Atorvastatin

Hypolipidaemic/Anti-atheroma · HMG-CoA reductase inhibitor

Indications

Adjunct to diet in primary hypercholesterolaemia, heterozygous and homozygous familial hypercholesterolaemia, mixed hyperlipidaemia.

Dosage

Adults: Initially 10 mg once daily. Increase as necessary at 4 wk intervals; max 80 mg once daily. Children: Under 10 yr, not recommended. Hyperlipidaemia including familial hypercholesterolaemia: 10-18 yr, initially 10 mg once daily, increased if necessary at intervals of at least 4 wk to usual max 20 mg once daily. Max 80 mg once daily in homozygous familial hypercholesterolaemia.

Adverse Effects

GI upset, headache, myalgia, asthenia, insomnia, dizziness, paraesthesia, fatigue, myalgia, hypoaesthesia, arthralgia, chest and back pain, hyperglycaemia, nasopharyngitis, pharyngolaryngeal pain, epistaxis, pain in extremity, muscle spasms, joint swelling, abnormal LFTs, raised creatine kinase levels. Elevated ALT and CPK levels. Reports of immune-mediated necrotising myopathy.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Active liver disease, persistent raised liver enzymes. Ensure adequate contraception. Precautions: History of alcohol abuse or liver disease. Perform liver function tests before and during therapy. Advise patients to report unexplained muscle weakness or pain; measure creatine kinase levels, withdraw if >5 × ULN. Renal impairment, hypothyroidism, history of muscle toxicity or muscle disorders, elderly. Interstitial lung disease; advise patients to report symptoms incl dyspnoea, non-productive cough, fatigue, wt loss, fever. Risk of new onset of diabetes; risk factors include hypertension, raised triglycerides, BMI and fasting blood glucose at baseline. Recent stroke or TIA.

Interactions

Cyclosporin, fibrates, azole antifungals, niacin, drugs metabolised by cytochrome P450 3A4, digoxin, erythromycin, oral contraceptives, antacids, warfarin, gemfibrozil, nicotinic acid, protease inhibitors, macrolides, rifampicin, other inhibitors, inducers or substrates of CYP3A4, grapefruit juice, colestipol, antacids, ezetimibe, diltiazem, verapamil, amiodarone, colchicine, with or within 7 days of systemic fusidic acid.

Advice to Patient

Take with or without meals. Take medication at the same time each day. Contact prescriber if there is unrelieved diarrhoea, fever, unusual muscle cramps, weakness, mood changes, memory changes, yellowing of skin or eyes, easy bruising or bleeding, or unusual fatigue. Take missed dose as soon as possible as you remember, unless it is nearly time for the next dose. Do not double the dose. Avoid high intake of grapefruit juice (> 1 litre per day). Take enough amount of fluid (2-3 litre per day) to prevent dehydration, unless advised by prescriber to restrict fluid intake. Laboratory tests are very important during therapy.

Pharmacokinetics

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.

Brands with this active ingredient

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

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