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Atorvastatin

The active ingredient Atorvastatin is one of the so-called statins – a drug group that is used for lowering elevated cholesterol levels. Too much cholesterol in the blood promotes the hardening of the arteries (atherosclerosis), which, inter alia, coronary heart disease (CHD) and stroke can result. Here you can read everything about the cholesterol-lowering drug Atorvastatin, side effects and use.

How acts Atorvastatin

Cholesterol is a vital substance that the body needs, among other things for the construction of the cell membranes and the formation of hormones and bile acids (for fat digestion). Approximately two-thirds of the required amount of cholesterol produced by the body itself forth in the liver itself. One third is obtained from food. To reduce elevated cholesterol levels, one can thus on the one hand reduce the body’s production drugs and on the other hand change unfavorable eating habits.

Atorvastatin reduced the cholesterol production in the liver. This is a complex process that involves many steps. An important and rate-limiting step in cholesterol biosynthesis is dependent on a specific enzyme called HMG-CoA reductase. Just this step inhibit statins such as Atorvastatin – in this way the House Production is reduced and decrease the cholesterol levels in the blood, notably that of the “bad” LDL cholesterol, which can lead to hardening of the arteries. The blood levels of “good” (vessel protective) HDL cholesterol on the other hand increase sometimes even.

absorption and excretion of Atorvastatin

Atorvastatin is rapidly absorbed into the body after ingestion by mouth (oral ingestion). It does not like other statins first in the liver to the active form is converted, but can be equal to exert its effect. The maximum effect is achieved about Atorvastatin one to two hours after ingestion. Because the body produces during the night most intensively cholesterol, Atorvastatin is usually taken in the evening.

Eliminated is the Atorvastatin metabolized mainly via the faeces.

When used Atorvastatin?

Atorvastatin is primarily used to treat elevated blood cholesterol levels (hypercholesterolemia). In general: A cholesterol-lowering drugs like Atorvastatin therapy should be initiated only when non-pharmacological measures for lowering cholesterol (healthy eating, sports and weight loss) have failed. Atorvastatin is also approved for prevention (prevention) of cardiovascular complications in patients with coronary heart disease (CHD) or an increased risk of cardiovascular disease (such as diabetes patients) -. Regardless of the amount of cholesterol

They are used in both cases, usually long term, to keep the cholesterol levels permanently to normal levels.

How is Atorvastatin applied

The intake of Atorvastatin carried out as a tablet usually once daily in the evening. The dosage is determined by the physician, but is usually between ten to eighty milligrams.

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The regular intake of cholesterol-lowering is important for the success of treatment, due to changes in cholesterol levels in the blood usually over a period of several weeks. The patients “remember” the effect of cholesterol-lowering directly, although it can be measured in the blood. From the unauthorized withdrawal of the cholesterol-lowering drug, because no “effect” is noted, is not recommended.

If necessary, Atorvastatin is combined with other drugs, for example, with the anion exchanger cholestyramine, another cholesterol-lowering drug. It prevents the undistributed in the gut to aid digestion bile acids are absorbed back into the blood again. As a result, the liver is forced to make new bile acids from cholesterol, whereby cholesterol decreases further.

What are the side effects of Atorvastatin?

Common side effects with Atorvastatin therapy (with one to ten of a hundred patients) include:

  • nausea, bloating
  • changed liver enzyme levels
  • muscle weakness, pain, cramps (especially in high doses)

and complaints under Atorvastatin therapy are serious side effects and should be discussed with the treating physician immediately.

What should be considered when taking Atorvastatin?

The treatment of children and adolescents (10 to 17 years) is only in special cases and subject to certain limitations abzuklärenden by the doctor. The use in children under ten years has not been studied.

pregnant and nursing mothers should not take Atorvastatin. Is an application in lactation absolutely necessary should be discontinued prior to initiation of Atorvastatin therapy.

Since Atorvastatin is broken down, inter alia, by the enzyme cytochrome 3A4, lead inhibitors for this enzyme to elevated levels and thus increased Atorvastatin side effects. The following Arzenistoffe should therefore not be combined with Atorvastatin:

  • Certain antibiotics: Erythromycin, Clarithromycin, fusidic
  • Certain antifungal (antifungal): ketoconazole, itraconazole, Fluconazole
  • HIV protease inhibitors (nelfinavir)

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

  • cyclosporine (in autoimmune diseases and organ transplant)
  • gemfibrozil and other fibrates (lipid-lowering drugs – reduce blood levels of cholesterol and other blood lipids)
  • Heart drugs and calcium channel blockers (Amiodarone, Verapamil, Diltiazem, Amlodipine)

During the Atorvastatin therapy should also be dispensed with grapefruit (juice, fruits). Already a glass of grapefruit juice in the morning causes the following night twice as high Atorvastatin levels are measured than usual -. The possible consequences are unexpected side effects

How to obtain medications with Atorvastatin

Atorvastatin is only available in pharmacies after a prescription, so it is only available on prescription.

Since when Atorvastatin is known?

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

1979 isolated scientists from Merck & amp; Co. (now MSD Sharp & Dohme) lovastatin from a fungus. During the investigation, also synthetically modified variants of lovastatin have been developed wherein the compound MK-733 (later Simvastatin) as therapeutically effective proved the starting material. For, a so-called type 1 statin, were later the newer Type 2 statins such as Atorvastatin (1985) develops, which affects two to three times stronger. It was approved in 1996 in the US and in Germany in 1997. on the market. Since the patent outlet 2011 numerous imitators preparations (generics as Atorvastatin ratiopharm, Atorvastatin CT) have been developed whereby the Atorvastatin price has fallen sharply.