Abstract:
:The effect of drinking grapefruit juice on the acute pharmacokinetic and haemodynamic actions of the dihydropyridine calcium antagonist felodipine given as a 5 mg plain tablet has been studied in nine, healthy, middle-aged males. Compared to water, grapefruit juice caused an increase in Cmax from mean 6 to 16 nmol.l-1, and in the AUC from 23 to 65 nmol.h.l-1. The change in AUC corresponded to an increase in the systemic availability of felodipine from 15 to 45%, assuming no change in its clearance. This change was probably caused by inhibition of the oxidation of felodipine to the inactive dehydrofelodipine by flavonoids in grapefruit juice. The interaction with grapefruit juice is believed to be a class effect for the dihydropyridines, as oxidation of the dihydropyridine ring to the corresponding pyridine derivative is a major metabolic route for all these drugs. The higher plasma concentrations of felodipine taken with grapefruit juice resulted in a greater change in blood pressure measured in the morning 3 h after dosing (-9%) than did water (0%).
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Edgar B,Bailey D,Bergstrand R,Johnsson G,Regårdh CGdoi
10.1007/BF00266354subject
Has Abstractpub_date
1992-01-01 00:00:00pages
313-7issue
3eissn
0031-6970issn
1432-1041journal_volume
42pub_type
杂志文章abstract::The relationship between the serum protein binding of carbamazepine (CBZ) and carbamazepine-10,11 epoxide (CBZ-E) and the concentration of alpha 1-acid glycoprotein (AAG) and albumin (HSA) was examined in 39 CBZ-treated epileptic children aged 4 months to 12 years. A significant inverse correlation was found between t...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00547424
更新日期:1985-01-01 00:00:00
abstract::The linearity of the pharmacokinetics of the metamizol metabolites 4-methyl-amino-antipyrine (4-MAA), 4-amino-antipyrine (4-AA), 4-formyl-aminoantipyrine (4-FAA), and 4-acetyl-amino-antipyrine (4-AcAA) has been studied after administration to 15 healthy male volunteers of single oral doses of 750, 1500, and 3000 mg me...
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/BF00314805
更新日期:1990-01-01 00:00:00
abstract::The diabetogenic effect of deflazacort (DF), an oxazolinic synthetic corticosteroid, was studied in 12 healthy adult subjects with a positive family history of diabetes mellitus. Three oral glucose tests (oGTT) were performed at 9.00 a.m., after a 12 h fast, following randomized administration of Placebo (PL), or Defl...
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/BF00542555
更新日期:1982-01-01 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:BACKGROUND:Cytochrome P450 2C9 (CYP2C9) allelic variant carriers have been shown to experience hyper-responsiveness to small doses of oral anticoagulants (OAs) (warfarin or acenocoumarol) and a higher bleeding rate. OBJECTIVES:To determine the relative frequencies of different risk factors for OA overdose including di...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-002-0538-2
更新日期:2003-03-01 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:OBJECTIVE:To assess the initial uptake in use and co-prescribing patterns of sildenafil. METHODS:We examined prescription details of the Eastern Health Board Region (including Dublin) of the General Medical Services (GMS) in Ireland, which provides detail on prescriptions dispensed in primary care for this population ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280000255
更新日期:2001-03-01 00:00:00
abstract::The effect of indenolol on heart rate and blood pressure at rest and after submaximal workload has been studied in 19 patients with established essential hypertension. A stepwise increase from moderate to submaximal exercise was chosen to mimic challenges normally occurring in daily life. After 4 weeks of once a day i...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/BF00544058
更新日期:1985-01-01 00:00:00
abstract::Plasma concentrations of caffeine and theophylline were simultaneously determined in 17 preterm infants after oral administration of aminophylline for treatment of apnoea. The ratio of caffeine/theophylline concentration in plasma increased during the first 2 weeks of treatment, owing to the longer time required for c...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00610057
更新日期:1983-01-01 00:00:00
abstract::The four sulphonamides studied--furosemide, tolbutamide, sulfafurazole and sulfonamidochlorobenzoic acid--bind to human albumin at the same sites but with decreasing affinity. These sites are also common to other drugs, namely acenocoumarin, chlorophenoxyisobutyric acid, phenylbutazone and warfarin. In plasma, the fou...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00609473
更新日期:1976-06-15 00:00:00
abstract:PURPOSE:To investigate interindividual variability in response to pain treatment, we characterized postoperative patients for morphine metabolism and for COMT, OPRM1 and UGT2B7 polymorphisms. METHODS:A total of 109 patients treated with morphine were genotyped by DNA sequencing for 12 DNA polymorphisms of the COMT, OP...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00228-013-1523-7
更新日期:2013-09-01 00:00:00
abstract:OBJECTIVES:To analyse reports of drug-induced myocardial infarction and chest pain sent to a national reporting centre. To review which drugs were suspected of exhibiting these adverse events and what mechanisms were involved. METHODS:During the 20-year period 1975 through 1994, a total of 19,141 reports on adverse re...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1007/s002280050346
更新日期:1997-01-01 00:00:00
abstract:PURPOSE:A variety of diagnostic methods are available to validate the performance of population pharmacokinetic models. Internal validation, which applies these methods to the model building dataset and to additional data generated through Monte Carlo simulations, is often sufficient, but external validation, which req...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-020-03036-2
更新日期:2020-11-11 00:00:00
abstract::The effect of spironolactone on cardiac contractility indices was studied by externally recording systolic time intervals in four digitalized and four non-digitalized patients with ischaemic heart disease. A negative inotropic effect was found after spironolactone 100mg b.i.d. in all eight patients, as measured by an ...
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/BF00637612
更新日期:1982-01-01 00:00:00
abstract::The aim of laboratory screening in Phase I is to exclude subjects with subclinical illness, who might be at increased risk in the study, and who might also adversely influence interpretation of the results. A new method for laboratory screening, based on Bayesian probability theory, is proposed, which consists of: 1. ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00280939
更新日期:1990-01-01 00:00:00
abstract::The effects of metolazone on the protein binding of glibenclamide were studied. It was found that increasing metolazone concentrations up to 100 ng/ml had no significant effect on the protein binding of glibenclamide studied at 10 micrograms/ml. Metolazone is unlikely to cause a clinically significant increase in the ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00314813
更新日期:1990-01-01 00:00:00
abstract::Tolbutamide (1 g/70 kg) was administered as a single intravenous dose to 31 healthy, non-smoking, drug-free males between 23 and 87 years old and the total amounts of hydroxy and carboxytolbutamide excreted in 24 h were measured. There was a significant decrease in the urinary recovery of both metabolites with age. Th...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF02336696
更新日期:1990-01-01 00:00:00
abstract:OBJECTIVE:To study the influence of CYP3A4 inhibition by ketoconazole on the disposition of venlafaxine in individuals with different CYP2D6 pheno- and genotypes. METHODS:In an open two-phase study, 21 healthy volunteers with known CYP2D6 pheno- and genotype [14 extensive metabolisers (EMs), 7 poor metabolisers (PMs)]...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00228-003-0627-x
更新日期:2003-09-01 00:00:00
abstract:PURPOSE:The study aimed to test the hypothesis that hospital electronic prescribing and medicine administration system (HEPMA) implementation impacted patient discharge letter quality, nature and frequency of prescribing errors. METHOD:A quasi experimental before and after retrospective case note review was conducted ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-017-2274-7
更新日期:2017-10-01 00:00:00
abstract::The pharmacokinetics of mexiletine, a Class I antiarrhythmic drug, was investigated in 6 healthy volunteers after single oral doses and 15 min intravenous infusions of 3 mg/kg. Cimetidine and ranitidine are commonly used H2-receptor antagonists, which interact adversely with many drugs, e.g. inhibition of the metaboli...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00558298
更新日期:1989-01-01 00:00:00
abstract::The pharmacokinetics of 3H-16-epi-gitoxin have been investigated after oral administration: The peak serum level occurred after 30-60 min, and its subsequent decline was in two phases with half-lives of 3.5 and 19.5 h, respectively. Within 3 days 66-70% of the administered radioactivity were eliminated by renal excret...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00562938
更新日期:1977-07-19 00:00:00
abstract::Right ventricular repolarisation and refractoriness after therapeutic doses of disopyramide have been studied in 10 patients with coronary artery disease by recording monophasic action potentials (MAP) during programmed stimulation. Using 2 catheters, with the tip of one in the apex and the other in the outflow tract ...
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/BF00558240
更新日期:1988-01-01 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::The effect of nevirapine once-daily dosing on the pharmacokinetics of methadone and its main metabolite, 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine, was evaluated in ten HIV positive patients on stable methadone therapy. Nevirapine 200 mg once daily was administered orally from day 1 to day 14. On day 15, nevir...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-007-0299-z
更新日期:2007-07-01 00:00:00
abstract:AIM:It has been reported that verapamil and atorvastatin are inhibitors of both P-glycoprotein (P-gp) and microsomal cytochrome P450 (CYP) 3A4, and verapamil is a substrate of both P-gp and CYP3A4. Thus, it could be expected that atorvastatin would alter the absorption and metabolism of verapamil. METHODS:The pharmaco...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00228-007-0447-5
更新日期:2008-05-01 00:00:00
abstract:OBJECTIVE:The efficacy of beta-adrenergic blocking agents and acetylsalicylic acid in the secondary prevention of myocardial infarction has been well recognized since the beginning of the 1980s. In a previous paper, however, we reported a lower than expected use of these drugs during the period 1982 1988. In 1989 the r...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280050446
更新日期:1998-05-01 00:00:00
abstract:OBJECTIVE:The aim of this study was to evaluate the pharmacokinetics of vancomycin in patients with severe acute pancreatitis (SAP). METHODS:Sixty-seven patients with SAP were included. The FPIA method was used to measure vancomycin serum trough concentrations, and the pharmacokinetic parameters were calculated using ...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00228-016-2018-0
更新日期:2016-06-01 00:00:00
abstract:BACKGROUND:A four-drug cytochrome P450 (CYP) phenotyping cocktail was developed to rapidly and safely determine CYP2D6, CYP2C19, CYP2C9 and CYP1A2 enzyme activity and phenotype. METHODS:The cocktail consisted of the single CYP phenotyping probes of 50 mg tramadol (CYP2D6), 20 mg omeprazole (CYP2C19), 25 mg losartan (C...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章
doi:10.1007/s00228-013-1561-1
更新日期:2013-12-01 00:00:00
abstract::We have previously shown that inhaled salbutamol further increases the bronchodilator response after the maximum effect of theophylline has been obtained in patients with severe chronic bronchitis. We now report the results of adding maximally effective doses of theophylline to the maximum response obtainable from sal...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00542540
更新日期:1982-01-01 00:00:00
abstract::Red cell folate concentrations were determined in 74 epileptic women in early pregnancy in a prospective study. All patients were treated continuously with antiepileptic drugs since before conception. The most frequently used drugs were carbamazepine (n = 39) and phenytoin (n = 26). Sixty-four patients (86%) were on m...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00198317
更新日期:1995-01-01 00:00:00