Ranolazine: A Contemporary Review

Rayner-Hartley, Erin; Sedlak, Tara

doi:10.1161/jaha.116.003196

Cited by 261 publications

(61 citation statements)

References 62 publications

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“…Ranolazine is an active piperazine derivative that is structurally related to trimetazidine 60 . The exact mechanism of action of ranolazine is difficult to elucidate.…”

Section: Ranolazinementioning

confidence: 99%

“…Subsequently, ranolazine was shown to cause concentration-dependent, voltage-dependent, and frequency-dependent inhibition of the late sodium current. By inhibiting late sodium efflux, ranolazine prevents intracellular calcium overload and its deleterious effects 60 . The therapeutic concentration needed to reduce calcium overload is similar to that at which an increase in glucose oxidation was observed.…”

Section: Ranolazinementioning

confidence: 99%

“…Reduction of chronic stable angina occurs without affecting heart rate, blood pressure, or myocardial perfusion. Under these circumstances, if one excludes a possible benefit from an improvement in anaerobic metabolism under ischaemic conditions, the only plausible explanation for the antianginal effects is reduced left ventricular wall tension and, therefore, a reduction in oxygen demand owing to prevention of calcium overload during ischaemia 60 . This property also accounts for a prolongation of the corrected QT interval, which leads to contraindication of the drug.…”

Section: Ranolazinementioning

confidence: 99%

“…• A systematic review of randomized, controlled trials and a Cochrane meta-analysis concluded that the extended-release formulation of 500 mg or 1,000 mg of ranolazine is effective in reducing symptoms of chronic stable angina, similarly to all the other currently used antianginal agents 60 , and its neutral haemodynamic profile could be useful in cases of bradycardia and/or hypotension.…”

Section: Key Points For Ranolazinementioning

confidence: 99%

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A 'diamond' approach to personalized treatment of angina

et al. 2017

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Chronic stable angina pectoris is the most prevalent symptomatic manifestation of ischaemic heart disease, and its management is a priority (BOX 1). Current clinical guidelines recommend antianginal therapy to control symptoms, before considering coronary artery revasculariza tion [1][2][3][4] . However, revascularization by either percutaneous coronary angioplasty or CABG surgery is indicated in patients who have significant artery steno sis (50% left main narrowing or proximal three-vessel disease) to reduce myocardial ischaemia and its adverse clinical manifestation. Antianginal agents are approved by documenting that they improve total exercise duration, together with a reduction in daily frequency of chronic stable angina compared with placebo and/or equivalence to an active comparator. Cardiovascular outcomes, although highly advocated, are not a pre requisite for regulatory approval. None of the antianginal drugs has been proved to reduce cardiovascular mortality or the rate of myocardial infarction. When patients are optimally treated, mortality for chronic stable angina is low, which might explain why all trials designed to improve prognosis have been negative. Guidelines recom mend a first-choice and a second-choice approach, based more on tradition and expert opinion, rather than evidence. This categorical approach has been questioned in the past couple of years 5-8 . Newer antianginal drugs, which are classified as second choice, have more evidence-based clinical data that are more contemporary to support their use than is available for the traditional first-choice drugs. Equally, the often-needed combin ation of double or triple therapy is based on expert opinion and not related to the underlying pathophysio logy. What constitutes optimal antianginal treatment, therefore, varies considerably between countries, and the majority of doctors treat their patients according to their own preconceptions.A group of experts with experience and interest in chronic stable angina met at the University of Ferrara, Italy, to discuss an individualized approach to medical treatment of chronic stable angina, on the basis E X P E RT C O N S E N S U S D O C U M E N TA 'diamond' approach to personalized treatment of angina Abstract | In clinical guidelines, drugs for symptomatic angina are classified as being first choice (β-blockers, calcium-channel blockers, short-acting nitrates) or second choice (ivabradine, nicorandil, ranolazine, trimetazidine), with the recommendation to reserve second-choice medications for patients who have contraindications to first-choice agents, do not tolerate them, or remain symptomatic. No direct comparisons between first-choice and second-choice treatments have demonstrated the superiority of one group of drugs over the other. Meta-analyses show that all antianginal drugs have similar efficacy in reducing symptoms, but provide no evidence for improvement in survival. The newer, second-choice drugs have more evidence-based clinical data that are more contemporary than is available for tr...

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“…Ranolazine is an active piperazine derivative that is structurally related to trimetazidine 60 . The exact mechanism of action of ranolazine is difficult to elucidate.…”

Section: Ranolazinementioning

confidence: 99%

Section: Ranolazinementioning

confidence: 99%

Section: Ranolazinementioning

confidence: 99%

Section: Key Points For Ranolazinementioning

confidence: 99%

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A 'diamond' approach to personalized treatment of angina

et al. 2017

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“…Ranolazine is a new medication indicated for the cases of refractory angina despite conventional anti‐ischemic regimens 1, 2. Its anti‐ischemic effects have been demonstrated by several clinical trials 3, 4, 5, 6.…”

Section: Introductionmentioning

confidence: 99%

Impact of ranolazine on ventricular arrhythmias – A systematic review

Bazoukis

Tse

Letsas

et al. 2018

Journal of Arrhythmia

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Ranolazine is a new medication for the treatment of refractory angina. However, except its anti‐anginal properties, it has been found to act as an anti‐arrhythmic. The aim of our systematic review is to present the existing data about the impact of ranolazine in ventricular arrhythmias. We searched MEDLINE and Cochrane databases as well clinicaltrials.gov until September 1, 2017 to find all studies (clinical trials, observational studies, case reports/series) reported data about the impact of ranolazine in ventricular arrhythmias. Our search revealed 14 studies (3 clinical trials, 2 observational studies, 8 case reports, 1 case series). These data reported a beneficial impact of ranolazine in ventricular tachycardia/fibrillation, premature ventricular beats, and ICD interventions in different clinical settings. The existing data highlight the anti‐arrhythmic properties of ranolazine in ventricular arrhythmias.

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Multitargeting in cardioprotection: An example of biaromatic compounds

Mokrov

2023

Archiv der Pharmazie

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A multitarget drug design approach is actively developing in modern medicinal chemistry and pharmacology, especially with regard to multifactorial diseases such as cardiovascular diseases, cancer, and neurodegenerative diseases. A detailed study of many well‐known drugs developed within the single‐target approach also often reveals additional mechanisms of their real pharmacological action. One of the multitarget drug design approaches can be the identification of the basic pharmacophore models corresponding to a wide range of the required target ligands. Among such models in the group of cardioprotectors is the linked biaromatic system. This review develops the concept of a “basic pharmacophore” using the biaromatic pharmacophore of cardioprotectors as an example. It presents an analysis of possible biological targets for compounds corresponding to the biaromatic pharmacophore and an analysis of the spectrum of biological targets for the five most known and most studied cardioprotective drugs corresponding to this model, and their involvement in the biological effects of these drugs.

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Ranolazine: A Contemporary Review

Cited by 261 publications

References 62 publications

A 'diamond' approach to personalized treatment of angina

A 'diamond' approach to personalized treatment of angina

Impact of ranolazine on ventricular arrhythmias – A systematic review

Multitargeting in cardioprotection: An example of biaromatic compounds

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