Ezetimibe

EZETIMIBE- ezetimibe tablet
Quallent Pharmaceuticals Health LLC

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 tablets are 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 the bile acid sequestrant [see Drug Interactions (7)].

3 DOSAGE FORMS AND STRENGTHS

10 mg tablets are white to off-white, capsule-shape, flat-face, beveled edge, uncoated tablets debossed with ‘773’ 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 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)].

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 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.

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 doubleblind, placebo-controlled clinical trials, 2,396 patients with primary hyperlipidemia (age range 9 years 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
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
Sinusitis 2.2 2.8
Pain in extremity 2.5 2.7
Fatigue 1.5 2.4
Influenza 1.5 2

Combination with a Statin

In 28 doubleblind, controlled (placebo or active-controlled) clinical trials, 11,308 patients with primary hyperlipidemia (age range 10 years 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

* All Statins = all doses of all statins

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

Combination with Fenofibrate

This clinical trial involving 625 patients with mixed dyslipidemia (age range 20 years 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 cholecystectomy were 0.6% and 1.7% for fenofibrate monotherapy and ezetimibe coadministered with fenofibrate, respectively [see Drug Interactions (7)].

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