Predicting Drug Extraction in the Human Gut Wall: Assessing Contributions from Drug Metabolizing Enzymes and Transporter Proteins using Preclinical Models.

abstract：:Since up to 90% of a theophylline dose is biotransformed, drugs influencing microsomal enzyme systems in the liver may affect the elimination of theophylline. Other integrated mechanisms (e.g. hepatic uptake) may also be altered by concurrent administration of other drugs. Whatever the mechanism, the interaction may b...

journal_title：Clinical pharmacokinetics

authors： Jonkman JH,Upton RA

更新日期：1984-07-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Febuxostat is a xanthine oxidase inhibitor indicated for gout and hyperuricemia. This work investigates potential clinically relevant covariates for febuxostat pharmacokinetics with a special focus on Asian race and bodyweight. METHODS:Febuxostat plasma concentrations from 141 male subjects we...

journal_title：Clinical pharmacokinetics

authors： Rekić D,Johansson S,Leander J

更新日期：2020-09-19 00:00:00

abstract：BACKGROUND:Bitopertin (RG1678) is a glycine reuptake inhibitor currently in phase 3 trials for treatment of schizophrenia. This paper describes the use of physiologically based pharmacokinetic (PBPK) modelling and preclinical data to gain insights into and predict bitopertin clinical pharmacokinetics. METHODS:Simulati...

journal_title：Clinical pharmacokinetics

authors： Parrott N,Hainzl D,Alberati D,Hofmann C,Robson R,Boutouyrie B,Martin-Facklam M

更新日期：2013-08-01 00:00:00

abstract：:Clinical pharmacokinetics emerged as a clinical discipline in the late 1960s and early 1970s. Clinical pharmacokinetic monitoring (CPM) helped many pharmacists to enter the clinical arena, but the focus was more on the pharmacists and tools. With the widespread acceptance of pharmaceutical care and patient-focused pha...

journal_title：Clinical pharmacokinetics

authors： Ensom MH,Davis GA,Cropp CD,Ensom RJ

更新日期：1998-04-01 00:00:00

abstract：:The pharmacokinetics and cardiovascular effects of the calcium entry blocker nisoldipine (10 mg twice daily) were studied in 6 patients with renal failure (creatinine clearance 23 +/- 9 ml/min) and 6 healthy control subjects after a single dose and 1 week of oral administration. No significant differences in eliminati...

journal_title：Clinical pharmacokinetics

authors： van Harten J,Burggraaf J,van Brummelen P,Breimer DD

更新日期：1989-01-01 00:00:00

abstract：:The ability to deliver safe and effective moderate sedation is crucial to the ability to perform invasive procedures. Sedative drugs should have a quick onset of action, provide rapid and clear-headed recovery, and be easy to administer and monitor. A number of drugs have been demonstrated to provide effective sedatio...

journal_title：Clinical pharmacokinetics

authors： Gan TJ

更新日期：2006-01-01 00:00:00

abstract：:For propofol clearance, allometric scaling has been applied successfully for extrapolations between species (rats and humans) and within the human bodyweight range (children and adults). In this analysis, the human bodyweight range is explored to determine for which range an allometric model with a fixed or estimated ...

journal_title：Clinical pharmacokinetics

authors： Peeters MY,Allegaert K,Blussé van Oud-Alblas HJ,Cella M,Tibboel D,Danhof M,Knibbe CA

更新日期：2010-04-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Daclatasvir is a potent, pangenotypic once-daily hepatitis C virus (HCV) NS5A inhibitor that is approved for the treatment of chronic HCV infection. The objective of this analysis was to characterize the pharmacokinetics of daclatasvir in subjects with chronic HCV infection. METHODS:A populati...

journal_title：Clinical pharmacokinetics

authors： Chan P,Li H,Zhu L,Bifano M,Eley T,Osawa M,Ueno T,Hughes E,Bertz R,Garimella T,AbuTarif M

更新日期：2017-10-01 00:00:00

abstract：:Acute coronary syndromes (ACS) remain life-threatening disorders associated with high morbidity and mortality, despite advances in treatment over the last decade. Adenosine diphosphate-induced platelet activation via P2Y(12) receptors plays a pivotal role in the pathophysiology of ACS. The current standard of treatmen...

journal_title：Clinical pharmacokinetics

authors： Teng R

更新日期：2012-05-01 00:00:00

abstract：:25 patients with different degrees of chronic stable renal failure received oral treatment with cimetidine over 6 days and a final dose in the morning of day 7. The doses of cimetidine were reduced according to the degree of renal failure. Plasma concentrations of cimetidine were determined before the morning dose on ...

journal_title：Clinical pharmacokinetics

authors： Larsson R,Norlander B,Bodemar G,Walan A

更新日期：1981-07-01 00:00:00

abstract：:The pharmacokinetics of cephradine, a cephalosporin with a low degree of protein binding, was studied in 12 women after oral and intravenous administration of the drug during and after pregnancy. Six of the 12 women also received a cephalosporin with a high degree of protein binding, cefazolin, intravenously during an...

journal_title：Clinical pharmacokinetics

authors： Philipson A,Stiernstedt G,Ehrnebo M

更新日期：1987-02-01 00:00:00

abstract：:The hypolipidaemic agent pravastatin differs from other US Food and Drug Administration (FDA)-approved HMG-CoA reductase inhibitors (e.g. lovastatin and simvastatin) because it has greater hydrophilicity, as a result of the hydroxyl group attached to its decalin ring. The hydrophilic nature of pravastatin accounts for...

journal_title：Clinical pharmacokinetics

authors： Quion JA,Jones PH

更新日期：1994-08-01 00:00:00

abstract：:Population pharmacokinetic modelling is widely used within the field of clinical pharmacology as it helps to define the sources and correlates of pharmacokinetic variability in target patient populations and their impact upon drug disposition; and population pharmacokinetic modelling provides an estimation of drug pha...

journal_title：Clinical pharmacokinetics

authors： Sherwin CM,Kiang TK,Spigarelli MG,Ensom MH

更新日期：2012-09-01 00:00:00

abstract：:Recent international guidelines on the detection, clinical assessment and management of patients with hypertension have highlighted a number of themes that should be incorporated into routine clinical practice. First, although antihypertensive therapy is having a major impact on reducing the incidence of coronary hear...

journal_title：Clinical pharmacokinetics

authors： Donnelly R

更新日期：1999-01-01 00:00:00

abstract：:The half-life and metabolic clearance rate (MCR) of antipyrine and phenytoin were determined in 14 young (mean age: 28.8 +/- 8.3 (SD) years] and in 14 elderly [mean age: 83.5 +/- 7.1 (SD) years] subjects and correlated with liver volume, which was determined by ultrasonic scanning, to see if an age-dependent differenc...

journal_title：Clinical pharmacokinetics

authors： Bach B,Hansen JM,Kampmann JP,Rasmussen SN,Skovsted L

更新日期：1981-09-01 00:00:00

abstract：BACKGROUND:Reducing the dose of efavirenz can improve safety, reduce costs, and increase access for patients with HIV infection. According to the World Health Organization, a similar dosing strategy for all patient populations is desirable for universal roll-out; however, it remains unknown whether the 400 mg daily dos...

journal_title：Clinical pharmacokinetics

authors： Schalkwijk S,Ter Heine R,Colbers AC,Huitema ADR,Denti P,Dooley KE,Capparelli E,Best BM,Cressey TR,Greupink R,Russel FGM,Mirochnick M,Burger DM

更新日期：2018-11-01 00:00:00

abstract：:Part I of this article, which appeared in the previous issue of the Journal, covered the following agents: histamine H2-receptor antagonists (cimetidine, ranitidine, famotidine, nizatidine); muscarinic-M1-receptor antagonists (pirenzepine); proton pump inhibitors (omeprazole); site-protective agents (colloidal bismuth...

journal_title：Clinical pharmacokinetics

authors： Lauritsen K,Laursen LS,Rask-Madsen J

更新日期：1990-08-01 00:00:00

abstract：:Dasabuvir is a nonstructural (NS) 5B non-nucleoside inhibitor of the hepatitis C virus (HCV) used in combination with ombitasvir/paritaprevir/ritonavir for the treatment of chronic HCV infection. It is primarily metabolized by cytochrome P450 (CYP) 2C8, with a minor contribution from CYP3A. Biotransformation of dasabu...

journal_title：Clinical pharmacokinetics

authors： King JR,Zha J,Khatri A,Dutta S,Menon RM

更新日期：2017-10-01 00:00:00

abstract：:Physiologically-based pharmacokinetic (PBPK) modeling is a powerful tool used to characterize maturational changes in drug disposition to inform dosing across childhood; however, its use is limited in pediatric drug development. Access to pediatric pharmacokinetic data is a barrier to widespread application of this mo...

journal_title：Clinical pharmacokinetics

authors： Hornik CP,Wu H,Edginton AN,Watt K,Cohen-Wolkowiez M,Gonzalez D

更新日期：2017-11-01 00:00:00

abstract：:Intraventricular administration of chemotherapy is one approach to overcoming the limited distribution of anticancer drugs and their active metabolites into the CNS. This form of regional chemotherapy has led to effective treatment of occult and overt meningeal leukaemia in humans. In contrast, the efficacy of this th...

journal_title：Clinical pharmacokinetics

authors： Fleischhack G,Jaehde U,Bode U

更新日期：2005-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Bayesian forecasting (BF) methods for tobramycin dose individualisation has not seen widespread clinical adoption, despite being endorsed by clinical practice guidelines. Several freeware and commercial programmes using BF methods are available to support personalised dosing. This study evalua...

journal_title：Clinical pharmacokinetics

authors： Burgard M,Sandaradura I,van Hal SJ,Stacey S,Hennig S

更新日期：2018-08-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Dosing of therapeutic monoclonal antibodies (mAbs) is often based on body size, with the perception that body size-based dosing would reduce inter-subject variability in drug exposure. However, most mAbs are target specific with a relatively large therapeutic window and generally a small contri...

journal_title：Clinical pharmacokinetics

authors： Bai S,Jorga K,Xin Y,Jin D,Zheng Y,Damico-Beyer LA,Gupta M,Tang M,Allison DE,Lu D,Zhang Y,Joshi A,Dresser MJ

更新日期：2012-02-01 00:00:00

abstract：:This review describes the pharmacokinetics of the major drugs used for the treatment of inflammatory bowel disease. This information can be helpful for the selection of a particular agent and offers guidance for effective and well tolerated regimens. The corticosteroids have a short elimination half-life (t1/2beta) of...

journal_title：Clinical pharmacokinetics

authors： Schwab M,Klotz U

更新日期：2001-01-01 00:00:00

abstract：:Clarithromycin is a semisynthetic macrolide antibiotic, structurally related to erythromycin. It has a more favourable pharmacokinetic profile than erythromycin, thus allowing twice-daily administration and possibly increasing compliance among outpatients. Clarithromycin is well absorbed from the gastrointestinal trac...

journal_title：Clinical pharmacokinetics

authors： Fraschini F,Scaglione F,Demartini G

更新日期：1993-09-01 00:00:00

abstract：:Routine use of therapeutic drug monitoring in children is helpful in individualizing the dosage during long term treatment (e.g. theophylline and antiepileptic drugs) and in checking against toxic accumulation of drug in neonates (e.g. digoxin, theophylline/caffeine and aminoglycoside antibiotics). In individual patie...

journal_title：Clinical pharmacokinetics

authors： Boréus LO

更新日期：1989-01-01 00:00:00

abstract：:Inadequate pain control in the postoperative period not only contributes to patient discomfort, but also causes physiological changes that may result in increased risk of myocardial ischaemia, deep vein thrombosis and pulmonary embolism. These events complicate postoperative recovery and may lead to longer hospital st...

journal_title：Clinical pharmacokinetics

authors： Sinatra R

更新日期：2005-01-01 00:00:00

abstract：:The ability of a new multiple-dose non-linear regression analysis program to predict steady-state aminoglycoside peak and trough serum concentrations was evaluated. 30 patients receiving either amikacin (7), gentamicin (10) or tobramycin (13) were studied. A standard method of prediction which requires the collection ...

journal_title：Clinical pharmacokinetics

authors： Koup JR,Killen T,Bauer LA

更新日期：1983-09-01 00:00:00

abstract：:The elderly are generally considered to be different from young people in terms of drug response and this applies particularly to quantitative differences. While altered drug handling is a major potential source of difference in responsiveness to drugs, the relative contribution of pharmacokinetics and pharmacodynamic...

journal_title：Clinical pharmacokinetics

authors： Crooks J,O'Malley K,Stevenson IH

更新日期：1976-01-01 00:00:00

abstract：:It should be recognized that children are not small adults, hence dosing in children should not be a 'small adult dose'. A mean population dose in all age groups is just an average dose and not necessarily the best or the correct dose for a given patient. The dose of a drug varies from patient to patient and individua...

journal_title：Clinical pharmacokinetics

authors： Mahmood I

更新日期：2014-04-01 00:00:00

abstract：:The alignment of drug metabolism and pharmacokinetic departments with drug discovery has not produced a radical improvement in the pharmacokinetic properties of new chemical entities. The reason for this is complex, reflecting in part the difficulty of combining potency, selectivity, water solubility, metabolic stabil...

journal_title：Clinical pharmacokinetics

authors： Smith D,Schmid E,Jones B

更新日期：2002-01-01 00:00:00