Abstract:
PURPOSE:A combination of clopidogrel and aspirin is the standard treatment for patients with acute coronary syndrome and those undergoing percutaneous coronary intervention. Two novel antiplatelet agents, ticagrelor and prasugrel, have been shown to rapidly and more effectively inhibit the P2Y12 receptor compared with clopidogrel. The aim of this study was to evaluate and compare the pharmacokinetics (PK) and pharmacodynamics (PD) of ticagrelor and prasugrel in healthy male Korean volunteers. METHODS:Two separate studies were conducted. One study was performed by using a single-sequence, open-label, crossover design in 12 volunteers who received a single oral dose of ticagrelor (180 mg) and then a single oral dose of prasugrel (60 mg for 4 volunteers and 30 mg for 8 volunteers) with a 7-day washout period. The other study was a randomized, open-label, parallel-group investigation in which 8 volunteers received a single oral dose of prasugrel (10 mg for 4 volunteers and 30 mg for 4 volunteers). In each study, blood samples for PK and platelet aggregation inhibition analysis were serially collected after the administration of each dose. Plasma concentrations of ticagrelor, AR-C124910XX (the active metabolite of ticagrelor), R-95913 (the inactive metabolite of prasugrel), and R-138727 (the active metabolite of prasugrel) were measured by using a validated LC-MS/MS method. PK was analyzed by using a noncompartmental method. Maximal platelet aggregations were assessed with light transmission aggregometry after induction with 20 μmol/L of adenosine diphosphate. FINDINGS:Twenty healthy male Korean volunteers participated in the 2 studies. Plasma concentrations of ticagrelor and AR-C124910XX were obtained from 12 subjects, R-95913 from 20 subjects, and R-138727 from 8 subjects. Both ticagrelor and prasugrel were rapidly absorbed, with the shortest median Tmax of 2.0 and 2.25 hours for ticagrelor and AR-C124910XX, respectively, and a Tmax of 0.5 hour for both R-95913 and R-138727. Strong inhibition of platelet aggregation was shown after administration of both ticagrelor and prasugrel, with slightly stronger and more rapid inhibition with prasugrel in the tested doses. Inhibitory activities of prasugrel lasted longer than those of ticagrelor, reflecting the difference in binding kinetics between the 2 drugs. IMPLICATIONS:Prasugrel 30 and 60 mg exhibited slightly stronger, more rapid, and sustainable platelet inhibitory effects compared with ticagrelor 180 mg. These differing effects should be considered when determining the efficacy and adverse effects of ticagrelor and prasugrel. ClinicalTrials.gov identifier: NCT01876797 and NCT02075268.
journal_name
Clin Therjournal_title
Clinical therapeuticsauthors
Jeon HS,Kim MJ,Choi HY,Kim YH,Kim EH,Kim AR,Park HJ,Bae KS,Lim HSdoi
10.1016/j.clinthera.2015.01.010subject
Has Abstractpub_date
2015-03-01 00:00:00pages
563-73issue
3eissn
0149-2918issn
1879-114Xpii
S0149-2918(15)00053-3journal_volume
37pub_type
杂志文章,随机对照试验abstract:BACKGROUND:Although third mandibular molar extraction is a widely used and validated model of acute pain for evaluating analgesic efficacy, a large proportion of patients experience moderate or severe pain following this procedure and require analgesia. Current treatment options have been associated with safety concern...
journal_title:Clinical therapeutics
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1016/j.clinthera.2012.01.004
更新日期:2012-02-01 00:00:00
abstract::A national multicentre trial was organized in order to compare the efficacy and safety of leuprorelin acetate depot and danazol in the treatment of endometriosis. Sixty-seven patients with pelvic endometriosis of different severity at laparoscopy were included in the study and followed during the 24 weeks of treatment...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,多中心研究
doi:
更新日期:1992-01-01 00:00:00
abstract:BACKGROUND:Previous health economic studies have demonstrated the cost-effectiveness of simvastatin in the treatment of coronary heart disease (CHD) based on clinical results of the Scandinavian Simvastatin Survival Study. A prior analysis evaluated the "cost of getting to goal," but ignored all costs after titration. ...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s0149-2918(01)80010-2
更新日期:2001-02-01 00:00:00
abstract::In a double-blind, randomized study, the clinical effects of 5 mg and 10 mg of cisapride three times daily were compared with those of 10 mg of metoclopramide three times daily in 114 patients with symptoms of gastroesophageal reflux, mainly diurnal and nocturnal heartburn and regurgitation. The symptoms significantly...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:
更新日期:1988-01-01 00:00:00
abstract:BACKGROUND:According to evidence-based guidelines, the combination of inhaled corticosteroids and inhaled long-acting beta(2)-agonists in a single inhaler is recommended for patients with chronic obstructive pulmonary disease (COPD) who are experiencing exacerbations. The relative effectiveness of combination products ...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2010.06.022
更新日期:2010-07-01 00:00:00
abstract:PURPOSE:The International Conference on Harmonisation E14 guideline mandates an intensive cardiac safety evaluation in a clinical thorough QT study, typically in healthy subjects, for all new non-antiarrhythmic drugs with systemic bioavailability. This thorough QT study investigated the effects of therapeutic (2 mg) an...
journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2015.09.006
更新日期:2015-11-01 00:00:00
abstract:BACKGROUND:Concomitant aspirin use is a risk factor for nonsteroidal anti-inflammatory drug (NSAID)-associated upper gastrointestinal toxicity. In high-risk individuals, such as those with a history of NSAID-related gastric ulcer bleeding, gastroprotective therapy with a proton pump inhibitor has been reported to reduc...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.1016/j.clinthera.2004.10.002
更新日期:2004-10-01 00:00:00
abstract:BACKGROUND:Inhaled antibacterial agents are used to manage chronic pulmonary infections in cystic fibrosis (CF) and non-CF bronchiectasis. However, established nebulized preparations impose a substantial time burden on patients. A dry powder formulation of ciprofloxacin for inhalation (ciprofloxacin DPI) has been devel...
journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2013.08.003
更新日期:2013-10-01 00:00:00
abstract::One hundred fourteen women undergoing vaginal hysterectomy (n = 63) or abdominal hysterectomy (n = 51) were randomly allocated to one of three groups: regimen 1--cefotaxime perioperatively; regimen 2--cefotaxime perioperatively and for 24 hours postoperatively; or regimen 3--cefazolin perioperatively and for 24 hours ...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验
doi:
更新日期:1982-01-01 00:00:00
abstract:PURPOSE:In critical burn patients, the pharmacokinetic parameters (absorption, distribution, metabolism, and excretion) of many classes of drugs, including antibiotics, are altered. The aim of this study was to compare 2 groups of burn patients undergoing treatment for health care-associated infections with and without...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2017.06.008
更新日期:2017-08-01 00:00:00
abstract::Enoxacin 400 mg twice daily was given orally to 40 patients who had Salmonella typhi- or Salmonella paratyphi-positive blood or bone marrow cultures. One patient was switched to parenteral therapy within 48 hours of study enrollment, but the remaining 39 patients were given enoxacin for 10 to 14 days. All 39 patients ...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1992-11-01 00:00:00
abstract:BACKGROUND:Preclinical studies have reported that the relative bioavailability of dalcetrapib, a modulator of cholesteryl ester transfer protein (CETP) inhibitor activity, was ∼60% higher when administered in the fed state compared with the fasting state. OBJECTIVE:This article reports on 3 studies conducted to assess...
journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2011.05.046
更新日期:2011-06-01 00:00:00
abstract::The bacteriologic profile in 1081 pediatric patients with culture-positive symptomatic bacteriuria was studied over a 30-month period in a 500-bed acute care hospital in Riyadh, Saudi Arabia. Microbial isolates were considered significant if their numbers equaled or exceeded 10,000 colony-forming units/mL in symptomat...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/s0149-2918(96)80010-5
更新日期:1996-03-01 00:00:00
abstract:PURPOSE:The objective of this study was to evaluate the impact of a listed penicillin allergy on the time to first dose of antibiotic in a Veterans Affairs hospital. Additional clinical outcomes of patients with penicillin allergies were compared with those of patients without a penicillin allergy. METHODS:A retrospec...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2017.09.012
更新日期:2017-11-01 00:00:00
abstract:OBJECTIVE:The objectives of this study were to observe a commercially insured sample diagnosed with a venous thromboembolism (VTE) event and treated postevent with warfarin and to detail the thromboembolic and bleeding outcomes in the time periods during warfarin therapy and after discontinuation of such therapy. METH...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/s0149-2918(04)90187-7
更新日期:2004-07-01 00:00:00
abstract:BACKGROUND:Attention-deficit/hyperactivity disorder (ADHD) has a substantial negative impact; however, within long-term follow-up studies, a proportion of patients do very well, both symptomatically and functionally, suggesting that the lower the symptom burden, the greater the functional improvements. Studies in major...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2006.11.006
更新日期:2006-11-01 00:00:00
abstract::Community-acquired pneumonia (CAP) is responsible for an average of 4.5 million visits annually to physicians' offices, emergency departments, and outpatient clinics. However, there have been few studies using national data on the costs of treating CAP. Without such data, it is difficult to assess whether new therapie...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/s0149-2918(98)80144-6
更新日期:1998-07-01 00:00:00
abstract::Steady-state bioavailability of a sustained-release quinidine gluconate formulation was compared with that of a sustained-release quinidine sulfate preparation in a crossover study. Sixteen healthy men were given multiple doses (two tablets every 12 hours) of the two drugs in randomized sequence. Blood samples were ob...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验
doi:
更新日期:1983-01-01 00:00:00
abstract:PURPOSE:The aim of this study was to evaluate the effects of a dietary supplement containing primarily an extract of salmon's milt (semen) on symptoms and blood levels of proinflammatory molecules in patients with fibromyalgia syndrome (FMS), a chronic, painful musculoskeletal disease without a distinct pathogenesis or...
journal_title:Clinical therapeutics
pub_type: 杂志文章,多中心研究
doi:10.1016/j.clinthera.2019.05.019
更新日期:2019-08-01 00:00:00
abstract::The Omnibus Budget Reconciliation Act of 1990 (OBRA-90) may be the most significant piece of legislation affecting the practice of pharmacy since the Durham-Humphrey amendments to the Food, Drug and Cosmetic Act. As part of the OBRA-90 legislation, the Health Care Financing Administration (HCFA) was required to publis...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1993-05-01 00:00:00
abstract:BACKGROUND:Nearly half of all US patients with type 2 diabetes mellitus (T2DM) are unable to maintain adequate glycosylated hemoglobin (HbA₁(c)) control (ie, <7.0%). OBJECTIVE:The aim of this work was to determine the long-term cost-effectiveness of incretin-based therapy with once-daily liraglutide (vs twice-daily ex...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2010.08.010
更新日期:2010-09-01 00:00:00
abstract:BACKGROUND:In the United States, patients with high-risk stage II or III melanoma are often treated with adjuvant interferon (IFN) therapy for 1 year after surgery. Adverse events associated with IFN alfa-2b use are primarily constitutional symptoms. However, hypertriglyceridemia requiring treatment has been reported. ...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2005.12.002
更新日期:2005-12-01 00:00:00
abstract::Healing rates were examined retrospectively in 124 outpatients with peptic ulcer who had received cimetidine for at least four weeks. Treatment was unsuccessful in 73 patients. A statistical analysis of the factors involved in treatment failure revealed that in patients with duodenal ulcers 60.6% of the treatment succ...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1984-01-01 00:00:00
abstract:BACKGROUND:Due to Mexico's complicated socioeconomic environment, causing a high occurrence of >1 person sharing a single room, respiratory conditions are spread easily. Respiratory conditions are the main reason for consultation with a physician. The most frequent symptoms are throat soreness and cough; therefore, a n...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s0149-2918(03)80215-1
更新日期:2003-08-01 00:00:00
abstract::Twenty men, aged 50 to 75 years (mean, 67 years), suffering from benign prostatic hypertrophy received 160 mg of a lyposterolic extract of Serenoa repens, twice daily for 30 days. Before and at the end of treatment, plasma levels of testosterone, follicle-stimulating hormone, and luteinizing hormone were determined. N...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1988-01-01 00:00:00
abstract:BACKGROUND:Conflicting results using the combination of ezetimibe and statins to reduce the risk of cardiovascular events in patients with acute coronary syndrome (ACS) have been reported. OBJECTIVE:The aim of this work was to assess the effectiveness of ezetimibe coadministered with statins in reducing cardiovascular...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2011.08.002
更新日期:2011-09-01 00:00:00
abstract:BACKGROUND:Cobalamin (vitamin B12) deficiency, the most common cause of megaloblastic anemia, is treated with intramuscular (IM) cobalamin. It has been suggested by some investigators that oral (p.o.) cobalamin treatment may be as effective in the treatment of this condition, with the advantages of ease of administrati...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s0149-2918(03)90096-8
更新日期:2003-12-01 00:00:00
abstract:PURPOSE:This study aimed to review and summarize clinical trial data, updated guidelines, and expert opinions on the recommendations for drug holidays in patients being treated for osteoporosis. METHODS:Three unique PubMed searches using the terms osteoporosis drug holiday, osteoporosis discontinuation, and osteoporos...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2015.03.023
更新日期:2015-07-01 00:00:00
abstract:BACKGROUND:Drug treatment can defer surgical intervention in benign prostatic hyperplasia (BPH), a common disorder in elderly men, and is widely practiced. Various herbal formulations have been used for the treatment of BPH, but few have been compared with established modern medicines in head-to-head clinical trials. ...
journal_title:Clinical therapeutics
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1016/j.clinthera.2011.11.005
更新日期:2011-12-01 00:00:00
abstract::Twenty-seven Escherichia coli test strains that were not susceptible to cephalothin were tested for susceptibility to cefazolin, cefamandole, and ceforanide. By zone-size criteria (greater than or equal to 18 mm), 67% of E coli were susceptible to cefazolin and cefamandole, and 93% were susceptible to ceforanide. By m...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1985-01-01 00:00:00