Abstract：
:Blood levels of racemic chloroquine and its main metabolites desethylchloroquine and bisdesethylchloroquine were measured in 29 patients treated chronically for rheumatoid arthritis. In six patients, the concentrations were followed during a one day dosage interval. There was considerable intersubject variability in the steady state blood concentrations of chloroquine (range 36.6 to 3895 ng.ml-1) and its two main biotransformation products; the latter represented, respectively, 47.7% and 12.9% of the concentration of chloroquine. This finding shows the need for further studies in view of the known toxic effects of chloroquine and the inevitable accumulation due to the exceptionally long residence time of the compound and its metabolites. The main requirement, which has not yet been met, for adding chloroquine to the list of drugs for which therapeutic drug monitoring is useful, is the lack of information about its mechanism of action, and consequently the dose-effect relationships of its therapeutic and toxic actions. Regular ophthalmic examination, in particular, is strongly recommended. The relatively high concentrations of desethylchloroquine and bisdesethylchloroquine found during chronic treatment show the need for more information about the therapeutic value and adverse effects of the metabolites.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Augustijns P,Geusens P,Verbeke Ndoi
10.1007/BF00280130subject
Has Abstractpub_date
1992-01-01 00:00:00pages
429-33issue
4eissn
0031-6970issn
1432-1041journal_volume
42pub_type
杂志文章abstract：PURPOSE:Propofol anesthesia is usually accompanied by hypotensive responses, which are at least in part mediated by nitric oxide (NO). Arginase I (ARG1) and arginase II (ARG2) compete with NO synthases for their common substrate L-arginine, therefore influencing the NO formation. We examined here whether ARG1 and ARG2 ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-020-03059-9
更新日期：2021-01-07 00:00:00
abstract：:The presence of a possible correlation between changes in left ventricular mass of hypertensive patients and the degree of blood pressure reduction with different antihypertensive drugs has been investigated in 40 outpatients by M-mode echocardiography. Ten of these, with blood pressure in normal limits with different...
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/BF00556886
更新日期：1984-01-01 00:00:00
abstract：:Verapamil, 0.1 mg/kg body wt, was injected i.v. over 2 minutes in 8 subjectively healthy middle-aged men, followed by a continuous infusion of 0.007 mg/kg body wt per minute. Prior to the injection several of the subjects had raised pulmonary or systemic arterial pressures. At rest, the central pressures increased sli...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00562656
更新日期：1975-06-13 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：:The effect of procainamide (P) on left ventricular function as measured by the systolic time intervals (STI) was studied in 14 patients with primary myocardial disease. P, 7.5 mg/kg body weight, was given intravenously at a rate of 100 mg per minute. Administration of P produced a decrease in left ventricular performa...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00561387
更新日期：1980-10-01 00:00:00
abstract：PURPOSE:To investigate pharmacokinetics (PK) of encapsulated CPT-11, released CPT-11 and the active metabolite SN-38 following administration of IHL-305 and to identify factors that may influence IHL-305 PK. METHODS:Plasma samples from 39 patients with solid tumors were collected in a phase I study. IHL-305 was admini...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-013-1580-y
更新日期：2013-12-01 00:00:00
abstract：:The kinetics of mefloquine were studied in 12 healthy Thai male and 12 healthy Thai female volunteers. Mefloquine (MQ) was administered either alone (750 mg orally) or in combination (MSP) with sulphadoxine (1.5 g) and pyrimethamine (75 mg) to each of 6 male and 6 female subjects. Plasma concentrations of MQ were meas...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00542191
更新日期：1987-01-01 00:00:00
abstract：:Ninety-six depressed outpatients from 5 centres were given viloxazine 200-400 mg/day. The treatment produced significant clinical improvement as evaluated by the Hamilton Rating Scale for Depression. Thirteen patients dropped-out because of possible side effects. Many untoward symptoms were described by all the patien...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00613832
更新日期：1983-01-01 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：:Intensive monitoring of adverse drug reactions (ADR) in infants and preschool children in the paediatric outpatient unit covering the town of Karlovac (150,000 inhabitants) was performed over a period of three months. Data were obtained by physical examination of children and the history given by their parents. In all...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00561025
更新日期：1989-01-01 00:00:00
abstract：OBJECTIVE:Psychotropic drug use among nursing home residents with regard to diagnostic indications and patient- and institution characteristics was analysed. METHODS:A cross-sectional study of medication data from 1552 residents at 23 nursing homes in Bergen, Norway, was performed. Psychotropic drug use (neuroleptics,...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s002280100348
更新日期：2001-09-01 00:00:00
abstract：OBJECTIVE:Case report of a pharmacokinetic interaction between diltiazem and nortriptyline. METHODS:Determination of plasma nortriptyline concentrations by HPLC. Calculation of nortriptyline clearances and half-life by formulae used routinely in therapeutic drug monitoring. RESULTS:The average plasma concentration of...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00203789
更新日期：1996-01-01 00:00:00
abstract：:Potentiation of the anticoagulant-effect of warfarin by amiodarone was studied in 30 patients. Thirteen received both drugs concurrently, and 17 received warfarin alone and the combination sequentially. Warfarin doses were adjusted to maintain the prothrombin time between 25-30% of control and its kinetics were compar...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00543320
更新日期：1985-01-01 00:00:00
abstract：:A radioreceptor assay (RRA) recently developed in this laboratory for beta-adrenoceptor antagonists in plasma was evaluated in normal volunteers and compared with a radioimmunoassay (RIA) for propranolol. The RRA depends upon the ability of beta-adrenoceptor antagonists to complete with a radiolabelled ligand for beta...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00558447
更新日期：1980-05-01 00:00:00
abstract：:Encainide is a new anti-arrhythmic drug, which is highly effective against ventricular extrasystoles, both single and coupled, in the dose range of 80--140 mg i.v. Ventricular extrasystoles were abolished in 31 out of 33 cases treated. The drug is also relatively effective against supraventricular extrasystoles, but h...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00605629
更新日期：1979-11-01 00:00:00
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：:A placebo-controlled, single blind, crossover study was done to evaluate the inotropic effects of single oral doses of mexiletine and disopyramide assessed by the measurement of Systolic Time Intervals (STI). Each of 8 healthy volunteers received five treatments in random order: 200 and 400 mg mexiletine, 100 and 200 ...
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/BF00541525
更新日期：1986-01-01 00:00:00
abstract：:The antihypertensive effects of urapidil and clonidine have been studied in a double-blind cross-over trial in 11 hypertensive outpatients with mild to moderate hypertension, at rest and during isometric exercise. Urapidil 30 mg b.i.d. significantly decreased the standing diastolic blood pressure (p less than 0.05) 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/BF00635705
更新日期：1985-01-01 00:00:00
abstract：:The purpose of the study was to examine long-term nicotine substitution and its variability during use of a nicotine patch. In two smoking cessation studies a 16-h nicotine patch, releasing 15 mg nicotine, was applied daily for 16 h over 12 weeks, to 167 smokers. Salivary cotinine was highly correlated with plasma cot...
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/BF02280755
更新日期：1992-01-01 00:00:00
abstract：:To evaluate the possible effect of quinidine on digoxin bioavailability, the steady state digoxin kinetics was examined with and without concomitant quinidine therapy, in 7 cardiac patients after simultaneous administration of oral digoxin and intravenous [3H]-digoxin. In the presence of quinidine, the absorption rate...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00613925
更新日期：1983-01-01 00:00:00
abstract：BACKGROUND:Drug reaction with eosinophilia and systemic symptoms syndrome (DRESS) is a delayed infrequent potentially life-threatening idiosyncratic drug reaction. Aromatic anticonvulsants and allopurinol are the most frequent causative agents. However, various reports of antibiotic-induced DRESS are available. In this...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章,评审
doi：10.1007/s00228-020-03005-9
更新日期：2020-10-06 00:00:00
abstract：:The interaction between the main components of the new glycopeptide antibiotic teicoplanin, A2-2, A2-3, A2-4, A2-5 and A3-1, and human serum albumin has been studied in vitro by equilibrium dialysis (pH 7.4, 37 degrees C). From Scatchard analysis of the data, the calculated association constants (Ka) were: A2-2, 2.47 ...
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00544566
更新日期：1987-01-01 00:00:00
abstract：:We examined the pharmacokinetics of nifedipine after acute and sustained oral therapy and the potential haemodynamic interaction between nifedipine and sublingual nitroglycerin in nine patients with chronic stable angina. Nifedipine pharmacokinetics after a single oral dose and sustained dosing (three times daily for ...
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/BF00637629
更新日期：1987-01-01 00:00:00
abstract：:Nicotine chewing gum (Nicorette 4 mg) and an identical placebo gum were administered on different days, in a double-blind cross over fashion, to 4 men, aged 25-52 years, and 4 women, aged 21-49 years, all healthy non-smokers. The subjects chewed the gum for 30 min and heart rate, blood pressure, electrocardiogram, fin...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00613610
更新日期：1982-10-01 00:00:00
abstract：PURPOSE:Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor, widely prescribed for type 1 human immunodeficiency virus infection. A small proportion of individuals treated with NVP experience severe cutaneous adverse events, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN)....
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/s00228-013-1549-x
更新日期：2013-11-01 00:00:00
abstract：:Six children, aged 2 months - 4 years, received theophylline 5-6 mg/kg intravenously. Its disposition could be described by a two-compartment open model, the mean serum half life (t 1/2 beta) was 3.75 h, i.e., shorter than in adults, but there was a considerable interindividual variation (1.8-7.0 h, in one patient 13....
journal_title：European journal of clinical pharmacology
pub_type： 杂志文章
doi：10.1007/BF00563120
更新日期：1979-09-01 00:00:00
abstract：:Interaction of the main metabolites of diazepam and chlordiazepoxide with alcohol was measured in two subacute double-blind cross-over experiments on 40 healthy, young volunteers. The drugs were administered for two week periods. The variables measured were choice reaction time and accuracy, eye-hand co-ordination, di...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/BF00644607
更新日期：1978-07-30 00:00:00
abstract：OBJECTIVE:To investigate the effects of rifampicin on the pharmacokinetics of itraconazole in humans. METHODS:Our study was conducted with six healthy normal volunteers and three AIDS patients. All subjects received a 200 mg single dose of oral itraconazole on day 1 and day 15 and 600 mg of oral rifampicin once daily ...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s002280050437
更新日期：1998-04-01 00:00:00
abstract：OBJECTIVE:To quantify the relation between local and systemic magnitudes of effects of inhaled formoterol and salbutamol. METHODS:Twenty-eight stable asthmatic patients completed this double-blind, randomised crossover study. Pre-drug administration FEV1 (mean 2.08 L) was 49-93% of predicted and reversibility 16-82% a...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章,随机对照试验
doi：
更新日期：2002-07-01 00:00:00
abstract：PURPOSE:To investigate the impact of valproic acid (VPA) and genetic polymorphism of the major metabolizing enzyme (UGT1A4, UGT2B7) of lamotrigine (LTG) and VPA on LTG concentration in Chinese epileptic children. METHODS:Three single nucleotide polymorphisms (UGT1A4*3, UGT2B7 -161C > T and UGT2B7*2) were analyzed by p...
journal_title：European journal of clinical pharmacology
pub_type： 临床试验,杂志文章
doi：10.1007/s00228-015-1925-9
更新日期：2015-11-01 00:00:00
