ProLipid

Each type of "hyperlipidemia" suchf as high cholesterol or high triglycerides must be treated with a different class or combination of drugs.

There is a difference between the "active ingredient" and the trade-name of a drug. The active ingredient is the chemical compound that actually causes the desired pharmacological effect, where as the trade name refers to the finished product, e.g. a pill with active ingredient and all the additives ("excipients") such as binding agents, colors or flavors. The trade names (such as Lipitor® or Zocor®) are familiar to us, whereas the active ingredients (in these cases, they are statins) may not.

In this article, I will talk about lipid disorders and active ingredients, before looking at actual drugs (Lipitor®, Niaspan®, Lopid®, Zetia® and the like) in the next article.

The following table contains an overview of cholesterol and triglyceride drugs, together with a rating of their effectiveness, tolerability and safety:

Prominent drugs containing statins include Lipitor® and Zocor®, the world's best selling and fifth best selling drugs in 2005, respectively.

Statins lower blood cholesterol levels by blocking a process in the liver responsible for producing cholesterol. This is done by inactivating an enzyme called HMG-CoA reductase, which is why statins are also known as HMG-CoA-reductase inhibitors.

Three aspects of statin drugs can be compared: efficacy (by how much is my LDL cholesterol reduced?), safety (what are the side effects and how frequently do they occur?) and price.

Fibrates (= Fibric Acids) are an older drug class than statins and have been used since 1967. Their main function is to lower serum triglycerides by approximately 40 to 60%. LDL cholesterol may be lowered slightly by up to 10%, and HDL cholesterol or the "good" cholesterol may rise by approximately 10 to 20%.

Ezetimibe: Inhibiting The Uptake Of Cholesterol In The Gut

Another method to reduce blood cholesterol levels is to inhibit its uptake in the gut. This is how ezetimibe, the active agent in the drug Zetia® marketed by Merck and Schering-Plough works.

Bile Acid Sequestrants ("Resins"): Removing Bile Acids To Deplete Cholesterol Supply

As the name suggests, bile acid sequestrants or "resins" bind bile acids. Instead of being recycled by re-uptake in the lower area of the gut, bile acids bound to sequestrants are excreted in stools. As a result, the supply of cholesterol (the raw material for bile acid) is depleted as new bile acid must be manufactured in the liver.