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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To Evaluate the Drug-drug Interaction Between Telmisartan and Atorvastatin in Healthy Male Volunteers

First Posted Date
2015-10-19
Last Posted Date
2015-10-19
Lead Sponsor
Samil Pharmaceutical Co., Ltd.
Target Recruit Count
48
Registration Number
NCT02579356
Locations
🇰🇷

Chonbuk National University Hospital, Seoul, Korea, Republic of

A Study to Compare the Pharmacokinetics of Fimasartan/Atorvastatin Combination Tablet

First Posted Date
2015-10-02
Last Posted Date
2016-02-25
Lead Sponsor
Boryung Pharmaceutical Co., Ltd
Target Recruit Count
99
Registration Number
NCT02566187
Locations
🇰🇷

Inje University Busan Paik Hospital, Busan, Korea, Republic of

Atorvastatin in the Recipient's Kidney Graft From a Living Donor

Phase 3
Completed
Conditions
Interventions
First Posted Date
2015-08-13
Last Posted Date
2018-09-10
Lead Sponsor
Instituto Mexicano del Seguro Social
Target Recruit Count
48
Registration Number
NCT02522117
Locations
🇲🇽

Western Medical Center, Mexican Institute of Social Security, Guadalajara, Jalisco, Mexico

LIpitor and biGuanide to Androgen Delay Trial

First Posted Date
2015-07-14
Last Posted Date
2021-04-19
Lead Sponsor
University Health Network, Toronto
Registration Number
NCT02497638
Locations
🇨🇦

Princess Margaret Cancer Centre, Toronto, Ontario, Canada

Protective Effect of Statin on Sleep Deprivation

Not Applicable
Conditions
Interventions
First Posted Date
2015-07-14
Last Posted Date
2015-07-14
Lead Sponsor
Shi Yang
Target Recruit Count
72
Registration Number
NCT02496962
Locations
🇨🇳

PLA General Hospital, Beijing, Beijing, China

Safety, Tolerability, and Effect of Alirocumab in High Cardiovascular Risk Patients With Severe Hypercholesterolemia Not Adequately Controlled With Conventional Lipid-modifying Therapies (ODYSSEY APPRISE)

First Posted Date
2015-06-19
Last Posted Date
2022-03-28
Lead Sponsor
Sanofi
Target Recruit Count
998
Registration Number
NCT02476006
Locations
🇦🇹

Investigational Site Number 040001, Graz, Austria

🇦🇹

Investigational Site Number 040002, Wien, Austria

🇦🇹

Investigational Site Number 040010, Wien, Austria

and more 150 locations

Effect of Atorvastatin on Glycemic Control in Prediabetic Patients

Completed
Conditions
Interventions
First Posted Date
2015-06-12
Last Posted Date
2015-08-17
Lead Sponsor
Shri Ramachandra Bhanj Medical College
Target Recruit Count
75
Registration Number
NCT02470455
Locations
🇮🇳

SCB Medical College, Cuttack, Odisha, India

Relationship Between Insulin Resistance and Statin Induced Type 2 Diabetes, and Integrative Personal Omics Profiling

First Posted Date
2015-05-07
Last Posted Date
2021-04-06
Lead Sponsor
Stanford University
Target Recruit Count
115
Registration Number
NCT02437084
Locations
🇺🇸

Stanford University School of Medicine, Stanford, California, United States

Atorvastatin in Active Vitiligo

Phase 2
Completed
Conditions
Interventions
First Posted Date
2015-05-04
Last Posted Date
2018-02-05
Lead Sponsor
Centre Hospitalier Universitaire de Nice
Target Recruit Count
28
Registration Number
NCT02432534
Locations
🇫🇷

CHU de Nice, Nice, Alpes-Maritimes, France

🇮🇩

National Skin center - 1 Mandalay Rd, Bedok, Singapore, Indonesia

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