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Atorvastatin

This is how atorvastatin works

Cholesterol is an essential substance that the body needs, among other things, to build cell membranes and to form hormones and bile acids (for fat digestion). The body itself produces around two thirds of the required amount of cholesterol in the liver. A third is obtained from food. In order to lower high cholesterol levels, one can reduce the body's own production with medication on the one hand and change unfavorable eating habits on the other.

Atorvastatin decreases the production of cholesterol in the liver. This is a complex process that involves many steps. An important and rate-limiting step in cholesterol biosynthesis depends on a specific enzyme called HMG-CoA reductase. Statins such as atorvastatin inhibit precisely this step - this reduces self-production and lowers the cholesterol levels in the blood, especially those of the "bad" LDL cholesterol, which can lead to hardening of the arteries. The blood values ​​of the "good" (vascular protecting) HDL cholesterol, on the other hand, sometimes even increase.

Atorvastatin uptake and excretion

Atorvastatin is quickly absorbed into the body after it has been taken by mouth (orally). Unlike other statins, it does not first have to be converted into the active form in the liver, but can take effect immediately. Atorvastatin reaches its maximum effect about one to two hours after ingestion. Since the body produces cholesterol most intensively during the night, atorvastatin is usually taken in the evening.

The metabolized atorvastatin is mainly excreted in the stool.

When is atorvastatin used?

Atorvastatin is mainly used to treat high levels of cholesterol in the blood (hypercholesterolaemia). In general, the following applies: therapy with cholesterol-lowering drugs such as atorvastatin should only be started if non-drug measures to lower cholesterol (healthy diet, exercise and weight loss) have not been successful. Atorvastatin is also approved for the prevention (prevention) of cardiovascular complications in patients with coronary artery disease (CHD) or an increased risk of cardiovascular disease (such as diabetes patients) - regardless of the level of cholesterol.

In both cases, the application is usually long-term in order to keep the cholesterol level permanently at normal values.

This is how atorvastatin is used

Atorvastatin is usually taken as a tablet once a day in the evening. The individual dose is determined by the doctor, but is usually between ten to eighty milligrams.

Regular intake of the cholesterol-lowering drug is important for the success of the treatment, as the cholesterol levels in the blood usually change over a period of several weeks. The patients do not "notice" the effect of the cholesterol lowering agent directly, although it can be measured in the blood. Unauthorized discontinuation of the cholesterol lowering drug because no "effect" is noticed is expressly discouraged.

If necessary, atorvastatin is combined with other drugs, for example with the anion exchanger colestyramine, also a cholesterol-lowering drug. It prevents the bile acids released in the intestines to aid digestion from being reabsorbed into the blood. This forces the liver to make new bile acids from cholesterol, which further lowers the cholesterol level.

What are the side effects of atorvastatin?

Common side effects with atorvastatin therapy (affecting 1 to 10 patients in 100) include:

Muscle pain and discomfort during atorvastatin therapy are serious side effects and should be discussed with the attending physician immediately.

What should be considered when taking atorvastatin?

The treatment of children and adolescents (10 to 17 years) is only carried out in special cases and is subject to certain restrictions to be clarified by the doctor. Use in children under ten years of age has not been studied.

Pregnant and breastfeeding women should not take atorvastatin. If use during breastfeeding is absolutely necessary, breastfeeding should be discontinued before starting atorvastatin therapy.

Since atorvastatin is broken down, among other things, by the enzyme cytochrome 3A4, inhibitors of this enzyme lead to increased levels and thus increased atorvastatin side effects. The following medicinal substances should therefore not be combined with atorvastatin:

Other drugs that should not be combined with the cholesterol lowering drug because of a possible increase in atorvastatin side effects are:

  • Gemfibrozil and other fibrates (lipid-lowering drugs - lower blood levels of cholesterol and other blood fats)

Grapefruit (juice, fruits) should also be avoided during atorvastatin therapy. Even a glass of grapefruit juice in the morning causes twice as high atorvastatin levels to be measured the following night as usual - the possible consequence is unexpected side effects.

How to get medication with atorvastatin

Atorvastatin is only available in pharmacies upon presentation of a doctor's prescription, so it requires a prescription.

How long has atorvastatin been known?

After the biosynthesis of cholesterol was elucidated in the early 1950s, it quickly became apparent that by inhibiting important key enzymes, one could produce effective drugs against high cholesterol levels. A first inhibitor called mevastatin was isolated from a fungus in Japan in 1976, specifically against the enzyme HMG-CoA reductase. However, this was never brought to market.

In 1979, Merck & Co. (now MSD Sharp & Dohme) scientists isolated lovastatin from a fungus. During the investigation, synthetically modified variants of lovastatin were also developed, whereby the compound MK-733 (later simvastatin) proved to be therapeutically more effective than the starting material. Simvastatin, a so-called type 1 statin, was later used to develop the newer type 2 statins such as atorvastatin (1985), which is two to three times more effective. It was approved in the USA in 1996 and launched in Germany in 1997. Since the patent expired in 2011, numerous copycat products (generics such as Atorvastatin-ratiopharm®, Atorvastatin-CT) have been developed, which has resulted in a sharp drop in the price of atorvastatin.

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