The importance of stereochemistry in drug action and disposition.

abstract：:The need for clinical pharmacology in research and education, drug development, and health care delivery is well known. However, a current profile of those working in the field is not available. The ACCP authorized a survey of clinical pharmacologists to provide such a profile. Members of the ACCP or ASCPT were solici...

journal_title：Journal of clinical pharmacology

authors： Wilson JT,Brown RD,Kimura KK,Whelton A

更新日期：1989-08-01 00:00:00

abstract：:Anisotropine methyl bromide, an anticholinergic, 80 mg given orally at 8 P.M., suppresses gastric acid secretion through the night without significant side effects. Thirty patients with endoscopy-proved symptomatic duodenal ulcer disease completed a randomized, double-blind, placebo-controlled trial of nighttime aniso...

journal_title：Journal of clinical pharmacology

authors： Bowers JH,Forbes JA,Freston JW

更新日期：1978-07-01 00:00:00

abstract：:Acute asthma exacerbations are primarily due to airway inflammation and remain one of the most frequent reasons for childhood hospitalizations. Although systemic corticosteroids remain the mainstay of therapy because of their anti-inflammatory properties, not all inflammatory pathways are responsive to systemic cortic...

journal_title：Journal of clinical pharmacology

authors： Arnold DH,Van Driest SL,Reiss TF,King JC,Akers WS

更新日期：2021-03-01 00:00:00

abstract：:The efficacy and tolerability of aminoglutethimide for the treatment of Cushing's syndrome was assessed in 66 cases three of which are described in the present paper. Aminoglutethimide provided palliation from the signs and symptoms of hypercorticism in 13 of 21 patients with metastatic adrenocortical carcinoma and fo...

journal_title：Journal of clinical pharmacology

authors： Misbin RI,Canary J,Willard D

更新日期：1976-11-01 00:00:00

abstract：:The pharmacokinetics and pharmacodynamics of ranitidine were studied in 13 term neonates with stable renal and hepatic function who were treated with extracorporeal membrane oxygenation (ECMO). Ranitidine was initially administered as a single 2 mg/kg dose over 10 minutes and intragastric pH was monitored to determine...

journal_title：Journal of clinical pharmacology

authors： Wells TG,Heulitt MJ,Taylor BJ,Fasules JW,Kearns GL

更新日期：1998-05-01 00:00:00

abstract：:Consumption of typical quantities of grapefruit juice (GFJ) increases the oral bioavailability of several CYP3A4 substrates without affecting their elimination, consistent with selective inhibition of intestinal but not hepatic CYP3A4. However, increases in the AUCs of CYP3A4 substrates recently associated with the co...

journal_title：Journal of clinical pharmacology

authors： Veronese ML,Gillen LP,Burke JP,Dorval EP,Hauck WW,Pequignot E,Waldman SA,Greenberg HE

更新日期：2003-08-01 00:00:00

abstract：:A double-blind, placebo-controlled, multiple oral dose escalation study was conducted to investigate the pharmacokinetics, safety, and tolerability of entecavir in healthy subjects. Eight subjects were assigned to each of the 3 dose panels (0.1 mg, 0.5 mg, and 1 mg or matched placebo once daily for 14 days). Blood and...

journal_title：Journal of clinical pharmacology

authors： Yan JH,Bifano M,Olsen S,Smith RA,Zhang D,Grasela DM,LaCreta F

更新日期：2006-11-01 00:00:00

abstract：:Cyclophosphamide-based regimens are front-line treatment for numerous pediatric malignancies; however, current dosing methods result in considerable interpatient variability in tumor response and toxicity. In this pediatric population, the authors' objectives were (1) to quantify and explain the pharmacokinetic variab...

journal_title：Journal of clinical pharmacology

authors： McCune JS,Salinger DH,Vicini P,Oglesby C,Blough DK,Park JR

更新日期：2009-01-01 00:00:00

abstract：:The primary objective of this study was to identify intravenous regimens of tipifarnib that would mimic the systemic exposure obtained after the current twice-daily oral administration of tipifarnib. After determination of an intravenous dose that 6 subjects with advanced cancer could tolerate, another 26 subjects wer...

journal_title：Journal of clinical pharmacology

authors： Zhang S,Zannikos P,Awada A,Piccart-Gebhart M,Dirix LY,Fumoleau P,Verhaeghe T,Francois M,De Porre P

更新日期：2006-10-01 00:00:00

abstract：:This study assessed the efficacy and safety of ketoprofen patch compared with placebo in patients who had rheumatoid arthritis and persistent wrist pain. Patients (N = 676)who had achieved systemic disease control with a disease-modifying antirheumatic drug and/or systemic corticosteroid, but still had persistent wris...

journal_title：Journal of clinical pharmacology

authors： Kawai S,Uchida E,Kondo M,Ohno S,Obata J,Nawata Y,Sugimoto K,Oribe M,Nagaya I

更新日期：2010-10-01 00:00:00

abstract：:The search for effective treatments of Alzheimer's disease (AD) is one of the major challenges facing modern medicine. Acetylcholinesterase (AChE) inhibitors (AChEIs) are effective for the treatment of mild to moderate AD, and memantine, an N-methyl-D-aspartate (NMDA) inhibitor, has been approved for moderate to sever...

journal_title：Journal of clinical pharmacology

authors： Geerts H,Grossberg GT

更新日期：2006-07-01 00:00:00

abstract：:Heparin-induced thrombocytopenia (HIT) is a high-risk adverse drug reaction because of its associated risk of life- and limb-threatening thrombosis. Rivaroxaban may be considered as an ideal nonheparin anticoagulant alternative for the management of HIT. In this preliminary retrospective study, the efficacy and safety...

journal_title：Journal of clinical pharmacology

authors： Farasatinasab M,Zarei B,Moghtadaei M,Nasiripour S,Ansarinejad N,Zarei M

更新日期：2020-10-01 00:00:00

abstract：:Varenicline is a novel selective α4β2 nicotinic acetylcholine partial agonist developed for smoking cessation. Single- and multiple dose studies were conducted to investigate pharmacokinetics, safety, and tolerability of varenicline in healthy male Japanese smokers. The single-dose study was conducted as a double-blin...

journal_title：Journal of clinical pharmacology

authors： Kikkawa H,Maruyama N,Fujimoto Y,Hasunuma T

更新日期：2011-04-01 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：:The effects of Zataria multiflora on clinical symptoms, pulmonary function tests, oxidative stress, and C-reactive protein levels in chronic obstructive pulmonary disease (COPD) patients were evaluated. Forty-five patients were allocated to 3 groups: placebo group and 2 groups that received 3 and 6 mg/kg/day Z. multif...

journal_title：Journal of clinical pharmacology

authors： Ghorani V,Rajabi O,Mirsadraee M,Rezaeitalab F,Saadat S,Boskabady MH

更新日期：2020-07-01 00:00:00

abstract：:Etoricoxib is a potent selective COX-2 inhibitor in man. Ex vivo whole-blood assays assessed COX-2 inhibition after oral administration of etoricoxib in single (5-500 mg) and multiple (25-150 mg) once-daily doses to healthy human subjects. A separate study examined ex vivo gastric mucosal PGE2 synthesis after etoricox...

journal_title：Journal of clinical pharmacology

authors： Dallob A,Hawkey CJ,Greenberg H,Wight N,De Schepper P,Waldman S,Wong P,DeTora L,Gertz B,Agrawal N,Wagner J,Gottesdiener K

更新日期：2003-06-01 00:00:00

abstract：:A selective thromboxane (TX) synthase inhibitor, CS-518, was orally administered to healthy male Japanese volunteers and the pharmacokinetic and pharmacodynamic properties were investigated. The time profile of drug concentrations in plasma was determined, and the effects of the drug on platelet aggregation in plasma ...

journal_title：Journal of clinical pharmacology

authors： Uematsu T,Nagashima S,Inaba H,Mizuno A,Kosuge K,Nakashima M

更新日期：1994-01-01 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：:To test the effects of fluvastatin on low-density lipoprotein (LDL) receptor activity in patients with heterozygous familial hypercholesterolemia, the authors measured LDL receptor activity in stimulated T-lymphocytes prepared from 34 patients before and after treatment with 40 mg fluvastatin daily for 12 weeks. Maxim...

journal_title：Journal of clinical pharmacology

authors： Raungaard B,Brorholt-Petersen JU,Jensen HK,Faergeman O

更新日期：2000-04-01 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：:Forty-two healthy Caucasian subjects were randomized in a double-blind, parallel three-group study (14 subjects per group) to investigate potential electrocardiographic and pharmacokinetic interactions between the antimalarials artemether-lumefantrine (six-dose regimen of Riamet over 3 days) and quinine (2-h intraveno...

journal_title：Journal of clinical pharmacology

authors： Lefèvre G,Carpenter P,Souppart C,Schmidli H,Martin JM,Lane A,Ward C,Amakye D

更新日期：2002-10-01 00:00:00

abstract：:HMR1031 is a potent and specific antagonist of the integrin VLA-4 (alpha4beta1) binding to vascular cell adhesion molecule-1 (VCAM-1) and fibronectin. HMR1031 is an inhaled drug being developed for the treatment of asthma using an Ultrahaler dry-powder inhalation device. A pharmacoscintigraphic study of HMR1031 sugges...

journal_title：Journal of clinical pharmacology

authors： Shah B,Jensen BK,Zhang J,Hunt T,Rohatagi S

更新日期：2003-12-01 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：:We administered 0.5-and 1.0-mg doses of bumetanide intravenously to eight normal subjects with and without pretreatment with probenecid. Probenecid did not effect either the cumulative response or the time course of response of bumetanide. These results are in contrast to results reported in dogs but consistent with s...

journal_title：Journal of clinical pharmacology

authors： Brater DC,Chennavasin P

更新日期：1981-07-01 00:00:00

abstract：:The pharmacokinetics (PK), pharmacodynamics (PD), and safety of a platelet GPIIb/IIIa receptor antagonist, RGD891, and its active metabolite, RGD039, were evaluated after administration of various intravenous regimens of RGD891 to healthy male volunteers in two Phase I studies. Plasma and urine concentrations of RGD89...

journal_title：Journal of clinical pharmacology

authors： Zannikos PN,Rohatagi S,Jensen BK,DePhillips SL,Massignon D,Calic F,Sibille M,Kirkesseli S

更新日期：2000-11-01 00:00:00

abstract：:The most thorough and clinically relevant approach to hypnotic drug evaluation is one that balances the strengths and weaknesses of clinical trials and sleep laboratory evaluations. Advantages of clinical trials include the ability to evaluate large numbers of subjects and specific target groups and to thoroughly asse...

journal_title：Journal of clinical pharmacology

authors： Kales A,Scharf MB,Soldatos CR,Bixler EO

更新日期：1979-07-01 00:00:00

abstract：:The effect of 6% hydroxyethyl starch (hetastarch) and 5% human serum albumin (albumin) infusion on coagulation in 12 patients with septic shock was evaluated. Patients were randomly assigned to receive either albumin (N = 6) or hetastarch (N = 6) infusion over a 24-hour study interval. The prothrombin time (PT), parti...

journal_title：Journal of clinical pharmacology

authors： Falk JL,Rackow EC,Astiz ME,Weil MH

更新日期：1988-05-01 00:00:00

abstract：:The pharmacokinetics of enoximone and its sulfoxide metabolite were determined following administration of a single oral dose of 1 or 2 mg/kg in seven patients with congestive heart failure, and in two normal volunteers following a single 75-mg capsule, and were compared to those published previously. Plasma concentra...

journal_title：Journal of clinical pharmacology

authors： Lima JJ,Leier CV,Holtz L,Sterechele J,Shields BJ,MacKichan JJ

更新日期：1987-09-01 00:00:00

abstract：:The objective of this study was to determine the absolute oral bioavailability and disposition of omapatrilat. This single-dose, randomized, crossover study of 20 mg intravenous and 50 mg oral [14C]omapatrilat was conducted in 12 healthy male subjects to determine the disposition and oral bioavailability of omapatrila...

journal_title：Journal of clinical pharmacology

authors： Malhotra BK,Iyer RA,Soucek KM,Behr D,Liao WC,Mitroka JG,Kaul S,Cohen MB,Knupp CA

更新日期：2001-08-01 00:00:00

abstract：:Propiverine extended release is expected to be better tolerated compared to immediate release tablets because of slower drug release and reduced formation of active metabolites in the colon. CYP3A4 and ABCC2, the major variables in pharmacokinetics of propiverine, are less expressed in the colon. Therefore, dispositio...

journal_title：Journal of clinical pharmacology

authors： May K,Westphal K,Giessmann T,Wegner D,Adam U,Lerch MM,Oertel R,Warzok RW,Weitschies W,Braeter M,Siegmund W

更新日期：2008-05-01 00:00:00