Glucosamine


Glucosamine Sulphate

Glucosamine is a naturally occuring substance, it is a sugar, produced in an animal's body (and in yours!) from glucose, and is used in the maintenance and regeneration of healthy cartilage in joints.

Cortaflex is the most effective glucosamine supplement.

Glucosamine sulphate and the healthy joint

Healthy Joint

The articulating surfaces of the bones (the ends of the bones that come/rub together forming the joint) are covered in articular cartilage and are bathed in Synovial Fluid - "joint oil". In a normal healthy joint the articular cartilage is smooth and the synovial fluid is of sufficient high quality to provide adequate lubrication.

Glucosamine sulphate

Glucosamine sulphate and chondroitin sulphate help the body repair damage and wear and tear to cartilage.

Glucosamine sulphate and chondroitin only work when they get absorbed into the body - the problem Glucosamine sulphate is a very large sized molecule.

There are many scientific articles proving the effectiveness of glucosamine sulphate and chondroitin...

There is now very little serious doubt that glucosamine helps in cases of degenerative joint disease like osteoarthritis

This is based (not just on the huge weight of testimony from thousands of "users") but on independent scientific tests, studies and field trials. If you are unfamiliar with these, have a look at the bottom of this page where we have colllated a selection of independent trials of glucosamine.

So... if glucosamine works... do all glucosamine supplements work?

Yes - in varying degrees. If you have never tried glucosamine you will probably find some benefit in most glucosamine supplements. However, the problem highlighted on the right of this page means that the real benefits of most supplements are lost. To try to overcome this, the trend has been to add higher and higher levels and concentrations of glucosamine into the supplements. Manufacturers constantly promote their product as having more glucosamine per mg (or dose) than any other. Very little glucosamine from a supplement gets into the cells in the joints where it is needed. So... if you just overload the body with huge amounts of glucosamine you will get more to where it is needed...

However, this is now an out of date concept because the science and technology of nutraceutical supplementation has moved on - the number one selling supplement in the world has surprisingly little actual glucosamine - see the bottom of the yellow section on the right of this page. Its effectiveness come through the supplementation of specific amino acids and amino-saccharides. These are the building blocks of glucosamine, which in turn forms the building blocks of cartilage. In other words - with this technology the body is given the chance to create more of its own glucosamine. A far better and more effective option than trying to cram ever higher levels through the digestive system - hardly a "natural" option!

Why extra glucosamine sulphate is needed when things go wrong

Articular cartilage is one of the first tissues to age and has relatively poor powers of regeneration because of the poor blood supply to the area, even in a healthy animal/human. The delicate balance between wear and renewal can be easily upset - a strain, a slip or fall, repeated heavy use, poor nutrition, even bad conformation or (in the horse) hoof imbalance through bad or irregular shoeing can start a cycle of events that will lead to progressive degeneration of the joint.

The natural reaction of joints to a strain, injury or wear and tear is to become inflamed, whether visibly so or not - a greater amount of synovial fluid is produced (which is often of poorer quality) and enzymes can be produced which actually degrade the cartilage and synovial fluid (Stashak - 1995). This causes sustained, if not greater, inflammation... a self perpetuating cycle leading to DJD in any animal (and human) as the body cannot produce enough glucosamine to keep up to the rate of repair and renewal that would be necessary. This is especially true of an older animal with the slowing down of body systems that comes with age.

How is Glucosamine sulphate used?

Glucosamine sulphate and chondroitin sulphate are used to relieve the symptoms and help in the healing of Degenerative Joint Disease (DJD) - osteoarthritis

This form of arthritis used to be thought of as a permanent, gradually worsening condition affecting many animals (and people) as they get older - an inevitable result of the ageing process coupled with wear and tear on joints. In many ways this is true but many animal owners have reported greatly improved mobility in their animals when fed Glucosamine & Chondroitin. Human patients taking glucosamine report relief of pain as well as improvements in mobility.

Glucosamine & Chondroitin how do they help?

Providing additional Glucosamine speeds up the repair and renewal of damaged or worn articulating cartilage whilst additional Chondroitin helps to neutralise the destructive enzymes and improve the quality of the synovial fluid.

Supplementation of a combination of glucosamine and chondroitin - two naturally occurring and essential substances - has been shown to be most effective.

Since DJD, once started, is a permanent condition, the treatment is long term - the animal (or human) must stay on the maintenance dose for the rest of its life - the joint will revert back to its degenerative condition if supplementation stops.

Many veterinary surgeons routinely inject Polysulfated Glycosaminoglycan (chondroitin) directly into a DJD joint or one that has been operated on and therefore will inevitably become degenerative. However, it can also be given by intramuscular injection and, more importantly for the average animal owner, orally - you can add glucosamine and chondroitin to their food! The advantage of the latter being that all joints are treated, not just the one injected (William E Jones).

There have been other studies which have shown that, while injecting locally into an affected joint gives the quickest improvement (almost immediate!), there is no significant difference in the benefits gained over oral administration of glucosamine and chondroitin after about 30 days. Giving a supplement by adding it daily to feed is, perhaps, more reasonable than having an injection every month or so.

There is at least one major dog food manufacturer which now produces a special dog food for older animals which contains Chondroitin and Glucosamine and there are several brands of supplement on the market which are designed to be added to normal food - these are available for human, as well as equine and canine treatment.

Scientific evidence for glucosamine sulphate


Glucosamine sulphate and Arthritis

Evidence there is that glucosamine is an effective treatment for arthritis from the University of Oxford Clinical School Infomation Management Services Unit

Conclusion/summary
"The bottom line is that there is a body of evidence supporting the efficacy of oral and intramuscular glucosamine in arthritis."


A search of PubMed at the National Library of Medicine reveals hundereds of scientific trials... here is a random selection...

Role of glucosamine in the treatment for osteoarthritis.

Reginster JY, Neuprez A, Lecart MP, Sarlet N, Bruyere O.

Department of Public Health Sciences, CHU Sart Tilman, University of Liège, Liège, Belgium.

Abstract

Over the last 20 years, several studies have investigated the ability of glucosamine sulfate to improve the symptoms (pain and function) and to delay the structural progression of osteoarthritis. There is now a large, convergent body of evidence that glucosamine sulfate, given at a daily oral dose of 1,500 mg, is able to significantly reduce the symptoms of osteoarthritis in the lower limbs. This dose of glucosamine sulfate has also been shown, in two independent studies, to prevent the joint space narrowing observed at the femorotibial compartment in patients with mild-to-moderate knee osteoarthritis. This effect also translated into a 50 % reduction in the incidence of osteoarthritis-related surgery of the lower limbs during a 5-year period following the withdrawal of the treatment. Some discrepancies have been described between the results of studies performed with a patent-protected formulation of glucosamine sulfate distributed as a drug and those having used glucosamine preparations purchased from global suppliers, packaged, and sold over-the-counter as nutritional supplements.

Effect of a glucosamine-based combination supplement containing chondroitin sulfate and antioxidant micronutrients in subjects with symptomatic knee osteoarthritis: A pilot study.

Nakasone Y, Watabe K, Watanabe K, Tomonaga A, Nagaoka I, Yamamoto T, Yamaguchi H. Source Kenkoukazoku, Inc., Kagoshima 892-0848;

Abstract

In the present study, we aimed to investigate the potential effect of a glucosamine (1,200 mg/day)-based dietary supplement combined with chondroitin sulfate and three antioxidant micronutrients, namely methylsulfonylmethane, guava leaf extract, and vitamin D (test supplement) on osteoarthritis (OA) of the knee. A 16-week, randomized, double-blinded, placebo-controlled trial was conducted involving 32 subjects with symptomatic knee OA. Clinical outcomes were measured using the Japanese Knee Osteoarthritis Measure (JKOM) for symptoms and a study diary-based visual analog scale (diary VAS) for pain at baseline and at weeks 4, 8, 12 and 16 during the 16-week intervention period. Furthermore, biomarkers for cartilage type II collagen degradation (C2C) and synovitis hyaluronan (HA) were measured. As compared with the baseline, the JKOM pain subscale was significantly improved at all of the four assessment time points in the test group, but was not at any time point in the placebo group. On the other hand, all of the four symptom subscales and the aggregated total symptoms were significantly improved in the two groups at one or more time points. However, all of these clinical improvements were greater in extent in the test group than in the placebo group, and there were significant differences between groups in the magnitude of changes from baseline for one subscale 'general activities' and the aggregated total symptoms at week 8 (P<0.05). The results of efficacy assessments with the diary VAS showed that all of the three pain subscales were significantly improved only in the test group at almost all the time points. Moreover, serum levels of C2C and HA were decreased by 10 and 25%, respectively, at week 16 in the test group, albeit not statistically significant, without any detectable changes in the placebo group. In conclusion, although the results obtained in this study were not conclusive, the tested glucosamine-based combination supplement is likely to have a beneficial effect on pain and other symptoms associated with knee OA.

Glucosamine and chondroitin sulfates in the treatment of osteoarthritis: a survey

de los Reyes GC, Koda RT, Lien EJ.

Department of Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90089, USA.

For more than 30 years, non-steroidal anti-inflammatory drugs (NSAIDs) have been used as standards in the treatment of osteoarthritis (OA). Serious and often life-threatening adverse effects due to these agents are common. Clinical findings have revealed that glucosamine sulfate and chondroitin sulfate are effective and safer alternatives to alleviate symptoms of OA. Experimental evidence indicates that these compounds and their low molecular weight derivatives have a particular tropism for cartilage where they serve as substrates in the biosynthesis of component building blocks. This paper is a literature review of the chemistry, mechanism of action, pharmacokinetics, clinical efficacy and safety of these two nutraceuticals.

Effect of glucosamine on interleukin-1-conditioned articular cartilage

Fenton JI, Chlebek-Brown KA, Caron JP, Orth MW.

Department of Animal Science, Michigan State University, East Lansing 48824, USA.

Glucosamine inhibits recombinant human interleukin-1 stimulated cartilage degradation in equine cartilage explants. Recently, recombinant equine interleukin-1 has been cloned and purified. Therefore, the objective of this study was to characterise the effects of glucosamine on indices of cartilage degradation in recombinant equine IL-1beta-stimulated equine articular cartilage explants. Cartilage discs were harvested from the weight-bearing region of the articular surface of the antebrachiocarpal and middle carpal joints of horses (age 2-8 years) and cultured under standard conditions. Explants were exposed to recombinant equine interleukin-1beta (reIL-1beta) on Days 1-4 in the presence or absence of glucosamine (0.25, 2.5 or 25 mg/ml), with appropriate controls. Nitric oxide, prostaglandin E2, sulphated proteoglycan, stromelysin and gelatinase/collagenase activity released into conditioned media and total tissue proteoglycan content were measured as indicators of cartilage catabolism. Glucosamine inhibited cartilage catabolic responses in a dose dependent manner that was statistically significant at a dose of 0.25 mg/ml for stromelysin activity and 2.5 mg/ml for collagenase/gelatinase activity. At 25 mg/ml glucosamine also prevented IL-1beta-induced increases in nitric oxide production, prostaglandin E2 and proteoglycan release to media. Glucosamine prevents equine articular cartilage degradation experimentally induced by reIL-1beta in vitro. These data provide further support for the use of glucosamine in treatment or prevention of cartilage loss in athletic horses.

Glucosamine sulfate use and delay of progression of knee osteoarthritis: a 3-year, randomized, placebo-controlled, double-blind study

Pavelka K, Gatterova J, Olejarova M, Machacek S, Giacovelli G, Rovati LC.

Department of Medicine and Rheumatology, Charles University, Prague, Czech Republic. pavelka@revma.cz

Over a three year period... 200 patients, 100 were given a supplement containing glucosamine the other 100 were given a placeboand the results monitored. Conclusion: Long-term treatment with glucosamine sulfate retarded the progression of knee osteoarthritis, possibly determining disease modification.

Glucosamine. A nutraceutical in osteoarthritis

Phoon S, Manolios N.

Westmead Hospital, New South Wales.

BACKGROUND: Glucosamine is an amine-sugar that has been marketed as a natural product for the treatment of osteoarthritis. It has been popularized in the complementary section of pharmacies as a safe over-the-counter treatment for osteoarthritic pain.
OBJECTIVE: We review the literature on the efficacy and safety of glucosamine in osteoarthritis.
DISCUSSION: Recent research suggests that it may not only provide symptomatic pain relief, but may have a role in chondroprotection.

Glucosamine therapy compared to ibuprofen for joint pain

Ruane R, Griffiths P.

Primary Care and Community Pharmacy, King's College London.

To determine the effectiveness of oral glucosamine with ibuprofen for the relief of joint pain in osteoarthritis a mini-review (Griffiths, 2002) of double-blind randomized controlled trials comparing the two was undertaken. The population was adult patients diagnosed with osteoarthritis at any site. The outcome was arthritic pain reduction. Searches on Medline, Embase, AMED, the Cochrane Library and the Merck index identified four trials. Of these, two studies were obtainable and were included in the review. Both compared 1.2 g ibuprofen daily with 1.5 g glucosamine sulphate daily, in three divided doses. The combined number of participants in the studies was 218. The results of these studies showed glucosamine to be of similar efficacy to ibuprofen. The conclusion is that glucosamine is effective in relieving joint pain associated with osteoarthritis. Glucosamine's pain-relieving effects may be due to its cartilage-rebuilding properties; these disease-modifying effects are not seen with simple analgesics and are of particular benefit. In practice glucosamine can be used as an alternative to anti-inflammatory drugs and analgesics or as a useful adjunct to standard analgesic therapy.

Glucosamine sulfate in osteoarthritis of the knee

Noack W, Fischer M, Forster KK, Rovati LC, Setnikar I.

Department of Orthopedics-Evangelisches Waldkrankenhaus, Berlin, Germany.

Glucosamine sulfate is a drug used for the treatment of osteoarthritis (OA), based on its pharmacological and metabolic activities on the cartilage and chondrocytes, complemented by mild anti-inflammatory properties and a favorable pharmacokinetic profile. The aim of this study was to define the activity and safety of glucosamine sulfate on the symptoms of patients with OA, using a multicenter, randomized, placebo-controlled, double-blind, parallel-group study design. The study included 252 outpatients with OA of the knee (Lequesne's criteria), radiological stage between I and III, and Lequesne's severity index of at least 4 points and symptoms for at least 6 months. Patients were treated with either placebo or oral glucosamine sulfate 500 mg t.i.d. for 4 weeks, with weekly, with weekly clinic visits. Responders to treatment were defined as patients with a reduction of at least 3 points in the Lequesne's index with a positive overall assessment by the investigator. The Lequesne's index was 10.6 +/- 0.45 S.E.M. points in both groups at the start of the study. This decreased to 7.45 +/- 0.5 points in the treatment group (average 3.2) and 8.4 +/- 0.4 points in the placebo group (average 2.2) (P < 0.05, Student's t-test). The responder rate in the evaluable patients was 55% with glucosamine (N = 120) vs 38% with placebo (N = 121). These proportions were 52% vs 37% in an intention-to-treat analysis (P = 0.014 and 0.016, respectively; Fisher's Exact Test). The medications were well tolerated throughout the study, with no difference between the glucosamine and placebo treated groups. It is concluded that glucosamine sulfate may be a safe and effective symptomatic Slow Acting Drug for OA

Publication Types:
Clinical Trial
Multicenter Study
Randomized Controlled Trial

PMID: 11548224 [PubMed - indexed for MEDLINE]

Glucosamine sulfate

Thorne Research

Glucosamine sulfate's role in halting or reversing joint degeneration appears to be directly due to its ability to act as an essential substrate for, and to stimulate the biosynthesis of, the glycosaminoglycans and the hyaluronic acid backbone needed for the formation of the proteoglycans found in the structural matrix of joints. Successful treatment of osteoarthritis must effectively control pain and should slow down or reverse the progression of the degeneration. Biochemical and pharmacological data combined with animal and human studies demonstrate that glucosamine sulfate is capable of satisfying both of these criteria.

The Problem with Glucosamine Sulphate

As we have seen, glucosamine is produced in the body and is used in cells within the cartlidge of the joints. If glucosamine is to be taken as a supplement it has to get into those cells.

Glucosamine sulphate has a large and complex molecular structure - too large to pass easily through the small pores in the capillary walls. It just doesn't get to where it's needed, it stays in the blood only to be filtered out by the body's waste system! Most glucosamine supplements do work, but only in a limited way. Most of the ingredients pass through the body... and out again.

To try to compensate for this manufacturers add ever increasing concentrations of glucosamine and chondroitin to their supplements. This is just a waste and simply puts extra pressure on the digestive and waste systems of the body which is a shame - especially if you are seeking "natural" and "safe" remedies!

The solution to the glucosamine problem

One manufacturer has produced a Glucosamine and Chondroitin supplement where these ingredients have been broken down into the smaller molecular sized base compounds which, when combined together, form glucosamine and chondroitin. These base compounds are pure amino acids and aminosaccharides and are far more easily absorbed into the cells which triggers them to produce their own glucosamine and chondroitin.

The Brand is Cortaflex and it is made for Humans as well as Dogs and Cats and the original Equine Cortaflex formulation.

Because of all this, we have used Cortaflex ourselves for about 12 years with great success.

You can get it from Cortaflex Online.