Physiologically based pharmacokinetic modelling to predict single- and multiple-dose human pharmacokinetics of bitopertin.

abstract：:Morphine, morphine-6-glucuronide (M6G), morphine-3-glucuronide (M3G) and normorphine were analysed with high performance liquid chromatography in plasma and urine, collected over 72 h after administration of single intravenous 5 mg and oral 20 mg doses of morphine to 7 healthy volunteers. Systemic plasma clearance of ...

journal_title：Clinical pharmacokinetics

authors： Hasselström J,Säwe J

更新日期：1993-04-01 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：:The treatment of epilepsy in pregnancy is particularly challenging in that the fetal and maternal risks associated with maternal seizures need to be balanced against the potential teratogenic effects of antiepileptic drugs (AEDs). Pregnancy is known to affect the pharmacokinetics of older-generation AEDs. Understandin...

journal_title：Clinical pharmacokinetics

authors： Tomson T,Battino D

更新日期：2007-01-01 00:00:00

abstract：BACKGROUND:Recombinant methionyl human leptin (r-metHuLeptin) has demonstrated efficacy in improving hormonal and metabolic parameters in leptin-deficient states, and it has been suggested that leptin replacement may reverse metabolic adaptations during weight loss interventions. The pharmacokinetics of subcutaneously ...

journal_title：Clinical pharmacokinetics

authors： Chan JL,Wong SL,Mantzoros CS

更新日期：2008-01-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Bosentan is a competitive antagonist on endothelin receptor A and B (ETA and ETB), displacing the endogenous binding partner endothelin-1 (ET-1) from its binding sites. After administration of escalating single doses of 10-750 mg as an intravenous (i.v.) infusion, bosentan showed dose-dependen...

journal_title：Clinical pharmacokinetics

authors： Volz AK,Krause A,Haefeli WE,Dingemanse J,Lehr T

更新日期：2017-12-01 00:00:00

abstract：BACKGROUND:Because of the vulnerability and frailty of elderly adults, clinical drug development has traditionally been biased towards young and middle-aged adults. Recent efforts have begun to incorporate data from paediatric investigations. Nevertheless, the elderly often remain underrepresented in clinical trials, e...

journal_title：Clinical pharmacokinetics

authors： Schlender JF,Meyer M,Thelen K,Krauss M,Willmann S,Eissing T,Jaehde U

更新日期：2016-12-01 00:00:00

abstract：INTRODUCTION:Neglected tropical diseases (NTDs) affect more than one billion people, mainly living in developing countries. For most of these NTDs, treatment is suboptimal. To optimize treatment regimens, clinical pharmacokinetic studies are required where they have not been previously conducted to enable the use of ph...

journal_title：Clinical pharmacokinetics

authors： Verrest L,Dorlo TPC

更新日期：2017-06-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Metformin is a biguanide used in the treatment of type 2 diabetes mellitus. In girls with a low birth weight, and early-normal and rapidly progressive puberty, metformin therapy is capable of modifying this outcome, prolonging pubertal growth, increasing height gain, delaying the age at menarch...

journal_title：Clinical pharmacokinetics

authors： Sánchez-Infantes D,Díaz M,López-Bermejo A,Marcos MV,de Zegher F,Ibáñez L

更新日期：2011-11-01 00:00:00

abstract：:Most of the currently available psychotropic drugs form 1 or more active metabolites during in vivo biotransformation in humans and/or animals. In some cases these metabolites are rapidly conjugated and excreted, but in others they attain blood and/or brain concentrations within the same range as, or even higher than,...

journal_title：Clinical pharmacokinetics

authors： Caccia S,Garattini S

更新日期：1990-06-01 00:00:00

abstract：:The pharmacokinetics of metoprolol have been studied in a group of patients with varying degrees of renal impairment and in healthy subjects after administration of 20 mg of metoprolol tartrate intravenously and 50 mg orally in a single dose and during steady-state conditions. There were no significant differences in ...

journal_title：Clinical pharmacokinetics

authors： Jordö L,Attman PO,Aurell M,Johansson L,Johnsson G,Regårdh CG

更新日期：1980-03-01 00:00:00

abstract：BACKGROUND:Febuxostat is a novel non-purine selective inhibitor of xanthine oxidase currently being developed for the management of hyperuricemia in patients with gout. OBJECTIVE:To investigate the pharmacokinetics, pharmacodynamics and safety of febuxostat over a range of oral doses in healthy subjects. METHODS:In a...

journal_title：Clinical pharmacokinetics

authors： Khosravan R,Grabowski BA,Wu JT,Joseph-Ridge N,Vernillet L

更新日期：2006-01-01 00:00:00

abstract：OBJECTIVE:To evaluate the dose proportionality and linearity and pharmacokinetic profile of desloratadine after single oral doses over the range of 5 to 20mg. DESIGN:Single centre, randomised, open-label, 4-way crossover study in which healthy adults received single doses of desloratadine (5, 7.5, 10 and 20mg) in 4 di...

journal_title：Clinical pharmacokinetics

authors： Gupta S,Banfield C,Affrime M,Marco A,Cayen M,Herron J,Padhi D

更新日期：2002-01-01 00:00:00

abstract：:The US Food and Drug Administration (FDA) draft guidance for industry on drug interaction studies recommends, but does not mandate, that both cigarette smokers and non-smokers can be used to study drug metabolism in clinical trials, and that important results related to smoking should be included in drug labelling to ...

journal_title：Clinical pharmacokinetics

authors： Li H,Shi Q

更新日期：2015-05-01 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：: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：:For the past 300 years antimalarial dosage regimens have not been based on pharmacokinetic information. However, now that this information is available, it is appropriate to examine current recommendations for prophylaxis and treatment. In healthy subjects, the cinchona alkaloids (quinine and quinidine), primaquine an...

journal_title：Clinical pharmacokinetics

authors： White NJ

更新日期：1985-05-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Caspofungin is an echinocandin antifungal agent used as first-line therapy for the treatment of invasive candidiasis. The maintenance dose is adapted to body weight (BW) or liver function (Child-Pugh score B or C). We aimed to study the pharmacokinetics of caspofungin and assess pharmacokineti...

journal_title：Clinical pharmacokinetics

authors： Martial LC,Brüggemann RJ,Schouten JA,van Leeuwen HJ,van Zanten AR,de Lange DW,Muilwijk EW,Verweij PE,Burger DM,Aarnoutse RE,Pickkers P,Dorlo TP

更新日期：2016-06-01 00:00:00

abstract：:The combination of artemether and lumefantrine (benflumetol) is a new and very well tolerated oral antimalarial drug effective even against multidrug-resistant falciparum malaria. The artemether component is absorbed rapidly and biotransformed to dihydroartemisinin, and both are eliminated with terminal half-lives of ...

journal_title：Clinical pharmacokinetics

authors： White NJ,van Vugt M,Ezzet F

更新日期：1999-08-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:This study proposes a model-informed approach for therapeutic drug monitoring (TDM) of rifampicin to improve tuberculosis (TB) treatment. METHODS:Two datasets from pulmonary TB patients were used: a pharmacokinetic study (34 patients, 373 samples), and TDM data (96 patients, 391 samples) colle...

journal_title：Clinical pharmacokinetics

authors： van Beek SW,Ter Heine R,Keizer RJ,Magis-Escurra C,Aarnoutse RE,Svensson EM

更新日期：2019-06-01 00:00:00

abstract：:Fluconazole was recently developed for the treatment of superficial and systemic fungal infections. Triazole groups and insertion of 2 fluoride atoms increase the polarity and hydrosolubility of the drug, allowing it to be used in a parenteral form. Bioassay methods using Candida pseudotropicalis as a test organism we...

journal_title：Clinical pharmacokinetics

authors： Debruyne D,Ryckelynck JP

更新日期：1993-01-01 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：:Intestinal metabolism can limit oral bioavailability of drugs and increase the risk of drug interactions. It is therefore important to be able to predict and quantify it in drug discovery and early development. In recent years, a plethora of models-in vivo, in situ and in vitro-have been discussed in the literature. T...

journal_title：Clinical pharmacokinetics

authors： Peters SA,Jones CR,Ungell AL,Hatley OJ

更新日期：2016-06-01 00:00:00

abstract：:A reduction in plasma albumin concentration, as seen in patients with the nephrotic syndrome, is usually associated with a decrease in plasma protein binding of highly bound drugs. Therefore, the fraction of the unbound drug increases, but the absolute free concentration remains essentially unchanged due to a compensa...

journal_title：Clinical pharmacokinetics

authors： Gugler R,Azarnoff DL

更新日期：1976-01-01 00:00:00

abstract：:Pregnancy is a specific dynamic state, and the potential usefulness of caring for a disorder in the fetus or the mother is now well established. Previously, pregnant women have been excluded from clinical trials, therefore only a few studies concerning evaluation of the pregestational metabolism or transplacental tran...

journal_title：Clinical pharmacokinetics

authors： Bourget P,Roulot C,Fernandez H

更新日期：1995-02-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:A simple approach is proposed to predict drug clearance in children when no paediatric data are available for drugs metabolised by cytochromes. METHODS:The maturation functions of cytochrome activity and binding proteins in plasma were combined with several measures of body size to describe dr...

journal_title：Clinical pharmacokinetics

authors： Cerruti L,Bleyzac N,Tod M

更新日期：2018-07-01 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：:Antipyrine pharmacokinetics were studied in 6 healthy women before and 2, 8 and 12 weeks after administering the injectable progestagen (progestin), norethisterone (norethindrone) enanthate 200mg intramuscularly. Additionally, antipyrine kinetics in 5 women who had previously used the injectable contraceptive for 8 to...

journal_title：Clinical pharmacokinetics

authors： Joshi JV,Gupta KC,Hazari KT,Gokral J,Pohujani S,Satoskar R

更新日期：1986-03-01 00:00:00

abstract：BACKGROUND:Enzyme replacement therapy (ERT) is currently the standard treatment for patients with Gaucher disease type I (GD1), but the pharmacokinetics have hardly been studied. This study aimed to quantify in vivo enzyme activity in peripheral leukocytes from patients receiving long-term treatment with imiglucerase o...

journal_title：Clinical pharmacokinetics

authors： Gras-Colomer E,Martínez-Gómez MA,Moya-Gil A,Fernandez-Zarzoso M,Merino-Sanjuan M,Climente-Martí M

更新日期：2016-09-01 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：:A method is presented for the simultaneous estimation of functional hepatic blood flow and intrinsic clearance. The method uses pharmacokinetic data of a therapeutically employed drug and one of its primary metabolites following intravenous and oral administration of the parent compound. When the disposition of the dr...

journal_title：Clinical pharmacokinetics

authors： Weber W,Looby M,Brockmöller J

更新日期：1992-07-01 00:00:00