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Eplerenone (INN) (IPA: [ɛpˈlɛrənoʊn]) is an aldosterone antagonist used as an adjunct in the management of chronic heart failure. It is similar to spironolactone, though it may be more specific for the mineralocorticoid receptor and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. It is marketed by Pfizer under the trade name Inspra. IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ...
CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences and alloys. ...
The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ...
A section of the Anatomical Therapeutic Chemical Classification System. ...
PubChem is a database of chemical molecules . ...
DrugBank is a database available at the University of Alberta that provides information about thousands of products. ...
A chemical formula (also called molecular formula) is a concise way of expressing information about the atoms that constitute a particular chemical compound. ...
The molecular mass of a substance (less accurately called molecular weight and abbreviated as MW) is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ...
In pharmacology, bioavailability is used to describe the fraction of an administered dose of medication that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ...
Santorio Santorio (1561-1636) in his steelyard balance, from Ars de statica medecina, first published 1614 Metabolism (from μεταβολισμος (metabolismos)) is the biochemical modification of chemical compounds in living organisms and cells. ...
The liver is an organ in vertebrates including humans. ...
Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ...
The elimination half-life of a drug (or any xenobiotic agent) refers to the timecourse necessary for the quantity of the xenobiotic agent in the body (or plasma concentration) to be reduced to half of its original level through various elimination processes. ...
Excretion is the biological process by which an organism chemically separates waste products from its body. ...
Kidneys viewed from behind with spine removed The kidneys are bean-shaped excretory organs in vertebrates. ...
X-Ray of the bile duct during a laprascopic cholecystectomy A bile duct is any of a number of long tube-like structures that carry bile. ...
The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother. ...
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The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...
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An International Nonproprietary Name (INN) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization. ...
The International Phonetic Alphabet (IPA) is a system of phonetic notation devised by linguists to accurately and uniquely represent each of the wide variety of sounds (phones or phonemes) used in spoken human language. ...
Aldosterone antagonist refers to drugs which antagonise the action of aldosterone at mineralocorticoid receptors. ...
Congestive heart failure (CHF) (also called congestive cardiac failure and heart failure) is the inability of the heart to pump a sufficient amount of blood throughout the body, or requiring elevated filling pressures in order to pump effectively. ...
Spironolactone (marketed as Aldactone or Spiritone) is a synthetic 17-lactone steroid which is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used primarily to treat low-renin hypertension, hypokalemia, and Conns syndrome. ...
The circulatory system or cardiovascular system is the organ system which circulates blood around the body of most animals. ...
A myocardial infarction occurs when an atherosclerotic plaque slowly builds up in the inner lining of a coronary artery and then suddenly ruptures, totally occluding the artery and preventing blood flow downstream. ...
Pfizer, Incorporated (NYSE: PFE), is a global pharmaceutical company, with headquarters in New York City. ...
Clinical use
Indications Eplerenone is specifically indicated for the reduction of risk of cardiovascular death in patients with heart failure and left ventricular dysfunction within 3–14 days of an acute myocardial infarction, in combination with standard therapies. The circulatory system or cardiovascular system is the organ system which circulates blood around the body of most animals. ...
In the heart, a ventricle is a chamber which collects blood from an atrium (another heart chamber) and pumps it out of the heart. ...
A myocardial infarction occurs when an atherosclerotic plaque slowly builds up in the inner lining of a coronary artery and then suddenly ruptures, totally occluding the artery and preventing blood flow downstream. ...
Contraindications Eplerenone is contraindicated in patients with hyperkalaemia, renal impairment, or severe hepatic impairment. The manufacturer of eplerenone also contraindicates concomitant treatment with ketoconazole, itraconazole or other potassium-sparing diuretics. Hyperkalemia (hyper is high, kalium is the Latin name for potassium) is an elevated blood level (above 5. ...
Renal failure is when the kidneys fail to function properly. ...
Ketoconazole Ketoconazole is a synthetic antifungal drug used to prevent and treat skin and fungal infections, especially in immunocompromised patients such as those with AIDS. Due to its side-effect profile, it has been superseded by newer antifungals, such as fluconazole and itraconazole. ...
Itraconazole (marketed as Sporanox® by Janssen Pharmaceutica) is an antifungal agent that is prescribed to patients with fungal infections. ...
Adverse effects Common adverse drug reactions (ADRs) associated with the use of eplerenone include: hyperkalaemia, hypotension, dizziness, altered renal function, and increased creatinine concentration. (Rossi, 2006) An adverse drug reaction (abbreviated ADR) is a term to describe the unwanted, negative consequences sometimes associated with the use of medications. ...
Hyperkalemia (hyper is high, kalium is the Latin name for potassium) is an elevated blood level (above 5. ...
In physiology and medicine, hypotension refers to an abnormally low blood pressure. ...
Drug interactions Eplerenone is primarily metabolised by the cytochrome P450 enzyme CYP3A4. Thus the potential exists for adverse drug interactions with other drugs that induce or inhibit CYP3A4. Specifically, the concomitant use of the CYP3A4 inhibitors ketoconazole and itraconazole is contraindicated. Other CYP3A4 inhibitors including erythromycin, fluconazole, saquinavir, and verapamil should be used with caution. Other drugs that increase potassium concentrations may increase the risk of hyperkalaemia associated with eplerenone therapy, including potassium supplements and other potassium-sparing diuretics. Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ...
Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ...
Ketoconazole Ketoconazole is a synthetic antifungal drug used to prevent and treat skin and fungal infections, especially in immunocompromised patients such as those with AIDS. Due to its side-effect profile, it has been superseded by newer antifungals, such as fluconazole and itraconazole. ...
Itraconazole (marketed as Sporanox® by Janssen Pharmaceutica) is an antifungal agent that is prescribed to patients with fungal infections. ...
Erythromycin is a macrolide antibiotic which has an antimicrobial spectrum similar to or slightly wider than that of penicillin, and is often used for people who have an allergy to penicillins. ...
To meet Wikipedias quality standards, this article or section may require cleanup. ...
Saquinavir (Fortovase®, Roche) is a protease inhibitor, used as a component of HIV therapy. ...
Verapamil (brand names: Isoptin®, Verelan®, Calan®) is a medical drug that acts as an L-type calcium channel blocker. ...
General Name, Symbol, Number potassium, K, 19 Chemical series alkali metals Group, Period, Block 1, 4, s Appearance silvery white Atomic mass 39. ...
See also Spironolactone (marketed as Aldactone or Spiritone) is a synthetic 17-lactone steroid which is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used primarily to treat low-renin hypertension, hypokalemia, and Conns syndrome. ...
Aldosterone antagonist refers to drugs which antagonise the action of aldosterone at mineralocorticoid receptors. ...
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