Dosing & Uses
Dosage Forms & Strengths
tablets, extended-release
- 20mg
- 40mg
- 60mg
tablets
- 10mg
- 20mg
- 40mg
Hypercholesterolemia
Mevacor (immediate-release): 20 mg PO qDay with evening meal initially, or may divide daily dose BID; adjust dose at 4-week intervals if increase required; not to exceed 80 mg/day
Altoprev (extended-release): 10-60 mg PO qHS
Dosing Considerations
Coadministration with danazol, diltiazem, or verapamil: Do not exceed 20 mg lovastatin daily
Coadministration with amiodarone: Do not exceed 40 mg lovastatin daily
Avoid large quantities of grapefruit juice (>1 qt/day)
Overdose management
- Adverse drug reactions from overdose may include peripheral neuropathy, diarrhea, increased K+, myopathy, rhabdomyolysis, acute renal failure, elevated LFTs, eye lens opacities
- Treatment is supportive
Dosing Modifications
Renal impairment (severe; CrCl <30 mL/min): Doses >20 mg/day should be carefully considered and, if deemed necessary, implemented cautiously
Dosage Forms & Strengths
tablets, extended-release
- 20mg
- 40mg
- 60mg
tablets
- 10mg
- 20mg
- 40mg
Heterozygous Familial Hypercholesterolemia
10-17 years: 20-40 mg PO qDay; not to exceed 40 mg/day
Initiate with 10 mg/day if patient requires smaller LDL-C reduction
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
CPK elevation (11%)
1-10%
Flatulence (4-5%)
Abdominal pain (2-3%)
Constipation (2-3%)
Diarrhea (2-3%)
Myalgia (2-3%)
Nausea (2-3%)
Dyspepsia (1-2%)
Weakness (1-2%)
Blurred vision (0.8-1%)
Rash (0.8-1%)
Muscle cramps (0.6-1%)
Dizziness (0.5-1%)
<1%
Dermatomyositis
Increased LFTs
Hepatotoxicity
Myopathy
Rhabdomyolysis
Postmarketing Reports
Interstitial lung disease
Warnings
Contraindications
Hypersensitivity to lovastatin or other components
Active liver disease, or unexplained elevated transaminases
Pregnancy, lactation
Concomitant administration with strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, cobicistat, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin, and nefazodone)
Cautions
Nonserious and reversible cognitive side effects may occur
Avoid coadministration with cyclosporine or gemfibrozil; caution with other fibrates or lipid-lowering doses of niacin (≥1 g/day) because of increased risk for myopathy
Use caution in heavy alcohol use, history of liver disease, or renal failure
Obtain baseline liver enzyme tests before initiating and then periodically thereafter
Increases in HbA1c and fasting serum glucose levels reported
HMG-CoA reductase inhibitor shown to reduce plasma testosterone response to HCG; effects of HMG-CoA reductase inhibitors on male fertility not studied in adequate numbers of male patients
Effects of therapy, if any, on pituitary-gonadal axis in premenopausal women are unknown; patients who develop clinical evidence of endocrine dysfunction should be evaluated appropriately
Use caution if an HMG-CoA reductase inhibitor or other agent used to lower cholesterol levels is administered to patients also receiving other drugs (e.g., spironolactone, cimetidine) that may decrease levels or activity of endogenous steroid hormones
Risk of myopathy increased by coadministration of CYP3A4 inhibitors or other drugs that cause myopathy
Myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria
- Increased risk can occur at any dose level, but increases in dose-dependent manner
- Predisposing factors for myopathy include advanced age (≥65 years), female gender, renal impairment, and inadequately treated hypothyroidism
- Immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, reported with statin use
- IMNM is characterized by muscle biopsy showing necrotizing myopathy without significant inflammation improvement with immunosuppressive agents, proximal muscle weakness, and elevated serum creatine kinase, which persist despite discontinuation of statin treatment
- Treatment with immunosuppressive agents may be required
- Advice all patients starting therapy or whose dose is being increased, about the risk of myopathy, including rhabdomyolysis
- Patients should report promptly any unexplained muscle pain, tenderness, or weakness particularly if accompanied by malaise or fever or if muscle signs and symptoms persist after discontinuing therapy; additional neuromuscular and serologic testing may be necessary
- Therapy should be discontinued immediately if myopathy is diagnosed or suspected
- Discontinue therapy if markedly elevated creatine kinase (CK) levels occur or if myopathy diagnosed or suspected
- Therapy should be temporarily withheld in any patient experiencing an acute or serious condition predisposing to development of renal failure secondary to rhabdomyolysis, eg, sepsis; hypotension; dehydration; major surgery; trauma; severe metabolic, endocrine, and electrolyte disorders; or uncontrolled epilepsy
- Consider risk of IMNM carefully prior to initiation of a different statin
- If therapy is initiated with a different statin, monitor for signs and symptoms of IMNM
Pregnancy & Lactation
Pregnancy category: X
Lactation: Contraindicated; unsafe
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
HMG-CoA reductase inhibitor; inhibits the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase
Absorption
Bioavailability: 5% (Mevacor)
Onset: 3 d (Mevacor)
Duration: 4-6 wk (Mevacor)
Max effect: 4-6 wk (Mevacor)
Peak plasma time: 2-4 hr; 14 hr (ext-rel Altoprev)
Peak plasma concentration: 7.8 ng/mL; 5.5 ng/mL (ext-rel Altoprev)
AUC: 45 ng.hr/mL; 77 ng.hr/mL (ext-rel Altoprev)
Distribution
Protein bound: 95% (Mevacor)
Metabolism
Extensive first pass in liver; activation to beta-hydroxyacid by nonenzymatic/nonspecific hydrolysis; major CYP3A4 substrate
Metabolite: Beta-hydroxyacid derivative (active) and others
Elimination
Half-life: 1.1-1.7 hr (Mevacor)
Excretion (Mevacor): Feces (83%), urine (10% urine)
Pharmacogenomics
SLCO1B1 (OATP1B1) CC genotype significantly increases AUCs of parent drug and metabolites compared with the CT or TT genotypes
This polymorphism is proposed to reduced transport into the liver, the main site of statin metabolism and elimination, resulting in elevated plasma concentrations
SLCO1B1 polymorphism is thought to have a lesser effect on the more hydrophilic statins (eg, rosuvastatin, fluvastatin) compared with those that are more lipophilic (eg, atorvastatin, pravastatin, simvastatin)
Other genetic polymorphisms of elimination (eg, CYP450, P-glycoprotein) for each individual drug must also be considered to explain variability for statin clearance among patients that exhibit SCLO1B1 polymorphism
SLCO1B1 CC genotype is most common in Caucasians and Asians (15%)
Risk of myopathy is 2.6- to 4.3-fold higher if the C allele is present and is 16.9-fold higher in CC homozygotes compared with TT homozygotes
Genetic testing laboratories
- Optivia Biotechnology, Inc (http://optiviabio.com)
Images
Patient Handout
Formulary
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