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The activity of each statin is dependent on the binding affinity of the compound for the substrate site and the length of time it binds to the site. [5] Type 2 statins have unique fluorophenyl group that causes additional polar interaction between the enzyme and the statins, which results in a tighter binding to the enzyme.
The best-selling statin is atorvastatin, also known as Lipitor, which in 2003 became the best-selling pharmaceutical in history. [12] The manufacturer Pfizer reported sales of US$12.4 billion in 2008. [13] Patient compliance with statin usage is problematic despite robust evidence of the benefits. [14] [15]
From 1996 to 2012, under the trade name Lipitor, atorvastatin became the world's best-selling medication of all time, with more than $125 billion in sales over approximately 14.5 years. [ 118 ] and $13 billion a year at its peak, [ 119 ] Lipitor alone "provided up to a quarter of Pfizer Inc.'s annual revenue for years."
Statins are linked to better health outcomes in older adults over the age of 70 with or without previous cardiovascular disease, a new study finds.
Clearance of a substance is sometimes expressed as the inverse of the time constant that describes its removal rate from the body divided by its volume of distribution (or total body water). In steady-state, it is defined as the mass generation rate of a substance (which equals the mass removal rate) divided by its concentration in the blood .
Lipid-lowering agents, also sometimes referred to as hypolipidemic agents, cholesterol-lowering drugs, or antihyperlipidemic agents are a diverse group of pharmaceuticals that are used to lower the level of lipids and lipoproteins, such as cholesterol, in the blood (hyperlipidemia).
Ezetimibe/atorvastatin (trade names Liptruzet, Atozet) is a cholesterol lowering combination drug. In the United States, it was approved in May 2013, by the Food and Drug Administration for the treatment of elevated low-density lipoprotein (LDL) in patients with primary or mixed hyperlipidemia as adjunctive therapy to diet. [ 1 ]
The strengths of the available cerivastatin medicine ranged from 0.2 - 0.8 mg, resulting in an actual dose of 1.9 - 13.1 μg/kg body weight for which rhabdomyolysis has been reported. [14] Although the mechanism of the cerivastatin induced myopathy is not exactly known, [ 15 ] the risk increases with statin dose.