Central nervous system penetration of antiretroviral drugs: pharmacokinetic, pharmacodynamic and pharmacogenomic considerations.

abstract：:Thienopyridines are inactive prodrugs that are converted in vivo to active metabolites, which irreversibly bind to and inactivate platelet P2Y(12) receptors, and inhibit platelet activation and aggregation. Prasugrel is a third-generation thienopyridine, recently approved for prevention of thrombotic cardiovascular co...

journal_title：Clinical pharmacokinetics

authors： Small DS,Farid NA,Payne CD,Konkoy CS,Jakubowski JA,Winters KJ,Salazar DE

更新日期：2010-12-01 00:00:00

abstract：:Carbamazepine is one of the most commonly prescribed antiepileptic drugs and is also used in the treatment of trigeminal neuralgia and psychiatric disorders, particularly bipolar depression. Because of its widespread and long term use, carbamazepine is frequently prescribed in combination with other drugs, leading to ...

journal_title：Clinical pharmacokinetics

authors： Spina E,Pisani F,Perucca E

更新日期：1996-09-01 00:00:00

abstract：BACKGROUND:Pemetrexed is used for the treatment for non-small cell lung cancer and mesothelioma. Patients with renal impairment are withheld treatment with this drug as it is unknown what dose is well tolerated in this population. OBJECTIVE:The purpose of our study was to investigate the pharmacokinetics (PK) of pemet...

journal_title：Clinical pharmacokinetics

authors： de Rouw N,Boosman RJ,Huitema ADR,Hilbrands LB,Svensson EM,Derijks HJ,van den Heuvel MM,Burger DM,Ter Heine R

更新日期：2021-01-09 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 of a wide variety of anionic, cationic, and neutral drugs to bind in a reversible manner to plasma proteins has long been recognised. Non-steroidal anti-inflammatory drugs (NSAIDs) are distinguished as a class by the high degree to which they bind to plasma protein. Plasma protein binding properties are pr...

journal_title：Clinical pharmacokinetics

authors： Lin JH,Cocchetto DM,Duggan DE

更新日期：1987-06-01 00:00:00

abstract：:Fluorouracil is used clinically against various solid tumours. Both fluorouracil toxicity and pharmacokinetics vary highly within and between individuals. The reasons why doses are not individualised routinely are difficulties in defining, predicting and achieving an optimal fluorouracil exposure or dose because of a ...

journal_title：Clinical pharmacokinetics

authors： Ploylearmsaeng SA,Fuhr U,Jetter A

更新日期：2006-01-01 00:00:00

abstract：:Platelets contribute significantly to arterial-occlusive thrombosis, one of the major causes of death and disease throughout the world. Consequently, inhibiting platelet function is a potentially important therapeutic goal. Among agents that inhibit platelet function, ticlopidine shows a wide spectrum of antiplatelet ...

journal_title：Clinical pharmacokinetics

authors： Desager JP

更新日期：1994-05-01 00:00:00

abstract：:Since 1989 there has been an exponential introduction of new antiepileptic drugs (AEDs) into clinical practice and these include eslicarbazepine acetate, felbamate, gabapentin, lacosamide, lamotrigine, levetiracetam, oxcarbazepine, perampanel, pregabalin, retigabine (ezogabine), rufinamide, stiripentol, tiagabine, top...

journal_title：Clinical pharmacokinetics

authors： Patsalos PN

更新日期：2013-11-01 00:00:00

abstract：:A substantial proportion of migraine patients have gastric stasis and suffer severe nausea and/or vomiting during their migraine attack. This may lead to erratic absorption from the gastrointestinal tract and make oral treatment unsatisfactory. For such patients, an intranasal formulation may be advantageous. Sumatrip...

journal_title：Clinical pharmacokinetics

authors： Fuseau E,Petricoul O,Moore KH,Barrow A,Ibbotson T

更新日期：2002-01-01 00:00:00

abstract：:A large body of evidence suggests that not only direct anticoagulant effects but also major bleeding events and stroke prevention depend on plasma concentrations of direct oral anticoagulants (DOACs). Concomitant drugs that cause drug-drug interactions (DDIs) alter DOAC exposure by increasing or decreasing DOAC bioava...

journal_title：Clinical pharmacokinetics

authors： Foerster KI,Hermann S,Mikus G,Haefeli WE

更新日期：2020-08-01 00:00:00

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：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：BACKGROUND AND OBJECTIVE:Proprotein convertase subtilisin/kexin type 9 inhibition with monoclonal antibodies such as alirocumab significantly reduces low-density lipoprotein-cholesterol levels ± other lipid-lowering therapies. We aimed to develop and qualify a population pharmacokinetics (PopPK) model for alirocumab in...

journal_title：Clinical pharmacokinetics

authors： Djebli N,Martinez JM,Lohan L,Khier S,Brunet A,Hurbin F,Fabre D

更新日期：2017-10-01 00:00:00

abstract：:Since its discovery in 1970, and introduction into clinical practice in 1978, cyclosporin has become the most important immunosuppressive drug used to prevent organ transplant rejection. This has been achieved by virtue of the improved graft survival rates and adverse effect profiles in patients when compared with tha...

journal_title：Clinical pharmacokinetics

authors： Jones TE

更新日期：1997-05-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Vicriviroc is a small-molecule CCR5 antagonist currently in development for the treatment of HIV in patients on a regimen containing a ritonavir-boosted protease inhibitor. As renal disease and renal dysfunction are prevalent in the HIV-infected population, patients with varying degrees of rena...

journal_title：Clinical pharmacokinetics

authors： Kasserra C,Sansone-Parsons A,Keung A,Tetteh E,Assaf M,O'Mara E,Marbury T

更新日期：2010-06-01 00:00:00

abstract：:Modifications to bodily functions and physiology are known to occur with age. These changes can have a considerable impact on the pharmacokinetic processes of absorption, distribution, metabolism and excretion and the pharmacodynamic properties of administered drugs. For many drugs with a high therapeutic index, this ...

journal_title：Clinical pharmacokinetics

authors： Wildiers H,Highley MS,de Bruijn EA,van Oosterom AT

更新日期：2003-01-01 00:00:00

abstract：:Despite progress in the treatment of metastatic colorectal cancer (mCRC) in the last 15 years, it is still a condition with a relatively low 5-year survival rate. Panitumumab, a fully human monoclonal antibody directed against the epidermal growth factor receptor (EGFR), is able to prolong survival in patients with mC...

journal_title：Clinical pharmacokinetics

authors： Ketzer S,Schimmel K,Koopman M,Guchelaar HJ

更新日期：2018-04-01 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

authors： Uribe M,Summerskill WH,Go VL

更新日期：1982-09-01 00:00:00

abstract：BACKGROUND AND OBJECTIVES:Tesamorelin is a synthetic analogue of growth hormone-releasing factor (GRF), which increases basal and pulsatile growth hormone (GH) secretion and subsequently increases insulin-like growth factor (IGF)-1. Limited information is available about the pharmacokinetics of this compound. Consequen...

journal_title：Clinical pharmacokinetics

authors： González-Sales M,Barrière O,Tremblay PO,Nekka F,Mamputu JC,Boudreault S,Tanguay M

更新日期：2015-03-01 00:00:00

abstract：BACKGROUND:Fondaparinux sodium is a novel antithrombotic agent, the first of a new class of selective factor Xa inhibitors. It has favourable pharmacokinetics including 100% bioavailability, low variability and a mean terminal half-life of 17 hours for young and 21 hours for elderly healthy volunteers, enabling once-da...

journal_title：Clinical pharmacokinetics

authors： Paolucci F,Claviés MC,Donat F,Necciari J

更新日期：2002-01-01 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：:Nintedanib is an oral, small-molecule tyrosine kinase inhibitor approved for the treatment of idiopathic pulmonary fibrosis and patients with advanced non-small cell cancer of adenocarcinoma tumour histology. Nintedanib competitively binds to the kinase domains of vascular endothelial growth factor (VEGF), platelet-de...

journal_title：Clinical pharmacokinetics

authors： Wind S,Schmid U,Freiwald M,Marzin K,Lotz R,Ebner T,Stopfer P,Dallinger C

更新日期：2019-09-01 00:00:00

abstract：:Dilevalol and labetalol are examples of a growing number of new beta-blockers which combine nonselective beta-adrenoceptor antagonism with vasodilator activity. Dilevalol is one of the 4 stereoisomers of labetalol, and is estimated to form approximately 25% of the racemic drug. Labetalol itself is an alpha 1-antagonis...

journal_title：Clinical pharmacokinetics

authors： Donnelly R,Macphee GJ

更新日期：1991-08-01 00:00:00

abstract：:All of the commonly used anticonvulsants drugs, except possibly primidone, are cleared from the human body mainly by metabolism. The metabolites of phenytoin, phenobarbital and ethosuximide have so far not been shown to possess significant pharmacological activity. However, carbamazepine-10,11-epoxide, derived from ca...

journal_title：Clinical pharmacokinetics

authors： Eadie MJ

更新日期：1991-07-01 00:00:00

abstract：BACKGROUND AND OBJECTIVE:Clearance is an important pharmacokinetic concept for scaling dosage, understanding the risks of drug-drug interactions and environmental risk assessment in children. Accurate clearance scaling to children requires prior knowledge of adult clearance mechanisms and the age-dependence of physiolo...

journal_title：Clinical pharmacokinetics

authors： Edginton AN,Schmitt W,Voith B,Willmann S

更新日期：2006-01-01 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

authors： Mackie AE,McDowall JE,Falcoz C,Ventresca P,Bye A,Daley-Yates PT

更新日期：2000-01-01 00:00:00

abstract：OBJECTIVE:To obtain a pharmacokinetic profile of cyclosporin microemulsion formulation in patients with inflammatory bowel disease. PATIENTS AND PARTICIPANTS:58 consecutive patients (19 women and 39 men), aged 16 to 64 years (mean age 38 years), with a diagnosis of ulcerative colitis (29 patients) or Crohn's disease (...

journal_title：Clinical pharmacokinetics

authors： Latteri M,Angeloni G,Silveri NG,Manna R,Gasbarrini G,Navarra P

更新日期：2001-01-01 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

authors： Negro RD

更新日期：1998-08-01 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：:Carboplatin shares some of the therapeutic advantages of cisplatin, but without a significant incidence of the dose-limiting neurotoxicity and nephrotoxicity which is experienced with cisplatin. However, its use is associated with dose-limiting bone marrow suppression. Carboplatin is present in the blood as 3 distinct...

journal_title：Clinical pharmacokinetics

authors： Duffull SB,Robinson BA

更新日期：1997-09-01 00:00:00