Ezetimibe
Tablet · Oral
Uses
Ezetimibe tablet is indicated: In combination with a statin, or alone when additional low-density lipoprotein cholesterol (LDL-C) lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH). In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric patients 10 years of age and older with HeFH. In combination with fenofibrate as an adjunct to diet to reduce elevated LDL-C in adults with mixed hyperlipidemia. In combination with a statin, and other LDL-C lowering therapies, to reduce elevated LDL-C levels in adults and in pediatric patients 10 years of age and older with homozygous familial hypercholesterolemia (HoFH). As an adjunct to diet for the reduction of elevated sitosterol and campesterol levels in adults and in pediatric patients 9 years of age and older with homozygous familial sitosterolemia. When ezetimibe tablet is used in combination with a statin, fenofibrate, or other LDL-C lowering therapies, refer to the Prescribing Information of these products for information on the safe and effective use. Ezetimibe tablet is indicated ( 1 ): In combination with a statin, or alone when additional low density lipoprotein cholesterol (LDL-C) lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH). In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric patients 10 years of age and older with HeFH. In combination with fenofibrate as an adjunct to diet to reduce elevated LDL-C in adults with mixed hyperlipidemia. In combination with a statin, and other LDL-C lowering therapies, to reduce elevated LDL-C levels in adults and in pediatric patients 10 years of age and older with homozygous familial hypercholesterolemia (HoFH). As an adjunct to diet for the reduction of elevated sitosterol and campesterol levels in adults and in pediatric patients 9 years of age and older with homozygous familial sitosterolemia. When Ezetimibe tablet is used in combination with a statin, fenofibrate, or other LDL-C lowering therapies, refer to the Prescribing Information of these products for information on the safe and effective use ( 1 ).
Dosage and administration
The recommended dose of ezetimibe tablet is 10 mg orally once daily, administered with or without food. If as dose is missed, take the missed dose as soon as possible. Do not double the next dose. Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating ezetimibe tablet. Administer ezetimibe tablet at least 2 hours before or 4 hours after the bile acid sequestrant [see Drug Interactions ( 7 )] . 10-mg orally once daily, with or without food ( 2 ) Administer Ezetimibe tablets either ≥2 hours before or ≥4 hours after administration of a bile acid sequestrant. ( 2 ) Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating Ezetimibe tablets. ( 2 )
Dosage forms and strengths
10-mg tablets are white to off-white, capsule-shaped tablets debossed with "OP" on one side and "70" on other side. Tablets: 10 mg ( 3 )
Contraindications
Ezetimibe tablet is contraindicated in patients with a known hypersensitivity to ezetimibe or any of the excipients in ezetimibe tablets. Hypersensitivity reactions including anaphylaxis, angioedema, rash, and urticaria have been reported [see Adverse Reactions ( 6.2 )] . When used in combination with a statin, fenofibrate, or other LDL-C lowering therapy, ezetimibe tablet is contraindicated in patients for whom a statin, fenofibrate, or other LDL-C lowering therapy are contraindicated. Refer to the Prescribing Information of these products for a list of their contraindications [see Warnings and Precautions ( 5.1 )] . Hypersensitivity to ezetimibe or any excipient of ezetimibe tablets. ( 4 ) When used in combination with a statin, fenofibrate, or other LDL-C lowering therapy, Ezetimibe tablet is contraindicated in patients for whom a statin, fenofibrate, or other LDL-C lowering therapy are contraindicated. Refer to the Prescribing Information of these products for a list of their contraindications. ( 4 )
Warnings and precautions
Risks Associated with Combination Treatment with a Statin, Fenofibrate, or Other LDL-C Lowering Therapies: Refer to the Prescribing Information of these products for a description of their risks including, but not limited to, the warnings and precautions. ( 5.1 ) Liver Enzyme Abnormalities and Monitoring: Increases in serum transaminases have been reported with use of Ezetimibe tablets. Perform liver enzyme testing as clinically indicated and consider withdrawal of Ezetimibe tablet if increases in ALT or AST ≥3 × ULN persist. ( 5.2 ) Skeletal Muscle Effects (e.g., Myopathy and Rhabdomyolysis): Ezetimibe tablets may cause myopathy and rhabdomyolysis. In post-marketing reports, most patients who developed rhabdomyolysis were taking a statin or other agents known to be associated with an increased risk of rhabdomyolysis, such as fibrates. If myopathy is suspected, discontinue Ezetimibe tablets and other concomitant medications, as appropriate. ( 5.3 ) 5.1 Risks Associated with Combination Treatment with a Statin, Fenofibrate, or Other LDL-C Lowering Therapies If ezetimibe tablet is administered with a statin, fenofibrate, or other LDL-C lowering therapies, refer to the Prescribing Information of these products for a description of their risks including, but not limited to, the warnings and precautions [see Contraindications ( 4 )] . 5.2 Liver Enzymes Increases in serum transaminases have been reported with use of ezetimibe tablets [see Adverse Reactions ( 6.1 )] . In controlled clinical combination studies of ezetimibe tablets initiated concurrently with a statin, the incidence of consecutive elevations (≥3 × ULN) in hepatic transaminase levels was 1.3% for patients treated with ezetimibe administered with statins and 0.4% for patients treated with statins alone. Perform liver enzyme testing as clinically indicated and consider withdrawal of ezetimibe tablets if increases in ALT or AST ≥3 × ULN persist. 5.3 Myopathy/Rhabdomyolysis Ezetimibe tablets may cause myopathy [muscle pain, tenderness, or weakness associated with elevated creatine kinase (CK)] and rhabdomyolysis [see Adverse Reactions ( 6.1 )] . In post-marketing reports, most patients who developed rhabdomyolysis were taking a statin or other agents known to be associated with an increased risk of rhabdomyolysis, such as fibrates. If myopathy is suspected, discontinue ezetimibe tablets and other concomitant medications, as appropriate.
Side effects
The following serious adverse reactions are discussed in greater detail in other sections of the label: Liver enzyme abnormalities [see Warnings And Precautions ( 5.2 )] Rhabdomyolysis and myopathy [see Warnings And Precautions ( 5.3 )] Common adverse reactions in clinical trials: o Ezetimibe administered alone (incidence ≥2% and greater than placebo): upper respiratory tract infection, diarrhea, arthralgia, sinusitis, pain in extremity, fatigue, and influenza ( 6.1 ) o Ezetimibe tablets coadministered with a statin (incidence ≥2% and greater than statin alone): nasopharyngitis, myalgia, upper respiratory tract infection, arthralgia, diarrhea, back pain, influenza, pain in extremity, and fatigue ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Marlex Pharmaceuticals, Inc. at 1-888-582-1953 or Drugsafety@marlexpharm.com or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in clinical practice. Monotherapy In 10 double-blind, placebo-controlled clinical trials, 2396 patients with primary hyperlipidemia (age range 9 to 86 years, 50% female, 90% White, 5% Black or African American, 2% Asians, 3% other races; 3% identified as Hispanic or Latino ethnicity) and elevated LDL-C were treated with ezetimibe 10 mg daily for a median treatment duration of 12 weeks (range 0 to 39 weeks). Adverse reactions reported in ≥2% of patients treated with ezetimibe and at an incidence greater than placebo in placebo-controlled studies of ezetimibere shown in Table 1 . Table 1. Adverse Reactions Occurring ≥2% and Greater than Placebo in Ezetimibe-treated Patients Adverse Reaction Placebo(%) n = 1,159 Ezetimibe 10 mg (%) n = 2,396 Upper respiratory tract infection 2.5 4.3 Diarrhea 3.7 4.1 Arthralgia 2.2 3.0 Sinusitis 2.2 2.8 Pain in extremity 2.5 2.7 Fatigue 1.5 2.4 Influenza 1.5 2.0 Combination with a Statin In 28 double-blind, controlled (placebo or active-controlled) clinical trials, 11,308 patients with primary hyperlipidemia (age range 10 to 93 years, 48% female, 85% White, 7% Black or African American, 3% Asians, 5% other races; 4% identified as Hispanic or Latino ethnicity) and elevated LDL-C were treated with ezetimibe 10 mg/day concurrently with or added to on-going statin therapy for a median treatment duration of 8 weeks (range 0 to 112 weeks). The incidence of consecutive increased transaminases (≥3 × ULN) was higher in patients receiving ezetimibe administered with statins (1.3%) than in patients treated with statins alone (0.4%). Adverse reactions reported in ≥2% of patients treated with ezetimibe + statin and at an incidence greater than statin are shown in Table 2 . Table 2: Adverse Reactions Occurring ≥2% in Ezetimibe-treated Patients Coadministered with a Statin and at an Incidence Greater than Statin Adverse Reaction All Statins (%) n = 9,361 Ezetimibe + All Statins (%) n = 11,308 Nasopharyngitis 3.3 3.7 Myalgia 2.7 3.2 Upper respiratory tract infection 2.8 2.9 Arthralgia 2.4 2.6 Diarrhea 2.2 2.5 Back pain 2.3 2.4 Influenza 2.1 2.2 Pain in extremity 1.9 2.1 Fatigue 1.6 2.0 *All Statins = all doses of all statins Combination with Fenofibrate This clinical trial involving 625 patients with mixed dyslipidemia (age range 20 to 76 years, 44% female, 79% White, 1% Black or African American, 20% other races; 11% identified as Hispanic or Latino ethnicity) treated for up to 12 weeks and 576 patients treated for up to an additional 48 weeks evaluated coadministration of ezetimibe and fenofibrate. Incidence rates for clinically important elevations (≥3 × ULN, consecutive) in hepatic transaminase levels were 4.5% and 2.7% for fenofibrate monotherapy (n=188) and ezetimibe coadministered with fenofibrate (n=183), respectively, adjusted for treatment exposure. Corresponding incidence rates for cholecystectomy were 0.6% and 1.7% for fenofibrate monotherapy and ezetimibe coadministered with fenofibrate, respectively [see Drug Interactions ( 7 )] . 6.2 Post-Marketing Experience Because the reactions below are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure. The following additional adverse reactions have been identified during post-approval use of ezetimibe tablets: Blood Disorders : thrombocytopenia Gastrointestinal Disorders : abdominal pain; pancreatitis; nausea Hepatobiliary Disorders : elevations in liver transaminases; including elevations more than 5 X ULN;hepatitis; cholelithiasis; cholecystitis Immune System Disorders : Hypersensitivity reactions including: anaphylaxis, angioedema, rash, and urticaria Musculoskeletal Disorders : elevated creatine phosphokinase; myopathy/rhabdomyolysis Nervous System Disorders : dizziness; paresthesia; depression; headache Skin and Subcutaneous Tissue Disorders : erythema multiforme
Drug interactions
Table 3 includes a list of drugs with clinically important drug interactions when administered concomitantly with Ezetimibe tablets and instructions for preventing or managing them. Table 3: Clinically Important Drug Interactions with Ezetimibe tablets Cyclosporine Clinical Impact: Concomitant use of ezetimibe and cyclosporine increases ezetimibe and cyclosporine concentrations. The degree of increase in ezetimibe exposure may be greater in patients with severe renal insufficiency [ see Clinical Pharmacology ( 12.3 )]. Intervention: Monitor cyclosporine concentrations in patients receiving ezetimibe and cyclosporine. In patients treated with cyclosporine, weigh the potential effects of the increased exposure to ezetimibe from concomitant use against the benefits of alterations in lipid levels provided by ezetimibe. Fibrates Clinical Impact: Both fenofibrate and ezetimibe may increase cholesterol excretion into the bile, leading to cholelithiasis. Co-administration of ezetimibe with fibrates other than fenofibrate is not recommended [ see Adverse Reactions ( 6.1 )]. Intervention: If cholelithiasis is suspected in a patient receiving ezetimibe and fenofibrate, gallbladder studies are indicated, and alternative lipid-lowering therapy should be considered. Bile Acid Sequestrants Clinical Impact: Concomitant cholestyramine administration decreased the mean exposure of total ezetimibe. This may result in a reduction of efficacy [see Clinical Pharmacology ( 12.3 )]. Intervention: In patients taking a bile acid sequestrant, administer ezetimibe at least 2 hours before or 4 hours after the bile acid sequestrant [see Dosage and Administration ( 2 )]. Cyclosporine: Combination increases exposure of ezetimibe and cyclosporine. Cyclosporine concentrations should be monitored in patients taking ezetimibe concomitantly. ( 7 ) Fibrates: Coadministration of ezetimibe with fibrates other than fenofibrate is not recommended until use in patients is adequately studied. If cholelithiasis is suspected in a patient receiving ezetimibe and fenofibrate, gallbladder studies are indicated, and alternative lipid-lowering therapy should be considered. ( 7 ) Bile Acid Sequestrants: Cholestyramine combination decreases exposure of ezetimibe. ( 7 ) See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling. Revised: 03/2024
Use in specific populations
8.1 Pregnancy Risk Summary There are insufficient data on ezetimibe use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. In animal reproduction studies, no adverse developmental effects were observed in pregnant rats and rabbits orally administered ezetimibe during the period of organogenesis at doses that resulted in up to 10 and 150 times, respectively, the human exposure at the MRHD, based on AUC ( see Data ). Ezetimibe tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. When ezetimibe tablets is administered with a statin, refer to the Prescribing Information for the statin. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In oral (gavage) embryo-fetal development studies of ezetimibe conducted in rats (gestation days 6-15) and rabbits (gestation days 7-19), there was no evidence of maternal toxicity or embryolethal effects at the doses tested (250, 500, 1,000 mg/kg/day). In rats, increased incidences of common fetal skeletal findings (extra pair of thoracic ribs, unossified cervical vertebral centra, shortened ribs) were observed at 1,000 mg/kg/day (~10 times the human exposure at 10 mg daily based on AUC 0-24hr for total ezetimibe). In rabbits treated with ezetimibe, an increased incidence of extra thoracic ribs was observed at 1,000 mg/kg/day (150 times the human exposure at 10 mg daily based on AUC 0-24hr for total ezetimibe). The animal-to-human exposure multiple for total ezetimibe at the no-observed effect level was 6 times for rat and 134 times for rabbit. Fetal exposure to ezetimibe (conjugated and unconjugated) was confirmed in subsequent placental transfer studies conducted using a maternal dose of 1,000 mg/kg/day. The fetal maternal plasma exposure ratio (total ezetimibe) was 1.5 for rats on gestation day 20 and 0.03 for rabbits on gestation day 22. The effect of ezetimibe on prenatal and postnatal development and maternal function was evaluated in pregnant rats at doses of 100, 300 or 1,000 mg/kg/day from gestation day 6 through lactation day 21. No maternal toxicity or adverse developmental outcomes were observed up to and including the highest dose tested (17 times the human exposure at 10 mg daily based on AUC 0-24hr for total ezetimibe). Multiple-dose studies of ezetimibe given in combination with statins in rats and rabbits during organogenesis resulted in higher ezetimibe and statin exposures. Reproductive findings occurred at lower doses in combination therapy compared to monotherapy. 8.2 Lactation Risk Summary There is no information about the presence of ezetimibe in human milk. Ezetimibe is present in rat milk (see Data) . When a drug is present in animal milk, it is likely that the drug will be present in human milk. There is no information about the effects of ezetimibe on the breastfed infant or the effects of ezetimibe on milk production. Ezetimibe tablets should not be used in nursing mothers unless the potential benefit justifies the potential risk to the infant. Data Ezetimibe was present in the milk of lactating rats. The pup to maternal plasma ratio for total ezetimibe was 0.5 on lactation day 12. 8.4 Pediatric Use The safety and effectiveness of ezetimibe in combination with a statin as an adjunct to diet to reduce LDL-C have been established in pediatric patients 10 years of age and older with HeFH. Use of ezetimibe tablets for this indication is based on a double-blind, placebo-controlled clinical trial in 248 pediatric patients (142 males and 106 postmenarchal females) 10 years of age and older with HeFH [see Clinical Studies ( 14 )] . In this limited controlled trial, there was no significant effect on growth or sexual maturation in the adolescent males or females, or on menstrual cycle length in females. The safety and effectiveness of ezetimibe in combination with a statin, and other LDL-C lowering therapies, to reduce LDL-C have been established in pediatric patients 10 years of age and older with HoFH. Use of ezetimibe tablets for this indication is based on a 12-week double-blind, placebo-controlled clinical trial followed by an uncontrolled extension period in 7 pediatric patients 11 years of age and older with HoFH [see Clinical Studies ( 14 )] . The safety and effectiveness of ezetimibe as an adjunct to diet for the reduction of elevated sitosterol and campesterol levels have been established in adults and pediatric patients 9 years of age and older with homozygous familial sitosterolemia. Use of ezetimibe tablets for this indication is based on an 8-week double-blind, placebo-controlled clinical trial in 4 patients 9 years of age and older with homozygous sitosterolemia with elevated plasma sitosterol levels (>5 mg/dL) [see Clinical Studies ( 14 )] . The safety and effectiveness of ezetimibe have not been established in pediatric patients younger than 10 years of age with HeFH or HoFH, in pediatric patients younger than 9 years of age with homozygous familial sitosterolemia, or in pediatric patients with other types of hyperlipidemia. 8.5 Geriatric Use Of the 2,396 patients who received ezetimibe in clinical trials, 669 (28%) were 65 years of age and older, and 111 (5%) were 75 years of age and older. Of the 11,308 patients who received ezetimibe in combination with a statin in clinical trials, 3587 (32%) were 65 years of age and older, and 924 (8%) were 75 years of age and older [see Clinical Studies ( 14 )] . No overall differences in safety or effectiveness of ezetimibe have been observed between patients 65 years of age and older and younger patients.
Overdosage
In the event of overdose, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.
Description
Ezetimibe is a dietary cholesterol absorption inhibitor. The chemical name of ezetimibe is 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone. The empirical formula is C 24 H 21 F 2 NO 3 . Its molecular weight is 409.4 and its structural formula is: Ezetimibe is a white, crystalline powder that is freely to very soluble in ethanol, methanol, and acetone and practically insoluble in water. Ezetimibe has a melting point of about 163°C and is stable at ambient temperature. Ezetimibe is available as a tablet for oral administration containing 10 mg of ezetimibe and the following inactive ingredients: mannitol, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulfate, magnesium stearate, anhydrous citric acid. structural formula
How supplied
Ezetimibe tablets, USP 10 mg, are white to off-white, capsule-shaped tablets debossed with “OP” on one side and “70” on other side and are supplied as follows: Package Size NDC Bottle of 30 tablets 10135-0787-30 Bottle of 90 tablets 10135-0787-90 Bottle of 500 tablets 10135-0787-05 Store Ezetimibe tablets, USP 10 mg at 25°C (77°F); excursions permitted to 15–30°C (59–86°F). [See USP Controlled Room Temperature.] Protect from moisture.
Patient information
Advise the patient to read the FDA-Approved Patient Labeling ( PATIENT INFORMATION ). Inform patients that ezetimibe may cause liver enzyme elevations [see Warnings and Precautions ( 5.2 )]. Muscle Pain Advise patients that ezetimibe may cause myopathy and rhabdomyolysis. Inform patients that the risk is also increased when taking certain types of medication and they should discuss all medication, both prescription and over the counter, with their healthcare provider. Instruct patients to promptly report any unexplained muscle pain, tenderness or weakness particularly if accompanied by malaise or fever [see Warnings and Precautions ( 5.3 ), and Drug Interactions ( 7 )]. Pregnancy Advise patients to inform their healthcare provider of a known or suspected pregnancy to discuss if ezetimibe should be discontinued [see Use in Specific Populations ( 8.1 )] . Breast feeding Advise patients who have a lipid disorder and are breastfeeding to discuss the options with their healthcare provider [see Use in Specific Populations ( 8.2 )] . Missed Dose Instruct patients to take ezetimibe only as prescribed. If a dose is missed, it should be taken as soon as possible. Advise patients not to double their next dose. Manufactured for/Distributed by: Marlex Pharmaceuticals, Inc. New Castle, DE 19720 Rev.1 03/24 OP
Label text from the FDA structured product label by Marlex Pharmaceuticals, Inc. (revised Nov 7, 2025). Long sections are shortened; the complete label is on DailyMed.
Active ingredients
- Ezetimibe in 40 products
Ezetimibe NDC products (40)
Frequently asked questions
What is Ezetimibe used for?
Ezetimibe tablet is indicated: In combination with a statin, or alone when additional low-density lipoprotein cholesterol (LDL-C) lowering therapy is not possible, as an adjunct to diet to reduce elevated LDL-C in adults with primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH). In combination with a statin as an adjunct to diet to reduce elevated LDL-C in pediatric…
What are the side effects of Ezetimibe?
The following serious adverse reactions are discussed in greater detail in other sections of the label: Liver enzyme abnormalities [see Warnings And Precautions ( 5.2 )] Rhabdomyolysis and myopathy [see Warnings And Precautions ( 5.3 )] Common adverse reactions in clinical trials: o Ezetimibe administered alone (incidence ≥2% and greater than placebo): upper respiratory tract infection, diarrhea,… See the full label for the complete list.
Who makes Ezetimibe?
Ezetimibe is listed by 23 labelers in the FDA NDC directory, including A-S Medication Solutions, Accord Healthcare Inc., American Health Packaging, Amneal Pharmaceuticals NY LLC.