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Oct 07, 2020
7 min read

Atorvastatin (Lipitor): warnings to be aware of

Statins are part of a drug class called HMG CoA reductase inhibitors. They are used by almost 30% of Americans over 40 years of age. Statins are often one of the first drugs healthcare providers turn to when treating people with high cholesterol levels or heart disease.

Disclaimer

If you have any medical questions or concerns, please talk to your healthcare provider. The articles on Health Guide are underpinned by peer-reviewed research and information drawn from medical societies and governmental agencies. However, they are not a substitute for professional medical advice, diagnosis, or treatment.

Anyone who has been sick—whether with a common cold or something a bit more serious—knows that they’ll likely do whatever it takes to feel better. It’s human nature; if there’s a tincture, tonic, or tablet to help with our pain and problems, we want it.

Enter statins. Regarded by healthcare professionals as the “gold-standard” treatment for high cholesterol, statins have been shown to significantly reduce the risk of heart attacks, strokes, and death among people who are at increased risk.

Statins are part of a drug class called HMG CoA reductase inhibitors. They are used by almost 30% of Americans over 40 years of age. Statins are often one of the first drugs healthcare providers turn to when treating people with high cholesterol levels or heart disease (Salami, 2017). They are often used in combination with other therapies, like weight loss, smoking cessation, and diet modifications.

One such statin drug is atorvastatin calcium. It was first approved in 1996 and sold by Pfizer under the brand name Lipitor; it is now available as either a generic or brand name prescription medicine. While it effectively treats high cholesterol, the drug does come with a list of warnings and contraindications. 

Let’s learn more about atorvastatin (brand name Lipitor) and its various warnings to see if this medication might be worth exploring with your healthcare provider.

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Atorvastatin warnings

Some people living with the following conditions may be more likely to experience adverse events. That said, just because there’s an association does not mean that the reaction will occur for most or even many people.  

Pregnancy and breastfeeding

HMG-CoA reductase inhibitors, like atorvastatin, are contraindicated for pregnant women and nursing mothers. The reasoning behind this is that cholesterol is essential for fetal development. Since atorvastatin decreases the synthesis of cholesterol and potentially substances derived from cholesterol, the medication could cause fetal harm.

To date, there’s been limited research identifying a link between atorvastatin and an increased risk of major congenital malformations or miscarriage. However, since there’s no conclusive evidence stating that atorvastatin is indeed safe during pregnancy, it’s advised to stop taking atorvastatin if you become pregnant or are trying to conceive. 

Also, there is minimal data regarding the risk from atorvastatin in breastmilk, so the FDA does not recommend breastfeeding while taking this drug (DailyMed, 2019).

Kidney disease

Research on whether statins are safe for people with kidney disease is conflicted; some studies show a benefit to the kidneys, whereas others show an increased risk of renal impairment, muscle damage, or kidney inflammation (Verdoodt, 2018).  

For example, a review published by the American Heart Association found that atorvastatin improved kidney function over time (Vogt, 2019). However, another study suggests that statin use increases the risk of kidney disease (Acharya, 2016). 

Despite the controversy, there is not enough data to prohibit the use of statins in people with kidney disease, as lowering cholesterol is beneficial for the kidney. However, there may be differences in which statin, the dose, other medications, etc. if you have kidney disease. So If you have both kidney disease and high cholesterol, work with your healthcare provider to compare the potential benefits versus risks for starting an atorvastatin treatment plan.

Liver disease

Healthcare providers may advise against statin therapy, including atorvastatin, for certain people with liver problems. Atorvastatin is contraindicated in people with active liver disease or unexplained abnormal liver function blood tests. 

Statins like atorvastatin both act on liver enzymes and are broken down by the liver. People with active liver disease or a poorly functioning liver are at higher risk of toxicity and liver damage from statins. 

However, providers can use statins with caution in people with chronic and stable (not active) liver disease (Jose, 2016). You should be aware that people with chronic liver disease, like chronic alcoholic liver disease, may experience higher than expected amounts of atorvastatin in their bloodstream (DailyMed, 2019). 

If you have a history of liver disease or any other concerns, discuss them with your provider. Before starting atorvastatin, your healthcare provider may perform a liver enzyme blood test. One side effect of atorvastatin is that it can cause abnormal liver blood test results. Contact your provider immediately if you have unusual fatigue or weakness, loss of appetite, pain in the upper abdomen, dark-colored urine, or yellowing of your skin or eyes.

Grapefruit

Research shows grapefruits contain a chemical that can interfere with the enzymes that break down the statins in your liver (known as cytochrome P450 system) (Bailey, 2013). Healthcare providers may advise against drinking grapefruit juice if you’re taking other statins, like simvastatin or lovastatin. However, they generally say that it is safe to consume grapefruit if you’re taking atorvastatin, especially if you are only having 8oz of grapefruit juice or half a grapefruit per day (Rosenson, 2020). 

Drinking grapefruit juice or eating grapefruit while taking atorvastatin can increase the risk of some side effects, such as liver disease and muscle damage, especially if you consume large quantities of grapefruit juice (more than 1.2 quarts per day). The good news is that an occasional glass is safe (Rosenson, 2020).

Type 2 diabetes

Atorvastatin may increase your blood sugar levels and raise your risk of developing type 2 diabetes. However, most healthcare providers agree that atorvastatin’s ability to reduce the risk of heart attacks and strokes outweighs the risk of developing diabetes.

A review published in The Lancet found that treating 10,000 patients with 40 mg of atorvastatin per day (high-intensity therapy) for five years would lead to only 50 to 100 new cases of type 2 diabetes. In contrast, it would prevent 500 major vascular events (like a heart attack or stroke) in people who have never had a vascular event before (Collins 2016).

Allergic reactions

Atorvastatin can cause severe allergic reactions such as trouble breathing, trouble swallowing, and swelling of face, lips, tongue, or throat (FDA, 2017). You should not take atorvastatin if you have had an allergic reaction to this medication in the past. 

Drug interactions 

Certain drugs, when taken along with atorvastatin, may increase the risk of side effects. Examples include (DailyMed, 2019)

  • Antibiotic medicines like clarithromycin 
  • Antifungal medications like itraconazole or ketoconazole
  • Cyclosporine
  • ​Niacin
  • Birth control pills
  • Fibrates like gemfibrozil 
  • Heart medications like digoxin
  • Antiretroviral drugs to treat HIV/AIDS like ritonavir, fosamprenavir, tipranavir, or saquinavir
  • Colchicine

Side effects of atorvastatin

Common side effects of Lipitor in placebo-controlled trials were nasopharyngitis (cold symptoms), joint pain (arthralgia), diarrhea, pain in the arms or legs, and urinary tract infections (FDA, 2017).

Other mild side effects include:

  • Heartburn
  • Nausea
  • Muscle aches, pain, or spasms
  • Gas
  • Headache
  • Forgetfulness or memory loss
  • Confusion
  • Trouble sleeping (insomnia)

Less often, atorvastatin can cause more serious side effects. You should seek immediate medical help if you experience any of the following (UpToDate, n.d.):

  • Anaphylaxis (severe allergic reaction with swelling and difficulty breathing)
  • Severe skin rash (including erythema multiforme and Stevens-Johnson syndrome)
  • Rhabdomyolysis
  • Liver failure
  • Unusual bleeding or bruising

Muscle injury

One of the most severe adverse effects of atorvastatin is myopathy, or muscle disease, in the form of myalgia (muscle aches/pain), myositis (muscle inflammation), or rhabdomyolysis (muscle breakdown) (Tomaszewski, 2011). 

Some people (5% or fewer) will notice muscle pain, muscle tenderness, or muscle weakness shortly after starting atorvastatin (Tomaszewski, 2011). Depending on your reaction, the effects could dissipate within two to three weeks, or the pain may continue and worsen. 

However, you should seek medical attention. If you notice that the muscle aches are accompanied by a fever, tiredness, or dark-colored urine—this might be a sign of a serious condition called rhabdomyolysis (muscle breakdown). Rhabdomyolysis can lead to kidney failure and even death (Tomaszewski, 2011). 

Liver complications 

Atorvastatin can cause abnormalities with liver function blood tests (elevated serum transaminases), and your provider will likely run baseline liver blood tests before starting atorvastatin (McIver, 2020). 

Seek medical advice right away if you have the following symptoms of liver problems or failed liver function: fatigue and weakness, dark urine, loss of appetite, stomach pain, yellowing of your skin, or the whites of your eyes. These can all be signs of liver problems.

What is atorvastatin used for?

Atorvastatin (brand name Lipitor) is FDA-approved for the following uses (DailyMed, 2019):

  • Reduce the risk of heart attacks and strokes in people with cardiovascular risk factors, like age, smoking, high blood pressure, diabetes, low HDL (“good” cholesterol), or a family history of early heart disease
  • Decrease the likelihood of heart surgery, as well as lower the risk of heart attacks and strokes, in people with heart disease
  • Lower total cholesterol and low-density lipoprotein (LDL) levels when used with dietary modifications
  • Increase “good” (HDL) cholesterol levels when used with dietary modifications
  • Lower triglyceride levels when used with dietary modifications
  • Treat adults with homozygous familial hypercholesterolemia and primary dysbetalipoproteinemia, disorders that cause abnormal cholesterol levels
  • Decrease the amount of cholesterol and other fatty substances in the blood of pediatric patients (aged 10-17 years) with heterozygous familial hypercholesterolemia (a genetic condition where cholesterol cannot be removed from the body normally) 

There are currently several types of prescription drug statins approved by the U.S. Food and Drug Administration (FDA). Aside from atorvastatin, other available statins include fluvastatin (brand name Lescol), lovastatin (brand name Mevacor), pitavastatin (brand name Livalo), pravastatin (brand name Pravachol), rosuvastatin (brand name Crestor), and simvastatin (brand name Zocor).

Regardless of which statin you choose, talk to your healthcare provider, and together, you can come up with the most appropriate treatment option for you.

References

  1. Acharya, T., Huang, J., Tringali, S., Frei, C. R., Mortensen, E. M., & Mansi, I. A. (2016). Statin Use and the Risk of Kidney Disease With Long-Term Follow-Up (8.4-Year Study). The American Journal of Cardiology, 117(4), 647–655. https://doi.org/10.1016/j.amjcard.2015.11.031. Retrieved from https://linkinghub.elsevier.com/retrieve/pii/S0002914915023152 
  2. American Heart Association (AHA). (2017). Prevention and treatment of high cholesterol (hyperlipidemia). Retrieved on Oct. 7, 2020 from https://www.heart.org/en/health-topics/cholesterol/prevention-and-treatment-of-high-cholesterol-hyperlipidemia
  3. Bailey, D. G. Dresser, G., & Arnold, J. M. (2013). Grapefruit-medication interactions: forbidden fruit or avoidable consequences?. CMAJ, 185(4): 309-316. doi: 10.1503/cmaj.120951. Retrieved from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3589309/
  4. Collins, R., Reith, C., Emberson, J., Armitage, J., Baigent, C.,  Blackwell, L. et al. (2016). Interpretation of the evidence for the efficacy and safety of statin therapy. The Lancet, 388(10059), 2532-2561. https://doi.org/10.1016/s0140-6736(16)31357-5. Retrieved from https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(16)31357-5/fulltext 
  5. DailyMed. (2019). Atorvastatin calcium, film coated tablets (2019). Retrieved on Oct. 7, 2020 from https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1daa6f20-a032-4541-939d-931f36a020dd#ID95
  6. Dormuth, C. R., Hemmelgarn, B.R., & Paterson, J.M. (2013). Use of high potency statins and rates of admission for acute kidney injury: multicenter, retrospective observational analysis of administrative databases. BMJ, 346: f880. doi: 10.1136/bmj.f880. Retrieved from https://www.bmj.com/content/346/bmj.f880
  7. Jose, J. (2016). Statins and its hepatic effects: Newer data, implications, and changing recommendations. Journal of Pharmacy & Bioallied Sciences, 8(1), 23–28. https://doi.org/10.4103/0975-7406.171699. Retrieved from https://www.jpbsonline.org/article.asp?issn=0975-7406;year=2016;volume=8;issue=1;spage=23;epage=28;aulast=Jose 
  8. McIver, L. A. & Siddique, M. S. (2020). Atorvastatin. StatPearls. Retrieved on Oct. 7, 2020 from https://www.ncbi.nlm.nih.gov/books/NBK430779/
  9. Rosenson, R. S. (2020). Statins: Actions, side effects, and administration. UpToDate. Retrieved on Oct. 7, 2020 from https://www.uptodate.com/contents/statins-actions-side-effects-and-administration?search=statins-and-kidney-disease
  10. Salami, J., Warraich, H., Valero-Elizondo, J., Spatz, E., Desai, N., Rana, J., et al. (2017). National Trends in Statin Use and Expenditures in the US Adult Population From 2002 to 2013. JAMA Cardiology, 2(1), 56. https://doi.org/10.1001/jamacardio.2016.4700. Retrieved from https://jamanetwork.com/journals/jamacardiology/fullarticle/2583425 
  11. Tomaszewski, M., Stępień, K. M., Tomaszewska, J., & Czuczwar, S. J. (2011). Statin-induced myopathies. Pharmacological Reports, 63(4), 859–866. doi: 10.1016/s1734-1140(11)70601-6. Retrieved from https://www.sciencedirect.com/science/article/abs/pii/S1734114011706016
  12. UpToDate. (n.d.). Atorvastatin: Drug Information. Retrieved on Oct. 7, 2020 from https://www.uptodate.com/contents/atorvastatin-drug-information
  13. U.S Food and Drug Administration (FDA). (May 2017). LIPITOR (atorvastatin calcium) tablets, for oral use. Parke-Davis. Retrieved Retrieved on Oct. 7, 2020 from https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020702s067s069lbl.pdf
  14. Verdoodt, A., Honore, P. M., Jacobs, R., De Waele, E., Van Gorp, V., De Regt, J., et al. (2018). Do Statins Induce or Protect from Acute Kidney Injury and Chronic Kidney Disease: An Update Review in 2018. Journal of Translational Internal Medicine, 6(1), 21–25. https://doi.org/10.2478/jtim-2018-0005. Retrieved from https://www.sciendo.com/article/10.2478/jtim-2018-0005 
  15. Vogt, L., Bangalore, S., Fayyad, R., Melamed, S., Hovingh, G. K., DeMicco, D. A., et al. (2019). Atorvastatin Has a Dose-Dependent Beneficial Effect on Kidney Function and Associated Cardiovascular Outcomes: Post Hoc Analysis of 6 Double-Blind Randomized Controlled Trials. Journal of the American Heart Association, 8(9), e010827. https://doi.org/10.1161/JAHA.118.010827. Retrieved from https://www.ahajournals.org/doi/10.1161/JAHA.118.010827