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ivabradine

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Description

Ivabradine: A benzazepine derivative and selective HYPERPOLARIZATION-ACTIVATED CYCLIC NUCLEOTIDE-GATED CHANNELS inhibitor that lowers the heart rate. It is used in the treatment of CHRONIC STABLE ANGINA in patients unable to take BETA-ADRENERGIC BLOCKERS, and in the treatment of HEART FAILURE. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ivabradine : A member of the class of benzazepines that is 7,8-dimethoxy-1,3,4,5-tetrahydro-3-benzazepin-2-one in which the amide hydrogen is replaced by a [{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]propyl} group. Used (as its hydrochloride salt) to treat patients with angina who have intolerance to beta blockers and/or heart failure. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID132999
CHEMBL ID471737
CHEBI ID85966
SCHEMBL ID23472
MeSH IDM0234009

Synonyms (57)

Synonym
3-[3-[[(8s)-3,4-dimethoxy-8-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1h-3-benzazepin-4-one
gtpl2357
s-16257
(s)-3-(3-(((3,4-dimethoxybicyclo(4.2.0)octa-1,3,5-trien-7-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-2h-3-benzazepin-2-one
s 16257-2
7,8-dimethoxy-3-(3-(((4,5-dimethoxybenzocyclobutan-1-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-2h-benzazepin-2-one
2h-3-benzazepin-2-one, 3-(3-(((3,4-dimethoxybicyclo(4.2.0)octa-1,3,5-trien-7-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-, (s)-
ivabradine [inn]
ivabradine
s 16257
3-(3-((((7s)-3,4-dimethoxybicyclo(4.2.0)octa-1,3,5-trien-7-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-2h-3-benzazepin-2-one
155974-00-8
ivabradine (usan/inn)
D07165
chebi:85966 ,
CHEMBL471737 ,
3-[3-[[(7s)-3,4-dimethoxy-7-bicyclo[4.2.0]octa-1,3,5-trienyl]methyl-methylamino]propyl]-7,8-dimethoxy-2,5-dihydro-1h-3-benzazepin-4-one
bdbm50326992
3-{3-[{[(7s)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)-amino]propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-2h-3-benzazepin-2-one
3-{3-[{[(7s)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]-propyl}-7.8-dimethoxy-1,3,4,5-tetrahydro-2h-3-benzazepin-2-one
3-{3-[{[(7s)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino]propyl}-7,8-dimethoxy-1,3,4,5-tetrahydro-2h-3-benzazepin-2-one
ACRHBAYQBXXRTO-OAQYLSRUSA-N
3h48l0lpzq ,
unii-3h48l0lpzq
ivabradine [usan:inn:ban]
ivabradine [usan]
ivabradine [who-dd]
ivabradine [mart.]
ivabradine [mi]
ivabradine [ema epar]
ivabradine [orange book]
S16257 ,
AKOS015896494
SCHEMBL23472
DTXSID2048240 ,
AB01566878_01
3-[3-({[(7s)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl}(methyl)amino)propyl]-7,8-dimethoxy-2,3,4,5-tetrahydro-1h-3-benzazepin-2-one
DB09083
AC-8848
BCP21052
Q425729
AR-270/43507923
NCGC00181343-03
AT22349
2h-3-benzazepin-2-one, 3-(3-((((7s)-3,4-dimethoxybicyclo(4.2.0)octa-1,3,5-trien-7-yl)methyl)methylamino)propyl)-1,3,4,5-tetrahydro-7,8-dimethoxy-
2h-3-benzazepin-2-one, 3-[3-[[[(7s)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]methyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-
CS-0012360
HY-B0162
EN300-20600170
c01eb17
3-(3-((((7s)-3,4-dimethoxybicyclo(4.2.0)octa-1,3,5-trien-7-yl)methyl)(methyl)amino)propyl)-7,8-dimethoxy-1,3,4,5-tetrahydro-2h-3-benzazepin-2-one
ivabradina
3-(3-((((7s)-3,4-dimethoxybicyclo(4.2.0)octa-1,3,5-trien-7-yl)methyl)(methyl)amino)propyl)-7,8-dimethoxy-2,3,4,5-tetrahydro-1h-3-benzazepin-2-one
dtxcid3028215
ivabradin
ivabradine (mart.)
ivabradinum

Research Excerpts

Overview

Ivabradine is an inhibitor of funny current (If) in cardiac pacemaker cells by blocking hyperpolarization-activated cyclic nucleotide-gated (HCN) It is an effective treatment for focal atrial tachycardia.

ExcerptReferenceRelevance
"Ivabradine is a 'heart rate-reducing' agent able to slow heart rate, without complicating side-effects. "( Properties of ivabradine-induced block of HCN1 and HCN4 pacemaker channels.
Baruscotti, M; Bucchi, A; DiFrancesco, D; Milanesi, R; Tognati, A, 2006
)
2.14
"Ivabradine is an inhibitor of funny current (If) in cardiac pacemaker cells by blocking hyperpolarization-activated cyclic nucleotide-gated (HCN)."( The use of ivabradine in a patient with idiopathic ventricular arrhythmia originating from the left ventricular summit.
Çinier, G; Gürkan, K; Hayıroğlu, Mİ; Özcan, KS; Pay, L; Tekkeşin, Aİ,
)
1.24
"Ivabradine is an effective treatment for focal atrial tachycardia. "( Report of a patient with refractory atrial tachycardia whose heart rate was controlled using ivabradine.
He, R; Liu, Y; She, F; Xie, Y; Zhang, P; Zhao, L, 2022
)
2.38
"Ivabradine is a drug that selectively reduces HR via If current inhibition in the sinoatrial node without a negative effect on inotropy."( Ivabradine in the Management of COVID-19-related Cardiovascular Complications: A Perspective.
Baka, T; Luptak, I; Repova, K; Simko, F, 2022
)
2.89
"Ivabradine is a specific heart rate (HR)-lowering agent which blocks the cardiac pacemaker I"( Effect of preoperative ivabradine on hemodynamics during elective off-pump CABG.
Geelani, MA; Mallik, I; Minhas, HS; Mohire, VB; Virmani, S,
)
1.88
"Ivabradine is an inhibitor of the If channel, the main determinant of the pacemaker function of the sinus node. "( Ivabradine for chronic heart rate control in persistent atrial fibrillation. Design of the BRAKE-AF project.
Arias, MÁ; Arribas, F; Fontenla, A; Gómez de la Cámara, A; López-Gil, M; Matía-Francés, R; Mejía-Martínez, E; Miracle-Blanco, Á; Montilla, I; Pastor-Fuentes, A; Rey-Blas, JR; Salgado-Aranda, R; Tamargo-Menéndez, J; Toquero-Ramos, J, 2020
)
3.44
"Ivabradine (IVA) is a pure heart rate-lowering agent with well-documented anti-anginal and anti-ischemic properties comparable to well-established anti-anginal agents, such as beta-blockers and calcium channel blockers."( Beneficial effect of ivabradine against cardiovascular diseases.
D'Orazio, N; Gammone, MA; Massari, F; Riccioni, G, 2020
)
1.6
"Ivabradine is a selective inhibitor of hyperpolarization-activated cyclic nucleotide-gated potassium channel 4 generated funny current (I"( Ventricular arrhythmia suppression with ivabradine in a patient with catecholaminergic polymorphic ventricular tachycardia refractory to nadolol, flecainide, and sympathectomy.
Aziz, Z; Beaser, AD; Kohli, U; Nayak, HM, 2020
)
1.55
"Ivabradine is a bradycardic drug used worldwide in the treatment of chronic stable angina and chronic heart failure. "( Fatal intoxication with ivabradine: First case report.
Alvarez, JC; de la Grandamison, GL; Knapp-Gisclon, A; Mayer-Duverneuil, C; Rambaud, C; Zerah, M, 2020
)
2.31
"Ivabradine is a unique medication that reduces the intrinsic heart rate by specifically blocking the inward funny current that controls the pacemaker activity of the sinus node. "( Ivabradine in children with postural orthostatic tachycardia syndrome: a retrospective study.
Grubb, BP; Karabin, B; Mangi, MA; Nesheiwat, Z; Towheed, A, 2020
)
3.44
"Ivabradine is a pure heart-rate lowering drug that is nowadays used, accordingly to the last ESC Guidelines, to reduce mortality and heart failure (HF) hospitalization in patients with HF with reduced ejection fraction and in symptomatic patiens with inappropriate sinus tachycardia. "( Ivabradine and endothelium: an update.
Dallapellegrina, L; Sciatti, E; Vizzardi, E,
)
3.02
"Ivabradine is a heart rate lowering drug with protective effects on heart failure despite increasing the risk of atrial fibrillation."( A genetic model of ivabradine recapitulates results from randomized clinical trials.
Barhdadi, A; de Denus, S; Dubé, MP; Legault, MA; Lemieux Perreault, LP; Lumbers, RT; Provost, S; Sandoval, J; Shah, S; Tardif, JC; Tyl, B, 2020
)
1.61
"Ivabradine (IVA) is an inhibitor of the If channel, the main determinant of the pacemaker function of the sinus node. "( Ivabradine: a new frontier in the treatment of stable coronary artery disease and chronic heart failure.
D'Orazio, N; Gammone, MA; Riccioni, G,
)
3.02
"Ivabradine is a selective inhibitor of the sinoatrial node "funny" current, prolonging the slow diastolic depolarization. "( Ivabradine-Induced Torsade de Pointes in Patients with Heart Failure Reduced Ejection Fraction.
Beak, YS; Choi, SH; Jang, JH; Kim, DH; Ko, KY; Kwan, J; Kwon, SW; Lee, MJ; Park, JH; Park, SD; Shin, SH; Woo, SI; Yoon, GS, 2020
)
3.44
"Ivabradine is a recently introduced selective I"( Implication of Ivabradine in Up-titrating Beta-blocker in a Patient with Advanced Heart Failure.
Hori, M; Imamura, T; Kinugawa, K; Nakamura, M, 2021
)
1.7
"Ivabradine is a new class of HR lowering drug and a specific inhibitor of the I"( Effect of ivabradine on left ventricular diastolic function of patients with heart failure with preserved ejection fraction -IVA-PEF study.
Hatani, Y; Hayashi, T; Hirata, KI; Imanishi, J; Tanaka, H; Yamauchi, Y, 2021
)
1.75
"Ivabradine is a unique agent that is distinct from beta-blockers and calcium channel blockers as it reduces heart rate without affecting myocardial contractility or vascular tone. "( Ivabradine in Cardiovascular Disease Management Revisited: a Review.
Bangalore, S; Chen, C; Godoy, LC; Kaur, G; Mehta, PK; Morrone, D; Sidhu, MS, 2021
)
3.51
"Ivabradine is a new pure bradycardic agent that has been used to treat angina or heart failure reduced ejection fraction (HFrEF) with sinus heart rate above 70 beats per minute."( Impact of ivabradine on the cardiac function of chronic heart failure reduced ejection fraction: Meta-analysis of randomized controlled trials.
Bryan Richard, S; Huang, B; Liu, G; Luo, S; Yang, Y, 2021
)
1.75
"Ivabradine is a selective heart rate-reducing agent, an inhibitor of hyperpolarization-activated, cyclic nucleotide-gated (HCN) channels, currently approved for treatment of coronary artery disease and chronic heart failure."( Effect of ivabradine on cardiac arrhythmias: Antiarrhythmic or proarrhythmic?
Mackiewicz, U; Mączewski, M; Marciszek, M; Oknińska, M; Paterek, A; Zambrowska, Z, 2021
)
1.75
"Ivabradine is a pure heart rate-lowering drug that acts directly on the sinus node and does not affect atrioventricular or intraventricular conduction times, myocardial contractility or ventricular repolarization. "( Efficacy of ivabradine in HIV-associated dilated cardiomyopathy.
Greco, S; Guadagnino, G; Mastroianni, A; Urso, F; Vangeli, V, 2021
)
2.44
"Ivabradine is an original drug that has been approved in two indications (systolic heart failure and angina). "( Limited role and benefit of ivabradine in the treatment of angina and heart failure with reduced ejection fraction.
Bouvaist, H; Cosgrove, S; Ennezat, PV; Le Jemtel, TH; Marechaux, S; Vital Durand, D, 2017
)
2.19
"Ivabradine is a selective I"( Ivabradine in the treatment of postural tachycardia syndrome (POTS), a single center experience.
Alhazmi, L; Ammari, Z; Dasa, O; Grubb, B; Karabin, B; Ruzieh, M; Sirianni, N, 2017
)
3.34
"Ivabradine is a selective and specific inhibitor of the I(f) current in the sinoatrial and atrioventricular nodes. "( Ivabradine in Postural Orthostatic Tachycardia Syndrome: Preliminary Experience in Children.
Daubeney, PEF; Delle Donne, G; Prasad, SK; Rosés Noguer, F; Salukhe, T; Till, J, 2018
)
3.37
"Ivabradine is a novel heart rate (HR) lowering agent that acts on the sinoatrial node cells by selectively inhibiting the If-current."( Ivabradine for the Treatment of Postural Orthostatic Tachycardia Syndrome: A Systematic Review.
Brown, JN; Gee, ME; Watkins, AK; Young, EJA, 2018
)
2.64
"Ivabradine is a pure HR-lowering agent, and it does not affect myocardial contractility, blood pressure, intracardiac conduction, or ventricular repolarization."( Novel drugs for heart rate control in heart failure.
Banach, M; Bielecka-Dabrowa, A; Rysz, J; von Haehling, S, 2018
)
1.2
": Ivabradine is a selective and specific inhibitor of If current. "( Real-life indications to ivabradine treatment for heart rate optimization in patients with chronic systolic heart failure.
Fragasso, G; Gemma, M; Godino, C; Margonato, A; Montanaro, C; Pinto, G; Salerno, A; Slavich, M; Spoladore, R; Tondi, L, 2018
)
1.51
"Ivabradine is a heart rate lowering agent that acts on the funny current (I"( Role of ivabradine and heart rate lowering in chronic heart failure: guideline update.
Chow, SL; Depre, C; Page, RL, 2018
)
1.64
"Ivabradine is a selective bradycardic agent that inhibits hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. "( Ivabradine preserves dynamic sympathetic control of heart rate despite inducing significant bradycardia in rats.
Hayama, Y; Kawada, T; Nishikawa, T; Shimizu, S; Shishido, T; Sugimachi, M; Uemura, K; Yamamoto, H, 2019
)
3.4
"Ivabradine is a selective inhibitor of the sinoatrial pacemaker modulating "f-current" (I"( The Use and Indication of Ivabradine in Heart Failure.
Dodd, K; Lampert, BC, 2018
)
1.5
"Ivabradine is a funny current inhibitor which is administered to patients with congestive heart failure to reduce their heart rate (HR) and attenuate oxidative stress. "( Effect of ivabradine, a funny current inhibitor, on portal hypertensive rats.
Chang, CC; Chuang, CL; Hsin, IF; Hsu, SJ; Huang, HC; Lee, FY; Lee, SD; Lee, WS, 2019
)
2.36
"Ivabradine is a heart rate-lowering drug that does not cause hypotension and may be used in heart failure with reduced left ventricular ejection fraction (LVEF)."( Ivabradine in Cancer Treatment-Related Left Ventricular Dysfunction.
Arboscello, E; Balbi, M; Bighin, C; Brunelli, C; Ghigliotti, G; Gualandi, F; Murialdo, R; Sarocchi, M; Sicbaldi, V; Spallarossa, P, 2018
)
2.64
"Ivabradine appears to be an effective alternative to Amiodarone in children with post-operative JET based on our initial clinical experience."( Ivabradine in Post-operative Junctional Ectopic Tachycardia (JET): Breaking New Ground.
Balaji, S; Krishna, MR; Kumar, RK; Kunde, MF, 2019
)
2.68
"Ivabradine is an interesting substance since it is known to produce migraine-like phosphenes frequently and the patient we report developed de novo migraine with aura. "( New onset migraine with aura after treatment initiation with ivabradine.
Goadsby, PJ; Sprenger, T; Supronsinchai, W, 2013
)
2.07
"Ivabradine is an anti-anginal and anti-ischaemic agent, which selectively and specifically inhibits the I f current in the sino-atrial node and provides pure heart rate reduction without altering other cardiac parameters, including conduction, and without directly affecting other haemodynamic parameters."( Selective and specific inhibition of If with ivabradine for the treatment of coronary artery disease or heart failure.
Deedwania, P, 2013
)
1.37
"Ivabradine is a pure heart rate-lowering agent that acts by inhibiting I(f), an important ionic current involved in pacemaker activity in the cells of the sinoatrial node. "( Pharmacokinetic and safety profile of ivabradine in healthy Chinese men: a phase I, randomized, open-label, increasing single- and multiple-dose study.
Huang, Y; Jiang, J; Li, Y; Tian, L; Xu, L, 2013
)
2.1
"Ivabradine is a new heart-rate-lowering drug; the aim of this review was to analyze its role in heart failure (HF)."( An evaluation of the pharmacokinetics and pharmacodynamics of ivabradine for the treatment of heart failure.
Brunelli, C; Ferrero, S; Ghione, P; Rosa, GM; Valbusa, A, 2014
)
2.09
"Ivabradine is a pure heart rate-reducing agent that has no effect on blood pressure and contractility, and can reverse left ventricular (LV) remodelling in patients with heart failure."( Effect of ivabradine on left ventricular remodelling after reperfused myocardial infarction: A pilot study.
Bonnet, J; Chasseriaud, W; Cochet, H; Coste, P; Douard, H; Gerbaud, E; Gilbert, S; Horovitz, A; Montaudon, M; Pucheu, Y, 2014
)
1.53
"Ivabradine is a selective inhibitor of the pacemaker current If and since If is impaired by lipopolysaccharide (LPS, endotoxin), a trigger of sepsis, we aimed to explore If blocking potency of ivabradine under elevated endotoxin levels in human atrial cardiomyocytes."( I(f) blocking potency of ivabradine is preserved under elevated endotoxin levels in human atrial myocytes.
Hallström, S; Koyani, CN; Lang, P; Lohner, K; Mächler, H; Malle, E; Pelzmann, B; Platzer, D; Scheruebel, S; Zorn-Pauly, K, 2014
)
1.43
"Ivabradine is a negative chronotropic drug with minimal effects on central hemodynamics. "( Acute effects of ivabradine on dynamic obstruction of the left ventricular outflow tract in cats with preclinical hypertrophic cardiomyopathy.
Blass, KA; Bonagura, JD; Li, X; Scansen, BA; Schober, KE,
)
1.91
"Ivabradine is a drug used for the treatment of angina and chronic heart failure in cases of intolerance or insufficiency of response to beta-blocker treatment. "( Case report of ivabradine intoxication.
Dulaurent, S; Gaulier, JM; Julia, F; Mathiaux, F, 2014
)
2.2
"Ivabradine is a heart rate (HR)-lowering agent acting by inhibiting the If-channel. "( Ivabradine treatment prevents dobutamine-induced increase in heart rate in patients with acute decompensated heart failure.
Cavusoglu, Y; Mert, U; Morrad, B; Mutlu, F; Nadir, A; Ulus, T, 2015
)
3.3
"Ivabradine is a novel specific heart rate (HR)-lowering agent that improves event-free survival in patients with heart failure (HF)."( Ivabradine improves heart rate variability in patients with nonischemic dilated cardiomyopathy.
Balta, S; Cuglan, B; Gozubuyuk, G; Kaplan, O; Karakus, Y; Kurtoglu, E; Yasar, E, 2014
)
3.29
"Ivabradine is a useful, effective and safe drug for therapy in NM patients with HF and should be considered when resting HR remains high despite beta-blockers' full titration or beta-blockers' underdosing due to intolerance or side effects."( Nemaline myopathy and heart failure: role of ivabradine; a case report.
Baviera, EP; Di Franco, A; Lanza, GA; Mandalà, G; Marazia, S; Salerno, Y; Sarullo, FM; Sarullo, S; Vassallo, L; Vitale, G, 2015
)
1.4
"Ivabradine is an effective and well-tolerated anti-anginal treatment in patients with stable angina after PCI. "( Ivabradine in combination with Beta-blockers in patients with chronic stable angina after percutaneous coronary intervention.
Ebelt, H; Höpfner, F; Müller-Werdan, U; Nuding, S; Stöckl, G; Werdan, K, 2015
)
3.3
"Ivabradine is a drug designed to lower heart rate without any other demonstrable pharmacologic effects; in other words, a pure heart rate-lowering drug."( Ivabradine: A Unique and Intriguing Medication for Treating Cardiovascular Disease.
Anderson, JR; Bowman, BN; Nawarskas, JJ,
)
2.3
"Ivabradine is a specific bradycardic agent used in coronary artery disease and heart failure, lowering heart rate through inhibition of sinoatrial nodal HCN-channels. "( hERG potassium channel blockade by the HCN channel inhibitor bradycardic agent ivabradine.
Brack, KE; Dempsey, CE; El Harchi, A; Hancox, JC; Melgari, D; Mitcheson, JS; Ng, GA; Zhang, C; Zhang, Y, 2015
)
2.09
"Ivabradine is an inhibitor of mixed Na+-K+ current that could combine with HCN channels to reduce the transmembrane velocity of funny current (If), heart rate, and cardiac efficiency, and thus be used for the treatment of cardiovascular diseases such as chronic heart failure. "( Effects of ivabradine on cardiac electrophysiology in dogs with age-related atrial fibrillation.
Hong, YF; Ji, YT; Jiang, T; Li, JX; Li, YD; Tang, BP; Xing, Q; Xiong, J; Yusufuaji, Y; Zhou, XH, 2015
)
2.25
"Ivabradine is an effective treatment for angina in patients with stable coronary artery disease (CAD) and for heart failure. "( Ivabradine reduces myocardial stunning in patients with exercise-inducible ischaemia.
Agricola, E; Camici, PG; Maranta, F; Margonato, A; Rimoldi, O; Tondi, L, 2015
)
3.3
"Ivabradine is a recent treatment option for heart failure."( Cardiac and Hemodynamic Benefits: Mode of Action of Ivabradine in Heart Failure.
Pereira-Barretto, AC, 2015
)
1.39
"Ivabradine is a novel If-channel antagonist that controls heart rate and may be helpful in treating patients with left ventricular dysfunction (LVD) who are unable to tolerate β-blockers or achieve a heart rate of 70 beats/min with standard therapy. "( Meta-analysis of Ivabradine in Patients With Stable Coronary Artery Disease With and Without Left Ventricular Dysfunction.
Cammarano, C; Comee, M; Donovan, JL; Malloy, MJ; Silva, M, 2016
)
2.22
"Ivabradine is a newly approved medication which reduces the heart rate by antagonizing the If channel. "( Acute on Chronic Ivabradine Overdose: a Case Report.
Maskell, K; Troendle, M; Tse, A; Wolf, CE, 2016
)
2.22
"Ivabradine is an oral medication that directly and selectively inhibits the hyperpolarization-activated cyclic-nucleotide gated funny (If) current in the sinoatrial node resulting in heart rate reduction."( Role of the Funny Current Inhibitor Ivabradine in Cardiac Pharmacotherapy: A Systematic Review.
Bishop, BM; Mauro, VF; Petite, SE,
)
1.13
"Ivabradine is a promising therapy in HFrEF based on the results of the SHIFT, but it is an adjunctive therapy, not a substitute for drugs with proven mortality benefits."( Role of Ivabradine in the Treatment of Patients With Cardiovascular Disease.
Nguyen, E; Weeda, ER; White, CM, 2016
)
1.59
"Ivabradine is a selective If channel blocker and acts by reducing firing rate of pacemaker cells in the sinoatrial node, without affecting the duration of action potential."( Ranolazine and Ivabradine: two different modalities to act against ischemic heart disease.
Cacciapuoti, F, 2016
)
1.51
"Ivabradine is a well-tolerated, safe and effective treatment option with the objective to improve prognosis, left ventricular structure and function, exercise tolerance and quality of life."( Ivabradine for the treatment of chronic heart failure.
De Denus, S; Elzir, L; Henri, C; O'Meara, E; Tardif, JC, 2016
)
2.6
"Ivabradine is a novel sinus node If 'funny current' inhibitor, which reduces the HR."( Inappropriate sinus tachycardia: focus on ivabradine.
Abed, HS; Fulcher, JR; Keech, AC; Kilborn, MJ, 2016
)
1.42
"Ivabradine is a heart rate-lowering agent approved to reduce the risk of hospitalization for worsening heart failure. "( Cost-Effectiveness of Ivabradine for Heart Failure in the United States.
Cowie, MR; Kansal, AR; Kielhorn, A; Krotneva, S; Tafazzoli, A; Yurgin, N; Zheng, Y, 2016
)
2.19
"Ivabradine is a safe and effective medication for HR reduction to reduce hospitalizations in patients with stable, symptomatic HF (ejection fraction < 35%), in sinus rhythm, and HR > 70 bpm."( Ivabradine, a novel medication for treatment of heart failure with reduced ejection fraction.
Bobadilla, RV; Foster, JL, 2016
)
3.32
"Ivabradine is a unique medication recently approved in the USA for the treatment of select heart failure patients. "( Ivabradine: A Review of Labeled and Off-Label Uses.
Bolorunduro, OB; Jha, SK; Oliphant, CS; Owens, RE, 2016
)
3.32
"Ivabradine is a blocker of the funny current channels in the sinoatrial node cells. "( Ivabradine.
Komajda, M, 2017
)
3.34
"Ivabradine is a heart rate reducing agent that exhibits anti-ischemic effects through the inhibition of funny electrical current in the sinus node resulting in heart rate reduction, thus enabling longer diastolic perfusion time, and reduced myocardial oxygen consumption without detrimental changes in arterial blood pressure, coronary vasomotion, and ventricular contractility. "( Ivabradine in acute coronary syndromes: Protection beyond heart rate lowering.
Borovac, JA; Camici, PG; Crea, F; Niccoli, G; Vetrugno, V, 2017
)
3.34
"Ivabradine is an inhibitor of mixed Na"( Effective suppression of atrial fibrillation by ivabradine: Novel target for an established drug?
Bögeholz, N; Dechering, DG; Eckardt, L; Ellermann, C; Fehr, M; Frommeyer, G; Kochhäuser, S; Pott, C; Sterneberg, M, 2017
)
2.15
"Ivabradine is a selective heart rate-lowering agent that acts by inhibiting the pacemaker current If in sinoatrial node cells. "( The BEAUTIFUL study: randomized trial of ivabradine in patients with stable coronary artery disease and left ventricular systolic dysfunction - baseline characteristics of the study population.
Ferrari, R; Ford, I; Fox, K; Steg, PG; Tendera, M, 2008
)
2.05
"Ivabradine is a heart rate-lowering agent devoid of other direct cardiovascular effects that has been approved for treatment of patients with stable angina pectoris. "( Characterization of the heart rate-lowering action of ivabradine, a selective I(f) current inhibitor.
Borer, JS; Le Heuzey, JY,
)
1.82
"Ivabradine is a new selective HR-lowering agent that selectively inhibits the pacemaker current I (f) in the sinus atrial node."( Ivabradine: beyond heart rate control.
D'Orazio, N; Riccioni, G; Vitulano, N, 2009
)
2.52
"Ivabradine is a novel pure heart rate-lowering agent that selectively and specifically inhibits pacemaker I(f) current. "( Effect of ivabradine, a novel antianginal agent, on driving performance: A randomized, double-blind, placebo-controlled trial in healthy volunteers.
Lévy, S; Macher, JP, 2009
)
2.2
"Ivabradine is a new efficient and safe therapeutic option in the treatment of coronary artery disease."( [Ivabradine, an I(f) current inhibitor--new treatment options in coronary heart disease].
Mach, F, 2009
)
1.98
"Ivabradine is an I(f) current inhibitor, that has documented antianginal efficacy. "( Impact of a pure reduction in heart rate for the treatment of left ventricular dysfunction: clinical benefits of ivabradine in the BEAUTIFUL trial.
Danchin, N,
)
1.78
"Ivabradine is a specific heart rate-lowering antianginal agent that was evaluated in a clinical development program involving approximately 3,000 patients with stable coronary artery disease, most with angina pectoris. "( Efficacy of ivabradine, a selective I(f) inhibitor, in patients with chronic stable angina pectoris and diabetes mellitus.
Borer, JS; Tardif, JC, 2010
)
2.18
"Ivabradine (IVA) is a novel, specific, heart rate (HR)-lowering agent that acts in sinoatrial node (SAN) cells by selectively inhibiting the pacemaker If current in a dose-dependent manner by slowing the diastolic depolarization slope of SAN cells, and reducing HR at rest and during exercise with minimal effect on myocardial contractility, blood pressure, and intracardiac conduction. "( Ivabradine: from molecular basis to clinical effectiveness.
Riccioni, G, 2010
)
3.25
"Ivabradine is a pure heart-rate-lowering agent with well-documented antianginal and anti-ischemic properties comparable to well-established anti-anginal agents."( Ivabradine: recent and potential applications in clinical practice.
Riccioni, G, 2011
)
2.53
"Ivabradine is a selective I(f) current inhibitor in the sinus node that decreases heart rate without negative inotropic effects. "( [Antianginal efficacy of ivabradine in a very old patient with aortic stenosis: effects on cardiac output and transvalvular aortic gradients].
Feola, M; Lombardo, E; Menditto, E; Nervo, E; Piccolo, S; Taglieri, C, 2010
)
2.11
"Ivabradine is a novel heart rate-lowering agent that selectively and specifically inhibits the depolarizing cardiac pacemaker If current in the sinus node. "( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
2.09
"Ivabradine is a novel negative chronotropic drug used for treatment of ischemic heart disease in people. "( Comparison of the effects of ivabradine and atenolol on heart rate and echocardiographic variables of left heart function in healthy cats.
Bonagura, JD; Cervenec, RM; Riesen, SC; Schober, KE,
)
1.87
"Ivabradine is a safe and effective drug in reducing resting heart rate, improving NYHA functional class without undesirable effects on conduction parameters or ectopic activity."( Ivabradine, a novel heart rate slower: is it a sword of double blades in patients with idiopathic dilated cardiomyopathy?
Alabd, A; Gamal, A; Rayan, M; Tawfik, M, 2011
)
3.25
"Ivabradine is a novel, heart rate-lowering drug which inhibits the pacemaker (I(f)) current in the heart with high selectivity and with minimal effect on haemodynamic parameters."( Selective pharmacological inhibition of the pacemaker channel isoforms (HCN1-4) as new possible therapeutical targets.
Baczkó, I; Cerbai, E; Gy Papp, J; Jaeger, K; Koncz, I; Romanelli, MN; Szél, T; Varró, A, 2011
)
1.09
"Ivabradine is a novel antianginal agent which inhibits the pacemaker current. "( Electrophysiological effects of ivabradine in dog and human cardiac preparations: potential antiarrhythmic actions.
Baczkó, I; Bitay, M; Cerbai, E; Fülöp, F; Jaeger, K; Jost, N; Koncz, I; Kristóf, A; Orvos, P; Papp, JG; Szél, T; Tálosi, L; Varró, A; Virág, L, 2011
)
2.1
"Ivabradine is a novel heart rate decreasing agent with selective and specific antagonist effects on the pacemaker current (I(f)). "( Effects of ivabradine on the pulmonary vein electrical activity and modulation of pacemaker currents and calcium homeostasis.
Chen, SA; Chen, YC; Chen, YJ; Cheng, CC; Kihara, Y; Lin, YK; Nakano, Y; Suenari, K, 2012
)
2.21
"Ivabradine is a selective HR-lowering agent that exclusively inhibits the I(f) current in sinoatrial node cells without having any effect on cardiac contractility or atrioventricular conduction."( Ivabradine versus metoprolol for heart rate reduction before coronary computed tomography angiography.
Dock, W; Mendel, H; Pichler, P; Pichler-Cetin, E; Sochor, H; Syeda, B; Vertesich, M, 2012
)
2.54
"Ivabradine is a new drug that reduces the firing rate of pacemaker cells in the sinoatrial node through a different mechanism with respect to betablockers."( The importance of reducing heart rate in cardiovascular diseases: effects of Ivabradine.
Bonadei, I; Bontempi, L; Curnis, A; D'Aloia, A; Dei Cas, L; Del Magro, F; Piovanelli, B; Vizzardi, E, 2011
)
1.32
"Ivabradine is a selective inhibitor of the hyperpolarisation activated cyclic-nucleotide-gated funny current (If) involved in pacemaker generation and responsiveness of the sino-atrial node (SAN), which result in HR reduction with no other apparent direct cardiovascular effects."( The biological effects of ivabradine in cardiovascular disease.
Franceschelli, S; Riccioni, G; Speranza, L, 2012
)
1.4
"Ivabradine is a novel heart rate lowering agent that inhibits I(f) ionic current in the sinus node and demonstrates antiischaemic and antianginal activity. "( Concomitant administration of different doses of simvastatin with ivabradine influence on PAI-1 and heart rate in normo- and hypercholesterolaemic rats.
Jasińska-Stroschein, M; Orszulak-Michalak, D; Owczarek, J, 2012
)
2.06
"Ivabradine is a new agent inhibiting sinus node I(f) current, resulting in a decrease of HR without haemodynamic compromise."( Metoprolol succinate vs. ivabradine in the treatment of inappropriate sinus tachycardia in patients unresponsive to previous pharmacological therapy.
Kaczmarek, K; Klingenheben, T; Ptaszynski, P; Ruta, J; Wranicz, JK, 2013
)
1.41
"Ivabradine is a selective inhibitor of the I(f) current, which primarily contributes to sinus node pacemaker activity, and has no significant direct cardiovascular effects such as reduction of blood pressure, cardiac contractility or impairment of cardiac conduction."( Safety and efficacy of oral ivabradine as a heart rate-reducing agent in patients undergoing CT coronary angiography.
Adile, KK; Garg, N; Goel, PK; Gupta, A; Jain, SK; Kapoor, A; Kumar, S; Tewari, S, 2012
)
1.39
"Ivabradine is a potentially attractive alternative to currently used drugs for reduction of heart rate in patients undergoing CTCA."( Safety and efficacy of oral ivabradine as a heart rate-reducing agent in patients undergoing CT coronary angiography.
Adile, KK; Garg, N; Goel, PK; Gupta, A; Jain, SK; Kapoor, A; Kumar, S; Tewari, S, 2012
)
2.12
"Ivabradine is a new selective antagonist of funny channels."( Ivabradine: potential clinical applications in critically ill patients.
De Santis, V; Magliocca, A; Nencini, C; Porto, AG; Santoro, A; Tritapepe, L; Vitale, D, 2013
)
2.55
"Ivabradine is a new heart rate (HR)-decreasing agent inhibiting sinus node If current."( Ivabradine in the treatment of inappropriate sinus tachycardia in patients after successful radiofrequency catheter ablation of atrioventricular node slow pathway.
Kaczmarek, K; Klingenheben, T; Ptaszynski, P; Ruta, J; Wranicz, JK, 2013
)
2.55
"Ivabradine is an effective treatment option to reduce HR and symptoms in patients with IST after RF ablation of atrioventricular node slow pathway. "( Ivabradine in the treatment of inappropriate sinus tachycardia in patients after successful radiofrequency catheter ablation of atrioventricular node slow pathway.
Kaczmarek, K; Klingenheben, T; Ptaszynski, P; Ruta, J; Wranicz, JK, 2013
)
3.28
"Ivabradine is a specific blocker of the pacemaker current (I(f)) used to decrease the sinus rate. "( Ivabradine for the prevention of inappropriate shocks due to sinus tachycardia in patients with an implanted cardioverter defibrillator.
Adler, A; Meir, I; Rosso, R; Viskin, S, 2013
)
3.28
"Ivabradine (IVA) is a novel specific HR-lowering agent that acts in sinus atrial node (SAN) cells by selectively inhibiting the pacemaker I(f) current in a dose-dependent manner by slowing the diastolic depolarization slope of SAN cells, and by reducing HR at rest during exercise in humans."( Ivabradine: an intelligent drug for the treatment of ischemic heart disease.
Riccioni, G, 2012
)
2.54
"Ivabradine (Procoralan®) is a pure heart rate-lowering drug that produces selective and specific inhibition of the cardiac pacemaker funny current (I(f)) in the sinus node that regulates heart rate. "( Ivabradine: in adults with chronic heart failure with reduced left ventricular ejection fraction.
Perry, CM, 2012
)
3.26
"Ivabradine is a specific heart rate-reducing agent approved as a treatment of chronic stable angina. "( Identification of the molecular site of ivabradine binding to HCN4 channels.
Barbuti, A; Baruscotti, M; Bolognesi, M; Bucchi, A; DiFrancesco, D; Micheloni, S; Nardini, M, 2013
)
2.1
"Ivabradine is a new antiarrhythmic agent with direct inhibition of the pacemaker (If) current. "( Potential new indication for ivabradine: treatment of a patient with congenital junctional ectopic tachycardia.
Al-Fayyadh, MI; Al-Ghamdi, S; Hamilton, RM, 2013
)
2.12
"Ivabradine is a new bradycardic agent with a potential indication for stable angina pectoris. "( Clinical trial simulation using therapeutic effect modeling: application to ivabradine efficacy in patients with angina pectoris.
Boissel, JP; Chabaud, S; Girard, P; Nony, P, 2002
)
1.99
"Ivabradine is a heart rate-lowering agent that selectively inhibits the pacemaker current, I(f), in the sinoatrial node. "( Electrophysiological effects of a single intravenous administration of ivabradine (S 16257) in adult patients with normal baseline electrophysiology.
Camm, AJ; Lau, CP, 2003
)
1.99
"Ivabradine (Procoralan) is a selective and specific I(f) inhibitor that acts on one of the most important ionic currents for the regulation of the pacemaker activity of sinoatrial node cells."( Heart rate slowing versus other pharmacological antianginal strategies.
Diaz, A; Tardif, JC, 2006
)
1.06
"Ivabradine is a novel heart-rate-lowering agent that acts specifically on the sinoatrial node by selectively inhibiting the I(f) current, which is the current predominantly responsible for the slow diastolic depolarization of pacemaker cells. "( Novel If current inhibitor ivabradine: safety considerations.
Camm, AJ; Savelieva, I, 2006
)
2.07
"Ivabradine is a new specific HR-reducing agent, which has been shown to have antianginal and anti-ischemic properties in patients with stable angina."( Rationale and design of a randomized, double-blind, placebo-controlled trial of ivabradine in patients with stable coronary artery disease and left ventricular systolic dysfunction: the morBidity-mortality EvAlUaTion of the I(f) inhibitor ivabradine in pa
Ferrari, R; Ford, I; Fox, K; Steg, PG; Tendera, M, 2006
)
1.28
"Ivabradine is a novel selective and specific I(f) inhibitor in the sinus node that reduces heart rate without any negative inotropic effect."( The heart rate-lowering agent ivabradine inhibits the pacemaker current I(f) in human atrial myocytes.
Bois, P; El Chemaly, A; Guinamard, R; Jayle, C; Magaud, C; Patri, S, 2007
)
1.35
"Ivabradine is a selective inhibitor of the If currents of the sinoatrial node cells."( Ivabradine: a selective If current inhibitor in the treatment of stable angina.
Andrikopoulos, G; Dasopoulou, C; Kappos, K; Koulouris, S; Kranidis, A; Manolis, AS; Sakellariou, D; Tzeis, S, 2006
)
2.5
"Ivabradine is a specific heart rate-lowering agent that acts via I(f) pacemaker channels in the sinoatrial node with no beta-adrenoreceptor activity."( Absence of respiratory effects with ivabradine in patients with asthma.
Babu, KS; Gadzik, F; Holgate, ST, 2008
)
1.34
"Ivabradine (S-16257) is a new bradycardic agent with a direct effect on the sinus node. "( Pharmacokinetic-pharmacodynamic modeling of the effects of ivabradine, a direct sinus node inhibitor, on heart rate in healthy volunteers.
Funck-Brentano, C; Jaillon, P; Jochemsen, R; Laveille, C; Ragueneau, I; Resplandy, G, 1998
)
1.99
"Ivabradine is a novel bradycardic agent that has been developed for the prevention of angina. "( Development of a sequential linked pharmacokinetic and pharmacodynamic simulation model for ivabradine in healthy volunteers.
Aarons, L; Duffull, SB, 2000
)
1.97
"Ivabradine is a novel bradycardic agent that has been developed for the prevention of angina. "( A pharmacokinetic simulation model for ivabradine in healthy volunteers.
Aarons, L; Chabaud, S; Duffull, SB; Girard, P; Laveille, C; Nony, P, 2000
)
2.02
"Ivabradine is an open-channel blocker; however, block is exerted preferentially when channels deactivate on depolarization, and is relieved by long hyperpolarizing steps."( Current-dependent block of rabbit sino-atrial node I(f) channels by ivabradine.
Baruscotti, M; Bucchi, A; DiFrancesco, D, 2002
)
1.27

Effects

Ivabradine also has a beneficial effect on hospital admissions. A quarter of HF patients can expect to be readmitted to hospital for HF within 1 month of discharge.

Ivabradine has proven therapeutic efficacy for cardiac ischaemia and, until proved otherwise, is a very specific inhibitor of the cardiac sinoatrial node I(f) current. The drug has been shown to improve heart failure with sinus tachycardia by reducing the heart rate.

ExcerptReferenceRelevance
"Ivabradine also has a beneficial effect on hospital admissions (-26 %, p < 0.0001), which is clinically relevant since a quarter of HF patients can expect to be readmitted to hospital for HF within 1 month of discharge."( Addressing Major Unmet Needs in Patients with Systolic Heart Failure: The Role of Ivabradine.
Pereira-Barretto, AC, 2016
)
1.38
"Ivabradine has an active metabolite S-18982."( Development of a sequential linked pharmacokinetic and pharmacodynamic simulation model for ivabradine in healthy volunteers.
Aarons, L; Duffull, SB, 2000
)
1.25
"Ivabradine has an active metabolite S-18982."( A pharmacokinetic simulation model for ivabradine in healthy volunteers.
Aarons, L; Chabaud, S; Duffull, SB; Girard, P; Laveille, C; Nony, P, 2000
)
1.3
"Ivabradine has potent actions in reducing heart rate and improving clinical outcomes of chronic heart failure with reduced ejection fraction (HFrEF). "( Sustained-Release Ivabradine Hemisulfate in Patients With Systolic Heart Failure.
Cui, D; Li, J; Liu, G; Liu, K; Lou, D; Lu, S; Ma, S; Pang, X; Wang, J; Wang, X; Wu, S; Xie, X; Xue, L; Yang, Z; Ye, F; Yu, H; Zhang, Y; Zhong, M, 2022
)
2.5
"Ivabradine has been shown to improve heart failure with sinus tachycardia by reducing the heart rate without affecting left ventricular systolic function or blood pressure. "( Discontinuation of Intravenous Catecholamine by Oral Ivabradine in a Patient with Decompensated Heart Failure with Low Cardiac Output Syndrome.
Bekki, M; Chibana, H; Fukumoto, Y; Honda, A; Itaya, N; Nohara, S; Sato, H; Shibao, K; Shibata, R; Takahashi, J, 2023
)
2.6
"Ivabradine has potential in the treatment of ventricular arrhythmias in heart failure patients with reduced ejection fraction patients."( Effect of ivabradine on ventricular arrhythmias in heart failure patients with reduced ejection fraction.
Çetin, T; Çınar, T; Çinier, G; Eren, S; Hayıroğlu, Mİ; Keskin, K; Pay, L; Tekkeşin, Aİ; Tezen, O; Yumurtaş, AÇ, 2023
)
2.03
"Ivabradine has been approved in heart failure with reduced ejection fraction (HFrEF) and elevated heart rate despite guideline-directed medical therapy (GDMT) to reduce cardiovascular (CV) death and hospitalization for worsening HF. "( Beneficial effects of ivabradine in patients with heart failure, low ejection fraction, and heart rate above 77 b.p.m.
Bernier, V; Bohm, M; Borer, JS; Bouabdallaoui, N; Ford, I; Komajda, M; O'Meara, E; Swedberg, K; Tardif, JC; Tavazzi, L, 2019
)
2.27
"Oral ivabradine has the potential to be used as an adjunct to amiodarone in the treatment of JET in infants after surgery for congenital heart disease."( Ivabradine as an Adjunct for Refractory Junctional Ectopic Tachycardia Following Pediatric Cardiac Surgery: A Preliminary Study.
Joshi, S; Kumar, G; Kumar, V; Ramamurthy, R; Sharma, V; Tiwari, N, 2019
)
2.47
"Ivabradine has been reported to be efficacious in an adult with paroxysmal atrial fibrillation as well as in children with junctional or ectopic atrial tachycardias."( Ivabradine as a stabilising anti-arrhythmic agent for multifocal atrial tachycardia.
Cohen, JA; Cohen, MI; Collazo, L; Shope, C; Stollar, L, 2020
)
2.72
"Ivabradine has no negative effect on inotropic contractility, conductivity, and systemic vascular resistance."( [Heart rate control in patients with sepsis and septic cardiomyopathy: the role of Ivabradine].
Fang, H; Shen, Z; Wang, L; Zhang, Y; Zhou, Z, 2020
)
1.5
"Ivabradine has been approved for the treatment of chronic heart failure and chronic stable angina pectoris in Europe. "( Ivabradine use in pregnant women-treatment indications and pregnancy outcome: an evaluation of the German Embryotox database.
Beck, E; Dathe, K; Hoeltzenbein, M; Lehmann, ML; Schaefer, C, 2021
)
3.51
"Ivabradine has been used in patients who have chronic heart failure (HF) with reduced ejection fraction (HFrEF) and concomitant sinus heart rate ≥70 bpm. "( The association between ivabradine and adverse cardiovascular events in acute decompensated HFrEF patients.
Chang, HY; Chiou, WR; Chung, FP; Hsu, CY; Huang, JL; Lee, YH; Liang, HW; Liao, CT; Lin, PL; Lin, WY, 2021
)
2.37
"Ivabradine has shown promising efficacy, but has not been evaluated in children."( Ivabradine in Children With Dilated Cardiomyopathy and Symptomatic Chronic Heart Failure.
Berger, F; Bonnet, D; Daubeney, PEF; Jokinen, E; Kantor, PF, 2017
)
2.62
"Ivabradine has recently been demonstrated to have antiarrhythmic properties in atrial fibrillation. "( Ivabradine Aggravates the Proarrhythmic Risk in Experimental Models of Long QT Syndrome.
Dechering, DG; Eckardt, L; Ellermann, C; Frommeyer, G; Kochhäuser, S; Lange, PS; Leitz, P; Weller, J, 2019
)
3.4
"Ivabradine has been successfully used in some patients."( Long-term outcomes of ivabradine in inappropriate sinus tachycardia patients: appropriate efficacy or inappropriate patients.
Benezet-Mazuecos, J; Farré, J; Macía, E; Quiñones, MÁ; Rubio, JM; Sanchez-Borque, P, 2013
)
1.43
"Ivabradine has demonstrated efficacy in reducing rehospitalizations and mortality in heart failure and in improving exercise tolerance and reducing angina attacks in patients with coronary artery disease, whereas selective heart rate reduction may also prove to be beneficial in therapeutic areas outside those in which ivabradine has already demonstrated clinical efficacy."( Resting heart rate: risk indicator and emerging risk factor in cardiovascular disease.
Böhm, M; Borer, JS; Deedwania, P; Kim, JB; Reil, JC, 2015
)
1.14
"Ivabradine that has been introduced in medical practice in last decade is a pure heart rate-slowing agent."( [The efficacy of ivabradine in chronic heart failure (review)].
Gvishiani, M; Isakadze, A; Makharadze, T, 2015
)
1.48
"Ivabradine has opened up new possibilities for treating stable angina and chronic heart failure by lowering heart rate. "( Effect of Ivabradine on Endothelial Function in Patients with Stable Angina Pectoris: Assessment with the Endo-PAT 2000 Device.
Chmelarova, A; Fedacko, J; Jackova, L; Janicko, M; Jedlickova, L; Majernik, J; Merkovska, L; Novakova, B; Pella, D, 2015
)
2.26
"Ivabradine, a new agent has been added to the current medical options for managing heart failure."( Ivabradine: Heart Failure and Beyond.
Chaudhary, R; Freudenberger, R; Garg, J; Krishnamoorthy, P; Lanier, G; Martinez, MW; Shah, N, 2016
)
2.6
"Ivabradine also has a beneficial effect on hospital admissions (-26 %, p < 0.0001), which is clinically relevant since a quarter of HF patients can expect to be readmitted to hospital for HF within 1 month of discharge."( Addressing Major Unmet Needs in Patients with Systolic Heart Failure: The Role of Ivabradine.
Pereira-Barretto, AC, 2016
)
1.38
"Ivabradine has been extensively evaluated for coronary artery disease wherein (2) large trials was shown to have no mortality benefit."( Role of the Funny Current Inhibitor Ivabradine in Cardiac Pharmacotherapy: A Systematic Review.
Bishop, BM; Mauro, VF; Petite, SE,
)
1.13
"Ivabradine has been shown to improve symptoms and to reduce rehospitalization and mortality in patients with severe chronic heart failure (HF). "( Clinical Experience with Ivabradine in Acute Heart Failure.
Alonso Salinas, GL; Camino López, A; Del Castillo Carnevalli, H; Jiménez Mena, M; Pascual Izco, M; Sanmartín Fernández, M; Zamorano Gómez, JL,
)
1.88
"Ivabradine has been approved as a heart rate-lowering agent for use in the treatment of chronic stable angina pectoris in case of contraindication or intolerance to beta-blockers. "( Ivabradine: pharmacodynamic aspects of its clinical use.
Stieber, J, 2008
)
3.23
"Ivabradine has been shown to have antianginal and anti-ischaemic properties in patients with stable angina pectoris."( Effect of ivabradine, a novel antianginal agent, on driving performance: A randomized, double-blind, placebo-controlled trial in healthy volunteers.
Lévy, S; Macher, JP, 2009
)
1.48
"Ivabradine has been shown to be effective in reducing sinus rate. "( Reversal of tachycardiomyopathy due to left atrial tachycardia by ivabradine.
Bohora, S; Lokhandwala, Y; Parekh, P; Vasavda, A, 2011
)
2.05
"Ivabradine has recently been recognized as a pure heart-rate-reducing agent and is being extensively studied."( Rate control with ivabradine: angina pectoris and beyond.
Bhargava, B; Parakh, N, 2011
)
1.42
"Ivabradine has anti-ischemic and antianginal efficacy equivalent to that of β-blockers and calcium channel antagonists in the treatment of chronic stable angina pectoris."( Ivabradine: recent and potential applications in clinical practice.
Riccioni, G, 2011
)
2.53
"Ivabradine has anti-ischemic and antianginal efficacy in monotherapy, as well as in combination with other antianginals, such as beta-blockers, and is safe and well tolerated."( Innovation in coronary artery disease and heart failure: clinical benefits of pure heart rate reduction with ivabradine.
Canet, E; Lerebours, G; Vilaine, JP, 2011
)
1.3
"Ivabradine has not been reported to improve cardiac involvement in Becker muscular dystrophy (BMD)."( Beneficial effect of ivabradine in dilated cardiomyopathy from Becker muscular dystrophy.
Berger, E; Finsterer, J; Stöllberger, C, 2012
)
1.42
"Ivabradine (Iva) has shown beneficial structural and functional effects in clinical and experimental heart failure (HF), but its action in combination with mechanical unloading (MU), such as during treatment with left ventricular assist devices (LVAD), is unknown. "( Influence of ivabradine on reverse remodelling during mechanical unloading.
Dias, P; Gandhi, A; Ibrahim, M; Navaratnarajah, M; Sarathchandra, P; Shah, A; Siedlecka, U; Terracciano, CM; van Doorn, C; Yacoub, MH, 2013
)
2.2
"Ivabradine has shown anti-ischaemic and anti-anginal activity in a placebo-controlled trial."( Efficacy of ivabradine, a new selective I(f) inhibitor, compared with atenolol in patients with chronic stable angina.
Bourassa, MG; Ford, I; Fox, K; Tardif, JC; Tendera, M, 2005
)
1.43
"Ivabradine has no negative inotropic or lusitropic effects, preserving ventricular contractility, and does not change any major electrophysiological parameters unrelated to heart rate."( Ivabradine -- the first selective sinus node I(f) channel inhibitor in the treatment of stable angina.
Sulfi, S; Timmis, AD, 2006
)
2.5
"Ivabradine has been shown to reduce heart rate, preserve myocardial contractility, increase diastolic filling and maintain both small and large coronary artery vasodilation, whatever the level of exercise, thus ensuring adequate endocardial blood perfusion during exercise."( Heart rate reduction by pharmacological If current inhibition.
Cargnoni, A; Ceconi, C; Ferrari, R; Stavroula, G, 2006
)
1.06
"Ivabradine has demonstrated dosedependent anti-ischemic and antianginal effects in a placebo-controlled study."( Heart rate slowing versus other pharmacological antianginal strategies.
Diaz, A; Tardif, JC, 2006
)
1.06
"Ivabradine has little effect on the atrioventricular node and ventricular refractoriness, but because of its effect on the sinus node, it should be avoided in patients with sick sinus syndrome."( Novel If current inhibitor ivabradine: safety considerations.
Camm, AJ; Savelieva, I, 2006
)
1.35
"Ivabradine has been recently approved for the treatment of stable angina."( Absence of respiratory effects with ivabradine in patients with asthma.
Babu, KS; Gadzik, F; Holgate, ST, 2008
)
1.34
"Ivabradine has proven therapeutic efficacy for cardiac ischaemia and, until proved otherwise, is a very specific inhibitor of the cardiac sinoatrial node I(f) current. "( Defying the economists: a decrease in heart rate improves not only cardiac but also endothelial function.
Triggle, CR, 2008
)
1.79
"Ivabradine has an active metabolite S-18982."( Development of a sequential linked pharmacokinetic and pharmacodynamic simulation model for ivabradine in healthy volunteers.
Aarons, L; Duffull, SB, 2000
)
1.25
"Ivabradine has an active metabolite S-18982."( A pharmacokinetic simulation model for ivabradine in healthy volunteers.
Aarons, L; Chabaud, S; Duffull, SB; Girard, P; Laveille, C; Nony, P, 2000
)
1.3

Actions

Ivabradine did not increase the prevalence of bradycardia in patients with LBBB. The drug increased quality of life on the Kansas City Cardiomyopathy Questionnaire (KCCQ) but the effect size was small and possibly without relevance to patients.

ExcerptReferenceRelevance
"Ivabradine seemed to increase quality of life on the Kansas City Cardiomyopathy Questionnaire (KCCQ) (mean difference (MD)=2.92; 95% CI 1.34 to 4.50; p=0.0003; low certainty of evidence), but the effect size was small and possibly without relevance to patients, and on the Minnesota Living With Heart Failure Questionnaire (MLWHFQ) (MD=-5.28; 95% CI -6.60 to -3.96; p<0.00001; very low certainty of evidence), but the effects were uncertain."( Ivabradine added to usual care in patients with heart failure: a systematic review with meta-analysis and trial sequential analysis.
Gluud, C; Jakobsen, JC; Liang, N; Maagaard, M; Nielsen, EE; Sethi, NJ; Yang, SH, 2022
)
2.89
"Ivabradine seems to increase the risk of atrial fibrillation, bradycardia and non-serious adverse events.PROSPERO registration number: CRD42018112082."( Ivabradine added to usual care in patients with heart failure: a systematic review with meta-analysis and trial sequential analysis.
Gluud, C; Jakobsen, JC; Liang, N; Maagaard, M; Nielsen, EE; Sethi, NJ; Yang, SH, 2022
)
2.89
"Ivabradine seemed to increase the risk of serious adverse events after removal of outliers (RR 1.07; 95% CI 1.03 to 1.11) as well as the following adverse events classified as serious: bradycardia, prolonged QT interval, photopsia, atrial fibrillation and hypertension."( Effects of adding ivabradine to usual care in patients with angina pectoris: a systematic review of randomised clinical trials with meta-analysis and Trial Sequential Analysis.
Gluud, C; Jakobsen, JC; Maagaard, M; Nielsen, EE; Ning, L; Sethi, NJ; Yang, SH, 2020
)
1.61
"Ivabradine did not increase the prevalence of bradycardia in patients with LBBB."( Impact of left bundle branch block on heart rate and its relationship to treatment with ivabradine in chronic heart failure.
Böhm, M; Borer, J; Ford, I; Komajda, M; Reil, JC; Robertson, M; Swedberg, K; Tavazzi, L, 2013
)
1.33
"The ivabradine-induced increase in A-H interval was inversely correlated with VR (r = -0.85, P = .03, at 130 bpm; r = -0.95, P = .003, at 180 bpm)."( If inhibition in the atrioventricular node by ivabradine causes rate-dependent slowing of conduction and reduces ventricular rate during atrial fibrillation.
Batatinha, JA; Belardinelli, L; Bonatti, R; Liu, G; Nearing, BD; Rajamani, S; Silva, AF; Verrier, RL; Zeng, D, 2014
)
1.14
"Ivabradine did not increase serious adverse drug reactions (OR, 0.99 [95% CI, 0.88-1.13]; P = 0.93) or cardiac disorders (OR, 1.03 [95% CI, 0.87-1.22]; P = 0.74)."( Meta-analysis of Ivabradine in Patients With Stable Coronary Artery Disease With and Without Left Ventricular Dysfunction.
Cammarano, C; Comee, M; Donovan, JL; Malloy, MJ; Silva, M, 2016
)
1.5
"Ivabradine induced an increase of aAPD (+9ms) and aERP (+30ms, p<0.05) leading to a marked increase of atrial post-repolarization refractoriness (aPRR), defined as the difference of aERP and aAPD (+21ms, p<0.05)."( Effective suppression of atrial fibrillation by ivabradine: Novel target for an established drug?
Bögeholz, N; Dechering, DG; Eckardt, L; Ellermann, C; Fehr, M; Frommeyer, G; Kochhäuser, S; Pott, C; Sterneberg, M, 2017
)
1.43

Treatment

Ivabradine treatment was associated with an increased risk of HF hospitalization in symptomatic HFrEF patients with a history of paroxysmal AF. The drug resulted in significant reduction in resting heart rate, average 24hECG heart rate and improvement in exercise capacity.

ExcerptReferenceRelevance
"Ivabradine treatment was associated with an increased risk of HF hospitalization in symptomatic HFrEF patients with a history of paroxysmal AF. "( Ivabradine in heart failure patients with reduced ejection fraction and history of paroxysmal atrial fibrillation.
Chang, JJ; Chen, MC; Jan, JY; Lin, MS; Lin, YS; Wang, PC; Yang, TY, 2022
)
3.61
"Ivabradine treatment resulted in significant reduction in resting heart rate, average 24hECG heart rate, improvement in exercise capacity and reduction of symptoms in both subgroups."( Baseline intrinsic heart rate and response to ivabradine treatment in patients with inappropriate sinus tachycardia.
Cygankiewicz, I; Kaczmarek, K; Klingenheben, T; Poddebska, I; Ptaszyński, P; Urbanek, I; Wranicz, JK, 2020
)
1.54
"Ivabradine treatment had a more significant benefit on improving haemodynamic stability, whereas sacubitril/valsartan treatment showed a more significant effect on improving LVEF."( Combination of ivabradine and sacubitril/valsartan in patients with heart failure and reduced ejection fraction.
Chang, HY; Chiou, WR; Chung, FP; Hsu, CY; Huang, JL; Lee, YH; Liang, HW; Liao, CT; Lin, PL; Lin, WY, 2021
)
1.7
"Ivabradine treatment improved left ventricular ejection fraction, and clinical status and QOL showed favorable trends."( Ivabradine in Children With Dilated Cardiomyopathy and Symptomatic Chronic Heart Failure.
Berger, F; Bonnet, D; Daubeney, PEF; Jokinen, E; Kantor, PF, 2017
)
2.62
"Ivabradine treatment resulted in occurrence of EAD and polymorphic VT in 9 of 12 sotalol-treated hearts (212 episodes), and 8 of 12 veratridine-treated hearts (155 episodes)."( Ivabradine Aggravates the Proarrhythmic Risk in Experimental Models of Long QT Syndrome.
Dechering, DG; Eckardt, L; Ellermann, C; Frommeyer, G; Kochhäuser, S; Lange, PS; Leitz, P; Weller, J, 2019
)
2.68
"Ivabradine treatment produced dose-dependent reductions in heart rate at rest and at peak exercise (91.9 ± 6.3 to 71.7 ± 4.8 and 114.4 ± 7.6 to 96.8 ± 4.8; P = 0.001 and P = 0.001, respectively). "( Effects of ivabradine on 6-minute walk test and quality of life in patients with previously implanted CRT-D.
Akpek, M; Ates, I; Cetinkaya, R; Doğru, M; Genç, A; Kaya, MG; Keser, A; Sarıkaya, M; Ulucan, Ş; Yavuz, AH, 2013
)
2.22
"Ivabradine treatment prevents dobutamine-induced increase in HR and may be useful in reducing HR-related adverse effects of dobutamine."( Ivabradine treatment prevents dobutamine-induced increase in heart rate in patients with acute decompensated heart failure.
Cavusoglu, Y; Mert, U; Morrad, B; Mutlu, F; Nadir, A; Ulus, T, 2015
)
3.3
"Ivabradine treatment was associated with a relative risk of AF of 1.15 (95% CI 1.07 to 1.24, p=0.0027) among 21 571 patients in the meta-analysis."( Atrial fibrillation associated with ivabradine treatment: meta-analysis of randomised controlled trials.
Bourke, JP; Keavney, BD; Koref, MS; Martin, RI; Pogoryelova, O; Teare, MD, 2014
)
1.4
"Ivabradine treatment was initiated according to the latest HF guidelines."( Ivabradine improves heart rate variability in patients with nonischemic dilated cardiomyopathy.
Balta, S; Cuglan, B; Gozubuyuk, G; Kaplan, O; Karakus, Y; Kurtoglu, E; Yasar, E, 2014
)
2.57
"Ivabradine-treated patients had a lower HR, and improved left ventricular dimensions and systolic function, versus placebo-treated ones (p < 0.05 for all)."( I(f) current inhibitor ivabradine in patients with idiopathic dilated cardiomyopathy: Impact on the exercise tolerance and quality of life.
Abdel-Barr, MG; Abdel-Salam, Z; Hussain, M; Nammas, W; Rayan, M; Saleh, A, 2015
)
1.45
"Ivabradine treatment led to a significant improvement in cardiac function."( I(f) current channel inhibitor (ivabradine) deserves cardioprotective effect via down-regulating the expression of matrix metalloproteinase (MMP)-2 and attenuating apoptosis in diabetic mice.
Chen, SL; Hu, ZY; Li, B; Li, MH; Zuo, GF, 2014
)
1.41
"Ivabradine is a recent treatment option for heart failure."( Cardiac and Hemodynamic Benefits: Mode of Action of Ivabradine in Heart Failure.
Pereira-Barretto, AC, 2015
)
1.39
"Ivabradine-treated patients are also at significantly lower risk of experiencing a second or third hospitalization for worsening HF."( Addressing Major Unmet Needs in Patients with Systolic Heart Failure: The Role of Ivabradine.
Pereira-Barretto, AC, 2016
)
1.38
"Ivabradine treatment on top of metoprolol decreases angina symptoms and improves QoL in patients with stable angina and coronary artery disease (CAD)."( Antianginal Efficacy of Ivabradine/Metoprolol Combination in Patients With Stable Angina.
Kallistratos, M; Katsivas, A; Zarifis, J, 2016
)
1.46
"Ivabradine treatment was not associated with adverse effects on glucose metabolism."( Efficacy of ivabradine, a selective I(f) inhibitor, in patients with chronic stable angina pectoris and diabetes mellitus.
Borer, JS; Tardif, JC, 2010
)
1.46
"Ivabradine treatment significantly improves hyperaemic coronary flow velocity and CFR in patients with stable CAD. "( Ivabradine improves coronary flow reserve in patients with stable coronary artery disease.
Chlouverakis, G; Hamilos, MI; Skalidis, EI; Vardas, PE; Zacharis, EA, 2011
)
3.25
"Ivabradine (0.6 mg/kg) treatment reduced the MDA levels and elevated the SOD and CAT enzyme activity."( Dose-dependent protective effect of ivabradine against ischemia-reperfusion-induced renal injury in rats.
Acet, A; Beytur, A; Binbay, M; Gunaydin, MO; Parlakpinar, H; Polat, A; Sarihan, ME, 2012
)
1.38
"Ivabradine treatment was discontinued in three patients due to adverse events within the first week."( Lasting reduction of heart transplant tachycardia with ivabradine is effective and well tolerated: results of 48-month study.
Bara, C; Bobylev, D; Haverich, A; Stiefel, P; Zhang, R, 2012
)
1.35
"Ivabradine-treated patients evidenced lower risk for a second or third additional HF hospitalization [hazard ratio (HR): 0.66, 95% CI, 0.55-0.79, P < 0.001 and HR: 0.71, 95% CI, 0.54-0.93, P = 0.012, respectively]."( Effect of ivabradine on recurrent hospitalization for worsening heart failure in patients with chronic systolic heart failure: the SHIFT Study.
Alings, M; Böhm, M; Borer, JS; Ford, I; Komajda, M; Lopez-de-Sa, E; Sendon, JL; Swedberg, K; Tavazzi, L, 2012
)
1.5
"Treatment with ivabradine for 6 months effectively reduced HR and improved functional class and QoL in Chinese patients with chronic HF. "( Real-World Effectiveness of Ivabradine in Chinese Patients with Chronic Heart Failure: Interim Analysis of the POSITIVE Study.
Baopeng, T; Caizhen, Q; Huiyuan, H; Jingmin, Z; Junbo, G; Wenhui, D; Yamei, X; Yuhui, Z, 2022
)
1.37
"Treatment with ivabradine should not be deferred in patients in sinus rhythm with a HR of ≥70 bpm to reduce the primary outcome and HF hospitalizations, in particular in patients with HR ≥75 bpm. "( Time to benefit of heart rate reduction with ivabradine in patients with heart failure and reduced ejection fraction.
Abdin, A; Batailler, C; Böhm, M; Borer, J; Ford, I; Komajda, M; Mahfoud, F; Slawik, J; Swedberg, K; Tavazzi, L, 2023
)
1.52
"Treatment with ivabradine became a new therapeutic alternative for patients with inappropriate sinus tachycardia (IST). "( Baseline intrinsic heart rate and response to ivabradine treatment in patients with inappropriate sinus tachycardia.
Cygankiewicz, I; Kaczmarek, K; Klingenheben, T; Poddebska, I; Ptaszyński, P; Urbanek, I; Wranicz, JK, 2020
)
1.17
"Treatment with ivabradine in patients within 2 years after HTX significantly reduced post-transplant heart rate and LV mass and was associated with a superior survival in comparison with patients receiving metoprolol succinate."( Control of cardiac chronotropic function in patients after heart transplantation: effects of ivabradine and metoprolol succinate on resting heart rate in the denervated heart.
Bruckner, T; Darche, FF; Doesch, AO; Ehlermann, P; Helmschrott, M; Katus, HA; Rahm, AK; Rivinius, R; Ruhparwar, A; Thomas, D, 2018
)
1.05
"Pre-treatment with ivabradine (10 μM) significantly attenuated the contractile response to CCh (1 μM; mean peak amplitude from 1493 ±216 mg to 680 ±95 mg; p < 0.003; n = 7)."( Ivabradine inhibits carbachol-induced contractions of isolated rat urinary bladder.
Ayar, A; Aydin, HR; Eren, H; Kalkan, ÖF; Kurt, A; Sahan, R; Turgut, H, 2018
)
2.24
"Treatment with ivabradine in experimental models of LQT2 and LQT3 increases proarrhythmia."( Ivabradine Aggravates the Proarrhythmic Risk in Experimental Models of Long QT Syndrome.
Dechering, DG; Eckardt, L; Ellermann, C; Frommeyer, G; Kochhäuser, S; Lange, PS; Leitz, P; Weller, J, 2019
)
2.3
"Treatment with ivabradine significantly lowered the HR (174 ± 20 vs. "( Effect of ivabradine, a funny current inhibitor, on portal hypertensive rats.
Chang, CC; Chuang, CL; Hsin, IF; Hsu, SJ; Huang, HC; Lee, FY; Lee, SD; Lee, WS, 2019
)
1.27
"Treatment with ivabradine was associated with a 13% relative risk reduction for the composite of cardiovascular mortality or HF hospitalization (P < 0.001 vs."( Effect of ivabradine in patients with left-ventricular systolic dysfunction: a pooled analysis of individual patient data from the BEAUTIFUL and SHIFT trials.
Böhm, M; Borer, JS; Ferrari, R; Ford, I; Fox, K; Komajda, M; Robertson, M; Steg, PG; Swedberg, K; Tavazzi, L; Tendera, M, 2013
)
1.13
"Treatment with ivabradine in severe HF was associated with relative risk reductions indistinguishable from those of less severe disease for the primary end point (16% reduction), all-cause death (22%), cardiovascular death (22%), HF death (37%), and HF hospitalization (17%; all p values for interaction: NS)."( Efficacy and safety of ivabradine in patients with severe chronic systolic heart failure (from the SHIFT study).
Böhm, M; Borer, JS; Ford, I; Komajda, M; Robertson, M; Swedberg, K; Tavazzi, L, 2014
)
1.05
"Treatment with ivabradine was associated with a significant reduction in resting heart rate after 3 weeks versus no change with placebo (-15.8±7.7 versus +0.3±5.8 bpm; P=0.0010)."( Impact of Ivabradine on Central Aortic Blood Pressure and Myocardial Perfusion in Patients With Stable Coronary Artery Disease.
Allée, G; Dillinger, JG; Henry, P; Levy, BI; Logeart, D; Maher, V; Manzo Silberman, S; Vitale, C, 2015
)
1.16
"Treatment with ivabradine did not affect the primary outcome of change in physical limitation score at 12 months. "( Quality of Life With Ivabradine in Patients With Angina Pectoris: The Study Assessing the Morbidity-Mortality Benefits of the If Inhibitor Ivabradine in Patients With Coronary Artery Disease Quality of Life Substudy.
Chassany, O; Ferrari, R; Ford, I; Fox, K; Steg, PG; Tardif, JC; Tendera, M, 2016
)
1.11
"Pre-treatment with ivabradine reduced infarct size from 35 +/- 4 (SEM) to 19 +/- 4% of area at risk (AAR)."( Improvement of regional myocardial blood flow and function and reduction of infarct size with ivabradine: protection beyond heart rate reduction.
Gres, P; Heusch, G; Schilawa, D; Schulz, R; Skyschally, A; van Caster, P, 2008
)
0.88
"Treatment with ivabradine, a pure HR-reducing agent, provides an opportunity to assess the effects of selectively lowering HR without altering other aspects of cardiac function."( Heart rate as a treatable cardiovascular risk factor.
Tardif, JC, 2009
)
0.69
"Treatment with ivabradine significantly reduced heart rate (p<0.01), with no effect on blood pressure. "( Heart rate reduction with ivabradine improves erectile dysfunction in parallel to decrease in atherosclerotic plaque load in ApoE-knockout mice.
Baumhäkel, M; Böhm, M; Custodis, F; Laufs, U; Schlimmer, N, 2010
)
1.01
"Treatment with ivabradine (5 mg twice a day) resulted in disappearance of syncopal episodes both during upright position and CSM."( Successful use of ivabradine in a case of exaggerated autonomic dysfunction.
Aliyev, F; Celiker, C; Türkoğlu, C; Uzunhasan, I, 2010
)
1.03
"Treatment with ivabradine was associated with a decrease in the primary end-point LVESVI (change from baseline to last value, -1.48 ± 13.00 mL/m(2)) versus an increase with placebo (1.85 ± 10.54 mL/m(2)) (P=0.018)."( Effect of heart rate reduction by ivabradine on left ventricular remodeling in the echocardiographic substudy of BEAUTIFUL.
Ceconi, C; Ferrari, R; Ford, I; Fox, K; Freedman, SB; Gueret, P; Hildebrandt, P; McDonagh, T; Parrinello, G; Robertson, M; Steg, PG; Tardif, JC; Tendera, M, 2011
)
0.99
"Treatment with ivabradine was associated with a decrease in 24-hour heart rate of 6.3 ± 9.5 beats/min at last assessment versus no change with placebo (0.4 ± 7.2 beats/min, p <0.001, between-group difference), with a greater decrease in waking heart rate with ivabradine than during sleep (6.8 ± 10.4 vs 5.2 ± 8.9 beats/min, respectively, at last visit)."( Safety of ivabradine in patients with coronary artery disease and left ventricular systolic dysfunction (from the BEAUTIFUL Holter Substudy).
Ferrari, R; Ford, I; Fox, K; Robertson, M; Steg, PG; Talajic, M; Tardif, JC; Tendera, M, 2011
)
1.11
"Treatment with ivabradine reduced LVESVI (primary substudy endpoint) vs."( Effects of selective heart rate reduction with ivabradine on left ventricular remodelling and function: results from the SHIFT echocardiography substudy.
Böhm, M; Borer, JS; Ford, I; Komajda, M; O'Meara, E; Swedberg, K; Tardif, JC; Tavazzi, L, 2011
)
0.97
"Treatment with ivabradine resulted in a significant reduction of HR, rate-pressure product, and LV contractile function and a significant increase in LV end-diastolic pressure, LV end-diastolic wall stress, and LV relaxation time constant (tau) in cats with HCM. "( Effects of ivabradine on heart rate and left ventricular function in healthy cats and cats with hypertrophic cardiomyopathy.
Bonagura, JD; Li, X; Otoni, CC; Riesen, SC; Schober, KE; Smith, DN, 2012
)
1.12
"Treatment with ivabradine irreversibly depressed basal firing frequency and markedly attenuated the enhancement effect of EtOH on firing."( Ethanol enhances human hyperpolarization-activated cyclic nucleotide-gated currents.
Chen, H; Chen, Y; Fan, X; Huang, C; Song, T; Wu, P; Yang, J, 2012
)
0.72
"Treatment with ivabradine, on a background of guidelines-based HF therapy, is associated with a substantial reduction in the likelihood of recurrent hospitalizations for worsening HF. "( Effect of ivabradine on recurrent hospitalization for worsening heart failure in patients with chronic systolic heart failure: the SHIFT Study.
Alings, M; Böhm, M; Borer, JS; Ford, I; Komajda, M; Lopez-de-Sa, E; Sendon, JL; Swedberg, K; Tavazzi, L, 2012
)
1.13
"Treatment with ivabradine significantly reduced HR and LVESD, improved SRcirc, S long and SRlong in the T4 group, and the average I Ca,L density at 0 mV in T4-Iva groups (9.9 ± 1.6 pA/pF) was restored to the control level."( Heart rate reduction with ivabradine prevents thyroid hormone-induced cardiac remodeling in rat.
Cho, KI; Han, J; Kim, BH; Kim, IJ; Kim, JY; Kim, N; Kim, SM, 2013
)
1.03
"When treated with ivabradine, these parameters of HRV such as square root of the mean of the squared differences between adjacent NN intervals (RMSSD) and HFnu were in the upward tendency, but low frequency normalized unit and low frequency/high frequency were in the opposite tendency."( Identification and detection of the isolated sinus venosus from the Asian toad.
Deng, X; Guan, C; Hao, L; Li, G; Li, S; Sun, G; Wang, Y; Zhang, B, 2013
)
0.71

Toxicity

Ivabradine combined with β-blockers can reduce the resting heart rate and improve heart function in patients with AMI while not increasing adverse events. Irrespective of diabetic status, ivabradin is effective and safe in these patients.

ExcerptReferenceRelevance
" The most frequent adverse events were visual symptoms and sinus bradycardia with ivabradine (0."( Antianginal efficacy and safety of ivabradine compared with amlodipine in patients with stable effort angina pectoris: a 3-month randomised, double-blind, multicentre, noninferiority trial.
Ford, I; Fox, KM; Ruzyllo, W; Tendera, M, 2007
)
0.84
" Safety was assessed on the basis of reported adverse events at 1, 3, 6, 9 and 12 months."( Long-term safety and efficacy of ivabradine in patients with chronic stable angina.
Filipova, S; López-Bescós, L; Martos, R, 2007
)
0.62
" Phosphene-like mild transient visual symptoms were the most frequently reported adverse events but led to treatment withdrawal in only 4 patients."( Long-term safety and efficacy of ivabradine in patients with chronic stable angina.
Filipova, S; López-Bescós, L; Martos, R, 2007
)
0.62
" The most common adverse events were visual symptoms in 16."( I f inhibition with ivabradine : electrophysiological effects and safety.
Camm, AJ; Savelieva, I, 2008
)
0.67
" A prospective follow-up study was conducted to identify possible adverse effects, tolerance, and drug effects on heart rate and control of symptoms."( Safety and effectiveness of ivabradine after cardiac transplantation.
Ballesteros-Pradas, S; Campos-Pareja, A; Fernández-Quero, M; Guisado-Rasco, A; Lage-Gallé, E; Machuca, MG; Martínez-Martínez, A; Nevado-Portero, J; Romero-Rodríguez, N; Sobrino-Márquez, M, 2010
)
0.65
"3) years, no substantial adverse effects were observed."( Safety and effectiveness of ivabradine after cardiac transplantation.
Ballesteros-Pradas, S; Campos-Pareja, A; Fernández-Quero, M; Guisado-Rasco, A; Lage-Gallé, E; Machuca, MG; Martínez-Martínez, A; Nevado-Portero, J; Romero-Rodríguez, N; Sobrino-Márquez, M, 2010
)
0.65
"Ivabradine is safe and effective in increasing the rate of patients at target HR and in reducing the need for additional IV beta-blockade in patients referred for CTCA."( Incremental value and safety of oral ivabradine for heart rate reduction in computed tomography coronary angiography.
Brunetti, ND; Cademartiri, F; Di Biase, L; Di Biase, M; Guaricci, AI; Ieva, R; Macarini, L; Maffei, E; Midiri, M; Montrone, D; Schuijf, JD; Tedeschi, C, 2012
)
2.09
" However, these agents can have undesirable adverse effects (AEs) and due to the risk of bronchoconstriction are contraindicated in patients with obstructive airway disease."( Heart rate-lowering efficacy and respiratory safety of ivabradine in patients with obstructive airway disease: a randomized, double-blind, placebo-controlled, crossover study.
Ciebiada, M; Gorski, P; Majewski, S; Slomka, S; Zielinska-Wyderkiewicz, E, 2012
)
0.63
" The effects of ivabradine on cardiovascular outcomes, changes in heart rate, and adverse events, particularly bradycardia, were evaluated according to age group."( Efficacy and safety of ivabradine in chronic heart failure across the age spectrum: insights from the SHIFT study.
Böhm, M; Borer, JS; Ford, I; Komajda, M; Lainscak, M; Swedberg, K; Tavazzi, L, 2013
)
1.05
" Adverse events were more common in COPD patients, but similar in treatment subgroups."( Clinical profiles and outcomes in patients with chronic heart failure and chronic obstructive pulmonary disease: an efficacy and safety analysis of SHIFT study.
Böhm, M; Borer, JS; Ford, I; Komajda, M; Lainscak, M; Robertson, M; Swedberg, K; Tavazzi, L, 2013
)
0.39
" Ivabradine is similarly effective and safe in chronic HF patients with or without COPD, and can be safely combined with beta-blockers in COPD."( Clinical profiles and outcomes in patients with chronic heart failure and chronic obstructive pulmonary disease: an efficacy and safety analysis of SHIFT study.
Böhm, M; Borer, JS; Ford, I; Komajda, M; Lainscak, M; Robertson, M; Swedberg, K; Tavazzi, L, 2013
)
1.3
" Tolerability was assessed throughout the study by physical and ophthalmologic examinations, vital signs measurement, laboratory analyses, and monitoring of adverse effects."( Pharmacokinetic and safety profile of ivabradine in healthy Chinese men: a phase I, randomized, open-label, increasing single- and multiple-dose study.
Huang, Y; Jiang, J; Li, Y; Tian, L; Xu, L, 2013
)
0.66
" There were small, nonsignificant differences in the number of adverse events between the two groups (66 in Iva and 73 in Aten, p > 0."( The efficacy and safety of ivabradine hydrochloride versus atenolol in Chinese patients with chronic stable angina pectoris.
Jia, Y; Jiang, J; Jiang, R; Jing, L; Li, T; Li, X; Li, Y; Liu, S; Lu, Q; Shou, X; Wang, L; Wang, X; Wang, Z; Wei, J; Xia, H; Xie, P; Xing, B; Yang, Z, 2014
)
0.7
" Adverse events were significantly more frequent in patients with diabetes (78%) than without (74%) (P < 0."( Efficacy and safety of ivabradine in patients with chronic systolic heart failure and diabetes: an analysis from the SHIFT trial.
Böhm, M; Borer, JS; Ford, I; Francq, BG; Komajda, M; Swedberg, K; Tavazzi, L, 2015
)
0.73
" Irrespective of diabetic status, ivabradine is effective and safe in these patients."( Efficacy and safety of ivabradine in patients with chronic systolic heart failure and diabetes: an analysis from the SHIFT trial.
Böhm, M; Borer, JS; Ford, I; Francq, BG; Komajda, M; Swedberg, K; Tavazzi, L, 2015
)
1.01
"Cardiovascular adverse effects in drug development are a major source of compound attrition."( An Integrative Approach for Improved Assessment of Cardiovascular Safety Data.
Gabrielsson, J; Jirstrand, M; Martel, E; Pairet, N; Scheuerer, S; Wallman, M, 2021
)
0.62
" The difference in adverse events was not statistically significant [odds ratio (OR) =2."( Effectiveness and safety of ivabradine in the treatment of acute myocardial infarction: a systematic review and meta-analysis.
Chen, J; Chen, Q; Chen, S; Wang, B; Wang, Q; Yang, S; Zhang, X, 2021
)
0.92
"Ivabradine combined with β-blockers can reduce the resting heart rate and improve heart function in patients with AMI while not increasing adverse events."( Effectiveness and safety of ivabradine in the treatment of acute myocardial infarction: a systematic review and meta-analysis.
Chen, J; Chen, Q; Chen, S; Wang, B; Wang, Q; Yang, S; Zhang, X, 2021
)
2.36

Pharmacokinetics

The paper considers the structural identifiability of a parent-metabolite pharmacokinetic model for ivabradine and one of its metabolites. Pharmacokinetic parameters were calculated using non-compartmental analysis and compared to determine if the differences were statistically significant.

ExcerptReferenceRelevance
" The pharmacodynamic data (heart rate) were pooled from two studies and included a total of 78 healthy subjects."( Development of a sequential linked pharmacokinetic and pharmacodynamic simulation model for ivabradine in healthy volunteers.
Aarons, L; Duffull, SB, 2000
)
0.53
" The aim of this study is to develop a pharmacokinetic simulation model."( A pharmacokinetic simulation model for ivabradine in healthy volunteers.
Aarons, L; Chabaud, S; Duffull, SB; Girard, P; Laveille, C; Nony, P, 2000
)
0.58
"The paper considers the structural identifiability of a parent-metabolite pharmacokinetic model for ivabradine and one of its metabolites."( An identifiability analysis of a parent-metabolite pharmacokinetic model for ivabradine.
Aarons, L; Chapman, MJ; Chappell, MJ; Duffull, SB; Evans, ND; Godfrey, KR, 2001
)
0.76
"To design a parsimonious population pharmacodynamic experiment that has the same or greater efficiency than that provided by two phase I studies."( Optimal design of a population pharmacodynamic experiment for ivabradine.
Aarons, L; Duffull, SB; Mentré, F, 2001
)
0.55
"A population pharmacodynamic trial design is presented that is more parsimonious than the original study and would be appropriate for inclusion in a premarketing clinical study."( Optimal design of a population pharmacodynamic experiment for ivabradine.
Aarons, L; Duffull, SB; Mentré, F, 2001
)
0.55
" An open-label, 2-period, nonrandomized, phase-I, pharmacokinetic interaction design was used."( Effects of Hypericum perforatum on ivabradine pharmacokinetics in healthy volunteers: an open-label, pharmacokinetic interaction clinical trial.
Calvo, A; Martínez, I; Portolés, A; Resplandy, G; Terleira, A, 2006
)
0.61
" An open-label, randomized, crossover, phase I, pharmacokinetic interaction design was used."( Lack of pharmacokinetic interaction between omeprazole or lansoprazole and ivabradine in healthy volunteers: an open-label, randomized, crossover, pharmacokinetic interaction clinical trial.
Calvo, A; Gorostiaga, C; Laredo, L; Moreno, A; Portolés, A; Resplandy, G; Terleira, A, 2006
)
0.56
" In experimental studies, it has been shown that ivabradine does have some unfavorable pharmacodynamic properties, such as the block of all four hyperpolarization-activated cyclic nucleotide-gated channels and block of other ion channels at high concentrations."( Ivabradine: pharmacodynamic aspects of its clinical use.
Stieber, J, 2008
)
2.04
" Our objective was to evaluate a possible pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers."( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.87
" Pharmacokinetic parameters of ivabradine administered in each treatment period were calculated using non-compartmental and compartmental analysis to determine if there were statistically significant differences."( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.93
" These differences were statistically significant for C(max) and AUC(0-∞) when ivabradine was administered with carbamazepine, whereas they were not for t(max), half-life and mean residence time."( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.87
"To determine the pharmacodynamic effects of oral ivabradine in cats."( Pharmacodynamic effects of ivabradine, a negative chronotropic agent, in healthy cats.
Bonagura, JD; Buffington, TC; Cober, RE; Li, X; Riesen, SC; Schober, KE, 2011
)
0.92
"The study objective was evaluation of the pharmacokinetic interaction between ivabradine and phenytoin in healthy subjects."( Pharmacokinetic interaction between ivabradine and phenytoin in healthy subjects.
Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2012
)
0.88
" Pharmacokinetic parameters of ivabradine administered in each treatment were calculated using non-compartmental analysis and compared to determine if the differences were statistically significant."( Pharmacokinetic interaction between ivabradine and phenytoin in healthy subjects.
Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2012
)
0.94
" Statistically significant differences were observed for the C(max) and AUC(∞) of ivabradine when administered alone or with phenytoin, whereas for t(max) and the half-life the differences were non-significant."( Pharmacokinetic interaction between ivabradine and phenytoin in healthy subjects.
Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2012
)
0.88
"The purpose of this study was to explore pharmacokinetic (PK) and pharmacodynamic (PD) characteristics and tolerability in healthy male Korean volunteers, as well as to compare them with PK/PD profiles of white subjects."( Evaluation of pharmacokinetic and pharmacodynamic profiles and tolerability after single (2.5, 5, or 10 mg) and repeated (2.5, 5, or 10 mg bid for 4.5 days) oral administration of ivabradine in healthy male Korean volunteers.
Ah Jung, J; Bae, KS; Cho, SH; Choe, S; Choi, HY; Ghim, JL; Kim, UJ; Lim, HS; Noh, YH, 2013
)
0.58
"5, 5, and 10 mg, respective mean Cmax levels of ivabradine were 9, 15, and 39 ng/mL, and mean AUC0-last values were 30, 52, and 121 ng h/mL."( Evaluation of pharmacokinetic and pharmacodynamic profiles and tolerability after single (2.5, 5, or 10 mg) and repeated (2.5, 5, or 10 mg bid for 4.5 days) oral administration of ivabradine in healthy male Korean volunteers.
Ah Jung, J; Bae, KS; Cho, SH; Choe, S; Choi, HY; Ghim, JL; Kim, UJ; Lim, HS; Noh, YH, 2013
)
0.84
" Finally, the method was successfully used in a pharmacokinetic study that measured ivabradine levels in healthy volunteers after a single 5 mg oral dose of ivabradine."( Development and validation of a sensitive LC-MS/MS-ESI method for the determination of ivabradine in human plasma: application to a pharmacokinetic study.
Huang, Y; Jiang, J; Li, Y; Tian, L, 2013
)
0.84
" After the single dose, plasma ivabradine Cmax and AUC increased approximately linearly with dosage, no statistically significant differences were found in t½ or Tmax between the dose groups."( Pharmacokinetic and safety profile of ivabradine in healthy Chinese men: a phase I, randomized, open-label, increasing single- and multiple-dose study.
Huang, Y; Jiang, J; Li, Y; Tian, L; Xu, L, 2013
)
0.95
" The serum concentrations of IVA and N-demethyl ivabradine were determined by ultra-performance liquid chromatography-mass spectrometry and pharmacokinetic parameters were calculated using DASver3."( The effect of clopidogrel on pharmacokinetics of ivabradine and its metabolite in rats.
Chen, H; Hu, GX; Huang, CK; Lian, QQ; Shang-Guan, WN; Sun, W; Wang, Z; Wang, ZS; Zhang, XD; Zhu, GH, 2015
)
0.93
" A significant number of cardiovascular drugs compete for transport by OCT1 or OCT2, introducing the potential to alter the pharmacokinetic profile of other concomitantly administered medications."( Organic Cation Transporter-Mediated Clearance of Cardiovascular Drugs: A Pharmacological Perspective.
Arora, RR; Hassan, OT; Hassan, RT,
)
0.13

Compound-Compound Interactions

Ivabradine combined with carvedilol improves LVDD, achieves THR more often and reduces risk of encephalopathy, acute kidney injury.

ExcerptReferenceRelevance
"Ivabradine effectively reduces heart rate and angina pectoris in combination with beta-blockers and is well tolerated by patients in every day practice."( Ivabradine in combination with beta-blocker therapy for the treatment of stable angina pectoris in every day clinical practice.
Ebelt, H; Kaehler, J; Koester, R; Meinertz, T; Soeffker, G; Werdan, K, 2010
)
3.25
"The antianginal and anti-ischemic efficacy of the selective I (f) inhibitor ivabradine is established in patients with stable angina in monotherapy and in combination with other antianginals, including beta-blocker."( Efficacy of ivabradine in combination with Beta-blocker versus uptitration of Beta-blocker in patients with stable angina.
Amosova, E; Andrejev, E; Ceconi, C; Ferrari, R; Rudenko, U; Zaderey, I, 2011
)
0.96
"Several clinical trials have demonstrated the antianginal and anti-ischemic efficacy of ivabradine in combination with beta-blocker in patients with stable angina pectoris."( Ivabradine in combination with beta-blocker improves symptoms and quality of life in patients with stable angina pectoris: results from the ADDITIONS study.
Ebelt, H; Hack, G; Höpfner, F; Müller-Werdan, U; Nuding, S; Werdan, K, 2012
)
2.04
" We induced biological pacing using the Ca(2+)-stimulated adenylyl cyclase AC1 gene expressed alone or in combination with HCN2 and compared outcomes with those with single-gene HCN2 transfer."( Ca(2+)-stimulated adenylyl cyclase AC1 generates efficient biological pacing as single gene therapy and in combination with HCN2.
Bobkov, Y; Boink, GJ; Cohen, IS; Danilo, P; Duan, L; Kryukova, Y; Nearing, BD; Robinson, RB; Rosen, MR; Shlapakova, IN; Tan, HL; Verrier, RL, 2012
)
0.38
"To investigate the effects of ivabradine in combination with perindopril on cerebral blood flow and endothelial functional activity."( [Cerebral blood flow and endothelial functional activity in patients with coronary heart disease and arterial hypertension during therapy with ivabradine in combination with perindopril].
Gapon, LI; Kolesnikova, SN; Musikhina, NA; Petelina, TI; Utesheva, AB, 2012
)
0.87
" Group 1 (n = 38) patients took ivabradine in combination with perindopril and Group 2 (n = 26) received metoprolol."( [Cerebral blood flow and endothelial functional activity in patients with coronary heart disease and arterial hypertension during therapy with ivabradine in combination with perindopril].
Gapon, LI; Kolesnikova, SN; Musikhina, NA; Petelina, TI; Utesheva, AB, 2012
)
0.86
"By unidirectionally affecting the vasomotor function of the endothelium, ivabradine in combination with perindopril versus metoprolol has a more favorable effect on circulatory resistance and blood flow velocity in the brachiocephalic arteries of patients with CHD and AH."( [Cerebral blood flow and endothelial functional activity in patients with coronary heart disease and arterial hypertension during therapy with ivabradine in combination with perindopril].
Gapon, LI; Kolesnikova, SN; Musikhina, NA; Petelina, TI; Utesheva, AB, 2012
)
0.81
"Clinical trials have proven the anti-anginal and anti-ischemic efficacy of the pacemaker current inhibitor ivabradine in combination with beta-blockers in patients with stable angina pectoris (AP)."( Ivabradine in combination with beta-blocker reduces symptoms and improves quality of life in elderly patients with stable angina pectoris: age-related results from the ADDITIONS study.
Ebelt, H; Höpfner, F; Müller-Werdan, U; Nuding, S; Stöckl, G; Werdan, K, 2014
)
2.06
" We describe a post hoc analysis in the ADDITIONS database to investigate effectiveness and tolerability of ivabradine in combination with beta-blocker in patients with angina who have had a percutaneous coronary intervention (PCI)."( Ivabradine in combination with Beta-blockers in patients with chronic stable angina after percutaneous coronary intervention.
Ebelt, H; Höpfner, F; Müller-Werdan, U; Nuding, S; Stöckl, G; Werdan, K, 2015
)
2.07
"ADDITIONS (prActical Daily efficacy anD safety of Procoralan® In combinaTION with betablockerS) was a multicenter, 4-month, noninterventional, prospective, open-label trial that involved stable-angina patients."( Ivabradine in Combination with Metoprolol Improves Symptoms and Quality of Life in Patients with Stable Angina Pectoris: A post hoc Analysis from the ADDITIONS Trial.
Ebelt, H; Höpfner, F; Müller-Werdan, U; Nuding, S; Stöckl, G; Werdan, K, 2016
)
1.88
"Ivabradine combined with metoprolol safely and effectively reduces heart rate, angina attacks and nitrate use, and improves QoL in stable-angina patients."( Ivabradine in Combination with Metoprolol Improves Symptoms and Quality of Life in Patients with Stable Angina Pectoris: A post hoc Analysis from the ADDITIONS Trial.
Ebelt, H; Höpfner, F; Müller-Werdan, U; Nuding, S; Stöckl, G; Werdan, K, 2016
)
3.32
"To assess therapy diltiazem-retard and ivabradine on structurally functional changes of a cardiac muscle and HR at patients with AH in combination with BA."( [Assessment of Efficiency of Medicamentous Therapy in Correction of Structurally Functional Changes of The Cardiac Muscle at Patients With Arterial Hypertension in Combination With Bronchial Asthma].
Odegova, AA; Tarlovskaya, EI, 2016
)
0.7
"Ivabradine combined with carvedilol improves LVDD, achieves THR more often and reduces risk of encephalopathy, acute kidney injury with improved survival in patients with cirrhosis."( Carvedilol Combined With Ivabradine Improves Left Ventricular Diastolic Dysfunction, Clinical Progression, and Survival in Cirrhosis.
Goyal, R; Khumuckham, JS; Kumar, G; Premkumar, M; Rangegowda, D; Sarin, SK; Shasthry, SM; Thomas, SS; Vyas, T, 2020
)
2.3
"To evaluate the myocardial protection of Ivabradine (IBD) combined with Trimetazidine (TMZ) in patients with coronary artery disease (CAD) after percutaneous coronary intervention (PCI), magnetic resonance imaging (MRI) images under convolutional neural network (CNN) algorithm were used."( Protection of Ivabradine Combined with Trimetazidine on Myocardial Injury after Percutaneous Coronary Intervention in Patients with Coronary Artery Disease Evaluated by Magnetic Resonance Image under Convolutional Neural Network.
Chen, C, 2021
)
1.25
" For patients with CAD, IBD combined with TMZ after PCI can effectively play the role of anti-inflammatory and antioxidative damage and improve intradermal function."( Protection of Ivabradine Combined with Trimetazidine on Myocardial Injury after Percutaneous Coronary Intervention in Patients with Coronary Artery Disease Evaluated by Magnetic Resonance Image under Convolutional Neural Network.
Chen, C, 2021
)
0.98
"Ivabradine may be valuable for tailoring early antianginal treatment when used in combination with beta-blockers for chronic stable angina inadequately controlled by beta-blockers."( Efficacy and Safety of Ivabradine in Combination with Beta-Blockers in Patients with Stable Angina Pectoris: A Systematic Review and Meta-analysis.
Karpov, Y; Nedoshivin, A; Petrova, PTS, 2022
)
2.47

Bioavailability

Phenytoin has an important effect on the pharmacokinetics of ivabradine in healthy subjects. Carbamazepine lowers its bioavailability by about 80%.

ExcerptReferenceRelevance
"T Carbamazepine interacts with ivabradine in healthy volunteers, and lowers its bioavailability by about 80%."( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.93
"This study showed that phenytoin has an important effect on the pharmacokinetics of ivabradine in healthy subjects, reducing its bioavailability by approximately 70%."( Pharmacokinetic interaction between ivabradine and phenytoin in healthy subjects.
Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2012
)
0.88
" A study was conducted in order to assess the relative bioavailability (Frel) of the paediatric formulation and a similar Frel was observed between the paediatric formulation and the adult marketed tablet."( Model-based approaches for ivabradine development in paediatric population, part I: study preparation assessment.
Bouzom, F; Brendel, K; Chenel, M; Fouliard, S; Gesson, C; Peigné, S, 2016
)
0.73
"The current research focused on improvement of oral bioavailability and decrease in dosing frequency of ivabradine (Iva) in order to enhance patient compliance by formulating novel sustained release Iva loaded solid lipid microparticles (SLMs) with the help of melt emulsification technique."( IVABRADINE LOADED SOLID LIPID MICROPARTICLES: FORMULATION, CHARACTERIZATION AND OPTIMIZATION BY CENTRAL COMPOSITE ROTATABLE DESIGN.
Afzal, S; Hanif, M; Khan, HU; Sher, M, 2017
)
2.11
" The developed nanoplatforms hence can be further used to formulate other drugs that suffer from low bioavailability due to extensive first-pass metabolism."( Simultaneous Optimization of Oral and Transdermal Nanovesicles for Bioavailability Enhancement of Ivabradine Hydrochloride.
Elsayed, I; Naguib, MJ; Teaima, MH, 2021
)
0.84

Dosage Studied

The results of this study indicate that repeated oral doses of ivabradine produced plasma drug concentrations suitable for 12-h dosing intervals in healthy cats. The limit to start a substitution is significantly higher than in patients without heart failure. A small proportion of patients with HF and SHIFT-like characteristics may potentially benefit from the addition of Ivab radine.

ExcerptRelevanceReference
" There were eight active dosing levels and placebo, and a no-dose run in the period before each study."( Development of a sequential linked pharmacokinetic and pharmacodynamic simulation model for ivabradine in healthy volunteers.
Aarons, L; Duffull, SB, 2000
)
0.53
" The multiple dose regimens were administered every 12 h and there were seven active dosing levels."( A pharmacokinetic simulation model for ivabradine in healthy volunteers.
Aarons, L; Chabaud, S; Duffull, SB; Girard, P; Laveille, C; Nony, P, 2000
)
0.58
" Therefore, our goal was to establish the dose-response curve of the effects of ivabradine (If channel inhibitor) on MVO2 and diastolic time."( Effect of graded heart rate reduction with ivabradine on myocardial oxygen consumption and diastolic time in exercising dogs.
Berdeaux, A; Colin, P; Ghaleh, B; Hittinger, L; Monnet, X, 2004
)
0.81
" However, broad use and appropriate dosing of commonly used rate-slowing drugs is limited by their poor tolerability."( Ivabradine: a selective If current inhibitor in the treatment of stable angina.
Andrikopoulos, G; Dasopoulou, C; Kappos, K; Koulouris, S; Kranidis, A; Manolis, AS; Sakellariou, D; Tzeis, S, 2006
)
1.78
" and atenolol at the commonly used dosage in clinical practice in patients with chronic stable angina pectoris produced additional efficacy with no untoward effect on safety or tolerability."( Efficacy of the I(f) current inhibitor ivabradine in patients with chronic stable angina receiving beta-blocker therapy: a 4-month, randomized, placebo-controlled trial.
Kahan, T; Ponikowski, P; Tardif, JC, 2009
)
0.62
"1-10microM) to establish a dose-response relationship."( Specific inhibition of HCN channels slows rhythm differently in atria, ventricle and outflow tract and stabilizes conduction in the anoxic-reoxygenated embryonic heart model.
Gardier, S; Pedretti, S; Raddatz, E; Sarre, A, 2010
)
0.36
" No statistically significant changes in immunosuppressive drug dosage or blood levels were observed, except from a lower mycophenolate mofetil dose at follow-up (P=0."( Heart rate reduction for 12 months with ivabradine reduces left ventricular mass in cardiac allograft recipients.
Ammon, K; Buss, S; Celik, S; Dengler, TJ; Doesch, AO; Frankenstein, L; Hardt, S; Katus, HA; Konstandin, M; Kristen, A; Sack, FU, 2009
)
0.62
" Attempts should be made to achieve HR <70 bpm by cardiac rehabilitation and routine use of appropriately dosed beta-blockers."( Role of heart rate in cardiovascular diseases: how the results of the BEAUTIFUL study change clinical practice.
Bruguera Cortada, J; Varela, A, 2009
)
0.35
" It was possible to reach the maximum drug dosage in all patients, achieving a reduction in basal heart rate of 33 (6."( Safety and effectiveness of ivabradine after cardiac transplantation.
Ballesteros-Pradas, S; Campos-Pareja, A; Fernández-Quero, M; Guisado-Rasco, A; Lage-Gallé, E; Machuca, MG; Martínez-Martínez, A; Nevado-Portero, J; Romero-Rodríguez, N; Sobrino-Márquez, M, 2010
)
0.65
" The results of this study indicate that repeated oral doses of ivabradine produced plasma drug concentrations suitable for 12-h dosing intervals in healthy cats."( Pharmacokinetics of oral ivabradine in healthy cats.
Carnes, CA; Lindsey, KJ; Ni, W; Phelps, MA; Riesen, SC; Schober, KE, 2011
)
0.91
" Cardiac dysfunction in C57BL/6J mice was induced by implantation of osmotic pumps for continuous subcutaneous dosing of angiotensin II (1."( Role of heart rate reduction in the prevention of experimental heart failure: comparison between If-channel blockade and β-receptor blockade.
Becher, PM; Lindner, D; Miteva, K; Savvatis, K; Schmack, B; Schultheiss, HP; Tschöpe, C; Van Linthout, S; Westermann, D; Zietsch, C, 2012
)
0.38
" For each of the 3 dosing groups, 9 subjects were randomized to receive ivabradine and 3 to receive placebo."( Evaluation of pharmacokinetic and pharmacodynamic profiles and tolerability after single (2.5, 5, or 10 mg) and repeated (2.5, 5, or 10 mg bid for 4.5 days) oral administration of ivabradine in healthy male Korean volunteers.
Ah Jung, J; Bae, KS; Cho, SH; Choe, S; Choi, HY; Ghim, JL; Kim, UJ; Lim, HS; Noh, YH, 2013
)
0.81
"5-mg ivabradine orally twice a day, and drug dosage was titrated to decrease the patients' average heart rate to 70 beats per minute."( Effects of ivabradine on 6-minute walk test and quality of life in patients with previously implanted CRT-D.
Akpek, M; Ates, I; Cetinkaya, R; Doğru, M; Genç, A; Kaya, MG; Keser, A; Sarıkaya, M; Ulucan, Ş; Yavuz, AH, 2013
)
1.29
"02), no statistically significant changes in immunosuppressive drug dosage or blood levels were detected."( Heart rate reduction for 36 months with ivabradine reduces left ventricular mass in cardiac allograft recipients: a long-term follow-up study.
Dengler, T; Doesch, AO; Ehlermann, P; Erbel, C; Frankenstein, L; Gleissner, CA; Hardt, S; Katus, HA; Mueller, S; Ruhparwar, A, 2013
)
0.66
"14 male patients (age 61 ± 3 years, LVEF 62 ± 1 %) with arterial hypertension and coronary artery disease (CAD) under chronic β-blocker therapy at moderate dosage and additional renin-angiotensin system-blocking therapy were included."( Ivabradine therapy to unmask heart rate-independent effects of β-blockers on pulse wave reflections.
Fichtlscherer, S; Fischer-Rasokat, U; Hamm, C; Honold, J; Leick, J; Liebetrau, C; Lochmann, D; Möllmann, H; Spyridopoulos, I, 2014
)
1.85
" The dosage of carvedilol had no detectable effect and there were no unexpected safety issues."( Effect of Combining Ivabradine and β-Blockers: Focus on the Use of Carvedilol in the SHIFT Population.
Bocchi, EA; Böhm, M; Borer, JS; Ford, I; Komajda, M; Swedberg, K; Tavazzi, L, 2015
)
0.74
" This model might be useful for predicting the plasma and urine PK of ivabradine, potentially helping to identify the optimal dosing regimens in various clinical situations."( Population plasma and urine pharmacokinetics of ivabradine and its active metabolite S18982 in healthy Korean volunteers.
Bae, KS; Cho, SH; Choe, S; Choi, HY; Ghim, JL; Jung, JA; Lim, HS, 2016
)
0.92
"This international survey shows that adherence to guideline-recommended medications is relatively satisfactory but the dosage of recommended CHF medications is usually suboptimal."( Physicians' adherence to guideline-recommended medications in heart failure with reduced ejection fraction: data from the QUALIFY global survey.
Anker, SD; Cowie, MR; Filippatos, GS; Komajda, M; Mengelle, B; Ponikowski, P; Tavazzi, L, 2016
)
0.43
" A small proportion of patients with HF and SHIFT-like characteristics may potentially benefit from the addition of Ivabradine, just approved in Canada; this number will be further reduced if target dosage for β-blockers is achieved."( Is There a Role for Ivabradine in the Contemporary Management of Patients with Chronic Heart Failure in Academic and Community Heart Failure Clinics in Canada?
Azeem, S; Fernando, C; Moe, GW; Roth, S, 2017
)
0.99
"The authors explored the dose-response relationship of ivabradine in children with dilated cardiomyopathy and symptomatic chronic HF."( Ivabradine in Children With Dilated Cardiomyopathy and Symptomatic Chronic Heart Failure.
Berger, F; Bonnet, D; Daubeney, PEF; Jokinen, E; Kantor, PF, 2017
)
2.15
"The current research focused on improvement of oral bioavailability and decrease in dosing frequency of ivabradine (Iva) in order to enhance patient compliance by formulating novel sustained release Iva loaded solid lipid microparticles (SLMs) with the help of melt emulsification technique."( IVABRADINE LOADED SOLID LIPID MICROPARTICLES: FORMULATION, CHARACTERIZATION AND OPTIMIZATION BY CENTRAL COMPOSITE ROTATABLE DESIGN.
Afzal, S; Hanif, M; Khan, HU; Sher, M, 2017
)
2.11
" Furthermore, achieving an optimal iron status (the limit to start a substitution is significantly higher than in patients without heart failure), decreasing the heart frequency with Ivabradine (if heart rate persists above 70 / min despite fully dosed betablocker) and «lifestyle changes» can add to the success of the medical treatment."( [Pharmacological therapy of heart failure with reduced ejection fraction].
Bösch, C; Dobner, S; Hunziker, L; Martinelli, M; Rhyner, D; Schnegg, B; Suter, T; Wieser, M; Wigger, O, 2018
)
0.67
" Ivabradine dosed at daytime (the rat's resting phase) reverted a night-to-day HR rise to HR dip by 14."( Ivabradine reversed nondipping heart rate in rats with l-NAME-induced hypertension.
Baka, T; Simko, F, 2019
)
2.87
" An analysis of drug exposure-time and high-resolution response-time data of HR and mean arterial blood pressure was performed after acute oral dosing of ivabradine, sildenafil, dofetilide, and pimobendan in Han-Wistar rats."( An Integrative Approach for Improved Assessment of Cardiovascular Safety Data.
Gabrielsson, J; Jirstrand, M; Martel, E; Pairet, N; Scheuerer, S; Wallman, M, 2021
)
0.82
" This report also lists the summaries of potential clinically significant interaction, likely to require additional monitoring, alteration of drug dosage or timing of administration, between ivabradine and antiretroviral drugs."( Efficacy of ivabradine in HIV-associated dilated cardiomyopathy.
Greco, S; Guadagnino, G; Mastroianni, A; Urso, F; Vangeli, V, 2021
)
1.19
"A simple and sensitive spectrofluorimetric method has been developed for the estimation of Ivabradine HCl in bulk and the tablet dosage form."( Fluorescence spectroscopy method for estimation of Ivabradine in bulk and the tablet dosage form.
Naik, K; Tailor, PM, 2022
)
1.19
"A novel, facile, rapid, and precise synchronous spectrofluorimetric method was evolved for the simultaneous estimation of bisoprolol fumarate and ivabradine in dosage forms and biological fluids."( First derivative synchronous spectrofluorimetric analysis of bisoprolol fumarate and ivabradine in pharmaceutical and biological matrices. Investigation of the method greenness.
Abo Elkheir, SM; Nasr, JJM; Walash, MI; Zeid, AM, 2022
)
1.15
"This study sought to evaluate the role of ivabradine hemisulfate sustained release (SR), a novel long-acting formulation of ivabradine dosed once daily, in stable patients with HFrEF."( Sustained-Release Ivabradine Hemisulfate in Patients With Systolic Heart Failure.
Cui, D; Li, J; Liu, G; Liu, K; Lou, D; Lu, S; Ma, S; Pang, X; Wang, J; Wang, X; Wu, S; Xie, X; Xue, L; Yang, Z; Ye, F; Yu, H; Zhang, Y; Zhong, M, 2022
)
1.32
" Ivabradine is indicated in the management of chronic coronary syndromes and heart failure with reduced ejection fraction for patients in whom heart rate targets cannot be achieved despite guideline-directed β-blocker dosing or having contraindication/intolerance to β-blockers."( Expert Consensus on Ivabradine-based Therapy for Heart Rate Management in Chronic Coronary Syndrome and Heart Failure with Reduced Ejection Fraction in India.
Agarwala, R; Kolapkar, V; Kumar, AS; Kumar, RVL; Mahala, BK; Mohan, JC; Panja, M; Patel, K; Ponde, CK; Sathyamurthy, I, 2023
)
2.14
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
cardiotonic drugA drug that has a strengthening effect on the heart or that can increase cardiac output.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
benzazepineA group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
carbobicyclic compoundA bicyclic compound in which all the ring atoms are carbon.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2Mus musculus (house mouse)EC50 (µMol)4.52004.52004.98505.4500AID515584
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1Mus musculus (house mouse)EC50 (µMol)4.50004.50004.50004.5000AID515582
Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)EC50 (µMol)4.28004.28006.42508.5700AID515585
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
regulation of heart ratePotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
sinoatrial node developmentPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
regulation of membrane depolarizationPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
monoatomic cation transportPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
muscle contractionPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
blood circulationPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
sodium ion transmembrane transportPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
regulation of membrane potentialPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
regulation of cardiac muscle contractionPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
cellular response to cAMPPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
cellular response to cGMPPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
potassium ion transmembrane transportPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
SA node cell action potentialPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
membrane depolarization during SA node cell action potentialPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
sodium ion import across plasma membranePotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
regulation of cardiac muscle cell action potential involved in regulation of contractionPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
potassium ion import across plasma membranePotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
intracellularly cAMP-activated cation channel activityPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
voltage-gated sodium channel activityPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
voltage-gated potassium channel activityPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
protein bindingPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
cAMP bindingPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
identical protein bindingPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
voltage-gated potassium channel activity involved in SA node cell action potential depolarizationPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membranePotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
perinuclear region of cytoplasmPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
HCN channel complexPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
axonPotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
dendritePotassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID1346502Mouse HCN1 (Cyclic nucleotide-regulated channels)2006The Journal of physiology, Apr-15, Volume: 572, Issue:Pt 2
Properties of ivabradine-induced block of HCN1 and HCN4 pacemaker channels.
AID1346533Mouse HCN2 (Cyclic nucleotide-regulated channels)2006Molecular pharmacology, Apr, Volume: 69, Issue:4
Bradycardic and proarrhythmic properties of sinus node inhibitors.
AID1346525Human HCN1 (Cyclic nucleotide-regulated channels)2006Molecular pharmacology, Apr, Volume: 69, Issue:4
Bradycardic and proarrhythmic properties of sinus node inhibitors.
AID1346522Human HCN3 (Cyclic nucleotide-regulated channels)2006Molecular pharmacology, Apr, Volume: 69, Issue:4
Bradycardic and proarrhythmic properties of sinus node inhibitors.
AID1346517Human HCN4 (Cyclic nucleotide-regulated channels)2006Molecular pharmacology, Apr, Volume: 69, Issue:4
Bradycardic and proarrhythmic properties of sinus node inhibitors.
AID515581Blockade of mouse HCN1 expressed in HEK293 cells at 5 uM at -120 f-current amplitude by patch-clamp electrophysiological assay relative to control2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.
AID406947Reversal of ischemia-induced ST segment elevation in anesthetized New Zealand white rabbit at 2.5 mg/kg, iv2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
AID515585Blockade of human HCN4 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.
AID406943Effect on heart rate in anesthetized New Zealand white rabbit myocardial ischemia model assessed as beats per minute at 0.16 mg/kg2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
AID1391632Reduction of cardiovascular events in patient with severe chronic heart failure assessed as reduction in heart rate at 7.5 mg, po bid for 14 days2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Next-generation small molecule therapies for heart failure: 2015 and beyond.
AID406944Effect on heart rate in anesthetized New Zealand white rabbit myocardial ischemia model assessed as beats per minute at 0.63 mg/kg2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
AID406942Effect on heart rate in anesthetized New Zealand white rabbit myocardial ischemia model assessed as beats per minute at 0.04 mg/kg2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
AID515584Blockade of mouse HCN2 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.
AID515582Blockade of mouse HCN1 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.
AID1391628Reduction of cardiovascular events in patient with acute MI and coronary revascularization assessed as reduction in death at 7.5 mg, po bid2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Next-generation small molecule therapies for heart failure: 2015 and beyond.
AID406939Reversal of ischemia-induced ST segment elevation in iv dosed anesthetized New Zealand white rabbit2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
AID1391629Reduction of cardiovascular events in patient with acute MI and coronary revascularization assessed as reduction in heart rate at 7.5 mg, po bid2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Next-generation small molecule therapies for heart failure: 2015 and beyond.
AID1391631Reduction of cardiovascular events in patient with severe chronic heart failure assessed as reduction in death at 7.5 mg, po bid for 14 days2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Next-generation small molecule therapies for heart failure: 2015 and beyond.
AID1391627Reduction of cardiovascular events in patient with coronary artery disease and left ventricular systolic dysfunction assessed as relative risk reduction at 7.5 mg, po bid2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Next-generation small molecule therapies for heart failure: 2015 and beyond.
AID406945Effect on heart rate in anesthetized New Zealand white rabbit myocardial ischemia model assessed as beats per minute at 2.5 mg/kg2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Sodium late current blockers in ischemia reperfusion: is the bullet magic?
AID515586Blockade of HCN in guinea pig spontaneously beating atria assessed as reduction of heart rate measured for 15 mins2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.
AID515583Blockade of human HCN4 expressed in HEK293 cells at 5 uM at -120 f-current amplitude by patch-clamp electrophysiological assay relative to control2010Journal of medicinal chemistry, Sep-23, Volume: 53, Issue:18
Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers.
AID1391630Reduction of cardiovascular events in patient with severe chronic heart failure and left ventricular systolic dysfunction assessed as relative risk reduction at 7.5 mg, po bid for 14 days2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Next-generation small molecule therapies for heart failure: 2015 and beyond.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,077)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's11 (1.02)18.2507
2000's173 (16.06)29.6817
2010's707 (65.65)24.3611
2020's186 (17.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 104.24

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index104.24 (24.57)
Research Supply Index7.20 (2.92)
Research Growth Index5.94 (4.65)
Search Engine Demand Index189.89 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (104.24)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials197 (17.24%)5.53%
Reviews257 (22.48%)6.00%
Case Studies100 (8.75%)4.05%
Observational24 (2.10%)0.25%
Other565 (49.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]