Abstract:
BACKGROUND:In vitro studies have demonstrated that ticagrelor, an oral antiplatelet agent, is a substrate, activator, and inhibitor of cytochrome P450 (CYP) 3A. Thus, potential CYP3A-mediated drug-drug interactions may occur. OBJECTIVES:The goal of this article was to report study results on the effect of ticagrelor on the pharmacokinetics of oral midazolam (oral midazolam study) and oral versus intravenous (IV) midazolam (oral/IV midazolam study). Secondary objectives included assessing the effect of midazolam on ticagrelor pharmacokinetic parameters, and the safety and tolerability of ticagrelor/midazolam coadministration. METHODS:Two randomized crossover studies were conducted in healthy volunteers (n = 28 in each) with ticagrelor and midazolam. In the first study, volunteers received oral ticagrelor (400 mg daily) or placebo for 6 days, then oral midazolam (7.5 mg). The second study regimen was a single dose of ticagrelor 270 mg, then ticagrelor 180 mg BID for 6 days with a single oral (7.5 mg) or IV (2.5 mg) dose of midazolam. RESULTS:After oral midazolam administration, ticagrelor significantly reduced the AUC(0-∞) of midazolam (30%-32%) and 4-hydroxymidazolam (42%-47%) but not 1-hydroxymidazolam. After administration of IV midazolam, ticagrelor reduced the AUC(0-∞) of midazolam (12%) and 4-hydroxymidazolam (23%) but not 1-hydroxymidazolam. CONCLUSIONS:These results indicate that ticagrelor can weakly activate the metabolism of midazolam to its major 1'-hydroxy metabolite, and at the same time, seems to weakly inhibit midazolam 4'-hydroxylation. Furthermore, ticagrelor affects both hepatic and intestinal CYP3A activity.
journal_name
Clin Therjournal_title
Clinical therapeuticsauthors
Teng R,Butler Kdoi
10.1016/j.clinthera.2013.06.003subject
Has Abstractpub_date
2013-07-01 00:00:00pages
1025-37issue
7eissn
0149-2918issn
1879-114Xpii
S0149-2918(13)00319-6journal_volume
35pub_type
临床试验,杂志文章,随机对照试验abstract:BACKGROUND:Many patients with type 2 diabetes mellitus (T2DM) also have hypertension, which is commonly treated with thiazide diuretics, including hydrochlorothiazide (HCTZ). Canagliflozin, a sodium glucose cotransporter 2 inhibitor developed for the treatment of T2DM, lowers plasma glucose by inhibiting renal glucose ...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2014.02.022
更新日期:2014-05-01 00:00:00
abstract::Flecainide, a new antiarrhythmic agent, was given to eight healthy men to ascertain plasma drug levels and to assess tolerance for the drug. Each subject received a single intravenous (IV) dose (0.5, 1, 1.5, or 2 mg/kg) of flecainide, and plasma levels of unchanged flecainide were measured by gas-liquid chromatography...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1984-01-01 00:00:00
abstract:PURPOSE:Therapy for patients with type 2 diabetes (T2DM) not achieving hemoglobin (Hb) A1c targets may progress from an oral antidiabetic drug (OAD) to added basal insulin and then to multiple daily injections of basal-bolus insulin (MDI); however, the relative clinical and economic burden experienced by patients presc...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2018.12.014
更新日期:2019-02-01 00:00:00
abstract::Patient counseling is an important aspect of family planning. Patient choice, compliance, and satisfaction with a contraceptive method depend heavily on the counseling experience. This is especially true in the United Kingdom where contraceptives are provided to patients at no direct cost to them. Women are therefore ...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/s0149-2918(96)80187-1
更新日期:1996-01-01 00:00:00
abstract:PURPOSE:Neglected tropical diseases (NTDs) impose a significant burden on public health, particularly in developing nations. Many can be treated cost-effectively with drugs donated or offered at or below marginal cost. In 2012, the World Health Organization published an NTD roadmap that outlined a strategy for the prev...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2016.02.031
更新日期:2016-05-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2009.12.003
更新日期:2009-12-01 00:00:00
abstract:PURPOSE:Huoxue-Tongluo lyophilized powder for injection (HTLPI), a traditional Chinese medicine preparation, is a compound of Persicae semen and Paeoniae Radix Rubra that is used mainly for treating blood-stasis obstruction syndrome in the acute stage of cerebral ischemic stroke. Amygdalin (AD) and paeoniflorin (PF) ar...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2015.12.005
更新日期:2016-02-01 00:00:00
abstract:BACKGROUND:The role of folate in pregnancy is well established, with most prenatal vitamins (PNVs) on the market containing at least 800 μg of folic acid. Folic acid must be converted in the body to L-methylfolate, the natural and biologically active form of folate. The role of vitamin B(12) in pregnancy is less charac...
journal_title:Clinical therapeutics
pub_type: 杂志文章,多中心研究
doi:10.1016/j.clinthera.2011.02.010
更新日期:2011-02-01 00:00:00
abstract:OBJECTIVE:This study evaluated the efficacy and tolerability of glimepiride in patients with type 2 diabetes mellitus that was inadequately controlled with a combination of immediate- or extended-release metformin and a thiazolidinedione. METHODS:This was a multicenter, randomized, double-blind, placebo-controlled, pa...
journal_title:Clinical therapeutics
pub_type: 杂志文章,多中心研究,随机对照试验
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更新日期:2005-10-01 00:00:00
abstract:BACKGROUND:Interferon (IFN) alfa is a clinically effective therapy used in a wide range of viral infections and cell-proliferative disorders. Combination therapy with IFN alfa-2b and ribavirin is the current standard of care for the treatment of chronic hepatitis C (CHC) infection. However, standard IFN alfa has the dr...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/s0149-2918(02)80042-x
更新日期:2002-09-01 00:00:00
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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)80116-9
更新日期:2003-03-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/s0149-2918(02)80102-3
更新日期:2002-12-01 00:00:00
abstract::Serum creatinine and beta 2-microglobulin levels, endogenous creatinine clearance, the urinary beta 2-microglobulin excretion rate, and urinary protein levels were monitored serially in 29 patients with duodenal ulcers randomly allocated to receive eight weeks of treatment with cimetidine, ranitidine, or an antacid. A...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1984-01-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2015.08.012
更新日期:2015-10-01 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
abstract:PURPOSE:The aim of this study was to assess the pharmacokinetic (PK) and pharmacodynamic (PD) properties and safety of single and multiple doses of cinacalcet in Chinese healthy volunteers (HVs) for the purposes of a New Drug Application package for the Chinese Food and Drug Administration. METHODS:In this randomized,...
journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2015.12.015
更新日期:2016-02-01 00:00:00
abstract:BACKGROUND:Belimumab, a monoclonal antibody that inhibits B-lymphocyte stimulating protein, was the first biologic agent approved for, and the first drug approved in 55 years for, the treatment of systemic lupus erythematosus (SLE) by the US Food and Drug Administration (FDA). OBJECTIVE:This article reviews the curren...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2012.02.028
更新日期:2012-05-01 00:00:00
abstract:PURPOSE:The objective of this study was to assess the frequency of tablet splitting of psychotropic drugs in a population of older adults with a diagnosis of dementia. METHODS:This retrospective, cross-sectional study examined a sample of geriatric outpatients seen at a public center specializing in the care of elderl...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2015.08.015
更新日期:2015-10-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/s0149-2918(03)80302-8
更新日期:2003-01-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2005.01.009
更新日期:2005-01-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2013.12.011
更新日期:2014-02-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2015.08.021
更新日期:2015-10-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,多中心研究
doi:10.1016/s0149-2918(03)80204-7
更新日期:2003-07-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2014.09.012
更新日期:2015-02-01 00:00:00
abstract:BACKGROUND:Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against both wild-type HIV and viruses harboring NNRTI resistance. Etravirine is mainly eliminated via the hepatobiliary route. OBJECTIVES:This study in HIV- patients with mild or moderate hepatic impairment and healthy mat...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2010.02.013
更新日期:2010-02-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/S0149-2918(00)88295-8
更新日期:1999-02-01 00:00:00
abstract:BACKGROUND:The use of dopamine agonists (DAs) for the treatment of restless legs syndrome (RLS) has been assessed in numerous randomized clinical trials (RCTs). OBJECTIVES:The aims of this study were to assess the reporting quality of published RCTs according to the Consolidated Standards of Reporting Trials (CONSORT)...
journal_title:Clinical therapeutics
pub_type: 杂志文章,meta分析,评审
doi:10.1016/j.clinthera.2010.01.028
更新日期:2010-02-01 00:00:00
abstract::A prospective, multicenter, open-label randomized trial was conducted to compare the efficacy and tolerability of imipenem-cilastatin (I-C) monotherapy with clindamycin+aminoglycoside (C+A) combination therapy. Forty-nine patients were able to be evaluated for clinical efficacy in the treatment of postpartum endometri...
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:1992-01-01 00:00:00
abstract:PURPOSE:The contribution of intestinal bacterial strains (gut microbiota) in human metabolism and obesity is being increasingly recognized. The goal of this article was to provide a commentary on the clinical usefulness of these data. METHODS:We performed a review of the currently available articles on PubMed. FINDIN...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2015.03.008
更新日期:2015-06-01 00:00:00
abstract:PURPOSE:The aim of this study was to evaluate prescription patterns of antiasthmatic medications in ambulatory care, guideline adherence by physician specialties and medical institutions, and the rate of hospitalization and emergency department visits due to asthma exacerbation. METHODS:The ambulatory visits between 2...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2015.07.024
更新日期:2015-10-01 00:00:00