Atorvastatin (Monograph)
Brand name: Lipitor
Drug class: HMG-CoA Reductase Inhibitors
- Statins
VA class: CV350
Molecular formula: ( C33H34FN2O5)2 • Ca • H2O
CAS number: 134523-03-8
Introduction
Antilipemic agent; hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor (i.e., statin).
Uses for Atorvastatin
Reduction in Risk of Cardiovascular Events
Adjunct to diet and lifestyle modifications in patients without clinical evidence of CHD who have multiple risk factors (e.g., age, smoking, hypertension, low HDL-cholesterol concentrations, family history of early CHD) to reduce the risk of MI, stroke, or angina and the risk of undergoing revascularization procedures.
Adjunct to diet and lifestyle modifications in patients without clinical evidence of CHD who have type 2 diabetes mellitus and multiple risk factors (e.g., retinopathy, albuminuria, smoking, hypertension) to reduce the risk of MI or stroke.
Adjunct to diet and lifestyle modifications in patients with clinical evidence of CHD to reduce the risk of nonfatal MI, fatal and nonfatal stroke, angina, or hospitalization for CHF, and the risk of undergoing revascularization procedures.
May use in fixed combination with amlodipine when treatment with both atorvastatin (for prevention of cardiovascular events) and amlodipine (for hypertension and/or CAD) is appropriate.
Extensive evidence demonstrates that statins can substantially reduce LDL-cholesterol concentrations and associated risk of atherosclerotic cardiovascular disease (ASCVD); may be used for secondary prevention or primary prevention in high-risk patients.
AHA/ACC cholesterol management guideline states that lifestyle modification is the foundation of ASCVD risk reduction. Patients with established ASCVD or high risk of ASCVD should also be treated with a statin.
Because relative ASCVD risk reduction is correlated with degree of LDL-cholesterol lowering, use maximum tolerated intensity of a statin to achieve greatest benefit. High-intensity statin therapy (defined as reducing LDL-cholesterol concentrations by ≥50%) is recommended; if high-intensity statin therapy not possible (e.g., because of a contraindication or intolerable adverse effect), may consider moderate-intensity statin therapy (defined as reducing LDL-cholesterol concentrations by 30–49%). AHA/ACC considers atorvastatin 40–80 mg daily to be a high-intensity statin and atorvastatin 10–20 mg daily to be a moderate-intensity statin.
The addition of a nonstatin drug (e.g., ezetimibe, PCSK9 inhibitor) to statin therapy may be considered in certain high-risk patients who require further reduction in LDL-cholesterol concentrations, particularly if there is evidence from randomized controlled studies suggesting that the addition of the nonstatin drug further reduces ASCVD events.
When considering whether to initiate statin therapy for primary prevention, AHA/ACC recommends an individualized approach and shared decision making between patient and clinician. According to the guidelines, statin therapy may be considered in certain high-risk groups such as adults 20–75 years of age with LDL cholesterol ≥190 mg/dL, adults 40–75 years of age with diabetes mellitus, adults 40–75 years of age without diabetes mellitus but with LDL-cholesterol levels ≥70 mg/dL and an estimated 10-year ASCVD risk ≥7.5%, and adults 40–75 years of age with chronic kidney disease (not treated with dialysis or transplantation) and LDL-cholesterol concentrations of 70–189 mg/dL who have a 10-year ASCVD risk ≥7.5%.
Dyslipidemias
Adjunct to nondrug therapies (e.g., dietary management) in adults to decrease elevated serum total cholesterol, LDL-cholesterol, apolipoprotein B (apo B), and triglyceride concentrations, and to increase HDL-cholesterol concentrations in the management of primary hypercholesterolemia (heterozygous familial and nonfamilial) or mixed dyslipidemia (Fredrickson type IIa or IIb). May use in combination with ezetimibe for additive antilipemic effects. Also used in combination with fenofibrate to decrease triglyceride concentrations and increase HDL-cholesterol concentrations in patients with mixed dyslipidemia and CHD (or CHD risk equivalents) who are on optimal statin therapy; however, no incremental benefit on cardiovascular morbidity and mortality beyond that provided by statin monotherapy.
Adjunct to nondrug therapies (e.g., dietary management) to decrease elevated serum total cholesterol, LDL-cholesterol, and apo B concentrations in the management of heterozygous familial hypercholesterolemia in boys and postmenarchal girls 10–17 years of age who, despite an adequate trial of dietary management, have a serum LDL-cholesterol concentration of ≥190 mg/dL or a serum LDL-cholesterol concentration of ≥160 mg/dL and either a family history of premature cardiovascular disease or ≥2 other cardiovascular risk factors.
Adjunct to nondrug therapies (e.g., dietary management) for the management of primary dysbetalipoproteinemia (Fredrickson type III).
Adjunct to nondrug therapies (e.g., dietary management) for the management of elevated serum triglyceride concentrations (Fredrickson type IV).
Reduction of elevated serum total and LDL-cholesterol concentrations in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering therapies (e.g., plasma LDL-apheresis) or when such therapies are not available. May use in combination with ezetimibe for additive antilipemic effects.
Has reduced total and LDL-cholesterol concentrations in patients with hypercholesterolemia associated with or exacerbated by renal transplantation† [off-label] undergoing use of protease inhibitors† [off-label].
Has reduced total and LDL-cholesterol concentrations in hypercholesterolemic patients undergoing peritoneal dialysis† [off-label].
May use in fixed combination with amlodipine when treatment with both atorvastatin (for dyslipidemias) and amlodipine (for hypertension and/or CAD) is appropriate.
Atorvastatin Dosage and Administration
General
Patient Monitoring
- Antilipemic Therapy
-
Manufacturer recommends obtaining lipoprotein concentrations within 2–4 weeks following initiation and/or titration of atorvastatin and adjusting dosage accordingly. AHA/ACC cholesterol management guideline recommends obtaining lipoprotein concentrations within 4–12 weeks following initiation of statin therapy and after dosage changes (to assess response and adherence); monitoring should continue every 3–12 months thereafter as clinically indicated.
-
Periodically reinforce adherence to lifestyle modifications. Antilipemic therapy is an adjunct to, not a substitute for, lifestyle modification therapies that reduce the risk of ASCVD.
Administration
Oral Administration
Administer orally at any time of day without regard to meals.
Dosage
Available as atorvastatin calcium; dosage expressed in terms of atorvastatin.
Dosage modifications may be necessary when used concomitantly with certain drugs (see Specific Drugs and Foods under Interactions).
Pediatric Patients
Dyslipidemias
Heterozygous Familial Hypercholesterolemia
OralChildren 10–17 years of age: Initially, 10 mg once daily.
Adjust dosage at intervals of ≥4 weeks until the desired effect on lipoprotein concentrations is observed or a daily dosage of 20 mg is reached.
Adults
Reduction in Risk of Cardiovascular Events
Oral
Use maximally tolerated statin intensity to achieve optimal ASCVD risk reduction. High-intensity statin therapy (defined as reducing LDL-cholesterol concentrations by ≥50%) is preferred; if high-intensity statin therapy not possible (e.g., because of a contraindication or intolerable adverse effect), may consider moderate-intensity statin therapy (defined as reducing LDL-cholesterol concentrations by 30–49%).
The AHA/ACC guideline panel considers atorvastatin 40–80 mg daily to be a high-intensity statin and atorvastatin 10–20 mg daily to be a moderate-intensity statin.
Dyslipidemias
Primary Hypercholesterolemia (Heterozygous Familial and Nonfamilial) or Mixed Dyslipidemia
OralInitially, 10 or 20 mg once daily.
Patients who require reductions of >45% in LDL-cholesterol concentration: May initiate therapy with 40 mg once daily.
Usual maintenance dosage: 10–80 mg once daily.
Homozygous Familial Hypercholesterolemia
Oral10–80 mg once daily.
Atorvastatin/Amlodipine Fixed-combination Tablets (Caduet)
OralPatients currently receiving atorvastatin in combination with amlodipine: Use fixed combination as a substitute for the individually titrated drugs. Can switch to the fixed-combination preparation containing corresponding individual doses of atorvastatin and amlodipine; alternatively, can increase the dosage of one or both components for additional antihypertensive, antianginal, and/or antilipemic effects.
Patients currently receiving either atorvastatin or amlodipine: Use fixed combination to provide additional therapy. Select atorvastatin and amlodipine doses independently.
Patients currently receiving neither atorvastatin nor amlodipine: Use fixed combination to initiate treatment in patients requiring therapy for dyslipidemias and hypertension and/or angina. Select atorvastatin and amlodipine doses independently.
Prescribing Limits
Pediatric Patients
Dyslipidemias
Oral
Children 10–17 years of age: Maximum 20 mg daily.
Special Populations
Hepatic Impairment
No specific dosage recommendations. (See Hepatic Impairment under Cautions and see Special Populations under Pharmacokinetics.)
Renal Impairment
Dosage modification not required.
Geriatric Patients
No specific dosage recommendations; however, use with caution. (See Geriatric Use under Cautions.)
Cautions for Atorvastatin
Contraindications
-
Active liver disease, including unexplained, persistent elevations of serum aminotransferases.
-
Lactation.
-
Known hypersensitivity to atorvastatin or any ingredient in the formulation.
Warnings/Precautions
Musculoskeletal Effects
Myopathy (defined as muscle pain or weakness in conjunction with CK [CPK] concentration increases >10 times the ULN) reported occasionally.
Rhabdomyolysis with acute renal failure secondary to myoglobinuria reported rarely.
Immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, reported rarely in patients receiving statins. Characterized by proximal muscle weakness and elevated CK concentrations that persist despite discontinuance of statin therapy, necrotizing myopathy without substantial inflammation, and improvement following therapy with immunosuppressive agents.
Risk of myopathy or rhabdomyolysis increased in geriatric patients (≥65 years of age) and in patients with uncontrolled hypothyroidism or renal impairment.
Certain drug or food interactions also may increase risk of myopathy and/or rhabdomyolysis. (See Interactions.)
May consider periodic monitoring of CK concentrations; however, there is no assurance that such monitoring will prevent severe myopathy.
AHA/ACC recommends measurement of CK levels in patients with severe statin-associated muscle symptoms; however, routine monitoring is not useful.
Consider myopathy in any patient with diffuse myalgias, muscle tenderness or weakness, and/or marked increases in CK concentrations.
Discontinue therapy if serum CK concentrations become markedly elevated or if myopathy is diagnosed or suspected.
Temporarily withhold or discontinue therapy in any patient experiencing an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (e.g., severe acute infection; hypotension; major surgery; trauma; severe metabolic, endocrine, or electrolyte disorders; uncontrolled seizures).
Hepatic Effects
Increases in serum aminotransferase (AST, ALT) concentrations reported. Concentrations returned to or near pretreatment levels following dosage reduction or therapy interruption or discontinuance. Not associated with jaundice or other clinical manifestations.
Fatal and nonfatal hepatic failure reported rarely.
Perform liver function tests before initiation of therapy and as clinically indicated (e.g., presence of manifestations suggestive of liver damage ). Serious statin-related liver injury is rare and unpredictable, and routine periodic monitoring of liver enzymes does not appear to be effective in detecting or preventing serious liver injury. AHA/ACC cholesterol management guideline states that it is reasonable to obtain liver function tests in patients with symptoms of hepatotoxicity (e.g., unusual fatigue or weakness, loss of appetite, abdominal pain, dark colored urine, yellowing of skin or sclera); however, routine monitoring not recommended.
If serious liver injury with clinical manifestations and/or hyperbilirubinemia or jaundice occurs, promptly interrupt atorvastatin therapy. If an alternate etiology is not found, do not restart atorvastatin.
Hyperglycemic Effects
Increases in HbA1c and fasting serum glucose concentrations reported. Possible increased risk of developing diabetes. May need to monitor glucose concentrations following initiation of statin therapy.
AHA/ACC cholesterol management guideline states that in patients with increased risk of diabetes mellitus or new-onset diabetes mellitus, statin therapy and lifestyle modifications should be continued to reduce risk of ASCVD.
Endogenous Steroid Production
Statins interfere with cholesterol synthesis and theoretically may blunt adrenal and/or gonadal steroid production.
No effects on basal plasma cortisol concentration or adrenal reserve observed with atorvastatin. Effects on male fertility or on pituitary-gonadal axis in premenopausal women not fully established.
Caution advised if a statin or another antilipemic agent is used concomitantly with drugs that may decrease concentrations or activity of endogenous steroid hormones (e.g. ketoconazole, spironolactone, cimetidine).
Cognitive Impairment
Cognitive impairment (e.g., memory loss, forgetfulness, amnesia, memory impairment, confusion) reported rarely.
Generally nonserious and reversible, with variable times to symptom onset (1 day to years) and resolution (median of 3 weeks following discontinuance of therapy). Not associated with fixed or progressive dementia (e.g., Alzheimer’s disease) or clinically important cognitive decline. Not associated with any specific statin, patient's age, statin dosage, or concomitant drug therapy.
FDA states that cardiovascular benefits of statins outweigh the small increased risk of cognitive impairment.
If manifestations consistent with cognitive impairment occur, National Lipid Association (NLA) statin safety assessment task force recommends evaluating and managing patients appropriately.
Use in Patients with Recent Stroke or TIA
In hypercholesterolemic patients without clinically evident CHD who had a stroke or TIA within the past 1–6 months, long-term (median of 4.9 years) therapy with high-dose atorvastatin (80 mg daily) associated with higher incidence of hemorrhagic stroke compared with placebo. Risk is increased in patients with history of hemorrhagic or lacunar stroke.
Increases in aminotransferase or CK concentrations (≥3 or >10 times the ULN, respectively) reported more frequently in such patients receiving high-dose atorvastatin compared with placebo. Diabetes also reported more frequently in such patients receiving high-dose atorvastatin.
Role as Adjunct Therapy
Prior to institution of antilipemic therapy, vigorously attempt to control serum cholesterol by appropriate dietary regimens, weight reduction, exercise, and treatment of any underlying disorder that might be the cause of lipid abnormality.
Use of Fixed Combinations
When used in fixed combination with amlodipine, consider cautions, precautions, contraindications, and interactions associated with amlodipine.
Specific Populations
Pregnancy
All statins were previously contraindicated in pregnant women because fetal risk was thought to outweigh any possible benefit. However, the totality of evidence to date indicates limited potential for statins to cause malformations and other adverse embryofetal effects; FDA has therefore requested removal of the contraindication. Most pregnant patients should still discontinue statins because of the possibility of fetal harm; however, some patients (e.g., those with homozygous familial hypercholesterolemia or established cardiovascular disease) may benefit from continued therapy. Consider patient's individual risks and benefits.
Patients who become pregnant or suspect that they are pregnant while receiving a statin should notify their clinician; clinician should advise patient on the appropriate course of action.
Increased risk of miscarriage reported in pregnant women exposed to statins; however, not clear whether drug-related or due to other confounding factors.
Lactation
Distributed into milk in rats; may distribute into milk in humans. Use is contraindicated in nursing women; women who require atorvastatin therapy should not breast-feed their infants. Many patients can stop statin therapy temporarily until breast-feeding is complete; patients who require ongoing statin treatment should not breast-feed and should use alternatives such as infant formula.
Pediatric Use
Safety and efficacy not established in prepubertal children or in children <10 years of age. Advise adolescent girls to use effective and appropriate contraceptive methods during therapy to reduce the likelihood of unintended pregnancy.
Safety and efficacy of atorvastatin in fixed combination with amlodipine not established in children.
Geriatric Use
No overall differences in efficacy or safety relative to younger adults, but increased sensitivity cannot be ruled out. (See Special Populations under Pharmacokinetics.)
Use with caution, since age ≥65 years is a predisposing factor for myopathy.
Patients >75 years of age may have a higher risk of adverse effects and lower adherence to therapy; consider expected benefits versus adverse effects before initiating statin therapy in this population.
Safety and efficacy of atorvastatin in fixed combination with amlodipine not established in geriatric patients.
Hepatic Impairment
Use with caution in patients who consume substantial amounts of alcohol and/or have a history of liver disease.
Contraindicated in patients with active liver disease or unexplained, persistent increases in serum aminotransferase concentrations.
Renal Impairment
Dosage modification not necessary in patients with renal impairment. However, monitor more closely for adverse musculoskeletal effects, since history of renal impairment may be a risk factor for development of rhabdomyolysis.
Safety and efficacy not established in patients with end-stage renal disease (ESRD); hemodialysis not expected to substantially enhance clearance since atorvastatin is extensively bound to plasma proteins.
Common Adverse Effects
Nasopharyngitis, arthralgia, diarrhea, pain in extremity, urinary tract infection, dyspepsia, nausea, musculoskeletal pain, muscle spasms, myalgia, insomnia, pharyngolaryngeal pain.
Drug Interactions
Metabolized by CYP3A4; does not inhibit CYP3A4.
When used in fixed combination with amlodipine, consider interactions associated with amlodipine. No formal drug interaction studies to date with fixed-combination preparation.
Drugs and Foods Affecting Hepatic Microsomal Enzymes
Inhibitors of CYP3A4: Potential pharmacokinetic interaction (variable increases in plasma atorvastatin concentrations); increased risk of myopathy or rhabdomyolysis. Carefully monitor for unexplained muscle pain, tenderness, or weakness, particularly following initiation of atorvastatin therapy or an increase in dosage of either drug. (See Specific Drugs and Foods under Interactions.)
Inducers of CYP3A4: Potential pharmacokinetic interaction (variable reductions in plasma atorvastatin concentrations). (See Specific Drugs and Foods under Interactions.)
Drugs Transported by Organic Anion Transport Polypeptide 1B1
Inhibitors of organic anion transport polypeptide (OATP) 1B1: Potential pharmacokinetic interaction (increased bioavailability of atorvastatin).
Specific Drugs and Foods
Drug |
Interaction |
Comments |
---|---|---|
Amlodipine |
Modest increase in atorvastatin exposure |
Not clinically relevant |
Antacids |
Decreased plasma atorvastatin concentrations |
|
Antifungals, azoles |
Increased risk of myopathy or rhabdomyolysis Itraconazole: Increased atorvastatin peak plasma concentration and AUC |
Weigh benefits against risks of concomitant use; carefully monitor for muscle pain, tenderness, or weakness, particularly during initial months of therapy and following an increase in dosage of either drug Itraconazole: Use lowest necessary dosage of atorvastatin; do not exceed atorvastatin dosage of 20 mg daily |
Bile acid sequestrants |
Additive cholesterol-lowering effects Decreased absorption of atorvastatin |
Administer statins 1 hour before or 4 hours after the bile acid sequestrant |
Colchicine |
Myopathy, including rhabdomyolysis, reported |
Use concomitantly with caution |
Cyclosporine |
Increased atorvastatin peak plasma concentration and AUC; increased risk of myopathy or rhabdomyolysis |
Avoid concomitant use |
Digoxin |
Increased plasma digoxin concentrations |
Monitor appropriately |
Efavirenz |
Possible variable reductions in plasma atorvastatin concentrations |
|
Fibric acid derivatives (e.g., fenofibrate, gemfibrozil) |
Increased risk of myopathy Fenofibrate: Slight increase in atorvastatin AUC Gemfibrozil: Increased atorvastatin AUC |
Gemfibrozil: Avoid concomitant use Other fibric acid derivatives (e.g., fenofibrate): Use concomitantly with caution and only if benefits outweigh risks; consider lower initial and maintenance dosages of atorvastatin (i.e., low- or moderate-intensity statin therapy); carefully monitor for muscle pain, tenderness, or weakness, particularly during initial months of therapy and following an increase in dosage of either drug |
Grapefruit juice |
Increased atorvastatin peak plasma concentration and AUC; more substantial increases in atorvastatin peak plasma concentration and/or AUC following ingestion of large quantities (≥750–1200 mL daily) of grapefruit juice Ingestion of large quantities (>1 L daily) of grapefruit juice may increase risk of myopathy |
|
HCV antivirals |
Glecaprevir and pibrentasvir: Plasma concentrations of atorvastatin increased by 8.3-fold Elbasvir and grazoprevir: Plasma concentrations of atorvastatin increased by 1.9-fold |
Glecaprevir and pibrentasvir: Concomitant use not recommended Elbasvir and grazoprevir: Do not exceed atorvastatin dosage of 20 mg daily |
HIV protease inhibitors |
Increased atorvastatin peak plasma concentration and AUC; increased risk of myopathy or rhabdomyolysis |
Weigh benefits against risks of concomitant use; carefully monitor for unexplained muscle pain, tenderness, or weakness, particularly during initial months of therapy and following an increase in dosage of either drug Ritonavir-boosted darunavir, fosamprenavir or ritonavir-boosted fosamprenavir, or ritonavir-boosted saquinavir: Use concomitantly with caution; use lowest necessary dosage of atorvastatin; do not exceed atorvastatin dosage of 20 mg daily Lopinavir/ritonavir: Use concomitantly with caution; use lowest necessary dosage of atorvastatin Nelfinavir: Monitor closely; use lowest necessary dosage of atorvastatin and do not exceed atorvastatin dosage of 40 mg daily Ritonavir-boosted tipranavir: Avoid concomitant use |
Letermovir |
Increased exposure of atorvastatin; magnitude of interaction may be greater when letermovir is coadministered with cyclosporine |
Do not exceed atorvastatin dosage of 20 mg daily Use of atorvastatin not recommended in patients receiving both letermovir and cyclosporine |
Lomitapide |
Increased peak plasma concentration and AUC of atorvastatin acid |
Adjustment of atorvastatin dosage not required; however, do not exceed lomitapide dosage of 30 mg daily |
Macrolides (i.e., clarithromycin, erythromycin) |
Clarithromycin, erythromycin: Increased atorvastatin peak plasma concentration and AUC; increased risk of myopathy or rhabdomyolysis |
Weigh benefits against risks of concomitant use; carefully monitor for unexplained muscle pain, tenderness, or weakness, particularly during initial months of therapy and following an increase in dosage of either drug Clarithromycin: Use concomitantly with caution; use lowest necessary dosage of atorvastatin; do not exceed atorvastatin dosage of 20 mg daily Erythromycin: Use concomitantly with caution; consider using lower initial and maintenance dosages of atorvastatin |
Niacin (antilipemic dosages [≥1 g daily]) |
Increased risk of myopathy Increased risk of severe adverse effects (disturbances in glycemic control requiring hospitalization, development of diabetes mellitus, adverse GI effects, myopathy, gout, rash, skin ulceration, infection, bleeding) with concomitant use of niacin (1.5–2 g daily) and simvastatin (40–80 mg daily, with or without ezetimibe) |
Weigh benefits against risks of concomitant use Use concomitantly with caution; consider using lower initial and maintenance dosages of atorvastatin; carefully monitor patients for unexplained muscle pain, tenderness, or weakness, particularly during initial months of atorvastatin therapy or following an increase in dosage of either drug |
Omega-3-acid ethyl esters |
No effect on rate or extent of exposure to atorvastatin, 2-hydroxyatorvastatin, or 4-hydroxyatorvastatin at steady state |
|
Oral contraceptives |
Increased peak plasma concentrations and AUC of ethinyl estradiol and norethindrone |
Caution when selecting an oral contraceptive |
Rifampin |
Variable effects on plasma atorvastatin concentrations; because delayed administration of atorvastatin following administration of rifampin associated with substantial reductions in plasma atorvastatin concentrations |
Administer simultaneously |
Warfarin |
No clinically important effect on PT |
Some experts recommend closer monitoring of INR when statin therapy is initiated or adjusted |
Atorvastatin Pharmacokinetics
Absorption
Bioavailability
Rapidly absorbed following oral administration; undergoes extensive first-pass metabolism in the liver.
Peak plasma concentrations attained at 1–2 hours.
Absolute bioavailability is approximately 14%.
Evening administration associated with a decrease in the extent of absorption; however, antilipemic activity remains unchanged.
Onset
Therapeutic response usually is apparent within 2 weeks; maximal response occurs within 4 weeks.
Food
Food decreases rate and extent of absorption but does not alter antilipemic effects.
Special Populations
Hepatic impairment (Child-Pugh class A and B) or alcoholic liver disease: Substantially increased concentrations.
Geriatric patients: Peak plasma concentration and AUC are 40 and 30% higher, respectively, in geriatric individuals (≥65 years of age) compared with younger adults.
Distribution
Extent
Statins are distributed mainly to the liver.
Distributes into milk in rats; may distribute into human milk.
Plasma Protein Binding
≥98% (principally albumin).
Elimination
Metabolism
Extensively metabolized in the liver, mainly by CYP3A4, to active metabolites.
Elimination Route
Excreted principally in feces; <2% of a dose excreted in urine.
Half-life
Approximately 14 hours.
Stability
Storage
Oral
Tablets
Atorvastatin: 20–25°C.
Atorvastatin/amlodipine fixed combination: 25°C (may be exposed to 15–30°C).
Actions
-
Selectively and competitively inhibits HMG-CoA reductase, causing subsequent reduction in hepatic cholesterol synthesis. Reduces serum concentrations of total cholesterol, LDL-cholesterol, apo B, triglycerides, VLDL-cholesterol, IDL-cholesterol, and non-HDL-cholesterol, and increases serum concentrations of HDL-cholesterol and apolipoprotein A-1.
-
Statins may slow progression of and/or induce regression of atherosclerosis in coronary and/or carotid arteries; modulate BP in hypercholesterolemic patients with hypertension; and possess anti-inflammatory activity.
Advice to Patients
-
Importance of adhering to nondrug therapies and measures, including adherence to a heart-healthy diet, regular exercise, avoidance of tobacco products, and maintenance of a healthy weight.
-
Importance of periodic monitoring of lipoprotein profile to determine goal attainment.
-
Risk of myopathy and/or rhabdomyolysis; risk is increased with higher dosages or when used concomitantly with certain drugs. Importance of patients promptly reporting any unexplained and/or persistent muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever, or if manifestations persist after discontinuance of therapy.
-
Risk of adverse hepatic effects. Importance of promptly reporting any symptoms suggestive of liver injury (e.g., fatigue, anorexia, right upper abdominal discomfort, dark urine, jaundice).
-
Risk of nonserious, reversible cognitive impairment (e.g., memory loss, forgetfulness, amnesia, memory impairment, confusion).
-
Risk of increased glucose concentrations and development of type 2 diabetes; may need to monitor glucose concentrations following initiation of statin therapy.
-
Importance of advising women to contact their clinician if they become pregnant during therapy.
-
Importance of avoiding breast-feeding during therapy. If the patient has a lipid disorder and is breast-feeding, importance of contacting a clinician to discuss other antilipemic treatment options.
-
Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.
-
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Oral |
Tablets, film-coated |
10 mg (of atorvastatin)* |
Atorvastatin Calcium Tablets |
|
Lipitor |
Pfizer |
|||
20 mg (of atorvastatin)* |
Atorvastatin Calcium Tablets |
|||
Lipitor |
Pfizer |
|||
40 mg (of atorvastatin)* |
Atorvastatin Calcium Tablets |
|||
Lipitor |
Pfizer |
|||
80 mg (of atorvastatin)* |
Atorvastatin Calcium Tablets |
|||
Lipitor |
Pfizer |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes |
Dosage Forms |
Strengths |
Brand Names |
Manufacturer |
---|---|---|---|---|
Oral |
Tablets, film-coated |
10 mg (of atorvastatin) with Amlodipine Besylate 2.5 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|
Caduet |
Pfizer |
|||
10 mg (of atorvastatin) with Amlodipine Besylate 5 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
10 mg (of atorvastatin) with Amlodipine Besylate 10 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
20 mg (of atorvastatin) with Amlodipine Besylate 2.5 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
20 mg (of atorvastatin) with Amlodipine Besylate 5 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
20 mg (of atorvastatin) with Amlodipine Besylate 10 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
40 mg (of atorvastatin) with Amlodipine Besylate 2.5 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
40 mg (of atorvastatin) with Amlodipine Besylate 5 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
40 mg (of atorvastatin) with Amlodipine Besylate 10 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
80 mg (of atorvastatin) with Amlodipine Besylate 5 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
|||
80 mg (of atorvastatin) with Amlodipine Besylate 10 mg (of amlodipine)* |
Atorvastatin Calcium and Amlodipine Besylate Tablets |
|||
Caduet |
Pfizer |
AHFS DI Essentials™. © Copyright 2024, Selected Revisions December 13, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
† Off-label: Use is not currently included in the labeling approved by the US Food and Drug Administration.
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