Simvastatin

Definition / active ingredient

The active ingredient simvastatin (Simvahexal® from Hexal) is a drug used to lower blood lipid levels.

It belongs to the group of so-called HMG-CoA reductase inhibitors (is pronouncedly called hydroxy-methylglutaryl-coenzyme A reductase inhibitor).
This enzyme plays a crucial role in the body's fat metabolism, because it is absolutely necessary for the formation of new cholesterol.
By inhibiting it, one can influence the fat levels in the blood.

Statins are therefore used to permanently lower high cholesterol levels.
Above all, the LDL cholesterol, the so-called bad cholesterol, is lowered.

In addition, they are used when fat levels are normal to prevent cardiovascular diseases.

Application / dosage form / dosage

If non-pharmacological measures such as diet and increased physical activity alone are not sufficient to lower an elevated cholesterol level in the patient, the additional intake of simvastatin makes sense.

Simvastatin (Simvahexal®) is available in tablet form and should be swallowed whole with as much liquid as possible in the evening, as the body's own cholesterol is formed in the evening in particular.

The tablet can be taken on an empty stomach or with a meal.

The dosage of simvastatin is sufficient from 5 milligrams up to 80 milligrams maximum dose per day and will once a day taken.
The level of dosage depends on the type of disease (hypercholesterolemia, Prevention or Familial Hypercholesterolemia) and the level of cholesterol / fat in the blood.

If a dose increase is necessary, this should be done at intervals of at least 4 weeks take place and not earlier.

If you should forget to take a tablet in the evening, continue with the usual dose the next day.
The additional intake of simvastatin (Simvahexal®) Tablets must be avoided at all costs.

The active ingredient simvastatin is also in the drug Zocor® contain.

Mechanism of action

Simvastatin will whole taken and the active ingredient is well absorbed by the intestinal mucosa.

The active ingredient as it is in the tablet represents a inactive form The first step in the body must therefore be the inactive one active form to produce the desired effect in the body for which it is intended, namely to lower blood lipid levels.
This activation takes place in the cells of the liver instead of.

Simvastatin (Simvahexal®) here on a very specific fat level in the blood, namely on the so-called LDL cholesterol.
LDL means "low density lipoprotein“And has something to do with the density of the fabric.

In addition to the LDL, there is also one HDL cholesterol (high for high density) and a VLDL cholesterol (very low for very low density).
HDL cholesterol represents the body's good cholesterol, LDL the bad cholesterol.

The fat lowering (especially those that lower LDL) Effect comes from the fact that simvastatin both the Decreases production of LDL, as well as the Promotes breakdown of LDL cholesterol.

In addition, simvastatin (Simvahexal®) a, if not high, Increase in HDL cholesterol and also one Decrease in triglycerides in blood.
Triglycerides are another form of fat molecule in the body.

Metabolism

Simvastatin (Simvahexal®) gets good when taken orally absorbed in the intestine.

Simvastatin is a inactive productthat must first be activated in order to work in the body. This activation takes place mainly in the liver instead, by causing the molecule to split up through the addition of water. This process is called hydrolysis.

Simvastatin is made via an enzyme that does CYP3A4 and is also found in the liver, metabolized. However, it is estimated that this enzyme also metabolizes half of the drugs in use.
Hence there can be a Variety of drug interactions come.

By inhibiting or increasing this enzyme, you can significant side effects that can pose a risk to the patient.
Become strong inhibitors of the CYP3A4 enzyme such as the drug at the same time in connection with simvastatin therapy Ketoconazole (Medicines for a fungal disease) or macrolide antibiotics like Erythromycin and Clarithromycin taken, simvastatin levels may increase.

A high simvastatin level increases the risk of dangerous side effects such as a so-called Rhabdomyolysiswhich causes the skeletal muscle fibers in the body to break down.

Application / indication

Main field of application of simvastatin (Simvahexal®) is mainly the Hypercholesterolemiawhich have high blood cholesterol levels.

Hypercholesterolemia can be caused by a unhealthy lifestyle caused, but also by a familial genetic burden.

Another very important area of ​​application is the prevention of Cardiovascular diseasescaused by certain diseases like Diabetes mellitus or high blood pressure can arise even with normal fat values.

In patients without risk factors, in whom a change in lifestyle cannot achieve a reduction in fat values, is under drug therapy a target total cholesterol of below 250 mg / dl and the LDL of below 160 mg / dl to strive for.

In patients who do not Coronary heart disease (CHD), but have risk factors for them, such as high blood pressure, is a total cholesterol of below 200 mg / dl and an LDL cholesterol of below 130 mg / dl desirable.

In patients who already have a CHD, the total cholesterol should if possible below 180 mg / dl and the LDL cholesterol below 100 mg / dl lie.

You can find out more about the topic here: Lipid metabolism disorder

Contraindication

Simvastatin (Simvahexal®) in the pregnancy and Lactationbecause there are no studies that could prove the safety of simvastatin. In addition, there are no disadvantages for the pregnant woman by discontinuing therapy.

Even with one Hypersensitivity The substance should not be given against the active ingredient or the ingredients of the tablets.

Unclear increases in liver values ​​or an active one Liver disease represent a contraindication for the ingestion, since the therapy with simvastatin often leads to increased liver values.

Since simvastatin has the Enzyme CYP3A4 is metabolized, parallel intake with inhibitors of this enzyme is not recommended. This can lead to an increase in simvastatin in the blood, which is associated with an increased incidence of undesirable side effects.

Side effects

As rare side effects of simvastatin (Simvahexal®) liver inflammation, constipation, nausea and vomiting can occur.

Furthermore, headaches, anemia (low hemoglobin, a type of red blood cell), Rash or itching occur as a side effect of the therapy.

In very rare cases, liver failure can also occur.

In addition, it can lead to dizziness and headaches.

The occurrence of myopathies is a very dangerous side effect. They are associated with muscle pain and weakness and are accompanied by an increase in the muscle enzyme creatine kinase (CK) hand in hand.

The muscle disease may also manifest itself as so-called rhabdomyolysis. This means a breakdown of the striated muscles in the body.

It is therefore particularly important to recognize this side effect at an early stage, so that patients must report to their doctor immediately if they develop muscle pain or weak muscles.

For this reason, if new muscle pain occurs during simvastatin therapy, the muscle enzyme creatine kinase (CK) to prove possible muscle damage.

The risk of muscle damage increases as the dose increases.
Other HMG-CoA reductase inhibitors can also cause this side effect.

Find out all about the topic here: Rhabdomyolysis.

Interactions

Interactions with other drugs occur, for example, when taking simvastatin at the same time (Simvahexal®) with other fat-lowering medicines such as the so-called Fibrates.

This increases the risk for a Myopathy or. Rhabdomyolysiswhich can occur even if the dose of simvastatin is increased alone.

This risk also increases if you take Inhibiting the enzyme CYP3A4.
These inhibitors include, for example, antibiotics such as Erythromycin or Clarithromycin or the drug ketoconazole. But some drugs that are used in HIV treatment also inhibit this enzyme.