Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Atorvastatin calcium trihydrate
Drug ID BADD_D00184
Description 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,[A181421] 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.[A181087, A181406] Atorvastatin and other statins including [lovastatin], [pravastatin], [rosuvastatin], [fluvastatin], and [simvastatin] are considered first-line treatment options for dyslipidemia.[A181087, A181406] 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.[A181084] An elevated cholesterol level (elevated low-density lipoprotein (LDL) levels in particular) is a significant risk factor for the development of CVD.[A181087,A181553] Several landmark studies demonstrate that the use of statins is associated with both a reduction in LDL levels and CVD risk.[A181090,A181093,A181096,A181427,A181475,A181538] 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.[A181087, A181406] 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.[A181397, A181403] Atorvastatin was first synthesized in 1985 by Dr. Bruce Roth and approved by the FDA in 1996.[T568] It is a pentasubstituted pyrrole [A177415] formed by two contrasting moieties with an achiral heterocyclic core unit and a 3,5-dihydroxypentanoyl side chain identical to its parent compound.[T571] Unlike other members of the statin group, atorvastatin is an active compound and therefore does not require activation.[A177436]
Indications and Usage May be used as primary prevention in individuals with multiple risk factors for coronary heart disease (CHD) and as secondary prevention in individuals with CHD to reduce the risk of myocardial infarction (MI), stroke, angina, and revascularization procedures. May be used to reduce the risk of cardiovascular events in patients with acute coronary syndrome (ACS). May be used in the treatment of primary hypercholesterolemia and mixed dyslipidemia, homozygous familial hypercholesterolemia, primary dysbetalipoproteinemia, and/or hypertriglyeridemia as an adjunct to dietary therapy to decrease serum total and low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (apoB), and triglyceride concentrations, while increasing high-density lipoprotein cholesterol (HDL-C) levels.
Marketing Status Prescription; Discontinued
ATC Code C10AA05
DrugBank ID DB01076
KEGG ID D02258
MeSH ID D000069059
PubChem ID 656846
TTD Drug ID D01QIN
NDC Product Code 64176-0043; 52562-005; 82608-000; 68554-0096; 55289-800; 68578-0010
Synonyms Atorvastatin | (3R,5R)-7-(2-(4-Fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-3,5-dihydroxyheptanoic acid | Atorvastatin Calcium | Atorvastatin, Calcium Salt | Liptonorm | Lipitor | Atorvastatin Calcium Hydrate | Atorvastatin Calcium Anhydrous | CI 981 | CI-981 | CI981 | Atorvastatin Calcium Trihydrate
Chemical Information
Molecular Formula C66H74CaF2N4O13
CAS Registry Number 134523-03-8
SMILES CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=CC=CC =C4.CC(C)C1=C(C(=C(N1CCC(CC(CC(=O)[O-])O)O)C2=CC=C(C=C2)F)C3=CC=CC=C3)C(=O)NC4=C C=CC=C4.O.O.O.[Ca+2]
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Acute myocardial infarctionStromelysin-1P08254T86702Not Available
Angina pectorisStromelysin-1P08254T86702Not Available
AngioplastyStromelysin-1P08254T86702Not Available
ArteriosclerosisLiver carboxylesterase 1P23141T76369Not Available
Cerebrovascular accidentStromelysin-1P08254T86702Not Available
DeathStromelysin-1P08254T86702Not Available
Myocardial ischaemiaApolipoprotein EP02649T21689Not Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal discomfort07.01.06.001--Not Available
Alanine aminotransferase increased13.03.01.003--
Amnesia19.20.01.001; 17.03.02.001--
Anaphylactic reaction24.06.03.006; 10.01.07.001--
Angioedema23.04.01.001; 10.01.05.009--Not Available
Arthralgia15.01.02.001--
Blood creatine phosphokinase increased13.04.01.001--
Cholestasis09.01.01.001--Not Available
Confusional state19.13.01.001; 17.02.03.005--
Death08.04.01.001--
Depression19.15.01.001--
Diarrhoea07.02.01.001--
Dizziness24.06.02.007; 17.02.05.003; 02.01.02.004--
Dyspepsia07.01.02.001--
Epistaxis24.07.01.005; 22.04.03.001--
Eructation07.01.02.003--
Erythema multiforme10.01.03.015; 23.03.01.003--
Fatigue08.01.01.002--
Flatulence07.01.04.002--
Hepatic failure09.01.03.002--
Hepatitis09.01.07.004--Not Available
Hyperglycaemia05.06.02.002; 14.06.02.002--
Insomnia19.02.01.002; 17.15.03.002--
Jaundice23.03.03.030; 09.01.01.004; 01.06.04.004--Not Available
Joint swelling15.01.02.004--Not Available
Laryngeal pain22.02.05.036--
Liver function test abnormal13.03.01.013--Not Available
Malaise08.01.01.003--
Memory impairment17.03.02.003; 19.20.01.003--
Muscle spasms15.05.03.004--
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