Atorvastatin: Everything You Need to Know

High cholesterol is a very common health problem in high-income countries. This medicine helps fight it.

Written and verified by el biólogo Samuel Antonio Sánchez Amador.

Last update: 08 March, 2023

Atorvastatin is a medication that can reduce cholesterol and triglyceride levels in the blood. For this reason, it’s used to prevent cardiovascular diseases with abnormal lipid levels in the body. This drug, along with other statins, is the first barrier to treatment in people with high cholesterol.

It should be noted that atorvastatin is the active substance of the drug, but its found under other brand names in pharmacies. Cardyl ®, Colator ®, Prevencor ®, Thervan ®, and Zarator ® are some of them, although there are also generic forms of the drug.

The active principle was patented in 1986 and began to be used generally in the United States in 1996. As indicated by the ClinCalc portal, in 2018 this drug ranked number 1 in the United States region (and today it continues to be so) for prescribed drugs, with more than 114 million prescriptions.

What is atorvastatin used for?

As we have said, atorvastatin is the most prescribed drug in the United States each year. In its commercial form in this territory, until 2012 (Lipitor ®), it had a turnover of about $13 million annually. Its price is relatively cheap (4.21 euros for 28 tablets), but its demand is what makes it an exceptional drug.

Atorvastatin belongs to the group of statins, a drug conglomerate used to lower cholesterol and triglycerides in their different forms. At a physiological level, they’re known as HMG-CoA reductase inhibitors, an enzyme that modulates the speed of the mevalonate pathway, that is, the metabolic pathway that produces cholesterol.

This drug acts as a competitive inhibitor of HMG-CoA reductase, but, unlike other statins, it’s an exclusively synthetic compound. The impediment of this enzymatic functionality translates into a lower synthesis of cholesterol, in addition to an increase in the expression of low-density lipoprotein receptors (LDL receptors) in hepatocytes.

This drug is rapidly absorbed, reaching its pharmacological peak within 1-2 hours after ingestion. The active principle and its metabolites are excreted in the bile and their half-life is about 14 hours, although the metabolites have slightly higher figures, from 20 to 30 hours.

FDA-approved uses

The United States Food and Drug Administration has approved the use of atorvastatin in the following settings:

• A clinical approach in adults with primary hyperlipidemia or mixed dyslipidemia.
• Treatment of hypertriglyceridemia (excess of complex fatty acids in the blood).
• Treatment of homozygous familial hypercholesterolemia.
• Management of the condition in pediatric patients with heterozygous familial hypercholesterolemia (in case of failure of the dietary guidelines).

On the other hand, it should be noted that atorvastatin is used in primary and secondary prevention. Its use is conceived in patients without coronary diseases, but who have a high risk of developing them due to their blood cholesterol level.

In addition, it’s also prescribed as secondary prevention in people who do have coronary heart disease. In addition to the uses already mentioned, in this population group it’s used to reduce the risk of hospitalization for congestive heart failure.

How is atorvastatin given?

As indicated by the StatPearls medical portal, this medication comes as a tablet to take orally. However, its concentration varies by brand. The variants are as follows: 10 milligrams, 20 milligrams, 40 milligrams, and 80 milligrams per pill.

The dosage is very simple, as it’s always taken orally before or after meals, with a glass of water. We show you everything you need to know about its dosage in the following list:

• The starting dose is 1 tablet of 10 milligrams once a day. This applies to adults and children over 10 years of age.
• This starting dose can be adjusted over time, according to the needs of the patient. Increases and decreases in concentrations occur at intervals of 4 weeks or more.
• The maximum dose is one 80-milligram tablet once a day.

The strength of each tablet depends on the health of the patient. Atorvastatin in its less powerful forms should lower the amount of bad cholesterol (LDL) by 30-50%.

Dosage in special cases

In the following list we explore the dosage of this drug in special patients:

• Pediatric population: There have not been many studies evaluating the treatment of familial hypercholesterolemia with more than 20 milligrams of atorvastatin daily in children. For this reason, doses above those mentioned aren’t usually recommended.
• Over 65s: Patients over 65 years of age have more difficulties to eliminate the drug. Therefore, lower doses may be necessary.
• Kidney failure patients: Atorvastatin and its metabolites don’t follow a renal elimination pathway. Therefore, patients with kidney failure don’t need a dose adjustment.
• Patients with liver failure: As this drug is metabolized in the liver, its use is contraindicated in patients with chronic liver failure.

Who shouldn’t take atorvastatin?

First of all, this drug shouldn’t be taken by anyone with a history of hypersensitivity to atorvastatin or any of its excipient compounds. Beyond the active principle, these are the elements that make up each tablet: microcrystalline cellulose; anhydrous sodium carbonate; maltose; croscarmellose sodium, and magnesium stearate, among others.

The information leaflet distributed with this medication states that the following people shouldn’t take the drug.

• Patients with liver failure: If the liver doesn’t filter well, the metabolites of the drug can accumulate in the blood and cause adverse effects. People with cirrhosis, hepatitis, and other conditions that affect this organ should refrain from consuming atorvastatin.
• Women of childbearing potential not using contraceptives: This drug is completely contraindicated in pregnancy and lactation.
• Patients using the glecaprevir / pibrentasvir combination for the treatment of hepatitis C.

Beyond these contraindications, there are some tables in which this drug can be used, but which require special monitoring. Notify your doctor before starting treatment if you have suffered a stroke, severe kidney problems, chronic alcoholism, hypothyroidism, or repeated muscle problems.

What are the possible side effects?

Like all existing medications, atorvastatin has certain side effects:

• Common side effects (affects up to 1 in 10 people): Inflammation of the nasal passages, sore throat, nosebleeds, physical manifestations of allergy, increased blood sugar levels, headaches, constipation, nausea, gas, diarrhea, joint pain.
• Uncommon (affects up to 1 in 100 people): Anorexia, weight gain, decreased blood sugar levels, insomnia, dizziness, numbness of the fingers, ringing in the ears, skin rash and itching, hives, hair loss, muscle pain, fatigue, feeling unwell, weakness, chest pain, and swollen ankles.
• Rare (1 in 1000 people): Visual disturbances, unexplained bleeding and bruising, yellowing of the skin, and tendon injuries.
• Very rare (1 in 10,000 people): allergic reactions, hearing loss and breast enlargement in men (gynecomastia).
• Not known: constant muscle weakness.

What should you do if you miss a dose?

As we have already said, this drug is almost always taken only once a day. The strength of each tablet varies, but not the number of tablets consumed in 24 hours. Therefore, if you forget your dose, you can take it a few hours later, with or without food.

However, as indicated by the National Library of Medicine of the United States, if there are less than 12 hours before the next dose, it’s better to skip the forgotten one. Never take 2 pills at the same time.

What should you do if you take an overdose of atorvastatin?

According to sources already cited, there’s no exclusive treatment for atorvastatin overdose. If a patient takes more of this medication than they should and begins to show adverse effects, the only way out is to go to the emergency room and provide supportive therapy until they improve.

As indicated by the Lagune Treatment Hospitals, patients with dependence on this drug have been detected, despite the fact that it doesn’t produce this effect on a physical level. Some people may develop a psychological urge to consume it or take more pills than necessary, as this could allow them to lead a less healthy lifestyle. Of course, there’s no truth in this at all.

How to store and dispose of this medicine?

This drug should be kept out of the reach of children at all times. Its safety hasn’t been established in children under 10 years of age, so special care must be taken. Otherwise, it must be stored below 30 degrees Celsius (86 Fahrenheit).

If you want to dispose of a box of atorvastatin because it has expired or you don’t need it, don’t throw it away or down the drain or toilet. Find an official medicine recycling point in your country.

The world’s most used prescription drug

Atorvastatin (in all its commercial forms) is the most widely used prescription drug in many regions of the world, such as the United States. This is mainly because high cholesterol is the sixth main risk factor for death after hypertension, tobacco use, hyperglycemia, lack of exercise, and obesity.

However, it should be noted that taking this medicine doesn’t exempt the patient from their responsibilities. Apart from taking medicine, you should ensure you have a healthy diet, lead an active lifestyle, and exercise regularly.