Glucosamine sulfate: Nature's arthritis cure

Arthritis refers to inflammation of the joints. The most common form of arthritis is osteoarthritis, which is also known as degenerative joint disease because it is characterized by joint degeneration and loss of cartilage -- the shock-absorbing gel-like material between joints.

The percentage of people with osteoarthritis increases dramatically with age. Surveys indicate that more than 40 million Americans have osteoarthritis, including 80% of persons over the age of 50. Under the age of 45, osteoarthritis is much more common in men. After age 45, it is much more common in women. (1)

NSAIDs harmful
The primary drugs used in the treatment of osteoarthritis are the so-called "nonsteroidal anti-inflammatory drugs or NSAIDs," which include aspirin. Although these drugs are used extensively in the United States, research indicates they may actually accelerate the progression of joint destruction and cause more problems down the road.

NSAIDs are also associated with side effects including gastrointestinal upset, headaches, and dizziness, and are therefore recommended for only short periods of time.

These drugs work by inhibiting enzymes involved in the production of inflammatory compounds. Enzymes are molecules that speed up chemical reactions. They either join molecules or split them by making or breaking the chemical bonds that keep molecules together. NSAIDs not only suppress the enzymes that produce inflammatory compounds, but they also inhibit enzymes that manufacture cartilage components. (2)

So, you see why the use of NSAIDs in the treatment of osteoarthritis is a classic example of a drug suppressing the symptom while promoting the progression of the disease process. A person may feel free of pain while on the NSAID, but his or her arthritis is silently getting worse, as noted in several clinical studies that have shown NSAID use is associated with acceleration of osteoarthritis and increased joint destruction. (3-6)

The natural alternative to NSAIDs in the treatment of osteoarthritis is glucosamine sulfate.

Glucosamine sulfate beneficial
Glucosamine is a simple molecule that can be naturally produced in the body. Its main function on joints is to stimulate the manufacture of key structural components of cartilage -- molecules known as glycosaminoglycans (GAGs).

It appears that as some people age, they lose the ability to manufacture sufficient levels of glucosamine. The result is that cartilage loses its ability to act as a shock absorber. The body's inability to manufacture glucosamine has been suggested to be the major factor leading to osteoarthritis. That's why supplementing your diet with stabilized glucosamine sulfate -- the proven form of glucosamine -- is so vital.

Glucosamine sulfate has been the subject of more than 300 scientific investigations and over 20 double-blind, clinical studies. The benefits of glucosamine sulfate in the treatment of osteoarthritis are impressive.

In one of the more recent studies comparing glucosamine sulfate to a placebo, 252 patients with osteoarthritis of the knee were given either a placebo or 500 mg of glucosamine sulfate three times daily for four weeks. (7)

Glucosamine sulfate was significantly effective in improving pain and movement after only four weeks of use. Previous studies have shown that the longer glucosamine sulfate is used, the more obvious the therapeutic benefit. These results are consistent with other double-blind studies versus a placebo.

In head-to-head double blind studies, glucosamine sulfate was shown to produce better results than NSAIDs in relieving the pain and inflammation of osteoarthritis, despite the fact that glucosamine sulfate exhibits very little direct anti-inflammatory effect and no direct analgesic or pain-relieving effects. (8-12)

While NSAIDs offer purely symptomatic relief and may actually promote the disease process, glucosamine sulfate appears to address the cause of osteoarthritis. By treating the root of the problem through actually building joint cartilage, glucosamine sulfate not only improves the symptoms -- including pain -- but it also helps the body repair damaged joints. The clinical effect is impressive, especially when glucosamine sulfate's safety and lack of side effects are considered.

All of the research has been done with glucosamine sulfate. It is the only form of glucosamine with proven effectiveness. Only glucosamine sulfate is approved as a treatment for osteoarthritis in more than 70 countries of the world and has been used by millions of people safely and effectively.

Consumers should be aware that many companies marketing other forms of glucosamine, such as N-actyl-glucosamine (NAG) and glucosamine hydrochloride (HCI) try to mislead people into believing that these forms are better absorbed, more stable, and better used than glucosamine sulfate. These contentions are without support in the scientific literature. Glucosamine sulfate is clearly the preferred form.

The sulfur in glucosamine sulfate is important. Sulfur is an essential nutrient for joint tissue where it functions in the stabilization of the connective tissue matrix of cartilage, tendons, and ligaments. The sulfur levels in the blood and joint fluid is very low in people with osteoarthritis. As far back as the 1930s, researchers demonstrated that individuals with arthritis are commonly deficient in this essential nutrient. Restoring sulfur levels brought about significant benefit to these patients. (12,13)

Chondroitin sulfate?
There is no additional benefit provided by a combination of glucosamine sulfate and chondroitin sulfate over glucosamine sulfate alone.

Chondroitin sulfate is composed of repeating units of derivatives of glucosamine sulfate with attached sugar molecules. While the absorption rate of glucosamine sulfate is 90% to 98%, the absorption of intact chondroitin sulfate is estimated to be less than 13%. (15-19)

The difference in absorption is largely due to the difference in size. Chondroitin sulfate is at least 50-to-300 times larger than glucosamine sulfate, too large to pass through the normal intact intestinal barrier. If chondroitin sulfate molecules were absorbed intact or partially digested, they are still unlikely to produce any significant benefit as the chondroitin sulfate molecules are too large to be delivered to cartilage cells.

One of the key reasons glucosamine sulfate is so effective is that its small molecule size allows it to penetrate the joint cartilage and be delivered to the chondrocyte (cartilage cell) and stimulate GAG synthesis. It would be nearly impossible for large chondroitin sulfate molecules to produce this effect.

Any clinical benefit from chondroitin sulfate is most likely due to the absorption of sulfur or smaller GAG molecules broken down by the digestive tract. (19)

But, even this is controversial. In one human study, a single gram of chondroitin sulfate failed to increase serum GAG concentration at all -- based on a highly sensitive measure of intact or depolymerized GAG absorption. These results prompted the researchers to conclude that, "chondroprotection by orally administered chondroitin sulfate is a biologically and pharmacologically unfounded theory." (17)

In a further analysis, these experts on chondroitin sulfate also concluded: "Pooled literature on chondroitin sulfate biochemistry offers enough information to assert that neither intact, nor polymerized chondroitin sulfate is absorbed by the mammalian gastrointestinal tract. Therefore, any direct action of orally administered chondroitin sulfate on cartilage and chondrocytes is not possible." (19)

The few clinical studies that have been done on orally administered chondroitin sulfate demonstrate it is much less effective than glucosamine sulfate. (21-24)

Far more impressive results have been achieved with glucosamine sulfate. The fact is, glucosamine sulfate is the only nutrient clinically proven to build cartilage. It's faster acting and provides much greater overall benefit.

Often asked questions
Does glucosamine sulfate interact with any drugs? There have been no reports of any adverse drug interactions with glucosamine sulfate. The only caveat is that individuals taking diuretics may need to take higher dosages (e.g., 20 mg per kilogram [2.2 pounds] body weight daily).
I am allergic to sulfur. Can I take glucosamine sulfate? People who say they are allergic to sulfur can take glucosamine sulfate. What they really mean is that they are allergic to the so-called sulfa drugs or sulfite-containing food additives. It is impossible to be allergic to sulfur, as sulfur is an essential mineral. The sulfate form of sulfur is present in relatively high concentrations in human blood. In short, glucosamine sulfate is extremely well-tolerated and no allergic reactions have been reported.
I am diabetic. Can I take glucosamine sulfate? Because 98% of glucosamine is absorbed intact, it has absolutely no effect on blood sugar levels. Individuals weighing more than 200 pounds may need higher dosages based on body weight (e.g., 20 mg per kilogram body weight daily).

No substitute
The standard dosage for glucosamine sulfate is 500 mg three times per day. It is important that the glucosamine sulfate you choose be stabilized and clinically proven. Most people who take stabilized glucosamine sulfate experience significant improvement within two-to- eight weeks. However, the longer stabilized glucosamine sulfate is used, the more obvious the results. The effects are cumulative and long-lasting. (10,11)

References
1. Bland JH and Cooper SM: "Osteoarthritis: A review of the cell biology involved and evidence for reversibility. Management rationally related to known genesis and pathophysiology." SemArthr Rheum 14:106-33, 1984.

2. Shield MJ: "Anti-inflammatory drugs and their effects on cartilage synthesis and renal function." Eur J Rheumatol Inflam 13:7-16, 1933.

3. Brooks PM, Potter SR, and Buchana WW: "NSAID and osteoarthritis-help or hindrance." J Rheumatol 9:3-5, 1982.

4. Newman NM and Ling RSM: "Acetabular bone destruction related to non-steroidal anti-inflammatory drugs." The Lancet ii: 11-13, 1985.

5. Ronningen H and Langeland N: "Indomethacin treatment in osteoarthritis of the hip joint." Acta Orthop Scand 50:169-174, 1979.

6. Solomon L: "Drug-induced arthropathy and necrosis of the femoral head." J Bone Joint Surg 55B:246-51, 1973.

7. Noack, W., et al: "Glucosamine sulfate in osteoarthritis of the knee." Osteoarthritis Cartilage 2:51-9, 1994.

8. Vaz AL: "Double-blind clinical evaluation of the relative efficacy of ibuprofen and glucosamine sulfate in the management of osteoarthrosis of the knee in outpatients." Curr Med Res Opn 8:145-9, 1982.

9. Muller-Fassbender H, et al.: "Glucosamine sulfate compared to ibuprofen in osteoarthritis of the knee." Osteoarthritis Cartilage 2:61-9, 1994.

10. Rovati LC, et al.: "A large, randomized, placebo-controlled, double-blind study of glucosamine sulfate vs. piroxicam and vs their association, on the kinetics of the symptomatic effect in knee osteoarthritis." Osteoarthritis Cartilage 2(Suppl.1):56, 1994.

11. Tapadinhas MJ, et al.: "Oral glucosamine sulfate in the management of arthrosis: report on a multi-centre open investigation in Portugal." Pharmatherapeutica 3:157-68, 1982.

12. Sullivan MX and Hess WC: "Cystine content of fingernails in arthritis." J Bone Joint Surg 16:185-8, 1935.

13. Senturia BD: "Results of treatment of chronic arthritis and rheumatoid conditions with colloidal sulphur." J Bone Joint Surg 16:119-25, 1934.

14. Vignon E, Richard M, and Annefeld M: "An in vitro study of glucosamine sulfate on human osteoarthritic cartilage metabolism." Manuscript in preparation.

15. Setnikar I, et al: "Pharmacokinetics of glucosamine in man." Arzneim Forsch 43:(10)1109-13, 1993.

16. Setnikar I, et al.: "Pharmacokinetics of glucosamine in the dog and man." Arzneim Forsch 36(4)729-35, 1986.

17. Baici A, et al. "Analysis of glycosaminoglycans in human sera after oral administration of chondroitin sulfate." Rheumatol Int 12:81-8, 1992.

18. Conte A, et al.: "Biochemical and pharmacokinetic aspects of oral treatment with chondroitin sulfate." Arzneim Forsch 45:918-25, 1995.

19. Baici A and Wagenhauser FJ: "Bioavailability of oral chondroitin sulfate." Rheumatology Int 13:41-43, 1993.

20. Pipitone VR: "Chondroprotection with chondroitin sulfate." Drugs Exptl Clin Res 18:3-7, 1991.

21. LiHirondel JL: "Double-blind clinical study with oral administration of chondroitin sulfate versus placebo in tibiofemoral gonarthrosis." Litera Rheumatologica 14:77-82, 1992.

22. Conrozier T and Vignon E: "The effect of chondroitin sulfate treatment in coxarthritis. A double-blind placebo study." Litera Rheumatologica 14:69-75, 1992.

23. Morreale P, et al: "Comparison of the anti-inflammatory efficacy of chondroitin sulfate and dielofenac sodium in patients with knee osteoarthritis." J Rheumatol 23:1385-91, 1996.(Michael T. Murray, N.D. is a respected author and leading authority in the field of natural medicine. He is a practicing naturopathic physician in Bellevue, Washington, and teaches botanical medicine at Bastyr University in Seattle. He has written more than 20 books, including the best-sellers "Encyclopedia of Natural Medicine," "Natural Alternatives to Over-the-Counter and Prescription Drugs," and "The Healing Power of Herbs.")

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