Active Ingredients

Lovastatin – Effect, Application & Risks


Lovastatin is a drug used to treat high cholesterol , heart attack , acute coronary syndrome , and unstable angina . In the human body, it mainly affects the formation of cholesterol and the liver , which stimulates it to absorb more cholesterol from the blood .

What is lovastatin?

Lovastatin is a drug from the group of statins . As is typical for this type of medication, it is used in the treatment of high cholesterol (hypercholesterolaemia), but also after a heart attack, in acute coronary syndrome and in unstable angina pectoris.

Cholesterol is a blood fat that has a bad reputation for its role in the development of heart disease . However, the human organism needs it in normal amounts to produce various hormones , vitamin D , bile acid and cell membranes . Cholesterol is one of the low-density lipoproteins (LDL).

In 1987, lovastatin became the first statin to lower blood lipid levels. The molecular formula of the colorless active ingredient is C24H36O5; industry produces the drug using the fungi Aspergillus terreus and Monascus ruber, with the microorganisms fermenting the starting materials in several process steps.

Pharmacological action

The mechanism of action of lovastatin is based on the inhibition of the enzyme HMG-CoA reductase, which the human body needs to make cholesterol. At the same time, the drug stimulates the liver to absorb and break down more cholesterol. LDL receptors in the liver respond to blood fats such as cholesterol: the LDL receptor binds to the molecule and takes it up into a depression in the cell membrane known as the spiny dimple. The occupied cavity then closes and becomes a small sac (vesicle) in the membrane. The trapped cholesterol is thus removed from the bloodstream .

Darüber hinaus hemmt Lovastatin die Neubildung von Cholesterin. Bei der normalen Cholesterin-Regulation bedient sich das Enzym HMG-COA-Reduktase des Koenzyms Nikotinamidadenindinukleotidphosphat (NADPH), das bei der biochemischen Reaktion die abgespaltenen Reste des Substrats aufnimmt.

In the body of a healthy person, cholesterol levels are self-regulating via thyroid hormones , insulin and glucagon , as well as the available amount of HMG-CoA reductase: as long as there is sufficient cholesterol, it binds to a special protein . However, if the cholesterol level drops, more and more of these binding proteins remain unoccupied and the activated proteins produce transcription factors, which in turn stimulate the synthesis of HMG-CoA reductase.

The increasing number of enzymes correspondingly leads to increased cholesterol formation, while conversely an increasing cholesterol level results in the automatic inhibition of synthesis. Lovastatin intervenes in this process by inhibiting HMG-CoA reductase and thus reducing the formation of new cholesterol.

Medical Application & Use

Lovastatin is used, among other things, in the treatment of high levels of cholesterol in the blood. This hypercholesterolemia is reflected in a laboratory test of the blood in increased LDL values. In a healthy person without risk factors, the value should not exceed 160 mg/dl; for patients with coronary heart disease or arteriosclerosis , the reference value is below 100 mg/dl. Elevated cholesterol levels are also a general risk factor for both of these diseases.

Atherosclerosis is characterized by deposits in the blood vessels that can restrict blood flow and consist of fat , thrombi , calcium or connective tissue . These can cause further complications and, among other things, contribute to the development of a heart attack, for the treatment of which the drug lovastatin is also indicated. During a heart attack or myocardial infarction, the blood supply to the heart is interrupted.

After a heart attack, survivors are often given various medications to reduce the likelihood of another event. Lovastatin comes into consideration in this case alongside other statins, beta- blockers , ACE inhibitors and other drugs and in this role it has both a remedial and a preventive position.

A less specific cardiac disease is Acute Coronary Syndrome, which presents with a variety of heart-related conditions. The syndrome is used by doctors as a “working diagnosis” until they can pinpoint the actual disease. One of the possible causes of acute coronary syndrome is unstable angina pectoris, which is due to a combination of arteriosclerosis and coronary artery disease. It can precede a heart attack and can also be treated with lovastatin.

Risks & side effects

With myopathy , bile stasis (cholestasis) or an increased concentration of liver enzymes, lovastatin is contraindicated. The most common side effects of the drug include headaches , increased liver function tests , indigestion and myopathies. In this case, the latter are among the toxic myopathies, since they can be traced back to a drug and lead to the typical muscle weakness of the diverse clinical picture. Overall, muscle symptoms occur in 0.025% of patients taking lovastatin.

In extreme cases, the muscle fibers can disintegrate ( rhabdomyolysis ), which leads to numerous other symptoms: muscle weakness and pain, edema in the muscle tissue, fever , diarrhea and vomiting are among the symptoms of rhabdomyolysis.

Furthermore, the uric acid level in the blood can increase ( hyperuricemia ), the body may excrete larger amounts of the muscle pigment myoglobin ( myoglobinuria ) and electrolyte disorders and consumption coagulopathy are possible in the context of rhabdomyolysis.

A patient’s risk of developing muscle fiber breakdown as a side effect of lovastatin increases when lovastatin is combined with fibrates : for example, concomitant use of gemfibrozil and lovastatin produces the severe side effect in 1-5% of cases. In addition, various antibiotics and antifungals can promote side effects of lovastatin. Foods like grapefruit juice can also cause this effect.

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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.