In clinical studies of more than 4,700 patients, discontinuation rate due to adverse events was similar for ZETIA and placebo.
ZETIA is unlikely to interact with commonly used drugs or cytochrome P450.
When administered with statins, ZETIA had no effect on the pharmacokinetics of digoxin, oral contraceptives (ethinyl estradiol and levonorgestrel), glipizide, tolbutamide, midazolam, or warfarin.
ZETIA is neither an inhibitor nor an inducer of selected cytochrome P450 isozymes; no significant effect on 1A2, 2D6, 2C8/9, or 3A4 pathways.
In studies of ZETIA alone vs placebo
ZETIA alone had no significant impact on liver enzymes; elevations in serum transaminases (≥3 x ULN) were similar to those with placebo.
Most frequent adverse events greater than placebo: back pain (4.1% vs 3.9%), arthralgia (3.8% vs 3.4%), and fatigue (2.2% vs 1.8%).
Important Information About ZETIA
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, and Apo B in patients with primary (heterozygous familial and nonfamilial) hypercholesterolemia when diet alone is not enough.
Contraindications: hypersensitivity to any component of this medication.
Contraindications when used with a statin: active liver disease; unexplained persistent elevations of serum transaminases. Statins are contraindicated in pregnant and nursing women; refer to the statin label for details.
When using ZETIA with a statin, also follow the label recommendations for that specific statin.
The effects of ZETIA, either alone or in addition to a statin, on the risk of cardiovascular morbidity and mortality have not been established.
Selected Cautionary Information: When ZETIA was coadministered with a statin, consecutive elevations in serum transaminases (≥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.
Patients should be advised to promptly report muscle pain, tenderness, or weakness. Discontinue drug if myopathy is diagnosed or suspected.
ZETIA is not recommended in patients with moderate or severe hepatic insufficiency.
The coadministration of ZETIA with fibrates other than fenofibrate is not recommended until use in patients is 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.
In clinical trials, the most frequent side effects for ZETIA alone vs placebo included back pain (4.1% vs 3.9%), arthralgia (3.8% vs 3.4%), and fatigue (2.2% vs 1.8%); for ZETIA + statin vs statin or placebo alone: back pain (4.3% vs 3.7% vs 3.5%), abdominal pain (3.5% vs 3.1% vs 2.3%), and fatigue (2.8% vs 1.4% vs 1.9%).
Before prescribing ZETIA, please read the Prescribing Information and Patient Product Information.
For non-US health care professionals, click here.
