New Cholesterol Lowering Drugs

Day after day, the need for discovering new cholesterol lowering drugs increases. High blood cholesterol level or hypercholesterolemia increases the risk for developing cardiovascular diseases, which are considered to be one of the most leading causes of death in the United States.

Therefore, 1ry and 2ry preventive measures utilizing 3-hydroxy-3-methylglutaryl coenzyme-A reductase inhibitor (known as statins) have clinically proved lowering the LDL “Bad” cholesterol levels in the blood; consequently, this has a significant influence in reducing death rates due to CVD.

Unfortunately, only forty percent of patients treated with statins will achieve their LDL targets.

Furthermore, this percentage will markedly decrease (reaching eighteen percent or less) in patients who already suffer from CVD.

This wide gap in achieving LDL targets with old cholesterol lowering drugs, like statin, is mainly due to inadequate starting doses and inability of many patients to tolerate high doses or combination therapy plans of these drugs.

Clinically, the side effects of most cholesterol-lowering regimes are directly proportional with dose taken; the higher the dose, the more the adverse effects.

Because of the limits of the present cholesterol-lowering medications, new cholesterol lowering drugs with similar mechanisms corresponding to statins, but with improved side effects can definitely help a lot of patients to achieve their LDL targets.

Selective cholesterol absorption inhibitors are a new cholesterol lowering drugs which can possess these criteria.

Ezetimibe is the first drug of this class approved by FDA (Food and Drug Administration) for the treatment of hypercholesterolemia in USA; it can be used as mono-therapy or in combination therapy.

Brand names

Zetia®

Brand names of combination products

Vytorin® (ezetimibe/simvastatin)

Ezetimibe mode of action is performed by the inhibition of the absorption of dietary cholesterol from the small intestine, while the absorption of fat soluble vitamins, bile acids, or triglycerides is not affected.

The efficiency and safety of the dose of 10 mg/daily ezetimibe have been clinically proved. In fact, ezetimibe was tested as monotherapy, or combination therapy with statins or fenofibrates, and it was used for treating patients with primary hypercholesterolemia, familial hypercholesterolemia and sitosterolemia.

Ezetimibe is found to lower LDL “Bad” cholesterol by 15-20%, elevate HDL “Good” cholesterol levels by 2.5-5%, while it has no effect on triglycerides. As ezetimibe is minimally absorbed by the body, it shows minimal side effects as well as deceased drug interaction.

These new cholesterol lowering drugs are ideal for reaching LDL targets in patients who can’t tolerate high doses of statins or for those who requireadditional reduction in their LDL levels despite taking maximum dosage of statins.

Ezetimibe can cause some side effects, including; headache, dizziness, diarrhea, sore throat, running nose, sneezing, painful joints, rashes, itching, swallowing and breathing difficulties, swelling of face and extremities, buffing of the eyes, extreme weakness, gastric upset, loss of appetite, bleeding and bruising.

Livalo is one of new cholesterol lowering drugs approved by U.S. Food and Drug Administration in august, 2009.

It has approved 4 milligram of Livalo (pitavastatin) maximally for the treatment of patients with high blood cholesterol levels.

Livalo belongs to statin group, thus it mainly reduces the liver's capability of making cholesterol by inhibiting HMG Co-A reductase enzyme.

Livalo efficacy and safety are clinically proved to be better than the 3 statin drugs found currently in the market. Livalo main side effects include pain in back, muscles, and joints, besides constipation.