What it does
Atorvastatin is a medication that helps lower cholesterol levels in the blood.
Commonly used for: high cholesterol (hyperlipidemia), prevention of heart disease
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 21:22:56 · updated 2026-07-20 10:56:58
About this medicine
Atorvastatin is a medication that helps lower cholesterol levels in the blood.
What it treats
- high cholesterol (hyperlipidemia)
- prevention of heart disease
How it works
It works by blocking a substance your body needs to make cholesterol, which helps reduce the amount of cholesterol in your blood.
Who it's for
It is typically prescribed for adults who have high cholesterol or those at risk of heart disease.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: atovastatin
Atorvastatin is a statin medication used to lower cholesterol levels in the blood. It is primarily indicated for the management of hyperlipidemia, including primary hypercholesterolemia and mixed dyslipidemia. As a competitive inhibitor of HMG-CoA reductase, atorvastatin plays a crucial role in reducing low-density lipoprotein (LDL) cholesterol and total cholesterol levels, thereby decreasing the risk of cardiovascular diseases.
Indications
- Primary hypercholesterolemia
- Mixed dyslipidemia
- Secondary prevention of cardiovascular events in patients with established coronary heart disease
- Prevention of cardiovascular disease in high-risk patients
Dosage
Children: Refer to the BNF for Children for appropriate pediatric dosing information.
Adults: Refer to relevant treatment guidelines or the BNF for specific dosing recommendations.
Mechanism of action
Atorvastatin inhibits HMG-CoA reductase, the rate-limiting enzyme in the cholesterol biosynthesis pathway. This inhibition leads to a decrease in intracellular cholesterol levels, which stimulates the upregulation of LDL receptors on hepatocyte surfaces. The increased number of LDL receptors enhances the clearance of LDL cholesterol from the bloodstream, effectively lowering plasma cholesterol levels.
Pharmacodynamics
Atorvastatin exhibits dose-dependent reductions in LDL cholesterol, total cholesterol, and triglycerides, while generally increasing high-density lipoprotein (HDL) cholesterol. The drug's effects on lipid profiles contribute to its cardiovascular protective effects, reducing the incidence of atherosclerotic events. Atorvastatin also has anti-inflammatory properties and may stabilize atherosclerotic plaques.
Pharmacokinetics
Atorvastatin is well absorbed after oral administration, with peak plasma concentrations occurring approximately 1 to 2 hours post-dose. It undergoes extensive first-pass metabolism in the liver, primarily via cytochrome P450 3A4. The drug has a half-life of approximately 14 hours. Atorvastatin is eliminated through both hepatic and biliary pathways, with metabolites excreted in urine and feces. Food intake may affect the absorption but does not significantly impact the overall drug efficacy.
Contra-indications
- Active liver disease
- Pregnancy
- Breastfeeding
- Hypersensitivity to atorvastatin or any of its components
- Concomitant use of potent CYP3A4 inhibitors
Adverse effects
- Myopathy
- Rhabdomyolysis
- Elevated liver enzymes
- Gastrointestinal disturbances
- Headache
- Muscle pain
- Fatigue
- Increased blood glucose levels
Interactions
- CYP3A4 inhibitors (e.g., erythromycin, ketoconazole, HIV protease inhibitors)
- CYP3A4 inducers (e.g., rifampicin, carbamazepine)
- Other lipid-lowering therapies (e.g., gemfibrozil)
- Warfarin and other anticoagulants
- Certain antiretrovirals
Precautions
- History of liver disease
- Heavy alcohol consumption
- Hypothyroidism
- Renal impairment
- Diabetes mellitus
- Muscle disorders
Pregnancy
Atorvastatin is contraindicated in pregnancy. It may cause fetal harm.
Breast-feeding
Atorvastatin is contraindicated during breastfeeding as it can pass into breast milk and may affect the nursing infant.
Storage
Store at room temperature, away from light and moisture. Keep out of reach of children.
Formulations
- Tablets: 10 mg, 20 mg, 40 mg, 80 mg
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.