Trimetazidine Revisited: A Comprehensive Review of the Pharmacological Effects and Analytical Techniques for the Determination of Trimetazidine

Onay-Beşi̇kçi̇, Arzu; Özkan, Síbel A.

doi:10.1111/j.1527-3466.2008.00043.x

Cited by 35 publications

(24 citation statements)

References 154 publications

(202 reference statements)

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“…TMZ is a crystalline white powder and it exhibits slight hygroscopic properties. TMZ as dihydrochloride has good water solubility and poor solubility in alcohol …”

Section: Introductionmentioning

confidence: 99%

“…TMZ as dihydrochloride has good water solubility and poor solubility in alcohol. [2] TMZ is an effective and well-tolerated anti-anginal drug that has protective properties against ischemia-induced heart injury by shifting cardiac energy metabolism from fatty acid oxidation to glucose oxidation. [3][4][5][6] It leads to the process of restoring coupling between glycolysis and carbohydrate oxidation and results in adenosine triphosphate production with a smaller amount of oxygen consumption.…”

Section: Introductionmentioning

confidence: 99%

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The prevalence of trimetazidine use in athletes in Poland: excretion study after oral drug administration

Jarek

Wójtowicz

Kwiatkowska

et al. 2014

Drug Testing and Analysis

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Stimulants, together with anabolic androgenic steroids, are regarded as one of the most popular doping substances in sport. Owing to a great variety of these substances and new designer drugs being introduced to the market, each year the World Anti-Doping Agency (WADA) updates the list of substances and methods prohibited in sport. On 1 January 2014, a new doping agent - trimetazidine (TMZ) - was added to the WADA Prohibited List. TMZ, a substance prohibited in competition, is classified in the S6b Specified Stimulant Group. TMZ is used as a well-known cardiologic drug with confirmed biochemical and clinical activity. According to knowledge of the pharmacology and mechanism of TMZ action, TMZ can be used by athletes to improve physical efficiency, especially in the case of endurance sports. This study presents the phenomena of TMZ use by Polish athletes involved in anti-doping control in the WADA-accredited laboratory in Warsaw (Poland) between 2008 and 2013. Samples were taken from the athletes of such disciplines as cycling, athletics, and triathlon. Moreover, the elimination study of TMZ has been conducted to establish the change of TMZ concentration in urine sample after oral administration of a single or double (during the long-term therapy) dose. TMZ was monitored in urine samples by gas chromatography-mass spectrometry-nitrogen phosphorus detection (GC-MS-NPD).

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“…TMZ is a crystalline white powder and it exhibits slight hygroscopic properties. TMZ as dihydrochloride has good water solubility and poor solubility in alcohol …”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

The prevalence of trimetazidine use in athletes in Poland: excretion study after oral drug administration

Jarek

Wójtowicz

Kwiatkowska

et al. 2014

Drug Testing and Analysis

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show abstract

“…Trimetazidine may affect myocardial substrate use by inhibiting oxidative phosphorylation and shifting energy production from free fatty acids (FFA) to glucose oxidation 7. It may also contribute to the preservation of intracellular levels of phosphocreatine and ATP,8 reduce calcium overload and free radical-induced injury,9 inhibit cell apoptosis10–12 and improve endothelial function 13. More recently, trimetazidine has been suggested to inhibit cardiac fibrosis through an NADPH oxidase-reactive oxygen species–connective tissue growth factor pathway14 (see figure 1).…”

mentioning

confidence: 99%

Trimetazidine: a meta-analysis of randomised controlled trials in heart failure

Gao

Ning

Niu

et al. 2010

Heart

167

105

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Objective To explore whether trimetazidine could improve symptoms, cardiac functions and clinical outcomes in patients with heart failure (HF). Methods A systematic literature search was conducted to identify randomised controlled trials (RCT) of trimetazidine for HF between 1966 and May 2010 in Pubmed, the Cochrane Central Registry of Clinical Trials and EMBASE. Reports of trials were sought that compared trimetazidine with placebo control for chronic HF in adults, with outcomes including all-cause mortality, hospitalisation, cardiovascular events, changes in cardiac function parameters and exercise capacity. Results 17 trials with data for 955 patients were identified by the literature search. Trimetazidine therapy was associated with a significant improvement in left ventricular ejection fraction in patients with both ischaemic (weighted mean difference (WMD) with placebo 7.37%; 95% CI 6.05 to 8.70; p<0.01) and non-ischaemic HF (WMD 8.72%; 95% CI 5.51 to 11.92; p<0.01). With trimetazidine therapy, left ventricular end-systolic volume was significantly reduced (WMD 10.37 ml; 95% CI 15.46 to 5.29; p<0.01) and New York Heart Association classification was improved (WMD 0.41; 95% CI 0.51 to 0.31; p<0.01) as was exercise duration (WMD, 30.26 s; 95% CI 8.77 to 51.75; p<0.01). More importantly, trimetazidine had a significant protective effect for all-cause mortality (RR 0.29; 95% CI 0.17 to 0.49; p<0.00001) and cardiovascular events and hospitalisation (RR 0.42; 95% CI 0.30 to 0.58; p<0.00001). Conclusion Trimetazidine might be an effective strategy for treating HF. More studies, especially larger multicentre RCT, are warranted to clarify the effect of trimetazidine on HF.With more than 5 million prevalent cases and nearly 1 million hospital discharges yearly, heart failure (HF) represents a rapidly growing therapeutic challenge for healthcare providers.

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“…Correcting energy insufficiency leads to reduced accumulation of sodium in cardiomyocyte cytoplasm, decreased formation of reactive oxygen species (ROS), and reduced neutrophil infiltration [5, 6]. This results in cellular membrane stabilization [7, 8]. …”

Section: Trimetazidine Mechanism Of Actionmentioning

confidence: 99%

Defining the Role of Trimetazidine in the Treatment of Cardiovascular Disorders: Some Insights on Its Role in Heart Failure and Peripheral Artery Disease

Chruściel

Rysz

Banach

2014

Drugs

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Trimetazidine is a cytoprotective drug whose cardiovascular effectiveness, especially in patients with stable ischemic heart disease, has been the source of much controversy in recent years; some have gone so far as to treat the medication as a ‘placebo drug’ whose new side effects, such as Parkinsonian symptoms, outweigh its benefits. This article is an attempt to present the recent key studies, including meta-analyses, on the use of trimetazidine in chronic heart failure, also in patients with diabetes mellitus and arrhythmia, as well as in peripheral artery disease. This paper also includes the most recent European Society of Cardiology guidelines, including those of 2013, on the use of trimetazidine in cardiovascular disease.

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Trimetazidine Revisited: A Comprehensive Review of the Pharmacological Effects and Analytical Techniques for the Determination of Trimetazidine

Cited by 35 publications

References 154 publications

The prevalence of trimetazidine use in athletes in Poland: excretion study after oral drug administration

The prevalence of trimetazidine use in athletes in Poland: excretion study after oral drug administration

Trimetazidine: a meta-analysis of randomised controlled trials in heart failure

Defining the Role of Trimetazidine in the Treatment of Cardiovascular Disorders: Some Insights on Its Role in Heart Failure and Peripheral Artery Disease

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