Abstract:
AIMS:A recent case report had suggested a citrus soft drink (Sun Drop) may have caused clinically relevant elevations in ciclosporin levels through a grapefruit juice-like mechanism via inactivation of intestinal cytochrome P450 3A4 (CYP3A4). This study was conducted to investigate the effect of grapefruit juice and citrus sodas Sun Drop and Fresca, the latter soda containing 83-fold higher concentration of the proposed CYP3A4 inhibitor bergamottin than Sun Drop, relative to water on oral ciclosporin pharmacokinetics. METHODS:In a randomized four-way crossover study with a washout of at least 1 week, 12 healthy volunteers received a single oral dose of ciclosporin (Neoral) with Sun Drop, Fresca, grapefruit juice and water (control). Each drink (591 ml) was consumed twice on the prior day and three times on the study day. Whole blood concentrations of ciclosporin were measured up to 24 h with a fluorescence polarization immunoassay. RESULTS:Grapefruit juice increased area under the concentration-time curve by 186% (P < 0.0001; 95% confidence interval of mean difference 3302-6240 ng ml h(-1)) and peak concentration by 150% (P < 0.0001) of ciclosporin with a significant decrease in oral clearance of 43% (P < 0.0001) when compared with water. Neither citrus soda altered significantly ciclosporin pharmacokinetic variables; changes in mean values ranged from +/- 3 to 11% of the corresponding water value. CONCLUSION:Although our results do not support a clinically relevant grapefruit juice-like interaction between oral ciclosporin and citrus constituent containing sodas Sun Drop or Fresca, an effect in the setting of chronic ciclosporin therapy cannot be ruled out.
journal_name
Br J Clin Pharmacoljournal_title
British journal of clinical pharmacologyauthors
Schwarz UI,Johnston PE,Bailey DG,Kim RB,Mayo G,Milstone Adoi
10.1111/j.1365-2125.2005.02519.xsubject
Has Abstractpub_date
2006-10-01 00:00:00pages
485-91issue
4eissn
0306-5251issn
1365-2125pii
BCP2519journal_volume
62pub_type
杂志文章,随机对照试验abstract:AIMS:The objective of this study is to develop a generic model for tacrolimus pharmacokinetics modelling using a meta-analysis approach, that could serve as a first step towards a prediction tool to inform pharmacokinetics-based optimal dosing of tacrolimus in different populations and indications. METHODS:A systemati...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章,meta分析
doi:10.1111/bcp.14110
更新日期:2019-12-01 00:00:00
abstract:AIM:Canagliflozin is an SGLT2 inhibitor approved for the treatment of type-2 diabetes. A dynamic population pharmacokinetic-pharmacodynamic (PK/PD) model relating 24-h canagliflozin exposure profiles to effects on glycosylated haemoglobin was developed to compare the efficacy of once-daily and twice-daily dosing. METH...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
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abstract::1 Theories linking 5-hydroxytryptamine (5-HT) with depression are briefly reviewed. The various experimental strategies adopted to investigate this relationship, examination of autopsy data, CSF metabolite data, 5-HT re-uptake patterns in human blood platelets and imipramine binding studies in human platelets, are dis...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1365-2125.1983.tb02130.x
更新日期:1983-01-01 00:00:00
abstract::The pharmacokinetics of CGP 15 210 G, a new 5-HT uptake inhibitor in poor and extensive metabolisers of debrisoquine, give indirect evidence of an association between its metabolism and polymorphic hydroxylation of the debrisoquine type. ...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1365-2125.1985.tb02802.x
更新日期:1985-07-01 00:00:00
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
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abstract:AIMS:To assess the antihistaminic activity of levocetirizine and fexofenadine 2 h and 24 h after drug administration using facial thermography and to compare the results with those using well-established parameters of antihistaminic activity in the nose and skin. METHODS:This was a randomized, double-blind, three-trea...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1111/j.1365-2125.2006.02647.x
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abstract:AIMS:Ibandronate, a highly potent nitrogen-containing bisphosphonate, is the subject of an ongoing clinical development programme that aims to maximize the potential of simplified, less frequent oral and intravenous (i.v.) administration in osteoporosis. A modelling and simulation project was undertaken to characterize...
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pub_type: 杂志文章,meta分析
doi:10.1111/j.1365-2125.2004.02224.x
更新日期:2004-12-01 00:00:00
abstract::1 A new osmotic pressure mediated delivery system for metoprolol (Lopresor Oros) has been evaluated by measuring the haemodynamic effects and pharmacokinetics after single and multiple oral dosing in young healthy volunteers. 2 Similar studies have been carried out in the same group using equivalent single and multipl...
journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1982-03-01 00:00:00
abstract::1 A 'low-dose' combined oral contraceptive steroid (OCS) preparation containing 30 microgram ethinylo-estradiol and 150 microgram levonorgestrel was found to reduce significantly antipyrine clearance in a group of women acting as their own controls. 2 An OCS preparation containing only a progestogen (75 microgram norg...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
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abstract::1 A total of three hundred and nineteen new chemical entities (NCEs) were investigated in man for the first time between 1964 and 1985 by seven UK-owned pharmaceutical companies. The majority (96.2%), were self-originated by the UK company or one of its overseas subsidiaries. 2 There was an increase in the number of N...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1365-2125.1988.tb03318.x
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abstract::1 Five normal subjects received pre-treatment with cimetidine 200 mg three times daily and 400 mg at night for 6 days, or matching placebo. 2 Caffeine (300 mg) was given orally before any treatment and at the beginning of the last day of each treatment course. Treatments were randomly allocated and separated by at lea...
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.1365-2125.1981.tb01194.x
更新日期:1981-08-01 00:00:00
abstract::The effect of acute migraine attack and rectally given metoclopramide on the absorption of orally given tolfenamic acid (300 mg) was investigated in seven female patients in a crossover study consisting of four phases, two without migraine and two during migraine. Metoclopramide hydrochloride (20 mg) or placebo was gi...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1365-2125.1984.tb05001.x
更新日期:1984-01-01 00:00:00
abstract::1 The new converting enzyme inhibitor RHC 3659 was tested in 15 male volunteers. The study consisted of two parts: first, the ability of a single oral dose (5, 10, 20, 40 or 80 mg) to inhibit the pressor response to exogenous angiotensin I was tested with blood pressure and heart rate monitored continuously through an...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1365-2125.1981.tb01327.x
更新日期:1981-12-01 00:00:00
abstract::1 Seventeen men, aged 45-57 yr, with essential hypertension showed obvious and, in the standing position, dose-related reductions in blood pressure during treatment with oral labetalol with weekly dose increments. 2 Pulse rate changes were not related to dose but reduced compared with pre-treatment values. 3 No postur...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:
更新日期:1976-08-01 00:00:00
abstract::1 The effect of pregnancy on the binding of phenytoin and phenobarbitone to serum proteins was studied in normal women and in drug treated epileptic women. 2 The binding of both drugs was reduced during pregnancy. The reduction correlated positively with the gestational age and negatively with the serum albumin concen...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1111/j.1365-2125.1982.tb01420.x
更新日期:1982-04-01 00:00:00
abstract::The effect of a high potency antacid and food on the bioavailability of famotidine was studied in 17 healthy volunteers in an open randomized three-way cross-over trial. After an overnight fast, famotidine was administered to each subject as follows: 40 mg famotidine orally alone; 40 mg orally with antacid; and 40 mg ...
journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
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journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
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journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
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更新日期:2006-05-01 00:00:00
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journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1111/bcp.12828
更新日期:2016-04-01 00:00:00
abstract::Widespread use of cocaine and its attendant toxicity has produced a wealth of benchwork studies and small animal investigations that evaluated the effects of cocaine on the cardiovascular system. Despite this wealth of knowledge, very little is known about the frequency or types of arrhythmias in patients with signifi...
journal_title:British journal of clinical pharmacology
pub_type: 杂志文章,评审
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更新日期:2010-05-01 00:00:00
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journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
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更新日期:2005-11-01 00:00:00
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journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1982-07-01 00:00:00
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journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1997-08-01 00:00:00
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pub_type: 杂志文章,随机对照试验
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更新日期:2008-01-01 00:00:00
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journal_title:British journal of clinical pharmacology
pub_type: 杂志文章
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更新日期:2020-11-01 00:00:00
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journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章
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更新日期:1991-02-01 00:00:00
abstract:AIMS:Voriconazole is a novel triazole with broad-spectrum antifungal activity. It is likely that some patients receiving voriconazole may also require treatment with the anticoagulant warfarin. Cytochrome P450 isoenzymes are important in the metabolism of both these drugs. This study investigated the effect of voricona...
journal_title:British journal of clinical pharmacology
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:2003-12-01 00:00:00
abstract::1. The efficacy of felodipine a new calcium channel blocker with selective vasodilator activity in the management of severe low output cardiac failure, secondary to coronary heart disease, was determined in 10 patients. 2. Haemodynamic measurements were made at rest and during dynamic exercise and left ventricular fun...
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pub_type: 杂志文章
doi:10.1111/j.1365-2125.1988.tb05254.x
更新日期:1988-06-01 00:00:00