Atorvastatin, also known as the brand name product Lipitor, is a lipid-lowering drug belonging to 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 of statin medications is considered a standard practice following any cardiovascular events and for people with a moderate to high risk of development of the cardiovascular disease, such as those with Type 2 Diabetes. The clear evidence of the benefit of statin use, coupled with minimal side effects or beneficial long term effects, has resulted in this drug class becoming one of the most widely prescribed medications in North America.
Atorvastatin and other drugs from the statin drug class of medications including lovastatin, pravastatin, rosuvastatin, fluvastatin, and simvastatin are considered first-line treatment options for dyslipidemia. The increasing use of the statin class of drugs is largely due to cardiovascular diseases (CVD) (such as heart attack, atherosclerosis, angina, peripheral artery disease, and stroke) becoming a leading cause of death in many countries and a major cause of morbidities. An elevated cholesterol level (elevated low-density lipoprotein (LDL) levels in particular) is an important risk factor for the development of CVD. Several landmark studies showed a reduction in LDL levels and the risk of CVD development associated with the use of statins.Stains 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) statins cause a 20%-22% relative reduction 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.