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Glucosamine Sulphate In The Treatment of Osteoarthritis

Osteoarthritis (OA) is the most common type of arthritis and typically damages the weight-bearing joints such as the hips, knees and spine.

Although primarily considered a disease of aging, OA can also result from sports-related injuries. In fact, about 10% of OA sufferers are in their 20’s. Figures from the Australian Bureau of Statistics reveal that more than 1.1 million Australians suffer from OA.

Ideally, treatment of the disease involves relief of the symptoms, and controls the progressive degeneration of the articular joints. Modern drug therapy has concentrated on symptomatic relief of pain using simple analgesics such as aspirin, or non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen. These drugs do not stop joint degeneration, and many are associated with side-effects such as the production of potentially fatal stomach ulcers.

Glucosamine sulphate is a natural substance, termed a "chondroprotective agent", which relieves the symptoms of OA without serious side-effects, and also appears to slow the progression of the disease.

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The Role Of Glucosamine

OA is caused by a degenerative process which affects the cartilage of the articular joints, resulting in symptoms of inflammation, pain and restricted movement. The degeneration appears to be caused by a disruption in the synthesis of important compounds (such as proteoglycans) from amino sugars within the chondrocytes (cartilage-producing cells).

Glucosamine is one of these amino sugars, and it is produced in the body from the sugar glucose and the amino acid glutamine through the action of the enzyme glucosamine synthetase.

Glucosamine stimulates the synthesis of proteoglycans, glycosaminoglycans (more commonly referred to as mucopolysaccharides), and collagen.

It therefore plays a role in the formation of cartilage and the cushioning synovial fluid between the joints, hence its "chondroprotective" classification.

The chondrocytes can either synthesize glucosamine themselves, or obtain it from circulating pre-formed glucosamine. Supplementary glucosamine can be an important source of this vital amino sugar for those with reduced capacity to produce glucosamine, such as the elderly.

Glucosamine Sulphate

Compared with other potential chondroprotective compounds such as chondroitin and animal cartilage, glucosamine is a much smaller molecule that is more readily absorbed and incorporated into cartilage and ligaments.

Glucosamine is available commercially as N-acetyl glucosamine, and the salts, glucosamine hydrochloride and glucosamine sulphate. Glucosamine sulphate is the form used in the majority of clinical studies - probably due to the stabilization of glucosamine with the sulphate ion.

Sulphur occurs throughout the body in amino acids, and occurs as sulfate in connective tissue as a binder and stabilizer. Sulphate is found in sulphated glucosaminoglycans and proteoglycans. Inorganic sulphate compounds have formed an important basis for Blackmores Celloid® Mineral therapy for over 60 years, with sulfate salts being used to help regulate body fluids and to stabilize intercellular connective tissue.

More recently, researchers at the World Health Organization’s Center for Rheumatology have discovered that sulphur inhibits the various enzymes which lead to cartilage destruction in joints.

The stabilization of glucosamine with sulphate appears to enhance the bioavailability of glucosamine and potentiate its therapeutic effect.

Clinical Trials With Glucosamine Sulphate

Glucosamine sulphate is the most clinically studied glucosamine compound. It has been used in more than 20 double-blind, placebo-controlled studies involving over 6,000 people, together with hundreds of scientific investigations into its mode of action.

One of the most important studies compared glucosamine sulphate with the drug ibuprofen in the treatment of osteoarthritis of the knee. In the study, 200 patients were divided into two groups, one group taking 500mg glucosamine sulphate three times daily (1500mg daily dosage), the other ibuprofen 400mg three times daily. The study lasted four weeks and patients were assessed weekly according to a standard rating index of relief of symptoms of pain and improvement in mobility.

While improvement appeared sooner in the drug-treated groups in the first week, there was no difference in scores from the end of the second week onward. At the end of the treatment, there was a success rate of 52% in the ibuprofen group and 48% in the group taking 500mg glucosamine sulphate three times daily.

Significantly 35% of patients taking ibuprofen suffered side-effects, mainly gastrointestinal, compared with only 6% in the glucosamine sulphate group. The researchers concluded that "glucosamine sulphate was therefore as effective as ibuprofen on symptoms of knee OA".

Summary

• Glucosamine sulphate plays an important biological role in the formation of cartilage and synovial fluid.
  
• Glucosamine sulphate appears to be more biologically active than other chondroprotective agents.
  
• Glucosamine sulphate has been studied in many randomized, double-blind clinical studies of osteoarthritis.
  
• In the treatment of OA, glucosamine sulphate appears to be as effective as a leading NSAID treatment, but with far fewer side-effects.
  
• Glucosamine sulphate is non-toxic, and is safe for long-term administration.
  
• Glucosamine sulphate is effective in reducing joint tenderness, swelling and pain associated with OA when administered 500mg three times daily.

References

1. Safe, M Joint Account, The Australian Magazine, March 20-21. (1999) p27.
2. Myers S & Callinan P, Celloid® Prescribers’ Reference. Sydney: Blackmores Ltd; 1992.
3. Adinfinitum Agency: Glucosamine sulfate proven superior to other forms of glucosamine and chondroitin sulfate. Press release 1998.
4. Werbach, M. Nutritional Influences on Illness 2nd Edition, Third Line Press, Ca. U.S.A. 1993, page 468, referring to paper by D’Ambrosio L et al. Glucosamine sulphate: A controlled clinical investigation in Arthrosis. Pharmatherapeutica 2(8): 504-8; 1981.
5. Mueller-FassbenderH. et al: Glucosamine sulfate compared to ibuprofen in osteoarthritis of the knee. Osteoarthritis and Cartilage (1994)2; 61-69.
6. Noack W etal Glucosamine sulfate in osteoarthritis of the knee. Osteoarthritis and Cartilage (1994)2; 51-59.

N.B. The spellings "sulphate" and "sulfate" have been interchangeable in the past. Scientific convention now prefers sulphate.

If you have osteoarthritis, we recommend reading a report on the latest advances in fighting osteoarthritis.

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