Statins
Also known as: HMG-CoA reductase inhibitors, cholesterol-lowering drugs
The main cholesterol-lowering medicines. They cut LDL cholesterol by 30-55% and reduce heart attacks and strokes in anyone at raised cardiovascular risk.
- Biological target
- HMG-CoA reductase
- Also called
- HMG-CoA reductase inhibitors, cholesterol-lowering drugs
Mechanism of action
Statins block HMG-CoA reductase, the enzyme that controls how much cholesterol the liver makes. The liver compensates by displaying more LDL receptors, pulling LDL out of the blood. Lower LDL means less cholesterol deposited in artery walls, and statins also stabilise existing plaques so they are less likely to rupture and cause a clot. High-intensity statins (atorvastatin 40-80 mg, rosuvastatin 20-40 mg) are used after heart attacks and strokes.
Members of the class
Members with a page on this site are linked.
Conditions treated
Class effects
- Muscle aches in a minority
- Headache, digestive upset
- Small rise in blood glucose
Cautions
- Interactions with clarithromycin, some antifungals and ciclosporin; grapefruit with simvastatin
- Unexplained muscle pain with dark urine needs a same-day creatine kinase test
- Not in pregnancy or active liver disease
Class warnings
- Muscle toxicity (myopathy, rarely rhabdomyolysis) is the main class hazard; unexplained muscle pain, weakness or dark urine needs a creatine kinase test. Risk rises with dose, interacting drugs, hypothyroidism, kidney impairment and older age. UK
- Contraindicated in active liver disease and in pregnancy and breastfeeding; liver function is measured before, within 3 months and at 12 months. UK
Class interactions
| With | Effect | Source |
|---|---|---|
| Strong CYP3A4 inhibitors (clarithromycin, itraconazole, ciclosporin, some HIV protease inhibitors) and grapefruit juice | Raise levels of atorvastatin and simvastatin (not rosuvastatin or pravastatin) and the risk of myopathy; doses are limited or the statin paused. | UK |
| Fusidic acid | Fatal rhabdomyolysis has occurred; the statin is paused during and for 7 days after systemic fusidic acid. | UK |
| Fibrates (particularly gemfibrozil) | Additive myopathy risk; gemfibrozil is avoided with statins. | UK |
| Warfarin | INR may rise when a statin is started or the dose changed; extra INR checks. | UK |
Open the Drug Interaction Checker