HMG-CoA Reductase Inhibitors (Statins)
Lescol (Brand Name)
Fluvastatin (Generic Name)
Livalo (Brand Name)
Pitavastatin (Generic Name)
Zocor (Brand Name)
Simvastatin (Generic Name)
Indications
Hypercholesterolemia (high cholesterol)
Lipitor (Brand Name)
Atorvastatin (Generic Name)
Mechanisms of Action
Cholesterol comes from 2 sources: dietary intake (by eating certain foods) and natural production of cholesterol inside the body. Statins work by inhibiting the enzyme HMG-CoA reductase, which is a key enzyme involved in the normal production of cholesterol. Most cholesterol produced in the human body is produced during the night, so statins are generally more effective at night. Certain statins (e.g. atorvastatin and rosuvastatin) are eliminated from the body at a very slow rate, as these drugs have a long half-life. For this reason, it isn't necessary to take atorvastatin or rosuvastatin at night; they can be taken at any time of the day. Since HMG-CoA reductase inhibitors only affect cholesterol production and not dietary intake of cholesterol, patients on a statin should also implement dietary changes to reduce the amount of cholesterol they consume from the foods they eat.
Mevacor (Brand Name)
Lovastatin (Generic Name)
Drug Interactions
Most drug interactions involving satins increase the risk of myopathy. For drugs in this class, the enzymes responsible for metabolism vary from one statin to the next, but, in general drugs that inhibit or induce certain CYP450 enzymes (e.g. ketoconazole, cyclosporine, carbamazepine, high quantities of grapefruit juice) lead to decreased or increased metabolism of statins. Enzyme inhibitors decrease the metabolism of stain, which accumulates in the body. Enzyme inducers increase the metabolism of the statin and ultimately decrease the statin's effectiveness.
Side Effects
Muscle Aches, constipation, liver impairment, myopathy, rhabdomyolysis (rare)
Pravachol (Brand Name)
Pravastatin (Generic Name)
Other Notes
Pregnancy Category X
Crestor (Brand Name)
Rosuvastatin (Generic Name)
