Statins

Statins competitively inhibit HMG-CoA reductase, the enzyme that sets the pace of cholesterol synthesis by turning HMG-CoA into mevalonate. Short of cholesterol, liver cells put more LDL receptors on their surface and take up more LDL from the blood, and the liver releases less VLDL. Plasma LDL cholesterol falls, and with it the risk of heart attack and stroke.

• AtorvastatinAfter a recent hemorrhagic stroke, its highest dose was linked to more hemorrhagic strokes (SPARCL), so the balance of risk and benefit is weighed.
• SimvastatinA lactone prodrug from a fungal fermentation product; its CYP3A4 interactions are serious enough that strong inhibitors are contraindicated.
• RosuvastatinBarely metabolized and long-acting; people of Asian descent, including South Asians, reach about double the exposure, so lower starting doses are used.
• PravastatinSwallowed in its active form, not as a prodrug; it has been shown to cut heart attacks and deaths both in people with known coronary disease and in those without.

• High LDL cholesterol, including familial forms
• Lowering the risk of heart attack and stroke
• High triglycerides (with diet)

• Muscle aches (myalgia)Known for
• Myopathy and rhabdomyolysisKnown forSerious
• Kidney injury from rhabdomyolysisSerious
• Immune-mediated necrotizing myopathy (rare)Serious
• Raised liver enzymes, rarely liver failureSerious
• Higher blood sugar and HbA1c
• Joint pain
• Nausea
• Diarrhea
• Headache

What the class has in common. Each drug's card has its own, and Known for marks what an exam expects you to know.

• Muscle harm is likelier at 65 or over, with uncontrolled hypothyroidism, kidney impairment, high doses, or with fibrates, niacin, cyclosporine or colchicine.
• Strong CYP3A4 inhibitors and large amounts of grapefruit juice raise simvastatin and atorvastatin levels and the muscle risk.
• Contraindicated in acute liver failure or decompensated cirrhosis; liver enzymes are checked before starting.
• Pregnancy: stopped once pregnancy is recognized; breastfeeding is not recommended.

Written for biofideX in plain words, after checking these references:

• Atorvastatin calcium tablets: label (DailyMed)
• Simvastatin tablets: label (DailyMed)
• HMG-CoA Reductase Inhibitor (NCI Thesaurus)
• Statins (NHS)

For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.