Statins Side Effects

What are statins?

statins side effectsStatins are lipid-lowering drugs. They are used to diminish and control especially the cholesterol levels, by inhibiting the production of this organic chemical substance in the liver. And since the high level of cholesterol is associated with heart disease, one of the secondary aims of statins is to prevent or reduce the risk of cardiovascular disease and heart attacks.

Although statins lower the LDL cholesterol (the “bad” cholesterol) level which reduces the number of negative cardiac events (heart attack, or sudden cardiac death), and also diminishes the risk of cerebrovascular accidents, these drugs also reduce the levels of triglycerides. A high blood level of triglycerides may also result in heart disease and stroke, and also may lead to atherosclerosis. Statins also increase the levels of HDL (the “good” cholesterol), which reduces the risk of heart attack. However, statins are less effective for the triglyceride reduction and the raising of the HDL levels, than niacin or fibrates.

There are two principal categories of statins: synthetic and fermentation-derived. The synthetic ones are: rosuvastatin, pitavastatin, fluvastatin, cerivastatin and atorvastatin. Cerivastatin was withdrawn from the market in 2001 because this drug presented increased risk of rhabdomyolysis.

The fermentation-derived statins are: lovastatin, mevastatin, pravastatin and simvastatin. Lovastatin and mevastatin are naturally found in red yeast rice.

Which are the side effects of statins?

Medication with statins usually features two side effects: muscle problems and a raised level of liver enzymes.

In terms of muscle problems, statins side effects can take quite a few forms. The most common ones are mylagia and muscle cramps. However, myositis and myopathy may occur as a one of the statins side effects.

Myositis is the inflammation of the muscles. In general, as a side effect from the treatment with statins, myositis is usually characterized by the swelling of the legs. Myopathy however, is a muscular disease, characterized by the disfunction of the muscle fibers. The main symptom of myopathy is general muscular weakness, often accompanied by muscle spasms, stiffness and cramps.

A serious condition that may occur due to the medication with statins, is rhabdomyolysis. This condition is given by the break down of the skeletal muscle cells and their passing into the bloodstream. The myoglobin protein, one of the breakdown products of damaged muscle cells, is extremely destructive to the kidneys and may lead the patient to acute renal failure.

Another side effect that may occur while under medication with statins is an increased level of liver enzymes. Now, this part may not show any symptoms, but in general, an elevated liver enzymes level points out the fact that the liver is fighting something.

There are other statins side effects that can occur, along or apart the one mentioned above. These could be: insomnia, skin rashes, drowsiness, general weakness, nausea, vomiting, abdominal pain, constipation, diarrhea, bloating.

Of course, just as for any drug, a patient can be allergic to statins. And an allergic reaction can cause angioedema (characterized through a burning sensation of the skin, not itchiness) and even anaphylaxis. If you have any history with allergic reactions to statins, you shouldn’t take these drugs. Or at least the medication should be under direct and specialized supervision.

Statins Interactions

The first aspect on the list of statins interactions and contraindications is pregnancy. Since statins are lipids and cholesterol reduction drugs, and fats and cholesterol are necessary for the formation and growth of the fetus, these drugs should not be administered during pregnancy. Also, breast-feeding mothers should not be taking statins.

The most important of the statins interactions regards the enzymes related to the elimination of statins by the liver. Some of the liver enzymes play a crucial role in the expulsion of statins from the human body. One of the main groups of enzymes in the liver that are responsible for this, are the cytochrome P-450 (CYP) enzymes. Now, there are various other drugs that block or diminish the action of these enzymes. And if that happens, it might lead to an increase level of statins (fluvastatin, lovastatin, simvastatin, atorvastatin, but not parvastatin and rosuvastatin) in your blood, which also may lead to muscle problems or even rhabdomyolysis. So, to avoid some of the most dangerous statins side effects, don’t associate statins with these drugs.

Here’s the list of the drugs that block the CYP enzymes, and therefore should not be administered along with statins: itraconazole, cyclosporine, telaprevir, voriconazole, boceprevir, telithromycin, erythromycin, clarithromycin, diltiazem. Some of the protease inhibitors used for treating AIDS have the same effect, and these are: indinavir and ritonavir.

Drugs that control and lower the blood triglyceride levels, like fibric acids (ex: clofibrate, gemfibrozil, fenofibrate), as well as niacin, should also not be taken along with statins. These drugs can cause rhabdomyolysis and combined with the statins, there’s an increased chance for this side effect to occur.

There are drugs that bind statins in the instestines and prevent their complete or partial absorbtion into the body. These are colestipol and cholestyramine. This won’t cause any dangerous statins side effects, but it prevents the statins to take effect. Therefore, if associated with these two drugs, statins should be taken four hours after colestipol or cholestyramine, or one hour before.

Last but not least, another agent that can interferes with statins and may cause statins side effects, is grapefruit juice. Grapefruit juice contains bergamottin and furanocoumarins which inhibit the break down of various drugs on intestinal level. If you consume grapefruit juice along with statins like simvastatin, lovastatin or atorvastatin, this may result in the passing of too much of the drugs’ active agents into the blood. This leads to liver or muscle damage. Take note that blood-orange juice may have the same effect as the grapefruit juice in conjunction with statins.

Final Word

Statins are recommended only after the patient has tried various other cholesterol and lipid-reduction methods, like a balanced diet and exercise. Only if these failed to reduce the cholesterol in your body, should you start medication with statins, and of course, only based on a physician’s recommendation. Also, statins should be associated with exercise and a balanced diet.