Ezetimibe

EZETIMIBE- ezetimibe tablet
Ohm Laboratories Inc.

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.

2 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 tablets.
  • Administer ezetimibe tablets at least 2 hours before or 4 hours after administration of a bile acid sequestrant [ see Drug Interactions (7)].

3 DOSAGE FORMS AND STRENGTHS

10 mg tablets are white to off-white, capsule-shaped uncoated tablets with ” E 10 ” debossed on one side and plain on other side.

4 CONTRAINDICATIONS

Ezetimibe tablets are 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 tablets are contraindicated in patients for whom a statin, fenofibrate, or other LDLC lowering therapy are contraindicated. Refer to the Prescribing Information of these products for a list of their contraindications [see Warnings and Precautions (5.1)]

5 WARNINGS AND PRECAUTIONS

5.1 Risks Associated with Combination Treatment with a Statin, Fenofibrate, or Other LDL-C Lowering Therapies

If ezetimibe tablets are 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 X ULN) in hepatic transaminase levels was 1.3% for patients treated with ezetimibe tablets 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 X 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.

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)]

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, 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 tablets 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 tablets and at an incidence greater than placebo in placebo-controlled studies of ezetimibe tablets are shown in Table 1.

TABLE 1: Adverse Reactions Occurring in ≥ 2% and Greater than Placebo in ezetimibe tablets -treated Patients

Adverse Reactions Placebo (%) n=1,159

Ezetimibe tablets 10mg (%)

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
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% Asian, 5% other races; 4% identified as Hispanic or Latino ethnicity) and elevated LDL-C were treated with ezetimibe tablets 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 times ULN) was higher in patients receiving ezetimibe tablets administered with statins (1.3%) than in patients treated with statins alone (0.4%).

Adverse reactions reported in ≥2% of patients treated with ezetimibe tablets + statin and at an incidence greater than statin are shown in Table 2.

TABLE 2: Adverse Reactions Occurring ≥2% in ezetimibe tablets -treated Patients Co-administered with a Statin and at an Incidence Greater than Statin

Adverse Reaction

All Statins*

(%)

All Statins*

(%)

n = 9,361

Ezetimibe Tablets + 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 co-administration of ezetimibe tablets 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 tablets co-administered 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 tablets co-administered with fenofibrate, respectively [see Drug Interactions (7)].

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