Atorvastatin and Ezetimibe

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

Indications

Adjunct to diet in primary hypercholesterolaemia for patients not appropriately controlled with a statin alone, or as monotherapy when a statin is inappropriate or not tolerated. Adjunct to diet in homozygous familial hypercholesterolaemia.

Dosage

Adults: 1 tab daily using the strength as clinically appropriate. Children: Not recommended.

Adverse Effects

GI upset, headache, myalgia, asthaenia, insomnia. Elevated ALT and CPK levels.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Moderate to severe hepatic impairment, concomitant use with a statin in active liver disease. Precautions: Monitor liver function, history of alcohol abuse.

Interactions

Fibrates, cyclosporin, cholestyramine, colestipol, azole antifungals, niacin, drugs metabolised by cytochrome P450 3A4, digoxin, erythromycin, oral contraceptives, antacids, warfarin.

Advice to Patient

Take with or without meals. Do not break, crush or chew tablet. Swallow whole. Complete full course of therapy even if you feel better before completion of course. Contact prescriber if there is any allergic reaction (rash, hives, itching, swelling on face/tongue/throat, difficulty in breathing), severe dizziness, muscle pain/tenderness/weakness. Avoid grapefruit products and red yeast rice products during therapy. Reduce alcohol intake. Certain laboratory tests are required during treatment, keep all doctors and lab appointments. Check blood sugar level regularly and inform prescriber about changes.

Pharmacokinetics

ATORVASTATIN: Onset of action: Initial changes: 3-5 days. Maximal reduction in plasma cholesterol and triglycerides: 2-4 wks. LDL reduction: 10 mg/day: 39%. Absorption: Oral: Rapidly absorbed; extensive first-pass metabolism in GI mucosa and liver. Metabolism: Hepatic. Bioavailability: Parent drug: Approx. 14%. Parent drug and equipotent metabolites: Approx. 30%. Half-life elimination: Parent drug: Approx. 14 hrs. Equipotent metabolites: 20-30 hrs. Time to peak, serum: 1-2 hrs. Excretion: Bile. Urine. 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…

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

Always consult a pharmacist or doctor.