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

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            Contraindicated (30)

            • atazanavir

              atazanavir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • clarithromycin

              clarithromycin will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

              clarithromycin will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Contraindicated.

            • cobicistat

              cobicistat will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Potential for serious reactions such as myopathy including rhabdomyolysis

            • conivaptan

              conivaptan will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • darunavir

              darunavir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Cobicistat is a CYP3A4 inhibitor; contraindicated with CYP3A4 substrates for which elevated plasma concentrations are associated with serious and/or life-threatening events.

            • erythromycin base

              erythromycin base will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • erythromycin ethylsuccinate

              erythromycin ethylsuccinate will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • erythromycin lactobionate

              erythromycin lactobionate will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • erythromycin stearate

              erythromycin stearate will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • fosamprenavir

              fosamprenavir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • idelalisib

              idelalisib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • indinavir

              indinavir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

              indinavir will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Contraindicated.

            • isoniazid

              isoniazid will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • itraconazole

              itraconazole will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of lovastatin with itraconazole is contraindicated during and 2 weeks after of itraconazole treatment.

            • ketoconazole

              ketoconazole will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • lonafarnib

              lonafarnib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • lopinavir

              lopinavir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • mifepristone

              mifepristone increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Contraindicated due to increased risk of rhabdomyolysis.

            • nefazodone

              nefazodone will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • nelfinavir

              nelfinavir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

              lovastatin will increase the level or effect of nelfinavir by P-glycoprotein (MDR1) efflux transporter. Contraindicated.

            • nicardipine

              nicardipine will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • ombitasvir/paritaprevir/ritonavir & dasabuvir

              ombitasvir/paritaprevir/ritonavir & dasabuvir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Increased risk of myopathy, including rhabdomyolysis

            • posaconazole

              posaconazole will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • quinidine

              quinidine will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            • red yeast rice

              lovastatin, red yeast rice. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. May increase creatine kinase levels and increase risk of myopathy or rhabdomyolysis; red yeast rice contains monocolin K (reportedly identical to lovastatin).

            • ritonavir

              ritonavir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

              lovastatin will increase the level or effect of ritonavir by P-glycoprotein (MDR1) efflux transporter. Contraindicated.

            • saquinavir

              lovastatin will increase the level or effect of saquinavir by P-glycoprotein (MDR1) efflux transporter. Contraindicated.

              saquinavir increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis.

            • tipranavir

              tipranavir increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. This interaction is the net effect of tipranavir being coadministered with ritonavir (boosted therapy); increased risk of myopathy including rhabdomyolysis.

            • voriconazole

              voriconazole will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Strong CYP3A4 inhibitors increase systemic statin exposure and risk of myopathy, including rhabdomyolysis

            Serious - Use Alternative (75)

            • abametapir

              abametapir will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

            • afatinib

              lovastatin increases levels of afatinib by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. Reduce afatinib daily dose by 10 mg if not tolerated when coadministered with P-gp inhibitors.

            • amiodarone

              amiodarone will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Do not exceed 40 mg of lovastatin

            • apalutamide

              apalutamide will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • aprepitant

              aprepitant will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • armodafinil

              armodafinil will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • artemether/lumefantrine

              artemether/lumefantrine will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • bosentan

              bosentan will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • butabarbital

              butabarbital will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • butalbital

              butalbital will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • carbamazepine

              carbamazepine will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • cimetidine

              cimetidine will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • colchicine

              colchicine, lovastatin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Increased risk of rhabdomyolysis (incl a fatality).

            • cyclosporine

              cyclosporine will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Do not exceed 20 mg/day of lovastatin

            • darifenacin

              darifenacin will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • dasatinib

              dasatinib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • dexamethasone

              dexamethasone will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • diltiazem

              diltiazem will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Do not exceed 20 mg/day of lovastatin

            • efavirenz

              efavirenz will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • eluxadoline

              lovastatin increases levels of eluxadoline by decreasing metabolism. Avoid or Use Alternate Drug. Decrease eluxadoline dose to 75 mg PO BID if coadministered with OATP1B1 inhibitors. .

            • enzalutamide

              enzalutamide will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • erdafitinib

              erdafitinib will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If coadministration unavoidable, separate administration by at least 6 hr before or after administration of P-gp substrates with narrow therapeutic index.

            • etravirine

              etravirine will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • everolimus

              lovastatin will increase the level or effect of everolimus by P-glycoprotein (MDR1) efflux transporter. Contraindicated.

            • fenofibrate

              fenofibrate, lovastatin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Fenofibrate may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs. Do not exceed 20 mg/day of lovastatin.

            • fenofibrate micronized

              fenofibrate micronized, lovastatin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Fenofibrate may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs. Do not exceed 20 mg/day of lovastatin.

            • fenofibric acid

              fenofibric acid, lovastatin. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Fenofibrate may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs. Do not exceed 20 mg/day of lovastatin.

            • fexinidazole

              fexinidazole will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • fluconazole

              fluconazole will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • fluvoxamine

              fluvoxamine will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • fosphenytoin

              fosphenytoin will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • gemfibrozil

              gemfibrozil, lovastatin. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Avoid or Use Alternate Drug. Gemfibrozil may further increase risk for rhabdomyolysis when added to optimal statin regimen to further decrease TG and increase HDLs. Do not exceed 20 mg/day of lovastatin.

            • glecaprevir/pibrentasvir

              glecaprevir/pibrentasvir increases levels of lovastatin by Other (see comment). Avoid or Use Alternate Drug. Comment: Increased statin concentrations resulting from OATP1B1 inhibition may increase risk of myopathy, including rhabdomyolysis. Coadministration of glecaprevir/pibrentasvir with lovastatin is not recommended.

            • grapefruit

              grapefruit will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid large quantities of grapefruit juice (ie, >1 quart daily)

            • griseofulvin

              griseofulvin will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • hydrocortisone

              hydrocortisone will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • ivosidenib

              ivosidenib will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.

            • lapatinib

              lapatinib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • lasmiditan

              lasmiditan increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • lomitapide

              lomitapide increases levels of lovastatin by decreasing metabolism. Avoid or Use Alternate Drug. Reduce lovastatin dose by 50% when initiating lomitapide dosing.

            • lumefantrine

              lumefantrine will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • marijuana

              marijuana will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • mesterolone

              mesterolone increases toxicity of lovastatin by decreasing metabolism. Avoid or Use Alternate Drug. Risk of rhabdomyolysis (case reports of combination of danazol and >20 mg/day lovastatin).

            • methylprednisolone

              methylprednisolone will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • metronidazole

              metronidazole will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • miconazole vaginal

              miconazole vaginal will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • modafinil

              modafinil will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nafcillin

              nafcillin will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • nevirapine

              nevirapine will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • niacin

              niacin, lovastatin. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Increased risk of rhabdomyolysis (>1 g/day niacin). Do not exceed 20 mg/day of lovastatin.

            • nifedipine

              nifedipine will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • nilotinib

              nilotinib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • oxcarbazepine

              oxcarbazepine will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • pentobarbital

              pentobarbital will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • phenobarbital

              phenobarbital will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • phenytoin

              phenytoin will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • pomalidomide

              lovastatin increases levels of pomalidomide by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • prednisone

              prednisone will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • primidone

              primidone will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • quinidine

              quinidine will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug.

            • quinupristin/dalfopristin

              quinupristin/dalfopristin will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • rifabutin

              rifabutin will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • rifampin

              rifampin will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • rifapentine

              rifapentine will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated.

            • riociguat

              lovastatin will increase the level or effect of riociguat by decreasing metabolism. Avoid or Use Alternate Drug. Coadministration of riociguat (substrate of CYP isoenzymes 1A1, 2C8, 3A, 2J2) with strong CYP inhibitors may require a decreased initial dose of 0.5 mg PO TID; monitor for signs of hypotension and reduce dose if needed

            • rufinamide

              rufinamide will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • secobarbital

              secobarbital will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • sotorasib

              sotorasib will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If use is unavoidable, refer to the prescribing information of the P-gp substrate for dosage modifications.

            • St John's Wort

              St John's Wort will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • tepotinib

              tepotinib will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Avoid or Use Alternate Drug. If concomitant use unavoidable, reduce the P-gp substrate dosage if recommended in its approved product labeling.

            • topiramate

              topiramate will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • tucatinib

              tucatinib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • verapamil

              verapamil will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Do not exceed 20 mg of lovastatin

            • voxelotor

              voxelotor will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            • zafirlukast

              zafirlukast will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            Monitor Closely (91)

            • amiodarone

              amiodarone will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • apalutamide

              apalutamide will decrease the level or effect of lovastatin by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and may decrease systemic exposure of drugs that are UGT substrates.

            • atorvastatin

              atorvastatin will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • avapritinib

              lovastatin will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • axitinib

              lovastatin increases levels of axitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • azithromycin

              azithromycin will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • bazedoxifene/conjugated estrogens

              lovastatin will increase the level or effect of bazedoxifene/conjugated estrogens by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • berotralstat

              berotralstat will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor or titrate P-gp substrate dose if coadministered.

            • bosutinib

              bosutinib increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

            • ceritinib

              lovastatin increases levels of ceritinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • cholestyramine

              cholestyramine decreases levels of lovastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • cholic acid

              lovastatin increases toxicity of cholic acid by decreasing elimination. Modify Therapy/Monitor Closely. Avoid concomitant use of inhibitors of the bile salt efflux pump (BSEP). May exacerbate accumulation of conjugated bile salts in the liver and result in clinical symptoms. If concomitant use is necessary, monitor serum transaminases and bilirubin.

            • clobetasone

              lovastatin will increase the level or effect of clobetasone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • clotrimazole

              clotrimazole will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • conjugated estrogens

              lovastatin will increase the level or effect of conjugated estrogens by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • conjugated estrogens, vaginal

              lovastatin will increase the level or effect of conjugated estrogens, vaginal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • crizotinib

              crizotinib increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Dose reduction may be needed for coadministered drugs that are predominantly metabolized by CYP3A.

              crizotinib increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • crofelemer

              crofelemer increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • dabrafenib

              dabrafenib will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.

            • daptomycin

              lovastatin, daptomycin. Either increases toxicity of the other by Other (see comment). Modify Therapy/Monitor Closely. Comment: Coadministration of daptomycin with HMG-CoA reductase inhibitors may increase CPK levels and risk for myopathy; consider temporary suspension of HMG-CoA reductase inhibitors during daptomycin therapy.

            • deferasirox

              deferasirox will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • deflazacort

              lovastatin will increase the level or effect of deflazacort by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dexamethasone

              lovastatin will increase the level or effect of dexamethasone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • docetaxel

              lovastatin will increase the level or effect of docetaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • dronedarone

              dronedarone will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Monitor for signs and symptoms of myopathy in patients receiving dronedarone concurrently with lovastatin.

              dronedarone will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • duvelisib

              duvelisib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.

            • elagolix

              elagolix will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              elagolix decreases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

            • elbasvir/grazoprevir

              elbasvir/grazoprevir increases levels of lovastatin by unknown mechanism. Modify Therapy/Monitor Closely. If coadministered, use lowest necessary lovastatin dose.

            • eliglustat

              eliglustat increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Monitor therapeutic drug concentrations, as indicated, or consider reducing the dosage of the P-gp substrate and titrate to clinical effect.

            • encorafenib

              encorafenib, lovastatin. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.

            • eslicarbazepine acetate

              eslicarbazepine acetate will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Dose adjustment of some statins may be needed if a clinically significant change in lipids is noted.

            • estradiol

              lovastatin will increase the level or effect of estradiol by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • finerenone

              lovastatin will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.

            • flibanserin

              lovastatin will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Increased flibanserin adverse effects may occur if coadministered with multiple weak CYP3A4 inhibitors.

            • fostamatinib

              fostamatinib will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Concomitant use of fostamatinib may increase concentrations of P-gp substrates. Monitor for toxicities of the P-gp substrate drug that may require dosage reduction when given concurrently with fostamatinib.

            • fostemsavir

              fostemsavir will increase the level or effect of lovastatin by Other (see comment). Modify Therapy/Monitor Closely. Fostemsavir inhibits OATP1B1/3 transporter. If possible, avoid coadministration or modify dose of OATP1B1/3 substrates coadministered with fostemsavir.

            • glecaprevir/pibrentasvir

              glecaprevir/pibrentasvir will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • hydrocortisone

              lovastatin will increase the level or effect of hydrocortisone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • iloperidone

              iloperidone increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • imatinib

              lovastatin will increase the level or effect of imatinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

              istradefylline will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of P-gp substrates in clinical trials. Consider dose reduction of sensitive P-gp substrates.

            • ivacaftor

              ivacaftor increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Ivacaftor and its M1 metabolite has the potential to inhibit P-gp; may significantly increase systemic exposure to sensitive P-gp substrates with a narrow therapeutic index.

            • ivermectin

              lovastatin will increase the level or effect of ivermectin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ketoconazole

              ketoconazole will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lanthanum carbonate

              lanthanum carbonate decreases levels of lovastatin by cation binding in GI tract. Use Caution/Monitor. Administer statin at least 2 hr before or 2 hr after lanthanum. Monitor serum concentrations.

            • lapatinib

              lapatinib will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lemborexant

              lovastatin will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.

            • letermovir

              lovastatin increases levels of letermovir by increasing metabolism. Use Caution/Monitor. Coadminstration of letermovir, an OATP1B1/3 substrate, with OATP1B1/3 inhibitors may increase letermovir plasma concentrations.

              letermovir increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of letermovir with lovastatin may require a dosage reduction. Closely monitor patients for myopathy and rhabdomyolysis. When letermovir is coadministered with cyclosporine, use of lovastatin is not recommended.

            • lomitapide

              lovastatin increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.

              lomitapide increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing dose when used concomitantly with lomitapide.

            • loperamide

              lovastatin will increase the level or effect of loperamide by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • lorlatinib

              lorlatinib will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • maraviroc

              lovastatin will increase the level or effect of maraviroc by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • midazolam intranasal

              lovastatin will increase the level or effect of midazolam intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Coadministration of mild CYP3A4 inhibitors with midazolam intranasal may cause higher midazolam systemic exposure, which may prolong sedation.

            • mipomersen

              mipomersen, lovastatin. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: Both drugs have potential to increase hepatic enzymes; monitor LFTs.

            • mitotane

              mitotane decreases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • nefazodone

              nefazodone will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nicardipine

              nicardipine will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nifedipine

              nifedipine will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • nilotinib

              lovastatin will increase the level or effect of nilotinib by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • paclitaxel

              lovastatin will increase the level or effect of paclitaxel by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • paclitaxel protein bound

              lovastatin will increase the level or effect of paclitaxel protein bound by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • paliperidone

              lovastatin will increase the level or effect of paliperidone by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • phenobarbital

              phenobarbital will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ponatinib

              ponatinib increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • quercetin

              quercetin will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ranolazine

              ranolazine will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • ribociclib

              ribociclib will increase the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rifampin

              rifampin will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • sacubitril/valsartan

              lovastatin will increase the level or effect of sacubitril/valsartan by Other (see comment). Use Caution/Monitor. The results from an in vitro study with human liver tissue indicate that valsartan is a substrate of the hepatic uptake transporter OATP1B1; coadministration with OATP1B1 inhibitors may increase valsartan systemic exposure

            • sarecycline

              sarecycline will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Monitor for toxicities of P-gp substrates that may require dosage reduction when coadministered with P-gp inhibitors.

            • silodosin

              lovastatin will increase the level or effect of silodosin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • simvastatin

              simvastatin will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • sirolimus

              lovastatin will increase the level or effect of sirolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • St John's Wort

              St John's Wort will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • stiripentol

              stiripentol, lovastatin. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.

              stiripentol will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Modify Therapy/Monitor Closely. Consider reducing the dose of P-glycoprotein (P-gp) substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.

            • tacrolimus

              lovastatin will increase the level or effect of tacrolimus by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • tazemetostat

              tazemetostat will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              lovastatin will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tecovirimat

              tecovirimat will decrease the level or effect of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.

            • ticagrelor

              ticagrelor increases levels of lovastatin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Avoid lovastatin doses greater than 40 mg.

            • tinidazole

              lovastatin will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tolvaptan

              lovastatin will increase the level or effect of tolvaptan by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

              tolvaptan will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • trazodone

              trazodone will decrease the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • tucatinib

              tucatinib will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Consider reducing the dosage of P-gp substrates, where minimal concentration changes may lead to serious or life-threatening toxicities.

            • valsartan

              lovastatin will increase the level or effect of valsartan by Other (see comment). Use Caution/Monitor. The results from an in vitro study with human liver tissue indicate that valsartan is a substrate of the hepatic uptake transporter OATP1B1; coadministration with OATP1B1 inhibitors may increase valsartan systemic exposure

            • vemurafenib

              vemurafenib increases levels of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • verapamil

              verapamil will increase the level or effect of lovastatin by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor. Avoid concomitant use of verapamil and lovastatin if possible. If used together, use lower doses of lovastatin and monitor for lovastatin toxicity (myositis, rhabdomyolysis).

            • vinblastine

              lovastatin will increase the level or effect of vinblastine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vincristine

              lovastatin will increase the level or effect of vincristine by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • vincristine liposomal

              lovastatin will increase the level or effect of vincristine liposomal by P-glycoprotein (MDR1) efflux transporter. Use Caution/Monitor.

            • warfarin

              lovastatin increases effects of warfarin by unknown mechanism. Use Caution/Monitor.

            Minor (13)

            • alvimopan

              lovastatin will increase the level or effect of alvimopan by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.

            • coenzyme Q10

              lovastatin decreases levels of coenzyme Q10 by unspecified interaction mechanism. Minor/Significance Unknown.

            • colestipol

              colestipol decreases levels of lovastatin by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • exenatide injectable solution

              exenatide injectable solution decreases levels of lovastatin by unspecified interaction mechanism. Minor/Significance Unknown.

            • exenatide injectable suspension

              exenatide injectable suspension decreases levels of lovastatin by unspecified interaction mechanism. Minor/Significance Unknown.

            • fexofenadine

              lovastatin will increase the level or effect of fexofenadine by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.

            • isradipine

              isradipine decreases levels of lovastatin by unknown mechanism. Minor/Significance Unknown.

            • liraglutide

              liraglutide decreases levels of lovastatin by unspecified interaction mechanism. Minor/Significance Unknown.

            • loratadine

              lovastatin will increase the level or effect of loratadine by P-glycoprotein (MDR1) efflux transporter. Minor/Significance Unknown.

            • orlistat

              orlistat increases effects of lovastatin by pharmacodynamic synergism. Minor/Significance Unknown.

            • ruxolitinib

              lovastatin will increase the level or effect of ruxolitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • trazodone

              trazodone increases levels of lovastatin by unspecified interaction mechanism. Minor/Significance Unknown.

            • voclosporin

              voclosporin will increase the level or effect of lovastatin by Other (see comment). Minor/Significance Unknown. Information suggests voclosporin (an OATP1B1 inhibitor) may increase in the concentration of OATP1B1 substrates is possible. Monitor for adverse reactions of OATP1B1 substrates when coadministered with voclosporin.

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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

            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

            Owing to HMG-CoA reductase inhibitors decrease cholesterol synthesis and possibly the synthesis of other biologically active substances derived from cholesterol, fetal harm may occur when administered to pregnant females; discontinue therapy as soon as pregnancy is recognized; limited published data are insufficient to determine a drug-associated risk of major congenital malformations or miscarriage

            Contraception

            Advise females of reproductive potential to use effective contraception during treatment

            FDA MedWatch

            • On July 20, 2021, the FDA request to remove the contraindication against HMG-CoA reductase inhibitors in pregnant females
            • Despite the changes, most females found to be pregnant should stop therapy

            Lactation

            There is no available information on effects of drug on breastfed infant or on milk production

            Unknown whether is present in human milk; it has been shown that drugs in this class pass into human milk and atorvastatin is present in rat milk

            Not recommended during treatment

            FDA MedWatch

            • On July 20, 2021, the FDA request to remove the contraindication against HMG-CoA reductase inhibitors in pregnant females
            • Breastfeeding is still not recommended if taking statins; drug may still pass through milk and pose a risk breastfed children
            • For patients with lower risk, temporarily stop statin therapy until breastfeeding ends
            • Patients who are at high risk of heart attack or stroke who require statins after delivery should not breastfeed and should use alternatives such as infant formula

            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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            Images

            BRAND FORM. UNIT PRICE PILL IMAGE
            lovastatin oral
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            10 mg tablet
            lovastatin oral
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            20 mg tablet
            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            40 mg tablet
            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            lovastatin oral
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            20 mg tablet
            lovastatin oral
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            10 mg tablet
            lovastatin oral
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            10 mg tablet
            Altoprev oral
            -
            60 mg tablet
            Altoprev oral
            -
            40 mg tablet
            Altoprev oral
            -
            20 mg tablet

            Copyright © 2010 First DataBank, Inc.

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            Patient Handout

            Patient Education
            lovastatin oral

            LOVASTATIN EXTENDED-RELEASE - ORAL

            (LOE-va-STAT-in)

            COMMON BRAND NAME(S): Altoprev

            USES: Lovastatin is used along with a proper diet to help lower "bad" cholesterol and fats (such as LDL, triglycerides) and raise "good" cholesterol (HDL) in the blood. It belongs to a group of drugs known as "statins." It works by reducing the amount of cholesterol made by the liver. Lowering "bad" cholesterol and triglycerides and raising "good" cholesterol decreases the risk of heart disease and helps prevent strokes and heart attacks.In addition to eating a proper diet (such as a low-cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking. Consult your doctor for more details.

            HOW TO USE: Take this medication by mouth with or without food as directed by your doctor, usually once daily at bedtime.Do not crush or chew extended-release tablets. Doing so can release all of the drug at once, increasing the risk of side effects. Also, do not split the tablets unless they have a score line and your doctor or pharmacist tells you to do so. Swallow the whole or split tablet without crushing or chewing.Dosage is based on your medical condition, response to treatment, age, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Avoid eating grapefruit or drinking grapefruit juice while using this medication unless your doctor instructs you otherwise. Grapefruit can increase the amount of this medication in your bloodstream. Consult your doctor or pharmacist for more details.If you also take certain other drugs to lower your cholesterol (bile acid-binding resins such as cholestyramine or colestipol), take lovastatin at least 1 hour before or at least 4 hours after taking these medications. These products can react with lovastatin, preventing its full absorption.Take this medication regularly in order to get the most benefit from it. Remember to take it at the same time each day. Keep taking this medication even if you feel well. Most people with high cholesterol or triglycerides do not feel sick.It is very important to continue to follow your doctor's advice about diet and exercise. It may take up to 4 weeks before you get the full benefit of this drug.

            SIDE EFFECTS: Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.A very small number of people taking lovastatin may have mild memory problems or confusion. If these rare effects occur, talk to your doctor.Rarely, statins may cause or worsen diabetes. Talk to your doctor about the benefits and risks.This drug may rarely cause muscle problems (which can rarely lead to very serious conditions called rhabdomyolysis and autoimmune myopathy). Tell your doctor right away if you develop any of these symptoms during treatment and if these symptoms persist after your doctor stops this drug: muscle pain/tenderness/weakness (especially with fever or unusual tiredness), signs of kidney problems (such as change in the amount of urine).This medication may rarely cause liver problems. If you notice any of the following rare but serious side effects, tell your doctor right away: yellowing eyes/skin, dark urine, severe stomach/abdominal pain, persistent nausea/vomiting.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

            PRECAUTIONS: Before taking lovastatin, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, alcohol use.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Limit alcoholic beverages. Daily use of alcohol may increase your risk for liver problems, especially when combined with lovastatin. Ask your doctor or pharmacist for more information.Older adults may be more sensitive to the side effects of this drug, especially muscle problems.This medication must not be used during pregnancy. Lovastatin may harm an unborn baby. It is important to prevent pregnancy while taking this medication. Consult your doctor for more details and to discuss the use of reliable forms of birth control (such as condoms, birth control pills) while taking this medication. If you become pregnant or think you may be pregnant, tell your doctor right away.It is unknown if this medication passes into breast milk. Because of the possible risk to the infant, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

            DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: "blood thinners" (such as warfarin), daptomycin, gemfibrozil.Other medications can affect the removal of lovastatin from your body, which may affect how lovastatin works. Examples include certain azole antifungals (such as itraconazole, ketoconazole, posaconazole, voriconazole), cobicistat, colchicine, cyclosporine, delavirdine, macrolide antibiotics (such as clarithromycin, erythromycin), nefazodone, HIV protease inhibitors (such as lopinavir, ritonavir), hepatitis C virus protease inhibitors (such as boceprevir, telaprevir), telithromycin, among others.Do not take any red yeast rice products while you are taking lovastatin since those products may also contain lovastatin. Taking lovastatin and red yeast rice products together can increase your risk of serious muscle and liver problems.

            OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

            NOTES: Do not share this medication with others.Laboratory and/or medical tests (such as blood cholesterol/triglyceride levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

            MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

            STORAGE: Store at room temperature between 68-77 degrees F (20-25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep all medicines away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

            Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

            IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            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.
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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.