Drugs in this class end with the “statin” suffix and generally have a similar mechanism of action and effect.
Statins inhibit the enzyme HMG-CoA reductase, which normally catalyzes the rate-limiting step in cholesterol biosynthesis. HMG-CoA reductase inhibitors are effective at decreasing low-density lipoprotein (LDL) and total cholesterol levels. Further, this class may increase the “good cholesterol”, referred to as high-density lipoprotein (HDL) and decrease triglycerides. This mechanism has been found to decrease the risk of heart disease and sudden death.
HMG-CoA reductase inhibitors are indicated for the treatment of high cholesterol levels (hypercholesterolemia). This class of medications decreases the “bad cholesterol” (low density lipoprotein, LDL), while simultaneously increasing the “good cholesterol” (high density lipoprotein, HDL), although the effects on HDL are a little more variable.
Hepatotoxicity may occur in patients receiving statin medications. The liver is responsible for the production of cholesterol; therefore, these medications may cause injury to hepatocytes. If signs or symptoms of liver injury such as jaundice develop, liver function tests should be performed.
One of the side effects of statins is the development of a rash.
Rhabdomyolysis, or the breakdown of muscle cells, can occur with statin use. Statins can damage myocytes and lead to myopathy. If this persists, rhabdomyolysis can occur as damaged cells release myoglobin into the bloodstream. This myoglobin is filtered into the kidneys and broken down into heme pigment. Heme pigment is toxic to the kidneys and results in acute kidney injury (AKI). A mainstay of treatment is judicious IV hydration.
Myopathy, or injury to muscle tissue, may occur with use of high-dose statins. Patients receiving statin therapy should be monitored for diffuse or local muscle aches, weakness, and tenderness. Creatinine kinase (CK) levels in the serum can be checked to assess for muscle cell damage in myositis or the more severe problem of rhabdomyolysis.
Because statins may cause liver damage, liver enzymes should be checked before starting this medication, and repeated if clinical concern for liver damage arises.
The liver produces the majority of cholesterol at night time. For this reason it is recommended that statins are administered at bedtime.
Grapefruits and their juice should be avoided in patients taking statins because grapefruits contain chemicals that inhibit the enzyme CYP3A4, causing levels of the statin to rise.
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