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Simvasterol is a drug used to treat hypercholesterolaemia. It is a condition that is associated with too high cholesterol in the blood, exceeding values above 200 mg / dl. Hypercholesterolaemia may be primary (congenital) or secondary, resulting from certain medications or the coexistence of liver disease or hypothyroidism. How does Simvasterol work? What potential side effects can it cause?
Manufacturer of the drug: Polpharma SA
Form, dose, packaging: coated tablets; (10; 20; 40) mg; 28 pcs.
Availability category: Rp – prescription drug
Active substance: simvastatin
Simvasterol – action
The action of Simvasterol, and more specifically the simvastatin it contains, is based on the inhibition of the processes leading to the synthesis of cholesterol. This is due to blocking the activity of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), which is involved in the conversion of HMG-CoA to mevalonate. This substance is a precursor in the process of cholesterol synthesis. By blocking the enzyme, simvastatin lowers the concentration of the so-called bad cholesterol (LDL-cholesterol) and triglycerides, while increasing the level of ‘good’ cholesterol (HDL-cholesterol) in the blood. It should be noted that the simvastatin contained in Simvasterol shows the described properties also when the blood cholesterol level is normal.
Simvasterol – indications
The main indication for the use of Simvasterol is hypercholesterolemia or the so-called mixed dyslipidemia. The drug should be taken when the cholesterol level does not decrease despite changes in the daily diet and exercise. It should be noted that hypercholesterolaemia may be primary (e.g. familial hypercholesterolaemia) or acquired, i.e. one that results from other diseases (e.g. hypothyroidism, acquired liver diseases). Simvastatin is recommended in both cases. In addition to the above-mentioned, Simvasterol is also indicated in the prevention of cardiovascular diseases, e.g. in patients suffering from atherosclerosis or diabetes.
Simvasterol – dosage
Simvasterol is available on the pharmacy market in three doses: 10; 20 and 40 mg. This medicine can be dosed from 5 to 80 mg once a day (the 10 mg film-coated tablets can be divided in half). Due to the fact that the highest cholesterol production occurs at night, Simvasterol should be taken in the evening. Taking the drug should be started with low doses (from 5 to 20 mg), gradually, every 4 weeks, increasing the dosage. Starting therapy with a higher dose of 40 mg is recommended in those people who need a relatively rapid lowering of cholesterol levels, as well as in patients struggling with family hypercholesterolaemia. The highest possible single dose of Simvasterol is 80 mg and is indicated for patients who suffer from severe hypercholesterolaemia.
Simvasterol – contraindications
Contraindications to the use of Simvasterol include: hypersensitivity to the active substance (simvastatin) or any of the excipients, pregnancy and lactation, liver ailments, increased activity of some liver enzymes. It should be added that Simvasterol in a dose higher than 40 mg should not be taken by people suffering from familial hypercholesterolaemia who are simultaneously taking lomitapide.
Simvasterol – warnings
Due to its mechanism of action, Simvasterol may damage skeletal muscles. It is manifested by tenderness and muscle pain. The degree of damage to these structures can be assessed by testing the concentration of creatine kinase (CK) in the blood. It is an enzyme whose level in the blood in the physiological state is negligible, and in the case of myopathy (muscle breakdown) its concentration increases even 10 times. In extreme cases, rhabdomyolysis, which is a severe myopathy leading to renal failure, may occur. Fatal cases have also been reported. The risk of developing myopathy or rhabdomyolysis is dose-dependent. It is advisable to test creatine kinase before starting treatment in women, patients over 65 years of age, people struggling with renal dysfunction and hypothyroidism, as well as in alcoholics. If muscle pain and weakness occur during treatment with Simvasterol, your CK levels should be measured. Attention! The determination of creatine kinase level cannot be performed after intense physical exercise, otherwise the test is unreliable.
Simvasterol – interactions
Avoid combining Simvasterol with:
- cytochrome P450 inhibitors e.g. ketoconazole, erythromycin, clarithromycin, cyclosporin, gemfibrozil;
- fusidic acid;
- anti-arrhythmic drugs e.g. diltiazem, verapamil;
- grapefruit juice (inhibition of cytochrome P450).
Simvasterol – side effects
Possible side effects of Simvasterol include: anemia, headache and dizziness, constipation, abdominal pain, hepatitis, myopathy.