Lovastatin

Class: HMG-CoA Reductase Inhibitors
VA Class: CV350
Chemical Name: 2-Methylbutanoic acid [1S - [1α(R*),3α,7β,8β(2S*,4S*),8aβ] - 1,2,3,7,8,8a - hexahydro - 3,7 - dimethyl - 8 - [2 - (tetrahydro - 4 - hydroxy - 6 - oxo - 2H - pyran - 2 - yl)ethyl] - 1 - naphthalenyl ester
Molecular Formula: C₂₄H₃₆O₅
CAS Number: 75330-75-5
Brands: Advicor, Altoprev, Mevacor

Special Alerts:

[Posted 09/30/2008] An FDA analysis provides new evidence that the use of statins does not increase incidence of amyotrophic lateral sclerosis (ALS), a neurodegenerative disease often referred to as “Lou Gehrig’s Disease.” The FDA analysis, undertaken after the agency received a higher than expected number of reports of ALS in patients on statins, is based on data from 41 long-term controlled clinical trials. The results showed no increased incidence of the disease in patients treated with a statin compared with placebo.

The FDA is anticipating the completion of a case-control or epidemiological study of ALS and statin use. Results from this study should be available within 6-9 months. FDA is also examining the feasibility of conducting additional epidemiologic studies to examine the incidence and clinical course of ALS in patients taking statins.

Based on currently available information, health care professionals should not change their prescribing practices for statins and patients should not change their use of statins. For more information visit the FDA website at: and .

Introduction

Antilipemic agent; hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor (i.e., statin).^{1 2 3 4 5}

Uses for Lovastatin

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Prevention of Cardiovascular Events

Adjunct to dietary therapy in patients with no evidence of cardiovascular disease who have normal or moderate elevations of LDL-cholesterol and below-average HDL-cholesterol concentrations to reduce the risk of a first major acute coronary event (i.e., MI, unstable angina) and to reduce the risk of undergoing coronary revascularization procedures.^{1 116}

Adjunct to dietary therapy in patients with clinical evidence of CHD to slow the progression of coronary atherosclerosis.^{1 116}

Dyslipidemias

Adjunct to dietary therapy to decrease elevated serum total and LDL-cholesterol, apolipoprotein B (apo B), and triglyceride concentrations and to increase HDL-cholesterol concentrations in the management of primary hypercholesterolemia and mixed dyslipidemia, including heterozygous familial hypercholesterolemia and other causes of hypercholesterolemia (e.g., polygenic hypercholesterolemia).^{1 2 8 9 18 23 24 29 30 31 32 33 35 36 40 44 49 50 90 116}

Adjunct to dietary therapy 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 years of age who have a serum LDL-cholesterol concentration of ≥190 mg/dL or in those who have a serum LDL-cholesterol concentration of >160 mg/dL and either a family history of premature cardiovascular disease or ≥2 cardiovascular risk factors despite an adequate trial of dietary management.¹

Management of primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia as lovastatin in fixed combination with extended-release niacin (Advicor) in patients receiving lovastatin who require further reductions in triglyceride or increases in HDL-cholesterol concentrations and in those receiving niacin who require further reductions in LDL-cholesterol concentrations.¹¹⁷ Lovastatin in fixed combination with extended-release niacin (Advicor) should not be used as initial antilipemic therapy in the management of hypercholesterolemia.¹¹⁷

Reduction of elevated LDL-cholesterol concentrations in patients with combined hypercholesterolemia and hypertriglyceridemia caused by genotypic familial combined hyperlipidemia,^{1 2 18 19 31 44 50} however, has not been studied in conditions where the major abnormality is elevation of chylomicrons, VLDLs, or IDLs.¹

Reduction of total and LDL-cholesterol concentrations in patients with familial dysbetalipoproteinemia^{34 50 104} or with hypercholesterolemia associated with or exacerbated by diabetes mellitus† (diabetic dyslipidemia),^{50 52} cardiac†^{50 53 54 102} or renal transplantation,†^{50 54 103} nephrotic syndrome† (nephrotic hyperlipidemia),^{27 50 55} or distal ileal bypass surgery†.^{23 33 56}

Reduction of total cholesterol, LDL-cholesterol, and/or apolipoprotein B in patients with hypoalphalipoproteinemia†⁹⁸ or in those with mild endogenous (primary) hypertriglyceridemia and borderline elevated total cholesterol, decreased HDL-cholesterol, and elevated apo B† (type IV hyperlipoproteinemia with elevated total apo B).^{42 43}

Lovastatin Dosage and Administration

General

• 
  

  Patients should be placed on a standard lipid-lowering diet before initiation of lovastatin therapy and should remain on this diet during treatment with the drug.^{1 116 117}

  
  

Administration

Oral Administration

Conventional Tablets

Administer orally with the evening meal.¹

Extended-release Tablets

Administer orally at bedtime.¹¹⁶

Swallow tablets whole; do not divide, crush or chew.¹¹⁶

Lovastatin in Fixed-combination with Extended-release Niacin Tablets

Administer orally at bedtime with a low-fat snack.¹¹⁷

Swallow tablets whole; do not break, crush or chew.¹¹⁷

Increase dosage slowly to minimize symptoms of flushing, pruritus, and GI distress associated with the niacin component; avoid administration on an empty stomach.¹¹⁷ Pretreatment with aspirin or other NSAIA 30 minutes prior to administration may reduce flushing.¹¹⁷

Dosage

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Pediatric Patients

Dyslipidemias

Conventional Tablets

Oral

Children 10-17 years of age: Initially, 10 mg once daily in patients who require small reductions in LDL-cholesterol.¹ In patients who require reductions of ≥20%, initiate therapy at a dosage of 20 mg once daily.¹

Adjust dosage at intervals of ≥ 4 weeks until the desired effect on lipoprotein concentrations is observed.¹ Usual dosage range is 10–40 mg daily.¹

Adults

Prevention of Cardiovascular Events or Dyslipidemias

Conventional Tablets

Oral

Initially, 10 mg once daily in patients who require small reductions in LDL-cholesterol; in those who require reductions of ≥20%, 20 mg once daily.¹

Adjust dosage at intervals of ≥ 4 weeks until the desired effect on lipoprotein concentrations is observed.¹ Usual dosage range is 10–80 mg daily given in 1 or 2 divided doses.¹

Extended-release Tablets

Oral

Initially, dosage is 20, 40, or 60 mg once daily.¹¹⁶ In patients who require small reductions in LDL-cholesterol, initiate therapy at a dosage of 10 mg once daily.¹¹⁶

Adjust dosage at intervals of ≥ 4 weeks until the desired effect on lipoprotein concentrations is observed.¹ Usual dosage range is 10–60 mg once daily.¹¹⁶

Lovastatin in Fixed Combination with Extended-release Niacin Tablets

Oral

Determine dosage by identifying a stable dosage of extended-release niacin (Niaspan).¹¹⁷ Patients receiving niacin preparations other than Niaspan should be switched from their existing niacin therapy to Niaspan and titrated to a stable dosage prior to switching to Advicor.¹¹⁷ Once a stable dosage of Niaspan is reached, switch patients directly to a niacin-equivalent dosage of Advicor.¹¹⁷ In patients currently receiving a stable dosage of lovastatin, add Niaspan and titrate slowly (using the recommended titration schedule) until a stable dosage of niacin has been reached, then switch patients to a niacin-equivalent dosage of Advicor.¹¹⁷

Increase dosage by no more than 500 mg (of the niacin component) at 4-week intervals.¹¹⁷ Usual maintenance dosage ranges from 20 mg of lovastatin and 500 mg of extended-release niacin to 40 mg of lovastatin and 2 g of extended-release niacin once daily.¹¹⁷ In patients in whom therapy with Advicor has been discontinued for an extended period (i.e., >7 days), reinstitute at the lowest available dosage.¹¹⁷ Because of differences in bioavailability, do not substitute 1 tablet of Advicor 1 g/40 mg for 2 tablets of Advicor 500 mg/20 mg, or vice versa.¹¹⁷

Prescribing Limits

Pediatric Patients

Prevention of Cardiovascular Events or Dyslipidemias

Conventional Tablets

Oral

Maximum 40 mg daily.¹

Adults

Prevention of Cardiovascular Events or Dyslipidemias

Conventional Tablets

Oral

Maximum 80 mg daily.¹

Lovastatin in Fixed-combination with Extended-release Niacin Tablets

Oral

Maximum 40 mg of lovastatin and 2 g of extended-release niacin daily.¹¹⁷

Special Populations

Hepatic Impairment

Use with caution in patients who consume substantial amounts of alcohol and/or have a history of liver disease.^{1 116 117} Contraindicated in patients with active liver disease or unexplained, persistent increases in serum aminotransferase concentrations.^{1 116 117}

Renal Impairment

Use with caution in patients with severe renal impairment (Cl_cr < 30 mL/min);^{1 116} dosage increases >20 mg daily should be carefully considered, and if deemed necessary, implemented with extreme caution.^{1 116}

Cautions for Lovastatin

Contraindications

• 
  

  Active liver disease or unexplained, persistent elevations of serum aminotransferases.^{1 116 117}

  
  


• 
  

  Pregnancy or lactation.¹ Administer to women of childbearing age only when such patients are highly unlikely to conceive and have been informed of the potential hazards.^{1 116 117}

  
  


• 
  

  Known hypersensitivity to lovastatin or any ingredient in the formulation.^{1 116 117}

  
  

Warnings/Precautions

Warnings

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Fetal/Neonatal Morbidity and Mortality

Suppression of cholesterol biosynthesis could cause fetal harm.^{1 116 117} Congenital anomalies following intrauterine exposure to statins reported rarely.^{1 116 117}

Administer to women of childbearing age only when such patients are highly unlikely to conceive and have been informed of the potential hazards.^{1 116 117} If the patient becomes pregnant while taking the drug, discontinue therapy and apprise the patient of the potential hazard to the fetus.^{1 116 117}

Hepatic Effects

Associated with increases in serum aminotransferase (AST, ALT) concentrations.^{1 116 117}

Pancreatitis,^{1 116 117} hepatitis (including chronic active hepatitis),^{1 116 117} cholestatic jaundice,^{1 116 117} fatty change in liver,^{1 116 117} increased serum alkaline phosphatase concentrations,^{1 116 117} increased serum γ-glutamyl transpeptidase concentrations,^{1 116 117} increased bilirubin concentrations,^{1 116 117} and, rarely, cirrhosis,^{1 116 117} fulminant hepatic necrosis,^{1 116 117} and hepatoma^{1 116 117} have been reported.^{1 116 117}

In patients receiving conventional or extended-release lovastatin, perform liver function tests before initiation of therapy, at 6 and 12 weeks after initiation of therapy or elevation of dose, and periodically (e.g., semiannually) thereafter.^{1 116} In patients receiving the fixed combination preparation, perform liver function tests before initiation of therapy, at 6 and 12 weeks after initiation of therapy for the first 6 months, and periodically (e.g., semiannually) thereafter.¹¹⁷

Patients who develop increased serum AST/ALT concentrations or manifestations of liver disease should be monitored with a second liver function evaluation to confirm the finding and should receive frequent liver function tests thereafter until the abnormalities return to normal.^{1 116 117} If increases in AST or ALT concentrations of 3 times the ULN or higher persist, discontinue therapy.^{1 116 117}

Musculoskeletal Effects

Myopathy (manifested as muscle pain, tenderness, or weakness and serum creatine kinase [CK, creatine phosphokinase, CPK] concentration increases >10 times the ULN) reported occasionally.^{1 116 117}

Rhabdomyolysis (characterized by muscle pain or weakness with marked increases [>10 times the ULN] in serum CK concentrations and increases in S_cr [usually accompanied by brown urine and urinary myoglobinuria]) with or without acute renal failure secondary to myoglobinuria has been reported;^{1 116 117} rare fatalities have occurred.¹

Risk of myopathy increased in patients receiving higher doses of statins; in patients with multisystem disease (e.g., renal or hepatic impairment); in patients with concurrent serious infections or hypothyroidism; in patients (particularly women) of advanced age (especially >80 years of age); in patients with small body frame and frailty; and in patients undergoing surgery (i.e., during perioperative periods). Risk also may be increased by concomitant administration of cyclosporine, niacin, fibric acid derivatives (e.g., gemfibrozil), macrolide antibiotics (i.e., erythromycin, clarithromycin), certain antifungal azoles (i.e., itraconazole, ketoconazole), alcohol, HIV protease inhibitors, nefazodone, amiodarone, verapamil, and large quantities (>1 quart daily) of grapefruit juice.¹ (See Interactions.)

Measure baseline serum CK concentrations prior to initiation of therapy, particularly in black men or in patients receiving concomitant therapy with fibric acid derivatives.

Obtain serum CK concentrations and compare with baseline concentrations in patients presenting with musculoskeletal symptoms suggestive of myopathy; because hypothyroidism may be a predisposing factor, thyrotropin (thyroid-stimulating hormone, TSH) concentrations also should be obtained in such patients.

Discontinue if myopathy is diagnosed or suspected.^{1 116 117}

Monitor patients weekly if myalgia (muscle pain, tenderness) is present with either no CK elevation or a moderate elevation (3–10 times the ULN) until manifestations improve; discontinue if manifestations worsen.

Dosage reduction or temporary discontinuance may be prudent in patients with muscle discomfort and/or weakness in the presence of progressive elevation of CK concentrations on serial measurements.

Temporarily withhold therapy a few days prior to elective major surgery and when any major medical or surgical condition supervenes.^{1 116 117}

General Precautions

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.^{1 116 117}

CNS Effects

CNS vascular lesions (e.g., perivascular hemorrhage and edema, mononuclear cell infiltration of perivascular spaces, perivascular fibrin deposits and necrosis of small vessels) observed in animals.^{1 116 117}

Ocular Effects

Cataracts and optic nerve degeneration observed in animals.^{1 116 117}

Other Precautions

When used in fixed combination with extended-release niacin, consider the cautions, precautions, and contraindications associated with niacin.¹¹⁷

Specific Populations

Pregnancy

Category X.^{1 116 117} (See Contraindications and also see Fetal/Neonatal Morbidity and Mortality, under Cautions.)

Lactation

Not known whether lovastatin is distributed into milk;^{1 116 117} however, other statins are distributed into milk.^{1 116 117} Use is contraindicated.^{1 116 117}

Pediatric Use

Safety and efficacy of conventional tablets not established in children <10 years of age or in prepubertal children.¹ Advise adolescent girls to use effective and appropriate contraceptive methods during therapy to reduce the likelihood of unintended pregnancy.¹

Safety and efficacy of extended-release or lovastatin in fixed-combination with extended-release niacin tablets have not been established in children or adolescents <20 or 18 years of age, respectively.^{116 117}

Geriatric Use

No substantial differences in safety or efficacy relative to younger adults.^{1 116 117}

Caution in patients (particularly women) of advanced age (especially >80 years of age) and in those with small body frame and frailty.

Hepatic Impairment

Use with caution in patients who consume substantial amounts of alcohol and/or have a history of liver disease.^{1 116 117}

Contraindicated in patients with active liver disease or unexplained, persistent increases in liver function test results.^{1 116 117}

Common Adverse Effects

For conventional and extended-release tablets: GI disturbances (e.g., flatulence, diarrhea, abdominal pain, constipation, nausea, dyspepsia), headache, myalgia, asthenia, blurred vision, rash, dizziness, muscle cramps.^{1 116}

For lovastatin in fixed-combination with extended-release niacin tablets: flushing, infection, headache, pain, flu syndrome, asthenia, back pain, GI disturbances (nausea, diarrhea, abdominal pain, dyspepsia, vomiting), pruritus, rash, hyperglycemia, myalgia.¹¹⁷

Interactions for Lovastatin

Lovastatin is metabolized by CYP3A4 but has no CYP3A4 inhibitory activity.^{1 116}

Specific Drugs and Foods

Drug or Food	Interaction	Comments
Amiodarone	Increased risk of myopathy and/or rhabdomyolysis when used with another statin1	If used concomitantly, lovastatin dosage should not exceed 40 mg daily1
Antileukotrienes (e.g., zileuton)	Inhibition of lovastatin metabolism via CYP3A4, resulting in increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided or undertaken with caution
Anticoagulants, oral (e.g., warfarin)	Bleeding and/or increased PT observed1 116 117	Closely monitor PT until stabilized if lovastatin is initiated or dosage is adjusted in patients receiving a coumarin anticoagulant.1 116 117 Thereafter, monitor PT at intervals usually recommended for patients receiving coumarin anticoagulants1 116 117
Antifungals, azoles (i.e., itraconazole, ketoconazole)	Inhibition of CYP3A4-dependent metabolism of lovastatin, resulting in decreased elimination of lovastatin and increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided.1 If concomitant use is unavoidable, suspend lovastatin therapy during the course of treatment with antifungal.1 117 Avoid concomitant use of lovastatin with other CYP3A4 inhibitors unless benefits of combined therapy outweigh risks1
Cyclosporine	Inhibition of CYP3A4-dependent metabolism of lovastatin, resulting in decreased elimination of lovastatin and increased risk of myopathy and/or rhabdomyolysis1 116	If lovastatin is used concomitantly, initiate lovastatin at 10 mg daily; lovastatin dosage should not exceed 20 mg daily.1 If Advicor is used concomitantly, Advicor dosage should not exceed 20 mg of lovastatin and 1 g of extended-release niacin once daily117
Digoxin	Concomitant use with other statins resulted in increased plasma digoxin concentrations
Diltiazem	Increased plasma lovastatin concentrations
Fibric acid derivatives (e.g., gemfibrozil)	Increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided unless benefits of combined therapy outweigh risks.1 117 If lovastatin is used concomitantly with gemfibrozil, lovastatin dosage should not exceed 20 mg daily.1 If Advicor is used concomitantly, Advicor dosage should not exceed 20 mg of lovastatin and 1 g of extended-release niacin once daily117
Fluvoxamine	Inhibition of lovastatin metabolism via CYP3A4, resulting in increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided or undertaken with caution
Grapefruit juice	Inhibition of CYP3A4-dependent metabolism of lovastatin, resulting in decreased elimination of lovastatin and increased risk of myopathy and/or rhabdomyolysis1 116	Consumption of large quantities (>1 quart daily) of grapefruit juice should be avoided1
HIV protease inhibitors	Inhibition of CYP3A4-dependent metabolism of lovastatin, resulting in decreased elimination of lovastatin and increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided1
Macrolide antibiotics (i.e., clarithromycin, erythromycin)	Inhibition of CYP3A4-dependent metabolism of lovastatin, resulting in decreased elimination of lovastatin and increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided.1 If concomitant use is unavoidable, suspend lovastatin therapy during the course of treatment with the antibiotic.1 117 Avoid concomitant use of lovastatin with other CYP3A4 inhibitors unless benefits of combined therapy outweigh risks1
Metronidazole	Inhibition of lovastatin metabolism via CYP3A4, resulting in increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided or undertaken with caution
Nefazodone	Inhibition of lovastatin metabolism via CYP3A4, resulting in increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided1
Niacin	Increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use with antilipemic dosages (≥1 g daily) of niacin generally should be avoided unless benefits of combined therapy outweigh risks.1 If used concomitantly, lovastatin dosage should not exceed 20 mg daily1
Troleandomycin	Inhibition of lovastatin metabolism via CYP3A4, resulting in increased risk of myopathy and/or rhabdomyolysis1 116	Concomitant use generally should be avoided or undertaken with caution
Verapamil	Increased plasma lovastatin concentrations. Increased risk of myopathy and/or rhabdomyolysis1 116	If used concomitantly, lovastatin dosage should not exceed 40 mg daily1

Lovastatin Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed following oral administration; undergoes extensive first-pass metabolism in the liver.¹ Peak plasma concentrations are attained at 2–4 hours.¹

Absolute bioavailability is <5%.¹

Bioavailability of 1 tablet containing 1 g of extended-release niacin in fixed combination with 40 mg of lovastatin (Advicor 1 g/40 mg) differs from that of 2 tablets each containing 500 mg of extended-release niacin in fixed combination with 20 mg of lovastatin (Advicor 500 mg/20 mg).¹¹⁷ (See Dosage: Lovastatin in Fixed Combination with Extended-release Niacin Tablets, under Dosage and Administration.)

Onset

Therapeutic response usually is apparent within 2 weeks; maximal response occurs within 4–6 weeks.¹

Distribution

Extent

Distributed mainly to the liver; crosses the blood-brain barrier.¹

Lovastatin crosses the placenta.¹ Distributed into milk in rats; not known whether distributed into human milk.¹

Plasma Protein Binding

>95%.¹

Elimination

Metabolism

Metabolized by CYP3A4.¹ Lovastatin has active metabolites.¹

Elimination Route

Excreted in urine (10%) and feces (83%).¹

Half-life

0.5–3 hours.

Special Populations

Renal impairment (Cl_cr 10–30 mL/min) may reduce clearance.¹

Stability

Storage

Oral

Conventional Tablets

Tight, light-resistant containers at 5–30°C.¹

Extended-release Tablets

20–25°C.¹¹⁶ Avoid excessive heat and humidity.¹¹⁶

Lovastatin in Fixed Combination with Extended-release Niacin Tablets

20–25°C.¹¹⁷

ActionsActions

• 
  

  Prodrug requiring hydrolysis in vivo for activity.^{1 116}

  
  


• 
  

  Inhibits HMG-CoA reductase, causing subsequent reduction in hepatic cholesterol synthesis.^{1 116} Reduces serum concentrations of total cholesterol, LDL-cholesterol, apolipoprotein B (apo B), and triglycerides.^{1 116}

  
  


• 
  

  Statins may slow progression of and/or induce regression of atherosclerosis in coronary and/or carotid arteries, modulate blood pressure in hypercholesterolemic patients with hypertension, and possess anti-inflammatory activity.

  
  

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

• 
  

  Importance of informing patients about risks, especially rhabdomyolysis, associated with statins alone or combined with other drugs.^{1 116 117} Importance of patients promptly reporting muscle pain, tenderness, or weakness;^{1 116 117} brown urine; flu-like symptoms; and malaise.

  
  


• 
  

  Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.^{1 116 117} Necessity for clinicians to advise women and adolescent girls to avoid pregnancy (i.e., using effective and appropriate contraceptive methods) during therapy and to advise pregnant women of risk to fetus.^{1 116 117}

  
  


• 
  

  Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.¹

  
  


• 
  

  Importance of adhering to nondrug therapies and measures (i.e., therapeutic life-style changes, including dietary management, weight control, physical activity, and management of potentially contributory disease [e.g., diabetes mellitus]).

  
  


• 
  

  Importance of informing patients of other important precautionary information.^{1 116 117} (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Lovastatin

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets*	10 mg*	Lovastatin Tablets	Carlsbad, Genpharm, Mylan, Purepac, Sandoz, Teva
			Mevacor	Merck
		20 mg*	Lovastatin Tablets	Carlsbad, Genpharm, Mylan, Purepac, Sandoz, Teva
			Mevacor	Merck
		40 mg*	Lovastatin Tablets	Carlsbad, Genpharm, Mylan, Purepac, Sandoz, Teva
			Mevacor	Merck
	Tablets, extended-release	10 mg	Altoprev (with propylene glycol)	Andrx
		20 mg	Altoprev (with propylene glycol)	Andrx
		40 mg	Altoprev (with propylene glycol)	Andrx
		60 mg	Altoprev (with propylene glycol)	Andrx

Lovastatin Combinations

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	20 mg with Extended-release Niacin 500 mg	Advicor (with povidone)	Kos
		20 mg with Extended-release Niacin 750 mg	Advicor (with povidone)	Kos
		20 mg with Extended-release Niacin 1 g	Advicor (with povidone)	Kos
		40 mg with Extended-release Niacin 1 g	Advicor (with povidone)	Kos

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 04/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Advicor 1000-20MG 24-hr Tablets (ABBOTT): 60/$257.99 or 180/$740.96

Advicor 1000-40MG 24-hr Tablets (ABBOTT): 90/$433.97 or 180/$863.95

Advicor 500-20MG 24-hr Tablets (ABBOTT): 90/$330.98 or 180/$650.97

Advicor 750-20MG 24-hr Tablets (ABBOTT): 60/$264.98 or 180/$772.93

Altoprev 20MG 24-hr Tablets (SHIONOGI PHARMA): 30/$239.99 or 90/$705.97

Altoprev 60MG 24-hr Tablets (SHIONOGI PHARMA): 30/$289.99 or 90/$849.97

Lovastatin 10MG Tablets (MYLAN): 45/$47.99 or 90/$55.96

Lovastatin 20MG Tablets (SANDOZ): 30/$22.99 or 90/$59.99

Lovastatin 40MG Tablets (SANDOZ): 30/$35.99 or 90/$99

Mevacor 20MG Tablets (MERCK SHARP &amp; DOHME): 30/$80.16 or 90/$215.92

Mevacor 40MG Tablets (MERCK SHARP &amp; DOHME): 30/$134.69 or 90/$379.44

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions October 01, 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Merck. Mevacor (lovastatin tablets) prescribing information. Whitehouse Station, NJ; 2002 Jun.

2. Merck Sharp & Dohme. Mevacor formulary information. West Point, PA; 1987.

3. United States Pharmacopeial Convention, Inc. USAN and the USP dictionary of drug names. Rockville, MD: United States Pharmacopeial Convention, Inc.; 1988: 311-2.

4. Tobert JA, Hitzenberger G, Kukovetz WR et al. Rapid and substantial lowering of human serum cholesterol by mevinolin (MK-803), an inhibitor of hydroxymethylglutaryl-coenzyme A reductase. Atherosclerosis. 1982; 41:61-5. [IDIS 232675] [PubMed 6918220]

5. Tobert JA, Bell GD, Birtwell J et al. Cholesterol-lowering effect of mevinolin, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase, in healthy volunteers. J Clin Invest. 1982; 69:913-9. [IDIS 148076] [PubMed 6918402]

6. 3-Hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors: a new class of cholesterol-lowering agents. Ann Intern Med. 1987; 107:759-60. Editorial.

7. Stacpoole PW, Alig J. Advances in the treatment of coronary heart disease: fish oils, cholestyramine, and mevinolin. Cardiovasc Clin. 1987; 18:267-79. [PubMed 3300984]

8. Illingworth DR. Mevinolin plus colestipol in therapy for severe heterozygous familial hypercholesterolemia. Ann Intern Med. 1984; 101:598-604. [IDIS 191769] [PubMed 6567462]

9. Illingworth DR, Sexton GJ. Hypocholesterolemic effects of mevinolin in patients with heterozygous familial hypercholesterolemia. J Clin Invest. 1984; 74:1972-8. [IDIS 194234] [PubMed 6569064]

10. Alberts AW, Chen J, Kuron G et al. Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent. Proc Natl Acad Sci USA. 1980; 77:3957-61. [PubMed 6933445]

11. Illingworth RD, Bacon S. Hypolipidemic effects of HMG-CoA reductase inhibitors in patients with hypercholesterolemia. Am J Cardiol. 1987; 60:33-42G. [PubMed 3604942]

12. Illingworth DR. Lipid-lowering drugs: an overview of indications and optimum therapeutic use. Drugs. 1987; 33:259-79. [IDIS 227903] [PubMed 3552597]

13. Brown MS, Goldstein JL. Drugs used in the treatment of hyperlipoproteinemias. In: Gilman AG, Goodman LS, Rall TW et al, eds. Goodman & Gilman’s the pharmacological basis of therapeutics. 7th ed. New York: Macmillan Publishing Company; 1985:827-45.

14. Minsker DH, MacDonald JS, Robertson RT et al. Mevalonate supplementation in pregnant rats suppresses the teratogenicity of mevinolinic acid, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. Teratology. 1983; 28:449-56. [PubMed 6665743]

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16. Cressman MD, Hoogwerf BJ, Moodie DS et al. HMG-CoA reductase inhibitors: a new approach to the management of hypercholesterolemia. Cleveland Clin J Med. 1988; 55:93-100.

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19. East C, Bilheimer DW, Grundy SM. Combination drug therapy for familial combined hyperlipidemia. Ann Intern Med. 1988; 109:25-32. [IDIS 243273] [PubMed 3288029]

20. Reviewers’ comments (personal observations); 1988 July.

21. Dal Pino EA (Merck Sharp & Dohme, West Point, PA): Personal communication; 1988 July.

22.