Ezetimibe
Indications
Ezetimibe is used for:
Hyperlipidaemias, Homozygous familial sitosterolaemia, Hypercholesterolaemia
Adult Dose
Oral
Hyperlipidaemias; Homozygous familial sitosterolaemia
Adult: 10 mg once daily.
Hepatic impairment
Mild (Child-Pugh class A): Dose adjustment not necessary
Moderate to severe (Child-Pugh class B or C): Not recommended
Child Dose
Child: >10 yr: 10 mg once daily.
Renal Dose
Renal impairment
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
Administration
May be taken with or without food.
Contra Indications
Hypersensitivity; moderate to severe liver disease or unexplained serum transaminase elevation. Children <10 yr, lactation.
Precautions
Renal or mild hepatic impairment. Monitor LFTs. Immediately discontinue ezetimibe and any HMG-CoA reductase inhibitor or fibrate if myopathy is diagnosed or suspected. Exclude or treat secondary causes of dyslipidaemia prior to initiating therapy.
Lactation: Excretion in milk unknown; use with caution
Pregnancy-Lactation
Pregnancy category: C
Lactation: Excretion in milk unknown; use with caution
Interactions
Reduced absorption w/ colestyramine. Increased plasma concentrations w/ ciclosporin. Concomitant use w/ oral anticoagulants may result in increased INR.
Adverse Effects
Side effects of Ezetimibe :
1-10%
Diarrhea (4%), Upper respiratory tract symptoms (2-4%), Cough (2-4%), Pain in extremity (3%), Sinusitis (3%), Arthralgia (2-3%), Fatigue (2%), Influenza (2%), Increased liver transaminases (with HMG-CoA reductase inhibitors; >3 x ULN; 1%)
Mechanism of Action
Ezetimibe localises at the brush border of the small intestine where it inhibits the absorption of cholesterol, thus decreasing its delivery to the liver. This results in decrease in cholesterol stores within the liver and an increase in cholesterol clearance from the blood.