New blood cholesterol lowering medicine: Ezetimib

Recently, the US Food and Drug Administration (FDA) has approved a new lipid-lowering drug, Ezetimib (nicknamed Zetia). Ezetimib is effective in lowering total cholesterol and LDL - cholesterol in the blood follows the mechanism of inhibiting the absorption of cholesterol from food through the intestinal mucosa to the bloodstream.

New antidote

The brand name is Zetia
(Photo: schering-plough)

There are many groups of drugs that have been used to treat dyslipidemia (mainly lowering lipids, especially LDL - cholesterol or 'bad' cholesterol in the blood). As drugs are bile acid renin (cholestyramine, colertipol), fibrates (clofibrat, fenofibrat, gemfiprozil, niacin (ie vitamin PP), statins (simvastatin, atorvastatin, pravastatin .).

Ezetimib in terms of chemical structure is a 2-agetidinone derivative. In the intestine, ezetimib is converted into a form of glucuronide that prevents cholesterol absorption through the intestinal mucosa. Tested on animal models, ezetimib can inhibit intestinal cholesterol absorption by 96%. Unlike drugs that are bile acid resin, ezetimib does not hinder the absorption of fat-soluble substances such as vitamins A, D or triglycerides.

Ezetimib does not give local effects but after oral administration, it is absorbed into the bloodstream (if taken with meals, it will increase the absorption to 30%), metabolize in the liver to convert new glucuronid to work. The half-life of ezetimib is 13 hours in young people and 21 hours in the elderly. Ezetimib and its glucuronide form combined with plasma proteins up to 90%, are excreted in the feces and urine.

The US FDA approves the indication of ezetimib to be used alone or in combination with treatment statins for people who need LDL lowering - cholesterol and total cholesterol. The US FDA also approved the use of ezetimib in hereditary disease as a 'family hypercholesterolemia '.

Prevention of side effects

When used alone, ezetimib can cause some side effects such as back pain, joint pain. When combined with statins, the combination causes side effects of back pain, epigastric pain, can increase liver enzymes AST and ALT.

Ezetimib is provided as a 10mg tablet. Dosage of 10mg once a day, can be taken on an empty stomach or full. During medication, patients are advised to eat meals that contain low cholesterol. When combined with the drug, ezetimib can be taken with statins at the same time, but ezetimib must be taken 2 hours before or 4 hours after administration of resin. For the elderly, people with liver and kidney disease, do not need to reduce the dose. Taking medication after 2 weeks can lower LDL - cholesterol to the maximum.

Dr. DS. NGUYEN HUU DUC (Ho Chi Minh City University of Medicine and Pharmacy)