Drug-binding cavities in long-lived biologics: cause for concern but also potential benefit.

abstract：:In this study, the authors assessed the bioequivalence of two fluoxetine tablet formulations in 24 healthy volunteers of both sexes who received a single 20 mg dose of each fluoxetine formulation, and a new sensitive method for the quantification of fluoxetine and norfluoxetine in human plasma was developed. The study...

journal_title：Journal of clinical pharmacology

authors： Moraes MO,Lerner FE,Corso G,Bezerra FA,Moraes ME,De Nucci G

更新日期：1999-10-01 00:00:00

abstract：:In the analysis of longitudinal pharmacokinetic data, both balanced (equal number of samples per subject) and unbalanced data are used. It is implicitly assumed that the process that caused the missing data can be ignored. A simulation study was performed to determine the effect of ignoring the missing data (i.e., "ig...

journal_title：Journal of clinical pharmacology

authors： Ette EI,Sun H,Ludden TM

更新日期：1998-03-01 00:00:00

abstract：:Pharmacokinetic values of cibenzoline, a new, investigational, antiarrhythmic drug, were determined in 13 patients with varying degree of renal impairment, creatinine clearance range between 5 and 53 mL/min. Cibenzoline plasma levels were measured after direct intravenous injection of one single 1 mg/kg dose. The appa...

journal_title：Journal of clinical pharmacology

authors： Canal M,Flouvat B,Aubert P,Guedon J,Prinseau J,Baglin A

更新日期：1985-04-01 00:00:00

abstract：:Alkamides are suspected to contribute to the activity of Echinacea preparations. They are mainly derived from undeca- and dodecanoic acid and differ in the degree of unsaturation and the configuration of the double bonds. In total, 6 alkamides have been isolated from the roots of Echinacea angustifolia as major lipoph...

journal_title：Journal of clinical pharmacology

authors： Woelkart K,Koidl C,Grisold A,Gangemi JD,Turner RB,Marth E,Bauer R

更新日期：2005-06-01 00:00:00

abstract：:Repaglinide is a novel insulin secretagogue developed in response to the need for a fast-acting, oral prandial glucose regulator for the treatment of type 2 (non-insulin-dependent) diabetes mellitus. Repaglinide is metabolized mainly in the liver; its pharmacokinetics may therefore be altered by hepatic dysfunction. T...

journal_title：Journal of clinical pharmacology

authors： Hatorp V,Walther KH,Christensen MS,Haug-Pihale G

更新日期：2000-02-01 00:00:00

abstract：:Recent initiatives calling for changes in medical education, such as the General Professional Education of the Physician and Robert Wood Johnson Reports, have recommended alternative teaching approaches to the lecture format. The Patient-Oriented Problem-Solving (POPS) exercises, sponsored by the Upjohn Company (Kalam...

journal_title：Journal of clinical pharmacology

authors： Ingenito AJ,Wooles WR

更新日期：1995-02-01 00:00:00

abstract：:Although there are many reports of the short-term effectiveness of antiarrhythmic drugs for suppression of ventricular ectopic depolarizations, there are less data available on the long-term use of these drugs. We treated 122 patients for up to 2 years with antiarrhythmic drugs for suppression of frequent ventricular ...

journal_title：Journal of clinical pharmacology

authors： Salerno DM,Fifield J,Hodges M

更新日期：1990-03-01 00:00:00

abstract：:Pharmacological target-mediated drug disposition (TMDD) represents a special source of nonlinear pharmacokinetics, and its occurrence in large-molecule compounds has been well recognized because numerous protein drugs have been reported to have TMDD due to specific binding to their pharmacological targets. Although TM...

journal_title：Journal of clinical pharmacology

authors： An G,Lee KSS,Yang J,Hammock BD

更新日期：2020-10-19 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：: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：: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 overall response rate (ORR) is a largely adopted outcome measure in early-phase oncology trials. ORR is highly relevant in cancer drug development at the time of deciding whether to move to confirmatory phase 3 trials; moreover, ORR is gaining increasing relevance in fast-track registration procedures. No systemat...

journal_title：Journal of clinical pharmacology

authors： Dello Russo C,Cappoli N,Pilunni D,Navarra P

更新日期：2020-11-26 00:00:00

abstract：:Atorvastatin is a common option among the HMG-CoA reductase inhibitors for the treatment of lipid disorders because of its excellent lipid-lowering efficacy and overall safety profile. Although these agents can rarely cause rhabdomyolysis by themselves, macrolides, among other agents, have been demonstrated to increas...

journal_title：Journal of clinical pharmacology

authors： Amsden GW,Kuye O,Wei GC

更新日期：2002-04-01 00:00:00

abstract：:This study was undertaken to determine the relationship of serum ACD levels to dosage in a group of patients who had been seizure free for at least two years. It demonstrated that some patients remain completely seizure free with DPH and/or phenobarbital serum concentrations which are well below the reported "optimal"...

journal_title：Journal of clinical pharmacology

authors： Feldman RG,Pippenger CE

更新日期：1976-01-01 00:00:00

abstract：:Oral contraceptives (OCs) are the most widely used form of birth control among women of childbearing potential. Knowledge of potential drug-drug interactions (DDIs) with OCs becomes imperative to provide information on the medication to women of childbearing potential and enable their inclusion in clinical trials, esp...

journal_title：Journal of clinical pharmacology

authors： Sun H,Sivasubramanian R,Vaidya S,Barve A,Jarugula V

更新日期：2020-12-01 00:00:00

abstract：:The aim of the study was to investigate the pharmacokinetics and removal of midazolam and unconjugated and glucuronidated 1-hydroxy-midazolam in 4 intensive care patients on continuous venovenous hemodialysis. Plasma midazolam and its metabolites were assessed by HPLC from blood samples collected during continuous inf...

journal_title：Journal of clinical pharmacology

authors： Bolon M,Bastien O,Flamens C,Paulus S,Boulieu R

更新日期：2001-09-01 00:00:00

abstract：:In June 1999, the Food and Drug Administration issued draft guidance for bioequivalence studies for nasal aerosols and nasal sprays for local action. The purpose of this opinion paper is to highlight the need for a balanced scientific debate before this guidance is used by underscoring the areas in the document that a...

journal_title：Journal of clinical pharmacology

authors： Harrison LI

更新日期：2000-07-01 00:00:00

abstract：:The pharmacokinetic characteristics of a slow-release formulation of clonidine (150 micrograms) were compared with those of a conventional formulation (75 micrograms) after acute and chronic (2 week) administration to 12 hypertensive subjects. The Tmax of the slow-release formulation was significantly later than for t...

journal_title：Journal of clinical pharmacology

authors： Conway EL,Anavekar SN,Howes LG,Louis WJ

更新日期：1992-05-01 00:00:00

abstract：:Everolimus is an immunosuppressant intended for use with cyclosporine in acute-rejection prophylaxis following organ transplantation. The possibility of a drug interaction of cyclosporine on everolimus was assessed. In this randomized, two-period, crossover study, 24 healthy subjects received a single oral dose of 2 m...

journal_title：Journal of clinical pharmacology

authors： Kovarik JM,Kalbag J,Figueiredo J,Rouilly M,Frazier OL,Rordorf C

更新日期：2002-01-01 00:00:00

abstract：:Lemborexant is a novel orexin receptor antagonist approved in the United States and Japan for the treatment of insomnia. This article describes the population pharmacokinetics (PK) of lemborexant and the relationship of its daily steady-state exposure (Cav,ss ) to the probability of most frequent treatment-emergent ad...

journal_title：Journal of clinical pharmacology

authors： Lalovic B,Majid O,Aluri J,Landry I,Moline M,Hussein Z

更新日期：2020-12-01 00:00:00

abstract：:Despite a robust exposure-response relationship of infliximab in inflammatory bowel disease (IBD), attempts to adjust dosing to individually predicted serum concentrations of infliximab (SICs) are lacking. Compared with labor-intensive conventional software for pharmacokinetic (PK) modeling (eg, NONMEM) dashboards are...

journal_title：Journal of clinical pharmacology

authors： Eser A,Primas C,Reinisch S,Vogelsang H,Novacek G,Mould DR,Reinisch W

更新日期：2018-06-01 00:00:00

abstract：:The effects of labetalol, diltiazem and verapamil on antipyrine and indocyanine green clearance were evaluated in a placebo-controlled, repeated measures evaluation. Twelve healthy subjects received either labetalol (200 mg every 12 hours), diltiazem (90 mg. every 8 hours), verapamil (80 mg every 8 hours), or placebo ...

journal_title：Journal of clinical pharmacology

authors： Rocci ML Jr,Vlasses PH,Lener ME,Fruncillo RA,Sirgo MA

更新日期：1989-10-01 00:00:00

abstract：:Esmolol is an intravenous beta blocker with a short duration of action. The pharmacokinetics of esmolol and its acid metabolite, ASL-8123, were studied in nine patients who had stable, biopsy-proved Laennec's cirrhosis and in three normal volunteer controls. Kinetics were determined after a four-hour continuous infusi...

journal_title：Journal of clinical pharmacology

authors： Buchi KN,Rollins DE,Tolman KG,Achari R,Drissel D,Hulse JD

更新日期：1987-11-01 00:00:00

abstract：:The selective T-cell costimulation modulator abatacept is approved for treatment of adult rheumatoid arthritis (RA) and polyarticular juvenile idiopathic arthritis (pJIA; 6-17 years [intravenous] and 2-17 years [subcutaneous]). An extrapolation approach was taken to determine subcutaneous weight-tiered doses of abatac...

journal_title：Journal of clinical pharmacology

authors： Gandhi Y,Passarell JA,Roy A,Murthy B

更新日期：2020-12-07 00:00:00

abstract：:The number of worldwide and Asian multiregional clinical trials (MRCTs) submitted for Japanese New Drug Applications increased markedly between 2009 and 2013, with an increasing number performed for simultaneously submission in the USA, EU, and Japan. Asian studies accounted for 32% of MRCTs (14/44 studies) and had co...

journal_title：Journal of clinical pharmacology

authors： Shirotani M,Kurokawa T,Chiba K

更新日期：2014-07-01 00:00:00

abstract：:Recently, a new latanoprost ophthalmic solution containing cyclodextrins was developed. The purpose of the present work was to compare the stability, clinical efficacy, and adverse effect profile of this formulation with the innovator product. The innovator formulation was stable at 4 degrees C but exhibited degradati...

journal_title：Journal of clinical pharmacology

authors： Gonzalez JR,Baiza-Duran L,Quintana-Hau J,Tornero-Montaño R,Castaneda-Hernandez G,Ortiz M,Alarcon-Oceguera F,Beltran-Loustaunau M,Cortez-Gastelum M,Garcidueñas-Mejia J,Gomez-Bastar P,Jimenez-Roman J,Korder-Ortega V,Paczka-Zapata

更新日期：2007-01-01 00:00:00

abstract：:The aim of this study was to determine the relationship, precision, and bias of a propofol target-controlled infusion (TCI) system during prolonged infusion in neurosurgical patients. We retrospectively included patients undergoing general anesthesia for elective neurosurgical removal of brain tumors and postoperative...

journal_title：Journal of clinical pharmacology

authors： Cortegiani A,Pavan A,Azzeri F,Accurso G,Vitale F,Gregoretti C

更新日期：2018-05-01 00:00:00

abstract：:A vast and continuously growing amount of material on drugs exists in the literature to read and evaluate. Frequently, the papers and their recommendations are conflicting and contradictory. Readers are faced with the dilemma of deciding what to believe. The need for evidence-based medicine as a foundation for optimal...

journal_title：Journal of clinical pharmacology

authors： Spector R,Vesell ES

更新日期：2002-09-01 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：:Adverse reactions to sulfonamides occur at a higher frequency in patients infected with the human immunodeficiency virus (HIV) than noninfected patients. Some studies have suggested that patients with the slow acetylator phenotype are predisposed to these reactions, whereas other studies suggest that the slow acetylat...

journal_title：Journal of clinical pharmacology

authors： O'Neil WM,MacArthur RD,Farrough MJ,Doll MA,Fretland AJ,Hein DW,Crane LR,Svensson CK

更新日期：2002-06-01 00:00:00