Contraindicated in:
Use Cautiously in:
CNS: dizziness, fatigue.
Resp: cough.
GI: abdominal pain, ↑ liver enzymes, nausea.
Derm: hot flushes.
F and E: hyperkalemia.
MS: MYOPATHY/RHABDOMYOLYSIS, arthralgia, musculoskeletal pain, muscle weakness.
Drug-Drug:
Drug-Food:
Therapeutic Classification: lipid-lowering agents
Pharmacologic Classification: hmg coa reductase inhibitors, cholesterol absorption inhibitors
Absorption: Atorvastatin rapidly absorbed but undergoes extensive gastrointestinal and hepatic metabolism resulting in 14% bioavailability (30% for lipid-lowering activity). Ezetimibe following absorption, rapidly converted to the active metabolite ezetimibe-glucaronide. Bioavailability is variable.
Distribution: Atorvastatin probably enters breast milk.
Protein Binding: Atorvastatin 98%.
Metabolism/Excretion: Atorvastatin extensively metabolized by the liver, most during first pass; excreted in bile and feces. <2% excreted unchanged by the kidneys. 2 metabolites have lipid-lowering activity. Ezetimibe undergoes enterhepatic recycling, mostly eliminated in feces, minimal renal excretion.
Half-life: Atorvastatin 14 hr (lipid-lowering activity due to atorvastatin and its metabolites 2030 hr). Ezetimibe 22 hr.
(cholesterol-lowering effect)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
atorvastatin PO | unknown | unknown | 2030 hr |
ezetimibe PO | unknown | unknown | unknown |