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Chondroitin - Uses, Benefits and Some Properties for Chondroitin

Common Trade Names

Multi-ingredient preparations: Chondroitin-4 Sulfate, Condroitin, 100% CSA, Purified Chondroitin Sulfate, Structum; Osteo- Biflex, Painfree

Common Forms

Available as capsules (200 mg, 400 mg), an oral gel, and, in Europe, an injection.

Source

Chondroitin is extracted from bovine tracheal cartilage.

Chemical Components

Chondroitin sulfates are large molecularly sized compounds of glycosaminoglycans and disaccharide polymers composed of equimolar amounts of D-acetylgalactosamine, D-glucuronic acid, and sulfates in 30 to 100 disaccharide units.

Purified commercial chondroitin preparations contain combinations of chondroitin-4-sulfate and chondroitin-6-sulfate, which are negatively charged because of carboxylic and dissociated sulfates. Structurally, chondroitin sulfates are related to the low-molecular-weight heparanoid danaproid sodium.

Actions

Because of their large molecular size, chondroitin sulfates are thought to be poorly absorbed orally (13% absolute bioavailability). They have been shown to control the formation of new cartilage matrix by stimulating chondrocyte metabolism and synthesis of collagen and proteoglycan.

Chondroitin sulfates are also reported to inhibit the enzymes human leukocyte elastase and hyaluronidase. High concentrations of human leukocyte elastase are found in the blood and synovial fluid of patients with rheumatic disease. Chondroitin sulfates also stimulate the production of highly polymerized hyaluronic acid by synovial cells. Viscosity is subsequently improved and synovial fluid levels return to normal. The ratio of chondroitin sulfate isomers (chondroitin-4-sulfate and chondroitin-6­sulfate) in human synovial fluid may serve as a marker for severity of disease in patients with hip osteoarthritis .

Reported Uses

Chondroitin is claimed to be useful as a dietary supplement in combination with glucosamine sulfate in osteoarthritis and related disorders. Chondroitin sulfates have been used in ischemic heart disease and hyperlipidemia, as a preservative of corneas for transplantation, and as an adjunct to eye surgery.

Chondroitin sulfates were first evaluated using parenteral administration (. Other small trials demonstrated improvement in subjective outcomes, such as use of NSAIDs, visual analogue scales for pain, Lequesne's Index, and patient or physician global assessment after oral administration. More recent information from moderately sized clinical trials seems to support this earlier evidence. Interestingly, chondroitin sulfates may exert beneficial effects in terms of slowing joint space narrowing in osteoarthritis of the knee and hand.

Dosage

• The oral dose is based on the patient's weight; chondroitin is usually given in combination with glucosamine sulfate.

• Patients who weigh less than 120 lb (54 kg): 1,000 mg of glucosamine sulfate plus 800 mg of chondroitin sulfates P.O.

• Patients who weigh between 120 and 200 lb (54 and 91 kg): 1,500 mg of glucosamine sulfate plus 1,200 mg of chondroitin sulfates P.O.

• Patients who weigh more than 200 lb: 2,000 mg of glucosamine sulfate plus 1,600 mg of chondroitin sulfates P.O.

The total daily dosage is usually taken with food in divided doses b.i.d. to q.i.d. Studies evaluating chondroitin sulfates alone used doses from 400 mg P.O. b.i.d. or t.i.d. to 1,200 mg P.O. daily as a single dose. The study by Bourgeois and others suggested that a 1,200­mg/day single dose of chondroitin sulfate was equally as effective as 400 mgt.i.d.

Adverse Reactions

• CNS: euphoria (reported with use of chondroitin sulfates headache, lack of coordination.

• GI: diarrhea, dyspepsia, nausea.

• Hematologic: decreased hematocrit, hemoglobin level, platelet and WBC counts, and segmented neutrophils; internal bleeding.

• Other: pain at injection site.

Interactions

Anticoagulants: May enhance effects. Avoid administration with chondroitin.

Contraindications And Precautions

Avoid using chondroitin in pregnant or breast-feeding patients; effects are unknown. Use cautiously in patients with bleeding disorders because of the risk of anticoagulation.

Special Considerations

• Offer additional support, such as intermittent moist heat application and exercise, to the patient with osteoarthritis.

• Instruct the patient to watch for signs of bleeding, especially if he is taking anticoagulants or has a bleeding disorder.

• Alert The risk of internal bleeding may exist because of chondroitin's structural similarity to heparin. Studies in animals found significantly decreased hematocrit, hemoglobin level, platelet and WBC counts, and segmented neutrophils and reduced aggregation in response to adenosine diphosphate and collagen . Bleeding as a result of chondroitin sulfate use in humans has not been reported.

• Advise women to avoid using chondroitin during pregnancy or when breast-feeding.

Points of interest

Public interest in the combined use of chondroitin sulfates and glucosamine sulfate has risen, especially since the publication of The Arthritis Cure which claims that the sulfate combination is "the medical miracle that can halt, reverse, and may even cure osteoarthritis."

Commentary

Although many of the data from older human trials are flawed in study design, new clinical trial evidence for the therapeutic application of chondroitin sulfate in osteoarthritis of the knee is mounting. Aside from symptom relief, of particular interest is the purported beneficial effect in deterring progression of joint space narrowing in both knee and finger osteoarthritis. If this effect continues to be substantiated, chondroitin sulfate will probably become a valuable entity in antarthritic treatment plans. Many questions remain to be answered definitively. Chondroitin sulfate appears to be well tolerated in the short term, but the current body of evidence does not adequately address longterm safety issues. Additional clinical trials in larger patient populations that address optimal dosing of standardized dosage forms and those that compare chondroitin sulfate with other pharmacologic treatments are needed.