lovastatin (Rx)

Brand and Other Names:Mevacor, Altoprev
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Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

and lovastatin

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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

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            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
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            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.

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            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)
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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.