Rosuvastatin and Ezetimibe

Hypolipidaemic/Anti-atheroma · Cholesterol absorption inhibitor/HMG-CoA reductase inhibitor

Indications

Hyperlipidemia. Homozygous familial hypercholesterolemia.

Dosage

Oral: Hyperlipidemia: Rosuvastatin/ezetimibe 10 mg/10 mg-40 mg/10 mg daily. Homozygous familial hypercholesterolemia: Rosuvastatin/ezetimibe 10 mg/10 mg-40 mg/10 mg daily. Switching to rosuvastatin/ezetimibe from coadministration of a statin and ezetimibe: Starting dose determined by rosuvastatin dose plus ezetimibe 10 mg. Dosing in Asian patients: Start at 5 mg/10mg daily, owing to genotypic slow metabolism resulting in increased rosuvastatin plasma concentrations.

Adverse Effects

Headache, dizziness, nausea, abdominal pain, diarrhoea, myalgia, arthralgia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Active liver disease/decompensated cirrhosis. Precautions: Severe renal impairment (dosage adjustment required). Chronic alcoholic liver disease. Age factor =65 yrs. Uncontrolled hypothyroidism. Assess LDL-C when clinically appropriate, as early as 2 weeks after initiating therapy and adjusting dosage, if necessary.

Interactions

Gemfibrozil (avoid). Atazanavir, clarithromycin, colchicine, cyclosporine, darolutamide, eltrombopag, fenofibrate, indinavir, ketoconazole, lopinavir, mifepristone, nelfinavir, niacin, ritonavir, saquinavir.

Advice to Patient

Take with or without meals. Swallow whole tabs, do not crush, dissolve or chew. Take at least 2 hrs before or 4 hrs after bile acid sequestrant. Take at least 2 hrs before aluminum/magnesium hydroxide combination antacid. Report any unexplained muscle pain, tenderness or weakness, particularly if accompanied by malaise or fever.

Pharmacokinetics

ROSUVASTATIN: Onset of action: Within 1 wk, maximal at 4 wks. Metabolism: Hepatic (10%). Bioavailability: 20% (high first-pass extraction by liver). Half-life elimination: 19 hrs. Time to peak, plasma: 3-5 hrs. Excretion: Faeces (90%). EZETIMIBE: Onset of action: Within 1 wk. Max effect: 2-4 wks. Metabolism: Small intestine and liver. Bioavailability: Variable. Hepatic impairment: Moderate hepatic impairment (Child-Pugh score 7-9): AUC increased 3-4 times. Severe hepatic impairment (Child-Pugh 10-15): AUC increased 5-6 times. Renal impairment: Severe renal dysfunction (CrCl <30 mL/min/1.73 m2): AUC increased 1.5 times. Half-life elimination: 22 hrs (ezetimibe and metabolite).

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.