Atorvastatin
A statin that lowers LDL cholesterol and cuts heart attack and stroke risk in people who have, or are at risk of, heart disease.
Drug card
- Class
- Statin
- How it works
- Blocking HMG-CoA reductase, so the liver makes less cholesterol
- Used for
- High LDL cholesterol, including familial forms
- Lowering heart attack and stroke risk
- High triglycerides (with diet)
- Known for
- Muscle aches (myalgia) and limb pain
- Myopathy and rhabdomyolysis
- Its name
- -vastatin means a statin (HMG-CoA reductase inhibitor)
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does atorvastatin work?
Selectively and competitively inhibits HMG-CoA reductase in the liver, which raises the number of hepatic LDL receptors and also lowers LDL production and particle numbers. Several of its metabolites are active too. It is a CYP3A4 and OATP1B1/1B3 substrate, and its LDL effect tracks the dose better than the plasma level.
Like other statins: Statins competitively inhibit HMG-CoA reductase, the enzyme that sets the pace of cholesterol synthesis by turning HMG-CoA into mevalonate. Short of cholesterol, liver cells put more LDL receptors on their surface and take up more LDL from the blood, and the liver releases less VLDL. Plasma LDL cholesterol falls, and with it the risk of heart attack and stroke.
Uses
What is atorvastatin used for?
- High LDL cholesterol, including familial forms
- Lowering heart attack and stroke risk
- High triglycerides (with diet)
Side effects
Side effects of atorvastatin
- Muscle aches (myalgia) and limb painKnown for
- Myopathy and rhabdomyolysisKnown forSerious
- Acute kidney injury from rhabdomyolysisSerious
- Immune-mediated necrotizing myopathy (rare)Serious
- Raised liver enzymes, rarely liver failureSerious
- Higher blood sugar and HbA1c
- Joint pain
- Diarrhea
- Indigestion
- Nausea
- Urinary tract infection
- Insomnia
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Contraindicated in acute liver failure or decompensated cirrhosis; consider liver enzyme tests before starting.
- Cyclosporine, gemfibrozil and some HIV and hepatitis C antivirals are not advised with it; azoles and macrolides need dose limits.
- Grapefruit juice in large amounts (over 1.2 liters daily) raises its levels and is not recommended.
- Stop it when pregnancy is recognized; breastfeeding is not recommended during treatment.
Good to know: After a recent hemorrhagic stroke, its highest dose was linked to more hemorrhagic strokes (SPARCL), so the balance of risk and benefit is weighed.
Remember it
A way to remember it
Statins shut the cholesterol factory, and the liver goes shopping for LDL.
With HMG-CoA reductase blocked, liver cells make less cholesterol and add LDL receptors to pull LDL out of the blood. The harms to watch for are in the muscles (myalgia, rhabdomyolysis) and the liver.
Written for biofideX
Its name
-vastatin means statin (HMG-CoA reductase inhibitor)
Atorvastatin, simvastatin, rosuvastatin and pravastatin block HMG-CoA reductase. WHO files the stem under -stat (enzyme inhibitors); nystatin, an antifungal, is not a statin.
- Every drug name stem
Its class
Statins
Other statins with a card:
Easily mixed up with fibrates and cholesterol absorption inhibitors.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Blood clots and cholesterol
Atorvastatin is one of 19 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
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