The Risks of Cholesterol Drugs Vary As Widely As The Choices

By Steven Di Joseph -

I – The Statins

Although more people worldwide suffer from high cholesterol than ever before, the problem has reached epidemic proportions in the United States. Fast food, junk food, exceptionally large portions, poor eating habits, misleading or inadequate labeling, and lack of exercise, among other things, have produced the highest percentage of overweight Americans in history. Morbidly obese men, women, and even children are no longer oddities, they are commonplace. In addition, many foods now contain high amounts of saturated fat and/or trans fatty acids.

Trans fatty acids are found in many foods such as packaged cookies, crackers, and snacks, commercially fried fast food, vegetable shortening, and some margarine. Packaged goods containing “partially-hydrogenated vegetable oils” or “shortening” probably contain trans fats, too.

Before the advent of trans fatty acids, foods were cooked in or with lard, palm oil, butter, or other substances high in saturated fats. Saturated fats increase low-density lipoprotein (LDL), which is commonly referred to simply as “bad” cholesterol and are associated with an increased risk of heart disease. As a result, manufacturers and restaurants started using vegetable oils in their food production. Since liquid vegetable oils are not stable to heat and spoil easily, the process of “hydrogenation” is used to stabilize the liquid oils in food production and to increase their shelf life. The process of hydrogenation causes the formation of trans fatty acids.

Unfortunately, it has been discovered that trans fatty acids also increase LDL (bad) cholesterol and lower the high-density lipoproteins (HDL or good) cholesterol and, thus, also create an increased risk of heart disease. There have been some studies that have shown a diet high in trans fatty acids may also be linked to a greater risk of Type 2 Diabetes.

Untreated levels of high LDL cholesterol are therefore a very serious public health problem which is associated with a number of serious medical problems – some of which are life-threatening.
Not surprisingly, pharmaceutical manufacturers quickly discovered that there was a vast market for prescription drugs that would help lower cholesterol. This has led to the development of several cholesterol medications. Some of these drugs are better than others, some are safe than others, and some even have beneficial secondary effects. Others, however, are extremely dangerous and all of them need to be carefully monitored.

The medications which are currently available fall into a number of categories or classes. These include (chemical names – the brand names will be given in the actual discussion of each drug):

• Resins (cholestyramine, colesevelam, and colestipol)

• Fibrates (bezafibrate, clofibrate, penofibrate, and gemfibrozil)

• Statins (atorvastatin, fluvastatin, itavastatin, lovastatin, pravastatin, rosuvastatin, and simvastatin)

• Niacin

The statins consist of eight brand name drugs in seven sub-categories. Mevacor, Altocor, and Advicor (lovastatin), Pravachol (pravastatin), Zocor (simvastatin), Lescol (fluvastatin), Lipitor (atorvastatin), Crestor (rosuvastatin), and Baycol (cerivastatin) (withdrawn from the market in August 2001).
Many people, especially those with high cholesterol, have come to see all cholesterol as a “bad,” yet cholesterol is needed to form important hormones and perform other vital cell functions. The truly “bad” cholesterol is known as low-density lipoprotein (LDL) and it clogs arteries. “Good” cholesterol, or high-density lipoprotein (HDL), however, works like a drain cleaner for arteries.

Statin drugs work by inhibiting HMG CoA, an enzyme that enables the liver to make cholesterol. When the liver cannot produce its own cholesterol, it removes it from the blood. This causes blood levels of cholesterol to fall which, in turn, decreases the risk of clogged arteries. Statins are designed to reduce LDL levels. Yet, for many people, their HDL levels can rise while taking a statin drug.
For all the good they were supposed to do, statin drugs have been quite problematic for those taking them. While some side effects of statins are mild, they have been responsible for causing severe muscle breakdown known as rhabdomyolysis, liver disorder, kidney failure, and death.

Of the seven statins mentioned above, the worst of the lot are Baycol and Crestor. Baycol was removed from the market in August of 2001 and Crestor may soon be on its way to the prescription drug graveyard since it has already gained the reputation of being “new but more dangerous.”

Baycol

Although this drug has been removed from the market, it was taken by millions of people for significant periods of time.
Baycol, a statin drug manufactured by Bayer and GlaxoSmithKline, is currently the only cholesterol-lowering drug to be withdrawn from the market because of adverse effects. On August 8, 2001, the Bayer Pharmaceutical Division announced Baycol was being removed from the U.S. market because of reports of an adverse reaction of rhabdomyolysis (rhabdo). Unfortunately, by that point at least 6 million people worldwide had taken the drug.

Rhabdomyolysis is a muscle disease which causes kidney injury. It is categorized by the destruction of muscle cells that are subsequently released into the bloodstream. Symptoms of rhabdo include isolated or generalized muscle pain, weakness, tenderness, fatigue, malaise, fever, dark urine, nausea, and vomiting.
All drugs in the statin group have been linked to reports of rhabdo, but Baycol has been responsible for more fatal cases of the muscle disease. Before taking Baycol off the market, the U.S. Food and Drug Administration (FDA) received reports of more than 50 rhabdo-related deaths among Baycol users worldwide. The fatal cases primarily involved elderly patients, interactions with other prescription drugs, and higher dosages. Even after the drug was finally removed, fatalities continued to climb to more than 100.

After Baycol was pulled off the market, numerous lawsuits were filed by people injured by the drug. 3,500 lawsuits were filed and 2,825 claims were settled for a total of $1.08 billion. During that litigation, it was discovered that Bayer and GlaxoSmithKline knew of the harmful effects of Baycol before its release in 1997. In fact, memos from Bayer’s safety officials in 1999 revealed that its staff was struggling to respond to the growing number of patients who developed rhabdo. While the risk of rhabdo was described in the drug’s warning label, Bayer may not have conducted an appropriate amount of research to determine just how severe the risk was and what was necessary to prevent this risk from becoming fatal. In order to avoid having to report negative data to the FDA, Bayer did not do a sufficient amount of testing regarding the higher dosage, 0.8mg pills.

The Baycol situation is disturbing for several reasons. It serves as a reminder that drugs are often rushed to market (“fast tracked”) without adequate testing and research. In fact, the majority of drugs that are recalled are recalled within their first 5 years on the market. This proves that longitudinal testing is often absent and therefore long-term effects of certain drugs are never revealed until it is too late. (The recent Vioxx debacle is another example of this serious problem). Even in situations where drugs are properly tested, there is no guarantee that negative results will force a manufacturer to withdraw it from the market. Many drugs are being released and kept on the market despite evidence of serious side effects. Such decisions are usually motivated by financial considerations since a successful drug can often generation billions of dollars in annual revenue.

Crestor

Crestor, another statin drug, seemed to have been following in Baycol’s footsteps. However, it remains on the market. After reports of kidney damage and muscle weakness, a precursor to rhabdo, AstraZeneca abruptly stopped ongoing clinical trials for Crestor involving patients taking 80 milligrams per day. Crestor has been listed by Public Citizen as a “DO NOT USE” drug because, like Lipitor and Lescor, it has not demonstrated a significant health benefit in terms of lowering cholesterol and minimizing the risk of heart attack or stroke. Dr. Sidney Wolfe, director of Public Citizen’s Health Research Group, has gone on record as stating: “It becomes clearer by the day that this drug is uniquely toxic but offers no unique benefit, and must be removed from the market.”

AstraZeneca, however, countered the medical and scientific evidence of the drug’s dangers with an expensive direct to consumer marketing campaign featuring actor Patrick Stewart (Captain Jean-Luc Picard of Star Trek: The Next Generation). Thus, Crestor, like all too many other dangerous drugs, remains a “cash cow” because of creative marketing and not because it is a safe and effective treatment for the medical condition it was designed to alleviate.

Crestor has been labeled particularly dangerous because of the threat of kidney toxicity in addition to rhabdo, a relatively common side effect connected to statin usage. Unlike other statins, however, Crestor causes abnormal elevations in urine protein and blood, both of which are indicators of severe kidney toxicity. While other statins have been responsible for sporadic cases of rhabdo, Crestor is the only statin that has revealed the potential for life-threatening rhabdo development prior to FDA approval. As reported in PharmaLive: “The FDA had evidence before approving the cholesterol drug Crestor that it caused an increased incidence of rhabdomyolysis (severe muscle deterioration), yet the agency approved it anyway, erroneously believing that this toxicity was limited to an 80 milligram dose that was not ultimately approved.”

The warning label for all statin drugs, including Crestor, indicates that liver function tests are recommended both before and 12 weeks after beginning treatment or changing dosage. Periodic tests are recommended for as long as treatment continues. Rhabdo is also mentioned as a rare side effect as is acute renal failure. Rare or not, however, these side effects need to be taken seriously as they are potentially fatal.

Public Citizen’s Health Research Group believes that the FDA should have required routine urine testing for Crestor patients taking both available dosages as this would have revealed traces of protein, an indicator of kidney problems. In a letter to the FDA dated October 29, 2004, the organization has petitioned for the drug to be taken off the market. (Public Citizen made a similar petition in March, 2003).

As of now, regular urine testing is only required for people who have diabetes or are pregnant. Urine testing is just one way in which treatment should be continually and closely monitored. Ongoing monitoring by a physician is perhaps the only way to catch serious medical problems before they become fatal.

Cases of serious Crestor-related side effects began surfacing even before the drug was released on the global market. (As reported in PharmaLive: “The rate of reports of kidney failure or damage among patients taking the cholesterol drug Crestor is 75 times higher than in all patients taking all other statins, according to a Public Citizen analysis of government data.”) The reports of 65 Crestor-related cases of rhabdomyolysis in the United States is a rate approaching that of Baycol which was taken off the market for that very reason. As a result, two major U.S. insurance companies, WellPoint, and Group Health Cooperative of Puget Sound, have refused to reimburse for Crestor citing Baycol as a precursor.

Pravachol and Lipitor

Pravachol, another member of the statin family manufactured by Bristol-Meyers Squibb, has been connected to rhabdo as well as liver and kidney problems. Other side effects include difficulty breathing, closing of the throat, swelling of the face, hives, decreased urine or rust-colored urine, blurred vision, gas, bloating, nausea, heartburn, abdominal pain, constipation, diarrhea, coughing, headache, and insomnia. Any of these side effects can be indicators for more serious health problems.

Lipitor, manufactured by Pfizer, is one of the well-known statins and is widely advertised on television and in periodicals. Warning labels for Lipitor indicate the risk for rhabdo and kidney failure as the two most serious side effects with gas, constipation, heartburn, and stomach pain as the less serious side effects. Lipitor, like all statins, is not recommended for use by pregnant women or people with pre-existing liver problems.

In a study comparing the benefits of Pravachol and Lipitor, Pravachol proved to be inferior. In those patients taking Pravachol, arthrosclerosis worsened during the 18-month treatment period. Despite these findings, however, Pravachol is still being prescribed to patients looking to lower their cholesterol.

Dr. Steven Nissen, an eminent cardiologist at the Cleveland Clinic who directed the study of 502 patients, said that while he had changed his practices based on the findings of the study, he would not force his decision on any of his colleagues and leave them to make their own minds up. However, if a uniform system for prescription drug distribution by physicians is not adopted, some conscientious doctors may choose to stop prescribing a drug which has been deemed harmful while others may continue to promote it.

Pravachol should not be taken by anyone with liver disease. It also should not be used to lower high cholesterol that stems from medical conditions such as alcoholism, poorly controlled diabetes, an under active thyroid, or kidney problems. Pravachol may have significant interactions with other drugs such as: Questran, Tagamet, Colestid, Cardizem, Dilacor, Tiazac, Sandimmune, Neoral, Erythromycin, Lopid, Sopranox, Niacor, Niaspan, and Coumadin.

There is also some suspicion that Pravachol may cause birth defects and so it should not be taken by pregnant women. It should also not be prescribed to women who are breastfeeding.

Lipitor should not be taken by anyone with liver disease, during pregnancy, or while breastfeeding. Serious drug interactions may occur if Lipitor is taken with: Antacids such as Maalox TC Suspension, Atromid-S, Colestid, Sandimmune, Neoral, Digoxin, Lanoxin, immune system suppressors, Erythromycin, Tricor, Diflucan, Lopid, Sporanox, Nizoral, Niaspan, Niacor, Slo-Niacin, and oral contraceptives.

Zocor

Although Zocor, also known as simvastatin, was not recalled for its potentially fatal issues, the FDA has put additional warnings out for the product. The FDA recommends “that simvastatin 80 mg be used only in patients who have been taking this dose for 12 months or more and have not experienced any muscle toxicity.” Zocor, which is marketed by Merck, has become one of the more popular statins as it is widely advertised on television and in periodicals.

While some side effects such as pain or weakness, liver complications, and harmful drug interactions do exist, Zocor is promoted as being “a cholesterol medication proven to significantly reduce the risk of heart attack and stroke in people with heart disease or diabetes – regardless of cholesterol level.” This may be one benefit to Zocor but new dangers were discovered in 2002.

In July of 2002, Merck was forced to revise the warning label for Zocor to include information about the potential risk for developing myopathy and rhabdo from taking the drug alone or in combination with other medicines. Again, this is a persistent problem for all statins and while some may have benefits that seem to place them at a level above the rest, the risk for these muscle illnesses should not be overlooked. A spokesperson for Merck said that the new FDA-required warning adds clarity but does not change the pre-established safety and “efficacy” of Zocor.

Zocor should be discontinued before major surgical procedures. Its interaction with certain other drugs must be carefully monitored. For example: Zocor tends to enhance he effects of Coumadin and Lanoxin. It also increases the chance of muscle damage when combined with: Cordarone, Biaxin, Atromid-S, Sandimmune, Neoral, Erythromycin, Tricor, Lopid, Sporanox, Nizoral, Serzone, Niaspan, Protease inhibitors (used in treatment of HIV), Calan. Zocor may also cause serious problems when combined with significant quantities of grapefruit juice. Zocor should be avoided by women who are pregnant or breastfeeding.

Lescol

Lescol is available in standard capsules and extended-release tablets (Lescol XL). As with all statins, liver damage is a possibility. Thus, liver enzyme levels should be tested on a regular basis. Signs of damage to muscle tissue should also be reported immediately. Serious drug interactions may occur when Lescol is taken with: Questran, Tagamet, Atromid-S, Sandimmune, Neoral, Voltaren, Lanoxin, Lanoxicaps, Erythromycin, Lopid, Micronase, Niaspan, Prilosec, Dilantin, Zantac, and Rifadin. Lescol should not be taken by women who are pregnant or breastfeeding.

Lovastatin (Altocor, Mevacor, and Advicor)

These three drugs are essentially the same. Mevacor is the “standard” form of lovastatin, Altocor is an extended-release form of the drug, and Advicor is Mevacor combined with extended-release Niacin.

Again, since the various forms of lovastatin are members of the statin class of drugs, liver and muscle tissue damage are possible side effects. Women who are pregnant or breastfeeding should avoid the drug as should those with liver disease. Altocor is not recommended for people below the age of 20. Advicor is not recommended for children. Mevacor may be prescribed for children between 10 and 17 but only if introduced in intervals of 4 weeks or more and in girls who have been menstruating for at least one year. The safety and effectiveness of Mevacor has not been studied in children under 10 or in children of any age in doses larger than 40 milligrams per day.

Lovastatin taken with large quantities of grapefruit juice may cause serious problems and should not be combined with certain other drugs such as: Antipyrine, Coumadin, Dicumarol, Tagamret, Diflucan, Blaxin, Sandimmune, Neoral, Erythromycin, Lopid, HIV protease inhibitors, Sporanox, Nizoral, Aldactone, Serzone, Niaspan, Niacor, Calan, and Verelan.

Statins, as a group of drugs, are often an acceptable solution for people who have undergone a long and arduous battle with cholesterol maintenance. Although the drugs do have potentially serious side effects, such problems are usually avoidable with careful medical monitoring and by patients being thoroughly aware of the warning signs associated with those side effects. Patient awareness cannot be overemphasized. The key is for all patients taking any of the statins to ask questions, read the product information, be aware of potential drug and food interactions, follow dosage and other instructions carefully, and make every effort to follow a proper and healthy diet and exercise plan. We also strongly urge all potential statin users to avoid the more risky drugs such as Crestor and Pravachol.

In addition to the aforementioned side effects relating to specific statins, the following information should be taken into account as it relates to most or all statins.

• Statin drugs such as Lipitor, Zocor, Pravachol, Crestor, Lescol, Mevacor, and Baycol may be linked to birth defects. These drugs may cause severe central nervous system defects and limb deformities when used within the first trimester of pregnancy. These are the types of problems which can be expected when the embryo does not get enough cholesterol during the early stages of pregnancy.

• Young people are specifically at risk for developing ailments associated with the statins as the drugs’ effects on that age group are not yet well understood. Patients age 45 and under have been the least studied age group in terms of statin use. Statins have been prescribed to younger men and women in response to the growing realization that high cholesterol early in life can lead to life-threatening cardiovascular consequences later on.

• Statins can cause nerve damage, or polyneuropathy, in extremely rare circumstances. A Danish physician noticed this side effect in 14 statin patients. This has not been listed as a primary side effect because of its rarity.

• Statins have been linked to memory loss following the outcome of a study at University of California at San Diego. Cholesterol, which is related to heart disease, is also an essential organic molecule in the brain. Some researchers have postulated that if cholesterol production is blocked, such as when statins enter the body, it can interfere with the brain’s performance and cause memory loss. Risk factors of memory problems are heart disease and stroke. More research is being conducted on this matter.

• One very vocal lung cancer sufferer believes his long-term use of Lipitor played a role in his development of that disease. He has carefully analyzed animal testing data which suggests that the statins may be the most carcinogenic drugs ever approved for wide scale human consumption. (Significantly, lab animals were exposed to dosages on the order of those prescribed to humans). He also claims that this grave side effect has been “missed” because it is so long-term, possibly up to 20 years. His story and links to additional material relating to the cancer study can be found at http://www.captainclark.com?Pages/lipitorhorror.html.

Many of the statin drug labels were updated as of February 28, 2012. The changes include topics, such as: monitoring liver enzymes, adverse event information, drug interactions, and more. Details on the label changes can be found at http://www.fda.gov/Drugs/DrugSafety/ucm293101.htm

II – The Non-Statins

Three other categories of cholesterol-lowering medications are fibrates, resins, and niacin (nicatonic acid). The fibrate group includes the drugs Bezalip, Atromid-S, Tricor, and Lopid. The resins are Cholybar, Questran, and Prevalite. Niacin based medications include Advicor, Niacor, Niaspan, Nicobid, and Nicolar.

In addition to these three categories of drugs, there are two new cholesterol medications on the market. These drugs are Zetia and Vytorin.

All cholesterol-lowering drugs are intended to supplement a healthy lifestyle of proper diet and exercise. They should never be seen as a means by which to continue (or start) poor eating habits or other problematic behavior.

FIBRATES

The cholesterol drugs known as fibrates lower LDL (“bad”) cholesterol and triglycerides while raising HDL (“good”) cholesterol. They achieve this result by inhibiting; (a) the liver’s production of proteins containing fat and cholesterol; and (b) the release of triglycerides from fat stores in the body. Generally, all of the fibrates act in a similar manner. It is important to know, however, that the severity of the side effects varies widely from one fibrate to another.

Lopid (gemfibrozil)

Lopid is used to help people who have had little success in lowering their cholesterol through diet and exercise alone as well as to reduce the risk of heart disease. Common side effects associated with Lopid include; abdominal pain, acute appendicitis, constipation, diarrhea, eczema, fatigue, headache, indigestion, nausea/vomiting, rash, and vertigo. Rare side effects have included; anemia, blood disorders, blurred vision, confusion, convulsions, decreased male fertility, decreased sex drive, depression, dizziness, fainting, hives, impotence, inflammation of the colon, irregular heartbeat, itching, joint pain, laryngeal swelling, muscle disease, muscle pain, muscle weakness, painful extremities, sleepiness, tingling sensation, weight loss, and yellow eyes and skin. Before taking Lopid, you should speak with your physician about the possibility that the drug may cause malignancy, gallbladder disease, abdominal pain leading to appendectomy, or other potentially fatal abdominal disorders.

Lopid should never be combined with any of the statin drugs as the combination can possibly cause serious muscle-wasting side effects. Blood-thinning drugs such as Coumadin should also be avoided while taking Lopid and anyone beginning treatment for high cholesterol with Lopid should consult their physician to find out about any other potentially harmful drug interactions.

The recommended dosage of Lopid is 2 doses of 600mg taken 30 minutes before breakfast and dinner. Lopid is not approved for use in children and should be used carefully by older adults. If you are experiencing sudden abdominal cramps, diarrhea, joint and muscle pain, nausea or vomiting, you may be having symptoms of an overdose and should seek medical help immediately.

Tricor (fenofibrate)

Tricor, or Lofibra, is used to lower triglyceride levels. Common side effects of Tricor include abdominal pain, headache, and various respiratory disorders. Less common side effects include constipation, diarrhea, flu-like symptoms, nausea, runny nose, and general weakness. Perhaps the most serious side effect is the rare, but possible, development of rhabdomyolysis, the muscle-wasting disease also associated with statins. Tricor also has the potential to cause gallstones and may affect liver function negatively.

Sometimes Tricor will be prescribed with other cholesterol lowering drugs, specifically in the resin group. If this is the case, always take Tricor at least 1 hour before or 4 to 6 hours after taking the other drug. Tricor should always be taken with meals and is not recommended for use by children or nursing mothers.

The dosage for Tricor depends on the level of cholesterol and triglycerides but usually, the initial dosage is 160mg per day which is also the maximum dosage. The initial dosage for Lofibra, however, is usually only 67mg per day with a maximum daily dosage of about 200mg.

Bezalip (bezafibrate)

Before beginning treatment with Bezalip, make sure to tell your doctor if you currently have or have ever had kidney or liver problems, or gallbladder disease (with or without gallstones). Women who are pregnant or breastfeeding should not take Bezalip.

Side effects associated with Bezalip include anemia, loss of appetite, unexplained bleeding, tendency to bruise more easily, cholestasis, dizziness, feelings of fullness, fever, gallstones, being more prone to infection, hair loss, headache, hypersensitivity reaction including angiodema, itchy skin, muscle weakness (potentially leading to rhabdo), myopathy, nausea, photosensitivity, sexual dysfunction, and sore throat.

Bezalip may interact negatively with hypoglycemics, insulin and sulphonylureas, MAOI inhibitors, warfarin (Coumadin) and other blood thinners, oral contraceptives, and, most notably, statins and resins.

Atromid-S (clofibrate)

The lipid-lowering agent Atromid-S works just like other fibrates yet it has been linked to more serious side effects. Although the most common side effect is nausea, there is a remarkably lengthy list of less common side effects, including; vomiting, loose stools, dyspepsia, flatulence, abdominal distress, headache, dizziness, fatigue, muscle pain, skin rash, dry brittle hair, alopecia, increased or decreased angina, cardiac arrhythmias, allergic reactions including urticaria, toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome, gallstones, hepatomegaly, gastritis, anemia, impotence and decreased libido, renal dysfunction, myalgia, rhabdo, and weight gain.

Pregnant and nursing women should not take Atromid-S. It is also not recommended for patients who have had clinically significant hepatic or renal dysfunction.

The extensive list of side effects relating to Atromid-S (as opposed to the other fibrates) is particularly problematic as it poses some sort of hazard to almost every part of, or system in, the body. As a result, both the doctor and the patient should be convinced that Atromid-S is, indeed, the right choice before a treatment regimen is commenced.

RESINS

Resins, otherwise called bile acid sequestrants, help to reduce high levels of bad cholesterol by binding with cholesterol-containing bile acids found in the intestines. By doing this, resins prevent the bile from being reabsorbed before it is eliminated by the body. The liver, which normally makes bile out of cholesterol, can then produce a replacement supply of bile acids and take the extra cholesterol out of the bloodstream. These medications lower LDL-cholesterol levels by about 10 to 20 percent but do not specifically lower triglyceride levels. Thus, resins are often used in combination with other cholesterol-lowering drugs.

Questran (cholestyramine)

Questran is prescribed to lower LDL levels in the blood as well as to relieve itching associated with gallbladder obstruction. It is also available in a less-potent form known as Questran Light. Questran prescribed in powder form, should never be taken dry. It should always be mixed with water or another liquid, applesauce, or crushed fruits.

The most common side effect associated with Questran is constipation. People with a history of constipation are often discouraged from using Questran. Less common or rare side effects include; abdominal discomfort, anemia, anxiety, arthritis, asthma, backache, belching, black stools, bleeding gums, blood in the urine, brittle bones, dental cavities, diarrhea, difficulty swallowing, dizziness, drowsiness, fainting, fatigue, fluid retention, gas, headache, heartburn, hiccups, hives, increased sex drive, increased tendency to bleed, inflammation of eye or pancreas, irritation around anal area or skin and tongue, joint pain, lack or loss of appetite, muscle pain, nausea, night blindness, painful or difficult urination, rash, rectal bleeding and/or pain, ringing in the ears, shortness of breath, sour taste, swollen glands, tingling sensations, ulcer attack, vertigo, vomiting, weight gain or loss, wheezing and vitamins A, D, E and K deficiencies.

People with phenylketonuria (an inherited disease characterized by inability to oxidize a metabolic product of phenylalanine and by severe mental deficiency — abbreviation PK) should be sure to check with their physician before taking Questran Light as it contains phenylalanine. Anyone taking drugs that may raise cholesterol levels or being treated for any disease contributing to increased blood cholesterol such as hypothyroidism, diabetes, nephritic syndrome, dysproteinemia, obstructive liver disease, or alcoholism should be especially careful when taking Questran.

Questran should not be taken in conjunction with hormones, oral diabetes drugs, Phenobarbital, thyroid medication such as Synthroid, and warfarin (Coumadin) amongst others. Consult your physician if you are taking any other medication prior to beginning treatment with Questran.

Welchol (colesevelam)

Welchol can be prescribed alone or in conjunction with statin drugs such as Lipitor or Zocor to help lower cholesterol. It should always be taken at mealtime with some kind of liquid unless your physician instructs you otherwise.

Side effects associated with Welchol include constipation, indigestion, muscle aches, sore throat, and weakness. If you have a bowel obstruction, have difficulty swallowing, or suffer from severe digestive problems, you should not take Welchol. There are no significant food or drug interactions pertaining to Welchol.

Colestid (colestipol)

Colestid can be prescribed in granule or tablet form. The granules must be mixed with liquids such as flavored drinks, milk, orange juice, pineapple juice, tomato juice, or water. Although carbonated beverages may also be used, they may sometimes cause stomach or intestinal discomfort. If Colestid granules are accidentally inhaled they may cause serious effects and thus should never be taken in their dry form.

The most common side effects associated with Colestid are constipation and worsening of hemorrhoids. Less common side effects include abdominal bloating or distention/cramping/pain, aches and pains in arms and legs, angina (crushing chest pain), anxiety, arthritis, backache, belching, bleeding hemorrhoids, blood in stool, bone pain, chest pain, diarrhea, dizziness, drowsiness, fatigue, gas, headache, heartburn, hives, indigestion, insomnia, joint pain, light-headedness, loose stools, loss of appetite, migraine, muscle pain, nausea, rapid heartbeat, rash, shortness of breath, sinus headache, skin inflammation, swelling of hands or feet, vertigo, vomiting, and weakness.

People with diseases that may cause increased blood cholesterol, such as underactive thyroid gland, diabetes, nephritic syndrome, dysproteinemia, obstructive liver disease and alcoholism should not take Colestid before consulting a physician. Colestid may cause or worsen constipation and therefore anyone who should avoid aggravated constipation, such as those with coronary artery disease or severe hemorrhoids, should talk to their physician before taking the drug. When Colestid is taken with other drugs including folic acid, certain vitamins, Hydrocortizone, Penicillin G, and the fibrate Lopid it may have negative interactions.

NIACIN (Nicatonic Acid)

The cholesterol drugs in the niacin group are Niacor, Niaspan, Nicobid, Nicolar, Slonacin, and Advicor which is a combination of nicatonic acid and Lovostatin. While the aforementioned drugs have virtually the same effect, they fall into three different categories: immediate release, timed release, and extended release. Niacin, otherwise known as the vitamin B3, has been proven to help lower cholesterol levels when taken in high dosages. It works by inhibiting the liver’s production of fat and cholesterol containing proteins.

General side effects for nicatonic acid include flushing or hot flashes, nausea, indigestion, gas, vomiting, diarrhea and activation of peptic ulcers. Flushing can be accompanied by dizziness, fainting, heartbeat irregularities, chills, hives, itchiness, shortness of breath, or swelling. Taking aspirin or a nonsteroidal anti-inflammatory medication (NSAID) such as Motrin or Aleve 30 minutes before taking Niaspan can help minimize flushing.

If you are taking a form of niacin, you must follow the instructions very carefully since many unpleasant side effects will result from not doing so. You must take the drug with food and avoid taking it with any warm or hot liquid. It must be taken in high dosages to be effective so most physicians recommend a gradual increase in the dosage until the maximum is reached. A sudden jolt of large doses of niacin may trigger some very unpleasant and even dangerous reactions.

Although things like hot flashes and hives sound relatively harmless, many people are made so uncomfortable they are unable to take massive doses of niacin. Imagine being at work, at an important meeting, or in a movie theater when you suddenly break out in hives, feel as if you are burning up, and become so itchy that you begin scratching yourself until you bleed. You might also feel so lightheaded or dizzy that you become disoriented and unable to stand. While none of this is life-threatening, it can be so unpleasant that repeating it on a daily basis is simply unacceptable. Sometimes, a patient will develop a tolerance for niacin after several days or weeks. Most people who suffer these side effects, however, never reach that point and simply give up on the therapy.

Advicor

Advicor is a combination of extended-release niacin and lovostatin, or Mevacor. Common side effects include; abdominal pain, back pain, diarrhea, flu-like symptoms, flushing, headache, high blood sugar, indigestion, infection, itching, muscle pain, nausea, pain, rash, vomiting, and weakness.

There is, however, an even longer list of less-common side effects including various allergic reactions, anxiety, chest pain, chills, constipation, darkening of skin color, decreased sex drive, difficulty sleeping, dizziness, dry mouth, dry skin, enlarged breasts in men, eye irritation, fainting, gas, general feeling of unwellness, gout, hair loss, heartbeat irregularities, hives, inflammation of pancreas, impotence, joint pain, liver disorders, loss of appetite, low blood pressure, memory loss, mental changes, migraine, muscle cramps, muscle disorders, nerve disorders, runny nose, shortness of breath, skin and nail changes, sweating, swelling, tingling, tremor, ulcers, vertigo, vision disorders, and yellowing of skin and eyes.

You should not take Advicor if you have liver disease, an ulcer, or arterial bleeding. It should be taken at bedtime with food, specifically a low-fat snack unless you are instructed otherwise by your physician.

Drugs that may interact negatively with Advicor are: Antifungal drugs such as Sporanox and Nizoral, blood pressure medications, cholesterol-lowering fibrates such as Lopid and Atromid, Erythromycin (E.E.S., Erythrocin), HIV protease inhibitors such as Viracept and Norvir, Nefazodone (Serzone), Nitroglycerin, Nutritional supplements containing niacin or nicotinamide, and warfarin (Coumadin).

Niacor is the extended-release version of Advicor.

Niaspan

Niaspan can be taken in conjunction with drugs from the resin group as well as the statin group to achieve lower LDL-cholesterol levels when diet and exercise have failed. Side effects associated with Niaspan include abdominal pain, hot flashes, chills, diarrhea, dizziness, fainting, flushing, headache, indigestion, hives and itching, nasal inflammation, nausea, pain, rapid heartbeat, rash, shortness of breath, sweating, swelling due to fluid retention, and vomiting.

As is the case with other niacin-based drugs, Niaspan can be hazardous for people with diabetes, heart conditions, or problems with gout. If you experience a change in blood-sugar levels while on Niaspan, tell your physician immediately. Preexisting kidney and liver problems or weaknesses can lead to complications with Niacin as well.

Since niacin therapy is essentially taking a vitamin in large doses, overdosing with drugs such as Niaspan has occurred. An excessive amount of Niacin is more than 2,000 milligrams a day. This can cause liver damage and stomach ulcers. Other signs of long-term overdose could be nausea, vomiting, abdominal cramps, faintness, and yellowish skin and eyes.

Slo-Niacin is the extended release form of the drug.

A NEWER CATEGORY

Since drugs designed to lower LDL-cholesterol levels and triglycerides have become increasingly popular, pharmaceutical companies are always seeking to cash in on the trend by developing new alternatives. One of the problems with the existing cholesterol remedies is that, more often than not, the bad outweighs the good. The possibility of trading high cholesterol for kidney or liver disease is an unpleasant choice that is made every day by people taking many of the drugs we have been discussing.

In the past year, however, two new cholesterol medications have been approved which might prove to be better options once all the results are in. Of course, in the unpredictable world of prescription drugs, they might also turn out to be more dangerous.

Zetia (ezetimibe)

Schering-Plough pharmaceuticals developed the non-statin Zetia in hopes of competing with the current cholesterol drug leader, Lipitor. Zetia works slightly differently from statins by reducing the absorption of bad cholesterol in the digestive tract. While Zetia can be prescribed on its own, it is often prescribed in conjunction with a statin for optimal results.

Common side effects for Zetia are abdominal or back pain, diarrhea, joint pain, and sinusitis. Rare side effects include coughing, fatigue, sore throat, sexual dysfunction and viral infection. These minor side effects are similar to those associated with the other cholesterol lowering agents. More severe problems such as liver damage and serious muscle pain are also under investigation.

The recommended dose for Zetia is 10mg per day. Zetia should never be combined with any of the fibrates such as Lopid and Tricor but it can be taken with resins such as Colestid, Questran, or WelChol.

Vytorin

Following Zetia’s approval, Merck and Schering-Plough launched Vytorin, a combination of exetimibe, the active ingredient in Zetia, and simvastatin, the chemical found in Zocor. Vytorin was approved on July 23, 2004. Vytorin’s approval coincided with the guidelines issued by The National Cholesterol Education Program which indicated that now more Americans need cholesterol-lowering medications than previously thought.

The starting dose of Vytorin is 10mg of Zetia and 10mf of Zocor. Side effects include allergic reactions including rash, inflammation of the pancreas, nausea, headache, dizziness, gallstones, inflammation of the gallbladder, and swelling of the face, lips, tongue, and or throat that may cause difficulty in breathing. The risk of muscle breakdown, a precursor to rhabdo, does exist with Vytorin and is categorized by muscle pain, tenderness or weakness. If you are experiencing any unexplained muscle pain while taking Vytorin, consult your physician immediately.

Those with liver problems or liver disease as well as any women who are pregnant or may become pregnant should not take Vytorin.

At present, Vytorin seems to be the safest existing solution for management of cholesterol and triglyceride levels. It is the first drug to reduce LDL-cholesterol by inhibiting cholesterol production in the liver as well as cholesterol absorption in the intestine. (This process is known as Dual Inhibition.) Bassem El-Masri, a cardiologist and cholesterol researcher at Cornell Weill Medical School believes that Vytorin will allow doctors to treat heart disease forcefully without worrying as much about safety.

Currently, no cholesterol drug is without potentially serious side effects which may ultimately do more damage than the condition they are intended to treat. Ideally, these drugs should have beneficial side effects such as raising “good” cholesterol levels or preventing heart attacks. Unfortunately, that is not yet the case.

Thus, before beginning any type of drug regimen for high cholesterol, make sure to get all of the facts from your physician to be sure that you are selecting the medication that is best (or least risky) for you. The wide range of existing options provides some flexibility to those in need of such treatment. However, most medical experts continue to stress the fact that lifestyle modifications with respect to diet and exercise are the single most important “regimen” for the reduction of cholesterol levels.

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