Adult: As an adjunct to diet: Monotherapy or in combination with a statin: 10 mg once daily. Child: ≥10 years Same as adult dose.
Oral Cardiovascular risk reduction
Adult: In patients with CHD and history of acute coronary syndrome: In combination with a statin: 10 mg once daily.
Oral Homozygous familial hypercholesterolaemia
Adult: As an adjunct to diet: In combination with a statin and other therapies (e.g. LDL apheresis): 10 mg once daily. Child: ≥10 years Same as adult dose.
Oral Homozygous familial sitosterolaemia
Adult: As an adjunct to diet to decrease elevated sitosterol and camposterol levels: 10 mg once daily. Child: ≥10 years Same as adult dose.
Hepatic Impairment
Moderate or severe (Child-Pugh class B or C): Not recommended.
Administration
May be taken with or without food.
Contraindications
Co-administration with a statin, fenofibrate or other LDL-C lowering therapies when contraindications for such agents are present (refer to the specific product information of concomitant agent used for the detailed contraindications).
Special Precautions
Patient with risk factors for myopathy/rhabdomyolysis (e.g. uncontrolled hypothyroidism). When co-administered with a statin, fenofibrate or other LDL-C lowering therapies, refer to the specific product information of the concomitant agent used for detailed risks or warnings. Renal and moderate or severe (Child-Pugh class B or C) hepatic impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Hepatic effects, including increased serum AST/ALT levels and acute liver injury (e.g. hepatocellular hepatitis, cholestatic hepatitis); muscle-related effects (e.g. myalgia, myopathy, rhabdomyolysis [very rarely]). Gastrointestinal disorders: Abdominal pain, flatulence, diarrhoea, nausea, dyspepsia, dry mouth. General disorders and administration site conditions: Fatigue. Immune system disorders: Anaphylaxis, angioedema. Investigations: Increased blood creatine phosphokinase (CPK). Musculoskeletal and connective tissue disorders: Arthralgia, muscle spasm, pain in extremity. Nervous system disorders: Headache, dizziness, paraesthesia. Respiratory, thoracic and mediastinal disorders: URTI, sinusitis. Skin and subcutaneous tissue disorders: Rash, urticaria, pruritus.
Obtain lipid profile before starting treatment, 4-12 weeks after treatment initiation and every 3-12 months thereafter. Monitor LFTs at baseline and as clinically indicated (particularly when combined with a statin); CPK levels. Monitor for signs and symptoms of myopathy and cholelithiasis (particularly when used with fenofibrate).
Drug Interactions
Decreased absorption with bile acid sequestrants (e.g. colestyramine); administer ezetimibe at least 2 hours before or 4 hours after the bile acid sequestrant. Increased plasma concentration with ciclosporin and gemfibrozil. Increased risk of cholelithiasis and gallbladder disease with fenofibrate. May result in increased INR with oral anticoagulants (e.g. warfarin, fluindione).
Action
Description: Mechanism of Action: Ezetimibe selectively inhibits cholesterol absorption at the brush border of the small intestine via the Niemann-Pick C1-Like 1 (NPC1L1) sterol transporter, thus reducing the delivery of intestinal cholesterol to the liver. This activity decreases the hepatic cholesterol stores and increases cholesterol clearance from the blood. Onset: Within 1 week. Pharmacokinetics: Absorption: Rapidly absorbed. Time to peak plasma concentration: 4-12 hours (ezetimibe); 1-2 hours (ezetimibe-glucuronide). Distribution: Plasma protein binding: >90%. Metabolism: Metabolised in the small intestine and liver via glucuronide conjugation into ezetimibe-glucuronide (active glucuronide metabolite); undergoes enterohepatic recycling. Excretion: Mainly via faeces (78%, 69% as unchanged drug); urine (11%, 9% as metabolite). Elimination half-life: 22 hours.
Chemical Structure
Ezetimibe Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 150311, Ezetimibe. https://pubchem.ncbi.nlm.nih.gov/compound/Ezetimibe. Accessed Jan. 25, 2024.
C10AX09 - ezetimibe ; Belongs to the class of other lipid modifying agents.
References
Anon. Ezetimibe. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 09/08/2023.Anon. Ezetimibe. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/12/2023.Buckingham R (ed). Ezetimibe. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/08/2023.Ezetimibe 10 mg Tablets (Key Pharmaceuticals Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 14/12/2023.Ezycor Tablet 10 mg (Y.S.P. Industries [M] Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 09/08/2023.Joint Formulary Committee. Ezetimibe. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 09/08/2023.Paediatric Formulary Committee. Ezetimibe. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 14/12/2023.Sandoz New Zealand Limited. Ezetimibe Sandoz 10 mg Tablet data sheet 20 March 2023. Medsafe. http://www.medsafe.govt.nz. Accessed 14/12/2023.Zetia Tablet (Organon LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 14/12/2023.
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