How atorvastatin works
Atorvastatin is a representative of the statins – a group of active ingredients that can lower high cholesterol levels.
Cholesterol is a vital substance that the body needs, among other things, to build cell membranes and to form hormones and bile acids (for fat digestion). The body produces around two thirds of the required amount of cholesterol itself in the liver. The remaining third is obtained from food.
In order to lower high cholesterol levels, it is therefore possible to reduce the body’s own production with medication on the one hand and to change unfavorable eating habits on the other.
Atorvastatin reduces the body’s own cholesterol production: this is a complex process that involves many steps. One important and rate-determining step depends on a specific enzyme called HMG-CoA reductase. This enzyme is inhibited by statins such as atorvastatin. This reduces its own production and lowers the cholesterol levels in the blood.
This mainly affects the blood levels of “bad” LDL cholesterol (LDL = low-density lipoprotein), which can lead to arteriosclerosis. The blood levels of the “good” (vascular-protecting) HDL cholesterol (HDL = high-density lipoprotein), on the other hand, sometimes even increase.
Absorption, breakdown and excretion
Atorvastatin is quickly absorbed into the body after being taken by mouth (oral intake). Unlike other statins, it does not have to be converted into the active form in the liver first, but can take effect immediately.
The maximum effect is achieved approximately one to two hours after ingestion. As the body forms cholesterol most intensively during the night, atorvastatin is usually taken in the evening.
Due to its long duration of action, once daily administration is sufficient. Atorvastatin, which is metabolized in the liver, is mainly excreted in the stool.
When is atorvastatin used?
Atorvastatin is mainly used to treat elevated cholesterol levels in the blood (hypercholesterolemia). In general, cholesterol-lowering drugs such as atorvastatin are only prescribed when non-drug measures to lower cholesterol (healthy diet, exercise and weight loss) have been unsuccessful.
Atorvastatin is also approved for the prevention of cardiovascular complications in patients with coronary heart disease (CHD) or an increased risk of cardiovascular disease (such as diabetes patients). This application is independent of the level of cholesterol.
How atorvastatin is used
Atorvastatin is usually taken as a tablet once a day in the evening. The dose is determined individually by the treating doctor, but is usually between ten and eighty milligrams.
Regular intake is important for the success of the treatment, as the cholesterol levels in the blood usually change over a period of several weeks. Patients do not “notice” the effect of the cholesterol-lowering drug directly, although it can be measured in the blood and is reflected in a reduced incidence of heart attacks and strokes.
Do not stop taking atorvastatin on your own just because you notice “no effect”.
If necessary, atorvastatin can be combined with other medications, for example colestyramine or ezetimibe (both of which also lower cholesterol levels).
What are the side effects of atorvastatin?
Common side effects (i.e. in one to ten out of one hundred patients) of atorvastatin therapy are
- headaches
- Gastrointestinal disorders (such as constipation, flatulence, nausea, diarrhea)
- Altered liver enzyme values
- muscle pain
Notify your doctor if you experience muscle pain and discomfort during atorvastatin therapy.
What should I bear in mind when taking atorvastatin?
Contraindications
Atorvastatin must not be taken if:
- severe liver dysfunction
- concomitant treatment with certain drugs for hepatitis C therapy (glecaprevir and pibrentasvir)
Interactions
Since atorvastatin is broken down by the enzyme cytochrome 3A4 (CYP3A4), among others, inhibitors of this enzyme lead to increased levels and thus increased atorvastatin side effects. Such CYP3A4 inhibitors should therefore not be combined with atorvastatin:
- certain antibiotics: Erythromycin, clarithromycin, fusidic acid
- HIV protease inhibitors (e.g. indinavir, ritonavir, nelfinavir)
- certain antifungals: ketoconazole, itraconazole, voriconazole
- certain heart medications: verapamil, amiodarone
Other drugs that should not be combined with the cholesterol-lowering drug due to a possible increase in atorvastatin side effects are
- Gemfibrozil (lipid-lowering drug from the fibrate group)
Grapefruit (juice, fruit) – also a CYP3A4 inhibitor – should also be avoided during atorvastatin therapy. Just one glass of grapefruit juice in the morning causes atorvastatin levels to be twice as high as usual the following night. This may result in unexpected side effects.
Age restriction
The treatment of children and adolescents is only carried out in special cases and is subject to certain restrictions to be clarified by the doctor. In principle, atorvastatin is approved for the treatment of hypercholesterolemia from the age of ten.
Pregnancy and breastfeeding
Pregnant women and breastfeeding mothers must not take atorvastatin. If use during breastfeeding is absolutely necessary, breastfeeding should be stopped before starting atorvastatin therapy.
How to obtain medication with atorvastatin
Atorvastatin is available on prescription in Germany, Austria and Switzerland and can be obtained from pharmacies on presentation of a doctor’s prescription.
How long has Atorvastatin been known?
After the biosynthesis of cholesterol was elucidated in the early 1950s, it quickly became apparent that effective drugs against high cholesterol levels could be produced by inhibiting important key enzymes.
The first inhibitor of the enzyme HMG-CoA reductase, mevastatin, was isolated from a fungus in Japan in 1976. However, this was never brought to market maturity.
In 1979, scientists isolated lovastatin from a mushroom. During the investigation, synthetically modified variants of lovastatin were also developed, with the compound MK-733 (later simvastatin) proving to be therapeutically more effective than the original substance.
Since the patent expired in 2011, numerous generic drugs have been developed, as a result of which the price of atorvastatin has fallen sharply.
