Ezetimibe 10 mg Tablet, 500-count
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Dietary Cholesterol Absorption Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Ezetimibe is used along with diet, alone or in combination with another cholesterol-lowering medications (HMG-CoA reductase inhibitors [statins]) to reduce the amount of low-density lipoprotein (LDL) cholesterol ('bad cholesterol') in the blood in adults and children 10 years of age or older who have familial heterozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally). It is also used along with diet, alone or in combination with other cholesterol-lowering medications (HMG-CoA reductase inhibitors [statins] or fenofibrate) in adults...
Read the full MedlinePlus article ↗- Great question — they actually work in completely different places. Statins lower cholesterol by slowing down how much your liver makes. Ezetimibe works in your gut, blocking a pro...
- What exactly does ezetimibe do, and how is it different from a statin?
- You can take it either way — with or without food. A big, fatty meal might slightly raise the peak level of the drug in your blood, but it doesn't change how much gets absorbed ove...
- Can I take ezetimibe with food, or does it need to be taken on an empty stomach?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Ezetimibe — tap one for details:
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Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
Where does this data come from?
IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.067 | $33.60 / 500 tablets |
| Medicaid paysCMS SDUD · 12 mo | $0.2175 | $108.75 / 500 tablets |
| Medicare drug plans payPart D · Q2 2026 | $0.2167 | $108.35 / 500 tablets |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Ezetimibe 10 mgthis 00591-3713-05 | Actavis | 500 tablets | $0.067 | AB | Discontinued | — |
| Ezetimibe 10 mg 00904-7103-04 | Major | 30 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 16714-0813-01 | NorthStar | 30 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 50228-0379-05 | ScieGen | 500 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 50268-0298-12 | AvPAK | 20 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 51660-0200-05 | Ohm | 500 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 59651-0052-05 | Aurobindo | 500 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 60687-0373-21 | American | 30 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 68462-0226-05 | Glenmark | 500 tablets | $0.067 | AB | Availability likely | +0% |
| ezetimibe 10 mg 82009-0024-05 | Quallent | 500 tablets | $0.067 | AB | Availability likely | +0% |
| Ezetimibe 10 mg 16729-0433-10 | Accord | 30 tablets | $0.071 | AB | Availability likely | +6% |
| Ezetimibe 10 mg 00781-5690-05 | Sandoz | 500 tablets | $0.084 | AB | FDA listed | +26% |
| Zetia 10 mg 78206-0178-01 | Organon | 30 tablets | $13.964 | AB | Availability likely | +20683% |
| Ezetimibe 10 mg 10135-0787-05 | Marlex | 500 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 31722-0628-01 | Camber | 100 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 33342-0373-07 | Macleods | 30 tablets | — | — | FDA listed | — |
| Ezetimibe 10 mg 50090-3422-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-3657-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-6630-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-6631-00 | A-S | 90 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-7099-00 | A-S | 90 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-7236-00 | A-S | 90 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-7338-00 | A-S | 90 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-7339-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-7689-00 | A-S | 90 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 50090-7690-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 60429-0982-05 | Golden | 500 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 63629-7413-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 67877-0490-01 | Ascend | 100 tablets | — | AB | FDA listed | — |
| ezetimibe 10 mg 68382-0773-01 | Zydus | 100 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 69238-1154-01 | Amneal | 1000 tablets | — | AB | FDA listed | — |
| ezetimibe 10 mg 70771-1109-00 | Zydus | 1000 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 71205-0145-30 | Proficient | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 71205-0277-30 | Proficient | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 71335-0684-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 71335-0933-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 71335-1127-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 71335-2123-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 71335-3092-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 76333-0170-15 | Orient | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 82804-0064-30 | Proficient | 30 tablets | — | AB | FDA listed | — |
| Ezetimibe 10 mg 82804-0211-30 | Proficient | 30 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
💊 Medicaid utilization by pack size
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Reporter sex
Serious outcomes
Where does this data come from?
📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 00591-3713-05 You're viewing this | 500 TABLET in 1 BOTTLE (0591-3713-05) | $0.0672 / ea | $33.60 | 2017-06-12 | Discontinued by firm |
| 00591-3713-19 | 90 TABLET in 1 BOTTLE (0591-3713-19) | $0.0672 / ea | $6.05 | 2017-06-12 | Discontinued by firm |
| 00591-3713-30 | 30 TABLET in 1 BOTTLE (0591-3713-30) | $0.0672 / ea | $2.02 | 2017-06-12 | Discontinued by firm |
| 00591-3713-00 | 100000 TABLET in 1 BOX (0591-3713-00) | — | — | — | Active |
You're viewing one of 4 pack sizes for this product.
This pack has the lowest per-ea cost of the 3 priced pack sizes ($0.0672 NADAC).
In Medicaid, this is the most-dispensed pack of this product — about 58% of fills over the last four reported quarters. See all packs ↓
Pack size FAQ
What quantity is in NDC 00591-3713-05?
What is the difference between NDC 00591-3713-05 and NDC 00591-3713-30?
What NDC number is used to bill for this package of Ezetimibe 10 mg Tablet?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | — Not published for this NDC No photo available yet for this listing. |
| Inactive ingredients (structured) | — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available. |
| NADAC pharmacy acquisition price (CMS) | ✓ Available |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | ✓ Available |
Questions about this listing
What does the discontinued status mean for this NDC?
Is the NDC printed on the package the same as the 11-digit billing NDC?
What do the three segments of this NDC mean?
Does this product come in other package sizes?
Who lists this product with the FDA?
Do I need a prescription for this product?
Where does this data come from?
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Ezetimibe tablets are 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 tablets are 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 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 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 ▾
2 DOSAGE AND ADMINISTRATION The recommended dose of ezetimibe tablets 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 tablets. Administer ezetimibe tablets at least 2 hours before or 4 hours after administration of a 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 ▾
3 DOSAGE FORMS AND STRENGTHS 10-mg tablets are white to off-white, capsule-shaped tablets debossed with “ 713 ” on one side and plain on the other side. Tablets: 10 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Ezetimibe tablets are contraindicated in patients with a known hypersensitivity to ezetimibe or any of the excipients in ezetimibe. 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 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. ( 4 ) When used in combination with a statin, fenofibrate, or other LDL-C lowering therapy, ezetimibe 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 Cautions ▾
5 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. Perform liver enzyme testing as clinically indicated and consider withdrawal of ezetimibe if increases in ALT or AST ≥3 X ULN persist.
( 5.2 ) Skeletal Muscle Effects (e.g., Myopathy and Rhabdomyolysis) : Ezetimibe 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 and other concomitant medications, as appropriate.
( 5.3 )
5.1Risks Associated with Combination Treatment with a Statin, Fenofibrate, or Other LDL-C Lowering Therapies If ezetimibe 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 )] .
5.2Liver Enzymes Increases in serum transaminases have been reported with use of ezetimibe [see Adverse Reactions ( 6.1 )] . In controlled clinical combination studies of ezetimibe initiated concurrently with a statin, the incidence of consecutive elevations (≥3 X 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 if increases in ALT or AST ≥3 X ULN persist.
5.3Myopathy / Rhabdomyolysis Ezetimibe 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 and other concomitant medications, as appropriate.
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS 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: Ezetimibe administered alone (incidence ≥2% and greater than placebo): upper respiratory tract infection, diarrhea, arthralgia, sinusitis, pain in extremity, fatigue, and influenza. ( 6.1 ) Ezetimibe 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 Teva at 1-888-838-2872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical 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, 2,396 patients with primary hyperlipidemia (age range 9 to 86 years; 50% female, 90% White, 5% Black or African American, 2% Asian, 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 ezetimibe are 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 Tablets 10 mg (%) n = 2,396 Upper respiratory tract infection 2.5
4.3Diarrhea 3.7
4.1Arthralgia 2.2
3.0Sinusitis 2.2
2.8Pain in extremity 2.5
2.7Fatigue 1.5
2.4Influenza 1.5
2.0Combination 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% Asian, 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 X 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
3.7Myalgia 2.7
3.2Upper respiratory tract infection 2.8
2.9Arthralgia 2.4
2.6Diarrhea 2.2
2.5Back pain 2.3
2.4Influenza 2.1
2.2Pain in extremity 1.9
2.1Fatigue 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 X 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 cho…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Table 3 includes a list of drugs with clinically important drug interactions when administered concomitantly with ezetimibe and instructions for preventing or managing them. Table 3: Clinically Important Drug Interactions with Ezetimibe 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 )
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy 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 should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
When ezetimibe 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.
8.2Lactation 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 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.
8.4Pediatric 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 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 growt…
🤰 Pregnancy ▾
8.1Pregnancy 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 should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
When ezetimibe 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.
🧒 Pediatric Use ▾
8.4Pediatric 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 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 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 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.
🧓 Geriatric Use ▾
8.5Geriatric 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.
No clinically meaningful differences in the pharmacokinetics of ezetimibe were observed in geriatric patients compared to younger adult patients [see Clinical Pharmacology ( 12.3 )] .
🆘 Overdosage ▾
10 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.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols. Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver.
This causes a reduction of hepatic cholesterol stores and an increase in LDL receptors, resulting in clearance of cholesterol from the blood.
12.2Pharmacodynamics Ezetimibe reduces total cholesterol (total-C), LDL-C, apolipoprotein (Apo) B, and non-high-density lipoprotein cholesterol (non-HDL-C) in patients with hyperlipidemia. In a 2-week clinical trial in 18 hypercholesterolemic patients, ezetimibe inhibited intestinal cholesterol absorption by 54%, compared with placebo. Ezetimibe had no clinically meaningful effect on the plasma concentrations of the fat-soluble vitamins A, D, and E (in a trial of 113 patients) and did not impair adrenocortical steroid hormone production (in a trial of 118 patients).
12.3Pharmacokinetics Absorption After oral administration, ezetimibe is absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide (ezetimibe-glucuronide). After a single 10-mg dose of ezetimibe to fasted adults, mean ezetimibe peak plasma concentrations (C max ) of 3.4 to 5.5 ng/mL were attained within 4 to 12 hours (T max ). Ezetimibe-glucuronide mean C max values of 45 to 71 ng/mL were achieved between 1 and 2 hours (T max ).
There was no substantial deviation from dose proportionality between 5 and 20 mg. The absolute bioavailability of ezetimibe cannot be determined, as the compound is virtually insoluble in aqueous media suitable for injection. Effect of Food Concomitant food administration (high-fat or non-fat meals) had no effect on the extent of absorption of ezetimibe when administered as ezetimibe 10-mg tablets.
The C max value of ezetimibe was increased by 38% with consumption of high-fat meals. Distribution Ezetimibe and ezetimibe-glucuronide are highly bound (>90%) to human plasma proteins. Elimination Metabolism Ezetimibe is primarily metabolized in the small intestine and liver via glucuronide conjugation (a phase II reaction) with subsequent biliary and renal excretion.
Minimal oxidative metabolism (a phase I reaction) has been observed in all species evaluated. In humans, ezetimibe is rapidly metabolized to ezetimibe-glucuronide. Ezetimibe and ezetimibe-glucuronide are the major drug-derived compounds detected in plasma, constituting approximately 10 to 20% and 80 to 90% of the total drug in plasma, respectively.
Both ezetimibe and ezetimibe-glucuronide are eliminated from plasma with a half-life of approximately 22 hours for both ezetimibe and ezetimibe-glucuronide. Plasma concentration-time profiles exhibit multiple peaks, suggesting enterohepatic recycling. Excretion Following oral administration of 14 C-ezetimibe (20 mg) to human subjects, total ezetimibe (ezetimibe + ezetimibe-glucuronide) accounted for approximately 93% of the total radioactivity in plasma.
After 48 hours, there were no detectable levels of radioactivity in the plasma. Approximately 78% and 11% of the administered radioactivity were recovered in the feces and urine, respectively, over a 10-day collection period. Ezetimibe was the major component in feces and accounted for 69% of the administered dose, while ezetimibe-glucuronide was the major component in urine and accounted for 9% of the administered dose.
Specific Populations Geriatric Patients In a multiple-dose trial with ezetimibe given 10 mg once daily for 10 days, plasma concentrations for total ezetimibe were about 2-fold higher in older (≥65 years) healthy subjects compared to younger subjects. However, the difference in plasma co…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. The molecular target of ezetimibe has been shown to be the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is involved in the intestinal uptake of cholesterol and phytosterols. Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver.
This causes a reduction of hepatic cholesterol stores and an increase in LDL receptors, resulting in clearance of cholesterol from the blood.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Ezetimibe tablets, USP 10 mg, are white to off white, capsule-shaped tablets debossed with " 713 " on one side and plain on the other side. They are supplied as follows: NDC 0591-3713-30 bottles of 30 NDC 0591-3713-19 bottles of 90 NDC 0591-3713-05 bottles of 500 Storage Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from moisture.
📋 Description ▾
11 DESCRIPTION Ezetimibe, USP 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, USP is a white, crystalline powder that is freely to very soluble in ethanol, methanol, and acetone and practically insoluble in water. Ezetimibe, USP has a melting point of about 163°C and is stable at ambient temperature. Ezetimibe, USP is available as a tablet for oral administration containing 10 mg of ezetimibe and the following inactive ingredients: croscarmellose sodium, crospovidone, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium lauryl sulfate. structural formula
💬 Information for Patients ▾
17 PATIENT COUNSELING 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 )] .
Breastfeeding 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. Dispense with Patient Package Insert available at: www.tevausa.com/PatientPI Manufactured In India By: Watson Pharma Private Limited Verna, Salcette Goa 403 722 INDIA Manufactured For: Teva Pharmaceuticals Parsippany, NJ 07054 Rev. C 3/2024