atorvastatin calcium trihydrate: clinical use

Prescribing considerations

• Review secondary causes of dyslipidaemia, cardiovascular risk, concurrent medicines, alcohol intake, hepatic history and factors predisposing to myopathy.
• Use caution with renal impairment, untreated hypothyroidism, previous statin or fibrate muscle toxicity, hereditary muscle disorders, substantial alcohol use, liver history and interacting medicines.
• Consider the individual benefit-risk balance after previous haemorrhagic stroke or lacunar infarction.
• Statins may induce or aggravate myasthenia gravis or ocular myasthenia; reassess treatment if symptoms worsen.

Contraindications and cautions

• Hypersensitivity to atorvastatin or a product excipient.
• Active liver disease or unexplained persistent serum transaminases above three times the upper limit of normal.
• Pregnancy; selected product licences also contraindicate breastfeeding and use in people of child-bearing potential without appropriate contraception.
• Concomitant glecaprevir/pibrentasvir.

Monitoring

• Before treatment, assess liver transaminases and a lipid profile; consider renal function, glycaemic status, thyroid function and CK according to clinical risk.
• Repeat lipids to assess response and adherence, and repeat liver tests after initiation and when clinically indicated.
• Measure CK when persistent unexplained muscle pain, tenderness or weakness occurs; interpret results clinically and avoid sampling immediately after strenuous exercise.
• Monitor glucose or HbA1c in people at increased risk of diabetes.

Clinical pharmacology

Atorvastatin selectively and competitively inhibits HMG-CoA reductase. It undergoes substantial first-pass metabolism, is highly protein-bound and is metabolised mainly by CYP3A4 to active metabolites. Hepatic uptake and elimination involve OATP1B1/OATP1B3, P-glycoprotein and BCRP pathways.

Formulation and product differences

• Film-coated tablets are swallowed with water; excipients vary by manufacturer, so check the specific SmPC where allergy or intolerance is relevant.
• Lipitor chewable tablets can be chewed or swallowed whole and contain aspartame, a source of phenylalanine.
• The oral suspension must be shaken well and measured with its oral syringe. It contains methyl, ethyl and propyl parahydroxybenzoates and a small amount of benzyl alcohol.

Chewable tablet

Route: Oral

Strengths: 10 mg, 20 mg

Oral suspension

Route: Oral

Strengths: 4 mg/mL

Tablet

Route: Oral

Strengths: 10 mg, 20 mg, 30 mg, 40 mg, 60 mg, 80 mg