Brand and Other Names:Zetia
Dosing & Uses
Dosage Forms & Strengths
10 mg PO qDay
Overdose management: Treatment should be supportive
- Monotherapy: No dosage adjustment required
- Moderate to severe: Renal impairment is a risk factor for statin-associated myopathy; caution when coadministered with doses of simvastatin exceeding 20 mg
- Mild (Child-Pugh class A): Dose adjustment not necessary
- Moderate to severe (Child-Pugh class B or C): Not recommended
Dosage Forms & Strengths
<10 years: Safety and efficacy not established
>10 years: 10 mg PO qDay
Serious - Use Alternative
Significant - Monitor Closely
Upper respiratory tract symptoms (2-4%)
Pain in extremity (3%)
Increased liver transaminases (with HMG-CoA reductase inhibitors; ≥3 x ULN; 1%)
Hepatitis/liver function test abnormalities (LFTs elevated slightly higher in combination with statin than with statin alone)
Hypersensitivity reactions (including anaphylaxis, angioedema, rash, urticaria)
Elevated creatine phosphokinase
Cholelithiasis and cholecystitis
Coadministration with a statin in the presence of active liver disease or persistent, unexplained elevations of hepatic transaminase levels
Use caution in patients with mild hepatic impairment or severe renal impairment
Cholelithiasis reported (when coadministered with fibric acid derivatives)
Rule out secondary causes of hyperlipidemia prior to therapy
Pregnancy & Lactation
Pregnancy category: C
Lactation: Excretion in milk unknown; use with caution
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Inhibits sterol transporter at brush border and, consequently, intestinal absorption of cholesterol, which in turn decreases delivery of cholesterol to the liver and reduces hepatic cholesterol stores
Peak plasma time: 4-12 hr (parent drug); 1-2 hr (metabolite)
Peak plasma concentration: 3.4-5.5 ng/mL (parent drug); 45-71 ng/mL (metabolite)
Protein bound: >90%
Metabolized by glucuronide conjugation
Metabolites: Ezetimibe-glucuronide (80-90%)
Half-life: 22 hr
Excretion: Bile (78%), urine (11%)
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|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
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|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
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