How Do HMG-CoA Reductase Inhibitors Work?

β-Hydroxy β-methylglutaryl-CoA (HMG-CoA) reductase inhibitors, more popularly known as statins, work by reducing the cholesterol levels in the body. HMG-CoA inhibitors interfere with the ability of the body to build cholesterol from dietary fat. This class of cholesterol-lowering drugs is often prescribed for patients with high cholesterol and heart problems.

Cholesterol is synthesized in the liver by a set of enzymes from the fat in our diet. HMG-CoA reductase is one such enzyme that when active produces a lot of cholesterol in certain conditions, much beyond the natural needs of the body. Excess cholesterol has been shown to cause several health conditions including blockage of blood vessels and heart attack.

HMG-CoA reductase inhibitors block the enzyme HMG-CoA reductase that is responsible for synthesizing cholesterol in the liver. Statins competitively inhibit the HMG-CoA reductase enzyme. Statins bind to the active site of the enzyme and change its structure. As the structure of the enzyme is changed, it cannot bind with the receptor, thus its activity is reduced.

HMG-CoA reductase inhibitors reduce total cholesterol, low-density lipoprotein cholesterol, and triglycerides concentrations and increase high-density lipoprotein in the blood.

HMG-CoA reductase inhibitors are used adjunctively with diet and exercise to treat and manage:

• Hypercholesterolemia (high cholesterol in blood)
• Primary and secondary prevention of coronary heart disease

The most common side effects of HMG-CoA reductase inhibitors include:

• Muscle aches, tenderness, or weakness (myalgia)
• Drowsiness
• Dizziness
• Headache
• Nausea or vomiting
• Bloating or gas
• Diarrhea
• Constipation
• Abdominal cramping or pain
• Difficulty sleeping
• Flushing of the skin
• Low levels of blood platelets
• Rash

Less common side effects include:

• Liver inflammation, which can make you feel like you have the flu
• Hair loss
• Pins and needles sensations, such as pricking, numbness, or tingling on your skin
• Pancreas inflammation, which can cause stomach pain
• Sexual problems, such as erectile dysfunction or a low sex drive

Rare but potentially serious side effects of HMG-CoA reductase inhibitors include:

• Myositis (inflammation of the muscles)
• Elevated levels of creatine phosphokinase or creatine kinase, a muscle enzyme that when elevated can cause muscle pain, mild inflammation, and muscle weakness
• Rhabdomyolysis (extreme muscle inflammation and damage)

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

Drug names of HMG-CoA reductase inhibitors include:

• Altoprev
• Amlodipine/atorvastatin
• Atorvastatin
• Caduet
• Crestor
• Ezallor Sprinkle
• Fluvastatin
• Lescol
• Lescol XL
• Lipitor
• Livalo
• Lovastatin
• Mevacor
• Pitavastatin
• Pravachol
• Pravastatin
• Rosuvastatin
• Simcor
• Simvastatin
• Simvastatin/ezetimibe
• Simvastatin/niacin
• Vytorin
• Zocor
• Zypitamag