Abstract:
OBJECTIVE:The pharmacokinetics and bioavailability of artemether and dihydroartemisinin were investigated in eight Thai males following the administration of single oral and intramuscular doses of artemether (300 mg) in a randomized two-way cross-over study. RESULTS:Both oral and intramuscular artemether were well-tolerated. In most cases, artemether and dihydroartemisinin were detected in plasma after 30 min and declined to levels below the limit of detection within 18-24 h. Compared with intramuscular administration, oral administration of artemether resulted in a relatively rapid but incomplete absorption [Cmax: 474 vs 540 ng.ml-1; tmax: 2.0 vs 3.9 h; AUC: 2.17 vs 5.20 micrograms.h.ml-1]. Geographic means of lag-time and absorption half-life (t1/2a) of oral vs intramuscular artemether were 0.28 and 1.1 h vs 0.30 and 2 h, respectively, t1/2z was significantly shortened after the oral dose [2.8 vs 6.9 h]. Mean oral bioavailability relative to intramuscular administration was 43.2%. The ratio of the AUCs of artemether to dihydroartemisinin was significantly lower after the oral than after the intramuscular dose (geometric mean: 0.29 vs 0.60). artemisinin, which is commercially available in China, Vietnam, Thailand and some African countries. The drug is administered as solution in oil for intramuscular injection or as oral tablets. The clinical efficacy of artemether is dependent on the formulation, dosing scheme, duration of treatment, and the severity of the disease [1, 2]. Oral artemether is effective but with short-term treatment, the relapse rate is high. While the efficacy of intramuscular artemether against multidrug-resistant P. falciparum in either uncomplicated or severe cases has been confirmed, its pharmacokinetic documentation is limited. Formulations with high bioavailability and low costs are essential. With high-performance liquid chromatography and electrochemical detection, more sensitive and reliable assay of artemisinin and derivatives in biological fluids has been achieved [3-4]. In the present study, we have assessed the pharmacokinetics and bioavailability of oral and intramuscular artemether, in healthy Thai males.
journal_name
Eur J Clin Pharmacoljournal_title
European journal of clinical pharmacologyauthors
Karbwang J,Na-Bangchang K,Congpuong K,Molunto P,Thanavibul Adoi
10.1007/s002280050295subject
Has Abstractpub_date
1997-01-01 00:00:00pages
307-10issue
4eissn
0031-6970issn
1432-1041journal_volume
52pub_type
临床试验,杂志文章,随机对照试验abstract::Drug utilization was studied in children below 14 years of age in Tenerife, Canary Islands, who were seen as outpatients by 15 paediatricians and 10 general practitioners. Data on diagnosis, previous drug exposure and prescriptions were collected from a random sample of 1327 children. Nose and throat infections (40.1%...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF01046708
更新日期:1988-01-01 00:00:00
abstract:PURPOSE:In the past few years, several fracture-related events have been reported with chronic use of selective serotonin reuptake inhibitors (SSRIs) throughout the globe. Hence, an updated systematic review and meta-analysis was necessary to ascertain the risk involved. The present work evaluated the association of SS...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-020-02893-1
更新日期:2020-10-01 00:00:00
abstract::Methylergometrine, the main metabolite of methysergide, has 40-times greater 5 HT antagonistic potency than methysergide in isolated segments of human temporal artery. It is suggested that methylergometrine is the "active" drug when methysergide is used in migraine prophylaxis, and that the two compounds should be com...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00610384
更新日期:1987-01-01 00:00:00
abstract:PURPOSE:It is well known that CPT-11 (irinotecan) is biotransformed to its active metabolite, SN-38, by carboxylesterase in the liver and other tissues. However, little is known about its pharmacokinetics (PK) when administered intraperitoneally. The aim of our study was to develop a population pharmacokinetic model fo...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-010-0885-3
更新日期:2010-12-01 00:00:00
abstract::Propranolol (P) and all of its major known metabolites were found in maternal plasma, cord plasma and neonatal plasma in 10 women at term, irrespective of the P doses administered and the time elapsed (up to 15 h) between administration of the last P dose and delivery. The ratios of cord plasma to simultaneous materna...
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/BF00607078
更新日期:1983-01-01 00:00:00
abstract::The plasma pharmacokinetics of adriamycin has been studied in 21 cancer patients (31-85 years old) without liver tumours after short (3.00 min) and prolonged (45 min-16 h) i.v. infusions. The area under the plasma concentration-time curve and the maximum plasma concentration compensated for dose variation showed a mor...
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/BF00609693
更新日期:1985-01-01 00:00:00
abstract:OBJECTIVE:The analgesic efficacy of intravenous doses of acetaminophen (paracetamol) 0.5 g, 1 g and 2 g (administered as propacetamol) was assessed in 11 healthy subjects in a randomised, double-blind, placebo-controlled crossover study. The antinociceptive effect was assessed over 8 h by measurement of the nociceptive...
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/s002280050386
更新日期:1998-01-01 00:00:00
abstract:INTRODUCTION:Body position may influence physiological characteristics, such as perfusion, gastrointestinal function and plasma volume. These characteristics may interact with key factors determining the pharmacokinetics of drugs (dissolution, absorption, distribution, metabolism, excretion). OBJECTIVES:Based on a sys...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,评审
doi:10.1007/s00228-008-0579-2
更新日期:2009-02-01 00:00:00
abstract::Sixty patients were treated for 1 year for essential uncomplicated hypertension, 30 with beta-blockers alone (BB) and 30 with BB and chlorthalidone (CTD). BB did not affect serum K+ or Mg++. In the BB-group there was a statistically significant trend towards retention of Mg++ in a loading test, but the effect was clin...
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/BF00543964
更新日期:1987-01-01 00:00:00
abstract::The biliary excretion of mebendazole has been investigated in two patients to whom it was given for the treatment of echinococcosis, although it was found to be only partly effective. Oral mebendazole was extensively metabolized and the conjugated parent substance and its metabolites were excreted in the bile. One pat...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00544020
更新日期:1983-01-01 00:00:00
abstract:PURPOSE:The purpose of this study is to investigate whether there is an association between anticholinergic burden and mortality or rehospitalization in older adults discharged from hospital. METHODS:Prospective multicenter cohort study carried out with patients aged 65 and older discharged from seven acute care hospi...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,多中心研究
doi:10.1007/s00228-017-2312-5
更新日期:2017-11-01 00:00:00
abstract::Prazosin is a post synaptic alpha adrenergic blocker effective in hypertension, whose hypotensive effect is unaccompanied by reflex tachycardia or hyperreninemia, nor by other evidence of increased sympathetic activity. We studied the baroreceptor reflex arc as a potential mediator of these effects. Twenty-two essenti...
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/BF00606418
更新日期:1982-01-01 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::Procaine esterase activity in plasma from patients with renal failure is decreased by 40%. Since cyanate is formed from urea and readily carbamylates certain blood proteins, a possible role for cyanate in the depression of plasma esterase activity in uraemic patients was considered. However, in vitro carbamylation of ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00609899
更新日期:1983-01-01 00:00:00
abstract::In the 3rd paragraph and 2nd line of the Conclusion section the correct sentence should be: It is now important to encourage policy and decision makers to facilitate and accommodate future linkage of data. ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,已发布勘误
doi:10.1007/s00228-017-2358-4
更新日期:2017-11-01 00:00:00
abstract:PURPOSE:The present study was carried out in order to assess the effects of chronic administration of flunitrazepam (as an oral hypnotic) on 24-h blood pressure (BP) and heart rate (HR) in healthy young adults. MATERIALS AND METHODS:Following a 2-week placebo run-in period, 28 healthy volunteers (13 males and 15 femal...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章,随机对照试验
doi:10.1007/s00228-018-2466-9
更新日期:2018-08-01 00:00:00
abstract:OBJECTIVE:The efficacy, safety, tolerability and speed of onset of the hypotensive action of the combination of oral enalapril (10 mg) prazosin (1 mg) and hydrochlorothiazide (50 mg) has been assessed in 12 Nigerians with severe hypertension (Diastolic BP > or = 115 mmHg). PATIENTS:The ages of the patients ranged from...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s002280050158
更新日期:1996-01-01 00:00:00
abstract:OBJECTIVES:To explore the views and perspectives of children on the unlicensed/off-label use of medicines in children and on the participation of children in clinical trials. METHODS:Focus-group discussions, involving school children, were carried out in a range of primary and secondary schools in Northern Ireland. A ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-011-1110-8
更新日期:2012-02-01 00:00:00
abstract:OBJECTIVE:Iloprost is a potent PGI2 mimetic, which has been shown to be therapeutically effective in several vascular disorders. Due to its rapid clearance from the central compartment, iloprost is administered mainly by i.v. infusion, which limits its use to hospitalized patients. In order to improve pharmacotherapeut...
journal_title:European journal of clinical pharmacology
pub_type: 临床试验,杂志文章,多中心研究
doi:10.1007/s002280050336
更新日期:1997-01-01 00:00:00
abstract:OBJECTIVES:To compare the systemic exposure for intranasal mometasone furoate (MF) and fluticasone propionate (FP) aqueous nasal sprays (ANS) in terms of serum and urinary cortisol parameters and plasma pharmacokinetics. METHODS:Twelve healthy subjects completed this three-way, cross-over study. They received FPANS (5...
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/s00228-004-0763-y
更新日期:2004-06-01 00:00:00
abstract::We have assessed the effect of omeprazole on various endocrine functions in man. Eight healthy subjects took 60 mg omeprazole or placebo daily for 1 week in a double-blind, randomized, cross-over study. On Day 7 basal concentrations of follicle-stimulating hormone (FSH), luteinising hormone (LH), prolactin, testostero...
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/BF00543980
更新日期:1987-01-01 00:00:00
abstract::A double blind crossover trial of baclofen against placebo in elderly stroke patients was discontinued because the drug produced an unacceptably high level of drowsiness. In a subsequent study baclofen 10 mg was given orally to 12 elderly stroke patients, and drug concentrations measured from a series of plasma sample...
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/BF00613463
更新日期:1985-01-01 00:00:00
abstract::To evaluate the magnitude and duration of the antihypertensive effect of sustained release (SRO) isradipine, 37 uncomplicated essential hypertensive patients (diastolic blood pressure 100-115 mm Hg after a one month run-in on placebo) were randomised to receive, according to a double-blind cross-over design, isradipin...
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/BF00315275
更新日期:1993-01-01 00:00:00
abstract:PURPOSE:Tigecycline is one of few antibiotics active against multidrug-resistant bacteria; however, the assessment of dosing strategies to optimize its activity is needed. The purpose was to use Monte Carlo Simulation (MCS) to determine if safe tigecycline dosing options attaining breakpoints for pharmacokinetic/pharma...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-020-02998-7
更新日期:2021-02-01 00:00:00
abstract:PURPOSE:The Drug Burden Index (DBI) is a tool to quantify the anticholinergic and sedative load of drugs. Establishing functional correlates of the DBI could optimize drug prescribing in patients with dementia. In this cross-sectional study, we determined the relationship between DBI and cognitive and physical function...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-017-2319-y
更新日期:2017-12-01 00:00:00
abstract::We have studied the transfer of the analgesic ketorolac tromethamine into breast milk in ten women aged between 22 and 35 years. Ketorolac administration was started between 2 and 6 days after delivery. The breast milk was not fed to the infant because of maternal antibiotic use (6 patients) or because of jaundice of ...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00558080
更新日期:1989-01-01 00:00:00
abstract::All forensic autopsy cases in southern Sweden in 1986-89 in which antidepressant drugs were found in the blood were assessed and the findings related to the sales of antidepressants as expressed as defined daily doses per 1,000 inhabitants per day. There was a total of 272 antidepressant-positive cases, which were div...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00194393
更新日期:1994-01-01 00:00:00
abstract:OBJECTIVE:The pharmacokinetics of orally and intravenously administered valsartan were determined in two studies. In a first pilot study, three i.v. doses of valsartan were given in an ascending manner (5, 10 and 20 mg) to evaluate tolerability and basic pharmacokinetics of the i.v. formulation. In a second study, the ...
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/s002280050259
更新日期:1997-01-01 00:00:00
abstract::The pharmacokinetics, hypotensive effect and tolerability of a new vasodilator, tolmesoxide (T), have been studied in 6 uncontrolled hypertensive patients receiving atenolol and diuretic. After a 50 mg oral dose mean (+/- SD) peak plasma concentration of T was 1.13 +/- 0.29 micrograms/ml-1 and occurred 0.79 +/- 0.40 h...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/BF00568397
更新日期:1981-01-01 00:00:00
abstract:PURPOSE:Oncological patients are at increasing risk of QT prolongation, a risk factor for ventricular arrhythmia. We assessed impact and risk factors for corrected QT (QTc) prolongation during multiple-cycle chemotherapy. METHODS:We enrolled 100 outpatients initiating chemotherapy in a university center specializing i...
journal_title:European journal of clinical pharmacology
pub_type: 杂志文章
doi:10.1007/s00228-015-1874-3
更新日期:2015-08-01 00:00:00