Lipitor – good for your cholesterol and your heart

September 29, 2008

Hello my friends,

Here’s the plan. I have a list of the top 200 drugs prescribed in America. Every week, I’ll write a little article on one drug. As a general rule, I will not favor one drug over another. I shall present scientific facts and logic, and if an opinion is expressed in the write-up, it’s strictly my opinion. Please do not try anything without first consulting your doctor.

This week, it’s cholesterol drug Lipitor. Lipitor has the generic name atorvastatin. It is used to maintain cholesterol levels in the body. Usually, your doctor would recommend diet control and exercise to control cholesterol. If that doesn’t work, and/or you have other risk factors for heart disease, lipitor or other statin drugs (like Zocor – available as generic simvastatin, Crestor, Pravachol – available as generic pravastatin, Mevacor – available as generic lovastatin, and Lescol) would be prescribed.

Is cholesterol bad? Certainly not. Our body and its organs are made up of cells. The cells have a cell membrane. Cholesterol is an essential component of the cell membrane. It’s necessary for the fluidity of the membrane, and plays a role in the permeability of the membrane. It is also the precursor of many hormones that we need – steroid hormones like testosterone, progesterone, estrogen …. yes, the sex hormones, as well as cortisol and aldosterone. Vitamin D is also formed from cholesterol. It’s involved in bile formation in the body too. Bile is necessary for digestion of fat in our diet.

So …… what’s the problem? Cholesterol is transported in the body by the blood. Cholesterol, which is a fat, is insoluble in blood which is aqueous (water-based). In order to transport cholesterol, here’s what the body does. It packages cholesterol molecules along with other fats called triglycerides, in a “suitcase” formed by water-soluble molecules called “lipo-proteins” (that’s a combination of lipids/fats and proteins). There are different sizes of lipoproteins. In decreasing size, the lipoproteins are called chylomicrons, very low density lipoprotein (VLDL), low density lipoproteins (LDL), and high density lipoprotein (HDL). All of the above except HDL transport cholesterol to peripheral tissues of the body. HDL transports cholesterol to the liver, to be excreted.

The more the numbers of LDL particles in the blood, the greater the incidence of atherosclerosis – hardening of arteries. This can eventually lead to a heart attack or an aneurysm which can burst and lead to death. On the other hand, larger HDL particles and larger numbers of them in the blood correlates to less incidence of arterial hardening. That’s why LDL is called bad cholesterol and HDL is called good cholesterol.

How do Lipitor and other statins work? Cholesterol is synthesized in the body by the liver. Statins competitively inhibit an enzyme called HMG-CoA reductase which catalyzes the rate-limiting step of cholesterol bio-synthesis. As a result, less cholesterol is synthesized in the body. This further results in genetic expression of LDL receptors on hepatocytes (these are a kind of liver cells). These LDL receptors take up LDL from the blood – as a result, LDL levels decrease. Along with this, there is also a reduction in triglycerides and a slight rise in HDL.

Does Lipitor have any side-effects? Yes. In a very small sub-section of the population – somewhere around 1 in 10,000 people – there is an alteration of the function of a gene that regulates drug uptake by the liver. This creates muscle pain. Out of these, in very rare cases, there can be muscle breakdown and fatal kidney failure. At some point in the future, there could possibly be a genetic test that tests a patient for the said genetic trait before administering a statin. Until then, when you start taking a statin for the first time, be watchful of any muscle pain or other side-effects, and inform your doctor or pharmacist immediately.

Other possible side-effects: headache, diarrhea, gas, constipation, nausea, drowsiness, flushing of the skin, and sleeplessness. However mostly, statins are well-tolerated. Please make sure you don’t ingest grapefruit or grapefruit juice. This fruit has an ingredient that inhibits Lipitor from being broken down by the liver, so it stays in the body for a longer time – that can increase its effects and side-effects. Imbibing alcohol while on statin therapy can cause additional stress on the liver leading to liver toxicity. My suggestion – drink no alcohol when on statin therapy. You do not want to destroy your liver.

My psychiatrist friend Dr. Adam Kaul pointed out an uncommon side-effect – statins can sometimes cause pseudo-dementia or a worsening of underlying dementia. The following is a possible reason for this: Cholesterol is widely distributed in the brain, as it is in the rest of the body, since it is part of the membrane of every cell in the body. When a statin decreases cholesterol, it might affect the function of certain brain cells that play a role in memory.

Okay, we talked about cholesterol being synthesized in the body. Another way of introducing cholesterol in the body is through food. Animal foods contain cholesterol, plant foods don’t. Minimizing animal fat is a good way of controlling cholesterol levels.

Looking at the bigger picture of heart health, a few more suggestions would be: decrease abdominal fat by aerobic and anaerobic exercise, control blood glucose levels by diet and if necessary medication, take regular multivitamins and ……… laugh a lot – I’m not joking, there are scientific studies showing increased health with good humor and laughter. Ah, the biochemistry of human emotions!

Thank you for reading. I hope it made sense. Until next time …. wish you good health!

Dr. Ajit Damodaran

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