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PharmSpace

Statins · Cardiovascular

Atorvastatin

Lipitor®(brand names vary by market)

A high-intensity statin that shrugs at the clock.

Illustration of Atorvastatin as a tabletATO

Mechanism

HMG-CoA reductase inhibitor: less hepatic cholesterol synthesis, more LDL-receptor expression, lower circulating LDL.

Indications

  • Atherosclerotic cardiovascular disease, secondary prevention
  • Primary prevention in elevated risk
  • Familial hypercholesterolemia

Formulations

Tablet

Dosing concepts

Timing

Long half-life means any time of day works. Unlike short-acting simvastatin's evening rule.

Intensity

Statin doses are chosen by intended LDL reduction (moderate vs high intensity), not titrated to a number alone.

Concepts, not prescribing instructions. Practice numbers live in current references and local protocols.

Pharmacokinetics

Bioavailability
~14% (high first-pass)
Half-life
14 h (active metabolites ~20-30 h)
Elimination
hepatic: CYP3A4 substrate: the source of its famous interactions
Play with these concepts in the PK Lab

Adverse effects

  • MyalgiacommonTrue statin-associated muscle symptoms are less common than reported; rechallenge and dose strategy usually succeed.
  • Transaminase elevationcommon
  • RhabdomyolysisseriousRare; risk climbs with CYP3A4 inhibitors and interacting fibrates.
  • New diabetes (small excess risk)commonOutweighed by vascular benefit in indicated patients.

Contraindications & precautions

Contraindications

  • Active liver disease
  • Pregnancy and breastfeeding

Precautions

  • Concurrent strong CYP3A4 inhibitors
  • Hypothyroidism (myopathy risk)
  • High alcohol intake

Interactions

Monitoring

Lipid panel

Confirms the intended intensity was achieved · Baseline and ~8-12 weeks after start

CK only if significant muscle symptoms

Routine CK surveillance is not useful

ALT at baseline

Routine repetition is not required without symptoms

Counselling points

  • Any time of day, with or without food.
  • Report unexplained muscle pain or dark urine, especially after starting a new antibiotic or antifungal.
  • This is long-term prevention; it works while you take it.

Clinical pearls

  • Muscle symptoms with normal CK usually tolerate a washout and careful rechallenge; most patients end up back on a statin.

References & review

  • Atorvastatin product monograph (consult the current version for your market) (monograph)
  • Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed. (reference-work)

Last reviewed 2026-08-15 · jurisdiction: global · drug information changes; verify against current references before practice use.