Dosing & Uses
Dosage Forms & Strengths
tablets, extended-release
- 20mg
- 40mg
- 60mg
tablets
- 10mg
- 20mg
- 40mg
Hypercholesterolemia
Mevacor (immediate-release): 20 mg PO qDay with evening meal initially, or may divide daily dose BID; adjust dose at 4-week intervals if increase required; not to exceed 80 mg/day
Altoprev (extended-release): 10-60 mg PO qHS
Dosing Considerations
Coadministration with danazol, diltiazem, or verapamil: Do not exceed 20 mg lovastatin daily
Coadministration with amiodarone: Do not exceed 40 mg lovastatin daily
Avoid large quantities of grapefruit juice (>1 qt/day)
Overdose management
- Adverse drug reactions from overdose may include peripheral neuropathy, diarrhea, increased K+, myopathy, rhabdomyolysis, acute renal failure, elevated LFTs, eye lens opacities
- Treatment is supportive
Dosing Modifications
Renal impairment (severe; CrCl <30 mL/min): Doses >20 mg/day should be carefully considered and, if deemed necessary, implemented cautiously
Dosage Forms & Strengths
tablets, extended-release
- 20mg
- 40mg
- 60mg
tablets
- 10mg
- 20mg
- 40mg
Heterozygous Familial Hypercholesterolemia
10-17 years: 20-40 mg PO qDay; not to exceed 40 mg/day
Initiate with 10 mg/day if patient requires smaller LDL-C reduction
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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 (92)
- 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.
- isavuconazonium sulfate
lovastatin will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. 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.
Adverse Effects
>10%
CPK elevation (11%)
1-10%
Flatulence (4-5%)
Abdominal pain (2-3%)
Constipation (2-3%)
Diarrhea (2-3%)
Myalgia (2-3%)
Nausea (2-3%)
Dyspepsia (1-2%)
Weakness (1-2%)
Blurred vision (0.8-1%)
Rash (0.8-1%)
Muscle cramps (0.6-1%)
Dizziness (0.5-1%)
<1%
Dermatomyositis
Increased LFTs
Hepatotoxicity
Myopathy
Rhabdomyolysis
Postmarketing Reports
Interstitial lung disease
Warnings
Contraindications
Hypersensitivity to lovastatin or other components
Active liver disease, or unexplained elevated transaminases
Concomitant administration with strong CYP3A4 inhibitors (eg, itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, cobicistat, boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin, and nefazodone)
Cautions
Nonserious and reversible cognitive side effects may occur
Avoid coadministration with cyclosporine or gemfibrozil; caution with other fibrates or lipid-lowering doses of niacin (≥1 g/day) because of increased risk for myopathy
Use caution in heavy alcohol use, history of liver disease, or renal failure
Obtain baseline liver enzyme tests before initiating and then periodically thereafter
Increases in HbA1c and fasting serum glucose levels reported
HMG-CoA reductase inhibitor shown to reduce plasma testosterone response to HCG; effects of HMG-CoA reductase inhibitors on male fertility not studied in adequate numbers of male patients
Effects of therapy, if any, on pituitary-gonadal axis in premenopausal women are unknown; patients who develop clinical evidence of endocrine dysfunction should be evaluated appropriately
Use caution if an HMG-CoA reductase inhibitor or other agent used to lower cholesterol levels is administered to patients also receiving other drugs (e.g., spironolactone, cimetidine) that may decrease levels or activity of endogenous steroid hormones
Risk of myopathy increased by coadministration of CYP3A4 inhibitors or other drugs that cause myopathy
Myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria
- Increased risk can occur at any dose level, but increases in dose-dependent manner
- Predisposing factors for myopathy include advanced age (≥65 years), female gender, renal impairment, and inadequately treated hypothyroidism
- Immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, reported with statin use
- IMNM is characterized by muscle biopsy showing necrotizing myopathy without significant inflammation improvement with immunosuppressive agents, proximal muscle weakness, and elevated serum creatine kinase, which persist despite discontinuation of statin treatment
- Treatment with immunosuppressive agents may be required
- Advice all patients starting therapy or whose dose is being increased, about the risk of myopathy, including rhabdomyolysis
- Patients should report promptly any unexplained muscle pain, tenderness, or weakness particularly if accompanied by malaise or fever or if muscle signs and symptoms persist after discontinuing therapy; additional neuromuscular and serologic testing may be necessary
- Therapy should be discontinued immediately if myopathy is diagnosed or suspected
- Discontinue therapy if markedly elevated creatine kinase (CK) levels occur or if myopathy diagnosed or suspected
- Therapy should be temporarily withheld in any patient experiencing an acute or serious condition predisposing to development of renal failure secondary to rhabdomyolysis, eg, sepsis; hypotension; dehydration; major surgery; trauma; severe metabolic, endocrine, and electrolyte disorders; or uncontrolled epilepsy
- Consider risk of IMNM carefully prior to initiation of a different statin
- If therapy is initiated with a different statin, monitor for signs and symptoms of IMNM
Pregnancy & Lactation
Pregnancy
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.Pharmacology
Mechanism of Action
HMG-CoA reductase inhibitor; inhibits the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase
Absorption
Bioavailability: 5% (Mevacor)
Onset: 3 d (Mevacor)
Duration: 4-6 wk (Mevacor)
Max effect: 4-6 wk (Mevacor)
Peak plasma time: 2-4 hr; 14 hr (ext-rel Altoprev)
Peak plasma concentration: 7.8 ng/mL; 5.5 ng/mL (ext-rel Altoprev)
AUC: 45 ng.hr/mL; 77 ng.hr/mL (ext-rel Altoprev)
Distribution
Protein bound: 95% (Mevacor)
Metabolism
Extensive first pass in liver; activation to beta-hydroxyacid by nonenzymatic/nonspecific hydrolysis; major CYP3A4 substrate
Metabolite: Beta-hydroxyacid derivative (active) and others
Elimination
Half-life: 1.1-1.7 hr (Mevacor)
Excretion (Mevacor): Feces (83%), urine (10% urine)
Pharmacogenomics
SLCO1B1 (OATP1B1) CC genotype significantly increases AUCs of parent drug and metabolites compared with the CT or TT genotypes
This polymorphism is proposed to reduced transport into the liver, the main site of statin metabolism and elimination, resulting in elevated plasma concentrations
SLCO1B1 polymorphism is thought to have a lesser effect on the more hydrophilic statins (eg, rosuvastatin, fluvastatin) compared with those that are more lipophilic (eg, atorvastatin, pravastatin, simvastatin)
Other genetic polymorphisms of elimination (eg, CYP450, P-glycoprotein) for each individual drug must also be considered to explain variability for statin clearance among patients that exhibit SCLO1B1 polymorphism
SLCO1B1 CC genotype is most common in Caucasians and Asians (15%)
Risk of myopathy is 2.6- to 4.3-fold higher if the C allele is present and is 16.9-fold higher in CC homozygotes compared with TT homozygotes
Genetic testing laboratories
- Optivia Biotechnology, Inc (http://optiviabio.com)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Altoprev oral - | 40 mg tablet |  | |
| Altoprev oral - | 20 mg tablet |  | |
| Altoprev oral - | 60 mg tablet |  | |
| lovastatin oral - | 10 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  | |
| lovastatin oral - | 10 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 10 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  | |
| lovastatin oral - | 10 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 40 mg tablet |  | |
| lovastatin oral - | 10 mg tablet |  | |
| lovastatin oral - | 10 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  | |
| lovastatin oral - | 20 mg tablet | | |
| lovastatin oral - | 10 mg tablet |  | |
| lovastatin oral - | 20 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
lovastatin oral
LOVASTATIN - ORAL
(LOE-va-STAT-in)
COMMON BRAND NAME(S): Mevacor
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 as directed by your doctor, usually once daily with your evening meal. Some patients may be directed to take this medication twice daily.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(s) 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 away from light and moisture. Storage temperature ranges differ according to different manufacturers, so consult your pharmacist for more information. 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.
Formulary
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.
