What are STATINS?
Cholesterol Synthesis in the Body
Have you been told you need to begin taking a "statin?" Have you heard the term "statin" thrown around and want to know what everyone is talking about? In this article I will briefly explain to you exactly what a "statin" is. I will tell you a little about the various types of statins and how we classify them. Finally, I will provide some answers to frequently asked questions about statins. These are things which I, as a pharmacist, think you ought to know.
What are statins? Statins are a family of prescription drugs (they all require a prescription in the U.S.) which are designed to reduce the amount of cholesterol your body creates. Yes, we make cholesterol. We actually need it to survive. But high levels of cholesterol, particlarly LDL (low density lipoprotein) cholesterol, are associated with a greater risk for heart disease. So statins interfere with the enzyme needed to produce cholesterol. They also, in varying degrees, help promote the breaking down of LDL choleseterol within the body.
Why are they called "statins?" Well, quite simply, because this family of drugs all end with the word "statin." For example: lovastatin, simvastatin and pravastatin are all "statins." Make sense? However, not every drug that ends in "statin" is a "statin." Nystatin, for example, is an antifungal drug...not a "statin." Confused yet? Don't be.
Also Known As: If you really want to impress your friends, rather than say you are on a "statin" you can give them the more scientific name for this family of drugs: HMG-CoA reductase inhibitors. Pronounce each of the first 3 letters "H" "M" "G" then the word "Co" (rhymes with "go") then the letter "A" then the words reductase (re-DUCT-ase) inhibitors. Practice this on your own before attempting it in public. Guarenteed to impress!!
HOW DO STATINS WORK?
Do you want a little more detail into how these statins actually do their job? Let me try to explain it. Think of an assembly line involved in the manufacturing of a product. Every person on that assembly line is necessary for that product to be made. If even just 1 person (lets call him 'Bob') in the line gets distracted from his job...the product cannot be produced. Well, cholesterol is the product of a series processes within the human body. It takes a whole assembly line of chemicals and enzymes and substrates to produce cholesterol. "Bob" is on that assembly line. Statins basically distract "Bob" from his duties on the assembly line of cholesterol creation. "Bob" in this case happens to be an ezyme by the name of HMG-CoA reductase (but 'Bob' is so much easier to say!). This enzyme is responsible for converting HMG-CoA into mevalonate...an important building block of cholesterol.
This helps explain why, for many people, diet alone cannot sufficiently reduce your cholesterol levels. Your body just makes more to compensate! You might skip the Twinkie, eat more fiber, and reduce your fat intake severely....but your body just cranks up it's own little cholesterol machine and makes as much as it wants.
A LITTLE STATIN HISTORY
Statins are NATURAL! Does that surprise you? You see, back when it was first discovered that the enzyme HMG-CoA reductase played an important role in the biological 'assembly line' of cholesterol production, scientists began the research for something that would inhibit this enzyme from doing it's job. This research eventually led, in 1979, to the discovery of lovastatin, which was isolated from a particular strain of the fungus (or mold) known as Aspergillus terreus. For what it's worth, this particular mold genus was cataloged by an Italian monk/scientist in 1729, who named it because it appeared (under a microscope) to look like an aspergillium, a religious instrument used to sprinkle holy water. I suppose it would be going too far to say that the statin class of drugs have a "holy" history...but we can certainly say they have a "natural" history. Today, however, statins are the product of a far more efficient synthetic process.
Okay, now that you know what statins are, we need to identify the statins that are currently on the market in the U.S. For the sake of organizing them, I will divide them into 3 generally useful categories. These categories are:
- Lower potency statins
- Higher potency statins, and
- Combinations (prescription drugs that combine a statin with another medication)
Below is a list of SOME of the currently available "statin" prescription drugs in the U.S. I have added a link to the drug names so that you can visit the manufacturer website if you like. All of the presently available strengths are also shown. Most statins are taken once daily.
LOWER POTENCY STATINS - Lower potency statins are neither better nor worse than higher potency statins, they simply require higher dosages to produce similar effects.
- Altoprev (lovastatin extended release): 10mg, 20mg, 40mg, 60mg tablets
- Lescol & Lescol XL (fluvastatin): 20mg (Lescol), 40mg (Lescol), 80mg (Lescol XL) capsules
- Mevacor (lovastatin): 10mg, 20mg, 40mg tablets
- Pravachol (pravastatin) 10mg, 20mg, 40mg, 80mg tablets
HIGHER POTENCY STATINS - Higher potency statins simply require smaller dosages to produce adequate reductions in cholesterol.
- Crestor (rosuvastatin): 5mg, 10mg, 20mg, 40mg tablets
- Lipitor (atorvastatin): 10mg, 20mg, 40mg, 80mg tablets
- Livalo (pitavastatin): 1mg, 2mg, 3mg - This drug is due to be released in 2010 from Kowa Pharmaceuticals
- Zocor (simvastatin): 5mg, 10mg, 20mg, 40mg, 80mg tablets
COMBINATION STATINS: These products combine the cholesterol reducing power of a "statin" along with another ingredient to either reduce triglycerides (like Niacin) or blood pressure (like amlodipine) or to reduce the absorption of cholesterol from foods (like ezetimibe).
- Advicor (lovastatin/niacin): 20/500mg, 20/750mg, 20/1000mg, 40/1000mg
- Caduet (atorvastatin/amlodipine): 2.5mg with 10, 20, or 40mg amlodipine/ 5mg with 10, 20, 40, or 80mg amlodipine/ 10mg with 10, 20, 40 or 80mg amlodipine
- Simcor (simvastatin/niacin): 20/500mg, 20/750mg, 20/1000mg
- Vytorin (simvastatin/ezetimibe): 10/10, 20/10, 40/10, 80/10mg tablets
FREQUENTLY ASKED QUESTIONS ABOUT STATINS
Now that we have reviewed the statins I would like to just answer several of the more commonly asked questions about this family of prescription medications.
1. What is the best way to take my statin?The cholesterol factory in your body does more work on the night-shift than the day-shift. The day shift enzymes are a bunch of slackers. Therefore, some statins should be taken in the evening (either with an evening meal or at bedtime). These include drugs like Mevacor, Zocor and Lescol. Other statins, however, stick around in your body so long that it really doesn't matter what time of day you take them (although taking them at the same time every day is advisable). Typically I like to tell everyone to take them with the evening meal or shortly thereafter.
2. Can I drink grapefruit juice with my statin? If you are taking Altoprev, Lipitor, Zocor (or generic), or Mevacor(or generic) you should NOT consume grapefruit or grapefruit juice at all while you are taking these statins. This also includes all the combination statins listed above. How come? It involves some complicated metabolism concepts, but let me simplify it. Some statins can only leave our body through "Door A" and some can only leave through "Door B." We do want them to leave, or eventually they build up to dangerous levels. Grapefruit blocks Door A! Statins that have to leave by Door A start to build up, get crowded, and then become rather rowdy and unruly. Not good. You must not drink or eat Grapefruit AT ALL if you are on one of these 3 statins or one of the combination statins listed above. If you MUST have grapefruit...talk to your MD about switching to a different statin.
3. Won't statins destroy my liver?A rare side effect of statins is a negative impact on your liver. This is serious, but quite uncommon. To protect you against this your doctor will probably take a blood test to evaluate your liver function before and during your statin therapy. If any concerns arise, they will discontinue the medication and your liver function will return to normal. As an added precaution, be sure to tell your doctor if notice any of the following:
muscle problems such as weakness, tenderness, or pain that happen without a good reason, especially if you also have a fever or feel more tired than usual you experience nausea and vomiting you pass brown or dark-colored urine you feel more tired than usual your skin and whites of your eyes get yellow you experience stomach pain
4. Aren't statin drugs very expensive?Mevacor, Pravachol and Zocor are all available generically and should be available at a very reasonable price, even if you do not have insurance. If you must take a brand name drug, consider asking for a HIGHER strength, and then splitting the tablet in half to get your dose. This can save lots of money. For more tips, read my article entitled HOW TO SAVE MONEY ON LIPITOR.
5. Can't I just watch my diet and exercise instead? You should watch your diet and we all should exercise. These often lower your cholesterol a little. But most of the time this isn't enough to reduce your risk of heart disease. I illustrate it this way: If you are drowning at the bottom of the pool, it does you no good for me to remove a bucket of water from the pool. Unless I can get the pool water down SO LOW that you now can breathe...it simply is a waste of time to lower the water by a foot or two. Get the point? Lowering your cholesterol by a little might seem better than nothing...but when it comes to preventing a heart attack or stroke...it really isn't any better at all.
6. But what if I am otherwise healthy? This is a tough question, and medical practioners come down on both sides of this issue. Elevated cholesterol with NO other risk factors, disease or family history remains an open question in my opinion. I personally think the evidence leans toward using low potency statins in this scenario, but I appreciate and understand the concerns raised by some patients.
For a fair-minded debate between two doctors on the subject, READ HERE.
For more information, a nice article was written by Consumer Reports several years ago which compares the Statin Drugs.