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Cholesterol Medication

* Cholesterol medication options

Cholesterol medication is generally recommended for patients who do not respond to diet changes, regular physical activity or weight loss campaigns, and who need further treatment for high blood cholesterol levels. In males less than 35 years of age and premenopausal women with LDL cholesterol levels of 190 to 219 mg/dL, cholesterol medication should not be undertaken except if the patient is high-risk such as having diabetes. In coronary heart disease patients with LDL cholesterol levels of 100 to 129 mg/dL, a doctor will consider cholesterol medication with discretion.

* A cholesterol lowering drug for cholesterol medication

Sometimes a doctor will prescribe a cholesterol lowering drugs at lower levels. However cholesterol medication therapy may not be appropriate for some patients, especially elderly patients, who meet the above criteria. The presence of other coronary heart disease risk factors, such as age, family history, high blood pressure, diabetes, or whether the patient is a smoker, will influence the use of a cholesterol lowering drug. For men, 45 years or older, women 55 years or older and people with high blood pressure (140/90 mm Hg or higher) cholesterol medication is generally prescribed.

* Common high cholesterol medication

The Cholesterol medication of first choice for high LDL cholesterol is the HMG CoA reductase inhibitors, or statins, such as atorvastatin, fluvastatin, lovastatin, pravastatin, rosuvastatin and simvastatin. Statin drugs, very effective for lowering LDL cholesterol levels, may have few short-term side effects, but with prolonged use this may change. Common side effects are constipation and abdominal pain and cramps, although they mostly subside as therapy continues. High cholesterol medication is easy to administer and mostly has high patient acceptance. Pregnant women or those with chronic liver disease, or with allergies to statins, shouldn't use this type of high cholesterol medication.

* Other high cholesterol medication options

Bile acid sequestrants such as colesevelam, cholestyramine and colestipol, and nicotinic acid (niacin) have been shown to reduce the risk for coronary heart disease. Both classes of high cholesterol medication appear to be free of serious side effects although patients have reported stomach cramps. Note that the dietary supplement niacin is not a high cholesterol medication and only FDA approved prescription niacin should be used for cholesterol lowering. If a patient doesn't respond adequately to single high cholesterol medication, combined drug therapy may be considered to further lower LDL cholesterol levels.

New discoveries offer promise for cholesterol drugs

New discoveries offer promise for developing drugs that improve on the therapeutic profile of niacin, the inexpensive, time-tested B-vitamin that boosts levels of HDL cholesterol, the good cholesterol with the potential to protect people against heart attacks and stroke, scientists report.

Graeme Semple, Ph.D., Vice President of Discovery Chemistry at Arena Pharmaceuticals, San Diego, Calif., described new insights into developing drugs that raise HDL via the same mechanism as niacin in a report presentated at the 233rd national meeting of the American Chemical Society.

In small doses, niacin is the familiar B-complex vitamin, which helps the body metabolize or breakdown carbohydrates, fats and protein into compounds that the body needs to maintain good health. In the high doses prescribed by a physician, niacin can increase HDL by as much as 35 percent and reduce levels of artery-clogging triglycerides by 50 percent.

Doctors have known since the 1970s that niacin can reduce the risk of heart attacks and strokes, but it has not been prescribed as widely as newer and more costly medications known as statins.

The use of niacin is limited by its side-effects, including a highly uncomfortable skin flushing, which contributes significantly to poor patient compliance," Semple explained. "Since currently marketed cholesterol drugs have a more modest HDL-raising activity than niacin, better tolerated HDL-targeted therapies with improved efficacy could provide additional clinical benefits to patients and potentially reduce the risk of heart attack and stroke."

Semple described research toward that goal, including Arena's discovery of a niacin receptor termed GPR109a. It is among a family of so-called G protein-coupled receptors (GPCRs) that have long been considered among scientists as good targets for the development of new drugs.

Molecules termed ligands from the environment outside cells bind with these receptors, which are located on the cell surface. Ligands activate the GPCRs, signaling biochemical machinery inside the cell to either inhibit or accelerate cellular processes.

Niacin activates GPCRs on fat cells, signaling the cells to stop producing fatty acids in a way believed to raise HDL levels. It also can activate GPR109b, a closely related receptor on immune system cells. Semple believes that activation of one or both of those receptors may be responsible for niacin's beneficial effects, and the undesirable side effects.

Semple said data from the joint Arena-Merck research program reinforces the hypothesis that it may be possible to identify a compound that activates the niacin receptor without causing flushing, thereby separating the beneficial effects on fatty acids from the flushing side effect.

"This work has not been reported previously and has been carried out within the last three years," Semple noted. "In addition, no other pharmaceutical companies have reported on new compounds for these targets in the open literature, although some patents have appeared."


Information on Cholesterol