How Do 2-Azetidiones Work?

Lipid-lowering agents also known as cholesterol-lowering, hypolipidemic, or antihyperlipidemic agents are a group of drugs used to reduce high levels of lipids (fats) and lipoproteins (fats with protein) in the blood. These drugs are used to treat cardiovascular abnormalities such as atherosclerosis (build-up of fats and other substances in the wall of arteries, causing obstruction of blood flow) and decrease the risk of potential heart attacks. Lipid-lowering agents include:

• 2-Azetidiones
• Adenosine triphosphate-citrate lyase (ACL) inhibitors
• Apolipoprotein B antisense oligonucleotides
• Microsomal triglyceride transfer protein inhibitors
• Statins (β-hydroxy β-methylglutaryl-CoA [HMG-CoA] reductase inhibitors)
• Fibrates
• Bile acid sequestrants
• Omega 3 acids
• Vitamin B3

2-azetidiones are a new class of drugs that work by blocking specific receptors present on the intestine which absorb the dietary cholesterol and thus inhibit intestinal absorption of cholesterol and phytosterols. As cholesterol levels decrease because of malabsorption of cholesterol, the liver cells increase the uptake of low-density lipoprotein (LDL, bad cholesterol) present in the blood to make cholesterol, and this reduces the levels of LDL cholesterol.

These drugs may be taken alone or in a combination with other lipid-lowering agents. A healthy diet and exercise are recommended while taking these drugs to maintain good levels of cholesterol.

2-azetidiones are taken orally and used to treat conditions such as:

• Familial hypercholesterolemia (a life-threatening genetic condition that increases LDL cholesterol levels in the body)
• Hypercholesterolemia (high levels of cholesterol in the blood)
• Hyperlipidemia (high levels of fats such as cholesterol and triglycerides in the blood)

Common side effects of 2-azetidiones include:

• Nausea and vomiting
• Joint pain
• Diarrhea
• Sore throat
• Stuffy nose
• Sinus pain
• Depression

Serious side effects of 2-azetidiones may include:

• Hypersensitivity reaction
• Chest pain
• Liver function abnormalities
  • Increase in liver enzymes
  • Yellow discoloration of skin and eyes
  • Abdominal pain
• Rhabdomyolysis (muscle tissue is damaged and releases myoglobin [a protein] into the blood that damages kidneys)
  • Muscle tenderness, weakness, or pain
  • Pain in leg, arm, or shoulders
  • Oliguria (low amount of urine is produced)
  • Dark-colored urine
• Tiredness
• Fever
• Dizziness
• Depression
• Confusion

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.

Generic and brand names of 2-azetidiones drugs include:

• Bempedoic acid/ezetimibe (Nexlizet)
• Ezetimibe (Zetia)
• Rosuvastatin/ezetimibe (Roszet)