Ezetimibe and rosuvastatin (United States and Canada: Not available): Drug information

For additional information see "Ezetimibe and rosuvastatin (United States and Canada: Not available): Patient drug information"

For abbreviations, symbols, and age group definitions show table

Brand Names: US

Roszet [DSC]

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]).

Dosage form information: Roszet tablets (brand and generic) have been discontinued in the United States for >1 year.

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.

Hyperlipidemia

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: Liver Impairment: Adult

Hepatic impairment prior to treatment initiation: 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 C_max); use is contraindicated in active liver disease or decompensated cirrhosis.

Hepatotoxicity during treatment:

ALT or AST ≥3 times the ULN: Consider discontinuing treatment if ALT or AST is persistently ≥3 times the ULN.

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 HbA_1c (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: Persistent elevations in serum transaminases have been reported with ezetimibe use. 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.

• 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.

• 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).

Product Availability

Roszet tablets (brand and generic) have been discontinued in the United States for >1 year.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral:

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

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

Generic Equivalent Available: US

Yes

Pricing: US

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. Administer ≥2 hours before or ≥4 hours after bile acid sequestrants. Administer ≥2 hours before aluminum and magnesium hydroxide combination antacids.

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).

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 drug interactions program by clicking on the “Launch drug interactions program” link above.

Abiraterone Acetate: May increase myopathic (rhabdomyolysis) effects of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor

Acipimox: May increase myopathic (rhabdomyolysis) effects of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor

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

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

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

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

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

Belumosudil: May increase serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Management: Avoid coadministration of belumosudil with these substrates of BCRP for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the BCRP substrate may be required. Risk D: Consider Therapy Modification

Belumosudil: May increase serum concentration of OATP1B1/1B3 (SLCO1B1/1B3) Substrates (Clinically Relevant with Inhibitors). Management: Avoid coadministration of belumosudil with these substrates of OATP1B1/1B3 for which minimal concentration increases can cause serious adverse effects. If coadministration is required, dose reductions of the OATP1B1/1B3 substrate may be required. Risk D: Consider Therapy Modification

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

Bulevirtide: Ezetimibe may decrease therapeutic effects of Bulevirtide. Risk X: Avoid

Capmatinib: May increase serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 10 mg daily or rosuvastatin/ezetimibe 10 mg/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 serum concentration of Rosuvastatin. Risk C: Monitor

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

Clopidogrel: May increase serum concentration of Rosuvastatin. Risk C: Monitor

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

CycloSPORINE (Systemic): May increase 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 serum concentration of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor

Danicopan: May increase serum concentration of Rosuvastatin. Management: Limit the rosuvastatin dose to 10 mg once daily if combined with danicopan. Risk D: Consider Therapy Modification

DAPTOmycin: HMG-CoA Reductase Inhibitors (Statins) may increase adverse/toxic effects 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 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

Darunavir: May increase serum concentration of Rosuvastatin. Management: Initiate rosuvastatin at the lowest dose and titrate slowly. Monitor for increased rosuvastatin toxicities when combined. The dose of rosuvastatin should not exceed 20 mg daily when used with darunavir/cobicistat. Risk D: Consider Therapy Modification

Dasabuvir: May increase 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 serum concentration of Rosuvastatin. Risk C: Monitor

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

Elafibranor: May increase adverse/toxic effects of HMG-CoA Reductase Inhibitors (Statins). Specifically, the risk of muscle toxicity may be increased. Risk C: Monitor

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

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

Elbasvir and Grazoprevir: May increase 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

Elexacaftor, Tezacaftor, and Ivacaftor: May increase serum concentration of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor

Eltrombopag: May increase 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 serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 10 mg once daily when combined with enasidenib. Patients treated with the rosuvastatin/ezetimibe combination product should not exceed doses of 10 mg/10 mg daily. Risk D: Consider Therapy Modification

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

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

Febuxostat: May increase serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 20 mg daily or rosuvastatin/ezetimibe 20 mg/10 mg 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 increase adverse/toxic effects of Ezetimibe. Specifically, the risk of myopathy and cholelithiasis may be increased. Fenofibrate and Derivatives may increase serum concentration of Ezetimibe. Risk C: Monitor

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

Fostamatinib: May increase serum concentration of Rosuvastatin. Management: Limit the dose of rosuvastatin to 20 mg daily or rosuvastatin/ezetimibe 20 mg/10 mg 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 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 increase adverse/toxic effects 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

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

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

Glecaprevir and Pibrentasvir: May increase serum concentration of Rosuvastatin. Management: Initiate rosuvastatin at 5 mg or rosuvastatin/ezetimibe at 5 mg/10 mg daily and limit doses to rosuvastatin 10 mg or rosuvastatin/ezetimibe 10 mg/10 mg daily. Risk D: Consider Therapy Modification

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

Lanthanum: May decrease 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 serum concentration of Rosuvastatin. Risk X: Avoid

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

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

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

Lopinavir: May increase serum concentration of Rosuvastatin. Management: Initiate rosuvastatin at 5 mg or rosuvastatin/ezetimibe 5 mg/10 mg daily and do not exceed rosuvastatin 10 mg or rosuvastatin/ezetimibe 10 mg/10 mg daily when used with lopinavir/ritonavir. Monitor for myopathy, and rhabdomyolysis. Risk D: Consider Therapy Modification

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

Momelotinib: May increase 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 increase myopathic (rhabdomyolysis) effects of Rosuvastatin. Risk C: Monitor

Nirmatrelvir and Ritonavir: May increase serum concentration of Rosuvastatin. Risk C: Monitor

Ombitasvir, Paritaprevir, Ritonavir, and Dasabuvir: May increase 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 serum concentration of Rosuvastatin. Management: Limit rosuvastatin doses to 20 mg once daily during concomitant therapy with pacritinib. Risk D: Consider Therapy Modification

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

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

Raltegravir: May increase myopathic (rhabdomyolysis) effects of HMG-CoA Reductase Inhibitors (Statins). Risk C: Monitor

Red Yeast Rice: May increase adverse/toxic effects of HMG-CoA Reductase Inhibitors (Statins). Risk X: Avoid

Regorafenib: May increase 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 serum concentration of Repaglinide. Risk C: Monitor

Resmetirom: May increase serum concentration of Rosuvastatin. Management: Limit the rosuvastatin dose to 20 mg daily during coadministration with resmetirom. Monitor for increased rosuvastatin adverse effects (eg, myalgias) during coadministration. Risk D: Consider Therapy Modification

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

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

Simeprevir: May increase serum concentration of Rosuvastatin. Management: Limit initial dose to rosuvastatin 5 mg or rosuvastatin/ezetimibe 5 mg/10 mg daily during treatment with simeprevir. The maximum dose should not exceed rosuvastatin 10 mg or rosuvastatin/ezetimibe 10 mg/10 mg with concurrent simeprevir. Risk D: Consider Therapy Modification

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

Tafamidis: May increase myopathic (rhabdomyolysis) effects of Rosuvastatin. Tafamidis may increase serum concentration of Rosuvastatin. Management: Avoid this combination if possible. If combined, initiate rosuvastatin 5 mg or rosuvastatin/ezetimibe 5 mg/10 mg once daily and do not exceed rosuvastatin 20 mg or rosuvastatin/ezetimibe 20 mg/10 mg daily. Monitor for signs of myopathy and rhabdomyolysis. Risk D: Consider Therapy Modification

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

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

Teriflunomide: May increase 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 increase myopathic (rhabdomyolysis) effects of Rosuvastatin. Ticagrelor may increase serum concentration of Rosuvastatin. Risk C: Monitor

Trabectedin: HMG-CoA Reductase Inhibitors (Statins) may increase myopathic (rhabdomyolysis) effects of Trabectedin. Risk C: Monitor

Trofinetide: May increase 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

Vadadustat: May increase serum concentration of Rosuvastatin. Management: Do not exceed rosuvastatin doses of 5 mg daily and monitor for rosuvastatin adverse effects (eg, myopathy) during coadministration with vadadustat. Risk D: Consider Therapy Modification

Vanzacaftor, Tezacaftor, and Deutivacaftor: May increase serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Risk C: Monitor

Velpatasvir: May increase 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

Vimseltinib: May increase serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Management: Avoid concomitant use of vimseltinib and BCRP substrates when possible. If combined, monitor for increased effects and toxicities of the BCRP substrate and consider dose adjustments. Risk D: Consider Therapy Modification

Vitamin K Antagonists: HMG-CoA Reductase Inhibitors (Statins) may increase anticoagulant effects of Vitamin K Antagonists. Risk C: Monitor

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

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

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 | Hipolipol ez | 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 | Refidoro | Rozetin | Rozor | Tintaros plus | Zenon;
(BR) Brazil: Coledue r | Zinpass eze;
(CH) Switzerland: Ezetim rosuv spirig hc | Ezetimib rosuvastatin axapharm | Ezetimib rosuvastatin mylan | Ezetimibe rosuvastatin mepha | Ezetimibe rosuvastatin sandoz | Ezetimibe rosuvastatin zentiva | Zenon;
(CL) Chile: Ervastin | Rosuvitae plus;
(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: Liparon plus | Rosimol e | Roslipid e;
(EE) Estonia: Rosazimib | Rozesta;
(EG) Egypt: Cholerose plus;
(ES) Spain: Alzil plus | Arrox plus | Ateroger | Rosuvastatina/ezetimiba alter | Rosuvastatina/ezetimiba cinfa | Rosuvastatina/ezetimiba krka | Rosuvastatina/ezetimiba sandoz | Rosuvastatina/ezetimiba teva | Twicor | Zenon;
(FI) Finland: Rosuvastatin/ezetimib krka | Rosuvastatin/ezetimibe teva;
(FR) France: Suvreza | Twicor;
(GR) Greece: Lipopen | Rosuben plus | Rosuvastatin + ezetimibe/velka | Rosuzet | Rozor | Zenon | Ziviba;
(HR) Croatia: Co roswera | Eprizet | Refidoro | Rosix Combi;
(HU) Hungary: Co xeter | Rosuvastatin/ezetimibe sandoz | Roxera plus;
(ID) Indonesia: Ezero;
(IE) Ireland: Rosuvastatin/ezetimibe krka | Suvezen | Twicor;
(IN) India: Consivas ez | Crevast ez | Novastat Ez | Razel ez | Roseday ez | Rosukem 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 | Rosuvastatina e ezetimibe sandoz | Rozetimad;
(JO) Jordan: Zympass;
(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 | Neustazet r | Roeze | Rosetibe | Rostorin | Rosu duo | 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 | Rosuvastatin/ezetimibe teva | Rozesta;
(MX) Mexico: Naxzalla;
(NO) Norway: Zenon;
(PA) Panama: Rosumibe | Rovartal;
(PE) Peru: Rosuvitae plus;
(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 | Rosuvastatina/ezetimiba ratiopharm | Rosuvastatina/ezetimiba sandoz | Rozetin | Rozor | Twicor | Zenon;
(QA) Qatar: Zympass;
(RO) Romania: Co-roswera | Rozetin | Suvezen | Twicor;
(RU) Russian Federation: Zenon;
(SA) Saudi Arabia: Zympass;
(SI) Slovenia: Rozor | Sorvitimb;
(SK) Slovakia: Rosazimib | Rozor | Ruzeb | Zenon;
(TR) Turkey: Ezeros;
(TW) Taiwan: Cretrol;
(UA) Ukraine: Roxera plus;
(UG) Uganda: Rolipeze;
(ZA) South Africa: Lypstaplus

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Roszet (ezetimibe and rosuvastatin) [prescribing information]. Wilmington, DE: Althera Pharmaceuticals LLC; August 2024.
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Topic 131212 Version 91.0

خرید پکیج

Ezetimibe and rosuvastatin (United States and Canada: Not available): Drug information