Abstract：
OBJECTIVE:We sought to quantify the influence of the CYP3A inhibitor erythromycin on the pharmacokinetics of everolimus, a CYP3A substrate. METHODS:This was a two-period, single-sequence, crossover study in 16 healthy subjects. In period 1, subjects received the reference treatment of a single 2-mg dose of everolimus. In period 2, they received the test treatment of erythromycin 500 mg three times daily for a total of 9 days and a single 2-mg dose of everolimus coadministered on the fifth day of erythromycin therapy. The test/reference ratio and 90% confidence interval (CI) were derived for everolimus C (max) and AUC. RESULTS:During erythromycin coadministration, everolimus C (max) increased 2.0-fold (90% CI, 1.8-2.3) from 20+/-5 ng/ml to 40+/-10 ng/ml. Everolimus AUC increased 4.4-fold (90% CI, 3.5-5.4) from 116+/-37 ng h/ml to 524+/-225 ng h/ml. Everolimus half-life was prolonged by 39% from 32+/-6 h to 44+/-6 h. Erythromycin predose concentrations were not changed after single-dose administration of everolimus. CONCLUSION:Multiple-dose erythromycin increased single-dose everolimus blood levels by an average 4.4-fold (range, 2.0-12.6). During erythromycin treatment, a compensatory everolimus dose reduction should be made guided by everolimus therapeutic drug monitoring.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Kovarik JM,Beyer D,Bizot MN,Jiang Q,Shenouda M,Schmouder RLdoi
10.1007/s00228-004-0866-5subject
Has Abstractpub_date
2005-03-01 00:00:00pages
35-8issue
1eissn
0031-6970issn
1432-1041journal_volume
61pub_type
临床试验,杂志文章abstract：:We have evaluated the pharmacokinetics of high doses of clonidine, as used in the prophylactic treatment of alcohol withdrawal syndrome, in 11 alcohol-dependent patients undergoing surgery for oesophagogastrectomy. Clonidine was given in a bolus of 150 micrograms followed by a continuous infusion. After a mean period ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00315500
更新日期：1993-01-01 00:00:00
abstract：:Pharmacokinetic and pharmacodynamic properties of a new controlled-release (CR) formulation of metoprolol have been compared with those of atenolol. Metoprolol CR (100 mg and 200 mg), atenolol (50 mg and 100 mg) and placebo were each given once daily for four days in a double-blind, cross-over study to ten healthy men...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00578408
更新日期：1988-01-01 00:00:00
abstract：:Atenolol 100 mg and penbutolol 40 mg given once a day were both effective in controlling moderate hypertension, as judged by a randomised controlled, double-blind trial in 45 patients treated for six weeks. Both drugs significantly reduced the resting supine and erect blood pressures. No serious adverse effects could ...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF00637507
更新日期：1981-01-01 00:00:00
abstract：PURPOSE:To investigate possible differences in the time course of vasodilating effects of atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP) in humans. METHODS:We measured forearm blood flow (FBF) by strain gauge plethymography and cyclic GMP spillover during and after intra-arterial infusions of BNP...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00228-008-0516-4
更新日期：2008-09-01 00:00:00
abstract：:The effects of the ingestion of food and digoxin on the cardiovascular system alone and in combination have been observed in eight healthy subjects. A positive inotropic response was seen following food (2.5 MJ) and intravenous digoxin (0.01 mg/kg) with significant decreases in QS2Index (QS2I) pre-ejection period (PEP...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00615959
更新日期：1986-01-01 00:00:00
abstract：PURPOSE:To assess the effect of a small economic inducement on the rate of spontaneous reporting of adverse drug reactions (ADRs) and the attitudes of general practitioners and physicians towards reporting of ADRs. METHOD:One intervention and one control county were selected for the study. Written information about th...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-005-0072-0
更新日期：2006-05-01 00:00:00
abstract：:In 6 normal volunteers given single oral doses of 250,500 and 1000 mg ticlopidine (T), the peak plasma level of unchanged drug was reached after about 2 h. There was no correlation between the plasma T level and its inhibitory effect on platelet function, expressed as % inhibition of ADP-induced aggregation. By means ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00626364
更新日期：1991-01-01 00:00:00
abstract：:Four subjects received 5 mg 14C-glipizide orally, 3 subjects 1 mg intravenously and 2 subjects 5 mg 14C-glibenclamide orally. Plasma levels of radioactivity, and urinary and faecal excretion were measured. For both drugs the disappearance of radioactivity from plasma followed complex kinetics and the apparent half-liv...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00616416
更新日期：1975-01-01 00:00:00
abstract：:The effect of treatment with diflunisal on the steady-state pharmacokinetics of indomethacin has been studied in 16 healthy volunteers. The steady-state plasma concentration and AUC of indomethacin were significantly increased two- to threefold during treatment with diflunisal and its total clearance and total volume ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00558077
更新日期：1989-01-01 00:00:00
abstract：PURPOSE:Pre-clinical experiments have shown that almorexant, a dual orexin receptor antagonist, is able to inhibit cytochrome P450 3A4 (CYP3A4). Therefore, a study was conducted to investigate the effects of multiple-dose almorexant on the pharmacokinetics of midazolam and simvastatin, two CYP3A4 model substrates. MET...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,随机对照试验
doi：10.1007/s00228-012-1403-6
更新日期：2013-03-01 00:00:00
abstract：PURPOSE:The survival of esophageal and gastric cancer patients treated with chemotherapy is rarely assessed outside of clinical trials. Therefore, we compared the effectiveness of various curative or palliative chemotherapy regimens on the survival of esophageal and gastric cancer patients in a "real world" clinical se...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-020-02883-3
更新日期：2020-07-01 00:00:00
abstract：:We have investigated the prevalence of poor metabolisers (PM) of S-mephenytoin in 373 unrelated, healthy Spanish Caucasian subjects, based on the enantiomeric S/R mephenytoin ratio in urine collected 0-8 h and 24-32 h after intake of the racemic drug. Five of the subjects were PM (1.34%, 95% confidence interval 0.18-2...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF02440867
更新日期：1993-01-01 00:00:00
abstract：:We have studied pharmacokinetics of a new H2-receptor antagonist, TZU-0460, in patients with varying degrees of renal impairment. The apparent volume of distribution at steady-state was 1.70 l/kg, and the plasma protein binding of TZU-0460 or its active metabolite, desacetyl TZU-0460 was less than 10% in normal subjec...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00608220
更新日期：1986-01-01 00:00:00
abstract：PURPOSE:To study the impact of gemfibrozil co-administration on the pharmacokinetics of sitagliptin in healthy Indian male volunteers. METHODS:A randomized open label two-period crossover study involving 12 healthy Indian male volunteers was conducted at a single center. In each phase, the volunteers were administered...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/s00228-011-1177-2
更新日期：2012-05-01 00:00:00
abstract：OBJECTIVE:To analyse whether first-time use of antidepressants (incidence) and selection of TCAs (tricyclic antidepressants) versus new-generation drugs are associated with socio-economic status and psychiatric history. METHOD:We conducted a population-based cohort study using registry data covering Funen County, Denm...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-003-0723-y
更新日期：2004-03-01 00:00:00
abstract：:The cardiovascular and respiratory actions of the adrenergic beta adrenoceptive drug sotalol have been studied in an open, short term trial. Fifteen patients with angina performed standardized orthostatic and exercise tests before and after injection of 20 mg sotalol intravenously. Although there was a significant red...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00562313
更新日期：1975-08-14 00:00:00
abstract：PURPOSE:Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated for ovarian and metastatic breast cancer. Increased serum creatinine levels have been observed in patients taking olaparib, but the underlying mechanism is unknown. This study aimed to investigate if patients receiving olaparib have increased...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-020-03070-0
更新日期：2021-02-01 00:00:00
abstract：:The effect of the angiotensin converting enzyme inhibitor, perindopril, on autonomic function was assessed in a double blind, placebo controlled, crossover study in 10 normotensive males. Eight milligram of perindopril given orally lowered blood pressure without a change in heart rate. Perindopril enhanced the vagally...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00614298
更新日期：1986-01-01 00:00:00
abstract：:The aim of this multicentre randomised double blind study was to compare the efficacy and safety of the 200-300 mg sustained release diltiazem formulation administered once daily (200-300 SR) with standard diltiazem (D) given three or four times daily to patients with stable angina. Patients aged 59 years, with a repr...
journal_title：European 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：10.1007/BF00193700
更新日期：1995-01-01 00:00:00
abstract：:A survey among hospital staff physicians was conducted in order to evaluate their attitudes towards systemic antimicrobial agents. Direct questions about the value of different agents and choice within pairs of antimicrobial drugs, stating the reasons for the preference, were included in the questionnaire used. Gentam...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00609876
更新日期：1979-03-26 00:00:00
abstract：:To elucidate the effect of Nicorandil on myocardial energy metabolism and myocardial sympathetic activity, we administered Nicorandil orally to eight patients with angina pectoris prior to exercise testing. Arterial and coronary sinus levels of lactate, ammonia, hypoxanthine (HX), adrenaline and noradrenaline were mea...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00198297
更新日期：1995-01-01 00:00:00
abstract：OBJECTIVE:Use of analgesic drugs in acute renal colic varies widely in different countries. In order to assess the prescribing patterns in acute renal colic in French emergency departments (EDs), the present study compared intentions of prescription, real prescription and evidence-based data in a sample of emergency pr...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s002280100366
更新日期：2001-11-01 00:00:00
abstract：OBJECTIVE:To determine the pharmacokinetics and organ distribution of i.v. and oral methylene blue, which is used to prevent ifosfamide-induced encephalopathy in oncology. METHODS:The concentration of methylene blue in whole blood was measured using high-performance liquid chromatography in seven volunteers after i.v....
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s002280000124
更新日期：2000-06-01 00:00:00
abstract：:Individual variation in the half-life of caffeine in the body was measured by HPLC analysis of saliva samples. The mean for adult males and non-pregnant females was 3.4 h (range 2-5 h, n = 25), and 8.3 h (range 3-16 h, n = 57) for pregnant women. After delivery, in most cases the values returned to normal within one m...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00637512
更新日期：1981-01-01 00:00:00
abstract：:In healthy normal subjects following the administration of labetalol the pharmacological effects were measured and compared with the plasma concentrations achieved. The inhibition of exercise induced tachycardia and inhibition of exercise induced increases in systolic pressure were significantly related to the adminis...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00562897
更新日期：1977-01-03 00:00:00
abstract：:The Danish retail pharmacies' drug subsidy system is completely computerized. The data are person-identifiable, making it possible to chart the population's drug use from the perspective of individual users. We decided to explore the potential of this data source and to analyse heavy drug users specifically. The analy...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00191170
更新日期：1994-01-01 00:00:00
abstract：OBJECTIVE:To study the effects of possible interactions between levosimendan and warfarin on pharmacokinetics and pharmacodynamics. Furthermore, the effects of levosimendan on blood coagulation were investigated. METHODS:Open, randomised cross-over design with two treatment phases was used. During one phase, levosimen...
journal_title：European 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：2000-12-01 00:00:00
abstract：PURPOSE:Serotonin receptor 1B (HTR1B) is involved in the regulation of the serotonin system, playing different roles in specific areas of the brain. We review the characteristics of the gene coding for HTR1B, its product and the functional role of HTR1B in the neural networks involved in motivation and memory; the cent...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,评审
doi：10.1007/s00228-009-0724-6
更新日期：2010-01-01 00:00:00
abstract：:The kinetics of 14C-metformin have been studied in five healthy subjects after oral and intravenous administration. The intravenous dose was distributed to a small central compartment of 9.9 +/- 1.61 (X +/- SE), from which its elimination could be described using three-compartment open model. The elimination half-life...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00562061
更新日期：1979-09-01 00:00:00
abstract：:The most convenient route of drug administration is peroral. To reach their target, drug molecules must be absorbed from the gastrointestinal tract and enter the systemic circulation in sufficient quantities. For this reason, understanding and anticipating the mechanisms and factors affecting gastrointestinal absorpti...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,评审
doi：10.1007/s002280100369
更新日期：2001-11-01 00:00:00
