Simvastatin + Ezetimibe


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Hypercholesterolaemia; Hyperlipidaemias; Hyperlipoproteinaemia; Hypertriglyceridaemia As tab containing ezetimibe (mg)/simvastatin (mg): 10/10, 10/20, 10/40, 10/80. Usual initial: 10/20 mg/day. Daily dose range: 10/10 mg to 10/80 mg.
Dosage Details
Oral
Hypercholesterolaemia, Hyperlipidaemias, Hypertriglyceridaemia, Hyperlipoproteinaemia
Adult: As tablet containing ezetimibe (mg)/simvastatin (mg): 10/10, 10/20, 10/40, 10/80. Usual starting dose: 10/20 mg daily. Dose may range from 10/10 mg daily to 10/80 mg daily.
Renal Impairment
CrClDosage
< 6010/20 mg in the evening. Higher dose to be used with caution.
Administration
May be taken with or without food. Avoid excessive consumption (>1 L/day) of grapefruit juice.
Contraindications
Hypersensitivity, acute liver disease or unexplained persistent elevations of serum transaminases. Pregnancy, lactation. Patients of Chinese descent should not take 80 mg of simvastatin with lipid-modifying dose of niacin-containing products (≥1g/day).
Special Precautions
History of liver disease. Risk of rhabdomyolysis increased in the presence of severe infection, hypotension, major surgical trauma, uncontrolled seizures and severe metabolic, endocrine and electrolyte disorder. Alcoholism; premenarcheal females; child <10 yr.
Adverse Reactions
Headache, nausea, flatulence, heartburn, abdominal pain, diarrhoea or constipation, dysgeusia; dose related myopathy (e.g. myalgia, muscle weakness and dark urine); serum transaminases and CPK elevations; hypersensitivity; lens opacities; blurring of vision; dizziness; sexual dysfunction; insomnia; depression, upper resp symptoms, dizziness, sinusitis, pharyngitis; chest pain, arthralgia and fatigue.
Potentially Fatal: Severe rhabdomyolysis with acute renal failure.
Drug Interactions
Simvastatin may cause slight elevation of serum digoxin. Cholestyramine and colestipol increase bioavailability of simvastatin. Increase in ezetimibe plasma levels with ciclosporin. Increased risk of myopathy when used with ciclosporin, gemfibrozil, danazol, amiodarone and verapamil.
Potentially Fatal: Concurrent use with itraconazole, ketoconazole, niacin, telithromycin, clarithromycin, erythromycin, nefazodone and HIV protease inhibitors may increase the risk of rhabdomyolysis and acute renal failure. Increased risk of hemorrhage with anticoagulants.
Food Interaction
Avoid intake of large quantities of grapefruit juice.
Action
Description: Simvastatin inhibits the conversion of HMG-CoA to mevalonic acid by blocking the enzyme HMG-CoA reductase, an early and rate limiting step in the biosynthesis of cholesterol. Ezetimibe localises at the brush border of the small intestine where it inhibits the absorption of cholesterol, decreasing the delivery of intestinal cholesterol to the liver. Cholesterol absorption is an active process and ezetimibe inhibits the protein transporters on small intestinal enterocyte brush border that bring about this active transport.
Pharmacokinetics:
Absorption: Ezetimibe: Absorbed and extensively conjugated to a pharmacologically active phenolic glucuronide after oral admin. Simvastatin: Extensive 1st pass extraction.
Distribution: Ezetimibe and simvastatin: Highly protein-bound.
Metabolism: Ezetimibe: Mainly metabolised in the small intestine and liver via glucuronide conjugation.
Excretion: Ezetimibe: Biliary and renal excretion. Simvastatin: Urine and faeces.
Disclaimer: This information is independently developed by MIMS based on Simvastatin + Ezetimibe from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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