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Ezetimibe and rosuvastatin: Drug information

Ezetimibe and rosuvastatin: Drug information
(For additional information see "Ezetimibe and rosuvastatin: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Special Alerts
Statin Pregnancy Contraindication Update July 2021

After a comprehensive review of all available data, the FDA is requesting all statin manufacturers to remove the contraindication in the prescribing information against using statins in pregnant patients. Although statin therapy should be discontinued in most pregnant patients, health care providers should consider the ongoing therapeutic needs of the individual patient, especially patients at very high risk of cardiovascular events during pregnancy, such as patients with homozygous familial hypercholesterolemia or those with established cardiovascular disease. Additionally, breastfeeding is still not recommended in patients taking a statin; health care providers should determine whether it is better to temporarily stop statin therapy while breastfeeding or to continue statin therapy and not have the patient breastfeed. If ongoing statin treatment is necessary, infant formula and other alternatives are available. The FDA expects that removing the contraindication will enable health care providers and patients to make individual decisions about benefit and risk, especially for those at very high risk of heart attack or stroke.

Further information is available at https://www.fda.gov/drugs/drug-safety-and-availability/fda-requests-removal-strongest-warning-against-using-cholesterol-lowering-statins-during-pregnancy.

Brand Names: US
  • Roszet
Pharmacologic Category
  • Antilipemic Agent, 2-Azetidinone;
  • Antilipemic Agent, HMG-CoA Reductase Inhibitor
Dosing: Adult

Dosage guidance:

Dosing: Rosuvastatin 20 to 40 mg/day is considered a high-intensity statin (generally reduces low-density lipoprotein cholesterol [LDL-C] by ≥50%). Rosuvastatin 5 to 10 mg/day is considered a moderate-intensity statin (generally reduces LDL-C by ~30% to 49%). Assess response ~1 to 3 months after initiation of therapy or dose adjustment and every 3 to 12 months thereafter (ACC/AHA [Grundy 2019]). In patients of East Asian descent, rosuvastatin exposure can be ~2-fold higher compared to White patients; consider initial dosage reduction and risk versus benefit in East Asian patients not adequately controlled with rosuvastatin 20 mg once daily before increasing dose further (Newman 2019; manufacturer's labeling).

Clinical considerations: Consider combination therapy in patients who do not meet cholesterol treatment goals with dietary modification plus maximally tolerated statin therapy. Refer to individual agents for more information (ACC/AHA [Grundy 2019]).

Homozygous familial hypercholesterolemia

Homozygous familial hypercholesterolemia: Oral: Initial: Dosing range: Ezetimibe 10 mg and rosuvastatin 5 to 40 mg once daily; titrate dose to achieve treatment goals.

Primary hyperlipidemia

Primary hyperlipidemia: Oral: Initial: Dosing range: Ezetimibe 10 mg and rosuvastatin 5 to 40 mg once daily; titrate dose to achieve treatment goals.

Patients switching from coadministration of rosuvastatin (or a different statin) and ezetimibe: Oral: Ezetimibe 10 mg and an equivalent dose of rosuvastatin.

Patients of Asian descent: Oral: Initial: Ezetimibe 10 mg and rosuvastatin 5 mg once daily; consider risk versus benefit in patients not adequately controlled with doses up to ezetimibe 10 mg and rosuvastatin 20 mg once daily.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

CrCl ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.

CrCl <30 mL/minute/1.73 m2: Initial: Ezetimibe 10 mg and rosuvastatin 5 mg once daily; maximum: Ezetimibe 10 mg and rosuvastatin 10 mg once daily.

Hemodialysis: There are no specific dosage adjustments provided in the manufacturer's labeling. Refer to individual agents.

Dosing: Hepatic Impairment: Adult

There are no specific dosage adjustments provided in the manufacturer's labeling; however, systemic exposure of rosuvastatin may be increased in patients with liver disease (increased AUC and Cmax); use is contraindicated in active liver disease or decompensated cirrhosis.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

See individual agents.

Contraindications

Hypersensitivity (eg, anaphylaxis, angioedema, erythema multiforme) to rosuvastatin, ezetimibe, or any component of the formulation; acute liver failure or decompensated cirrhosis.

Warnings/Precautions

Concerns related to adverse effects:

• Diabetes mellitus: Small increases in HbA1c (mean: ~0.1%) and fasting blood glucose have been reported with rosuvastatin; however, the benefits of statin therapy far outweigh the risk of dysglycemia.

• Elevated hepatic transaminases: A higher incidence of elevated transaminases (≥3 × ULN) has been observed with concomitant use of ezetimibe and statins compared to statin monotherapy; transaminase changes were generally not associated with symptoms or cholestasis and returned to baseline with or without discontinuation of therapy. Consider discontinuation of ezetimibe and/or the statin for persistently elevated transaminases (ALT or AST ≥3 × ULN).

• Hematuria/proteinuria: Hematuria (microscopic) and proteinuria have been observed; more commonly reported in adults receiving rosuvastatin 40 mg daily. Typically, transient and not associated with a decrease in renal function. Consider dosage reduction if unexplained hematuria and proteinuria persists.

• Hepatotoxicity: Postmarketing reports of fatal and nonfatal hepatic failure due to rosuvastatin are rare. If serious hepatotoxicity with clinical symptoms and/or hyperbilirubinemia or jaundice occurs during treatment, interrupt therapy. If an alternate etiology is not identified, do not restart rosuvastatin.

• Myopathy/rhabdomyolysis: Rhabdomyolysis with acute renal failure secondary to myoglobinuria and/or myopathy has been reported; patients should be monitored closely. This risk is dose related and is increased with concomitant use of interacting medications. Consult drug interactions database for more detailed information. If concurrent use is warranted, consider lower starting and maintenance doses of rosuvastatin. Use caution in patients with inadequately treated hypothyroidism, patients taking other drugs associated with myopathy (eg, colchicine), patients ≥65 years of age, and women; these patients are predisposed to myopathy. Immune-mediated necrotizing myopathy (IMNM) associated with HMG-CoA reductase inhibitors use has also been reported. Patients should be instructed to report unexplained muscle pain, tenderness, weakness, or brown urine, particularly if accompanied by malaise or fever. Discontinue therapy if markedly elevated CPK levels occur or myopathy is diagnosed/suspected; consider treatment with immunosuppressants and additional neuromuscular and serologic testing. Prior to initiating a different HMG-CoA reductase inhibitor, consider risk of IMNM; monitor closely.

Disease-related concerns:

• Hepatic impairment and/or ethanol use: Use with caution in patients who consume large amounts of ethanol or have a history of liver disease. Use is contraindicated with active liver disease or decompensated cirrhosis.

• Myasthenia gravis: May rarely worsen or precipitate myasthenia gravis (MG); monitor for worsening MG if treatment is initiated (AAN [Narayanaswami 2021]).

• Renal impairment: Dosage adjustment is required in patients with a CrCl <30 mL/minute/1.73 m2 and not receiving hemodialysis.

Special populations:

• Asian population: There is an increased risk of rosuvastatin-associated myopathy in certain subgroups; dosage adjustment is recommended for patients of Asian descent.

• Older adult: Use with caution in patients with advanced age; these patients are more predisposed to myopathy.

• Surgical patients: Based on current research and clinical guidelines, HMG-CoA reductase inhibitors should be continued in the perioperative period for noncardiac and cardiac surgery (ACC/AHA [Fleisher 2014]; ACC/AHA [Hillis 2011]). Perioperative discontinuation of statin therapy is associated with an increased risk of cardiac morbidity and mortality.

Other warnings/precautions:

• Appropriate use: Secondary causes of hyperlipidemia should be ruled out prior to therapy. Rosuvastatin has not been studied when the primary lipid abnormality is chylomicron elevation (Fredrickson types I and V).

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Roszet: Ezetimibe 10 mg and rosuvastatin calcium 5 mg, Ezetimibe 10 mg and rosuvastatin calcium 10 mg, Ezetimibe 10 mg and rosuvastatin calcium 20 mg, Ezetimibe 10 mg and rosuvastatin calcium 40 mg

Generic: Ezetimibe 10 mg and rosuvastatin calcium 10 mg, Ezetimibe 10 mg and rosuvastatin calcium 20 mg, Ezetimibe 10 mg and rosuvastatin calcium 40 mg, Ezetimibe 10 mg and rosuvastatin calcium 5 mg

Generic Equivalent Available: US

Yes

Pricing: US

Tablets (Ezetimibe-Rosuvastatin Oral)

10-5 mg (per each): $3.00

10-10 mg (per each): $3.00

10-20 mg (per each): $3.00

10-40 mg (per each): $3.00

Tablets (Roszet Oral)

10-5 mg (per each): $10.00

10-10 mg (per each): $10.00

10-20 mg (per each): $10.00

10-40 mg (per each): $10.00

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral: Administer at approximately the same time each day. May be administered without regard to meals. Swallow whole; do not chew, crush, or dissolve tablets.

Use: Labeled Indications

Homozygous familial hypercholesterolemia: Alone or as an adjunct to other LDL cholesterol (LDL-C)–lowering therapies to reduce LDL-C in adults with homozygous familial hypercholesterolemia (HoFH).

Primary hyperlipidemia: As an adjunct to diet to reduce LDL-C in adults with primary nonfamilial hyperlipidemia.

Metabolism/Transport Effects

Refer to individual components.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Abiraterone Acetate: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy

Acipimox: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy

Antacids: May decrease the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Apalutamide: May decrease the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Asciminib: May increase the serum concentration of Rosuvastatin. Risk X: Avoid combination

Asunaprevir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy

Atazanavir: May increase the serum concentration of Rosuvastatin. Rosuvastatin may increase the serum concentration of Atazanavir. Management: Initiate rosuvastatin at 5 mg daily and do not exceed rosuvastatin 10 mg daily if coadministered with atazanavir/ritonavir. If combined, monitor for signs and symptoms of myopathy and rhabdomyolysis and for increased atazanavir toxicities. Risk D: Consider therapy modification

BCRP/ABCG2 Inhibitors: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Bile Acid Sequestrants: May decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Risk D: Consider therapy modification

Capmatinib: May increase the serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 10 mg daily when combined with capmatinib. Monitor closely for increased rosuvastatin effects/toxicities (eg, myalgias, rhabdomyolysis) when these agents are combined. Risk D: Consider therapy modification

CarBAMazepine: May decrease the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Cobicistat: May increase the serum concentration of Rosuvastatin. Management: If coadministeed with cobicistat/atazanavir or cobicistat/darunavir, initiate rosuvastatin at the lowest dose. Do not exceed rosuvastatin 10 mg/day with concurrent use of atazanavir/cobicistat or 20 mg/day with concurrent use of darunavir/cobicistat. Risk D: Consider therapy modification

Colchicine: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Colchicine may increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). HMG-CoA Reductase Inhibitors (Statins) may increase the serum concentration of Colchicine. Risk C: Monitor therapy

CycloSPORINE (Systemic): May increase the serum concentration of Rosuvastatin. Management: Limit rosuvastatin to 5 mg daily in patients who are also receiving cyclosporine, and monitor patients for increased rosuvastatin toxicities. Canadian labeling contraindicates concomitant use of rosuvastatin with cyclosporine. Risk D: Consider therapy modification

Daclatasvir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy

DAPTOmycin: HMG-CoA Reductase Inhibitors (Statins) may enhance the adverse/toxic effect of DAPTOmycin. Specifically, the risk of skeletal muscle toxicity may be increased. Management: Consider temporarily stopping statin (HMG-CoA reductase inhibitor) therapy prior to daptomycin. If daptomycin is used with a statin, creatine phosphokinase (CPK) monitoring could be considered. Risk D: Consider therapy modification

Darolutamide: May increase the serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 5 mg daily when combined with darolutamide. Monitor closely for increased rosuvastatin effects/toxicities (eg, myalgias, rhabdomyolysis) when these agents are combined. Risk D: Consider therapy modification

Dasabuvir: May increase the serum concentration of Rosuvastatin. Management: Limit the rosuvastatin dose to a maximum of 10 mg per day when used with the ombitasvir/paritaprevir/ritonavir/dasabuvir combination product. Labeling outside of the US recommends limiting the rosuvastatin dose to 5 mg per day. Risk D: Consider therapy modification

Dronedarone: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Elacestrant: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Elagolix: May decrease the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Elagolix, Estradiol, and Norethindrone: May decrease the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Elbasvir and Grazoprevir: May increase the serum concentration of Rosuvastatin. Management: Initiate rosuvastatin at 5 mg daily and limit the rosuvastatin dose to a maximum of 10 mg per day during coadministration with elbasvir/grazoprevir. Monitor closely for evidence of rosuvastatin toxicities (eg, myopathy, rhabdomyolysis). Risk D: Consider therapy modification

Eltrombopag: May increase the serum concentration of Rosuvastatin. Management: Consideration a preventive 50% reduction in rosuvastatin adult dose when starting this combination. Risk D: Consider therapy modification

Enasidenib: May increase the serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 10 mg once daily when combined with enasidenib. Risk D: Consider therapy modification

Encorafenib: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Eslicarbazepine: May decrease the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Febuxostat: May increase the serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 20 mg daily when combined with febuxostat. Monitor closely for increased rosuvastatin effects/toxicities (eg, myalgias, rhabdomyolysis) when these agents are combined. Risk D: Consider therapy modification

Fenofibrate and Derivatives: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Fenofibrate and Derivatives may increase the serum concentration of Ezetimibe. Risk C: Monitor therapy

Fibric Acid Derivatives: May enhance the adverse/toxic effect of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Fibric Acid Derivatives may increase the serum concentration of Ezetimibe. Risk X: Avoid combination

Fostamatinib: May increase the serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 20 mg daily when combined with fostamatinib. Monitor closely for increased rosuvastatin effects/toxicities (eg, myalgias, rhabdomyolysis) when these agents are combined. Risk D: Consider therapy modification

Fostemsavir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Management: Use the lowest possible starting statin dose and monitor patients closely for statin-related adverse effects (eg, muscle aches and pains) during coadministration with fostemsavir. Risk D: Consider therapy modification

Fusidic Acid (Systemic): May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Specifically, the risk for muscle toxicities, including rhabdomyolysis may be significantly increased. Management: Avoid concurrent use whenever possible. Use is listed as contraindicated in product characteristic summaries in several countries, although UK labeling suggests that use could be considered under exceptional circumstances and with close supervision. Risk X: Avoid combination

Futibatinib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Gilteritinib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Glecaprevir and Pibrentasvir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Management: Use the lowest statin dose possible if combined with glecaprevir/pibrentasvir and monitor for increased statin effects/toxicities. Avoid concomitant use with atorva-, simva-, or lovastatin. Limit rosuvastatin to 10 mg daily and reduce pravastatin dose 50% Risk D: Consider therapy modification

Itraconazole: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Lanthanum: May decrease the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Management: Administer HMG-CoA reductase inhibitors (eg, statins) at least two hours before or after lanthanum. Risk D: Consider therapy modification

Ledipasvir: May increase the serum concentration of Rosuvastatin. Risk X: Avoid combination

Leflunomide: May increase the serum concentration of Rosuvastatin. Management: Limit the maximum adult rosuvastatin dose to 10 mg/day in patients receiving leflunomide, and monitor for evidence of rosuvastatin toxicity (eg, muscle toxicity, elevated transaminase concentrations). Risk D: Consider therapy modification

Leniolisib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination

Leniolisib: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination

Letermovir: May increase the serum concentration of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy

Lopinavir: May increase the serum concentration of Rosuvastatin. Management: Initiate rosuvastatin at 5 mg daily and limit the rosuvastatin dose to a maximum of 10 mg per day when used with lopinavir/ritonavir. Monitor patients closely for evidence of rosuvastatin toxicities (eg, myopathy, rhabdomyolysis). Risk D: Consider therapy modification

Maribavir: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Momelotinib: May increase the serum concentration of Rosuvastatin. Management: In patients who are receiving momelotinib, initiate rosuvastatin at a dose of 5 mg once daily and limit the rosuvastatin dose to a maximum of 10 mg once daily. Risk D: Consider therapy modification

Niacin: May enhance the myopathic (rhabdomyolysis) effect of Rosuvastatin. Risk C: Monitor therapy

Nirmatrelvir and Ritonavir: May increase the serum concentration of Rosuvastatin. Management: Consider temporarily discontinuing rosuvastatin during treatment with nirmatrelvir/ritonavir. It is not necessary to hold rosuvastatin either prior to or after completion of nirmatrelvir/ritonavir treatment. Risk D: Consider therapy modification

Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir: May increase the serum concentration of Rosuvastatin. Management: Initiate rosuvastatin at 5 mg daily and limit the rosuvastatin dose to a maximum of 10 mg per day when used with the ombitasvir/paritaprevir/ritonavir/dasabuvir combination product. Monitor for rosuvastatin toxicities (eg, myopathy, rhabdomyolysis). Risk D: Consider therapy modification

Pacritinib: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination

Pretomanid: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Protease Inhibitors: May increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Raltegravir: May enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor therapy

Red Yeast Rice: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Risk X: Avoid combination

Regorafenib: May increase the serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 10 mg daily when combined with regorafenib. Monitor closely for increased rosuvastatin effects/toxicities (eg, myalgias, rhabdomyolysis) when these agents are combined. Risk D: Consider therapy modification

Repaglinide: HMG-CoA Reductase Inhibitors (Statins) may increase the serum concentration of Repaglinide. Risk C: Monitor therapy

RifAMPin: May decrease the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Rupatadine: May enhance the adverse/toxic effect of HMG-CoA Reductase Inhibitors (Statins). Specifically, the risk for increased CPK and/or other muscle toxicities may be increased. Risk C: Monitor therapy

Simeprevir: May increase the serum concentration of Rosuvastatin. Management: Limit initial rosuvastatin dose to 5 mg/day when being started in a patient who is also being treated with simeprevir. The maximum rosuvastatin dose should not exceed 10 mg/day with concurrent use of simeprevir. Risk D: Consider therapy modification

Sparsentan: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination

Tafamidis: May enhance the myopathic (rhabdomyolysis) effect of Rosuvastatin. Tafamidis may increase the serum concentration of Rosuvastatin. Management: Avoid this combination if possible. If combined, initiate rosuvastatin at a dose of 5 mg once daily and do not exceed a dose of rosuvastatin 20 mg daily. Monitor for signs of myopathy and rhabdomyolysis. Risk D: Consider therapy modification

Taurursodiol: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk X: Avoid combination

Tedizolid: May increase the serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Teriflunomide: May increase the serum concentration of Rosuvastatin. Management: Limit the maximum adult rosuvastatin dose to 10 mg/day in patients receiving teriflunomide, and monitor for evidence of rosuvastatin toxicity (eg, muscle toxicity, elevated transaminase concentrations). Risk D: Consider therapy modification

Ticagrelor: May enhance the myopathic (rhabdomyolysis) effect of Rosuvastatin. Ticagrelor may increase the serum concentration of Rosuvastatin. Risk C: Monitor therapy

Trabectedin: HMG-CoA Reductase Inhibitors (Statins) may enhance the myopathic (rhabdomyolysis) effect of Trabectedin. Risk C: Monitor therapy

Trofinetide: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid concurrent use with OATP1B1/1B3 substrates for which small changes in exposure may be associated with serious toxicities. Monitor for evidence of an altered response to any OATP1B1/1B3 substrate if used together with trofinetide. Risk D: Consider therapy modification

Velpatasvir: May increase the serum concentration of Rosuvastatin. Management: Initiate rosuvastatin at 5 mg daily and limit the rosuvastatin dose to a maximum of 10 mg per day during coadministration with sofosbuvir/velpatasvir. Monitor closely for evidence of rosuvastatin toxicities (eg, myopathy, rhabdomyolysis). Risk D: Consider therapy modification

Vitamin K Antagonists (eg, warfarin): HMG-CoA Reductase Inhibitors (Statins) may enhance the anticoagulant effect of Vitamin K Antagonists. Risk C: Monitor therapy

Voclosporin: May increase the serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor therapy

Voxilaprevir: May increase the serum concentration of Rosuvastatin. Risk X: Avoid combination

Pregnancy Considerations

Use during pregnancy is not recommended. Discontinue ezetimibe/rosuvastatin if pregnancy occurs during treatment.

Refer to individual monographs for additional information.

Breastfeeding Considerations

Rosuvastatin is present in breast milk; excretion of ezetimibe is not known.

Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer. Refer to individual monographs for additional information.

Dietary Considerations

Red yeast rice contains variable amounts of several compounds that are structurally similar to HMG-CoA reductase inhibitors, primarily monacolin K (or mevinolin), which is structurally identical to lovastatin; concurrent use of red yeast rice with HMG-CoA reductase inhibitors may increase the incidence of adverse and toxic effects (Lapi 2008; Smith 2003).

Monitoring Parameters

Manufacturer's labeling:

Consider neuromuscular and serologic testing if immune-mediated necrotizing myopathy is suspected.

American College of Cardiology/American Heart Association blood cholesterol guideline recommendations (ACC/AHA [Grundy 2019]; ACC/AHA [Stone 2014 ]):

Lipid panel (total cholesterol, HDL, LDL, triglycerides): Baseline lipid panel; fasting lipid profile within 4 to 12 weeks after initiation or dose adjustment and every 3 to 12 months (as clinically indicated) thereafter. If 2 consecutive LDL levels are <40 mg/dL, consider decreasing the dose.

Hepatic transaminase levels: Baseline measurement of hepatic transaminase levels (AST and ALT); measure AST, ALT, total bilirubin, and alkaline phosphatase if symptoms suggest hepatotoxicity (eg, unusual fatigue or weakness, loss of appetite, abdominal pain, dark-colored urine, yellowing of skin or sclera) during therapy.

CPK: CPK should not be routinely measured. Baseline CPK measurement is reasonable for some individuals (eg, family history of statin intolerance or muscle disease, clinical presentation, concomitant drug therapy that may increase risk of myopathy). May measure CPK in any patient with symptoms suggestive of myopathy (pain, tenderness, stiffness, cramping, weakness, or generalized fatigue).

Evaluate for new-onset diabetes mellitus during therapy; if diabetes develops, continue statin therapy and encourage adherence to a heart-healthy diet, physical activity, a healthy body weight, and tobacco cessation.

If patient develops a confusional state or memory impairment, may evaluate patient for nonstatin causes (eg, exposure to other drugs), systemic and neuropsychiatric causes, and the possibility of adverse effects associated with statin therapy.

Mechanism of Action

Ezetimibe: Inhibits absorption of cholesterol at the brush border of the small intestine, leading to a decreased delivery of cholesterol to the liver. Ezetimibe inhibits the enzyme Niemann-Pick C1-Like1 (NPC1L1), a sterol transporter.

Rosuvastatin: Inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis (reduces the production of mevalonic acid from HMG-CoA); this then results in a compensatory increase in the expression of LDL receptors on hepatocyte membranes and a stimulation of LDL catabolism. In addition to the ability of HMG-CoA reductase inhibitors to decrease levels of high-sensitivity C-reactive protein (hsCRP), they also possess pleiotropic properties, including improved endothelial function, reduced inflammation at the site of the coronary plaque, inhibition of platelet aggregation, and anticoagulant effects (de Denus 2002; Ray 2005).

Pharmacokinetics (Adult Data Unless Noted)

See individual agents.

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AE) United Arab Emirates: Roxymib | Zympass;
  • (AR) Argentina: Artomey plus | Lipex plus | Rosuber plus | Rosufen duo | Roszet;
  • (AT) Austria: Arosuva plus Ezetimib | Ezerosu | Rosamib;
  • (BE) Belgium: Ezetimibe/rosuvastatin sandoz | Ezetimibe/rosuvastatine teva | Myrosor | Suvezen;
  • (BG) Bulgaria: Co roswera | Rozetin | Rozor | Tintaros plus | Zenon;
  • (BR) Brazil: Zinpass eze;
  • (CH) Switzerland: Ezetim rosuv spirig hc | Ezetimib rosuvastatin mylan;
  • (CL) Chile: Ervastin;
  • (CO) Colombia: Cardiomax plus | Rosuvax e;
  • (CZ) Czech Republic: Rosumop combi | Rosuvastatin/ezetimibe teva | Rozetin | Ruzeb | Sorvasta plus | Twicor | Zenon | Zenon neo;
  • (DE) Germany: Ezehron duo;
  • (DO) Dominican Republic: Desgratin | Lopraxin ez | Rosuvast Ez | Rosuvina Ultra | Skorlat ez;
  • (EC) Ecuador: Rosuvina e | Vascuvid plus;
  • (EE) Estonia: Rosazimib | Rozesta;
  • (EG) Egypt: Cholerose plus;
  • (ES) Spain: Alzil plus | Ateroger | Rosuvastatina/ezetimiba cinfa | Rosuvastatina/ezetimiba teva | Twicor | Zenon;
  • (FI) Finland: Rosuvastatin/ezetimibe teva;
  • (FR) France: Suvreza | Twicor;
  • (GR) Greece: Lipopen | Rozor | Zenon;
  • (HR) Croatia: Co roswera | Eprizet | Rosix Combi;
  • (HU) Hungary: Co xeter | Roxera plus;
  • (ID) Indonesia: Ezero;
  • (IE) Ireland: Rosuvastatin/ezetimibe krka | Suvezen | Twicor;
  • (IN) India: Consivas ez | Crevast ez | Novastat Ez | Razel ez | Roseday ez | Rosumac ez | Rozavel ez | Rozucor ez | Turbovas ez;
  • (IT) Italy: Aurozeb | Compuna | Ezateros | Maoris | Quiloga | Rosetem | Rosumibe | Rosuvastatin/ezetimibe teva | Rosuvastatina e ezetimibe doc | Rozetimad;
  • (JP) Japan: Rosuzet;
  • (KE) Kenya: Rosu ez;
  • (KR) Korea, Republic of: Chlowzet | Clowzet | Creazine plus | Credouble | Crestibe | Cretrol | Crezet | Daviduo | Droptop | Duonon | Duoroban | Duorovan | Esuba | Ezelow | Ezerosu | Ezerova | Ezesant | Kvazet | Lypstaplus | Megarozet | Rosetibe | Rostorin | Rosuemzet | Rosueze | Rosutanzet | Rosuvamibe | Rosuzet | Rotimibe | Rovazet | Rozeduo | Rozelow | Rozet | Rozetib | Suvazet | Topstatin f;
  • (KW) Kuwait: Zympass;
  • (LT) Lithuania: Sorvitimb;
  • (LU) Luxembourg: Myrosor;
  • (LV) Latvia: Rosazimib | Rozesta;
  • (MX) Mexico: Naxzalla;
  • (NO) Norway: Zenon;
  • (PH) Philippines: Rosuzet;
  • (PK) Pakistan: Rovista ez;
  • (PL) Poland: Coroswera | Ezehron duo | Rozesta | Rozor | Sorento | Suvardio Plus | Suvezen;
  • (PR) Puerto Rico: Roszet;
  • (PT) Portugal: Colroset | Rosumibe | Rosuvastatina + ezetimiba alter | Rosuvastatina + ezetimiba bistenibe | Rosuvastatina + ezetimiba ferrer | Rosuvastatina + Ezetimiba Krka | Rosuvastatina + ezetimiba teva | Rozetin | Rozor | Twicor | Zenon;
  • (QA) Qatar: Zympass;
  • (RO) Romania: Co-roswera | Rozetin | Suvezen | Twicor;
  • (SI) Slovenia: Rozor | Sorvitimb;
  • (SK) Slovakia: Rosazimib | Rozor | Ruzeb | Zenon;
  • (TR) Turkey: Ezeros;
  • (TW) Taiwan: Cretrol;
  • (ZA) South Africa: Lypstaplus
  1. de Denus S, Spinler SA. Early statin therapy for acute coronary syndromes. Ann Pharmacother. 2002;36(11):1749-1758. doi:10.1345/aph.1A413 [PubMed 12398573]
  2. Fleisher LA, Fleischmann KE, Auerbach AD, et al. 2014 ACC/AHA guideline on perioperative cardiovascular evaluation and management of patients undergoing noncardiac surgery: executive summary: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines. Circulation. 2014;130(24):2215-2245. doi:10.1161/CIR.0000000000000105 [PubMed 25085962]
  3. Grundy SM, Stone NJ, Bailey AL, et al. 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of blood cholesterol: a report of the American College of Cardiology/American Heart Association task force on clinical practice guidelines. Circulation. 2019;139(25):e1082-e1143. doi:10.1161/CIR.0000000000000625 [PubMed 30586774]
  4. Hillis LD, Smith PK, Anderson JL, et al. 2011 ACCF/AHA guideline for coronary artery bypass graft surgery: a report of the American College of Cardiology Foundation/American Heart Association task force on practice guidelines. Circulation. 2011;124(23):e652-e735. doi:10.1161/CIR.0b013e31823c074e [PubMed 22064599]
  5. Lapi F, Gallo E, Bernasconi S, et al. Myopathies associated with red yeast rice and liquorice: spontaneous reports from the Italian Surveillance System of Natural Health Products. Br J Clin Pharmacol. 2008;66(4):572-574. doi:10.1111/j.1365-2125.2008.03224.x [PubMed 18637891]
  6. Narayanaswami P, Sanders DB, Wolfe G, et al. International consensus guidance for management of myasthenia gravis: 2020 update. Neurology. 2021;96(3):114-122. doi:10.1212/WNL.0000000000011124 [PubMed 33144515]
  7. Newman CB, Preiss D, Tobert JA, et al. Statin safety and associated adverse events: a scientific statement from the American Heart Association. Arterioscler Thromb Vasc Biol. 2019;39(2):e38-e81. doi:10.1161/ATV.0000000000000073 [PubMed 30580575]
  8. Ray KK, Cannon CP. The potential relevance of the multiple lipid-independent (pleiotropic) effects of statins in the management of acute coronary syndromes. J Am Coll Cardiol. 2005;46(8):1425-1433. doi:10.1016/j.jacc.2005.05.086 [PubMed 16226165]
  9. Refer to the manufacturer's labeling. [PubMed manu.1]
  10. Roszet (ezetimibe and rosuvastatin) [prescribing information]. Morristown, NJ: Althera Pharmaceuticals LLC; March 2021.
  11. Smith DJ, Olive KE. Chinese red rice-induced myopathy. South Med J. 2003;96(12):1265-1267. doi:10.1097/01.SMJ.0000100117.79718.DC [PubMed 14696880]
  12. Stone NJ, Robinson JG, Lichtenstein AH, et al; American College of Cardiology/American Heart Association Task Force on Practice Guidelines. 2013 ACC/AHA guideline on the treatment of blood cholesterol to reduce atherosclerotic cardiovascular risk in adults: a report of the American College of Cardiology/American Heart Association task force on practice guidelines. J Am Coll Cardiol. 2014;63(25, pt B):2889-2934. doi:10.1016/j.jacc.2013.11.002 [PubMed 24239923]
Topic 131212 Version 60.0

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