Ivabradine

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Ivabradine
Systematic (IUPAC) name
(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
Identifiers
CAS number	155974-00-8
ATC code	C01EB17
PubChem	132999
Chemical data
Formula	C27H36N2O5
Mol. mass	468.585 g/mol
Pharmacokinetic data
Bioavailability	40%
Protein binding	70%
Metabolism	Hepatic (first-pass) >50%, CYP3A4-mediated
Half life	2 hours
Excretion	Renal and fecal
Therapeutic considerations
Licence data	EU
Pregnancy cat.	D(AU)
Legal status	POM(UK)
Routes	Oral

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Ivabradine (INN) (pronounced /ɪˈvæbrədin/) is a novel medication used for the symptomatic management of stable angina pectoris. It is marketed under the trade name Procoralan (Servier Laboratories), and was also known as S-16257 during its development. Ivabradine acts by reducing the heart rate in a mechanism different from beta blockers and calcium channel blockers, two commonly prescribed antianginal drugs. It is classified as a cardiotonic agent.

Mode of action

Ivabradine acts on the I_f (f is for "funny", so called because it had unusual properties compared with other current systems known at the time of its discovery) ion current, which is highly expressed in the sinoatrial node. I_f is a mixed Na⁺–K⁺ inward current activated by hyperpolarization and modulated by the autonomic nervous system. It is one of the most important ionic currents for regulating pacemaker activity in the sinoatrial (SA) node. Ivabradine selectively inhibits the pacemaker I_f current in a dose-dependent manner. Blocking this channel reduces cardiac pacemaker activity, slowing the heart rate and allowing more time for blood to flow to the myocardium.^[1][1]

Uses

Ivabradine was approved by the European Medicines Agency in 2005. It is indicated for the symptomatic treatment of stable angina pectoris in patients with normal sinus rhythm, who have a contraindication to or intolerance to beta blockers. It has been shown to be non-inferior to the beta-blocker atenolol for this indication^[1] and amlodipine.

Apart from angina, it is also being used off-label in the treatment of inappropriate sinus tachycardia.^[1]

Dosage

A dose of 5 mg twice daily is recommended initially; after 1 month, it is recommended to increase to 7.5 mg twice daily to get the optimal efficacy linked to heart rate reduction. Given limited experience in the elderly, the manufacturer recommends a starting dose of 2.5 mg^[1].

Adverse effects

14.5% of all patients taking ivabradine experience luminous phenomena (by patients described as sensations of enhanced brightness in a fully maintained visual field). This is probably due to blockage of I _h ion channels in the retina which are very similar to cardiac I_f. These symptoms are mild, transient, fully reversible and non-severe. In clinical studies about 1% of all patients had to discontinue the drug because of these sensations, which occurred on average 40 days after commencement of the drug.^[1]

Bradycardia (unusually slow heart rate) occurs at 2% and 5% for doses of 7.5 and 10 mg respectively (compared to 4.3% in atenonol)^[1]. 2.6-4.8% reported headaches^[1]. Other common adverse drug reactions (1–10% of patients) include first-degree AV block, ventricular extrasystoles, dizziness and/or blurred vision.^[1]

Contraindications

Ivabradine is contraindicated in sick sinus syndrome, and cannot be used concominantly with inhibitors of CYP3A4 such as azole antifungals (such as ketoconazole), macrolide antibiotics, nefazodone and the anti-HIV drugs nelfinavir and ritonavir^[1].

References

External links

• Official site
• Manufacturer´s web site
• Procoralan UK
• Źródło: "http://pl.wikipedia.org/wiki/Iwabradyna"

v • d • e Electrocardiography
Overview	History of the EKG • EKG interpretation basics • Normal sinus rhythm
EKG Complexes	P wave • QRS complex • ST Segment • T wave • U wave Osborn wave • H wave • K wave • Delta wave NSSTW changes
EKG Intervals	PR Interval • QRS Interval • ST Interval • QT Interval
Conduction System & Bradycardia	Cardiac pacemaker • SA node • AV node• Bundle of His • Purkinje fibers • Sinus bradycardia • First Degree AV Block • Second Degree AV Block • Complete or Third-Degree AV Block • Concealed conduction • AV Junctional Rhythms • LBBB • LAHB • LPHB • RBBB • Trifascicular block
Atrial Arrhythmias	Sinus tachycardia • Premature Atrial Contractions (PACs) • Ectopic Atrial Rhythm • Paroxysmal Atrial Tachycardia (PAT) • Paroxysmal Atrial Tachycardia (PAT) with Block • Multifocal Atrial Tachycardia (MAT) • Atrial Flutter • Atrial Fibrillation • Wandering atrial pacemaker
Ventricular Arrhythmias	Differential Diagnosis of Tachycardia with a Wide QRS Complex • Accelerated Idioventricular Rhythm • Ventricular Parasystole • Premature Ventricular Contractions (PVCs) • Ventricular tachycardia • Ventricular Fibrillation • Sudden cardiac death
EKG Abnormalities in Disease States	Hypertrophy & Dilatation • Right atrial enlargement • Left atrial enlargement • Biatrial enlargement • Left Ventricular Hypertrophy • Right Ventricular Hypertrophy • Biventricular Hypertrophy • Acute myocardial infarction • NSTEMI • STEMI • Right ventricular myocardial infarction • Atrial infarction Pre-excitation Syndromes • Wolff-Parkinson-White Syndrome • Lown Ganong Levine Syndrome • Mahaim Type Preexcitation Cardiomyopathies • Arrhythmogenic Right Ventricular Dysplasia • Dilated Cardiomyopathy • Hypertrophic Cardiomyopathy Drug Effects on the EKG • Adenosine • β-blockers • Digitalis • Quinidine • Procainamide • Disopyramide • Lidocaine • Tocainide and Mexiletine • Phenytoin • Encainide, Flecainide and Propafenone • Amiodarone • Bretylium • Ca Channel Blockers • Phenothiazines • Tricyclic Antidepressants • Lithium Congenital Heart Disease • Dextrocardia • Atrial Septal Defect • Ventricular Septal Defect • Tetralogy of Fallot • Conjoined Twins or Siamese Twins Electrolyte Disturbances • Hyperkalemia • Hypokalemia • Hypercalcemia • Hypocalcemia • Nonspecific Changes Other Heart Diseases • Pericarditis • Myocarditis • Tamponade • Heart Transplantation • Sick Sinus Syndrome • Long QT Syndrome Inherited Disease • Brugada Syndrome Systemic Diseases • CNS Disease • Cardiac Tumors Heart Transplantation • EKG Changes in patient with Heart Transplantation Exogenous Effects • Hypothermia • Chest Trauma • Insect Bites • Electric Injuries
Technical Issues and Potential Errors in Interpretation	Artifacts • Lead Placement Errors • The EKG in a Patient with a Pacemaker

v • d • e Circulatory system pathology (I, 390-459)
Hypertension	Hypertensive heart disease - Hypertensive nephropathy - Secondary hypertension (Renovascular hypertension)
Ischaemic heart disease	Angina pectoris (Prinzmetal's angina) - Myocardial infarction (heart attack) - Dressler's syndrome
Pulmonary circulation	Pulmonary embolism - Cor pulmonale
Pericardium	Pericarditis - Pericardial effusion - Cardiac tamponade
Endocardium/heart valves	Endocarditis - mitral valve (regurgitation, prolapse, stenosis) - aortic valve (stenosis, insufficiency) - pulmonary valve (stenosis, insufficiency) - tricuspid valve (stenosis, insufficiency)
Myocardium	Myocarditis - Cardiomyopathy (Dilated cardiomyopathy, Hypertrophic cardiomyopathy, Loeffler endocarditis, Restrictive cardiomyopathy) - Arrhythmogenic right ventricular dysplasia
Electrical conduction system of the heart	Heart block: AV block (First degree, Second degree, Third degree) - Bundle branch block (Left, Right) - Bifascicular block - Trifascicular block Pre-excitation syndrome (Wolff-Parkinson-White, Lown-Ganong-Levine) - Long QT syndrome - Adams-Stokes syndrome - Cardiac arrest - Sudden cardiac death Arrhythmia: Paroxysmal tachycardia (Supraventricular, AV nodal reentrant, Ventricular) - Atrial flutter - Atrial fibrillation (Familial) - Ventricular fibrillation - Premature contraction (Atrial, Ventricular) - Ectopic pacemaker - Sick sinus syndrome
Other heart conditions	Heart failure - Cardiovascular disease - Cardiomegaly - Ventricular hypertrophy (Left, Right)
Cerebrovascular diseases	Stroke - Transient ischemic attack - Intracranial hemorrhage/cerebral hemorrhage: Extra-axial hemorrhage (Epidural hemorrhage, Subdural hemorrhage, Subarachnoid hemorrhage) Intra-axial hematoma (Intraventricular hemorrhages, Intraparenchymal hemorrhage) - Anterior spinal artery syndrome - Binswanger's disease - Moyamoya disease
Arteries, arterioles and capillaries	Atherosclerosis (Renal artery stenosis) - Aortic dissection/Aortic aneurysm (Abdominal aortic aneurysm) - Aneurysm - Raynaud's phenomenon/Raynaud's disease - Buerger's disease - Vasculitis/Arteritis (Aortitis) - Intermittent claudication - Arteriovenous fistula - Hereditary hemorrhagic telangiectasia - Spider angioma - Dissection (Carotid artery, Vertebral artery)
Veins, lymphatic vessels and lymph nodes	Thrombosis/Phlebitis/Thrombophlebitis (Deep vein thrombosis, May-Thurner syndrome, Portal vein thrombosis, Venous thrombosis, Budd-Chiari syndrome, Renal vein thrombosis, Paget-Schroetter disease) - Varicose veins / Portacaval anastomosis (Hemorrhoid, Esophageal varices, Varicocele, Gastric varices, Caput medusae) - Superior vena cava syndrome - Lymph (Lymphadenitis, Lymphedema, Lymphangitis)
Other	Hypotension (Orthostatic hypotension) - Rheumatic fever
See also congenital (Q20-Q28, 745-747)

v • d • e WikiDoc Research Resources for Ivabradine
Articles on Ivabradine	Most recent articles on Ivabradine • Most cited articles on Ivabradine • Review articles on Ivabradine • Articles on Ivabradine in N Eng J Med, Lancet, BMJ
Media (Slides, Video, Images, MP3) on Ivabradine	Powerpoint slides on Ivabradine • Images of Ivabradine • Photos of Ivabradine • Podcasts & MP3s on Ivabradine • Videos on Ivabradine
Evidence Based Medicine Regarding Ivabradine	Cochrane Collaboration on Ivabradine • Bandolier on Ivabradine • TRIP on Ivabradine
Cost Effectiveness of Ivabradine	Cost Effectiveness of Ivabradine
Clinical Trials Involving Ivabradine	Ongoing Trials on Ivabradine at Clinical Trials.gov • Trial results on Ivabradine • Clinical Trials on Ivabradine at Google
Guidelines / Policies / Government Resources (FDA/CDC) Regarding Ivabradine	US National Guidelines Clearinghouse on Ivabradine • NICE Guidance on Ivabradine • NHS PRODIGY Guidance • FDA on Ivabradine • CDC on Ivabradine
Textbook Information on Ivabradine	Books and Textbook Information on Ivabradine
Pharmacology Resources on Ivabradine	Dosing of Ivabradine • Drug interactions with Ivabradine • Side effects of Ivabradine • Allergic reactions to Ivabradine • Overdose information on Ivabradine • Carcinogenicity information on Ivabradine • Ivabradine in pregnancy • Pharmacokinetics of Ivabradine •
Genetics, Pharmacogenomics, and Proteinomics of Ivabradine	Genetics of Ivabradine • Pharmacogenomics of Ivabradine • Proteomics of Ivabradine
Newstories on Ivabradine	Ivabradine in the news • Be alerted to news on Ivabradine • News trends on Ivabradine
Commentary on Ivabradine	Blogs on Ivabradine
Patient Resources on Ivabradine	Patient resources on Ivabradine • Discussion groups on Ivabradine • Patient Handouts on Ivabradine • Directions to Hospitals Treating Ivabradine • Risk calculators and risk factors for Ivabradine
Healthcare Provider Resources on Ivabradine	Symptoms of Ivabradine • Causes & Risk Factors for Ivabradine • Diagnostic studies for Ivabradine • Treatment of Ivabradine
Continuing Medical Education (CME) Programs on Ivabradine	CME Programs on Ivabradine
International Resources on Ivabradine	Ivabradine en Espanol • Ivabradine en Francais
Business Resources on Ivabradine	Ivabradine in the Marketplace • Patents on Ivabradine
Informatics Resources on Ivabradine	List of terms related to Ivabradine

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Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .