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Medication Overview Simvastatin (Zocor) for High Cholesterol Management
Simvastatin, referred to by the brand name Lipitor, belongs to a class of medications known as HMG-CoA reductase inhibitors, also known as statins. Statins work to lower lipid levels in the body. Lipids are fats found in the blood and include things like cholesterol and triglycerides.
When you have high lipid levels, you are at increased risk for things like stroke, heart attack, and other cardiovascular issues. Because simvastatin lowers lipid levels, it prevents coronary heart diseases that lead to downstream complications and death.
Because of its mechanism of action, simvastatin has several uses approved by the Food and Drug Administration (FDA) that are related to dyslipidemias. It also has two off-label indications.
Medication Indications for Simvastatin (Zocor) for High Cholesterol Management
Simvastatin is used as an adjunct to proper diet to do the following:
- Lower the risk of coronary heart disease deaths and non-fatal stroke, heart attack, and revascularization procedures for those at increased risk of heart events.
- Lower cholesterol, apo B, and triglycerides in those with primary hyperlipidemia
- Lower triglyceride levels in individuals with hypertriglyceridemia
- Lower triglycerides and cholesterol in individuals with primary dysbetalipoproteinemia
- Lower cholesterol in individuals with homozygous familial hypercholesterolemia
- Lower cholesterol and Apo B in adolescents with heterozygous familial hypercholesterolemia after diet therapy failure.
Although all these indications may be confusing, they all share one commonality: lowering lipid levels to prevent downstream complications.
Additionally, simvastatin may be used off-label for prophylaxis of heart issues after post-acute coronary syndrome hospitalization or for prophylaxis of atrial fibrillation in those with stable coronary artery disease.
Dosage and Administration of Simvastatin (Zocor) for High Cholesterol Management
Simvastatin is available as tablets in 5, 10, 20, 40, and 80 mg strengths.
The starting dose for simvastatin is usually between 10 and 20 mg once daily at nighttime. However, suppose you have a high risk of a coronary heart disease event because of diabetes, peripheral vessel disease, stroke, or coronary heart disease. In that case, you may need to start at 40 mg daily. From there, the average dosage range is between five and 40 mg daily. Typical dosing for the following conditions is as follows:
- Homozygous familial hypercholesterolemia: The dose is 40 mg daily at night in combination with other lipid-lowering treatments.
- Adolescents with heterozygous familial hypercholesterolemia: The starting dose is 10 mg once daily at night, which can be increased every four weeks up to 40 mg daily. The maximum suggested dose is 40 mg daily.
- Renal impairment: Dose adjustments should only be made in instances of severe renal impairment, in which the dose should begin at 5 mg daily and monitored closely (1).
- Chinese patients also on >1 g daily of niacin. When taken with more than one gram daily of niacin, simvastatin can increase one’s risk of myopathy. Likewise, Chinese patients also taking niacin should use caution when taking a dose higher than 20 mg daily. Additionally, Chinese patients also on niacin therapy should not take 80 mg of simvastatin.
Potential Side Effects of Simvastatin (Zocor) for High Cholesterol Management
The most common side effects of simvastatin are those that affect more than five percent of people, and these include stomach pain, headache, constipation, nausea, and upper respiratory infection. Simvastatin can also cause more serious side effects, which are noted below:
- Myopathies/rhabdomyolysis. Myopathies are conditions that affect your skeletal muscle and include things like muscle pain, weakness, and tenderness. This is accompanied by increased creatine phosphokinase, which is ten times the upper limit of normal.
- In addition, rhabdomyolysis can occur, a severe condition characterized by damaged muscle that produces electrolytes and proteins in the blood. This can cause injury to your kidneys or heart, resulting in serious complications or death. Your risk of muscle complications is increased with kidney impairment, increased age, female sex, and uncontrolled hypothyroidism.
- Liver problems. Statins like atorvastatin may cause marked increases in liver enzyme levels.
- Diabetes. Statins may increase fasting blood sugar levels or HbA1c. Despite this, the ACC/AHA still believes the benefits of statin therapy outweigh the risks for diabetes.
Precautions and Contraindications
There are several contraindications to simvastatin therapy. These include:
- Active liver disease. Because of its potential effect on liver enzymes, simvastatin should not be used in patients with active liver disease, as simvastatin may cause increased levels of liver enzymes.
- Coadministration with strong CYP3A4 inhibitors. CYP3A4 inhibitors include HIV medications, ketoconazole, erythromycin, itraconazole, and clarithromycin, amongst others. These can affect the levels of simvastatin in the body when taken together.
- Pregnancy. Simvastatin is contraindicated in patients who are pregnant or who may become pregnant.
- Nursing mothers. A small portion of simvastatin can pass via the breast milk to an infant, causing serious effects. Thus, if a woman needs simvastatin therapy, they should not breastfeed.
- Allergy. Allergy to simvastatin or any part of the medication is contraindicated.
Interactions
Caution should be taken when taking atorvastatin with other medications that may increase one’s risk of myopathy. This risk is increased with:
- Niacin
- Cyclosporine
- Fibric acid derivatives
- Strong CYP3A4 inhibitors (e.g., clarithromycin, itraconazole, HIV medications)
- Calcium channel blockers, amiodarone, ranolazine, or dronedarone
- Colchicine
Other medications that may interact with atorvastatin include digoxin.
Effectiveness and Expectations of Simvastatin (Zocor) for High Cholesterol Management
The efficacy and safety of statins, specifically simvastatin, is well-established. One study, for example, analyzed over 4,000 patients with coronary heart disease. In this study, individuals were randomized to receive either simvastatin or placebo in conjunction with standard of care (which included diet).
Simvastatin therapy was associated with reductions in total cholesterol, LDL cholesterol, and triglycerides of 25, 35, and 10 percent, respectively. Additionally, HDL cholesterol (“good cholesterol”) increased by eight percent. The risk of death by coronary heart disease decreased by 42 percent, and the risk of major coronary events by 34 percent.
Long-Term Use and Monitoring of Simvastatin (Zocor) for High Cholesterol Management
Your provider should monitor your lipids four weeks after beginning treatment and regularly afterward to provide appropriate dose adjustments. Your provider should also take labs to assess your liver at baseline and afterward as needed to ensure no liver toxicity. Additionally, creatine kinase levels should be monitored in individuals with renal insufficiency.
Because of the many drug interactions that can occur with simvastatin, providers should regularly review patients’ medication lists to ensure no drug interactions. This will prevent the development of myopathies and other complications.
Alternatives and Complementary Therapies of Simvastatin (Zocor) for High Cholesterol Management
Other pharmacologic and herbal therapies can also help to lower cholesterol levels. Other pharmacologic therapies include:
- Fibrates. Fibrates can decrease triglyceride levels and may have a modest effect (about 15 to 20 percent reduction) on cholesterol levels. However, fibrates do not seem to lower your risk of stroke and heart attack. Thus, they are not a full alternative to statins.
- Niacin. Some research suggests that niacin can reduce bad cholesterol and increase good cholesterol. However, like fibrates, they do not decrease your risk of stroke or heart attack and thus are not a good alternative to statins.
- Cholestyramine. Cholestyramine, along with other bile acid-binding resins, are not used much anymore because of their inability to lower heart attack and stroke risk.
Simvastatin should always be used in adjunct to diet to lower cholesterol. The American Heart Association (AHA) suggests limiting saturated fat in your diet to less than six percent of your total daily calories. In addition, you should avoid trans fat when possible. This means avoiding things like dairy, red meat, and fried foods.
Other complementary therapies involve engaging in regular exercise. 150 minutes of moderate-intensity aerobic workouts can benefit your blood pressure and cholesterol levels. Several ways to do this include cycling, quick walking, and swimming. Regular exercise and a proper diet together can help you to lose weight. Thankfully, weight loss of five to 10 percent of body weight can significantly improve cholesterol levels.
If you smoke or vape, you should consider quitting. Both smoking and vaping lower your good cholesterol. Stopping can decrease your bad cholesterol while increasing your good cholesterol. Quitting smoking also has several other benefits outside of just cholesterol levels.
Frequently Asked Questions (FAQs) of Simvastatin (Zocor) for High Cholesterol Management
What do I do if I get side effects from simvastatin?
If you experience side effects from simvastatin, discuss these with your doctor. Your provider may lower your dose or change you to a different type of statin.
How long will I be on simvastatin for?
You are typically on statins for the rest of your life to ensure that your cholesterol levels are maintained at a healthy level.
How do I know if simvastatin is working?
We cannot feel our cholesterol levels, so it is difficult to know if simvastatin works unless you get blood tests. Usually, your cholesterol levels should decrease significantly around the four-week mark as long as you take the medication as directed. After four weeks of therapy, you should check your cholesterol levels to ensure that atorvastatin works.
Can I drink while on simvastatin?
You can drink alcohol while on simvastatin. However, alcohol use can elevate your risk of developing muscle and liver side effects.
Resources
- https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019766s087s088lbl.pdf
- https://www.ncbi.nlm.nih.gov/books/NBK532919/
- https://www.bhf.org.uk/informationsupport/heart-matters-magazine/medical/cholesterol-lowering-alternatives
- https://www.heart.org/en/health-topics/cholesterol/prevention-and-treatment-of-high-cholesterol-hyperlipidemia#:~:text=The%20American%20Heart%20Association%20recommends,fat%2Dfree%20dairy%20products%20instead.