Statins
Other names: HMG-CoA reductase inhibitors
What are Statins?
What are the differences between statins?
Statins differ in how effective they are at lowering total cholesterol, triglycerides, LDL-cholesterol, or increasing HDL-cholesterol; how likely they are to interact with other medications; and how safe they are for people with kidney disease.
Atorvastatin and simvastatin are the most effective at reducing LDL cholesterol levels. Atorvastatin and fluvastatin are preferred in people with kidney disease. Pravastatin and fluvastatin have a lower risk of drug interactions because they are not metabolized by cytochrome p450 3A4. Atorvastatin and fluvastatin are considered the most cost-effective statins.
Grapefruit juice increases levels of atorvastatin, lovastatin, and simvastatin, which may increase the risk of side effects. Grapefruit juice should be avoided with these statins.
Pitavastatin has a similar effectiveness to atorvastatin but reportedly produces greater increases in HDL-cholesterol that are sustained over the long-term. It is effective at low dosages and has minimal drug interactions.
| Generic name | Brand name examples |
|---|---|
| atorvastatin | Lipitor |
| fluvastatin | Lescol XL |
| lovastatin | Altoprev |
| pitavastatin | Livalo, Zypitamag |
| pravastatin | Generic |
| rosuvastatin | Crestor |
| simvastatin | Zocor |
What are the side effects of statins?
The most common side effects reported with statins include:
- a headache
- belching or excessive gas
- constipation
- heartburn, indigestion, nausea or stomach discomfort
- hoarseness
- lower back or side pain
- muscle pain, tenderness, or weakness
- pain or tenderness around the eyes and cheekbones
- painful or difficult urination
- a stuffy or a runny nose
- sweating
- trouble sleeping.
Are statins safe?
Statins are generally safe when used at recommended dosages.
Serious muscle effects have been reported with statins, including rhabdomyolysis – this is the destruction of muscle cells. People aged older than 65, taking certain medications (for example cyclosporine, itraconazole, or HIV antivirals), who drink more than two alcoholic drinks per day, or with kidney disease, appear to be more at risk of serious side effects. Initial reports of muscle pain should be investigated by a doctor. Mild muscle pain is a common side effect of statins.
Rarely, statins may affect affect the liver or cause jaundice (a yellowing of the skin). This may require a reduction in dosage or discontinuation.
Statins may also affect some diabetes markers (such as HbA1c or fasting glucose), and may not be suitable in those with liver or kidney disease.
Some statins may not be suitable for some people including those with a recent history of stroke or transient ischemic attack (TIA). People with active liver disease or who are pregnant or breastfeeding should not take statins.
Rarely, statin use has been associated with memory loss, forgetfulness, amnesia, memory impairment, and confusion. These symptoms typically resolve with discontinuation.
Some statins, particularly those metabolized by CYP 3A4 (such as atorvastatin, lovastatin and simvastatin), can interact with several other drugs, such as clarithromycin, protease inhibitors, cyclosporine, gemfibrozil, oral contraceptives, and digoxin.
Statins help lower total cholesterol and reduce the risk of a heart attack or stroke. Statins include atorvastatin (Lipitor), fluvastatin (Lescol XL), lovastatin (Altoprev), pitavastatin (Livalo), pravastatin, rosuvastatin (Crestor) and simvastatin (Zocor).
Statins are a class of medicines used to lower cholesterol. While some of the cholesterol in your blood comes from food, most is made by the liver. Statins work by reducing the amount of cholesterol made by the liver and helping the liver remove cholesterol that is already in the blood.
Statins inhibit endogenous cholesterol production by competitive inhibition of HMG-CoA reductase (HMGCR), the enzyme that catalyzes conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol synthesis.
While statins are generally safe, well-tolerated, and effective for most people, they can rarely cause side effects such as muscle pain, liver inflammation, and an increased risk of diabetes.
Metformin is a widely used drug in the treatment of diabetes, possessing beneficial effects on the glucose and lipid metabolism. However, statins are a class of drugs that decrease plasma cholesterol levels and are prescribed as first choice to patients suffering from cardiovascular diseases.
Statins act by inhibiting 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and thereby reducing cholesterol synthesis. In X-ray crystallographic studies, we have determined the structures of the catalytic portions of the enzyme in complex with statin molecules.
List of Statins
