Ezetimibe

Indications
 Oral
Hyperlipidaemias, Homozygous familial sitosterolaemia
Adult: 10 mg once daily.
Contraindications
 Hypersensitivity; moderate to severe liver disease or unexplained serum transaminase elevation. Children <10 yr, lactation.
Warnings / 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.
Adverse Reactions
 Abdominal discomfort, headache, dizziness, sinusitis, pharyngitis; diarrhoea, chest pain, arthralgia, myalgia, resp infection and fatigue.
Drug Interactions
 Concomitant admin of ezetimibe with cholestyramine may decrease serum levels of ezetimibe resulting in lower efficacy. Concurrent use of ezetimibe and cyclosporine may lead to increased exposure to both drugs, thus caution should be exercised.
See Below for More ezetimibe Drug Interactions
Mechanism of Actions
 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.
Absorption: Peak plasma concentrations after 4-12 hr.
Distribution: Protein-binding: >90%.
Metabolism: Undergoes conjugation in small intestines and liver.
Excretion: Faeces (69% unchanged drug); urine (9% metabolite); 22 hr (elimination half-life).
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store at 25°C.
ATC Classification
 C10AX09 - ezetimibe ; Belongs to the class of other lipid modifying agents.
Storage
 Oral: Store at 25°C.
Available As
  • Ezetimibe 10 mg
  • Ezetimibe 5 mg

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