No significant effect of ABCB1 haplotypes on the pharmacokinetics of fluvastatin, pravastatin, lovastatin, and rosuvastatin.

Abstract:

AIMS:This study aimed to investigate possible effects of ABCB1 genotype on fluvastatin, pravastatin, lovastatin, and rosuvastatin pharmacokinetics. METHODS:In a fixed-order crossover study, 10 healthy volunteers with the ABCB1 c.1236C/C-c.2677G/G-c.3435C/C (CGC/CGC) genotype and 10 with the c.1236T/T-c.2677T/T-c.3435T/T (TTT/TTT) genotype ingested a single 20-mg dose of fluvastatin, pravastatin, lovastatin, and rosuvastatin. Plasma fluvastatin, pravastatin, and lovastatin concentrations were measured up to 12 h and plasma and urine rosuvastatin concentrations up to 48 and 24 h, respectively. RESULTS:The ABCB1 genotype had no significant effect on the pharmacokinetics of any of the investigated statins. The geometric mean ratio (95% confidence interval) of the area under the plasma concentration-time curve from 0 h to infinity (AUC(0-infinity)) in participants with the TTT/TTT genotype to that in those with the CGC/CGC genotype was 0.96 (0.77, 1.20; P= 0.737) for fluvastatin, 0.92 (0.53, 1.62; P= 0.772) for pravastatin, 0.83 (0.36, 1.90; P= 0.644) for lovastatin, 1.25 (0.72, 2.17; P= 0.400) for lovastatin acid, and 1.10 (0.73, 1.65; P= 0.626) for rosuvastatin. The AUC(0-infinity) of lovastatin acid correlated significantly with that of rosuvastatin (r= 0.570, P= 0.009), but none of the other AUC(0-infinity) pairs showed a significant correlation. CONCLUSIONS:These data suggest that the ABCB1 c.1236C-c.2677G-c.3435C and c.1236T-c.2677T-c.3435T haplotypes play no significant role in the interindividual variability in the pharmacokinetics of fluvastatin, pravastatin, lovastatin, and rosuvastatin.

journal_name

Br J Clin Pharmacol

authors

Keskitalo JE,Kurkinen KJ,Neuvonen M,Backman JT,Neuvonen PJ,Niemi M

doi

10.1111/j.1365-2125.2009.03440.x

subject

Has Abstract

pub_date

2009-08-01 00:00:00

pages

207-13

issue

2

eissn

0306-5251

issn

1365-2125

pii

BCP3440

journal_volume

68

pub_type

杂志文章
  • Beta-adrenoceptor responsiveness in hypertension: effects of dietary NaCl intake.

    abstract::1. Adrenergic responsiveness may be an important determinant of peripheral resistance in man. We have demonstrated that vascular beta-adrenergic responsiveness is reduced in young borderline hypertensive subjects. A parallel defect in beta-adrenergic mediated adenylyl cyclase activity and beta-adrenoceptor affinity fo...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1365-2125.1990.tb05469.x

    authors: Feldman RD

    更新日期:1990-01-01 00:00:00

  • The influence of protein containing meals on the pharmacokinetics of levodopa in healthy volunteers.

    abstract::1. The pharmacokinetics of levodopa and paracetamol after single oral doses have been investigated in eight healthy young volunteers in the fasted state and following isocaloric meals containing either 10.5 g or 30.5 g of protein. 2. The initial peak and maximum plasma drug concentrations and the times at which these ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1991.tb05555.x

    authors: Robertson DR,Higginson I,Macklin BS,Renwick AG,Waller DG,George CF

    更新日期:1991-04-01 00:00:00

  • Adverse drug reactions in elderly patients.

    abstract::Many studies from around the world show a correlation between increasing age and adverse drug reaction (ADR) rate, at least for some medical conditions. More than 80% of ADRs causing admission or occurring in hospital are type A (dose-related) in nature, and thus predictable from the known pharmacology of the drug and...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1046/j.1365-2125.2003.01875.x

    authors: Routledge PA,O'Mahony MS,Woodhouse KW

    更新日期:2004-02-01 00:00:00

  • Effect of charcoal-drug ratio on antidotal efficacy of oral activated charcoal in man.

    abstract::The effect of charcoal-drug ratio on the antidotal efficacy of oral activated charcoal was studied in six healthy volunteers in a randomized cross-over study and compared with the adsorption capacity of activated charcoal in vitro. Aminosalicylic acid (PAS) 1 g and 5 g were ingested on an empty stomach in 30 ml of wat...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1985.tb02712.x

    authors: Olkkola KT

    更新日期:1985-06-01 00:00:00

  • Evaluation of the effect on heart rate variability of a beta2-adrenoceptor agonist and antagonist using non-linear scatterplot and sequence methods.

    abstract:AIMS:To examine the impact on heart rate variability (HRV), of agonism or antagonism at the cardiac beta2-adrenoceptor in healthy volunteers, using standard time-domain summary statistics and non-linear methods (scatterplot and quadrant analysis). METHODS:Under double-blind and randomised conditions (Latin square desi...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1046/j.1365-2125.1999.00862.x

    authors: Hanratty CG,Silke B,Riddell JG

    更新日期:1999-02-01 00:00:00

  • Efficacy, safety and pharmacokinetics of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control.

    abstract:AIMS:The objectives were to investigate the pharmacokinetics, pharmacodynamics and safety of ilaprazole infusion in healthy subjects and patients with esomeprazole as positive control, and then recommend the dosage regimen for Phase 2b/3 studies. METHODS:Three clinical studies were performed. First, 16 healthy subject...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1111/bcp.14076

    authors: Wang H,Shao F,Liu X,Xu W,Ou N,Qin X,Liu F,Hou X,Hu H,Jiang J

    更新日期:2019-11-01 00:00:00

  • A study of the effects of atenolol and propranolol on renal function in patients with essential hypertension.

    abstract::1 The effects of propranolol and atenolol given in random order in a cross-over study to fifteen patients with essential hypertension have been studied. 2 Both drugs were effective in lowering blood pressure and side effects were not markedly different. 3 There was no change in exchangeable sodium or potassium or in t...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1980.tb00501.x

    authors: Wilkinson R,Stevens IM,Pickering M,Robson V,Hawkins T,Kerr DN,Harry JD

    更新日期:1980-07-01 00:00:00

  • Plasma melatonin during desmethylimipramine treatment: evidence for changes in noradrenergic transmission.

    abstract::Plasma melatonin was used to determine overall beta-adrenergic transmission through pineal neuro-effector junctions during desmethylimipramine (DMI) treatment in 10 normal subjects. Changes in plasma melatonin indicated that an initial increase in noradrenaline (NA) transmission produced by DMI was counteracted by ada...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1985.tb02717.x

    authors: Cowen PJ,Green AR,Grahame-Smith DG,Braddock LE

    更新日期:1985-06-01 00:00:00

  • Rapid screening for polymorphisms in dextromethorphan and mephenytoin metabolism.

    abstract::1. The phenotyping parameters for dextromethorphan and mephenytoin were assessed in 48 normal male volunteers following administration of each metabolic probe drug on separate occasions and together according to a randomized 3-way crossover design. 2. Neither the urinary S-/R-mephenytoin ratio nor the dextromethorphan...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1990.tb03653.x

    authors: Guttendorf RJ,Britto M,Blouin RA,Foster TS,John W,Pittman KA,Wedlund PJ

    更新日期:1990-04-01 00:00:00

  • Multifactorial pharmacogenetic analysis in colorectal cancer patients receiving 5-fluorouracil-based therapy together with cetuximab-irinotecan.

    abstract:AIM:To examine the predictive value of gene polymorphisms potentially linked to toxicity, clinical response, time to progression and overall survival, following cetuximab-tegafur-uracil (UFT)-irinotecan therapy. METHODS:Fifty-two patients with advanced colorectal cancer were enrolled in an ancillary pharmacogenetic st...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2011.04141.x

    authors: Etienne-Grimaldi MC,Bennouna J,Formento JL,Douillard JY,Francoual M,Hennebelle I,Chatelut E,Francois E,Faroux R,El Hannani C,Jacob JH,Milano G

    更新日期:2012-05-01 00:00:00

  • Effect of age on the pharmacokinetics of duloxetine in women.

    abstract:AIMS:The effect of age on duloxetine pharmacokinetics was evaluated in healthy volunteers and in patients with urinary incontinence. METHODS:Twenty-four healthy subjects (12 women 65-77 years, and 12 women 32-50 years) were given a single 40-mg oral dose of duloxetine in Study 1. Plasma concentration-time data were an...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,多中心研究,随机对照试验

    doi:10.1046/j.1365-2125.2003.01963.x

    authors: Skinner MH,Kuan HY,Skerjanec A,Seger ME,Heathman M,O'Brien L,Reddy S,Knadler MP

    更新日期:2004-01-01 00:00:00

  • Effects of single green tea ingestion on pharmacokinetics of nadolol in healthy volunteers.

    abstract:AIMS:The aim of this study was to investigate the effects of a single green tea (GT), administered concomitantly or 1 hour before nadolol intake on nadolol pharmacokinetics. METHODS:In a randomized 3-phase crossover study, 11 healthy volunteers received an oral administration of nadolol with, or 1 hour after preingest...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.14315

    authors: Misaka S,Abe O,Ono T,Ono Y,Ogata H,Miura I,Shikama Y,Fromm MF,Yabe H,Shimomura K

    更新日期:2020-11-01 00:00:00

  • Effectiveness, safety and cost of drug substitution in hypertension.

    abstract::Cost-containment measures in healthcare provision include the implementation of therapeutic and generic drug substitution strategies in patients whose condition is already well controlled with pharmacotherapy. Treatment for hypertension is frequently targeted for such measures. However, drug acquisition costs are only...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2010.03681.x

    authors: Johnston A,Stafylas P,Stergiou GS

    更新日期:2010-09-01 00:00:00

  • Morphine metabolism in neonates and infants.

    abstract::The metabolism of morphine was studied in seven fullterm neonates and five infants receiving a continuous infusion of morphine. All the patients had detectable plasma concentrations of morphine 3-glucuronide (M3G) and 10 had detectable concentrations of morphine 6-glucuronide (M6G). The mean plasma clearance of morphi...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1992.tb05652.x

    authors: Choonara I,Lawrence A,Michalkiewicz A,Bowhay A,Ratcliffe J

    更新日期:1992-11-01 00:00:00

  • Pharmacokinetics of phenytoin in children.

    abstract::1 Apparent Vmax and Km for phenytoin were estimated in 40 children (aged 8--33 months) and 21 adults (aged 18--66 years). 2 The derived values of Vmax and Km were used to predict the plasma and salivary concentrations of phenytoin following a change in dose. There was a highly significant correlation between observed ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1981.tb01285.x

    authors: Blain PG,Mucklow JC,Bacon CJ,Rawlins MD

    更新日期:1981-11-01 00:00:00

  • A preliminary study of the effect of norfenfluramine on lipogenesis by human adipose tissue in vitro.

    abstract::1 Norfenfluramine is thought to be the major active metabolite of fenfluramine in man. Therefore its in vitro effect on lipogenesis in human adipose tissue from twelve patients was investigated. 2 Although inhibition of lipogenesis was demonstrated, the concentrations of norfenfluramine necessary (>1 mM) were much hig...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1974.tb00279.x

    authors: Ashwell M

    更新日期:1974-10-01 00:00:00

  • Maprotiline metabolism appears to co-segregate with the genetically-determined CYP2D6 polymorphic hydroxylation of debrisoquine.

    abstract::The plasma concentrations of the tetracyclic antidepressant maprotiline and its effect on histamine-induced bronchoconstriction were measured after single (50 mg) and multiple (50 mg twice daily) oral doses in healthy subjects. Histamine-induced bronchoconstriction was abolished after a single dose of maprotiline and ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1994.tb04293.x

    authors: Firkusny L,Gleiter CH

    更新日期:1994-04-01 00:00:00

  • Delta-9-tetrahydrocannabinol and gastric emptying.

    abstract::The effects of delta-9-tetrahydrocannabinol (0.5 and 1 mg i.v.) on gastric emptying of liquid were investigated in seven normal volunteers and compared with placebo. Despite significant change in pulse rate and psychological parameters consistent with cannabis activity there was no significant effect on the pattern of...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1983.tb01561.x

    authors: Bateman DN

    更新日期:1983-06-01 00:00:00

  • Dose-linearity of the pharmacokinetics of an intravenous [14 C]midazolam microdose in children.

    abstract:AIMS:Drug disposition in children may vary from adults due to age-related variation in drug metabolism. Microdose studies present an innovation to study pharmacokinetics (PK) in paediatrics; however, they should be used only when the PK is dose linear. We aimed to assess dose linearity of a [14 C]midazolam microdose, b...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,多中心研究

    doi:10.1111/bcp.14047

    authors: van Groen BD,Vaes WH,Park BK,Krekels EHJ,van Duijn E,Kõrgvee LT,Maruszak W,Grynkiewicz G,Garner RC,Knibbe CAJ,Tibboel D,de Wildt SN,Turner MA

    更新日期:2019-10-01 00:00:00

  • Effect of beta-adrenoceptor agents on the blood flow in carotid arteries in normal volunteers.

    abstract::The effects on carotid artery blood flow of atenolol (a selective beta 1-adrenoceptor antagonist) and xamoterol (a beta 1-adrenoceptor partial agonist with 43% agonist activity) were measured using a Doppler technique in eight healthy volunteers. Atenolol produced a decrease in blood pressure and blood velocity flow, ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1989.tb03578.x

    authors: Fitzgerald DE,Harry JD

    更新日期:1989-01-01 00:00:00

  • Population pharmacokinetic/pharmacodynamic analysis of CCR5 receptor occupancy by maraviroc in healthy subjects and HIV-positive patients.

    abstract:BACKGROUND:Maraviroc, a noncompetitive antagonist of the CCR5 coreceptor, was recently approved in the USA as a treatment of HIV infection. For antiretroviral agents that target the virus, antiviral effect can be related to some extent to plasma drug concentrations. For CCR5 antagonists that target the host cells, rece...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1111/j.1365-2125.2008.03140.x

    authors: Rosario MC,Jacqmin P,Dorr P,James I,Jenkins TM,Abel S,van der Ryst E

    更新日期:2008-04-01 00:00:00

  • Prospective validation of a model-informed precision dosing tool for vancomycin in intensive care patients.

    abstract:AIMS:Vancomycin is an important antibiotic for critically ill patients with Gram-positive bacterial infections. Critically ill patients typically have severely altered pathophysiology, which leads to inefficacy or toxicity. Model-informed precision dosing may aid in optimizing the dose, but prospectively validated tool...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.14360

    authors: Ter Heine R,Keizer RJ,van Steeg K,Smolders EJ,van Luin M,Derijks HJ,de Jager CPC,Frenzel T,Brüggemann R

    更新日期:2020-12-01 00:00:00

  • Antidepressant use and risk of coronary heart disease: meta-analysis of observational studies.

    abstract:AIMS:Our goal was to evaluate the association between antidepressant use and the risk of coronary heart disease (CHD) among subjects with no history of coronary heart disease. METHODS:A search of Medline, EMBASE, PsycINFO and the Cochrane Library was performed in January 2013. Two authors independently reviewed and se...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1111/bcp.12383

    authors: Oh SW,Kim J,Myung SK,Hwang SS,Yoon DH

    更新日期:2014-10-01 00:00:00

  • Sildenafil improves renal function in patients with pulmonary arterial hypertension.

    abstract:AIM:Elevated serum creatinine (sCr) and low estimated glomerular filtration rate (eGFR) are associated with poor outcomes in patients with pulmonary arterial hypertension (PAH) whereas sildenafil treatment improves PAH outcomes. This post hoc analysis assessed the effect of sildenafil on kidney function and links with ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,多中心研究,随机对照试验

    doi:10.1111/bcp.12616

    authors: Webb DJ,Vachiery JL,Hwang LJ,Maurey JO

    更新日期:2015-08-01 00:00:00

  • Effects of xamoterol on resting and exercise haemodynamics in patients with chronic heart failure.

    abstract::1. A bicycle exercise test was used to investigate functional capability and haemodynamics in 30 patients with heart failure (13 NYHA Class II, 17 Class III), before and after i.v. xamoterol (Corwin, Carwin, Corwil, Xamtol, ICI 118,587) 0.2 mg kg-1. 2. Resting heart rate fell from 78 to 74 beats min-1 (P less than 0.0...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Virk SJ,Davies MK

    更新日期:1989-01-01 00:00:00

  • Selective beta-adrenoceptor partial agonist effects of pindolol and xamoterol on skeletal muscle assessed by plasma creatine kinase changes in healthy subjects.

    abstract::1. The effects of selective beta-adrenoceptor partial agonist activity on plasma creatine kinase (CK) and skeletal muscle symptoms were studied in normal volunteers. 2. A drug with beta 1-selective partial agonist activity (xamoterol) and one with partial agonist activity acting mainly through beta 2-adrenoceptors (pi...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1990.tb03834.x

    authors: Tomlinson B,Cruickshank JM,Hayes Y,Renondin JC,Lui JB,Graham BR,Jones A,Lewis AD,Prichard BN

    更新日期:1990-11-01 00:00:00

  • Clinical pharmacological studies with prazosin during pregnancy complicated by hypertension.

    abstract::The disposition and effect of orally administered prazosin have been studied in eight women with hypertension which was uncontrolled by beta-adrenoceptor blockade during the last trimester of pregnancy. Results were compared with healthy men of similar age. The median time to peak concentration was 165 min during preg...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1983.tb02213.x

    authors: Rubin PC,Butters L,Low RA,Reid JL

    更新日期:1983-11-01 00:00:00

  • Plasma concentrations and ocular effects of cyclopentolate after ocular application of three formulations.

    abstract::1. Eight volunteers received in randomized order two 30 microliters drops of either 1% w/v cyclopentolate hydrochloride or a corresponding amount of cyclopentolate polygalacturonate in saline or in acetate buffer in one eye. Cyclopentolate concentrations in plasma were measured by a radioreceptor assay. 2. Peak plasma...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1993.tb04173.x

    authors: Lahdes K,Huupponen R,Kaila T,Monti D,Saettone MF,Salminen L

    更新日期:1993-05-01 00:00:00

  • Integrated semi-physiological pharmacokinetic model for both sunitinib and its active metabolite SU12662.

    abstract:AIMS:Previously published pharmacokinetic (PK) models for sunitinib and its active metabolite SU12662 were based on a limited dataset or lacked important elements such as correlations between sunitinib and its metabolite. The current study aimed to develop an improved PK model that circumvented these limitations and to...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.12550

    authors: Yu H,Steeghs N,Kloth JS,de Wit D,van Hasselt JG,van Erp NP,Beijnen JH,Schellens JH,Mathijssen RH,Huitema AD

    更新日期:2015-05-01 00:00:00

  • Why are converting enzyme inhibitors vasodilators?

    abstract::1. The primary action of the converting enzyme inhibitors to prevent the formation of angiotensin II can explain a decrease in peripheral vascular resistance in patients with elevated, but not in those with normal or reduced plasma renin levels. 2. The inhibition of the breakdown of bradykinin will potentiate the vaso...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1365-2125.1989.tb03585.x

    authors: Vanhoutte PM,Auch-Schwelk W,Biondi ML,Lorenz RR,Schini VB,Vidal MJ

    更新日期:1989-01-01 00:00:00