Safety and Tolerability

ZETIA + a statin: Overall safety profile compared to a statin alone, median duration of 8 weeks

  • The effect of ZETIA on cardiovascular morbidity and mortality has not been determined.
  • ZETIA, administered alone or in combination with an HMG-CoA reductase inhibitor (statin), is indicated as adjunctive therapy to diet for the reduction of elevated TOTAL-C, LDL-C, Apo B, and non–HDL-C in patients with primary (heterozygous familial and nonfamilial) hyperlipidemia when diet alone is not enough.
  • Contraindications: hypersensitivity to any component of this medication.
  • Statin contraindications apply when used with a statin: active liver disease; unexplained persistent elevations in hepatic transaminase levels. Statins are contraindicated in pregnant and nursing women. Refer to the statin label for details.
Clinical adverse reactionsa
Body System/Organ Class
Adverse Reaction
All Statins,b %
(n=9,361)
ZETIA + All Statins,b %
(n=11,308)
aClinical adverse reactions occurring in >2% of patients treated with ZETIA coadministered with a statin and at an incidence greater than statin, regardless of causality.
bAll statins = all doses of all statins.
Gastrointestinal Disorders
Diarrhea

2.2

2.5
General Disorders and
Administration Site Conditions

Fatigue


1.6


2.0
Infection and Infestations
Influenza
Nasopharyngitis
Upper respiratory tract infection

2.1
3.3
2.8

2.2
3.7
2.9
Musculoskeletal and Connective Tissue Disorders
Arthralgia
Back pain
Myalgia
Pain in extremity


2.4
2.3
2.7
1.9


2.6
2.4
3.2
2.1
 

SELECTED CAUTIONARY INFORMATION

  • When using ZETIA with a statin, also follow the label recommendations for that specific statin.
  • When ZETIA was coadministered with a statin, consecutive elevations in hepatic transaminase levels (≥3 × ULN) were slightly higher (1.3%) than those of statins alone (0.4%). Liver function tests should be performed when ZETIA is added to statin therapy and according to statin recommendations. Should an increase in ALT or AST ≥3 × ULN persist, consider withdrawal of ZETIA and/or the statin.
  • Patients should be advised to promptly report muscle pain, tenderness, or weakness. Risk for skeletal muscle toxicity increases with higher statin doses, advanced age (>65), hypothyroidism, renal impairment, and depending on the statin used, concomitant use of other drugs. Discontinue drug if myopathy is diagnosed or suspected.
  • Because renal impairment is a risk factor for statin-associated myopathy, doses of simvastatin exceeding 20 mg should be used with caution and close monitoring when administered concomitantly with ZETIA in patients with moderate to severe renal impairment (eGFR <60 mL/min/1.73 m2).
  • ZETIA is not recommended in patients with moderate to severe hepatic impairment.
  • The coadministration of ZETIA with fibrates other than fenofibrate is not recommended until use in patients is adequately studied.
  • Exercise caution when using ZETIA and cyclosporine concomitantly because exposure to both drugs is increased. Cyclosporine concentrations should be monitored in these patients.
  • ZETIA should be used in pregnant or nursing women only if the benefit outweighs the risk.
Before prescribing ZETIA, please read the Prescribing Information. The Patient Information also is available.
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ZETIA® (ezetimibe) Tablets