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
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An Open Labeled Pilot Study of Atorvastatin in Systemic Lupus Erythematosus

First Posted Date
2007-02-07
Last Posted Date
2007-03-20
Lead Sponsor
Buddhist Tzu Chi General Hospital
Target Recruit Count
40
Registration Number
NCT00432354
Locations
🇨🇳

Dalin Tzu Chi General Hospital, Chia-yi, Taiwan

🇨🇳

Buddhist Dalin Tzu Chi General Hospital, Chia-Yi, Taiwan

Study of Asian Patients With Hypercholesterolaemia in the UK - Rosuvastatin 5mg Versus Atorvastatin 10mg

First Posted Date
2007-01-29
Last Posted Date
2010-12-16
Lead Sponsor
AstraZeneca
Target Recruit Count
55
Registration Number
NCT00427960
Locations
🇬🇧

Research Site, Newcastle, United Kingdom

🇬🇧

Research SIte, Slough, United Kingdom

Investigations on Differences in Atorvastatin Metabolites Ratios as a Diagnostic Tool in Detecting Atorvastatin Induced Myotoxicity

Phase 4
Completed
Conditions
Interventions
First Posted Date
2006-12-21
Last Posted Date
2014-12-03
Lead Sponsor
University of Oslo School of Pharmacy
Target Recruit Count
53
Registration Number
NCT00414531
Locations
🇳🇴

Rikshospitalet-Radiumhospitalet HF, Lipid clinic, Oslo, Norway

Atorvastatin to Prevent Avascular Necrosis of Bone in Steroid Treated Exacerbated Systemic Lupus Erythematosus

First Posted Date
2006-12-19
Last Posted Date
2018-11-23
Lead Sponsor
NYU Langone Health
Target Recruit Count
43
Registration Number
NCT00412841
Locations
🇺🇸

The New York University Hospital For Joint Diseases, New York, New York, United States

Study To Determine The Effects Of Doses Of Relacatib On The Metabolism Of Acetaminophen, Ibuprofen And Atorvastatin

First Posted Date
2006-12-13
Last Posted Date
2017-10-04
Lead Sponsor
GlaxoSmithKline
Target Recruit Count
32
Registration Number
NCT00411190
Locations
🇧🇪

GSK Investigational Site, Liège, Belgium

ROMEO (Rosuvastatin in Metabolic syndrOme)

Phase 4
Completed
Conditions
Interventions
First Posted Date
2006-11-03
Last Posted Date
2011-07-11
Lead Sponsor
AstraZeneca
Target Recruit Count
258
Registration Number
NCT00395486
Locations
🇰🇷

Research Site, Suwon, Korea, Republic of

Regulation of Lipoprotein Metabolism in Obese Men

Phase 3
Completed
Conditions
First Posted Date
2006-10-26
Last Posted Date
2006-10-26
Lead Sponsor
The University of Western Australia
Target Recruit Count
48
Registration Number
NCT00392717
Locations
🇦🇺

Royal Perth Hospital, Perth, Western Australia, Australia

This Study Uses Ultrasound to Determine Whether Atorvastatin or Pravastatin Effects the Progression of Coronary Plaque.

Phase 4
Completed
Conditions
First Posted Date
2006-09-27
Last Posted Date
2006-12-04
Lead Sponsor
Pfizer
Target Recruit Count
600
Registration Number
NCT00380939
Locations
🇺🇸

Pfizer Investigational Site, Seattle, Washington, United States

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