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What a mess! Nearly 2 years after Merck & Co. yanked its blockbuster painkiller, Voixx®, off the market, the furor is still raging. How could a drug climb to $2.5 billion in annual sales, despite evidence that it caused heart problems? The company continues to face personal injury lawsuits that will cost billions. The firm’s share price has plummeted, knocking tens of billions of dollars off the value of the world’s fourth largest drug company. As the lawsuits pile up, the proud, insular giant is giving every indication that it has no idea what it is dealing with. Many say the firm is “bewildered”. The Food & Drug Administration has also been widely criticized for its role in assessing Vioxx, and the agency is scrambling to look as if it is overhauling its broken system of drug approvals. Congress is holding hearings to try to figure out who’s to blame, and it might not stop just with Vioxx. Celebrex® and Bextra® could be next!

Research and Development Strengthen the Future for Natural Arthritis Remedies

The most common chronic health problem and a leading cause of disability in America, arthritis, is a family of more than 100 diseases, the most prevalent of which are osteoarthritis (OA) and rheumatoid arthritis (RA). While this group of diseases affects areas in or around joints, arthritic action can also impact other parts of the body. Fortunately, the over-the-counter (OTC) arthritis market is a hotbed for natural remedies, as pharmaceutical medications, such as Vioxx® and Bextra®, have continuously failed safety investigations. Research on natural products and all aspects of arthritis have exploded.

Non-steroidal an anti-inflammatory drugs (NSAIDS) are the most commonly used class of arthritis medication. They function by blocking cyclooxygenase (COX) enzymes. Drugs that selectively inhibited the COX-2 enzyme (in theory, less likely to provoke gastrointestinal bleeding) reached the market in 1998, and screeches to a near halt in 2004-05 when Vioxx® (voluntarily) exited the U.S. market. Celebrex® is still prescribed, however, more cautiously than before. Arcoxia® and Prexige® are approved in some countries, but not in the US.

GLUCOSAMINE

Glucosamine is an amino monosaccharide found in chitin, glycoproteins and glycosaminoglycans (formerly known as mucopolysaccharides), such as hyaluronic acid and heparin sulfate. Glucosamine is also known as 2-amino-2-deoxyglucose, 2-amino-2-deoxy-beta-D-glucopyranose and chitosamine. Glucosamine has the following chemical structure:

Glucosamine is available commercially as a nutritional supplement in three forms: glucosamine hydrochloride (glucosamine HCL), glucosamine sulfate and N-acetyl-glucosamine.

At neutral, as well as physiologic pH, the amino group in glucosamine is protonated, resulting in it having a positive charge. Salt forms of glucosamine contain negative anions to neutralize the charge. In the case of glucosamine hydrochloride, the anion is chloride, and in glucosamine sulfate the anion is sulfate. N-acetylgucosamine is a delivery form og glucosamine in which the amino group is acetylated, thas neutralizing its charge. To date, most of the clinical studies examining the effect of glucosamine on osteoarthritis have been performed with either the sulfate or the chloride salts of glucosamine. All three forms are water soluble.

PHARMACOKINETICS

Pharmacokinetics of glucosamine are derived primarily from animal studies. About 90% of glucosamine administered orally as a glucosamine salt gets absorbed from the small intestine, and from there it is transported via the portal circulation to the liver. It appears that a significant fraction of the ingested glucosamine is catabolized by first-pass metabolism in the liver. Free glucosamine is not detected in the serum after oral intake, and it is nor presently known how much of an iingested dose is taken up in the joints in human. Some uptake in the articular cartilage is seen in animal studies.

INDICATIONS

Glucosamine mau be indicated for the treatment and prevention of osteoarthritis, either by itself or in combination with chondroitin sulfate (see Chondroitin sulfate). Pharmaceutical-grade crystalline 99% glucosamine HCL is the most absorbable version available.

Nexrutine® Phellodendron Amurense: A Natural COX-2 Inhibitor

Phellodendrone amurense contains, amongst other alkaloids, berberine – a COX-2 inhibitor that has the ability to inhibit thromboxane – a COX-2 inflammatory hormone.  Berberine inhibits COX-2, without inhibiting COX-1, meaning that it is a selective inhibitor. It has been shown to block 95% of COX-2 production, essentially “shutting off” the source where inflammation occurs. Unlike other COX-2 inhibitors, phellodendron does not act directly on the enzyme itself. Instead, phellodendron’s true strength lies in its ability to inhibit the actual production of the enzyme that leads to the inflammation. Phellodendron inhibits the gene expression of the COX-2 enzyme, and is free of any cardio-vascular problems. Phellodendron’s safety is further enhanced by the fact that the major compound (berberine) does not cause platelets to aggregate. The anti-inflammatory products, like Vioxx® and Bextra®, have shown to increase the risk for cardio-vascular problems by causing platelets to aggregate. Phellodendron amurense has been used safely for centuries for various conditions in traditional medicine. Research has reported phellodendron not only has COX-2 inhibiting qualities, but also protects the gastrointestinal tract against ulceration. Phellodendron has been used for centuries in Chinese medicine for individuals with gastroenteritis, abdominal pain, and diarrhea. A Japanese study of laboratory animals with alcohol and aspirin induced ulcers, concluded that phellodendron actually decreased gastric acid content, protecting the stomach lining and suppressing ulceration. This is exciting news, as we now have a natural product that not only can be used for inflammatory conditions, but may also aid in protecting the stomach lining against the main problem resulting from the use of NSAIDs (such as acetaminophen and ibuprofen) – gastric ulceration. Phellodendron is a very significant alternative to prescription and OTC pain killers. Phellodendron blocks the “bad” chemical (95% inhibition of COX-2) and does not interfere with the “good” chemicals (no inhibition of COX-1).

MSM (methyl-sulfonyl-methane)

Methyl-sulfonyl-methane (MSM) is a naturally occurring sulfuric compound found in the human body, as well as in many common beverages and foods, including milk, coffee, tea, and green vegetables. In its purified chemical form, MSM is an odorless, essentially tasteless, white, water soluble crystalline solid. MSM is one of the least toxic substances in biology, similar in toxicity to water.

MSM is a relative to dimethyl sulfoxide (DMSO), a unique therapeutic agent used worldwide in the treatment of many painful and inflammatory conditions. MSM has many of DMSO’s properties, but without the oyster-like odor and other side effects. MSM is a naturally occurring sulfuric compound that plays a critical role in forming muscles, nails, hair and skin, as well as building healthy cells. In their book, The Miracle of MSM; The Natural Solution for Pain, Stanley W. Jacoob, M.D., and Ronald M. Lawrence, M.D., Ph. D., state: “MSM offers a natural way to reduce pain and inflammation without serious side effects. MSM may even deliver as much or even more relief as some of the standard painkillers – MSM just doesn’t work as fast. That’s because MSM is not a drug; MSM is a nutritional supplement. But you will often begin to experience noticeable easing of pain and discomfort, along with more energy, and in general feel better, within days of starting MSM.”

Many years of clinical use at Oregon Health Sciences University have demonstrated that MSM provides major pain relief through the following actions:

>> MSM inhibit pain impulses along nerve fibers (analgesic effect)

>> MSM lessens inflammation

>> MSM increases blood supply

>> MSM reduces muscle spasm

>> MSM aides in the softening of scar tissue

Boswellia / Boswellic Acid

Boswellia serrata

5-LOXIN® is a product that was recently introduced to the supplement market. It cites an ayurvedic heritage for boswellia serrata as evidence, while also claiming that it is much more potent that traditional products (mostly boswellic acid preparations) because the 3-O-acetyl-1`-keto-beta-boswellic acid (AKBA) content is 10 to 15 times higher. All of the clinical evidence on boswellia has been performed with 700-1000 mg per day of low AKBA products (which are typically described as containing 50-70% total boswellic acids). 5-LOXIN, however, is recommended in only 100 mg per day doses due to its high AKBA content.

5-LOXIN is a new, patent-pending dietary supplement with significant potential for joint health, and other inflammatory disorders. 5-LOXIN inhibits several inflammatory mediators and inhibits collagen degradation, an important component of connective tissues.

5-LOXIN inhibits an enzyme called 5-lipoxygenase. Less famous than COX-2, 5-LOX inhibitors follow a distinctly different inflammation pathway, one without the potentially negative effects associated with COX-2 inhibitors, and 5-LOXIN is a selective, non-redox 5-LOX inhibitor, which means that its action is very targeted, not affecting other systems. 5-LOXIN’s safety is supported by historic usage and recent toxicity and safety studies.

5-LOXIN is a standardized extract of boswellia serrata, providing 30% acetyl-11-keto-beta boswellic acid (AKBA). Recent research has identified AKBA as the most potent of all boswellic acids. While other extracts contain 2-3% AKBA, the patented process for creating 5-LOXIN results in a 30% standardized AKBA extract, providing the highest concentration available.

5-LOXIN is a potent inhibitor of inflammation, and it inhibits the breakdown of joint cartilage and tissues:

◊ 5-LOXIN inhibits inflammation in two ways:

1.  5-LOXIN is a potent inhibitor of 5-lipoxygenase (5-LOX), a key enzyme involved in the mediation of inflammation (leukotriene biosynthesis).

(5-LOX inhibition is a separate pathway to COX-2 inhibition)

There are two types of 5-Lipoxygenase inhibitors, redox and non-redox. Redox inhibitors also iteract with other biological redox systems, which may lead to side effects. Non-redox type 5-Lipoxygenase inhibitors do not.

Further, 5-LOXIN is not only a non-redox type, but also selective 5-Lipoxygenase inhibitor, resulting in a very targeted benefit.

2.  5-LOXIN inhibits ICAM and VCAM, adhesion molecules that are directly involved in inflammation.

Endothelial VCAM-1, for example, is a central player in reruiting white blood cells to the area of inflammation.

SAM-e

SAM-e is best known as a natural remedy for depression, but it can also ease the moderate pain and decreases mobility associated with osteoarthritis. (SAM-e stands for S-adenosylmethionine, a molecule that assists in several chemical reactions in your body.) Clinical trials on more than 22,000 patients have shown that SAM-e can relieve osteoarthritis pain, and doctors in Europe have been treating osteoarthritis and depression with it for decades. “Depressions can make the symptoms of osteoarthritis more intolerable”, notes Graeme Shaw, M.D., an integrative medicine physician in Los Altos, CA. Nearly all the experts we spoke to recommended SAM-e.

SAM-e delivers sulfur to your cartilage, where it helos build the collagen (protein fiber) bonds that strengthen your joints. “The sulfur SAM-e also help relieve pain and inflammation”, says Lisa Stein, D.C., a chiropractor in Cupertino, CA. Experts aren’t sure how SAM-e alleviates depression. “Some believe that SAM-e helps produce mood-boosting chemical messengers in the brain”, explains Jonathan Alpert, M.D., Ph.D., Associate Director of the Depression Clinical and Research Program at Massachusetts General Hospital in Boston.

A 2002 review of 11 randomized, controlled studies concluded that SAM-e is more effective in improving joint function in osteoarthritis patients than placebo, and that it is just as effective in reducing pain and improving joint function as nonsteroidal anti-inflammatory drugs (like ibuprofen). The review has published in the Journal of Family Practice. In a 1987 double-blind study in the American Journal of Medicine, 22 people with osteoarthritis of the knee took 1200 mg of SAM-e daily and 23 took the drug piroxicam. Both treatments significantly relieved pain and improved morning stiffness and mobility. However, patients who took SAM-e maintained these benefits longer after stopping the supplement than patients who took the conventional drug.

Turmeric

Most people know turmeric as a culinary herb (it’s the spice curry powder that makes it yellow), but also possesses potent medicinal properties. A member of the ginger family, turmeric (Curcuma longa) treats mild osteoarthritis pain and inflammation. Only animal studies have proven its ability to reduce joint inflammation, but the herb has a centuries-long history of being used for inflammation in Ayurveda, the traditional medical system in India. Several of our experts agreed that turmeric can effectively relieve joint pain.

“Doctors and researchers are unsure exactly how turmeric works, although it appears to inhibit the production of inflammatory chemicals called prostaglandins and leukotrienes”, Hobbs says. A 1997 study in Molecular and Cellular Biochemistry showed that turmeric lowered inflammation. Other studies have been done on inflammation not related to joints; one of this studies involved rats, and another involved surgery patients with post-operative inflammation. Both the studies showed that turmeric reduced inflammation as powerfully as the drug phenylbutazone.

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As a result of the vacuum created by the withdrawal of COX-2 inhibitor drugs, fierce competition rages on between the medical and supplement industries, which are both vying for customers that suffer from various joint ailments. Due to the withdrawal of Vioxx® and Bextra®, and the “black-box” warnings added to the labels of Celebrex® and the NSAIDS, the market for pain relief remains open. Because of all the problems with pharmaceuticals and the many nutritional products that are ineffective in providing pain relief… the market is wide open, indeed. Baby boomers are reaching the age of arthritis, which means that any supplement that can prove safety, plus pain relief and/or maintenance of joint health, has a strong future in the US and worldwide.