Statins

Extracted Attributes

• Drug Class

  HMG-CoA reductase inhibitors

• US Sales (2005)

  $19 billion

• US Sales (2024)

  $5-6 billion (estimated)

• Scientific Field

  Pharmacology, Cardiology

• Contraindications

  Pregnancy, liver disease

• Common Side Effects

  Muscle pain (myalgia), increased risk of diabetes, abnormal liver enzyme levels

• Mechanism of Action

  Competitive inhibition of HMG-CoA reductase in the mevalonate pathway

• Primary Application

  Lowering LDL cholesterol and prevention of cardiovascular disease

• Average LDL Reduction

  1.8 mmol/L (70 mg/dL)

• Stroke Risk Reduction

  17% decrease

• Severe Adverse Effects

  Muscle damage, rhabdomyolysis (rare)

• Cardiac Event Reduction

  60% decrease

Timeline

• Atorvastatin (Lipitor) becomes the best-selling pharmaceutical in history. (Source: Wikipedia)

  2003-01-01

• Annual US sales for the statin class reach a peak of approximately $19 billion. (Source: Wikipedia)

  2005-12-31

• Atorvastatin annual sales reach $12 billion. (Source: Wikipedia)

  2008-12-31

• NHS completes a formal review of statin medicinal guidance. (Source: NHS)

  2022-10-03

• Estimated US sales for statins projected at $5-6 billion, reflecting the impact of generic availability. (Source: Wikipedia)

  2024-01-01

• Scheduled next review date for NHS statin clinical guidelines. (Source: NHS)

  2025-10-03

Statin

Statins (or HMG-CoA reductase inhibitors) are a class of medications that lower cholesterol. They are prescribed typically to people who are at high risk of cardiovascular disease. Low-density lipoprotein (LDL) carriers of cholesterol play a key role in the development of atherosclerosis and coronary heart disease via the mechanisms described by the lipid hypothesis. As lipid-lowering medications, statins are effective in lowering LDL cholesterol; they are widely used for primary prevention in people at high risk of cardiovascular disease, as well as in secondary prevention for those who have developed cardiovascular disease. Side effects of statins include muscle pain, increased risk of diabetes, and abnormal blood levels of certain liver enzymes. Additionally, they have rare but severe adverse effects, particularly muscle damage, and very rarely rhabdomyolysis. They act by inhibiting the enzyme HMG-CoA reductase, which plays a central role in the production of cholesterol. High cholesterol levels have been associated with cardiovascular disease. There are various forms of statins, some of which include atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin. Combination preparations of a statin and another agent, such as ezetimibe/simvastatin, are also available. The class is on the World Health Organization's List of Essential Medicines with simvastatin being the listed medicine. In 2024, US sales were estimated at $5-6B, down from $19B in 2005. The best-selling statin is atorvastatin, also known as Lipitor, which in 2003 became the best-selling pharmaceutical in history at $12B in 2008. Patient compliance with statin usage is problematic despite robust evidence of its benefits.

Web Search Results

• Statin - Wikipedia

  Statins, by inhibiting the HMG CoA reductase pathway, inhibit downstream synthesis of isoprenoids, such as farnesyl pyrophosphate and geranylgeranyl pyrophosphate. Inhibition of protein prenylation for proteins such as RhoA (and subsequent inhibition of Rho-associated protein kinase) may be involved, at least partially, in the improvement of endothelial function, modulation of immune function, and other pleiotropic cardiovascular benefits of statins, as well as in the fact that a number of other drugs that lower LDL have not shown the same cardiovascular risk benefits in studies as statins, and may also account for some of the benefits seen in cancer reduction with statins. In addition, the inhibitory effect on protein prenylation may also be involved in a number of unwanted side effects [...] Statins are effective in decreasing mortality in people with pre-existing cardiovascular disease. Pre-existing disease can have many manifestations. Defining illnesses include a prior heart attack, stroke, stable or unstable angina, aortic aneurysm, or other arterial ischemic disease, in the presence of atherosclerosis. They are also advocated for use in people at high risk of developing coronary heart disease. On average, statins can lower LDL cholesterol by 1.8 mmol/L (70 mg/dL), which translates into an estimated 60% decrease in the number of cardiac events (heart attack, sudden cardiac death) and a 17% reduced risk of stroke after long-term treatment. A greater benefit is observed with high-intensity statin therapy. They have less effect than the fibrates or niacin "Niacin [...] ## Mechanism of action [edit] Main article: Cholesterol § Homeostasis Statins act by competitively inhibiting HMG-CoA reductase, the rate-limiting enzyme of the mevalonate pathway. Because statins are similar in structure to HMG-CoA on a molecular level, they will fit into the enzyme's active site and compete with the native substrate (HMG-CoA). This competition reduces the rate by which HMG-CoA reductase is able to produce mevalonate, the next molecule in the cascade that eventually produces cholesterol. A variety of natural statins are produced by Penicillium and Aspergillus fungi as secondary metabolites. These natural statins probably function to inhibit HMG-CoA reductase enzymes in bacteria and fungi that compete with the producer. ### Inhibiting cholesterol synthesis [edit]

• Statins - NHS

  # Overview - Statins Statins are a group of medicines that can help lower the level of low-density lipoprotein (LDL) cholesterol in the blood. LDL cholesterol is often referred to as "bad cholesterol", and statins reduce the production of it inside the liver. ## Why have I been offered statins? Having a high level of LDL cholesterol is potentially dangerous, as it can lead to a hardening and narrowing of the arteries (atherosclerosis) and cardiovascular disease (CVD). CVD is a general term that describes a disease of the heart or blood vessels. It's a very common cause of death in the UK. The main types of CVD are: [...] Statins come as tablets that are taken once a day. Your dose will depend on why you need the medicine, your cholesterol levels, and other medicines you're taking. Your GP may increase your statins to the maximum dose. This helps to manage your cholesterol levels and prevent cardiovascular disease. For some types of statin it does not matter what time of day you take it, as long as you stick to the same time. Some types of statin should be taken in the evening. Check with your doctor whether there's a particular time of day you should take your statin. You usually have to continue taking statins for life because if you stop taking them, your cholesterol will return to a high level. [...] eating ahealthy, balanced diet exercising regularly maintaining a healthy weight limiting the amount of alcohol you drink stopping smoking Statins may be recommended if these measures do not help. Read more about treating high cholesterol and preventing CVD. ## Types of statin There are 5 types of statin available on prescription in the UK: atorvastatin (Lipitor) fluvastatin (Lescol) pravastatin (Lipostat) rosuvastatin (Crestor) simvastatin (Zocor) Most people start with atorvastatin. Not all statins are suitable for everyone, so you may need to try different types until you find one that's suitable. Page last reviewed: 03 October 2022 Next review due: 03 October 2025

• Statins: Types, uses, side effects, and alternatives - Harvard Health

  ## What are statins? Statins are prescription drugs you take as pills to lower cholesterol. Cholesterol is an essential component of cell membranes. However, when you have too much, it can build up inside the walls of your arteries. This is called plaque. Cholesterol-laden plaque contributes to heart disease in different ways. A buildup of cholesterol can make your arteries narrow and even block them. If a cholesterol plaque ruptures, a blood clot forms there and this can lead to a heart attack or stroke. Cholesterol also provokes inflammation in the arteries, which can contribute to the formation of artery-blocking clots. [...] People who are pregnant or who have liver disease should not take statins. ### What types of statins are available? Eight statins are approved by the U.S. Food and Drug Administration (FDA): atorvastatin (Lipitor) fluvastatin (Lescol) lovastatin (Mevacor) lovatstatin extended release (Altoprev) pitavastatin (Livalo) pravastatin (Pravachol) rosuvastatin (Crestor) simvastatin (Zocor). Your doctor picks which statin may work best for you by considering a few things. They include how much you need to lower your LDL by, and other medicines you are taking. Sometimes people will have a side effect with one statin but are able to tolerate another one. ## What are possible side effects of statins? [...] Sometimes, just changing what you eat and being more active can lower cholesterol. But if your cholesterol stays high, you may need a statin or other cholesterol-lowering medication. ### How do statins work? Statins interfere with how your liver makes cholesterol; most importantly, LDL, the "bad" kind. Triglycerides are a second kind of cholesterol that can contribute to plaque buildup. HDL has traditionally been referred to as the "good" cholesterol because it helps your body get rid of LDL. However, changing HDL has not been seen to reduce the risk of heart disease, so this is no longer a focus of cholesterol management. Statins work to lower LDL levels. This slows the buildup of cholesterol in your arteries.

• Understanding statins: benefits & risks | UnitedHealthcare

  # What to know about statins Statins are prescription drugs that can help lower low-density lipoprotein (LDL) – otherwise known as “the bad cholesterol.” Cholesterol is a substance found in your blood. While our bodies need cholesterol to build healthy cells, high levels can increase your risk of heart disease. Statin drugs lower the amount of LDL in the liver. This may lower the risk of heart disease and stroke. Like with any medication, there are benefits and side effects to consider when taking statins.1 ## What are statins?

• Statins - MedlinePlus

  Cholesterol is made by your liver. It travels through the blood on proteins called lipoproteins. One type of lipoprotein, LDL, is sometimes called the "bad" cholesterol. A high LDL level leads to a buildup of cholesterol in your arteries. Another type, HDL, is sometimes called the "good" cholesterol. It carries cholesterol from other parts of your body back to your liver. Then your liver removes the cholesterol from your body. ### What are statins? Statins are a type of cholesterol medicine. Your health care provider may prescribe them if you have high cholesterol and making lifestyle changes does not lower your cholesterol enough. Statins are the most common medicines used to treat high cholesterol. ### How do statins lower cholesterol?