Close
New

Medscape is available in 5 Language Editions – Choose your Edition here.

 

lovastatin (Rx)Brand and Other Names:Mevacor, Altoprev

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablets, extended-release

  • 10mg
  • 20mg
  • 40mg
  • 60mg

tablets

  • 10mg
  • 20mg
  • 40mg
more...

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

  • 10mg
  • 20mg
  • 40mg
  • 60mg

tablets

  • 10mg
  • 20mg
  • 40mg
more...

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

Next

Interactions

Interaction Checker

lovastatin and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
             activity indicator 
            Previous
            Next

            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

            Previous
            Next

            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

            Increased blood sugar and glycosylated hemoglobin (HbA1c) levels reported with statin intake

            Rhabdomyolysis, risk of myopathy: Risk increased by coadministration CYP3A4 inhibitors or other drugs that cause myopathy

            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

            Heavy alcohol use, history of liver disease, renal failure

            Discontinue if markedly elevated CPK levels occur or myopathy is diagnosed or suspected; also, temporarily withhold in any patient experiencing an acute or serious condition predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis; hypotension; major surgery; trauma; severe metabolic, endocrine, or electrolyte disorders; uncontrolled epilepsy)

            Rare reports of immune-mediated necrotizing myopathy (IMNM), characterized by increased serum creatine kinase that persists despite discontinuation of statin

            Obtain baseline liver enzyme tests before initiating and then periodically thereafter

            Brand Altocor renamed Altoprev due to confusion with Advicor

            Previous
            Next

            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.

            more...
            Previous
            Next

            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)
            Previous
            Next

            Images

            Previous
            Next

            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            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.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Add or Remove Plans
            Plans for
            Select State:
            Non-Medicare PlansMedicare Plans

            Select a box to add or remove a plan.

            Select a class to view formulary status for similar drugs

            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
             
             
             
            All material on this website is protected by copyright, Copyright © 1994-2016 by WebMD LLC. This website also contains material copyrighted by 3rd parties.