Simvastatin: 6 things you should know
Medically reviewed by C. Fookes, BPharm. Last updated on Aug 21, 2018.
1. How it works
- Simvastatin works by blocking an enzyme in the liver known as HMG-CoA reductase that is responsible for the conversion of HMG-CoA to mevalonate, an important substance necessary for the synthesis of cholesterol and coenzyme Q10.
- Simvastatin also boosts the breakdown of lipids.
- Simvastatin belongs to a group of drugs known as HMG-CoA reductase inhibitors or statins.
- Simvastatin, in conjunction with dietary measures, is used in people at high risk of having a heart event to:
- Reduce the risk of death from cardiovascular disease
- Reduce the incidence of non-fatal heart attack and stroke
- Reduce the need for revascularization procedures.
- People considered at increased risk of a heart event include those with diabetes, a history of stroke or a similar event, with pre-existing heart disease, or with peripheral vascular disease.
- Simvastatin is also used to reduce high levels of lipids in people with elevated cholesterol levels. Simvastatin reduces total cholesterol, LDL-cholesterol, apolipoprotein B, triglycerides and increases high-density lipoproteins.
- Simvastatin is also indicated in some genetic lipid disorders (such as heterozygous familial hypercholesterolemia) in adolescents aged 10 to 17 meeting certain criteria.
- The dosage of simvastatin does not need adjusting in mild-to-moderate kidney disease. Patients with severe kidney disease should be started on simvastatin 5mg daily and monitored.
- Generic simvastatin is available.
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- A headache, abdominal pain, nausea, and constipation.
- Myopathy (muscle pain), tenderness, or weakness - initially needs further investigation to determine severity.
- Rarely, severe muscle pain and rhabdomyolysis (a breakdown in muscle tissue) have been reported. The risk is greater in people taking more than 80mg of simvastatin per day, older than 65, of female gender, with uncontrolled hypothyroidism, or kidney disease.
- People of Chinese descent are more likely to develop myopathy. The risk is greater at dosages greater than 20 mg/day or when simvastatin is combined with niacin-containing products.
- Should not be used by people with active liver disease or in women planning a pregnancy or who are pregnant.
- May interact with a number of other medications including:
- Verapamil, diltiazem, dronedarone: Dosage of simvastatin should not exceed 10mg
- Amiodarone, amlodipine, ranolazine: Dosage of simvastatin should not exceed 20mg.
- May increase liver enzymes (increases of up to three times the upper normal limit have been reported).
Notes: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. For a complete list of all side effects, click here.
- Take once daily in the evening and avoid large quantities of grapefruit juice.
- Adhere to the National Cholesterol Education program diet while taking simvastatin.
- Regular exercise is also important as well as avoiding smoking.
- Dosage needs to be individualized but higher dosages (ie, 80 mg/day) should not be used unless they are shown to be tolerated without causing muscle pain. If higher dosages are needed, your doctor may consider an alternative statin (ie, atorvastatin, rosuvastatin).
- Regular blood tests are needed (after 4 weeks of therapy then periodically thereafter) to determine the effect of simvastatin on lipids and other factors (such as liver function).
- Report to your doctor immediately if you experience any unexplained muscle pain, tenderness, or weakness, particularly if associated with tiredness or fever.
6. Response and Effectiveness
- Simvastatin is a prodrug, which means it is converted into its active beta-hydroxyacid form, after administration.
- Peak levels are seen within 1.3 to 2.4 hours following administration; however, it may take up to one to two weeks of regular dosing before improvements in lipid levels are seen.
- Simvastatin reduces cholesterol, Very Low-Density Lipoproteins (VLDL) and triglycerides while increasing HDL-cholesterol.
Simvastatin [Package Insert]. Revised 03/2018. Cadila Healthcare Limited https://www.drugs.com/pro/simvastatin.html
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use simvastatin only for the indication prescribed.
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