Atorvastatin

Generic Name
Atorvastatin
Brand Names
Atorvaliq, Caduet, Lipitor, Lypqozet
Drug Type
Small Molecule
Chemical Formula
C33H35FN2O5
CAS Number
134523-00-5
Unique Ingredient Identifier
A0JWA85V8F
Background

Atorvastatin (Lipitor®), is a lipid-lowering drug included in the statin class of medications. By inhibiting the endogenous production of cholesterol in the liver, statins lower abnormal cholesterol and lipid levels, and ultimately reduce the risk of cardiovascular disease. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase, which catalyzes the conversion of HMG-CoA to mevalonic acid. This conversion is a critical metabolic reaction involved in the production of several compounds involved in lipid metabolism and transport, including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very-low-density lipoprotein (VLDL). Prescribing statins is considered standard practice for patients following any cardiovascular event, and for people who are at moderate to high risk of developing cardiovascular disease. The evidence supporting statin use, coupled with minimal side effects and long term benefits, has resulted in wide use of this medication in North America.

Atorvastatin and other statins including lovastatin, pravastatin, rosuvastatin, fluvastatin, and simvastatin are considered first-line treatment options for dyslipidemia. The increasing use of this class of drugs is largely attributed to the rise in cardiovascular diseases (CVD) (such as heart attack, atherosclerosis, angina, peripheral artery disease, and stroke) in many countries. An elevated cholesterol level (elevated low-density lipoprotein (LDL) levels in particular) is a significant risk factor for the development of CVD. Several landmark studies demonstrate that the use of statins is associated with both a reduction in LDL levels and CVD risk. Statins were shown to reduce the incidences of all-cause mortality, including fatal and non-fatal CVD, as well as the need for surgical revascularization or angioplasty following a heart attack. Some evidence has shown that even for low-risk individuals (with <10% risk of a major vascular event occurring within five years) statin use leads to a 20%-22% relative reduction in the number of major cardiovascular events (heart attack, stroke, coronary revascularization, and coronary death) for every 1 mmol/L reduction in LDL without any significant side effects or risks.

Atorvastatin was first synthesized in 1985 by Dr. Bruce Roth and approved by the FDA in 1996. It is a pentasubstituted pyrrole formed by two contrasting moieties with an achiral heterocyclic core unit and a 3,5-dihydroxypentanoyl side chain identical to its parent compound. Unlike other members of the statin group, atorvastatin is an active compound and therefore does not require activation.

Indication

Atorvastatin is indicated for the treatment of several types of dyslipidemias, including primary hyperlipidemia and mixed dyslipidemia in adults, hypertriglyceridemia, primary dysbetalipoproteinemia, homozygous familial hypercholesterolemia, and heterozygous familial hypercholesterolemia in adolescent patients with failed dietary modifications.

Dyslipidemia describes an elevation of plasma cholesterol, triglycerides or both as well as to the presence of low levels of high-density lipoprotein. This condition represents an increased risk for the development of atherosclerosis.

Atorvastatin is indicated, in combination with dietary modifications, to prevent cardiovascular events in patients with cardiac risk factors and/or abnormal lipid profiles.

Atorvastatin can be used as a preventive agent for myocardial infarction, stroke, revascularization, and angina, in patients without coronary heart disease but with multiple risk factors and in patients with type 2 diabetes without coronary heart disease but multiple risk factors.

Atorvastatin may be used as a preventive agent for non-fatal myocardial infarction, fatal and non-fatal stroke, revascularization procedures, hospitalization for congestive heart failure and angina in patients with coronary heart disease.

Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.

Associated Conditions
Anginal Pain, Cardiovascular Complications, Cardiovascular Disease (CVD), Coronary Artery Disease (CAD), Coronary artery thrombosis, Dysbetalipoproteinemia, Fredrickson Type III lipidemia, Heterozygous Familial Hypercholesterolemia (HeFH), High Cholesterol, Homozygous Familial Hypercholesterolaemia (HoFH), Hospitalizations, Hypertension, Essential Hypertension, Hypertriglyceridemias, Mixed Dyslipidemias, Mixed Hyperlipidemia, Myocardial Infarction, Non-familial hypercholesterolemia, Nonfatal Myocardial Infarction, Postoperative Thromboembolism, Primary Hypercholesterolemia, Stroke, Thrombosis, Transient Ischemic Attack, Elevation of serum triglyceride levels, Heterozygous familial hyperlipidemia, Non-familial hyperlipidemia, Primary Hyperlipidemia, Revascularization procedures
Associated Therapies
-

Atorvastatin Treatment to Attenuate the Progression of Cardiovascular Disease in Hemodialysis Patients

First Posted Date
2007-06-01
Last Posted Date
2013-09-09
Lead Sponsor
Ercan OK
Target Recruit Count
446
Registration Number
NCT00481364
Locations
🇹🇷

Ege University School of Medicine, Division of Nephrology, Bornova, Izmir, Turkey

Atorvastatin Pre-Treatment Influences the Risk of Percutaneous Coronary Intervention Study

Phase 3
Completed
Conditions
Interventions
First Posted Date
2007-05-04
Last Posted Date
2009-01-27
Lead Sponsor
University Hospital, Motol
Target Recruit Count
200
Registration Number
NCT00469326
Locations
🇨🇿

Department of Cardiology, CardioVascular Center, University Hospital Motol, Prague, Czech Republic

Effect of Statins on Asthma Control in Smokers With Asthma

Phase 2
Completed
Conditions
Interventions
First Posted Date
2007-04-20
Last Posted Date
2017-03-28
Lead Sponsor
NHS Greater Clyde and Glasgow
Target Recruit Count
71
Registration Number
NCT00463827
Locations
🇬🇧

Gartnavel General Hospital, Glasgow, United Kingdom

Atorvastatin in Moderate Active Crohns Disease

Phase 2
Completed
Conditions
First Posted Date
2007-03-30
Last Posted Date
2007-10-22
Lead Sponsor
Skane University Hospital
Target Recruit Count
12
Registration Number
NCT00454545
Locations
🇸🇪

Department of Medicine, Division of Gastroenterology and Hepatology, Malmö, Sweden

Statin for Immunomudulation in Sepsis

Phase 2
Conditions
Interventions
First Posted Date
2007-03-27
Last Posted Date
2009-06-26
Lead Sponsor
Hospital de Clinicas de Porto Alegre
Target Recruit Count
80
Registration Number
NCT00452608
Locations
🇧🇷

HCPA - Clinical Hospital fo Porto Alegre, Porto Alegre, Rio Grande do Sul, Brazil

Silent Cerebrovascular Lesion and Cognitive Decline Prevention by Cholesterol Lowering in Elderly AF Patients

First Posted Date
2007-03-20
Last Posted Date
2007-03-20
Lead Sponsor
Radboud University Medical Center
Target Recruit Count
35
Registration Number
NCT00449410
Locations
🇳🇱

Gheorghe AM Pop, Nijmegen, Netherlands

Dose Finding Trial of Rosuvastatin and Atorvastatin Versus Hepatitis C

Phase 2
Completed
Conditions
First Posted Date
2007-03-13
Last Posted Date
2008-09-09
Lead Sponsor
Bader, Ted, M.D.
Target Recruit Count
16
Registration Number
NCT00446940
Locations
🇺🇸

VA Hospital, OKlahoma City, Oklahoma, United States

Does Atorvastatin Reduce Ischemia-Reperfusion Injury in Humans in-Vivo?

First Posted Date
2007-03-01
Last Posted Date
2009-03-17
Lead Sponsor
Radboud University Medical Center
Target Recruit Count
30
Registration Number
NCT00441597
Locations
🇳🇱

Radboud University Nijmegen Medical Centre, Nijmegen, Netherlands

Statins to Reduce D-dimer Levels in Patients With Venous Thrombosis

First Posted Date
2007-02-21
Last Posted Date
2011-08-19
Lead Sponsor
Università degli Studi dell'Insubria
Target Recruit Count
10
Registration Number
NCT00437892
Locations
🇮🇹

University of Bologna, Bologna, Italy

🇮🇹

Ospedale di Piacenza, Piacenza, Italy

🇮🇹

University Of Insubria, Varese, Italy

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