- |||||||||| ranolazine ER / Generic mfg.
Review, Journal: Calcium Signaling Silencing in Atrial Fibrillation: Implications for Atrial Sodium Homeostasis. (Pubmed Central) - Nov 4, 2021
Here, we review calcium signaling silencing and changes in intracellular Na homeostasis during AF. We summarize the proposed arrhythmogenic mechanisms associated with increases in I during AF and discuss the evidence from clinical trials that have tested the pharmacological I blocker ranolazine in the treatment of AF.
- |||||||||| ranolazine ER / Generic mfg.
Clinical, Journal: Plasma Omega-3 Fatty Acids and the Risk of Cardiovascular Events in Patients After an Acute Coronary Syndrome in MERLIN-TIMI 36. (Pubmed Central) - Oct 28, 2021
P3
Methods and Results Baseline plasma ω3-PUFA composition (α-linolenic acid, eicosapentaenoic acid, docosapentaenoic acid, and docosahexaenoic acid) was assessed through gas chromatography with flame ionization detection in a case-cohort study involving 203 patients with cardiovascular death, 325 with myocardial infarction, 271 with ventricular tachycardia, and 161 with atrial fibrillation, and a random sample of 1612 event-free subjects as controls from MERLIN-TIMI 36 (Metabolic Efficiency With Ranolazine for Less Ischemia in Non-ST-Elevation-Acute Coronary Syndrome-Thrombolysis in Myocardial Infarction 36), a trial of patients hospitalized with non-ST-segment-elevation -acute coronary syndrome...Registration URL: https://www.clinicaltrials.gov. Unique identifier: NCT00099788.
- |||||||||| ranolazine ER / Generic mfg.
Clinical, Journal: Arrhythmogenic and antiarrhythmic actions of late sustained sodium current in the adult human heart. (Pubmed Central) - Oct 22, 2021
These effects could be reversed by late INa inhibitors, ranolazine and GS-967...These findings reveal a critical role for the late INa in cardiac arrhythmias and suggest that inhibition of this conductance could provide an effective therapeutic strategy. Finally, this study highlights the utility of human ex-vivo heart models for advancing cardiac translational sciences.
- |||||||||| Procoralan (ivabradine) / Amgen, Servier, Ono Pharma
Journal: Achieving Optimal Medical Therapy: Insights From the ORBITA Trial. (Pubmed Central) - Oct 15, 2021
P=N/A
Isosorbide mononitrate and nicorandil were stopped for adverse effects in 36 of 172 (20.9%) and 32 of 141 (22.7%) of patients, respectively...Truly optimal medical therapy can be achieved in clinical trials, and translating this into longer-term clinical practice should be a focus of future study. Registration URL: https://www.clinicaltrials.gov; Unique identifier: NCT02062593.
- |||||||||| cetirizine oral / Generic mfg., spironolactone / Generic mfg., epoprostenol intravenous / Generic mfg.
[VIRTUAL] SEVERE THROMBOCYTOPENIA DUE TO IV EPOPROSTENOL: DON'T MUCK WITH THE PLATELETS () - Oct 13, 2021 - Abstract #CHEST2021CHEST_2256;
It appears to have a dose-dependent relationship and may improve with changing to an alternative prostacyclin. It is critical to recognize this phenomenon as profound thrombocytopenia can not only be dangerous, but also preclude lung transplant candidacy, should it become necessary
- |||||||||| spironolactone / Generic mfg.
[VIRTUAL] BRASH SYNDROME: A DOWNWARD SPIRAL () - Oct 13, 2021 - Abstract #CHEST2021CHEST_534;
Treatment is tailored to correcting the individual abnormalities. Many of these case reports had favorable outcomes.
- |||||||||| Minnebro (esaxerenone) / Daiichi Sankyo
Journal: Effective Accentuation of Voltage-Gated Sodium Current Caused by Apocynin (4'-Hydroxy-3'-methoxyacetophenone), a Known NADPH-Oxidase Inhibitor. (Pubmed Central) - Sep 29, 2021
Likewise, in HL-1 murine cardiomyocytes, the aPO presence increased the peak amplitude of I as well as decreased the inactivation or deactivation rate of the current, and further addition of ranolazine or esaxerenone attenuated aPO-accentuated I. Altogether, this study provides a distinctive yet unidentified finding that, despite its effectiveness in suppressing NOX activity, aPO may directly and concertedly perturb the amplitude, gating and voltage-dependent hysteresis of I in electrically excitable cells. The interaction of aPO with ionic currents may, at least in part, contribute to the underlying mechanisms through which it affects neuroendocrine, endocrine or cardiac function.
- |||||||||| verapamil / Generic mfg.
Journal: Confounders and Pharmacological Characterization When Using the QT, JTp, and Tpe Intervals in Beagle Dogs. (Pubmed Central) - Sep 25, 2021
Dofetilide (0.1, 0.3, 1.0 mg/kg), ranolazine (100, 140, 200 mg/kg), and verapamil (7, 15, 30, 43, 62.5 mg/kg) were administered to evaluate pharmacological effects...Results highlight potential confounders on QTc interval, but also on JTpca and Tpeca intervals in nonclinical studies. These potential confounding effects may be relevant to the interpretation of ECG data obtained from nonclinical drug safety studies with Beagle dogs.
- |||||||||| ranolazine ER / Generic mfg.
Journal: The mechanism underlying transient weakness in myotonia congenita. (Pubmed Central) - Sep 15, 2021
Inhibiting NaPIC with ranolazine prevents the development of plateau potentials and eliminates transient weakness in vivo. These data suggest that targeting NaPIC may be an effective treatment to prevent transient weakness in myotonia congenita.
- |||||||||| ranolazine ER / Generic mfg.
Preclinical, Journal: Cardiac calcium dysregulation in mice with chronic kidney disease. (Pubmed Central) - Sep 10, 2021
Electrocardiography showed that CKD mice exhibited longer QT interval, corrected QT (QTc) prolongation, faster spontaneous activities, shorter action potential duration (APD) and increased ventricle arrhythmogenesis, and ranolazine (10 µmol/L) blocked these effects...In conclusions, the modulation of CaMKII, PLB and late Na current in CKD significantly altered cardiac Ca regulation and electrophysiological characteristics. These findings may apply on future clinical therapies.
- |||||||||| Vimpat (lacosamide) / UCB, Daiichi Sankyo
Journal: Buprenorphine may be effective for treatment of paramyotonia congenita. (Pubmed Central) - Sep 10, 2021
The exercise test may be useful for quantitative assessment of treatment response. Further studies on a larger number of patients, under carefully controlled conditions, should be considered to address effectiveness and long-term tolerability of this possible therapeutic option.
- |||||||||| Tectin (tetrodotoxin) / WEX Pharma
Journal: Effectiveness of Columbianadin, a Bioactive Coumarin Derivative, in Perturbing Transient and Persistent I. (Pubmed Central) - Sep 9, 2021
The delayed-rectifier or erg-mediated K current was mildly inhibited by 10 µM CBN, while it also slightly inhibited the amplitude of hyperpolarization-activated cation current. In HL-1 atrial cardiomyocytes, CBN inhibited peak I and raised the inactivation rate of the current; moreover, further application of 10 µM Tef attenuated CBN-mediated decrease in I. Collectively, this study provides an important yet unidentified finding revealing that CBN modifies I in electrically excitable cells.
- |||||||||| trimetazidine / Generic mfg., ranolazine ER / Generic mfg.
Review, Journal: Contemporary approach to understand and manage COVID-19-related arrhythmia. (Pubmed Central) - Aug 31, 2021
Of these drugs, we discuss the potential role of adrenergic antagonists, trimetazidine, ranolazine, and the debatable angiotensin converting enzyme inhibitors drugs. We also recommend monitoring the level of: unbound free fatty acids, serum electrolytes, troponin, and QTc (even in the absence of apparent pro-arrhythmic drug use) as these may be the only indicators for patients at risk for arrhythmic complications.
- |||||||||| ranolazine ER / Generic mfg.
Journal: Abnormalities in Sodium Current and Calcium Homeostasis as Drivers of Arrhythmogenesis in Hypertrophic Cardiomyopathy. (Pubmed Central) - Aug 25, 2021
As an array of novel experimental opportunities have emerged to investigate these mechanisms, including novel "disease-in-the-dish" cellular models with patient-specific induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs), important gaps in knowledge remain. Accordingly, the aim of the present review is to provide a contemporary reappraisal of the cellular basis of SCD-predisposing arrhythmias in patients with HCM and discuss the implications for risk stratification and management.
- |||||||||| ranolazine ER / Generic mfg.
Journal: A critical appraisal of the pharmacological management of stable angina. (Pubmed Central) - Aug 20, 2021
In this paper, we propose an alternative approach to the medical management of patients with chronic CAD and stable angina, based on the properties of the drugs currently available in the anti-ischemic armamentarium in relation to the pathophysiology of myocardial ischemia. In this approach, pharmacological therapy is organized into three steps, including disease-modifying therapy for all patients with chronic CAD, pathophysiology-based anti-ischaemic therapy for patients with stable angina and symptomatic therapy in patients with persistent anginal symptoms.
- |||||||||| mavacamten (SAR439152) / BMS
Journal: Isogenic models of hypertrophic cardiomyopathy unveil differential phenotypes and mechanism-driven therapeutics. (Pubmed Central) - Aug 14, 2021
Our data show that hypercontractility and molecular signaling within HCM are not uniform between different gene mutations, suggesting that a 'one-size fits all' treatment underestimates the complexity of the disease. Understanding where the similarities (arrhythmogenesis, bioenergetics) and differences (contractility, molecular profile) lie will allow development of therapeutics that are directed towards common mechanisms or tailored to each disease variant, hence providing effective patient-specific therapy.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
Review, Journal: Diabetogenic effects of cardioprotective drugs. (Pubmed Central) - Jul 11, 2021
Dihydropyridine calcium channel blockers, low dose diuretics, vasodilating beta blockers, alfa-blockers and pitavastatin have little or no effect on glycemic control. Blockers of the renin-angiotensin-aldosterone system, colesevelam, ranolazine and verapamil through slowing breakdown of bradykinin, vasodilation, increasing cholecystokinin levels, blocking sodium channels, and decreasing beta cell apoptosis may improve glycemic control and avoid the development of diabetes.
- |||||||||| ranolazine ER / Generic mfg.
Preclinical, Journal: Mechanical effects of ranolazine on normal and diabetic-isolated rat heart. (Pubmed Central) - Jul 6, 2021
It is concluded that in the isolated rat heart preparation, ranolazine has no benefit on diabetic cardiomyopathy and may even worsen it. It seems that these effects are related to the metabolic effects of ranolazine.
- |||||||||| verapamil / Generic mfg., ranolazine ER / Generic mfg.
Journal: Relaxant and antiadrenergic effects of ranolazine in human saphenous vein. (Pubmed Central) - Jun 22, 2021
Ranolazine diminishes the adrenergic vasoconstriction, acting as α1 antagonist, and by increasing large conductance Ca2+-activated K+ channel involvement. The relaxant effects of ranolazine are partially mediated by endothelial nitric oxide, large conductance Ca2+-activated K+ channels and the blockade of voltage-dependent Ca2+ channels.
- |||||||||| ranolazine ER / Generic mfg.
Preclinical, Journal: Protective effects of Ranolazine on testicular torsion and detorsion injury in rats. (Pubmed Central) - Jun 22, 2021
As a result of the objective biochemical and pathological criteria used in this study, this protective effect of ranolazine was observed in testis torsion. The results obtained in this study may suggest that ranolazine is a drug that could be applied after detorsion to patients diagnosed with torsion.
- |||||||||| trimetazidine / Generic mfg., ranolazine ER / Generic mfg.
Journal: Antinociceptive Effect of Ranolazine and Trimetazidine. (Pubmed Central) - Jun 16, 2021
Ranolazine and trimetazidine are two effective drugs in antianginal treatment. While both drugs are effective on general systemic musculoskeletal pain and anxiety, the efficacy of ranolazine is more pronounced.
- |||||||||| ranolazine ER / Generic mfg.
Journal: 18β-Glycyrrhetinic Acid Improves Cardiac Diastolic Function by Attenuating Intracellular Calcium Overload. (Pubmed Central) - Jun 11, 2021
Ranolazine, a late sodium current inhibitor, has been demonstrated to be effective on heart failure...The study demonstrates that 18β-GA and glycyrrhizin could improve diastolic dysfunction induced by ischemia-reperfusion injury in Langendorff-perfused rat hearts and pressure-overloaded rats. The mechanism may be attributed to the inhibition of enhanced late sodium currents.
- |||||||||| Nurtec ODT (rimegepant ODT) / Portage
[VIRTUAL] Effect of strong P-gp and BCRP inhibition, using cyclosporine and quinidine as probes, on the pharmacokinetics of oral rimegepant 75 mg in healthy subjects () - Jun 4, 2021 - Abstract #AHS2021AHS_385;
The moderate effect on rimegepant exposure may be generalizable to other strong P-gp inhibitors, such as amiodarone, carvedilol, dronedarone, lapatinib, propafenone, ranolazine, and verapamil. The similar effect of cyclosporine and quinidine on rimegepant exposure suggests that BCRP inhibition has minimal influence on rimegepant exposure.
- |||||||||| ranolazine ER / Generic mfg.
Clinical, Journal: Angina relates to coronary flow in women with ischemia and no obstructive coronary artery disease. (Pubmed Central) - May 29, 2021
Among women with suspected INOCA, angina relates to high bAPV, a result supported by the concomitant greater use of anti-anginal drugs. These results suggest that high bAPV contributes to impaired CFR and may represent a specific pathophysiologic contributor to CMD and may be a treatment target in INOCA subjects.
- |||||||||| ranolazine ER / Generic mfg.
Enrollment open: REACT: Reduce Crohn's-Associated Diarrhea With Sodium Channel Therapy (clinicaltrials.gov) - May 13, 2021
P2, N=16, Enrolling by invitation,
This information may be helpful for selecting drugs for treating SQT1-patients with hERG channel mutation. Not yet recruiting --> Enrolling by invitation
- |||||||||| verapamil / Generic mfg., dofetilide / Generic mfg., ranolazine ER / Generic mfg.
Clinical, Journal, Heterogeneity: Changes In Global Electrical Heterogeneity Associated With Dofetilide, Quinidine, Ranolazine, And Verapamil. (Pubmed Central) - May 6, 2021
These changes, which differ by gender, are likely driven by alterations in ion-channel function and dispersion of depolarization or repolarization. GEH measurement may allow early assessment of favorable or adverse AAD effects.
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