Ezetimibe Brand Name– Zetia
What is Ezetimibe
Ezetimibe is an oral antilipemic agent, approved for use as monotherapy or in combination with HMG-CoA reductase inhibitors (‘statins’) or fenofibrate for the treatment of hypercholesterolemia.
It is the first available 2-azetidinone compound, a potent cholesterol absorption inhibitor. Ezetimibe selectively blocks the intestinal absorption of cholesterol and related phytosterols.
Monotherapy is primarily effective in reducing total cholesterol (total-C, 13%), LDL-cholesterol (LDL-C, 18%), and Apo-B (16%). Its effects to reduce triglycerides (8%) or to lower HDL-cholesterol (1%) are less prominent; ezetimibe typically increases HDL-cholesterol.
The reduction in LDL-cholesterol seen with ezetimibe monotherapy (18%) is less compared with more potent reductions (25—40%) typically achieved with statin monotherapy.
Combining ezetimibe with a statin results in synergistic cholesterol-lowering effects; and coadministration is more effective in improving serum total cholesterol, LDL-cholesterol, Apo-B, triglyceride, and HDL-cholesterol concentrations than either treatment given as monotherapy. When used in combination with 10—80 mg of either simvastatin or atorvastatin, LDL reductions of approximately 51 or 56%, respectively, are seen compared to LDL reductions of 36% with simvastatin or 44% with atorvastatin monotherapy.
When used in combination with 10—40 mg of either pravastatin or lovastatin, LDL reductions of approximately 39% or 40%, respectively, are seen compared to LDL reductions of 25% with either pravastatin or lovastatin monotherapy. The adverse effect profile for combined ezetimibe/statin therapy is similar to statin monotherapy, except for an increase in the incidence of hepatic enzyme elevations.
Administration of ezetimibe with fenofibrate is effective in improving serum total cholesterol, LDL-cholesterol, Apo-B, and non-HDL cholesterol concentrations in patients with mixed hyperlipidemia compared to monotherapy with either treatment.
The percent decrease in triglycerides and percent increase in HDL-cholesterol for ezetimibe coadministered with fenofibrate are comparable to values achieved by fenofibrate monotherapy
Indications
- hypercholesterolemia
- hyperlipoproteinemia
Side Effects
- abdominal pain
- anaphylactoid reactions
- angioedema
- arthralgia
- back pain
- cholecystitis
- cholelithiasis
- cough
- depression
- diarrhea
- dizziness
- elevated hepatic enzymes
- erythema multiforme
- fatigue
- headache
- hepatitis
- infection
- influenza
- muscle cramps
- musculoskeletal pain
- myalgia
- myasthenia
- myoglobinuria
- myopathy
- nausea
- pancreatitis
- paresthesias
- pharyngitis
- rash
- rhabdomyolysis
- sinusitis
- thrombocytopenia
- urticaria
Monitoring Parameters
- LFTs
- serum cholesterol profile
Contraindications
- breast-feeding
- children
- geriatric
- hepatic disease
- myopathy
- pregnancy
- renal impairment
Interactions
- Antacids
- Aspirin, ASA; Citric Acid; Sodium Bicarbonate
- Calcium Carbonate
- Calcium Carbonate; Magnesium Hydroxide
- Calcium Carbonate; Risedronate
- Calcium Carbonate; Simethicone
- Cholestyramine
- Colesevelam
- Colestipol
- Cyclosporine
- Eltrombopag
- Fenofibrate
- Fenofibric Acid
- Gemfibrozil
- Omeprazole; Sodium Bicarbonate
- Sodium Bicarbonate
- Warfarin
