What to Know About Lipitor (Atorvastatin)

A statin used to lower cholesterol

Lipitor, a cholesterol-lowering drug
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Lipitor (atorvastatin) is a cholesterol-lowering medication that belongs to the statin class of drugs. Statins lower cholesterol levels in the blood by blocking 3-hydroxy-3methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme that's needed for the liver to produce cholesterol.

Lipitor comes in oral tablets and is available as a generic.

Uses

Lipitor is an adjunct therapy to diet and is typically prescribed in cases where lifestyle changes (diet, physical activity) or other medications are not effective in lowering cholesterol. For example, it may be used for people with primary hyperlipidemia (high lipid levels due to genetic factors) or mixed dyslipidemia (both triglycerides and cholesterol levels are high).

Lipitor is used to treat elevated:

  • Total cholesterol
  • Low-density lipoprotein (LDL, considered "bad" cholesterol)
  • Triglycerides
  • Apolipoprotein B (apo B, a protein involved in the metabolism of lipids that is also part of lipoproteins, such as LDL)

It can also raise high-density lipoprotein (HDL, considered "good" cholesterol).

Cholesterol and triglycerides can clog blood vessels and increase heart disease risks. Due to this link, statins such as Lipitor are also commonly prescribed to reduce the risk of heart attack, stroke, and angina in people with heart disease or those who have multiple risk factors for developing heart disease.

Lipitor is approved for adults and children age 10 and up.

Off-Label Uses

Statins like Lipitor are sometimes prescribed off-label to try to stop the progression of autoimmune or chronic inflammatory diseases, such as secondary progressive multiple sclerosis (SPMS).

That's because, in addition to lowering lipids (fats), Lipitor and other statins appear to have some novel effects such as influencing immune responses, enhancing anti-inflammatory processes, and altering additional signaling pathways that aren't yet fully understood.

Statins are also sometimes used off-label for neurodegenerative diseases, such as Alzheimer's disease or Parkinson's disease, since high cholesterol levels are associated with disease progression. Patients with HIV or a bacterial infection, such as tuberculosis (TB), may also benefit from the potential effects of these drugs on the immune system.

Before Taking

There are multiple types of statins and Lipitor is one of the more potent options. It is also one of the most commonly prescribed lipid-lowering medications in the United States.

Each type of statin has unique interactions with other medications and risks of side effects, so your doctor will take into account what other medications you're on, how elevated your cholesterol levels are, and what other conditions you have when determining which statin to prescribe.

Other types of statin tablets include Mevacor (lovastatin), Pravachol (pravastatin), Crestor (rosuvastatin), Zocar (simvastatin), and Livalo (pitavastatin). Most of these tablets are also available as generics. Statin capsules include Lescol (fluvastatin) and Ezallor (rosuvastatin), and there is an oral suspension option called FloLipid (simvastatin)

Extended-release tablets are available as Lescol XL (fluvastatin) and Altoprev (lovastatin).

Lipitor is highly effective at lowering cholesterol, yet a study found that compared with other statins, it had the highest number of patients stop taking it due adverse effects, such as muscle pain or damage, followed by the statin Crestor (rosuvastatin), another high-potency option. Simvastatin and pravastatin were more well-tolerated in the study, yet not as potent or effective at lowering cholesterol as atorvastatin or rosuvastatin. Fluvastatin and lovastatin are additional low-potency options.

Research has found that rosuvastatin reduces LDL cholesterol by an average of 51% followed by atorvastatin at 45%, simvastatin at 37%, and pravastatin at 25%.

Precautions and Contraindications

If you have certain medical conditions, you should not take Lipitor. In these cases, your healthcare provider may place you on a different treatment to lower your lipids:

  • Allergy or hypersensitivity: If you have had a previous allergy to Lipitor or any of its ingredients, you should not take this medication.
  • Active liver disease: If you have active liver disease or unexplained, abnormally elevated liver enzyme levels, Lipitor should not be taken. This includes chronic alcoholic liver disease.
  • Pregnancy: Lipitor is categorized as a Pregnancy Category X. The drug has been shown to cross the placental barrier in rats and there have been reports of miscarriages and fetal abnormalities in animal studies. Additionally, this has also been reported in pregnant women taking statin medications. If you are planning to become pregnant or are already pregnant and are taking Lipitor, stop taking it and contact your healthcare provider.
  • Nursing: Lipitor may cross into breast milk and it is not known what type of effect this can have on your child.

Talk to your doctor about all medications, supplements, and vitamins that you currently take. While some drugs pose minor interaction risks, others may outright contraindicate use or prompt careful consideration as to whether the pros of treatment outweigh the cons in your case.

Dosage

Lipitor tablets come in 10, 20, 40, and 80 milligram (mg) doses that are taken once a day, as directed by your healthcare provider.

The standard starting dose for adults is 10 to 20 mg. Those who require at least a 45% reduction in LDL cholesterol may be begin with a 40-mg dose.

Your physician may slowly increase the dose as needed based upon your LDL levels and your response to the medication.

The starting dose for adolescents ages 10 to 17 with an inherited form of high cholesterol is 10 mg up to a maximum dose of 20 mg once daily.

All listed dosages are according to the drug manufacturer. Check your prescription and talk to your doctor to make sure you are taking the right dose for you. Never increase your dose without your doctor's OK.

Modifications

Patients who are 65 or older are at a greater risk of musculoskeletal side effects with Lipitor and may need to take a lower dose or discontinue use of the drug if they experience muscle weakness or breakdown.

How to Take and Store

Lipitor can be taken with or without food. It is quickly absorbed, reaching its peak concentration in the blood within about two hours. Lipitor starts to lower cholesterol within about two weeks of starting the medication.

Lipitor should always be taken in conjunction with a diet to lower your cholesterol and triglycerides.

Store the tablets at a controlled room temperature that's ideally 68 to 77 degrees F.

If you miss a dose of Lipitor, take it as soon as you remember. But if it has been more than 12 hours since the missed dose, skip it and just take your next scheduled dose. Do not take two doses at once.

If you take too much Lipitor or overdose, seek immediate medical care.

Side Effects

As with all drugs and all statins, Lipitor comes with the risk of side effects. Some can be serious or require treatment, so it's important to be aware of them.

Common

  • Swollen/sore nasal passages and the back of your throat (nasopharyngitis)
  • Joint pain
  • Diarrhea
  • Leg pain
  • Urinary tract infections (UTIs)

If you are experiencing any side effects from taking Lipitor that become prolonged or bothersome, you should let your healthcare provider know.

Severe

  • Unexplained muscle aches, weakness, or soreness
  • Brown or dark-colored urine
  • Malaise (general feeling of discomfort or illness)
  • Fever
  • Difficulty breathing
  • Swelling of the face or throat

Some people experience allergic reactions to atorvastatin. If you experience any signs of allergic reaction, seek urgent medical attention.

There are also rare but serious side effects that affect skeletal muscles. Lipitor can cause muscle myopathy (muscle disease that causes muscle aches or weakness) and rhabdomyolysis (muscle breakdown).

Symptoms of rhabdomyolysis include muscle soreness/weakness and dark urine. There have also been cases of rhabdomyolysis that lead to kidney problems, including kidney failure, while taking Lipitor.

If you experience any unexplained muscle pain, tenderness, soreness, or weakness, especially if it is accompanied with malaise and fever, notify your healthcare provider right away. Your dosage of Lipitor may need to be lowered or stopped.

Your risk of experiencing rhabdomyolysis can increase if you are taking other medications or are older than 65.

Warnings and Interactions

While you are taking Lipitor, your doctor will have you come in periodically for blood tests to monitor your cholesterol levels and to check if your dosage needs to be adjusted.

You may also need to be monitored more closely if you have certain medical conditions that could be aggravated by taking the medication or increase the risk of side effects.

If you have any of the following conditions, your healthcare provider may decide to start you on a lower dose of Lipitor and will need to monitor you to determine whether or not taking Lipitor will be potentially harmful to you:

  • Elevated liver enzymes: Lipitor can increase the liver enzymes aspartate aminotransferase (AST) and alanine aminotransferase (ALT). Although this increase is mild and temporary in most cases, your healthcare provider will monitor these levels to make sure that your liver enzymes are not elevated to dangerous levels that indicate liver injury. If the levels of these enzymes are high, you may need to switch to a less potent statin, such as pravastatin, or discontinue taking statins altogether.
  • Elevated blood glucose levels: Studies have shown that atorvastatin may increase hemoglobin A1C and fasting glucose levels. If you have diabetes or at risk of developing the disease, your healthcare provider may monitor these measures in your blood and adjust your dose of Lipitor.
  • Kidney impairment: If you have a history of kidney impairment, you will need to be closely monitored for any muscular or kidney effects while taking Lipitor as the condition may be a risk factor for the development of rhabdomyolsis with kidney failure.
  • Thyroid problems: Uncontrolled hypothyroidism (underactive thyroid) may increase the risk of myopathy and rhabdomyolsis with Lipitor.

Lipitor may also need to be temporarily withheld or discontinued with certain conditions that can lead to myopathy or kidney failure with rhabdomyolysis. This may include the following:

  • Severe infections
  • Hypotension (low blood pressure)
  • Major surgery
  • Physical trauma from injuries
  • Severe metabolic, endocrine, and electrolyte disorders
  • Uncontrolled seizures

Lipitor can cause liver problems, so tell your healthcare provider if you drink alcohol daily. You may need blood tests to check your liver.

Do not drink grapefruit juice while taking this medication since it can impair your body's ability to metabolize the drug and increase blood concentrations of Lipitor.

Drugs and supplements can also interact with Lipitor, and some can increase the likelihood of experiencing side effects, especially myopathy. If you are taking any of these drugs with Lipitor, your healthcare provider may need to adjust your dose, monitor you more closely for side effects, or discontinue one of the drugs:

  • Other cholesterol-lowering drugs: Taking fibrates (also called fibric-acid derivatives) along with Lipito, increases the risk of myopathy.
  • Niacin supplements: Taking vitamin B3 (nicotinic acid) can have some lipid-modifying effects. When niacin supplements are taken with Lipitor there may be an increased risk of myopathy.
  • Sandimmune (cyclosporine): If you are taking this immunosuppressive drug to reduce the risk that your body will reject an organ transplant, do not exceed 10 mg of Lipitor daily due to an increased risk of myopathy and rhabdomyolysis.
  • Biaxin (clarithromycin): This antibiotic used for a variety of bacterial infections strongly inhibits the liver enzyme CYP3A4, which can increase blood levels of Lipitor, as well as the risk of myopathy and rhabdomyolysis. The dosage of Lipitor should not exceed 20 mg per day without close monitoring.
  • Onmel (itraconazole): This antifungal medication is also a strong CYP3A4 inhibitor. Lipitor should not exceed 20 mg per day without close monitoring.
  • HIV protease inhibitors: Norvir (ritonavir) plus Invirase (saquinavir) or Kaletra (lopinavir, ritonivir) are also strong CYP3A4 inhibitors, and Lipitor should not exceed 20 mg per day without close monitoring.
  • Oral contraceptives: If the oral contraceptives contain norethindrone (a form of progesterone) or ethinyl estradiol (a form of estrogen), these hormones may be increased when taken with Lipitor.
  • Lanoxin (digoxin): Blood levels of digoxin, which is used to treat heart failure or abnormal heart rhythms, can increase about 20% when taken with Lipitor. Careful monitoring is needed.
  • Rifadin (rifampin): Rifadin, which is used to treat tuberculosis (TB), should be taken at the same time as Lipitor. If Lipitor is taken after Rifampin, it can reduce blood levels of Lipitor.
  • Colcrys (colchicine): Both colchicine and Lipitor carry the risk of myopathy and taking them together may increase this side effect.
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