Anti cholesterol drug: statins, when, dangerous?

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Anti cholesterol drug: statins, when, dangerous?

Anti-cholesterol drugs (or hypolipidemics) help to lower the level of cholesterol in the blood or reduce its intestinal absorption. Statins are today the most widely used anti-cholesterol drugs (Tahor, Crestor, etc.).

What is an anti cholesterol drug?

Anti-cholesterol (or lipid-lowering) drugs contribute to decrease the level of cholesterol in the blood or reduce its intestinal absorption. Some may also lower blood triglyceride levels. Cholesterol is a lipid (fatty substance) naturally produced by the body, but which is also found in food. Although this element is essential for the production of hormones and the structure of cells, an excess of cholesterol, on the other hand, can have harmful consequences for health. In case of high cholesterol, the arteries lose their elasticity, clog, and diseases of the heart and blood vessels can occur. There are two forms of cholesterol, LDL and HDL. The good cholesterol (HDL) helps eliminate the bad cholesterol (LDL). There are several types of lipid-lowering drugs : them statins (lower the level of LDL-cholesterol in the blood and slightly increase HDL), fibrates (lower the blood level of LDL-cholesterol, triglycerides and uric acid), ezetimibe (prevents the intestinal absorption of cholesterol and can be taken alone or in combination with another drug), anti-PCSK9 monoclonal antibodies (increase the cholesterol entering the liver, and thus decrease the blood level, the latter being generally prescribed in addition to another anti-cholesterol treatment), lomitapide (reduces cholesterol and triglyceride levels in the blood, indicated in combination with other hypolipidemic agents in the event of homozygous familial hypercholesterolemia), colestyramine (resin which decreases the intestinal absorption of cholesterol and increases its elimination) or even omega-3s (prevent the formation of LDL-cholesterol). Finally, there are also food supplements (which are not drugs) intended to fight against bad cholesterol and stimulate the production of HDL-cholesterol, such as omega-3 and red yeast rice.

When should I take cholesterol-lowering medication?

An anti-cholesterol drug will be prescribed by the doctor if, after several months of lifestyle and dietary measures, the level of cholesterol in the blood remains too high (hypercholesterolemia). A suitable diet and the practice of physical exercise must be maintained assiduously during treatment. Anti-cholesterol drugs may also be indicated in prevention of cardiovascular disease in people at risk, or in case of high blood triglyceride levels. Most often in combination, some may be indicated in case of particular genetic pathology (familial hypercholesterolemia) or even during proven cardiovascular disease. Anti-cholesterol drugs are usually taken once a day, except colestyramine and omega-3 which are usually taken 2 to 3 times a day. Monoclonal antibodies are administered by injection once or twice a month.

Cholesterol medication with or without statins

The most common regimen in the treatment of hypercholesterolemia is start a statin first-line. Statins are the most commonly used anti-cholesterol drugs today and are among the most recent treatments for the management of hypercholesterolemia. These are drugs that have proven themselves and are generally well tolerated. They effectively reduce cardiovascular morbidity and mortalitys. However, it is possible to use other drugs, especially when statins are poorly tolerated or insufficient to lower cholesterol levels. In this case, they can be combined or replaced by ezetimibe or fibrates, which are therefore most often second-line drugs. There are also other anti-cholesterol treatments which are indicated alone or in combination with statins or fibrates, and which are prescribed when certain medical situations justify it.

Examples: what are the main anti-cholesterol drugs in France?

The anti-cholesterol drugs currently marketed in France are as follows:

  • Statins : atorvastatin (Tahor®), rosuvastatin (Crestor®), simvastatin (Zocor®), pravastatin (Vasten®), fluvastatin (Lescol®) and pitavastatin (Lippiza®, Trolise®)
  • Fibrates : fenofibrate (Lipanthyl®, Fegenor®), ciprofibrate (Lipanor®), bezafibrate (Befizal®), gemfibrozil (Lipur®)
  • Ezetimibe : Ezetrol® (alone), Liptruzet® and Reselip® (in combination with atorvastatin), Liporosa®, Suvreza® and Twicor® (in combination with rosuvastatin), Inegy® (in combination with simvastatin) and their generics
  • Colestyramine (Questran®)
  • Monoclonal antibodies : evolocumab (Repatha®) and alirocumab (Praluent®)
  • lomitapide (Lojuxta®)
  • Omega-3 triglycerides (Omacor®, Ethyl esters of omega 3 acids EG Labo conseil®)

What are the side effects of cholesterol lowering drugs?

The main side effects of anti-cholesterol drugs are digestive (most frequent symptoms), muscular, hepatic and cutaneous. Of the dizziness or fatigue can also occur. Allergic reactions are possible, although rarer. The gastrointestinal effects observed are generally benign and transient. It can be constipation, nausea, abdominal pain, diarrhea, flatulence or heartburn. The muscle disorders that may occur are in some cases mild, but may also be evidence of drug toxicity and thus require discontinuation of treatment. They can manifest as myalgia, muscle fatigue, crampsand more rarely, but with potentially serious consequences, rhabdomyolysis (damage to muscle cells and presence of myoglobin in the urine, which can lead to kidney failure). Listed liver diseases may be accompanied by elevated transaminases, transient and moderate effect, more rarely significant but which can lead to hepatitis. There are also risk of pancreatitis, particularly with fibrates. The skin reactions observed are eruptions, rashes, itching, hives or photosensitization. A few isolated cases of neuropathy (peripheral nerve damage) and joint pain, reversible on stopping treatment, have been observed with statins. Of the nosebleeds, headaches, low blood pressure, taste disturbances, gout, high blood sugar and gastrointestinal bleeding may possibly occur with taking Omacor®.

What are the contraindications of anti-cholesterol drugs?

The common contraindication to all anti-cholesterol drugs is hypersensitivity to the drug substance or excipient. In addition, anti-cholesterol treatments are generally contraindicated in case of muscular, renal, hepatic or biliary damage. Indeed, concerning statins and ezetimibe, these drugs are contraindicated in case of myopathies (muscle disorders) and active liver disease (or with prolonged elevated hepatic transaminases). Pravastatin is also contraindicated in severe kidney failure. Fibrates are contraindicated in case liver failure and kidney failure. Colestyramine, fenofibrate and gembibrozil are also contraindicated in case of gallbladder disease, pancreatitis, or severe liver failure.

Blood tests must therefore be carried out regularly before and during treatment.

Blood tests must therefore be carried out regularly before and during anti-cholesterol treatment, with increased monitoring of liver enzymes. Also, any unexplained muscle pain should be reported to the doctor. Certain anti-cholesterol drugs are contraindicated during pregnancy and lactation. Colestyramine is contraindicated in case of phenylketonuria due to the presence of aspartame. Fibrates are contraindicated in case of sun allergy or phototoxicity. Finally, some other drugs are not compatible with taking anti-cholesterol treatment. The risk of drug interactions must be ruled out before taking an anti-cholesterol drug, such as statins and fibrates in particular, with the taking of an anticoagulant. Similarly, vigilance is required when taking a statin with grapefruit juice or other drugs that inhibit CYP3A4, likely to increase its toxicity. The combination of a fibrate and a statin (or two fibrates) is potentially dangerous, in particular being able to cause rhabdomyolysis (muscle toxicity). Similarly, in certain cases such as liver damage or pregnancy, the combination of ezetimibe with a statin is also contraindicated.

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