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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

Overview

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.

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

Research Report

Published: May 1, 2025

Comprehensive Report: Atorvastatin

1. Atorvastatin: Overview and Identification

1.1 Introduction to Atorvastatin and Therapeutic Class

Atorvastatin is a widely prescribed synthetic lipid-lowering agent belonging to the statin class of medications.1 As a selective inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, atorvastatin plays a critical role in managing dyslipidemia and preventing cardiovascular disease (CVD).1 Its primary therapeutic action involves reducing elevated levels of total cholesterol (Total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (apo B), and triglycerides (TG) in the blood, while variably increasing high-density lipoprotein cholesterol (HDL-C) levels.1 By modifying these lipid parameters, particularly by lowering LDL-C (often termed "bad cholesterol"), atorvastatin significantly reduces the risk of major cardiovascular events such as myocardial infarction (MI) and stroke.1

The development and widespread adoption of statins, including atorvastatin, represent a major advancement in cardiovascular medicine. Elevated cholesterol levels, especially high LDL-C, are established risk factors for atherosclerosis and subsequent CVD.[1] Atorvastatin, along with other statins like simvastatin, pravastatin, rosuvastatin, and lovastatin, is considered a first-line treatment option for managing dyslipidemia and is integral to standard care protocols following cardiovascular events or for individuals at moderate to high risk of developing CVD.[1] The extensive clinical evidence supporting the efficacy of statins, combined with a generally favorable safety profile for most patients, has led to their extensive use globally.[1]

Continue reading the full research report

FDA Approved Products

ATORVASTATIN CALCIUM
Manufacturer:DirectRX
Route:ORAL
Strength:20 mg in 1 1
Approved: 2021/11/10
NDC:72189-291
ATORVASTATIN CALCIUM
Manufacturer:Marlex Pharmaceuticals Inc
Route:ORAL
Strength:10 mg in 1 1
Approved: 2018/09/12
NDC:10135-649
ATORVASTATIN CALCIUM
Manufacturer:Marlex Pharmaceuticals Inc
Route:ORAL
Strength:20 mg in 1 1
Approved: 2018/09/12
NDC:10135-650
ATORVASTATIN CALCIUM
Manufacturer:Marlex Pharmaceuticals Inc
Route:ORAL
Strength:80 mg in 1 1
Approved: 2018/09/12
NDC:10135-653
ATORVASTATIN CALCIUM
Manufacturer:Marlex Pharmaceuticals Inc
Route:ORAL
Strength:40 mg in 1 1
Approved: 2018/09/12
NDC:10135-651

Singapore Approved Products

BEATORVA 10 FILM COATED TABLET 10 MG
Manufacturer:ACTAVIS LTD
Form:TABLET, FILM COATED
Strength:10 mg
Online:Yes
Approved: 2017/11/16
Approval:SIN15363P
ATSWIFT 20 TABLET 20MG
Manufacturer:Ind-Swift Limited
Form:TABLET, FILM COATED
Strength:20mg
Online:Yes
Approved: 2014/12/12
Approval:SIN14695P
ATORVASTATIN SANDOZ FILM COATED TABLET 80MG
Manufacturer:Lek S.A.
Form:TABLET, FILM COATED
Strength:80.0mg
Online:Yes
Approved: 2022/06/28
Approval:SIN16524P
Tulip Film coated tablets 10mg
Manufacturer:Lek Pharmaceuticals d.d. (Ljubljana site), Lek d.d., PE PROIZVODNJA LENDAVA (Primary and secondary packager)
Form:TABLET, FILM COATED
Strength:10.000 mg
Online:Yes
Approved: 2012/10/18
Approval:SIN14252P
DUALPRESS FILM-COATED TABLET 5MG/10MG
Manufacturer:2nd Plant, Standard Chem. & Pharm. Co. Ltd.
Form:TABLET, FILM COATED
Strength:10mg
Online:Yes
Approved: 2022/05/11
Approval:SIN16490P

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