Abstract：
:The plasma protein binding of drugs, particularly those that are highly bound, may have significant clinical implications. Although protein binding is a major determinant of drug action, it is only one of a myriad of factors that influence drug disposition. The extent of protein binding is a function of drug and protein concentrations, the affinity constant for the drug-protein interaction and the number of protein binding sites per class of binding site. Age-related changes in protein binding are usually not clinically important in drug therapy. Albumin levels are generally decreased in the elderly, whereas alpha1-acid glycoprotein levels are not altered by age per se. Alterations in plasma protein binding that occur in the elderly are generally not attributed to age, but rather to physiological and pathophysiological changes or disease states that may occur more frequently in the elderly and most often account for altered protein binding. Age-related physiological changes, such as decreased renal function, decreased hepatic function and decreased cardiac output, generally produce more clinically significant alterations in drug disposition than that seen with alterations in drug plasma protein binding. An understanding of the inter-relationships between drug concentrations, protein binding, the physiology of aging, disease, pharmacokinetics and pharmacodynamics is necessary for effective therapeutic monitoring. Monitoring of unbound drug concentrations simplifies these relationships and provides the fundamental information needed for dosage regimen development and adjustment. Drug therapy in the elderly should be individualised taking into account all of these factors.
journal_name
Clin Pharmacokinetjournal_title
Clinical pharmacokineticsauthors
Grandison MK,Boudinot FDdoi
10.2165/00003088-200038030-00005keywords:
subject
Has Abstractpub_date
2000-03-01 00:00:00pages
271-90issue
3eissn
0312-5963issn
1179-1926journal_volume
38pub_type
杂志文章,评审abstract：:Few of the articles published on antibiotics and pregnancy are concerned with pharmacokinetics. It is particularly difficult to evaluate possible alterations in pharmacokinetic parameters that may be due to pregnancy. Most data available have been obtained in connection with abortion or delivery. Such data may not be ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-197904040-00003
更新日期：1979-07-01 00:00:00
abstract：BACKGROUND AND OBJECTIVE:Losmapimod is an orally available, potent p38 mitogen-activated protein kinase inhibitor. It is in development as an anti-inflammatory drug in different therapeutic areas. Clinical studies have shown that losmapimod is well tolerated and safe in humans and several studies have shown its pharmac...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.1007/s40262-012-0025-6
更新日期：2013-03-01 00:00:00
abstract：:The effects of anaesthesia and surgery on the pharmacokinetics of ketobemidone were studied in 12 patients. Plasma ketobemidone concentrations were assayed with a mass-fragmentographic method. The peroperative Vd(area) was 5.9 +/- 2.6L/kg and the terminal half-life was 3.9 +/- 1.7 h. In the postoperative period Vd(are...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-198207030-00005
更新日期：1982-05-01 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
pub_type： 杂志文章,评审
doi：10.2165/00003088-199937001-00004
更新日期：1999-01-01 00:00:00
abstract：:Following administration of equivalent oral doses (30mg) of either prednisone or prednisolone to 5 patients with chronic active liver disease who had failed to respond to therapy, 5 patients with chronic active liver disease in remission induced by prednisone, and 7 healthy volunteers, corticosteroid concentrations we...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-198207050-00005
更新日期：1982-09-01 00:00:00
abstract：:The effects of diabetes mellitus on the pharmacokinetics and pharmacodynamics of drugs have been well described in experimental animal models; however, only minimal data exist for humans and the current knowledge regarding the effects of diabetes on these properties remains unclear. Nevertheless, it has been observed ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/11631900-000000000-00000
更新日期：2012-08-01 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
pub_type： 杂志文章
doi：10.1007/s40262-020-00943-6
更新日期：2020-09-19 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200039010-00004
更新日期：2000-07-01 00:00:00
abstract：OBJECTIVE:The aim of this study was to evaluate the pharmacokinetics (PK) of trastuzumab emtansine (T-DM1) and relevant analytes in patients with human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer and hepatic impairment. METHODS:Patients were enrolled in three independent parallel cohort...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,多中心研究
doi：10.1007/s40262-016-0496-y
更新日期：2017-09-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200039020-00005
更新日期：2000-08-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/00003088-199324040-00007
更新日期：1993-04-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-017-0525-5
更新日期：2017-11-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-018-00733-1
更新日期：2019-07-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:NXY-059 (disufenton sodium, Cerovive, a nitrone with neuroprotective and free radical trapping properties (in experimental stroke) is under development for the treatment of acute stroke. The objectives of this study were to develop a population pharmacokinetic model for NXY-059 in acute stroke...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,多中心研究,随机对照试验
doi：10.2165/00003088-200544080-00007
更新日期：2005-01-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-198916040-00002
更新日期：1989-04-01 00:00:00
abstract：BACKGROUND:Fast-acting insulin aspart (faster aspart) is an ultra-fast-acting formulation of insulin aspart (IAsp). This post hoc analysis investigated the pharmacokinetics of faster aspart versus IAsp, measured as free or total IAsp, and the relationship between anti-IAsp antibodies and the pharmacokinetics/pharmacody...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,多中心研究,随机对照试验
doi：10.1007/s40262-018-0718-6
更新日期：2019-05-01 00:00:00
abstract：OBJECTIVE:To assess the differences between patients with hepatic insufficiency and healthy subjects with regard to the pharmacokinetics, cardiac safety and overall safety of ebastine and its active metabolite carebastine. DESIGN:Open-label parallel-group study. PARTICIPANTS:24 patients with varying degrees of hepati...
journal_title：Clinical pharmacokinetics
pub_type： 临床试验,杂志文章
doi：10.2165/00003088-200443020-00004
更新日期：2004-01-01 00:00:00
abstract：:Low-molecular-weight heparins are anticoagulants used in the treatment of thrombosis. They have effectiveness and safety profiles similar to those of unfractionated heparin but are considered an attractive alternative because of their predictable pharmacokinetic characteristics. In this article, we demonstrate the nee...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.2165/11532960-000000000-00000
更新日期：2010-09-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199120060-00003
更新日期：1991-06-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-016-0398-z
更新日期：2016-10-01 00:00:00
abstract：:The prevalence of HIV-associated neurocognitive disorder (HAND) is increasing despite the widespread use of combination antiretroviral therapy (ART). Initial reports suggest that the use of antiretrovirals with good central nervous system (CNS) penetration leads to better neurocognitive outcomes, but this has not yet ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s40262-015-0257-3
更新日期：2015-06-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-200342140-00003
更新日期：2003-01-01 00:00:00
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journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-198510030-00001
更新日期：1985-05-01 00:00:00
abstract：:The isoenzymes which catalyse the polymorphic hydroxylations of debrisoquine/sparteine and S-mephenytoin are cytochromes P450 2D6 and P450 2C19 (CYP2D6 and CYP2C19), respectively. CYP2D6 is involved in the stereospecific metabolism of several important groups of drugs, for example antiarrhythmics, antidepressants and ...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199529030-00005
更新日期：1995-09-01 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
pub_type： 杂志文章
doi：10.2165/00003088-198106040-00006
更新日期：1981-07-01 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
pub_type： 杂志文章,评审
doi：10.1007/s40262-017-0519-3
更新日期：2017-10-01 00:00:00
abstract：:The critically ill patient occupies an increasing amount of time and bed space in modern hospital practice, and also commands increasing expenditure. Drug therapy in these patients has, in the past, been based on data derived from healthy volunteers, fit anaesthetised patients undergoing minor operative procedures, or...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-198814060-00003
更新日期：1988-06-01 00:00:00
abstract：INTRODUCTION:The inhaled corticosteroid (ICS) fluticasone furoate is in development, in combination with the long-acting beta2-agonist vilanterol for the once-daily treatment of asthma and chronic obstructive pulmonary disease and as a monotherapy treatment for asthma. Corticosteroids, including ICSs, have the potentia...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,meta分析
doi：10.1007/s40262-013-0078-1
更新日期：2013-10-01 00:00:00
abstract：:The safety profile of any pharmacological agent is defined on the basis of its toxicity, tolerability and potential for pharmacokinetic and/or pharmacodynamic interactions with other compounds, which may belong to the same or to a different pharmacological class. Drug-drug interactions are important in clinical practi...
journal_title：Clinical pharmacokinetics
pub_type： 杂志文章,评审
doi：10.2165/00003088-199835020-00003
更新日期：1998-08-01 00:00:00
abstract：OBJECTIVE:The aim of these studies was to determine the absolute bioavailability in healthy volunteers of inhaled fluticasone propionate (FP) administered as a single dose via the Diskhaler and Diskus powder devices, and the pharmacokinetics of inhaled FP after repeated administration via the Diskhaler device. METHODS...
journal_title：Clinical pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.2165/00003088-200039001-00004
更新日期：2000-01-01 00:00:00
