II. Indications
- See Hyperlipidemia Management for formal criteria
- See Statin
- Hyperlipidemia
- Primary of vascular disease progression (e.g. CAD, CVA, DM, CKD, PAD)
- Atorvastatin is a preferred Statin in Renal Insufficiency
III. Contraindications
- See Statin
- Drug Interactions
- Pregnancy (Teratogen)
- Acute Liver Failure or decompensated Cirrhosis
IV. Mechanism
- See Statin
V. Efficacy
- See Statin
- Atorvastatin 10 mg lowers LDL 38% (recommended starting dose)
- Atorvastatin 20 mg lowers LDL 43 to 46%
- Atorvastatin 40 mg lowers LDL 50 to 51%
- Atorvastatin 80 mg lowers LDL 54 to 60%
- Triglycerides lowered 40%
VI. Adverse Effects
- See Statin
- See Statin-Induced Myopathy
VII. Safety
- Pregnancy Category X
- Contraindicated in Lactation
VIII. Pharmacokinetics
- See Statin
- Undergoes first pass metabolism as with most Statins (except Pravastatin)
-
Protein binding
- As with most Statins (except Pravastatin), Atorvastatin is 90% Protein bound
- Cytochrome P450 Metabolism
IX. Dosing: Adults
- Specific LDL and HDL targets have been replaced with high-intensity Statin if 10 year Cardiovascular Risk >20%
- High intensity Statin (age <75 years with 10 year Cardiovascular Risk >20%)
- Atorvastatin 40-80 mg orally daily
- Low intensity Statin (age >75 years, or Statin intolerant)
- Atorvastatin 10-20 mg orally daily
X. Dosing: Children
- May use in age 10 years old and older
- Start 10 mg orally daily
- Maximum: 20 mg/day
XI. Monitoring
XII. Drug Interactions (See Contraindications above)
- See Statin
-
CYP3A4 Inhibitors
- Azole Antifungals (Intraconazole, Ketoconazole - 10-20 fold increase in Statin serum levels)
- Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
- Avoid with Atorvastatin over 20 mg daily
- Calcium Channel Blocker
- Diltiazem (limit to 240 mg daily)
- Remain alert for Statin Myopathy with Atorvastatin
- Verapamil (6-10 fold increase in Statin serum levels)
- Remain alert for Statin Myopathy with Atorvastatin
- Diltiazem (limit to 240 mg daily)
- Grapefruit juice increases some Statin levels
- Drugs affected moderately: Atorvastatin
- Limit Grapefruit juice to 8-16 ounces daily (effects more likely to manifest at 32 ounces)
- Limit juice timing to opposite Statin dose
- Take juice at night, if Statin taken in morning
- Drugs affected moderately: Atorvastatin
- Azole Antifungals (Intraconazole, Ketoconazole - 10-20 fold increase in Statin serum levels)
-
CYP3A4/organic anion transporting polypeptide inhibitors
- Cyclosporine (10-20 fold increase in Statin serum levels)
- Avoid with Atorvastatin over 10 mg daily
- Macrolides (Erythromycin, Clarithromycin - 6-10 fold increase in Statin serum levels)
- Avoid with Atorvastatin over 20 mg daily
- Azithromycin appears to be safe with Statins
- Protease inibitors (Atazanavir, Ritonavir, Lopinavir/Ritonavir)
- Avoid with Atorvastatin over 20 mg daily
- Cyclosporine (10-20 fold increase in Statin serum levels)
-
CYP3A4/CYP2C9 Inhibitor
- Amiodarone
- Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
- Caution with Atorvastatin (consider dose adjustment)
- Warfarin (Increased INR and bleeding risk)
- Lower risk with Atorvastatin (compared with other Statins)
- Amiodarone
- CYP2C9, CYP2C19/oragnic anion transporting polypeptide inhibitors
- Other interactions
- Mibefradil (Posicor)
- Niacin
- Alcohol
- Increases risk of liver enzyme elevations
XIII. Resources
- See Statin
- Atorvastatin (DailyMed)
XIV. References
- (2017) Presc Lett 24(11): 62
- (2012) Presc Lett 19(5): 25
- (2012) Presc Lett, Characteristics of Various Statins, #280502
- Carpenter (2019) Am Fam Physician 99(9):558-64 [PubMed]
- Chong (2001) Am J Med 111:390-400 [PubMed]
- Crouch (2001) Am Fam Physician 63(2):309-20 [PubMed]
- Gillett (2011) Am Fam Physician 83(6): 711-6 [PubMed]
- Jones (1998) Am J Cardiol 81:582-7 [PubMed]
- Sasaki (1998) Clin Ther 20:539-48 [PubMed]
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atorvastatin (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
ATORVASTATIN 10 MG TABLET | Generic | $0.03 each |
ATORVASTATIN 20 MG TABLET | Generic | $0.04 each |
ATORVASTATIN 40 MG TABLET | Generic | $0.07 each |
ATORVASTATIN 80 MG TABLET | Generic | $0.10 each |
lipitor (on 3/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
LIPITOR 10 MG TABLET | Generic | $0.03 each |
LIPITOR 20 MG TABLET | Generic | $0.04 each |
LIPITOR 40 MG TABLET | Generic | $0.07 each |
Ontology: atorvastatin (C0286651)
Definition (CHV) | a kind of cholesterol lowering drug |
Definition (NCI) | A synthetic lipid-lowering agent. Atorvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. Atorvastatin also increases the number of LDL receptors on hepatic cell surfaces to enhance uptake and catabolism of LDL and reduces LDL production and the number of LDL particles. This agent lowers plasma cholesterol and lipoprotein levels and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. (NCI04) |
Definition (NCI_NCI-GLOSS) | The active ingredient in a drug used to lower the amount of cholesterol in the blood and to prevent stroke, heart attack, and angina (chest pain). It is also being studied in the prevention and treatment of some types of cancer and other conditions. Atorvastatin blocks an enzyme that helps make cholesterol in the body. It also causes an increase in the breakdown of cholesterol. It is a type of HMG-CoA reductase inhibitor and a type of statin. |
Definition (CSP) | a synthetic lipid-lowering agent; an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis. |
Definition (PDQ) | A synthetic lipid-lowering agent. Atorvastatin competitively inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. Atorvastatin also increases the number of LDL receptors on hepatic cell surfaces to enhance uptake and catabolism of LDL and reduces LDL production and the number of LDL particles. This agent lowers plasma cholesterol and lipoprotein levels and modulates immune responses by suppressing MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=460239&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=460239&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C28837" NCI Thesaurus) |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C065179 |
SnomedCT | 391791009, 108600003, 373444002 |
LNC | LP171386-8 |
English | atorvastatin, (betaR,deltaR)-2-(p-Fluorophenyl)-beta,delta-dihydroxy-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-pyrrole-1-heptanoic Acid, (betaR,deltaR)-2-(4-Fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic Acid, atorvastatin [Chemical/Ingredient], liptonorm, ATORVASTATIN, Atorvastatin - chemical (substance), Atorvastatin - chemical, Atorvastatin, Atorvastatin (product), Atorvastatin (substance) |
Spanish | atorvastatina (producto), atorvastatina (sustancia), atorvastatina |
Ontology: Lipitor (C0593906)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C065179 |
English | Lipitor, lipitor |