an in vitro model based on human liver microsomes. Ritonavir was a highly potent inhibitor of P450-3A activity (triazolam hydroxylation), having i...

journal_title：Journal of clinical pharmacology

authors： von Moltke LL,Greenblatt DJ,Grassi JM,Granda BW,Duan SX,Fogelman SM,Daily JP,Harmatz JS,Shader RI

更新日期：1998-02-01 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：:This experiment represents the first time that it has been possible to measure a body fluid compartment by direct means during spaceflight. Based on the results observed in the five crewmen in this study, it is concluded that TBW decreases by 3.4% after 1 to 3 days of exposure to microgravity in the Space Shuttle. Som...

journal_title：Journal of clinical pharmacology

authors： Leach CS,Inners LD,Charles JB

更新日期：1991-10-01 00:00:00

abstract：:Inhaled glucocorticoids induce therapeutic and adverse systemic effects via the same types of receptors. Analysis of the pharmacokinetic/pharmacodynamic parameters of inhaled glucocorticoids generates a risk-benefit value (RBV). Targeted efficacy with minimal adverse effects helps to quantify an appropriate RBV. High ...

journal_title：Journal of clinical pharmacology

authors： Rohatagi S,Appajosyula S,Derendorf H,Szefler S,Nave R,Zech K,Banerji D

更新日期：2004-01-01 00:00:00

abstract：:ABT-761 is a second-generation 5-lipoxygenase inhibitor in clinical development for the treatment of asthma. The effects of ABT-761 on the pharmacokinetics of an oral contraceptive were assessed in 21 female adult volunteers in a phase I, multiple-dose, open-label study. Subjects received a single dose of oral contrac...

journal_title：Journal of clinical pharmacology

authors： Wong SL,O'Dea RF,Dube LM,Awni WM

更新日期：1998-07-01 00:00:00

abstract：:The anxiolytic triazolobenzodiazepine alprazolam was administered to six male patients, aged 26 to 46 years, with panic disorder or agoraphobia (with panic attacks) to assess clinical effects and steady-state pharmacokinetics following multiple dosing at three levels: 3.0 mg/d, 6.0 mg/d, and 9.0 mg/d. Multiple-dose ki...

journal_title：Journal of clinical pharmacology

authors： Ciraulo DA,Barnhill JG,Boxenbaum HG,Greenblatt DJ,Smith RB

更新日期：1986-04-01 00:00:00

abstract：:The aim of this study was to investigate if the concomitant administration of the positive inotropic drug enoximone (100 mg tid) has any effect on the morning through levels of the cardiac glycoside digoxin in 17 patients with congestive heart failure (NYHA II-IV). Plasma concentrations of digoxin were 1.05 +/- 0.37 n...

journal_title：Journal of clinical pharmacology

authors： Trenk D,Hertrich F,Winkelmann B,Glauner T,Dieterich HA,Jähnchen E

更新日期：1990-03-01 00:00:00

abstract：:Because of the key role blood viscosity plays in the regulation of blood pressure (BP) and the hemorheological effects of pentoxifylline (PTX), this study was conducted to evaluate whether PTX can reduce BP when added to captopril in patients with stage 1 hypertension. In this randomized clinical trial 62 patients wit...

journal_title：Journal of clinical pharmacology

authors： Namdar H,Khani E,Pourrashid MH,Entezari-Maleki T

更新日期：2020-02-01 00:00:00

abstract：:The authors evaluated the effect of high-dose aspirin at a therapeutic dose, using chlorzoxazone as a probe for CYP2E1 enzyme activity. In a randomized, open-label, 2-way crossover study, 10 healthy men were treated 3 times daily for 6 days with 1 g aspirin or placebo. On day 7, 1 dose of 400 mg chlorzoxazone was admi...

journal_title：Journal of clinical pharmacology

authors： Park JY,Kim KA,Park PW,Ha JM

更新日期：2006-01-01 00:00:00

abstract：:Neutropenia is the most commonly reported hematologic toxicity following treatment with palbociclib, a cyclin-dependent kinase 4/6 inhibitor approved for metastatic breast cancer. Using data from 185 advanced cancer patients receiving palbociclib in 3 clinical trials, a pharmacokinetic-pharmacodynamic model was develo...

journal_title：Journal of clinical pharmacology

authors： Sun W,O'Dwyer PJ,Finn RS,Ruiz-Garcia A,Shapiro GI,Schwartz GK,DeMichele A,Wang D

更新日期：2017-09-01 00:00:00

abstract：:BIA 10-2474 (a fatty acid amide hydrolase inhibitor) was evaluated in a first-in-human phase 1 study in normal volunteers to assess safety/tolerability, pharmacokinetics, pharmacodynamics, and food effect. The dose-escalation process consisted of a single-ascending-dose phase (SAD) and multiple-ascending-dose phase (M...

journal_title：Journal of clinical pharmacology

authors： Chaikin P

更新日期：2017-06-01 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