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Last Updated on January 15, 2019

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The active substance belongs to statins and Simvastatin is an important drug at elevated cholesterol levels. He was AMP in Germany MSD Sharp & 1990; Dohme brought to the market and is now included in many medications. He is generally well tolerated, a rare side effect of Simvastatin is muscle pain. Here you can read everything about Simvastatin, side effects and use.

How Simvastatin works

For the transport of fats in the blood, the body needs cholesterol, among other things. Approximately two-thirds of the required amount of cholesterol produced by the body forth in the liver itself, one third is obtained from food. Too high cholesterol may therefore on the one hand the natural production can be reduced, often it helps but even to convert the diet radically.

The production of cholesterol in the liver is a complex process, but effectively arises from activated acetic acid, a widely occurring cell material, many steps cholesterol while. An important and rate-limiting step in cholesterol biosynthesis, this depends on a specific enzyme called “HMG-CoA reductase” ab. Just this step inhibit statins such as Simvastatin – in this way the self-production is reduced and the cholesterol levels in the blood to fall (especially the “bad” LDL cholesterol, raise “good” HDL cholesterol is sometimes even)

Simvastatin is rapidly absorbed after oral administration and converted by the liver into the active form. The maximum Simvastatin effect occurs about one to two hours after ingestion. Because the body produces during the night most intensively cholesterol, Simvastatin is usually taken in the evening.

Eliminated is the Simvastatin metabolized mainly via the faeces, only a small part is in the urine.

When is Simvastatin used?

Simvastatin is mainly with elevated cholesterol levels (hypercholesterolemia) used in the blood. Should always be tried, the cholesterol levels to normalize non-drug, such as a healthy diet, exercise and weight loss before starting treatment.

Simvastatin 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) – regardless of the amount of cholesterol

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They are used in both cases usually the long term.

How Simvastatin is used

Taking Simvastatin takes place as a tablet usually once daily in the evening. The dosage is determined by the physician, but is usually between five to eighty milligrams.

Regular intake is important for the success of treatment, due to changes in cholesterol levels in the blood usually over a period of weeks. The patients “remember” the effect of cholesterol-lowering directly, although it can be measured in the blood. From unauthorized discontinuation of cholesterol-lowering agent, if any “effect” is noted, is not recommended.

Often Simvastatin is combined with other drugs, for example, with the anion exchanger cholestyramine – another cholesterol-lowering drug. It prevents the intestinal distributed in to aid digestion bile acids are absorbed back into the blood again. Thus, the liver is forced to make new bile acids from cholesterol – the cholesterol level falls

What are the side effects of Simvastatin?

Side effects may occur with Simvastatin therapy only rarely (in a thousand to ten thousand patients). These include:

  • anemia,
  • nausea, vomiting,
  • muscle weakness, pain, cramps (especially at high doses of Simvastatin)

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

What should be considered when taking Simvastatin?

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 Simvastatin. Is an application in lactation absolutely necessary should be discontinued prior to initiation of Simvastatin therapy.

Because Simvastatin is broken down, inter alia, by the enzyme cytochrome 3A4, lead inhibitors for this enzyme to elevated levels and thus increased Simvastatin side effects. Therefore, the following drugs should not be combined with Simvastatin:

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

Other drugs that should not be combined because of a possible increase in Simvastatin side effects are:

  • cyclosporine (in autoimmune diseases and organ transplant)
  • gemfibrozil and other fibrates (lipid-lowering)
  • Heart drugs and calcium channel blockers (Amiodarone, Verapamil, Diltiazem, Amlodipine)

During the Simvastatin therapy is also to refrain from grapefruit juice. Just one glass of grapefruit juice in the morning causes the following night twice the Simvastatin levels are measured than usual -. The possible consequences are unexpected side effects

How to obtain drugs with Simvastatin

Simvastatin is a prescription only available in pharmacies.

Since when Simvastatin 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 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. Both substances were Merck & amp from; Then placed Co. for approval.