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
-

Multiple Ascending Dose and DDI Study

First Posted Date
2017-01-25
Last Posted Date
2017-09-06
Lead Sponsor
Pfizer
Target Recruit Count
62
Registration Number
NCT03031119
Locations
🇧🇪

Pfizer Clinical Research Unit, Brussels, Belgium

Statin for Preventing Hepatocellular Carcinoma Recurrence After Curative Treatment

Phase 4
Active, not recruiting
Conditions
Interventions
First Posted Date
2017-01-19
Last Posted Date
2024-11-12
Lead Sponsor
Chiayi Christian Hospital
Target Recruit Count
240
Registration Number
NCT03024684
Locations
🇨🇳

Ditmanson Medical Foundation Chiayi Christian Hospital, Chiayi City, Taiwan

🇨🇳

E-DA Hospital, Kaohsiung, Taiwan

🇨🇳

Taichung Veterans General Hospital, Taichung, Taiwan

and more 3 locations

The Effect of HMG-CoA Reductase Inhibition on Postprandial GLP-1 Secretion

First Posted Date
2017-01-12
Last Posted Date
2017-03-03
Lead Sponsor
University Hospital, Gentofte, Copenhagen
Target Recruit Count
15
Registration Number
NCT03018444
Locations
🇩🇰

University Hospital, Gentofte, Copenhagen, Hellerup, Region Hovedstaden, Denmark

Effect of PCSK9-Antibody (Alirocumab) on Dyslipidemia Secondary to Nephrotic Syndrome

First Posted Date
2016-12-28
Last Posted Date
2022-08-19
Lead Sponsor
Gloria Vega
Target Recruit Count
3
Registration Number
NCT03004001
Locations
🇺🇸

DallasVAMC, Dallas, Texas, United States

Evaluation of Effect of Alirocumab on Coronary Atheroma Volume in Japanese Patients Hospitalized for Acute Coronary Syndrome With Hypercholesterolemia

First Posted Date
2016-12-07
Last Posted Date
2019-09-09
Lead Sponsor
Sanofi
Target Recruit Count
206
Registration Number
NCT02984982
Locations
🇯🇵

Investigational Site Number 392008, Gifu-shi, Japan

🇯🇵

Investigational Site Number 392022, Chiyoda-ku, Japan

🇯🇵

Investigational Site Number 392039, Hiroshima-shi, Japan

and more 36 locations

Statin Immune Study

Phase 4
Completed
Conditions
Interventions
First Posted Date
2016-12-06
Last Posted Date
2018-12-03
Lead Sponsor
University of Dundee
Target Recruit Count
18
Registration Number
NCT02984293
Locations
🇬🇧

University of Dundee, Dundee, United Kingdom

A Comparative Study of Rosuvastatin and Atorvastatin in Patients With Hyperlipidemia

First Posted Date
2016-12-02
Last Posted Date
2016-12-02
Lead Sponsor
Bangabandhu Sheikh Mujib Medical University, Dhaka, Bangladesh
Target Recruit Count
90
Registration Number
NCT02979704
Locations
🇧🇩

BSMMU, Dhaka, Bangladesh

Atorvastatin for the Treatment of Lithium-Induced Nephrogenic Diabetes Insipidus

First Posted Date
2016-11-18
Last Posted Date
2020-09-16
Lead Sponsor
Lady Davis Institute
Target Recruit Count
60
Registration Number
NCT02967653
Locations
🇨🇦

McGill University Health Centre, Montréal, Quebec, Canada

🇨🇦

Douglas Mental Health University Institute, Montréal, Quebec, Canada

🇨🇦

Jewish General Hospital, Montréal, Quebec, Canada

The Effect on EPCs by Statin Loading in "All Comers" With an ACS

First Posted Date
2016-11-06
Last Posted Date
2019-04-12
Lead Sponsor
University Hospitals of North Midlands NHS Trust
Target Recruit Count
40
Registration Number
NCT02957162
Locations
🇬🇧

University Hospitals of North Midlands NHS Trust, Stoke-on-Trent, Staffordshire, United Kingdom

STOP-CA (Statins TO Prevent the Cardiotoxicity From Anthracyclines)

Phase 2
Completed
Conditions
Interventions
First Posted Date
2016-10-24
Last Posted Date
2023-12-18
Lead Sponsor
Massachusetts General Hospital
Target Recruit Count
300
Registration Number
NCT02943590
Locations
🇺🇸

Massachusetts general Hospital, Boston, Massachusetts, United States

🇺🇸

University of Pennsylvania Medical System, Philadelphia, Pennsylvania, United States

🇨🇦

McGill University Health Center, Toronto, Canada

and more 1 locations
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