Adult: Ezetimibe 10 mg and atorvastatin 10 mg tab Ezetimibe 10 mg and atorvastatin 20 mg tab Ezetimibe 10 mg and atorvastatin 40 mg tab Ezetimibe 10 mg and atorvastatin 80 mg tab
As an adjunct to diet and other lipid-lowering treatments (e.g. LDL apheresis): 10 mg/10 mg to 10 mg/80 mg once daily. Dose is individualised according to patient response. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Oral Cardiovascular risk reduction
Adult: Ezetimibe 10 mg and atorvastatin 10 mg tab Ezetimibe 10 mg and atorvastatin 20 mg tab Ezetimibe 10 mg and atorvastatin 40 mg tab Ezetimibe 10 mg and atorvastatin 80 mg tab
In patients with coronary heart disease and history of acute coronary syndrome: Usual dose range: 10 mg/10 mg to 10 mg/80 mg once daily. Dose is individualised according to patient response. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
Adult: Ezetimibe 10 mg and atorvastatin 10 mg tab Ezetimibe 10 mg and atorvastatin 20 mg tab Ezetimibe 10 mg and atorvastatin 40 mg tab Ezetimibe 10 mg and atorvastatin 80 mg tab
As an adjunct to diet: Usual dose range: 10 mg/10 mg to 10 mg/80 mg once daily. Dose is individualised according to patient response. Dosage and treatment recommendations may vary among countries and between individual products (refer to specific product guidelines).
What are the brands available for Ezetimibe + Atorvastatin in Hong Kong?
Patients taking lopinavir/ritonavir combination: Use the lowest necessary dose. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Patients taking clarithromycin, itraconazole, fosamprenavir, ritonavir (plus darunavir, fosamprenavir or saquinavir), elbasvir or grazoprevir: Max: 10 mg ezetimibe/20 mg atorvastatin daily. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Patients taking boceprevir, nelfinavir: Max: 10 mg ezetimibe/40 mg atorvastatin daily. Dosage recommendations may vary among countries and between individual products (refer to specific product guidelines).
Pharmacogenomics:
Atorvastatin
SLCO1B1 gene encodes OATP1B1, an influx transporter that mediates the hepatic uptake of statins and other exogenous and endogenous compounds (e.g. bilirubin and 17-β-glucuronosyl estradiol) for subsequent clearance. Polymorphisms in the SLCO1B1 gene (e.g. c.521T>C [rs4149056]) may cause increased systemic exposure to statins, which is thought to be the contributor to statin-associated musculoskeletal symptoms (SAMS). Genetic testing may be considered to identify those at significant risk, reduce the incidence of SAMS and optimise patient adherence.
Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline as of January 2022:
Phenotype and Genotype
Implications
Recommendations
SLCO1B1 decreased function
Patients carrying 1 normal or increased functional allele plus 1 non-functional allele e.g. *1/*5, *1/*15
Increased risk of myopathy due to increased atorvastatin exposure in comparison with normal function.
Initiate treatment at a dose of ≤40 mg and adjust doses according to disease-specific guidelines. Monitor for myopathy, particularly with 40 mg dose. If >40 mg dose is needed for desired efficacy, may consider combination therapy with a non-statin guideline-directed medical therapy; refer to specific country guidelines.
SLCO1B1 possible decreased function
Patients carrying 1 non-functional allele plus 1 unknown/uncertain functional allele e.g. *5/*6, *15/*10, *5/*43
Increased risk of myopathy due to increased atorvastatin exposure in comparison with normal function.
Initiate treatment at a dose of ≤40 mg and adjust doses according to disease-specific guidelines. Monitor for myopathy, particularly with 40 mg dose. If >40 mg dose is needed for desired efficacy, may consider combination therapy with a non-statin guideline-directed medical therapy; refer to specific country guidelines.
SLCO1B1 poor function
Patients carrying 2 non-functional alleles e.g. *5/*5, *5/*15, *15/*15
Increased risk of myopathy due to increased atorvastatin exposure in comparison to normal and decreased function.
Initiate treatment at a dose of ≤20 mg and adjust doses according to disease-specific guidelines. If >20 mg dose is needed for desired efficacy, may consider an alternative statin (rosuvastatin) or combination therapy with a non-statin guideline-directed medical therapy; refer to specific country guidelines.
Administration
Atorvastatin + Ezetimibe May be taken with or without food.
Contraindications
Active liver disease or unexplained persistent elevations of serum transaminases. Pregnancy and lactation. Concomitant use with glecaprevir/pibrentasvir combination.
Special Precautions
Patient with predisposition for myopathy or rhabdomyolysis (e.g. uncontrolled hypothyroidism); history of liver disease; diabetes mellitus; recent stroke or TIA. Patients who consume large amounts of alcoholic beverages. Patients with known SLCO1B1 gene polymorphism. Patients undergoing major surgery. Renal impairment. Elderly. Concomitant use with lopinavir/ritonavir combination, clarithromycin, itraconazole, fosamprenavir, ritonavir (plus darunavir, fosamprenavir or saquinavir), elbasvir, grazoprevir, boceprevir, nelfinavir and fusidic acid.
Adverse Reactions
Significant: Myopathy; increased HbA1c and fasting blood glucose; persistent serum transaminase elevations; new-onset or worsening of pre-existing myasthenia gravis or ocular myasthenia; interstitial lung disease. Rarely, immune-mediated necrotising myopathy. Gastrointestinal disorders: Diarrhoea, abdominal pain, nausea, dysgeusia. General disorders and administration site conditions: Asthenia, fatigue, malaise, oedema. Metabolism and nutrition disorders: Hyperkalaemia. Musculoskeletal and connective tissue disorders: Arthralgia, back pain. Nervous system disorders: Dizziness, headache, paraesthesia. Psychiatric disorders: Depression, insomnia. Respiratory, thoracic and mediastinal disorders: Dyspnoea, cough, bronchitis, sinusitis. Vascular disorders: Hot flush. Potentially Fatal: Rarely, hepatic failure; rhabdomyolysis with acute renal failure secondary to myoglobinuria.
Obtain lipid profile before treatment initiation; fasting lipid profile at baseline and during therapy. Monitor LFTs and creatine phosphokinase levels. Assess for signs and symptoms of myopathy, rhabdomyolysis, hepatotoxicity or new-onset diabetes mellitus.
Drug Interactions
Ezetimibe: Decreased absorption with bile acid sequestrants (e.g. colestyramine); administer at least 2 hours before or 4 hours after bile acid sequestrants.
Atorvastatin: Increased risk of myopathy and rhabdomyolysis with potent CYP3A4 inhibitors (e.g. ciclosporin, clarithromycin, itraconazole, HIV protease inhibitors), moderate CYP3A4 inhibitors (e.g. erythromycin, diltiazem, verapamil, fluconazole), hepatitis C antiviral agents (e.g. telaprevir, boceprevir, elbasvir/grazoprevir), fibric acid derivatives (e.g. gemfibrozil), niacin, colchicine, daptomycin. May increase the plasma concentration of digoxin, norethisterone and ethinylestradiol. Decreased plasma concentrations with CYP3A4 inducers (e.g. efavirenz, rifampicin). Potentially Fatal: Atorvastatin: Increased risk of myopathy and rhabdomyolysis with glecaprevir/pibrentasvir. Increased risk of rhabdomyolysis and toxic effects with fusidic acid; avoid concurrent use with or within 7 days of discontinuing fusidic acid.
Food Interaction
Increased risk of hepatic adverse effects with alcohol.
Atorvastatin: Increased plasma concentration with grapefruit juice. Decreased plasma concentrations with St. John's wort.
Action
Description: Mechanism of Action: Ezetimibe inhibits cholesterol absorption at the brush border of the small intestine through the sterol transporter Niemann-Pick C1-Like1 (NPC1L1), resulting in reduced cholesterol delivery to the liver, decreased hepatic cholesterol stores, and increased cholesterol clearance from the blood.
Atorvastatin selectively and competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyses the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis. This action results in a compensatory increase in the expression of LDL receptors on hepatic cell surfaces and a subsequent increase in the hepatic uptake and clearance of LDL-C from the blood. Onset: Ezetimibe: Within 1 week.
Atorvastatin: 3-5 days (initial changes); 2-4 weeks (Max reduction in plasma cholesterol and triglycerides). Pharmacokinetics: Absorption: Ezetimibe: Rapidly absorbed. Time to peak plasma concentration: 4-12 hours (ezetimibe); 1-2 hours (active metabolite).
Atorvastatin: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 14% (atorvastatin); approx 30% (atorvastatin and equipotent metabolites). Time to peak plasma concentration: 1-2 hours. Distribution: Ezetimibe: Plasma protein binding: >90%.
Atorvastatin: Volume of distribution: Approx 381 L. Plasma protein binding: ≥98%. Metabolism: Ezetimibe: Metabolised in the liver and small intestine via glucuronide conjugation into ezetimibe glucuronide (active metabolite); undergoes enterohepatic recycling.
Atorvastatin: Metabolised in the liver by CYP3A4 isoenzyme into active ortho- and parahydroxylated derivatives and inactive β-oxidation products. Undergoes extensive first-pass metabolism in the gastrointestinal mucosa and liver. Excretion: Ezetimibe: Mainly via faeces (78%, 69% as unchanged drug); urine (11%, 9% as metabolite). Elimination half-life: 22 hours.
Atorvastatin: Mainly via bile; urine (<2% as unchanged drug). Elimination half-life: Approx 14 hours (atorvastatin); approx 20-30 hours (equipotent metabolites).
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.
Atorvastatin Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 60823, Atorvastatin. https://pubchem.ncbi.nlm.nih.gov/compound/60823. Accessed July 28, 2022.
Storage
Store between 15-30°C. Protect from light and moisture.
C10BA05 - atorvastatin and ezetimibe ; Belongs to the class of HMG CoA reductase inhibitors in combination with other lipid modifying agents. Used in the treatment of hyperlipidemia.
References
Cooper-DeHoff R, Niemi M, Ramsey L et al. The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 Genotypes and Statin-Associated Musculoskeletal Symptoms. Clinical Pharmacology and Therapeutics. 2022 Feb;111(5):1007-1021. doi: 10.1002/cpt.2557. Accessed 25/07/2025. PMID: 35152405Annotation of CPIC Guideline for Atorvastatin and SLCO1B1. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org. Accessed 25/07/2025.Atorvastatin Calcium. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 25/07/2025.Atorvastatin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 25/07/2025.Atozet 10 mg/10 mg and 10 mg/20 mg Film-coated Tablets (Organon Hong Kong Limited). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 19/08/2025.Atozet 10 mg/10 mg, 10 mg/20 mg, 10 mg/40 mg and 10 mg/80 mg Film-coated Tablets (Organon Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 25/07/2025.Brayfield A, Cadart C (eds). Atorvastatin Calcium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/07/2025.Brayfield A, Cadart C (eds). Ezetimibe. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/07/2025.Ezetimibe and Atorvastatin. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 25/07/2025.Ezetimibe. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 25/07/2025.Ezetimibe. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 25/07/2025.Lypqozet Tablet (Althera Pharmaceuticals, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 25/07/2025.SLCO1B1 - Atorvastatin. UpToDate Lexidrug, Pharmacogenomics Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 25/07/2025.The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 Genotypes and Statin-Associated Musculoskeletal Symptoms. Clinical Pharmacogenetics Implementation Consortium (CPIC). https://cpicpgx.org. Accessed 25/07/2025.
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