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Lovastatin: 7 things you should know

Medically reviewed by Carmen Fookes, BPharm. Last updated on Oct 1, 2021.

1. How it works

  • Lovastatin 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.
  • Lovastatin also boosts the breakdown of lipids.
  • Lovastatin belongs to a group of drugs known as HMG-CoA reductase inhibitors. It may also be called a statin.

2. Upsides

  • Lovastatin, in conjunction with dietary measures, is used to lower total cholesterol and LDL-cholesterol in people at increased risk of cardiovascular disease if initial dietary measures fail to lower their cholesterol.
  • Lovastatin is also used to reduce the risk of heart attack, unstable angina, and revascularization procedures in people with moderately elevated total cholesterol and LDL-cholesterol, and low HDL-cholesterol.
  • Lovastatin may also slow the progression of atherosclerosis in people with preexisting coronary heart disease.
  • Lovastatin is also indicated in some genetic lipid disorders (such as heterozygous familial hypercholesterolemia) in adolescents aged 10 to 17 meeting certain criteria.

3. Downsides

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:

  • Gastrointestinal side effects (such as abdominal pain, diarrhea, constipation, flatulence, nausea), muscle pain, headache, and dizziness.
  • Lovastatin, like other statins, may affect liver function, manifesting as changes in liver function tests (more than three times the upper limit of normal) or jaundice requiring dosage reduction or discontinuation.
  • Rarely, severe muscle pain and rhabdomyolysis (a breakdown in muscle tissue) have been reported. Risk is greater in people taking more than 30mg lovastatin per day, older than 65, taking certain medications (for example cyclosporine, itraconazole, HIV antivirals, grapefruit juice), who drink more than two alcoholic drinks per day, or who have a low body weight or with certain medical conditions such as hypothyroidism, diabetes, kidney or liver disease.
  • Rarely, lovastatin has been associated with memory loss, forgetfulness, amnesia, memory impairment, and confusion. These symptoms typically resolve with discontinuation.
  • May interact with some other medications including amiodarone, danazol, diltiazem, dronedarone, and verapamil. Should not be taken with cyclosporine or gemfibrozil or other lipid-lowering agents.
  • Grapefruit juice may enhance the effects and the side effects of lovastatin.
  • High dosages of lovastatin are not recommended in kidney disease.
  • Do not use during pregnancy, and women who are taking lovastatin should not breastfeed. If taken during pregnancy, lovastatin may interfere with the synthesis of steroids and cell membranes in the fetus.

Note: 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. View complete list of side effects

4. Bottom Line

Lovastatin is effective at lowering cholesterol; however, its use may be limited by side effects such as muscle pain. Lovastatin interacts with grapefruit and grapefruit juice products.

5. Tips

  • Take lovastatin with the evening meal. Do not take with grapefruit juice or grapefruit products.
  • Seek urgent medical advice if you develop any acute severe muscle pain.
  • Adhere to the TLC diet, designed by the National Cholesterol Education Program (NCEP), or a similar diet, while taking lovastatin.
  • Plan to do exercise regularly and stop smoking if you smoke. Try to avoid second-hand smoke.
  • Dosage needs to be individualized and should be guided by the results of cholesterol tests taken 2 to 4 weeks later.
  • See your doctor straight away if you notice any yellowing of your skin or shortness of breath, unexplained cough or general tiredness.   
  • Lovastatin should not be taken during pregnancy or while breastfeeding. Ensure you use effective contraception while taking lovastatin if you are a woman of childbearing age and talk to your doctor if you intend to become pregnant before you actually become pregnant.

6. Response and effectiveness

  • Lovastatin is converted to its active form after oral administration. Peak levels are seen within two hours following administration; however, it may take one to two weeks of regular dosing before improvements in your cholesterol level are seen, and up to four weeks before the maximal cholesterol-lowering effects of lovastatin are apparent.  
  • Lowers LDL-cholesterol and apolipoprotein B.
  • Secondary reasons for abnormally high cholesterol levels (such as uncontrolled diabetes mellitus, low thyroid levels, alcoholism, liver disease) should be ruled out before starting lovastatin.

7. Interactions

Medicines that interact with lovastatin may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with lovastatin. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Common medications that may interact with lovastatin include:

  • amiodarone
  • antibiotics, such as erythromycin
  • anticonvulsants, such as fosphenytoin or phenytoin
  • antidepressants, such as nefazodone
  • antifungals, such as itraconazole, ketoconazole, posaconazole, or voriconazole
  • aprepitant
  • azithromycin
  • bezafibrate
  • calcium channel blockers such as amlodipine, diltiazem, or verapamil
  • colchicine
  • cyclosporine
  • dabigatran
  • digoxin
  • fusidic acid
  • gemfibrozil
  • grapefruit juice
  • HIV medications such as tipranavir or ritonavir
  • letermovir
  • mifepristone
  • niacin
  • oral contraceptives
  • other lipid-lowering drugs such as gemfibrozil and bezafibrate
  • red yeast rice
  • St John's Wort
  • CYP3A4 inducers such as efavirenz or rifampin
  • CYP3A4 inhibitors, such as clarithromycin or cyclosporine
  • warfarin.

Note that this list is not all-inclusive and includes only common medications that may interact with lovastatin. You should refer to the prescribing information for lovastatin for a complete list of interactions.

References

Lovastatin. Revised 05/2021. Mylan Institutional Inc. https://www.drugs.com/pro/lovastatin.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use lovastatin only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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